|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|
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...
SU11652 is a cell-permeable and sunitinib-like inhibitor of tyrosine kinase receptor (RTK) and angiogenesis with antineoplastic property. It selectively inhibit...
Amuvatinib, also known as MP-470, is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. MP470 inhibits activities of other ...
Masitinib is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity.
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...
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...
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.
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...
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...
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.
Motesanib is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors. It also pote...
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...
Sitravatinib, a new inhibitor of tyrosine kinase, has been studied to have effective in inhibiting tyrosine kinases receptors involved in driving sarcoma cell g...
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 ...