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

Osimertinib dimesylate  (Synonyms: AZD-9291 dimesylate; Mereletinib dimesylate)

Cat. No.: HY-79077 Purity: 99.19%
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Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

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

Osimertinib dimesylate Chemical Structure

Osimertinib dimesylate Chemical Structure

CAS No. : 2070014-82-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 91 In-stock
Solution
10 mM * 1 mL in Water USD 91 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 70 In-stock
50 mg USD 100 In-stock
100 mg USD 120 In-stock
200 mg USD 140 In-stock
500 mg USD 160 In-stock
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Customer Review

Based on 113 publication(s) in Google Scholar

Other Forms of Osimertinib dimesylate:

Osimertinib dimesylate Related Antibodies

Top Publications Citing Use of Products

102 Publications Citing Use of MCE Osimertinib dimesylate

Proliferation Assay
WB

    Osimertinib dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50)

    EGFRL858R/T790M

    1 nM (IC50)

    In Vitro

    Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for Osimertinib (AZD-9291). Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM[1].

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

    Osimertinib dimesylate Related Antibodies
    In Vivo

    The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth[1]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day[2].

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

    691.82

    Formula

    C30H41N7O8S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (144.55 mM; Need ultrasonic)

    DMSO : 2.63 mg/mL (3.80 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 1.4455 mL 7.2273 mL 14.4546 mL
    5 mM 0.2891 mL 1.4455 mL 2.8909 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    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

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

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation
    References
    Cell Assay
    [1]

    PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM ZD1839, 1.5 μM BIBW 2992, 1.5 μM WZ4002 or 160 nM Osimertinib (AZD-9291) are achieved[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Mice[1]
    The EGFRL858R and EGFRL858R+T790M mice (male and female) are used. Osimertinib (AZD-9291) is suspended in 1% Polysorbate 80 and administered via oral gavage once daily at the doses of 7.5 mg/kg and 5 mg/kg, respectively. Mice are imaged weekly at the Vanderbilt University Institute of Imaging Science. For immunoblot analysis, mice are treated for eight hours with drug as described before dissection and flash freezing of the lungs. Lungs are pulverized in liquid nitrogen before lysis.
    Rats[2]
    The male RccHan:WIST rats (10-week-old) are received a single oral dose of Osimertinib (AZD-9291) (200 mg/kg). Blood glucose levels are measured using an Accuchek Active meter.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.4455 mL 7.2273 mL 14.4546 mL 36.1366 mL
    H2O 5 mM 0.2891 mL 1.4455 mL 2.8909 mL 7.2273 mL
    10 mM 0.1445 mL 0.7227 mL 1.4455 mL 3.6137 mL
    15 mM 0.0964 mL 0.4818 mL 0.9636 mL 2.4091 mL
    20 mM 0.0723 mL 0.3614 mL 0.7227 mL 1.8068 mL
    25 mM 0.0578 mL 0.2891 mL 0.5782 mL 1.4455 mL
    30 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2046 mL
    40 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.9034 mL
    50 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 mL
    60 mM 0.0241 mL 0.1205 mL 0.2409 mL 0.6023 mL
    80 mM 0.0181 mL 0.0903 mL 0.1807 mL 0.4517 mL
    100 mM 0.0145 mL 0.0723 mL 0.1445 mL 0.3614 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • 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.

    Keywords:

    Osimertinib dimesylate2070014-82-1AZD-9291 dimesylateMereletinib dimesylateEGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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