HER2

Erbb2 (HER2) belongs to Erbb family lacks the capacity to interact with a ligand because its extracellular region exists in a fixed, unfolded conformation. Erbb2 (HER2) acts as an amplifier of the Erbb signaling network. The adaptors and effector of Erbb2 includes Shc, Syk, RasGAP, Grb2/7, Abl, Mapk8, PLC and STAT1/3. Erbb3 lacks kinase activity and can form heterodimeric complexes with Erbb2. The ERBB2–ERBB3 dimer can be an important cancer therapeutic target.

Protein Tyrosine Kinase

Hedgehog Wnt/beta-catenin OCT Hippo pathway PORCN Fascin SFRP

All (32)
HER2 Inhibitors (32)
New HER2 Products

Cat.No.	Product Name	Information	Product Use Citations
S2111	Lapatinib	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.	Nat Cancer, 2025, 6(1):67-85 J Exp Clin Cancer Res, 2025, 44(1):19 Cells, 2025, 14(10)703
S1011	Afatinib (BIBW2992)	Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. This compound induces autophagy.	Cell Res, 2025, 10.1038/s41422-025-01110-x Nat Genet, 2025, 10.1038/s41588-025-02158-6 Cell Rep Med, 2025, 6(2):101929
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.	Cell, 2024, 187(3):712-732.e38 Signal Transduct Target Ther, 2024, 9(1):153 J Invest Dermatol, 2024, S0022-202X(23)03210-4
S1028	Lapatinib Ditosylate	Lapatinib Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.	Cell Death Dis, 2025, 16(1):118 bioRxiv, 2025, 2025.05.29.656249 NPJ Breast Cancer, 2024, 10(1):65
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.	Front Immunol, 2024, 15:1335302 Cells, 2024, 13(17)1452 Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
S2150	Neratinib (HKI-272)	Neratinib 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.	J Microbiol, 2025, 63(2):e2409001 Res Sq, 2025, rs.3.rs-5931887 Exp Mol Med, 2024, 56(11):2382-2394
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.	Cell Rep Med, 2025, 6(8):102284 Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01097-y Nat Commun, 2024, 15(1):2742
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. This compound is more potent against NSCLC cell and 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.	Cell Death Dis, 2025, 16(1):457 Biomolecules, 2025, 15(5)698 Cell Death Dis, 2024, 15(12):912
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.	Cells, 2022, 11(3)425 Cells, 2022, 11(3)425 Front Mol Biosci, 2022, 9:952651
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.	Int J Biol Macromol, 2024, 282(Pt 2):136760 Int J Mol Sci, 2023, 24(7)6228 Biochem Biophys Rep, 2023, 34:101436
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.	Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694 Cell Rep, 2025, 44(6):115799 Front Pharmacol, 2024, 15:1403424
S2216	Mubritinib (TAK 165)	Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; this compound shows no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in the same cell line.	Cell, 2025, S0092-8674(25)01233-4 Biochem Biophys Res Commun, 2025, 742:151056 Sci Adv, 2024, 10(12):eadl4018
S7358	Poziotinib (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.	Clin Cancer Res, 2025, 31(14):3002-3018 Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9 iScience, 2024, 27(2):108839
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.	J Am Heart Assoc, 2025, 14(1):e037400 Nat Commun, 2023, 14(1):2095 Nat Commun, 2023, 14(1):2095
S8362	Tucatinib (Irbinitinib)	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.	Cancer Cell, 2025, 43(4):776-796.e14 Res Sq, 2025, rs.3.rs-5931887 Oncogenesis, 2024, 13(1):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, 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.	Cell Rep Med, 2022, 3(1):100492 Genome Med, 2020, 18;12(1):17 Oncotarget, 2019, 10(68):7185-7197
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. This compound is in Phase 1.	Int J Mol Sci, 2022, 23(22)14023 Genome Med, 2020, 18;12(1):17 Oncotarget, 2016, 7(24):36956-36970
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.	Nat Commun, 2023, 14(1):1516 Nat Commun, 2023, 14(1):1516 Br J Pharmacol, 2015, 172(13):3370-82
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.	Transl Oncol, 2024, 49:102073 Transl Lung Cancer Res, 2021, 10(8):3659-3670 Biomed Chromatogr, 2021, e5221
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.	Int J Mol Sci, 2024, 25(7)3992 J Thorac Oncol, 2023, S1556-0864(23)00797-9 Lung Cancer, 2020, 152:135-142
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
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.	Front Pharmacol, 2021, 12:804327
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 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. It shows antitumor activity.	J Thorac Oncol, 2023, S1556-0864(23)00802-X
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, reapectively. This compound exhibits anticancer activity.	Chem Biol Interact, 2024, 395:111033 J Transl Med, 2023, 21(1):89 J Transl Med, 2023, 21(1):89
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. This compound is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.	Gut Microbes, 2025, 17(1):2518338
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.
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 signaling. It exhibits effective and tolerable oral treatment for patients with HER2 aberration-positive solid tumors.
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.	JCI Insight, 2025, 10(16)e187151
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.
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	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.	Nat Cancer, 2025, 6(1):67-85 J Exp Clin Cancer Res, 2025, 44(1):19 Cells, 2025, 14(10)703
S1011	Afatinib (BIBW2992)	Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. This compound induces autophagy.	Cell Res, 2025, 10.1038/s41422-025-01110-x Nat Genet, 2025, 10.1038/s41588-025-02158-6 Cell Rep Med, 2025, 6(2):101929
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.	Cell, 2024, 187(3):712-732.e38 Signal Transduct Target Ther, 2024, 9(1):153 J Invest Dermatol, 2024, S0022-202X(23)03210-4
S1028	Lapatinib Ditosylate	Lapatinib Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.	Cell Death Dis, 2025, 16(1):118 bioRxiv, 2025, 2025.05.29.656249 NPJ Breast Cancer, 2024, 10(1):65
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.	Front Immunol, 2024, 15:1335302 Cells, 2024, 13(17)1452 Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
S2150	Neratinib (HKI-272)	Neratinib 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.	J Microbiol, 2025, 63(2):e2409001 Res Sq, 2025, rs.3.rs-5931887 Exp Mol Med, 2024, 56(11):2382-2394
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.	Cell Rep Med, 2025, 6(8):102284 Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01097-y Nat Commun, 2024, 15(1):2742
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. This compound is more potent against NSCLC cell and 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.	Cell Death Dis, 2025, 16(1):457 Biomolecules, 2025, 15(5)698 Cell Death Dis, 2024, 15(12):912
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.	Cells, 2022, 11(3)425 Cells, 2022, 11(3)425 Front Mol Biosci, 2022, 9:952651
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.	Int J Biol Macromol, 2024, 282(Pt 2):136760 Int J Mol Sci, 2023, 24(7)6228 Biochem Biophys Rep, 2023, 34:101436
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.	Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694 Cell Rep, 2025, 44(6):115799 Front Pharmacol, 2024, 15:1403424
S2216	Mubritinib (TAK 165)	Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; this compound shows no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in the same cell line.	Cell, 2025, S0092-8674(25)01233-4 Biochem Biophys Res Commun, 2025, 742:151056 Sci Adv, 2024, 10(12):eadl4018
S7358	Poziotinib (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.	Clin Cancer Res, 2025, 31(14):3002-3018 Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9 iScience, 2024, 27(2):108839
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.	J Am Heart Assoc, 2025, 14(1):e037400 Nat Commun, 2023, 14(1):2095 Nat Commun, 2023, 14(1):2095
S8362	Tucatinib (Irbinitinib)	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.	Cancer Cell, 2025, 43(4):776-796.e14 Res Sq, 2025, rs.3.rs-5931887 Oncogenesis, 2024, 13(1):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, 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.	Cell Rep Med, 2022, 3(1):100492 Genome Med, 2020, 18;12(1):17 Oncotarget, 2019, 10(68):7185-7197
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. This compound is in Phase 1.	Int J Mol Sci, 2022, 23(22)14023 Genome Med, 2020, 18;12(1):17 Oncotarget, 2016, 7(24):36956-36970
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.	Nat Commun, 2023, 14(1):1516 Nat Commun, 2023, 14(1):1516 Br J Pharmacol, 2015, 172(13):3370-82
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.	Transl Oncol, 2024, 49:102073 Transl Lung Cancer Res, 2021, 10(8):3659-3670 Biomed Chromatogr, 2021, e5221
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.	Int J Mol Sci, 2024, 25(7)3992 J Thorac Oncol, 2023, S1556-0864(23)00797-9 Lung Cancer, 2020, 152:135-142
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
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.	Front Pharmacol, 2021, 12:804327
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 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. It shows antitumor activity.	J Thorac Oncol, 2023, S1556-0864(23)00802-X
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, reapectively. This compound exhibits anticancer activity.	Chem Biol Interact, 2024, 395:111033 J Transl Med, 2023, 21(1):89 J Transl Med, 2023, 21(1):89
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. This compound is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis.	Gut Microbes, 2025, 17(1):2518338
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.
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 signaling. It exhibits effective and tolerable oral treatment for patients with HER2 aberration-positive solid tumors.
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.	JCI Insight, 2025, 10(16)e187151
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.
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

HER2

Protein Tyrosine Kinase

Signaling Pathway Map