PF-3758309,898044-15-0

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产品名称：PF-3758309

产品别名：PF 3758309；PF3758309

英文别名：PF 3758309;PF3758309

靶点：PAK1；PAK6；PAK5；PAK4；PAK3

CAS：898044-15-0

纯度：>98%

外观：Yellowish-white powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

PF-3758309 is a small-molecule p21-activated kinase inhibitor inhibiting oncogenic signaling and tumor growth.

溶解性：DMSO : 91 mg/mL (185.5 mM)
Ethanol : 91 mg/mL (185.5 mM)

体外研究：

PF-3758309 is a potent (Kd = 2.7 nM), ATP-competitive inhibitor of PAK4 with Ki of 18.7 nM. In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50 = 20 nM) and anchorage-independent growth (IC50 = 27 nM) of A549 cells.

体内研究：PF-3758309 blocks the growth of multiple human tumor xenografts, with a plasma EC50 value of 0.4 nM in the most sensitive model. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.

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