中文名称:

FRAX1036

中文同义词:

PAK小分子抑制剂(FRAX1036);FRAX1036游离态

英文名称:

FRAX1036

英文同义词:

FRAX1036;FRAX1036 (Free base);FRAX-1036;FRAX 1036;CS-2271;Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-[2-chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]-

CAS号:

1432908-05-8

分子式:

C28H32ClN7O

分子量:

518.05

EINECS号:

相关类别:

细胞生物学试剂;抑制剂

Mol文件:

1432908-05-8.mol

生物活性

FRAX1036 是一种 PAK 抑制剂，对 PAK1，PAK2 和 PAK4 的 Ki 值分别为 23.3 nM，72.4 nM 和 2.4 μM。

靶点

PAK1 23.3 nM (Ki) PAK2 72.4 nM (Ki) PAK4 2.4 μM (Ki)

PAK1 23.3 nM (Ki)

PAK2 72.4 nM (Ki)

体外研究

FRAX1036 is a PAK inhibitor with K i s of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively. FRAX1036 (2.5 μM) incombination with docetaxel alters stathmin phosphorylation, induces the apoptotic marker cleaved PARP and increases kinetics of apoptosis in MDA-MB-175 and HCC2911 cells; also alters microtubule organization, mitosis and cell fate in U2OS cells. Moreover, FRAX1036 shows significantly effective inhibition on U2OS cells. FRAX1036 (10 μM) affects the proliferation of non-small cell lung cancer (NSCLC) cells when added to KRAS prenylation inhibitors.