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EGFR/HER2 inhibitor

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153111

    EGFR Cancer
    EGFR/HER2-IN-9 (Compound 1) is an EGFR and HER2 inhibitor with IC50s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively .
    EGFR/HER2-IN-9
  • HY-153856

    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

    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-162623

    EGFR Cancer
    EGFR/HER2-IN-15, a dihydropyrimidine, is a potent EGFR/HER2 inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFR wt activity with an IC50 of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects .
    EGFR/HER2-IN-15
  • HY-151161

    EGFR Cancer
    EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
    EGFR/HER2-IN-8
  • HY-172623

    EGFR Caspase Apoptosis Bcl-2 Family Cancer
    EGFR/HER2-IN-17 (Compound 7h) is a dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-17 inhibits cancer cell proliferation. EGFR/HER2-IN-17 interacts with the binding pockets of EGFR and HER2, activating caspase-3 and caspase-8, and decreases the expression of Bcl-2, thereby inducing apoptosis. EGFR/HER2-IN-17 is promising for research of cancers .
    EGFR/HER2-IN-17
  • HY-151156

    EGFR Apoptosis Cancer
    EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
    EGFR/HER2-IN-6
  • HY-157399

    EGFR Cancer
    EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC50s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma .
    EGFR/HER2-IN-10
  • HY-174841

    EGFR Cancer
    EGFR/HER2-IN-19 (Compound L1) is a dual inhibitor against epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-19 is promising for research of cancers driven by EGFR/HER2 .
    EGFR/HER2-IN-19
  • HY-115951

    EGFR Cancer
    EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of EGFR and HER2 with IC50 values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively .
    EGFR/HER2-IN-2
  • HY-115952

    EGFR Cancer
    EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2 .
    EGFR/HER2-IN-3
  • HY-174414

    EGFR Cancer
    EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 and 0.08 μM respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer .
    EGFR/HER2-IN-18
  • HY-153557

    EGFR Potassium Channel Cancer
    HER2-IN-13 (Compound 33) is an HER2 inhibitor with an IC50 of 8 nM. HER2-IN-13 also inhibits wt-EGFR with an IC50 of 0.40 μM .
    HER2-IN-13
  • HY-153557A

    EGFR Cancer
    HER2-IN-14 (Compound 34) is an HER2 inhibitor with an IC50 of 18 nM. HER2-IN-14 also inhibits wt-EGFR with an IC50 of 6.3 μM .
    HER2-IN-14
  • HY-146238

    EGFR Thymidylate Synthase Apoptosis Cancer
    EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .
    EGFR/HER2/TS-IN-1
  • HY-151158

    EGFR Cancer
    EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
    EGFR/HER2-IN-7
  • HY-160682

    EGFR Others
    EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
    EGFR/HER2-IN-12
  • HY-143734

    EGFR Cancer
    HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11) .
    HER2-IN-6
  • HY-161602

    EGFR Cancer
    EGFR/HER2-IN-13 (Compd 38) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research .
    EGFR/HER2-IN-13
  • HY-161603

    EGFR Cancer
    EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research .
    EGFR/HER2-IN-14
  • HY-144053

    EGFR Cancer
    EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .
    EGFR-IN-36
  • HY-149633

    EGFR Dihydrofolate reductase (DHFR) Apoptosis Cancer
    EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
    EGFR/HER2/DHFR-IN-3
  • HY-159519

    Apoptosis EGFR Cancer
    EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
    EGFR/HER2-IN-16
  • HY-136789
    Tuxobertinib
    1 Publications Verification

    BDTX-189

    EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .
    Tuxobertinib
  • HY-13501
    Mubritinib
    5+ Cited Publications

    TAK-165

    EGFR Cancer
    Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
    Mubritinib
  • HY-147798

    EGFR CDK Cancer
    EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity .
    EGFR/HER2/CDK9-IN-3
  • HY-147796

    EGFR CDK Cancer
    EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 90.17, 131.39, and 67.04 nM, respectively. EGFR/HER2/CDK9-IN-1 exhibits remarkable antitumor activity .
    EGFR/HER2/CDK9-IN-1
  • HY-147797

    EGFR CDK Cancer
    EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity .
    EGFR/HER2/CDK9-IN-2
  • HY-147994

    EGFR Cancer
    EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
    EGFR/HER2-IN-5
  • HY-147992

    EGFR Cancer
    EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
    EGFR/HER2-IN-4
  • HY-137786

    EGFR Cancer
    EGFR-IN-16 (compound 3) is a potent EGFR inhibitor with pIC50 of 4.85 and 4.74 for EGFR and HER-2, respectively .
    EGFR-IN-16
  • HY-151154

    EGFR Cancer
    EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
    EGFR/HER2/DHFR-IN-1
  • HY-160613

    EGFR Cancer
    EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM .
    EGFR/HER2-IN-11
  • HY-156639

    EGFR Cancer
    EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor .
    EGFR/ErbB-2 inhibitor-1
  • HY-146239

    EGFR Thymidylate Synthase Cancer
    EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
    EGFR/HER2/TS-IN-2
  • HY-143319

    EGFR Cancer
    SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 WT and EGFR WT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .
    SPH5030
  • HY-17632
    Tarloxotinib bromide
    1 Publications Verification

    TH-4000

    EGFR Cancer
    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
    Tarloxotinib bromide
  • HY-149632

    EGFR Dihydrofolate reductase (DHFR) Cancer
    EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
    EGFR/HER2/DHFR-IN-2
  • HY-163453

    EGFR Cancer
    HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50 NCI-N87 = 1.63 nM, IC50 BT474= 15.17 nM, IC50 BaF3-HER2YVMA = 1.49 nM .
    HER2-IN-19
  • HY-108931

    EGFR Cancer
    AG 1406 (compound M19) is a HER2 inhibitor, with an IC50 of 10.57 μM for HER2 in BT474 cell and >50 μM for EGFR in EGF-3T3 cell .
    AG 1406
  • HY-112293

    EGFR Cancer
    GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .
    GW2974
  • HY-157229

    EGFR Others
    STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .
    STX-721
  • HY-147303

    Trk Receptor EGFR Cancer
    Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity .
    Sacibertinib
  • HY-164489

    EGFR Akt ERK Apoptosis Cancer
    KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative .
    KU004
  • HY-132842
    Sunvozertinib
    1 Publications Verification

    DZD9008

    EGFR Btk Cancer
    Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
    Sunvozertinib
  • HY-104065
    Pyrotinib
    10+ Cited Publications

    SHR-1258

    EGFR Cancer
    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
    Pyrotinib
  • HY-32721
    Neratinib
    15+ Cited Publications

    HKI-272

    EGFR Cancer
    Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively .
    Neratinib
  • HY-32721B
    Neratinib maleate
    15+ Cited Publications

    HKI-272 maleate

    EGFR Cancer
    Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively .
    Neratinib maleate
  • HY-146262

    EGFR Cancer
    LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .
    LDC0496
  • HY-104065B
    Pyrotinib dimaleate
    10+ Cited Publications

    SHR-1258 dimaleate

    EGFR Cancer
    Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
    Pyrotinib dimaleate

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