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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
PF-03758309
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
898044-15-0
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥544.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥494.0 |
| 规格： | 10 mg | 产品价格： | ￥790.0 |
| 规格： | 50 mg | 产品价格： | ￥2350.0 |
| 规格： | 100 mg | 产品价格： | ￥4400.0 |
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PF-3758309
CAS No. : 898044-15-0
MCE 国际站：PF-3758309
产品活性：PF-3758309 (PF-03758309) 是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (Kd= 2.7 nM; Ki=18.7 nM)。PF-3758309 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
In Vitro: PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=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 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.
In Vivo: PF-3758309 (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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