货号:A125108 同义名: PF-03758309;PF-309
PF-3758309 is an inhbitor of PAKs with IC50 of 1.3 nM for PAK4, which inhbits tumor growth in HCT116, A549, M24met and other xenograft tumor models.
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产品名称 | PAK ↓ ↑ | PAK1 ↓ ↑ | PAK2 ↓ ↑ | PAK3 ↓ ↑ | PAK4 ↓ ↑ | PAK5 ↓ ↑ | PAK6 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IPA-3 |
+
PAK1, IC50: 2.5 μM |
+
PAK1, IC50: 2.5 μM |
99%+ | ||||||||||||||||
FRAX486 |
+++
PAK1, IC50: 14 nM PAK4, IC50: 39 nM |
+++
PAK1, IC50: 14 nM |
++
PAK2, IC50: 33 nM |
++
PAK3, IC50: 39 nM |
+
PAK4, IC50: 575 nM |
99%+ | |||||||||||||
FRAX1036 |
++
PAK2, Ki: 72.4 nM PAK4, Ki: 23.3 nM |
++
PAK1, Ki: 23.3 nM |
++
PAK2, Ki: 72.4 nM |
+
PAK4, Ki: 2.4 μM |
99%+ | ||||||||||||||
FRAX597 |
++++
PAK2, IC50: 13 nM PAK3, IC50: 13 nM |
++++
PAK1, IC50: 8 nM |
++++
PAK2, IC50: 13 nM |
+++
PAK3, IC50: 19 nM |
98+% | ||||||||||||||
PF-3758309 |
++++
PAK6, Ki: 17.1 nM PAK3, IC50: 190 nM |
++++
PAK1, Ki: 13.7 nM |
+
PAK2, IC50: 190 nM |
++
PAK3, IC50: 99 nM |
+++
PAK4, Ki: 18.7 nM |
+++
PAK5, Ki: 18.1 nM |
+++
PAK6, Ki: 17.1 nM |
99%+ | |||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | PF-3758309 is a potent, orally bioavailable, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). It exhibits typical cellular functions associated with PAK4 inhibition, including inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3]. |
体内研究 | PF-3758309 (7.5-30 mg/kg; pO.; twice daily for 9-18 days) induces statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models[1]. |
体外研究 | PF-3758309 exhibits comparable enzymatic potency against the kinase domains of other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but displays lower activity against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM)[1]. PF-3758309, in cellular context, suppresses phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and inhibits anchorage-independent growth across various tumor cell lines (IC50=4.7 nM)[1]. PF-3758309 additionally suppresses the accumulation of endogenous pGEF-H1 in HCT116 cells. It demonstrates potent inhibition of cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) in A549 cells[1]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human MDA-MB-436 cells | Cytotoxic assay | 24-48 h | Cytotoxicity against human MDA-MB-436 cells assessed as reduction in cell viability after 24 to 48 hrs by Celltiter-glo luminescence assay, IC50=0.79 nM | 24432870 |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.19mL 2.04mL 1.02mL |
20.38mL 4.08mL 2.04mL |
CAS号 | 898044-15-0 |
分子式 | C25H30N8OS |
分子量 | 490.624 |
别名 | PF-03758309;PF-309 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(214.01 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |