1783816-74-9|NVS-PAK1-1|CsnPharm

CAS No.: 1783816-74-9

NVS-PAK1-1 Catalog No. CSN20017

NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1, a serine-threonine kinase that is upregulated in many cancers. NVS-PAK1-1 has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro dephosphorylation assay.

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400-920-2911

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技术信息

生物活性

描述PAK1 is a serine/threonine protein kinase involved in cytoskeletal signaling and oncogenic transformation. The dysregulation of PAK1 has been reported in breast, squamous NSCLC, and pancreatic cancers. NVS-PAK1-1 is a potent, selective, allosteric PAK1 Inhibitor with an IC50 value of 5nM. It has a biochemical PAK1 K_d of 7nM and a PAK2 K_d of 400nM. NVS-PAK1-1 significantly inhibited pMEK Ser289 at a concentration of 6–20μM. It inhibited the proliferation of Su86.86 cells at a concentration of 2μM. NVS-PAK1-1 at 0.21μM also significantly inhibited downstream signaling and cell proliferation when applied together with PAK2 shRNA. NVS-PAK1-1 exhibited high Caco2 permeability (P_app A-B 42.8 × 10^-8cm/s). NVS-PAK1-1 showed a relatively poor stability in rat liver microsomes (t_1/2=3.5min)^[2].
参考文献

[1] Karpov AS, Amiri P, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.
[2] Karpov AS, Amiri P, Bellamacina C. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0837 mL
- 10.4183 mL
- 20.8366 mL
- 5 mM
- 0.4167 mL
- 2.0837 mL
- 4.1673 mL
- 10 mM
- 0.2084 mL
- 1.0418 mL
- 2.0837 mL

技术信息

CAS号

1783816-74-9

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H25ClF3N5O

运输

蓝冰

分子量

479.93

别名

溶解度

DMSO	125.0 mg/mL (260.5 mM)

动物实验配方

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