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Results for "

EGFR-IN-1

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

3

Inhibitory Antibodies

7

Isotope-Labeled Compounds

2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19617B
    EGFR-IN-1 TFA

    		EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity [1].
    EGFR-IN-1 TFA
  • HY-78869
    Mutated EGFR-IN-1
    1 Publications Verification

    OsimertINib analog

    		 EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
    Mutated EGFR-IN-1
  • HY-163726
    GLUT1/EGFR-IN-1

    		GLUT EGFR Apoptosis Cancer
    GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research [1].
    GLUT1/EGFR-IN-1
  • HY-158310
    SOS1/EGFR-IN-1

    		EGFR Ras Cancer
    SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) [1].
    SOS1/EGFR-IN-1
  • HY-19617
    EGFR-IN-1

    		EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity [1].
    EGFR-IN-1
  • HY-19617A
    EGFR-IN-1 hydrochloride

    		EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity [1].
    EGFR-IN-1 hydrochloride
  • HY-169428
    EGFR-IN-138

    		EGFR Cancer
    EGFR-IN-138 (compound 19) is a potent EGFR inhibitor，with IC50s of 37，2.6 and 1.9 nM for Wild-type，L858R and T790M EGFR，respectively .
    EGFR-IN-138
  • HY-168492
    TrxR/EGFR-IN-1

    		Ferroptosis EGFR TrxR Apoptosis Cancer
    TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor. TrxR/EGFR-IN-1 is active against both Gefitinib (HY-50895)-sensitive and resistant lung cancers, effectively inhibiting tumor proliferation and promoting apoptosis. TrxR/EGFR-IN-1 promotes the degradation of GPX4 protein through autophagolysosomal and proteasomal pathways, leading to ferroptosis. In addition, TrxR/EGFR-IN-1 can induce endoplasmic reticulum stress and trigger immunogenic cell death. TrxR/EGFR-IN-1 can be used for the research of Gefitinib (HY-50895)-resistant lung cancer [1].
    TrxR/EGFR-IN-1
  • HY-155227
    ALK/EGFR-IN-1

    		Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research [1].
    ALK/EGFR-IN-1
  • HY-163434
    PRMT5/EGFR-IN-1

    		EGFR Histone Methyltransferase Cancer
    PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors [1].
    PRMT5/EGFR-IN-1
  • HY-157402
    Topoisomerase II/EGFR-IN-1

    		Topoisomerase EGFR Cancer
    Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer [1].
    Topoisomerase II/EGFR-IN-1
  • HY-155227S
    ALK/EGFR-IN-1-d5

    		Isotope-Labeled Compounds EGFR Anaplastic lymphoma kinase (ALK) BRK Apoptosis Mitochondrial Metabolism Cancer
    ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment [1]
    ALK/EGFR-IN-1-d5
  • HY-168433
    LSD1/EGFR-IN-1

    		Histone Demethylase EGFR Cancer
    LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFR T790M/L858R and EGFR L858R/T790M/C797S, with IC50s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research [1].
    LSD1/EGFR-IN-1
  • HY-170543
    Dual Galectin-3/EGFR-IN-1

    		Galectin EGFR Apoptosis Inflammation/Immunology
    Dual Galectin-3/EGFR-IN-1 (Compound 29) is the dual inhibitor for Galectin-3 and EGFR with the KD of 52.29 μM and 3.31 μM. Dual Galectin-3/EGFR-IN-1 inhibits TGF-β-induced hepatic stellate cell (HSCs) activation, induces apoptosis in LX-2 cell, and exhibits anti-liver fibrotic efficacy [1].
    Dual Galectin-3/EGFR-IN-1
  • HY-P990408
    Anti-ERBB1/EGFR/HER1 Antibody

    		EGFR Inflammation/Immunology
    The Anti-ERBB1/EGFR/HER1 Antibody is a CHO-expressed human antibody that targets ERBB1/EGFR/HER1. The Anti-ERBB1/EGFR/HER1 Antibody consists of a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-ERBB1/EGFR/HER1 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-ERBB1/EGFR/HER1 Antibody
  • HY-100962
    (E)-AG 99
    1 Publications Verification

    (E)-TyrphostIN 46; (E)-TyrphostIN AG 99

    		 EGFR Cancer
    (E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor .
    (E)-AG 99
  • HY-153744
    JGK-068S

    		EGFR Cancer
    JGK-068S (compound I) is a potent EGFR inhibitor .
    JGK-068S
  • HY-141486
    (Rac)-PROTAC PARP/EGFR ligand 1

    		Target Protein Ligand-Linker Conjugates Cancer
    (Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP [1].
    (Rac)-PROTAC PARP/EGFR ligand 1
  • HY-P99892
    Serclutamab

    PR-1594407; DC-1630423

    		 EGFR Others
    Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ. Mainly expressed by CHO (Chinese Hamster Ovary) cells [1].
    Serclutamab
  • HY-18957A
    rel-Lifirafenib

    rel-BGB-283

    		 Raf EGFR Cancer
    rel-Lifirafenib (rel-BGB-283) is the relative configuration of Lifirafenib (HY-18957). Lifirafenib is a potent Raf Kinase and EGFR inhibitor .
    rel-Lifirafenib
  • HY-141486A
    PROTAC PARP/EGFR ligand 1

    		PARP EGFR Ligands for Target Protein for PROTAC Others
    PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology [1].
    PROTAC PARP/EGFR ligand 1
  • HY-138627A
    AST5902 trimesylate

    		EGFR Drug Metabolite Cancer
    AST5902 trimesylate is the principal metabolite of Alflutinib (AST2818) both in vitro and in vivo. AST5902 trimesylate exerts antineoplastic activity. Alflutinib is an EGFR inhibitor .
    AST5902 trimesylate
  • HY-18957B
    Lifirafenib maleate

    BGB-283 maleate

    		 EGFR Raf Others Cancer
    Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively .
    Lifirafenib maleate
  • HY-50896S1
    Erlotinib-13C6

    CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6

    		 Isotope-Labeled Compounds EGFR Autophagy Cancer
    Erlotinib- 13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].
    Erlotinib-13C6
  • HY-135805A
    (Rac)-JBJ-04-125-02

    		EGFR Cancer
    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor .
    (Rac)-JBJ-04-125-02
  • HY-135805B
    (Rac)-JBJ-04-125-02 acetate

    		EGFR Cancer
    (Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, selective mutagenesis, allosteric and orally active EGFR inhibitor .
    (Rac)-JBJ-04-125-02 acetate
  • HY-21292
    SU5214

    SU4949

    		 VEGFR Cancer
    SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has IC50s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively .
    SU5214
  • HY-10531
    ARRY-380 analog

    		EGFR Cancer
    ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249 [1]. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2 .
    ARRY-380 analog
  • HY-D1464
    CH1055
    1 Publications Verification

    		 Fluorescent Dye Cancer
    CH1055 is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody .
    CH1055
  • HY-D1464A
    CH1055 triethylamine
    1 Publications Verification

    		 Fluorescent Dye Cancer
    CH1055 triethylamine is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 triethylamine is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 triethylamine also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody .
    CH1055 triethylamine
  • HY-125841
    EGFR mutant-IN-1

    		EGFR Cancer
    EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR L858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFR WT (IC50 >1.0 μM) [1].
    EGFR mutant-IN-1
  • HY-P99715
    Losatuxizumab

    		EGFR Cancer
    Losatuxizumab is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC50s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFR C271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers [1] .
    Losatuxizumab
  • HY-10260B
    Vandetanib hydrochloride

    ZD6474 hydrochloride

    		 VEGFR Autophagy Apoptosis Cancer
    Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) [1].
    Vandetanib hydrochloride
  • HY-10260
    Vandetanib
    Maximum Cited Publications
    23 Publications Verification

    ZD6474

    		 VEGFR Autophagy Apoptosis Cancer
    Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) [1].
    Vandetanib
  • HY-10260A
    Vandetanib trifluoroacetate

    ZD6474 trifluoroacetate

    		 VEGFR Autophagy Apoptosis Cancer
    Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) [1].
    Vandetanib trifluoroacetate
  • HY-156112
    LM2I

    		Ser/Thr Protease Cancer
    LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
    LM2I
  • HY-162575
    Anticancer agent 231

    		ERK Cancer
    Anticancer agent 231 (Compound P5) is a tyrosine protein kinase inhibitor with a IC50 value of 3.95 μM. Anticancer agent 231 inhibits the cell viability, cell proliferation, cell migration and cancer dryness of triple negative breast cancer (TNBC) cells by targeting EGFR-ERK 1/2 signaling pathway, and is expected to play an important role in the field of TNBC disease therapy [1].
    Anticancer agent 231
  • HY-50896S
    Erlotinib-d6

    CP-358774-d6; NSC 718781-d6; OSI-774-d6

    		 EGFR Cancer
    Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-d6
  • HY-153856
    TAS2940

    		EGFR Cancer
    TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .
    TAS2940
  • HY-153856A
    TAS2940 fumarate

    		EGFR Cancer
    TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .
    TAS2940 fumarate
  • HY-168968S
    ZJY-54

    		EGFR Histone Demethylase Cancer
    ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity [1].
    ZJY-54
  • HY-10260S
    Vandetanib-d6

    ZD6474-d6

    		 Isotope-Labeled Compounds VEGFR Autophagy Apoptosis Cancer
    Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
    Vandetanib-d6
  • HY-10260R
    Vandetanib (Standard)

    		VEGFR Autophagy Apoptosis Cancer
    Vandetanib (Standard) is the analytical standard of Vandetanib. This product is intended for research and analytical applications. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) [1].
    Vandetanib (Standard)
  • HY-10260S2
    Vandetanib-13C6

    ZD6474-13C6

    		 Isotope-Labeled Compounds VEGFR Autophagy Apoptosis Cancer
    Vandetanib-13C6 is a deuterated labeled Vandetanib [1]. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
    Vandetanib-13C6
  • HY-10260S1
    Vandetanib-d4

    		Isotope-Labeled Compounds VEGFR Autophagy Apoptosis Cancer
    Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].
    Vandetanib-d4
  • HY-116624
    MAZ51
    4 Publications Verification

    		 VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity [1] .
    MAZ51
  • HY-149695
    EGFR-IN-91

    		EGFR Cancer
    EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
    EGFR-IN-91
  • HY-15196
    TAK-285
    2 Publications Verification

    		 EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity [1]. TAK-285 can cross the blood-brain barrier (BBB) .
    TAK-285
  • HY-156470
    Multi-kinase-IN-6

    		Trk Receptor Anaplastic lymphoma kinase (ALK) c-Kit EGFR Pim Casein Kinase Checkpoint Kinase (Chk) CDK Apoptosis Cancer
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect [1].
    Multi-kinase-IN-6

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