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NVS-PAK1-1

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Chemical Structure| 1783816-74-9 同义名 : -
CAS号 : 1783816-74-9
货号 : A605423
分子式 : C23H25ClF3N5O
纯度 : 99%+
分子量 : 479.926
MDL号 : MFCD30723183
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(218.78 mM)，配合低频超声助溶，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：
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 Kd of 7nM and a PAK2 Kd 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 (Papp A-B 42.8 × 10-8cm/s). NVS-PAK1-1 showed a relatively poor stability in rat liver microsomes (t1/2=3.5min)[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.42mL

2.08mL

1.04mL

20.84mL

4.17mL

2.08mL
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.