AC480 HCl (also known as BMS-599626 HCl) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1 and HER2 (human epidermal growth factor receptors) with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.
AG-494 (formerly also known as Tyrphostin AG-494) is a novel and potent inhibitor of epidermal growth factor receptor (EGFR) kinase with an IC50 value of 1 µM in HT-22 cells.
EGFR-IN-5 is a novel and potent EGFR-TKI with potential anticancer effects.
ARRY-380 analog, an analog of ARRY-380 (Irbinitinib, formerly known as ARRY-380 and ONT-380 or Tucatinib) which is a potent and selective small molecule inhibitor of HER2 with IC50 value of 8 nM, it is equally potent against truncated p95-HER2, and is 500-fold more selective for HER2 versus EGFR.
PD153035 is reported to be a novel, potent, specific, and ATP competitive inhibitor of EGFR (Epidermal growth factor receptor) tyrosine kinase with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays, and to a lesser degree, of the closely related HER2/neu receptor; PD153035 inhibits EGF-dependent EGFR phosphorylation in a variety of human […]
Olmutinib (also known as HM61713 and BI-1482694; Olita) is a novel, potent, orally bioavailable, third-generation and irreversible EFGR/epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI).
FIIN-3 is a novel, potent, selective, irreversible and the next-generation covalent FGFR inhibitor with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Rociletinib hydrobromide (CO-1686; AVL-301; CNX-419), the hydrobromide salt of Rociletinib, is an oral, irreversible/covalent, and mutant-selective EGFR inhibitor (EGFR-TKI) with antitumor activity.
Erlotinib mesylate (also known as OSI-744 mesylate, trade name: Tarceva) is the mesylate salt of erlotinib which is an EGFR (epidermal growth factor receptor) inhibitor with IC50 of 2 nM in cell-free assays, and is >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
4557W is a potent and reversible inhibitor of EGFR(Epidermal growth factor receptor) and c-ErbB2 (IC50s = 20 and 79 nM, respectively).