HER2

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1028 Lapatinib (GW-572016) Ditosylate <1 mg/mL 100 mg/mL <1 mg/mL
S1011 Afatinib (BIBW2992) <1 mg/mL 97 mg/mL 15 mg/mL
S2150 Neratinib (HKI-272) <1 mg/mL 5 mg/mL <1 mg/mL
S1019 Canertinib (CI-1033) <1 mg/mL 2 mg/mL 9 mg/mL
S2111 Lapatinib <1 mg/mL 100 mg/mL <1 mg/mL
S2752 HER2-Inhibitor-1 <1 mg/mL 100 mg/mL 3 mg/mL
S8362 Irbinitinib (ARRY-380, ONT-380) <1 mg/mL 96 mg/mL 15 mg/mL
S1167 CP-724714 <1 mg/mL 94 mg/mL 94 mg/mL
S2192 Sapitinib (AZD8931) <1 mg/mL 40 mg/mL <1 mg/mL
S1194 CUDC-101 <1 mg/mL 20 mg/mL <1 mg/mL
S2216 Mubritinib (TAK 165) <1 mg/mL 13 mg/mL <1 mg/mL
S1056 AC480 (BMS-599626) <1 mg/mL 113 mg/mL 20 mg/mL
S1486 AEE788 (NVP-AEE788) <1 mg/mL 88 mg/mL <1 mg/mL
S2784 TAK-285 <1 mg/mL 110 mg/mL 54 mg/mL
S2816 Tyrphostin AG 879 <1 mg/mL 36 mg/mL 3 mg/mL
S2250 (-)-Epigallocatechin Gallate 23 mg/mL 72 mg/mL 83 mg/mL
S7810 Afatinib (BIBW2992) Dimaleate <1 mg/mL 100 mg/mL <1 mg/mL
S7358 Poziotinib (HM781-36B) <1 mg/mL 98 mg/mL <1 mg/mL
Catalog No. Information Product Use Citations Product Validations
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.

S1011

Afatinib (BIBW2992)

Afatinib (BIBW2992) 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 in cell-free assays, respectively.

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.

S1019

Canertinib (CI-1033)

Canertinib (CI-1033) 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.

S2111

Lapatinib

Lapatinib, 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.

A2007New

Trastuzumab

Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD.

A2008New

Pertuzumab

Pertuzumab, 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.

S2752New

HER2-Inhibitor-1

HER2-Inhibitor-1 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. Phase 1.

S8362New

Irbinitinib (ARRY-380, ONT-380)

ARRY-380 (ONT-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

S7358

Poziotinib (HM781-36B)

Poziotinib (HM781-36B) 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. Phase 2.

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