288383-20-0

溶解度:Soluble in DMSO

储存条件:-20C 2 years

生物活性

A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound.The L-alanine prodrug 8 (also known as brivanib alaninate/BMS-582664��an orally available) was selected as a development candidate and is presently in phase II clinical trials.The potency of BMS-540215on the VEGFR-2 and FGFR-1 kinases revealed IC50 values of 25 nM and 148 nM, respectively. BMS-540215 inhibits both VEGF- and basic fibroblast growth factor�Cstimulated human umbilical vascular endothelial cell growth in vitro but does not inhibit tumor cell growth in vitro. In multiple preclinical models of human tumor xenografts, both BMS-582664 and BMS-540215 have shown potent antitumor activity when dosed orally on a once-a-day schedule with complete induction of tumor stasis.

参考文献

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