CP-673451 343787-29-1

CP-673451  343787-29-1

CP-673451
分子式：C24H27N5O2   分子量：417.5
 
产品描述
CP 673451 是选择性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。
靶点
           
IC50
           
体外研究
CP 673451 is a pharmacologically selective PDGFR-beta inhibitor and PDGF-BB-stimulated autophosphorylation of PDGFR-beta in cells (IC50 = 1 nmol/L) being more than 450-fold selective for PDGFR-beta versus other angiogenic receptors. Inhibition of PDGFR-beta phosphorylation in tumors correlates with plasma and tumor levels of CP673451. A dose of 33 mg/kg was adequate to provide >50% inhibition of receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at C(max).
体内研究
In a sponge angiogenesis model, CP 673451 inhibited 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. x 5, p.o., corresponding to 5.5 ng/mL at C(max)). In vivo, CP 673451 inhibits tumor PDGFR-beta phosphorylation, and it also selectively inhibits PDGF-BB-stimulated angiogenesis. CP 673451 causes significant tumor growth inhibition in multiple human xenograft models.
溶解性
DMSO 42 mg/mL，水 <1 mg/mL，乙醇 4 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO