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CAS No.: 1432908-05-8

FRAX1036 Catalog No. CSN17853

Synonyms: FRAX1036

FRAX-1036 is a potent and selective PAK1 inhibitor.

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技术信息

生物活性

描述The p21-activated kinases (PAKs) have generated significant interest as therapeutic targets in cancer. PAK1 signaling has been shown to be important for regulating cytoskeletal organization and cell migration via both its catalytic activity and protein-protein interactions. FRAX1036, a small molecule pyridopyrimidinone, is a PAK inhibitor. Its biochemical potency (Ki) against PAK1 and PAK2 is 23.3 and 72.4 nM, respectively, with high selectivity against PAK4. Potent cellular inhibition of group I PAK substrate phosphorylation was observed at 2.5 to 5 μM concentrations of FRAX1036 in PAK1-amplified MDA-MB-175 cells. FRAX1036 (5 μM) and docetaxel (0.2 μM) combination treatment for 24 hours of PAK1-amplified lines, MDA-MB-175 and HCC2911, elevated a major apoptotic marker (cleaved PARP) and attenuated a cell cycle regulator (cyclin D1). After 20 hours of treatment with 2.5 μM FRAX1036 for 20 hours, microtubules were disorganized and were not evenly distributed throughout the cytoplasm, between the microtubule organizing center and the periphery. Furthermore, FRAX1036-treated cells completed normal mitoses with the majority of apoptosis occurring during interphase (66.7%)^[3].
参考文献

[1] Ong CC, Gierke S, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res. 2015 Apr 23;17:59.
[2] Kosoff RE, Aslan JE, et al. Pak2 restrains endomitosis during megakaryopoiesis and alters cytoskeleton organization. Blood. 2015 May 7;125(19):2995-3005.
[3] Ong CC, Gierke S, Pitt C, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res. 2015;17(1):59

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
- 1.9303 mL
- 9.6515 mL
- 19.3030 mL
- 5 mM
- 0.3861 mL
- 1.9303 mL
- 3.8606 mL
- 10 mM
- 0.1930 mL
- 0.9652 mL
- 1.9303 mL

技术信息

CAS号

1432908-05-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H32ClN7O

运输

蓝冰

分子量

518.05

别名

FRAX1036

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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