HER2

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HER2 Inhibitors (14)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1028 Lapatinib (GW-572016) Ditosylate Lapatinib Ditosylate (GW572016, GW2016) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
  • Nat Commun, 2014, 5:3384
  • Proc Natl Acad Sci U S A, 2012, 109(17):6584-9
  • Oncogene, 2012, 32(37):4331-42
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, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.
  • Cancer Discov, 2013, 3(2):168-81
  • Cancer Research, 2014, 74(1):341-52
  • Oncogene, 2013, 32(37):4427-35
S2150 Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; 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.
  • Cancer Discov, 2012, 2(5):458-71
  • Cancer Discov, 2013, 3(2):168-81
  • Cancer Discov, 2013, 3(2):224-37
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.
  • Cancer Discov, 2012, 2(5):458-71
  • J Cell Sci, 2010, 123(Pt 18):3102-11
  • Carcinogenesis, 2010, 31(11):1948-55
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, respectively.
  • Cancer Cell, 2012, 21(4):488-503
  • ACS Nano, 2012, 6(10):8525-35
  • Proc Natl Acad Sci U S A, 2014, 109(17):6584-9
S1167 CP-724714 CP-724,714 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. Phase 2.
  • Cancer Res, 2014, 74(1):341-52
  • Cell Death Dis, 2014, 5:e1194
S2192 AZD8931 (Sapitinib) AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
  • Oncogene, 2014, 10.1038/onc.2014.161
  • J Immunol, 2014, 192(2):722-31
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.
  • Cancer Cell, 2012, 22(5):656-67
  • J Cell Mol Med, 2013, 17(5):648-56
  • Head Neck, 2014, 10.1002/hed.23822.?
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.
  • J Chem Inf Model, 2014, 54(3):881-93
  • ACS Med Chem Lett, 2013, 4(9):858-62
  • Theriogenology, 2014, 81(4):572-8
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.
  • Prostate, 2013, 73(13):1453-61
S2216 Mubritinib (TAK 165) Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk. Phase 1.
  • Cell Death Dis, 2013, 4:e810
  • Br J Pharmacol, 2012, 166(3):858-76
  • Leuk Res, 2014, 38(3):402-10
S2752 HER2-Inhibitor-1 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. Phase 1.
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.
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