Fruquintinib;HMPL-013,1194506-26-7

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产品名称：Fruquintinib;HMPL-013

产品别名：见爱必信官网

英文别名：Fruquintinib

靶点：VEGFR3 ,VEGFR1 ,VEGFR2

CAS：1194506-26-7

纯度：0.99

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：Fruquintinib (HMPL-013) is a small molecule vascular endothelial growth factor receptors inhibitor.

溶解性：10 mM in DMSO

体外研究：

In in vitro enzymatic and cellular assays, Fruquintinib inhibits VEGFR family kinases and suppressed VEGF/VEGFR cell signaling in human umbilical vein endothelial cell (HUVEC) and human lymphatic endothial cell (HLEC) with IC50 at low nanomolar level. Few kinases are inhibited other than VEGFRs in a panel of 253 kinases test. Fruquintinib is a highly potent inhibitor of VEGF-induced angiogenesis.

体内研究：Fruquintinib demonstrates favorable pharmacokinetic profile in multiple animal species, oral administration of fruquintinib strongly suppressed VEGF-induced VEGFR2 phosphorylation in the lung tissue in mice. The extent and duration of the inhibition of VEGFR2 phosphorylation correlated well with drug exposures. The strong anti-angiogenic effect resulted in robust anti-tumor efficacy in a number of human tumor xenograft models with good dose response.

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