HER2 Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| 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. |
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| E1791 | Zongertinib | Zongertinib (BI 1810631, BI 764532) is a selective and potent inhibitor of human HER2 and EGFR tyrosine kinase that covalently binds to both wild-type and mutated HER2 receptors, including exon 20 insertion mutations, while sparing EGFR signalling. It exhibits effective and tolerable oral treatment for patients with HER2 aberration-positive solid tumours. |
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| 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. This compound inhibits 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. It shows antitumor activity. |
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| E2851 | Trastuzumab-Emtansine（T-DM1） | Trastuzumab Emtansine (T-DM1, Ado-Trastuzumab emtansine) is an Antibody-Drug Conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the Microtubule-inhibitory agent DM1. Trastuzumab emtansine has a molecular weight of 145kDa. This product is supplied as 10mg/ml PBS solution. This product is discontinued. We recommend the replacement products: D4003 | ||
| S2111 | Lapatinib (GW572016) | Lapatinib 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. |
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| S7810 | Afatinib Dimaleate | Afatinib 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. |
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| S2727 | Dacomitinib | Dacomitinib is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. This compound inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. It is effective against NSCLCs with EGFR or ERBB2 mutations as well as those harboring the EGFR T790M mutation. This chemical inhibits cell growth and induces apoptosis. Phase 2. |
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| S1019 | Canertinib (CI-1033) | Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor targeting EGFR and ErbB2 with IC50 values of 1.5 nM and 9.0 nM, respectively. It shows no activity against PDGFR, FGFR, InsR, PKC, or CDK1/2/4. This compound has reached Phase 3 clinical trials. |
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| S2250 | EGCG ((-)-Epigallocatechin Gallate) | EGCG ((-)-Epigallocatechin Gallate) 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. |
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| S7358 | Poziotinib (NOV120101, HM781-36B) | Poziotinib 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. |
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| 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 this compound inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
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| S1486 | AEE788 (NVP-AEE788) | AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, respectively. It is less potent against VEGFR2/KDR, c-Abl, c-Src, and Flt-1, and does not inhibit Ins-R, IGF-1R, PKCα, or CDK1. This compound has reached Phase 1/2 clinical trials. |
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| 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. |
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| S8852 | Pyrotinib dimaleate | Pyrotinib 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. |
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| S6813 | Mobocertinib (TAK788) | Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. This compound is an antineoplastic agent. |
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| S9786 | Tuxobertinib (BDTX-189) | BDTX-189 (Tuxobertinib) 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, respectively. This compound exhibits anticancer activity. |
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| 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 recognised 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. |
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| 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. |
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| E0200 | Trastuzumab-deruxtecan (DS-8201a, T-DXd) | Trastuzumab-deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab-deruxtecan shows durable antitumor activity. Trastuzumab-deruxtecan has a molecular weight of 153KDa. This product is supplied as 10mg/ml PBS solution.This product is discontinued. We recommend the replacement products: D4001. |
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| E4819 | Afatinib free base | Afatinib free base (Gilotrif, BIBW2992, Boehringer Ingelheim) is a second-generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 14 nM and 1 nM for wild-type EGFR, EGFR-L858R, HER2, ErbB4, respectively. | ||
| 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. This compound 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. This compound exhibits antitumor activity. |
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