|Description||Imatinib (INN), marketed by Novartis as Gleevec (Canada, South Africa and the USA) or Glivec (Australia, Europe and Latin America), and sometimes referred to by its investigational name STI-571, is a tyrosine-kinase inhibitor used in the treatment of multiple cancers, most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML).|
|Synonyms||CGP-57148B, Gleevec, Imatinib|
Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
DCC-2618 inhibits normal and mutant KIT kinase at the nanomol level. The targets are wt c-KIT, c-KIT mutants, PDGFR alpha, PDGFR beta, KDR and cFMS. DCC-2618 in...
Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
Flumatinib is a multi-kinase inhibitor of c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM respectively. It can predominantly inhibit th...
ISCK03, a phenyl-imidazolosulfonamide compound, is a cell-permeable, specific SCF/c-Kitinhibitor (IC50 <<2.5 μM in cell-free kinase assays).
Dovitinib (TKI258) potently inhibited FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R with IC50 values of 1, 2, 5, 10, 8, 27, 36 nM respectively. Dovitinib sel...
Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the...
Sitravatinib, a new inhibitor of tyrosine kinase, has been studied to have effective in inhibiting tyrosine kinases receptors involved in driving sarcoma cell g...
Motesanib is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors. It also pote...
Imatinib (INN), marketed by Novartis as Gleevec (Canada, South Africa and the USA) or Glivec (Australia, Europe and Latin America), and sometimes referred to by...
Masitinib is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity.
BLU-285 is a potent and selective inhibitor of exon 17 mutant KIT (IC50= 0.27 nM for KIT D816V). BLU-285 showed dose-dependent, robust anti-tumor efficacy in a ...
Amuvatinib, also known as MP-470, is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. MP470 inhibits activities of other ...
SU11652 is a cell-permeable and sunitinib-like inhibitor of tyrosine kinase receptor (RTK) and angiogenesis with antineoplastic property. It selectively inhibit...
Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more...