PF-3758309

产品说明书

Print
Chemical Structure| 898044-15-0 同义名 : PF-03758309; PF-309
CAS号 : 898044-15-0
货号 : A125108
分子式 : C25H30N8OS
纯度 : 99%+
分子量 : 490.62
MDL号 : MFCD18633226
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
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
生物活性
靶点

  • PAK

    PAK6, Ki:17.1 nM

    PAK3, IC50:190 nM

  • PAK1

    PAK1, Ki:13.7 nM

  • PAK3

    PAK3, IC50:99 nM

  • PAK2

    PAK2, IC50:190 nM
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
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
参考文献

[1]Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(20), 9446-9451, S94

[2]Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.

[3]Ryu BJ, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings. Mol Cell Biochem. 2014 Apr;389(1-2):69-77.