Description
Ponatinib (AP24534) can inhibit abl, PDGFR-beta, VEGFR, FGFR1, Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM.
Storage
2 years at -20centigrade Powder
Targets
Abl, PDGFR-alpha, VEGFR2, FGFR1 Src
Molecular Formula
C29H27F3N6O
Chemical Name
3-(2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide
Solubility
DMSO 30 mg/mL Water
In vitro
As an oral multitargeted tyrosine kinase inhibitor(TKI), ponatinib (AP24534) is a novel multi-targeted kinase inhibitor thatpotently inhibits native and mutant BCR-ABL. In vitro, ponatinib also hasinhibitory activity against a set of kinases implicated in the pathogenesis ofother hematologic malignancies, including FLT3, KIT, fibroblast growth factorreceptor 1 (FGFR1), and platelet derived growth factor receptor alpha (PDGFR-alpha)with IC50 of 13, 13, 2, and 1 nmol/L. The potency and activity profile of ponatinib wasnext compared to sorafenib and sunitinib. Ponatinib can inhibit leukemic cell lines harboringmutations in FLT3, KIT, fibroblast growth factor receptor 1 (FGFR1), andplatelet derived growth factor receptor alpha (PDGFR-alpha) with IC50of 0.3 to 20 nM.
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