Home Protein Tyrosine Kinase HER2

HER2 inhibitors

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.

Other Protein Tyrosine Kinase Related Inhibitors

VEGFR EGFR c-Met PDGFR CSF-1R IGF-1R c-Kit ALK Tie-2 c-RET
Cat.No. Product Name Information Product Use Citations Product Validations
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.
Nat Genet, 2025, 57(6):1452-1462
Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0605
J Microbiol, 2025, 63(2):e2409001
Verified customer review of Neratinib (HKI-272)
S8362 Tucatinib (Irbinitinib, ONT-380, Arry-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.
Cancer Cell, 2025, 43(4):776-796.e14
Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0605
Res Sq, 2025, rs.3.rs-5931887
S1011 Afatinib (BIBW2992) Afatinib 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. 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
Verified customer review of Afatinib (BIBW2992)
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
Verified customer review of Lapatinib Ditosylate
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
Verified customer review of CP-724714
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
Verified customer review of Sapitinib (AZD8931)
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
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
Verified customer review of Mubritinib (TAK 165)
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
Verified customer review of AC480 (BMS-599626)
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
Br J Pharmacol, 2015, 172(13):3370-82
Br J Pharmacol, 2015, 10.1111/bph.13127
Verified customer review of Tyrphostin AG 879

Signaling Pathway Map