PF-3758309

PAK3:99 nM, PAK6:17.1 nM(Ki), PAK5:18.1 nM(Ki), PAK4:1.3 nM, PAK2:190 nM, PAK4:18.7 nM(Ki), PAK1:13.7 nM (Ki)

PF-3758309 (PF-03758309) 是一种可口服的、可逆的 ATP 竞争性 PAK4抑制剂。它是一种 PAK4 抑制剂，可抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。

PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

490.62

97.70%

PF-3758309 (Kd = 2.7 nM), an effective inhibitor of PAK4 （Ki=18.7 nM）, has ATP competition. PF-3758309 (IC50 = 1.3 nM) inhibits phosphorylation of the PAK4 substrate GEF-H1 in cells. In the tumor cell, PF-3758309(IC50 = 4.7 nM) grows in a linesanchorage-independent manner. In HCT116 cells, PF-3758309 inhibits endogenous pGEF-H1 accumulation. In A549 cells, PF-3758309 effectively inhibits cellular proliferation in IC50 of 20 nM and anchorage-independent growth in IC50 of 27 nM.

In the HCT116 tumor model, PF-3758309 act as an antiproliferative inducing apoptosis. In the sensitive model, PF-3758309 (EC50=0.4 nM) blocks the growth of multiple human tumor xenografts.

PF-309, PF-03758309, PF 3758309

C25H30N8OS

898044-15-0

1.325 g/cm3 (Predicted)

DMSO: 91 mg/mL (185.48 mM), Sonication is recommended. Ethanol: 91 mg/mL (185.48 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble)

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.