PF-3758309 dihydrochloride

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PF-3758309 dihydrochloride

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MCE 国际站：PF-3758309 dihydrochloride

产品活性：PF-3758309 (PF-03758309) dihydrochloride是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (K_d= 2.7 nM; K_i=18.7 nM)。PF-3758309 dihydrochloride 具有 PAK4 抑制剂的预期细胞功能：抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶点：PAK  |  Apoptosis

In Vitro: PF-3758309 dihydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, K_i=18.1 nM; PAK6, K_i=17.1 nM) and group A PAK1 (K_i=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC₅₀=190 nM; PAK3, IC₅₀=99 nM).
In cells, PF-3758309 dihydrochloride 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 dihydrochloride 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.

In Vivo: PF-3758309 dihydrochloride (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models.

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