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HER2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

240

Inhibitors & Agonists

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5

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1

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12

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13631D
    DXd
    10+ Cited Publications

    Exatecan derivative for ADC

    Topoisomerase ADC Payload Cancer
    DXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
    DXd
  • HY-138298
    Trastuzumab deruxtecan (solution)
    5 Publications Verification

    T-DXd (solution); DS-8201 (solution); DS-8201a (solution)

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab deruxtecan (T-DXd; DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
    Trastuzumab deruxtecan (solution)
  • HY-138298A
    Trastuzumab deruxtecan
    5 Publications Verification

    T-DXd; DS-8201; DS-8201a

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
    Trastuzumab deruxtecan
  • HY-16069
    Tucatinib
    10+ Cited Publications

    Irbinitinib; ARRY-380; ONT-380

    EGFR Cancer
    Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib
  • HY-32721
    Neratinib
    20+ 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-148810
    Zongertinib
    1 Publications Verification

    BI 1810631

    c-Met/HGFR Cancer
    Zongertinib (BI 1810631) is a potent and selective HER2 and EGFR tyrosine kinase inhibitor with IC50 values of 13 nM and 579 nM, respectively. Zongertinib has antitumor activity and can be used in the study of multiple solid tumors .
    Zongertinib
  • HY-P9912
    Pertuzumab
    Maximum Cited Publications
    9 Publications Verification

    EGFR Cancer
    Pertuzumab, a humanized IgG1 monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
    Pertuzumab
  • HY-104065
    Pyrotinib
    15+ 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-32721B
    Neratinib maleate
    20+ 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-13631DS

    Exatecan-d5 derivative for ADC

    Topoisomerase ADC Payload Cancer
    DXd-d5 is a deuterium labeled DXd. DXd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
    DXd-d5
  • HY-164718

    BAY 2927088

    EGFR Cancer
    Sevabertinib (BAY 2927088) is an orally active and reversible dual EGFR-HER2 inhibitor (IC 50 <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD). Sevabertinib has anticancer activity against lung cancer .
    Sevabertinib
  • 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-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-P9912A

    EGFR Cancer
    Pertuzumab (anti-HER2), a humanized monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
    Pertuzumab (anti-HER2)
  • HY-10213
    SNX-5422
    1 Publications Verification

    PF-04929113

    HSP Cancer
    SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
    SNX-5422
  • HY-N9330

    Xanthine Oxidase Ras EGFR MEK PERK Apoptosis Cancer
    Broussoflavonol F is a potent dual inhibitor of the HER2-RAS-MEK-ERK signaling pathway and mushroom tyrosinase with an IC50 value of 82.3 μM. Broussoflavonol F downregulates the expression of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk proteins. Broussoflavonol F induces cell cycle arrest and apoptosis, and exhibits cytotoxicity in colon cancer cells. Broussoflavonol F inhibits endothelial proliferation, migration and tube formation, suppresses subintestinal vascular development, and reduces the mRNA levels of angiogenesis-associated genes.Broussoflavonol F can be used for colon cancer research .
    Broussoflavonol F
  • HY-164762

    SHR-A1811

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab rezetecan (SHR-A1811) is a HER2-targeting antibody-drug conjugate (ADC). Trastuzumab rezetecan is composed of a humanized anti-HER2 antibody (HY-P9907), a cleavable linker MC-Gly-Gly-Phe-Gly (HY-44246), and a topoisomerase I inhibitor payload Rezetecán (HY-147408). Trastuzumab rezetecan can be used for research in HER2-positive breast cancer .
    Trastuzumab rezetecan
  • HY-16069A
    Tucatinib hemiethanolate
    10+ Cited Publications

    Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate

    EGFR Cancer
    Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib hemiethanolate
  • HY-150024

    EGFR Cancer
    BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM .
    BI-4142
  • HY-17632
    Tarloxotinib bromide
    1 Publications Verification

    TH-4000

    EGFR Cancer
    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
    Tarloxotinib bromide
  • HY-104065B
    Pyrotinib dimaleate
    15+ 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
  • HY-177008

    PROTACs EGFR Apoptosis Akt ERK Cancer
    PROTAC HER2 degrader-1 is a highly selective HER2 PROTAC degrader, with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 induces apoptosis in BT-474 cells. PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573) .
    PROTAC HER2 degrader-1
  • 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-15732

    JNJ-26483327

    EGFR Cancer
    BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
    BGB-102
  • HY-P990238

    EGFR Inflammation/Immunology Cancer
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4) is an anti-human and anti-rat HER2 IgG2a monoclonal antibody. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) reduces tumor cell proliferation by inhibiting the HER2 signaling pathway. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can activate CD8 + T cells. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can be used for research on cancer such as breast cancer .
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4)
  • 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-164763

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    SHR-A1201 is a HER2-targeting antibody-drug conjugate (ADC). SHR-A1201 is composed of a humanized anti-HER2 antibody (HY-P9907), a linker SMCC (HY-42360), and a microtubulin inhibitor payload Mertansine (HY-19792). SHR-A1201 can be used for research in HER2-positive breast cancer .
    SHR-A1201
  • HY-P99969

    CMAB-302; Cipterbin

    EGFR Cancer
    Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab alone or together with tyrosine kinase inhibitors has antitumor activities .
    Inetetamab
  • HY-111553

    EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMXHER4BLK、EGFR、JAK3SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors .
    TAS0728
  • 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-157297

    CDK Cancer
    CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .
    CDK-IN-13
  • 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-178116

    EGFR PARP Cancer
    HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer .
    HER2-IN-23
  • HY-176744

    EGFR Apoptosis Cancer
    HER2-IN-22 is a potent and selective HER2 inhibitor with an IC50 of 215 μM. HER2-IN-22 possesses killing activity against various tumor cells and can induce cell apoptosis. HER2-IN-22 significantly inhibits tumor growth. HER2-IN-22 can be used in the study for tumors such as HER2+ breast cancer .
    HER2-IN-22
  • HY-163418

    EGFR Cancer
    HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
    HER2-IN-17
  • HY-151162

    EGFR Cancer
    HER2-IN-12 is a HER2 inhibitor (IC50: 121 nM). HER2-IN-12 can be used in the research of cancers, such as breast cancer .
    HER2-IN-12
  • HY-174414

    EGFR Cancer
    EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 (EGFR) and 0.08 μM (HER2) 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-143733

    EGFR Cancer
    HER2-IN-5 is a potent and orally active HER-2 inhibitor, example 10, extracted from patent WO2021164697 .
    HER2-IN-5
  • HY-P10793

    EGFR Apoptosis Cancer
    Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
    Cyclic(YCDGFYACYMDV)
  • HY-168285

    Drug-Linker Conjugates for ADC Topoisomerase Cancer
    LE01 is a drug-linker conjugate for ADC. LE01 contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D). LE01 can be used to synthesize HER2-targeting ADC (HER2-LE01) .
    LE01
  • HY-172820

    DP303c

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer .
    Trastuzumab envedotin
  • HY-10213A

    PF-04929113 mesylate

    HSP Cancer
    SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
    SNX-5422 mesylate
  • HY-16069R

    Irbinitinib (Standard); ARRY-380 (Standard); ONT-380 (Standard)

    EGFR Reference Standards Cancer
    Tucatinib (Standard) is the analytical standard of Tucatinib. This product is intended for research and analytical applications. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
    Tucatinib (Standard)
  • HY-164487

    Proteasome Cancer
    JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer .
    JBJ-08-178-01
  • HY-104065A

    (Rac)-SHR-1258

    Drug Isomer Cancer
    (Rac)-Pyrotinib ((Rac)-SHR-1258) is the racemic form of Pyrotinib (HY-104065). Pyrotinib is a potent and selective dual EGFR/HER2 receptor inhibitor.
    (Rac)-Pyrotinib
  • 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-143323

    EGFR Cancer
    HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers .
    HER2-IN-9
  • HY-163417

    EGFR Cancer
    HER2-IN-15 (Compound 1) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-15 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
    HER2-IN-15
  • HY-163420

    EGFR Cancer
    HER2-IN-16 (Compound 14) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-16 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
    HER2-IN-16
  • 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

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