|Description||Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.|
Dacomitinib, aslo known as PF-299 and PF-00299804; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the p...
EGF816, also called as Nazartinib, a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M resistance mutation while sparing wild-type EGFR. ...
PD158780 is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity with IC50 values of 0.008, 49 and 52 nM for EGFR, Er...
Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Neratinib, also known as HKI-272 or PB272, is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 recep...
NT113 is a pan-ERBB inhibitor with high brain penetrance. It can inhibit the growth of glioblastoma xenografts with EGFR amplification. NT113 is active against ...
Sapitinib, also known as AZD-8931, is an erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. AZD8931 binds to and inhibits erbB tyro...
Naquotinib is irreversible, third-generation, epidermal growth factor receptor (EGFR) inhibitor with IC50 value of 70 nM for NCI-H1650 cell growth. It can coval...
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.
MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the...
Irbinitinib,also known as ARRY-380 and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also...
AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become ...
MP-412 (AV-412) is a second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to an...
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. WZ8040 is about 30-fold more potent against EGFR T790M, ...
Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis and is under Phase III trail ...
Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. EKB-569 irreversibly binds covalently to epidermal gr...
RG13022, a non-phenolic tyrphostin analog, is an epidermal growth factor (EGF) receptor tyrosine kinase inhibitor with potential antiproliferative effect.
WZ-3146 is an irreversiblely inhibitor against EGFR T790M with potential anticancer activity.
CP-724714 is An orally bioavailable quinazoline with potential antineoplastic activity. CP-724,714 selectively binds to the intracellular domain of HER2, revers...