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CP-673451
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产品介绍
产品介绍
产品信息
抗原名称
PDGFRβ ,PDGFRα
商品描述
CP-673451是一种选择性的PDGFRα/β抑制剂，IC50为10 nM/1 nM，比作用于其他血管生成受体选择性高450倍以上，具有抗血管生成和抗肿瘤活性。
分子量
417.5
纯度
>98%
可溶性
DMSO ：≥25mg/mL(warmed)
In vitro(体外研究)
CP 673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors. In glioblastoma tumors, CP-673451 (33 mg/kg) provides >50% inhibition of PDGFR-β receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at Cmax. In a sponge angiogenesis model, CP-673451 inhibits 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. ×5, p.o., corresponding to 5.5 ng/mL at Cmax). CP-673451 decreases cell proliferation rate through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. In both RD and RUCH2 cultures, CP-673451 impairs rhabdosphere-forming capacity and cell differentiation, causes increased senescence.
In vivo(体内研究)
CP 673451 (once-daily p.o. ?0 days dosing routinely) inhibits tumor growth (ED50 In RUCH2 xenograft-bearing mice, CP 673451 reduces tumor growth and stromal cell infiltration.
背景
分子式
C24H27N5O2
CAS号
343787-29-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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