现货供应对照品CP-547632 C13504 上海佰世凯化学科技有限公司

现货供应对照品CP-547632

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产品名称：现货供应对照品CP-547632
产品型号：C13504
产品展商：Chembest
产品文档：无相关文档

简单介绍

Chemical Name: 3-(4-Bromo-2,6-difluorobenzyloxy)-5-[3-[4-(1-pyrrolidinyl)butyl]ureido]isothiazole-4-carboxamide 分子式：C20H24BrF2N5O3S 分子量：532.40 纯度：>99% CAS：252003-65-9

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Chemical Name: 3-(4-Bromo-2,6-difluorobenzyloxy)-5-[3-[4-(1-pyrrolidinyl)butyl]ureido]isothiazole-4-carboxamide
分子式：C20H24BrF2N5O3S
分子量：532.40
纯度：>99%
CAS：252003-65-9
Biological Activity:
CP-547,632 is asa potent inhibitor of the VEGFR-2 and basic fibroblast growthfactor (FGF) kinases (IC₅₀ = 11 and 9 nM, respectively). Itis selective relative to epidermal growth factor receptor, platelet-derivedgrowth factor ß, and other related TKs. It also inhibitsVEGF-stimulated autophosphorylation of VEGFR-2 in a whole cellassay with an IC₅₀ value of 6 nM. After oral administrationof CP-547,632 to mice bearing NIH3T3/H-ras tumors, VEGFR-2 phosphorylationin tumors was inhibited in a dose-dependent fashion (EC₅₀ =590 ng/ml). These plasma concentrations correlated well withthe observed concentrations of the compound necessary to inhibitVEGF-induced corneal angiogenesis in BALB/c mice. A sponge angiogenesisassay was used to directly compare the inhibitory activitiesof CP-547,632 against FGF receptor 2 or VEGFR-2; this compoundpotently inhibits both basic FGF and VEGF-induced angiogenesisin vivo. The antitumor efficacy of this agent was evaluatedafter once daily p.o. administration to athymic mice bearinghuman xenografts and resulted in as much as 85% tumor growthinhibition. CP-547,632 is a well-tolerated, orally-bioavailableinhibitor presently under clinical investigation for the treatmentof human malignancies.

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现货供应对照品CP-547632