Potent ATP-competitive PDGFR and VEGFR inhibitor (Ki= 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppresses the growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also inhibits FGFR1 (Ki= 0.5μM
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of fibroblast growth factor receptor 1;Inhibitor of kinase insert domain receptor;Inhibitor of platelet derived growth factor receptor alpha
Note
50mg、10mg卖完停产，不再备货
Product Description
Toceranib(SU 11654; PHA 291639) is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.
1.Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA. (2002) Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors.. Blood, 100 (2):(585-93). [PMID:12091352]
2.Sun L, Liang C, Shirazian S, Zhou Y, Miller T, Cui J, Fukuda JY, Chu JY, Nematalla A, Wang X et al.. (2003) Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.. J Med Chem, 46 (7):(1116-9). [PMID:12646019]
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F1523067