| 产品描述： | VEGFR2 选择性抑制剂;VEGFR2 Selective Inhibitors;产品介绍：SKLB-610是一种多靶点的酪氨酸激酶 (tyrosine kinases)抑制剂。它对VEGFR2的抑制作用最为有效，是FGFR2和PDGFR的弱抑制剂。;InformationSKLB-610 is a multi-target inhibitor of thetyrosine kinases. It is most potent againstVEGFR2and exhibits slightly weaker inhibitor ofFGFR2 and PDGFR.TargetsVEGFR2 ; FGFR2 ; PDGFR ; PDGFR ; FGFR2In vitroSKLB610 shows selective inhibition of VEGF-stimulated human umbilical vein endothelial cells (HUVECs) proliferation, and this proliferation inhibitory effect is associated with decreased phosphorylation of VEGFR2 and p42/44 mitogen-activated protein kinase (p42/44 MAPK). SKLB610 inhibits a panel of human cancer cells proliferation in a concentration-dependent manner and human nonsmall cell lung cancer cell line A549 and human colorectal cancer cell line HCT116 are most sensitive to SKLB610 treatment. At concentration of 10μM, SKLB610 inhibits 65% FGFR2 activity and 55% PDGFRE activity, respectively. Relative to PDGFR2 and FGFR2 SKLB610 has more selective inhibition of VEGFR2 which shows 97% inhibition of VEGFR2 activity at 10μM in vitro. No inhibition of enzyme activity is detected when 10μM of SKLB610 is examined against PI3K, EGFR, Aurora-A, CDK2/cyclinE and CDK6/cyclinD3.In vivochronic intraperitoneally administration of SKLB610 at dose of 50mg/kg/d results in significant inhibition in the growth of established human A549 and HCT116 tumor xenografts in nude mice without exhibit toxicity. |
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