1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Osimertinib

Osimertinib  (Synonyms: AZD-9291; Mereletinib)

Cat. No.: HY-15772 Purity: 99.96%
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Osimertinib (AZD-9291) est un inhibiteur sélectif irréversible et mutant de EGFR avec des IC50s de 12 et 1 nM contre EGFRL858R et EGFRL858R/T790M, respectivement.

Osimertinib (AZD-9291) ist ein irreversibler und mutantenselektiver EGFR-Inhibitor mit IC50S-Werten von 12 und 1 nM gegen EGFRL858R bzw. EGFRL858R/T790M.

Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

For research use only. We do not sell to patients.

Osimertinib Chemical Structure

Osimertinib Chemical Structure

CAS No. : 1421373-65-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
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Solid
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Customer Review

Based on 120 publication(s) in Google Scholar

Other Forms of Osimertinib:

Top Publications Citing Use of Products

109 Publications Citing Use of MCE Osimertinib

Proliferation Assay
WB

    Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are exposed to indicated concentrations of AZD9291 for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

    Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are treated with AZD9291 or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

    Osimertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    Measurement of antiproliferation effects of AZD9291 by EdU incorporation assay.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595.  [Abstract]

    MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly

    Osimertinib purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.  [Abstract]

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.  [Abstract]

    Effect of PCI-32765, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.
    • Biological Activity

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    Description

    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50, Enzyme assays)

    EGFRL858R/T790M

    1 nM (IC50, Enzyme assays)

    Cellular Effect
    Cell Line Type Value Description References
    A-431 IC50
    0.4 μM
    Compound: AZD9291
    Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay
    Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay
    [PMID: 31889606]
    A-431 GI50
    0.596 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    A-431 IC50
    0.61 μM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    A-431 EC50
    0.67 μM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    A-431 IC50
    0.685 μM
    Compound: AZD-9291
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    [PMID: 29534926]
    A-431 EC50
    0.7 μM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    [PMID: 28603991]
    A-431 IC50
    0.77 μM
    Compound: AZD9291
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    A-431 IC50
    0.77 μM
    Compound: AZD9291
    Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay
    Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay
    [PMID: 34534838]
    A-431 IC50
    0.821 μM
    Compound: AZD9291
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35447433]
    A-431 IC50
    0.85 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    A-431 IC50
    0.893 μM
    Compound: AZD9291
    Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay
    Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay
    [PMID: 27131639]
    A-431 IC50
    0.945 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    [PMID: 30471829]
    A-431 EC50
    0.956 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    A-431 IC50
    0.956 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    [PMID: 28987609]
    A-431 IC50
    1.19 μM
    Compound: 4
    Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    A-431 IC50
    1.226 μM
    Compound: AZD9291
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 34218082]
    A-431 IC50
    1.24 μM
    Compound: AZD9291
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    A-431 IC50
    1.26 μM
    Compound: 5; AZD9291
    Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay
    Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay
    [PMID: 29730192]
    A-431 IC50
    1.3 μM
    Compound: 4
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    [PMID: 31869655]
    A-431 IC50
    1.325 μM
    Compound: 4
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 36288657]
    A-431 IC50
    1.44 μM
    Compound: 4; AZD9291
    Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay
    Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay
    [PMID: 31223440]
    A-431 IC50
    1.51 μM
    Compound: 6, AZD9291
    Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay
    Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay
    [PMID: 32631532]
    A-431 IC50
    1.604 μM
    Compound: 3
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay
    [PMID: 28033579]
    A-431 IC50
    1310 nM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 35254067]
    A-431 IC50
    138.7 nM
    Compound: AZD9291
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    [PMID: 33459024]
    A-431 IC50
    2.035 nM
    Compound: 5
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    A-431 GI50
    40.1 nM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    A-431 IC50
    5.32 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33640672]
    A-431 IC50
    742 nM
    Compound: AZD9291
    Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
    [PMID: 32883633]
    A-431 IC50
    795.2 nM
    Compound: AZD9291
    Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
    Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
    [PMID: 33667898]
    A-431 EC50
    830 nM
    Compound: 1
    Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    [PMID: 37197473]
    A-431 IC50
    84 nM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    A-431 CC50
    967 nM
    Compound: Osimertinib
    Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
    Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
    [PMID: 31560541]
    A549 IC50
    0.14 μM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay
    [PMID: 31889606]
    A549 IC50
    0.31 μM
    Compound: 2
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    [PMID: 30108918]
    A549 IC50
    0.335 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    [PMID: 34794818]
    A549 IC50
    0.445 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    A549 IC50
    0.462 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 31683104]
    A549 IC50
    0.53 μM
    Compound: osimertinib
    Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 29853340]
    A549 IC50
    0.53 μM
    Compound: AZD
    Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
    [PMID: 29466773]
    A549 IC50
    0.615 μM
    Compound: 6; AZD9291
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30530173]
    A549 IC50
    0.67 μM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    A549 IC50
    0.672 μM
    Compound: AZD9291
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay
    [PMID: 34534838]
    A549 IC50
    0.72 μM
    Compound: 4
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    A549 IC50
    0.784 μM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35447433]
    A549 IC50
    0.87 μM
    Compound: AZD9291
    Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay
    [PMID: 29486953]
    A549 IC50
    0.9 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    A549 IC50
    1.557 nM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    A549 EC50
    1.83 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    A549 IC50
    1.87 μM
    Compound: 3
    Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
    [PMID: 35696862]
    A549 IC50
    1.97 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 32961382]
    A549 IC50
    150 nM
    Compound: 9; AZD9291
    Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
    Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
    [PMID: 26756222]
    A549 IC50
    3.242 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30471829]
    A549 GI50
    3.5 μM
    Compound: 5; AZD9291
    Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
    Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
    [PMID: 28282122]
    A549 IC50
    486 nM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 29576272]
    A549 IC50
    5 μM
    Compound: Osimertinib
    Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    ASPC1 IC50
    3.985 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay
    [PMID: 30471829]
    BaF3 IC50
    > 1 μM
    Compound: 65, AZD9291
    Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
    Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
    [PMID: 26258521]
    BaF3 IC50
    > 3000 nM
    Compound: 4
    Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
    Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
    [PMID: 34464874]
    BaF3 EC50
    > 5000 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    0.033 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 36064123]
    BaF3 GI50
    0.347 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    BaF3 EC50
    0.545 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    BaF3 IC50
    0.859 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 36064123]
    BaF3 IC50
    1 nM
    Compound: Osimertinib
    Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BaF3 GI50
    1.2 μM
    Compound: 5; AZD9291
    Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28282122]
    BaF3 IC50
    10.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    110 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    1100 nM
    Compound: Osimertinib
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BaF3 IC50
    1200 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    1320.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 EC50
    14 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay
    [PMID: 36518696]
    BaF3 IC50
    1409.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    1475 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    1503.9 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    154.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    16 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 EC50
    16 nM
    Compound: Osimertinib
    Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 EC50
    1748 nM
    Compound: Osimertinib
    Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 EC50
    18 nM
    Compound: Osimertinib
    Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    2 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    2.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    2.885 μM
    Compound: AZD9291; 5
    Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    BaF3 IC50
    2.893 μM
    Compound: AZD9291; 5
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    BaF3 EC50
    20 nM
    Compound: Osimertinib
    Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    21.5 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    [PMID: 33459024]
    BaF3 EC50
    2956 nM
    Compound: 1
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    [PMID: 37197473]
    BaF3 IC50
    3 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 EC50
    3.2 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay
    [PMID: 36518696]
    BaF3 IC50
    3.3 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    3.52 μM
    Compound: 5
    Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    BaF3 IC50
    3.93 μM
    Compound: 4; AZD9291
    Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
    Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
    [PMID: 31223440]
    BaF3 IC50
    300.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    3100 nM
    Compound: Osimertinib
    Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
    Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
    [PMID: 31689114]
    BaF3 EC50
    34 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay
    Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay
    [PMID: 36518696]
    BaF3 IC50
    4 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    [PMID: 33459024]
    BaF3 IC50
    4.27 μM
    Compound: 5
    Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    BaF3 IC50
    4.3 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    4.427 μM
    Compound: AZD9291; 5
    Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    BaF3 IC50
    4.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    4.61 μM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    BaF3 IC50
    5.11 μM
    Compound: 4; AZD9291
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
    [PMID: 31223440]
    BaF3 IC50
    5.15 μM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    BaF3 IC50
    5.47 μM
    Compound: 6, AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay
    [PMID: 32631532]
    BaF3 IC50
    53.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 EC50
    6 nM
    Compound: 1
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    [PMID: 37197473]
    BaF3 EC50
    6 nM
    Compound: Osimertinib
    Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    6.071 nM
    Compound: 5
    Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 35446588]
    BaF3 IC50
    60.6 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 EC50
    66 nM
    Compound: Osimertinib
    Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    780 nM
    Compound: Osimertinib
    Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BaF3 IC50
    8 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    800 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    81 nM
    Compound: Osimertinib
    Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BEAS-2B IC50
    14.9 μM
    Compound: 1; AZD9291
    Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay
    Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay
    [PMID: 28716641]
    BJ IC50
    > 10 μM
    Compound: AZD9291
    Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    Calu-3 IC50
    0.75 μM
    Compound: Osimertinib
    Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    Calu-3 GI50
    264 nM
    Compound: 8
    Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    [PMID: 25271963]
    Calu-6 IC50
    5.86 μM
    Compound: Osimertinib
    Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    CHO GI50
    4.2 μM
    Compound: 5; AZD9291
    Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
    Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28282122]
    CL97 IC50
    0.1 μM
    Compound: Osimertinib
    Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    EA.hy 926 IC50
    1.161 μM
    Compound: Osimertinib
    Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    HaCaT IC50
    73.7 nM
    Compound: 5; AZD9291
    Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
    Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
    [PMID: 27433829]
    HCC827 EC50
    < 0.014 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    HCC827 IC50
    0.00173 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    [PMID: 34794818]
    HCC827 IC50
    0.00248 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    HCC827 IC50
    0.003 μM
    Compound: 4
    Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    HCC827 IC50
    0.011 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay
    Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    HCC827 IC50
    0.027 μM
    Compound: osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay
    [PMID: 29853340]
    HCC827 IC50
    0.027 μM
    Compound: AZD
    Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
    [PMID: 29466773]
    HCC827 IC50
    0.036 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    HCC827 IC50
    0.2 μM
    Compound: AZD9291
    Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay
    [PMID: 31889606]
    HCC827 IC50
    0.97 nM
    Compound: AZD9291
    Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    [PMID: 32883633]
    HCC827 IC50
    1 nM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 35254067]
    HCC827 IC50
    25.4 nM
    Compound: AZD9291
    Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay
    [PMID: 29576272]
    HEK293 IC50
    0.57 μM
    Compound: AZD9291
    Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis
    Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis
    [PMID: 28426996]
    HEK293-A IC50
    2.418 μM
    Compound: AZD9291
    Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    HeLa IC50
    0.975 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 31683104]
    HeLa IC50
    1.83 μM
    Compound: AZD9291
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    HepG2 IC50
    1.605 μM
    Compound: 6; AZD9291
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    [PMID: 30530173]
    HK-2 IC50
    2.399 μM
    Compound: Osimertinib
    Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    HK-2 IC50
    2.719 μM
    Compound: AZD9291
    Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay
    [PMID: 33429247]
    HK-2 IC50
    3.565 μM
    Compound: AZD9291
    Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    HT-29 IC50
    0.65 μM
    Compound: AZD9291
    Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 29486953]
    HUVEC IC50
    7.278 μM
    Compound: AZD9291
    Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
    Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 32619886]
    KG-1 IC50
    0.53 μM
    Compound: Osimertinib
    Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay
    [PMID: 32961382]
    L02 IC50
    > 40 μM
    Compound: Osimertinib
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33640672]
    L02 IC50
    > 50 μM
    Compound: AZD9291
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    L02 IC50
    0.3 μM
    Compound: AZD9291
    Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay
    [PMID: 31889606]
    L02 IC50
    1.602 μM
    Compound: AZD9291
    Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    L02 IC50
    1.975 μM
    Compound: AZD9291
    Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay
    [PMID: 33429247]
    LoVo IC50
    480 nM
    Compound: AZD9291
    Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
    Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
    [PMID: 26968253]
    LoVo IC50
    480 μM
    Compound: 8
    Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
    Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
    [PMID: 25271963]
    MCF7 IC50
    3.67 μM
    Compound: AZD9291
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    MDA-MB-468 IC50
    1.3 μM
    Compound: Osimertinib
    Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay
    [PMID: 32961382]
    NCI-H1299 IC50
    > 10 μM
    Compound: AZD9291; 5
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
    [PMID: 35178175]
    NCI-H1299 IC50
    2.84 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    [PMID: 34794818]
    NCI-H1299 IC50
    3.24 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    NCI-H1975 EC50
    < 0.014 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    NCI-H1975 IC50
    < 1 μM
    Compound: 4
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay
    [PMID: 31869655]
    NCI-H1975 IC50
    0.011 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
    [PMID: 33429247]
    NCI-H1975 IC50
    0.012 μM
    Compound: 4
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    NCI-H1975 IC50
    0.013 μM
    Compound: 2
    Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    [PMID: 30108918]
    NCI-H1975 IC50
    0.014 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    NCI-H1975 IC50
    0.0148 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
    [PMID: 34794818]
    NCI-H1975 IC50
    0.016 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay
    [PMID: 32550993]
    NCI-H1975 IC50
    0.019 nM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    NCI-H1975 EC50
    0.019 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    [PMID: 28603991]
    NCI-H1975 IC50
    0.019 μM
    Compound: osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    [PMID: 29853340]
    NCI-H1975 IC50
    0.019 μM
    Compound: AZD
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    [PMID: 29466773]
    NCI-H1975 IC50
    0.023 μM
    Compound: AZD-9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
    [PMID: 29534926]
    NCI-H1975 IC50
    0.03 μM
    Compound: 4; AZD9291
    Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay
    Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay
    [PMID: 31223440]
    NCI-H1975 IC50
    0.03 μM
    Compound: 3
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay
    [PMID: 28033579]
    NCI-H1975 IC50
    0.0305 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    NCI-H1975 IC50
    0.041 μM
    Compound: 5; AZD9291
    Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay
    Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay
    [PMID: 29730192]
    NCI-H1975 IC50
    0.044 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    NCI-H1975 IC50
    0.05 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    NCI-H1975 IC50
    0.052 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay
    [PMID: 27131639]
    NCI-H1975 IC50
    0.06 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    NCI-H1975 IC50
    0.06 μM
    Compound: AZD9291
    Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    [PMID: 29486953]
    NCI-H1975 IC50
    0.064 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    [PMID: 28987609]
    NCI-H1975 IC50
    0.07 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay
    [PMID: 31718182]
    NCI-H1975 IC50
    0.072 μM
    Compound: 3
    Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
    [PMID: 35696862]
    NCI-H1975 IC50
    0.073 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 31683104]
    NCI-H1975 IC50
    0.073 μM
    Compound: 6; AZD9291
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    [PMID: 30530173]
    NCI-H1975 IC50
    0.076 μM
    Compound: AZD9291
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay
    [PMID: 34534838]
    NCI-H1975 IC50
    0.091 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 34218082]
    NCI-H1975 IC50
    0.095 μM
    Compound: 4
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 36288657]
    NCI-H1975 IC50
    0.096 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay
    [PMID: 30471829]
    NCI-H1975 IC50
    0.1 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    [PMID: 35178185]
    NCI-H1975 IC50
    0.1 μM
    Compound: 4
    Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay
    Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay
    [PMID: 30472599]
    NCI-H1975 IC50
    0.125 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36173763]
    NCI-H1975 IC50
    0.13 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    NCI-H1975 IC50
    0.74 μM
    Compound: 6, AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay
    [PMID: 32631532]
    NCI-H1975 IC50
    0.98 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33640672]
    NCI-H1975 IC50
    10.5 nM
    Compound: 1; AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay
    [PMID: 28716641]
    NCI-H1975 IC50
    15 nM
    Compound: 9; AZD9291
    Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA
    Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA
    [PMID: 26756222]
    NCI-H1975 IC50
    15 μM
    Compound: 8
    Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
    Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
    [PMID: 25271963]
    NCI-H1975 IC50
    17 nM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 35254067]
    NCI-H1975 IC50
    18.21 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
    [PMID: 33667898]
    NCI-H1975 IC50
    2.08 μM
    Compound: Osimertinib
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay
    [PMID: 33640672]
    NCI-H1975 GI50
    2.8 nM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    NCI-H1975 GI50
    24 nM
    Compound: 8
    Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    [PMID: 25271963]
    NCI-H1975 IC50
    3.1 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay
    [PMID: 31718182]
    NCI-H1975 IC50
    3.85 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36173763]
    NCI-H1975 IC50
    4.32 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36173763]
    NCI-H1975 IC50
    42 nM
    Compound: AZD9291
    Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    [PMID: 32883633]
    NCI-H1975 IC50
    47.2 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    [PMID: 29576272]
    NCI-H1975 IC50
    47.3 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    [PMID: 33459024]
    NCI-H1975 IC50
    73.4 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
    [PMID: 32679450]
    NCI-H292 IC50
    0.22 μM
    Compound: 1
    Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay
    Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay
    [PMID: 32550993]
    NCI-H292 IC50
    0.924 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay
    Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay
    [PMID: 33429247]
    NCI-H292 IC50
    1.084 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    NCI-H460 IC50
    415.9 nM
    Compound: 1; AZD9291
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay
    [PMID: 28716641]
    PC-9 IC50
    < 0.01 μM
    Compound: Osimertinib
    Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    PC-9 IC50
    > 1000 nM
    Compound: Osimertinib
    Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    PC-9 IC50
    0.011 nM
    Compound: AZD9291
    Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay
    Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay
    [PMID: 33429247]
    PC-9 IC50
    0.011 μM
    Compound: AZD9291; 5
    Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    PC-9 IC50
    0.016 μM
    Compound: AZD9291
    Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    PC-9 IC50
    0.023 nM
    Compound: Osimertinib
    Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    PC-9 IC50
    0.16 μM
    Compound: Osimertinib
    Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay
    Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    PC-9 IC50
    17 nM
    Compound: AZD9291
    Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
    Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
    [PMID: 26968253]
    PC-9 IC50
    17 μM
    Compound: 8
    Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
    Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
    [PMID: 25271963]
    PC-9 GI50
    23 nM
    Compound: 8
    Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    [PMID: 25271963]
    PC-9 IC50
    3.21 μM
    Compound: AZD9291; 5
    Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    PC-9 IC50
    3.248 μM
    Compound: AZD9291
    Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35447433]
    PC-9 IC50
    5.431 nM
    Compound: 5
    Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    PC-9 IC50
    56 nM
    Compound: 9; AZD9291
    Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
    Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
    [PMID: 26756222]
    PC-9 IC50
    6.5 nM
    Compound: 1; AZD9291
    Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay
    Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay
    [PMID: 28716641]
    Sf9 IC50
    0.002 μM
    Compound: Osimertinib
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k
    [PMID: 31718182]
    Sf9 IC50
    0.09 μM
    Compound: Osimertinib
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki
    [PMID: 31718182]
    Sf9 IC50
    1.23 μM
    Compound: Osimertinib
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
    [PMID: 31718182]
    Sf9 IC50
    20.8 nM
    Compound: 6; AZD-9291
    Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    [PMID: 30471829]
    Sf9 IC50
    567.5 nM
    Compound: 6; AZD-9291
    Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    [PMID: 30471829]
    U-87MG ATCC IC50
    4.5 μM
    Compound: 4
    Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    [PMID: 31869655]
    Vero CC50
    13.23 μM
    Compound: Osimertinib
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    3.26 μM
    Compound: Osimertinib
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    In Vitro

    Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
    ? Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].
    ? Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)[2].
    ? Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively)[1].
    ? Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=6, 7, 74 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Dramatically inhibited cell proliferation (IC50s=41, 26, 41, 31 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=16, 701, 230, 38 nM, respectively)

    Apoptosis Analysis[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
    Concentration: 0.1 μM
    Incubation Time: 48 hours
    Result: Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.
    In Vivo

    Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
    Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
    Administration: p.o.; daily for 14 days
    Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
    Clinical Trial
    Molecular Weight

    499.61

    Formula

    C28H33N7O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (200.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0016 mL 10.0078 mL 20.0156 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% HPMC/1% Tween-80 in Saline water

      Solubility: 5 mg/mL (10.01 mM); Suspened solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0016 mL 10.0078 mL 20.0156 mL 50.0390 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 mL 10.0078 mL
    10 mM 0.2002 mL 1.0008 mL 2.0016 mL 5.0039 mL
    15 mM 0.1334 mL 0.6672 mL 1.3344 mL 3.3359 mL
    20 mM 0.1001 mL 0.5004 mL 1.0008 mL 2.5020 mL
    25 mM 0.0801 mL 0.4003 mL 0.8006 mL 2.0016 mL
    30 mM 0.0667 mL 0.3336 mL 0.6672 mL 1.6680 mL
    40 mM 0.0500 mL 0.2502 mL 0.5004 mL 1.2510 mL
    50 mM 0.0400 mL 0.2002 mL 0.4003 mL 1.0008 mL
    60 mM 0.0334 mL 0.1668 mL 0.3336 mL 0.8340 mL
    80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6255 mL
    100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5004 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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