HER2

Choose Selective HER2 Inhibitors

HER2 Signaling Pathway Map

HER2 Signaling Pathways

HER2 Products

  • All (29)
  • HER2 Inhibitors (27)
  • HER2 Antibodies (2)
  • New HER2 Products
Catalog No. Product Name Information Product Use Citations Product Validations
S0290 SU5204 SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
S1011 Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Eur J Med Chem, 2022, 230:114100
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(20)30609-7
S1019 Canertinib (CI-1033) Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Acta Physiol (Oxf), 2021, 10.1111/apha.13661
ACS Chem Biol, 2021, 10.1021/acschembio.0c01000
S1028 Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Nat Cell Biol, 2021, 23(4):377-390
Nat Commun, 2021, 12(1):6667
Cancer Lett, 2021, 527:10-23
S1056 AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
Genome Med, 2020, 18;12(1):17
PLoS Genet, 2016, 12(9):e1006279
Asian J Androl, 2016, 10.4103/1008-682X
S1167 CP-724714 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
Biochem J, 2021, BCJ20210173
Int J Mol Sci, 2020, 22(1)E82
NPJ Breast Cancer, 2020, 6:30
S1194 CUDC-101 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
Cancer Sci, 2020, 112(1):133-143
Anticancer Drugs, 2020, 31(2):158-168
NPJ Breast Cancer, 2020, 6:30
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
Genome Med, 2020, 18;12(1):17
Mol Pharmacol, 2019, 95(5):528-536
Oncotarget, 2019, 10(68):7185-7197
S2111 Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Cell Metab, 2022, 34(1):90-105.e7
Sci Adv, 2022, 8(2):eabh3375
Cancer Cell, 2021, S1535-6108(21)00659-0
S2150 Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
Cell Metab, 2022, 34(1):90-105.e7
Cell Commun Signal, 2022, 20(1):4
Cancer Cell, 2021, S1535-6108(21)00284-1
S2192 Sapitinib (AZD8931) Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
Cell Rep, 2021, 35(11):109233
Cancer Lett, 2021, 519:328-342
Nature, 2020, 584(7822):608-613
S2216 Mubritinib (TAK 165) Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.
Nat Commun, 2021, 12(1):4566
Eur J Cancer, 2021, 159:16-23
Cancers (Basel), 2021, 13(24)6158
S2250 (-)-Epigallocatechin Gallate (-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
Exp Cell Res, 2022, 411(1):113000
Int J Mol Med, 2022, 49(1)11
EMBO Rep, 2021, e53166
S2727 Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.
Cancer Med, 2022, 10.1002/cam4.4504
Int J Mol Sci, 2021, 23(1)81
Lung Cancer, 2021, 162:79-85
S2752 HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.
Commun Biol, 2021, 4(1):762
S2784 TAK-285 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
Oncotarget, 2020, 11(46):4224-4242
Mol Pharmacol, 2019, 95(5):528-536
Sci Signal, 2018, 11(549)
S2816 Tyrphostin AG 879 Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
Br J Pharmacol, 2015, 10.1111/bph.13127
Br J Pharmacol, 2015, 172(13):3370-82
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5241 Lapatinib ditosylate monohydrate Lapatinib ditosylate monohydrate (Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate, Lapatinib tosilate hydrate)is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways, used for treatment of solid tumours such as breast and lung cancer.
Nat Cell Biol, 2021, 23(4):377-390
Nat Commun, 2021, 12(1):6667
Cancer Lett, 2021, 527:10-23
S6805 Tyrphostin AG-528 Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity.
S6897 Epertinib hydrochloride Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.
S7358 Poziotinib (HM781-36B) Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.
Cancer Cell, 2021, S1535-6108(21)00284-1
Mol Cancer Ther, 2021, molcanther.0371.2021
Transl Lung Cancer Res, 2021, 10(8):3659-3670
S7810 Afatinib (BIBW2992) Dimaleate Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
Eur J Med Chem, 2022, 230:114100
Cancer Cell, 2021, S1535-6108(21)00284-1
Nat Cell Biol, 2021, 23(4):377-390
S8362 Tucatinib (Irbinitinib, ONT-380) Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity.
Cell Metab, 2022, 34(1):90-105.e7
Cancer Cell, 2021, S1535-6108(21)00284-1
Cancer Discov, 2020, 10(5):674-687
S8833 TAS0728 TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of HER2 (human epidermal growth factor receptor 2) with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity.
S8852 Pyrotinib (SHR-1258) dimaleate Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.
Transl Lung Cancer Res, 2021, 10(8):3659-3670
Biomed Chromatogr, 2021, e5221
Clin Transl Med, 2020, 10(8):e254
S9786New BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
A2007 Trastuzumab (anti-HER2) Trastuzumab (anti-human HER2) is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD.
Nat Commun, 2021, 12(1):3946
J Control Release, 2021, 340:243-258
BMC Cancer, 2021, 21(1):923
A2008 Pertuzumab (anti-HER2) Pertuzumab (anti-HER2), a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.
PLoS One, 2021, 16(8):e0255585
Cancer Lett, 2020, 472:119-131
S0290 SU5204 SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
S1011 Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Eur J Med Chem, 2022, 230:114100
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(20)30609-7
S1019 Canertinib (CI-1033) Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Acta Physiol (Oxf), 2021, 10.1111/apha.13661
ACS Chem Biol, 2021, 10.1021/acschembio.0c01000
S1028 Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Nat Cell Biol, 2021, 23(4):377-390
Nat Commun, 2021, 12(1):6667
Cancer Lett, 2021, 527:10-23
S1056 AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
Genome Med, 2020, 18;12(1):17
PLoS Genet, 2016, 12(9):e1006279
Asian J Androl, 2016, 10.4103/1008-682X
S1167 CP-724714 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
Biochem J, 2021, BCJ20210173
Int J Mol Sci, 2020, 22(1)E82
NPJ Breast Cancer, 2020, 6:30
S1194 CUDC-101 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
Cancer Sci, 2020, 112(1):133-143
Anticancer Drugs, 2020, 31(2):158-168
NPJ Breast Cancer, 2020, 6:30
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
Genome Med, 2020, 18;12(1):17
Mol Pharmacol, 2019, 95(5):528-536
Oncotarget, 2019, 10(68):7185-7197
S2111 Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Cell Metab, 2022, 34(1):90-105.e7
Sci Adv, 2022, 8(2):eabh3375
Cancer Cell, 2021, S1535-6108(21)00659-0
S2150 Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
Cell Metab, 2022, 34(1):90-105.e7
Cell Commun Signal, 2022, 20(1):4
Cancer Cell, 2021, S1535-6108(21)00284-1
S2192 Sapitinib (AZD8931) Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
Cell Rep, 2021, 35(11):109233
Cancer Lett, 2021, 519:328-342
Nature, 2020, 584(7822):608-613
S2216 Mubritinib (TAK 165) Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.
Nat Commun, 2021, 12(1):4566
Eur J Cancer, 2021, 159:16-23
Cancers (Basel), 2021, 13(24)6158
S2250 (-)-Epigallocatechin Gallate (-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
Exp Cell Res, 2022, 411(1):113000
Int J Mol Med, 2022, 49(1)11
EMBO Rep, 2021, e53166
S2727 Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.
Cancer Med, 2022, 10.1002/cam4.4504
Int J Mol Sci, 2021, 23(1)81
Lung Cancer, 2021, 162:79-85
S2752 HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.
Commun Biol, 2021, 4(1):762
S2784 TAK-285 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
Oncotarget, 2020, 11(46):4224-4242
Mol Pharmacol, 2019, 95(5):528-536
Sci Signal, 2018, 11(549)
S2816 Tyrphostin AG 879 Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
Br J Pharmacol, 2015, 10.1111/bph.13127
Br J Pharmacol, 2015, 172(13):3370-82
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5241 Lapatinib ditosylate monohydrate Lapatinib ditosylate monohydrate (Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate, Lapatinib tosilate hydrate)is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways, used for treatment of solid tumours such as breast and lung cancer.
Nat Cell Biol, 2021, 23(4):377-390
Nat Commun, 2021, 12(1):6667
Cancer Lett, 2021, 527:10-23
S6805 Tyrphostin AG-528 Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity.
S6897 Epertinib hydrochloride Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.
S7358 Poziotinib (HM781-36B) Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.
Cancer Cell, 2021, S1535-6108(21)00284-1
Mol Cancer Ther, 2021, molcanther.0371.2021
Transl Lung Cancer Res, 2021, 10(8):3659-3670
S7810 Afatinib (BIBW2992) Dimaleate Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
Eur J Med Chem, 2022, 230:114100
Cancer Cell, 2021, S1535-6108(21)00284-1
Nat Cell Biol, 2021, 23(4):377-390
S8362 Tucatinib (Irbinitinib, ONT-380) Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity.
Cell Metab, 2022, 34(1):90-105.e7
Cancer Cell, 2021, S1535-6108(21)00284-1
Cancer Discov, 2020, 10(5):674-687
S8833 TAS0728 TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of HER2 (human epidermal growth factor receptor 2) with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity.
S8852 Pyrotinib (SHR-1258) dimaleate Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.
Transl Lung Cancer Res, 2021, 10(8):3659-3670
Biomed Chromatogr, 2021, e5221
Clin Transl Med, 2020, 10(8):e254
S9786New BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
A2007 Trastuzumab (anti-HER2) Trastuzumab (anti-human HER2) is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD.
Nat Commun, 2021, 12(1):3946
J Control Release, 2021, 340:243-258
BMC Cancer, 2021, 21(1):923
A2008 Pertuzumab (anti-HER2) Pertuzumab (anti-HER2), a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.
PLoS One, 2021, 16(8):e0255585
Cancer Lett, 2020, 472:119-131
S9786New BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
Tags: HER2 inhibition | HER2 cancer | HER2 positive cancer | HER2 receptor | HER2 breast cancer treatment | HER2 negative breast cancer | HER2 overexpression | HER2 protein | HER2 amplification | HER2 immunohistochemistry | Neu receptor | Neu protein | HER2-overexpressing breast cancer | HER2 pathway | ErbB2 receptor | HER2 mutation | HER2-positive advanced breast cancer | ErbB2 protein | Neu mutation | HER2 activation | HER2 kinase inhibitor | HER2 phosphorylation | HER2 inhibitor review