CP-673451  343787-29-1

CP-673451
分子式：C24H27N5O2   分子量：417.5
 
產(chǎn)品描述
CP 673451 是選擇性PDGFRα/β抑制劑，IC50為10 nM/1 nM, 比作用于其他血管生成受體選擇性高450倍以上。
靶點(diǎn)
           
IC50
           
體外研究
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).
體內(nèi)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
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO