产品描述: | FRAX-1036是一种有效的、选择性PAK抑制剂, 其对PAK1和PAK2的Ki值分别为23.3 nM和72.3 nM |
靶点: |
PAK1(Cell-free assay):23.3 nM(Ki); PAK2(Cell-free assay):72.4 nM(Ki); PAK4(Cell-free assay):2.4 μM(Ki);PAK |
体外研究: |
在PAK1扩增的MDA-MB-175种,2.5-5 μM FRAX1036的处理下,对1型PAK底物的磷酸化有抑制效果。用FRAX1035处理PAK1增殖的乳腺癌细胞能诱导凋亡。用FRAX103处理OVCAR-3细胞导致p53和p21的上调、cyclinc B1 的下调 |
体内研究: |
在小鼠中,处理以FRAX1-26导致KT21肿瘤生长变慢。FRAX1-26很难通过血脑屏障 |
细胞实验: |
Cell lines: MDA-MB175细胞 Concentrations: 0, 0.5, 1, 2.5, 5 μM Incubation Time: 24 h Method: 将MDA-MB175细胞用不同浓度的FRAX1036处理24小时,然后用生物标记抗体对细胞裂解物进行免疫沉淀分析 |
动物实验: |
Animal Models: Pak2-deficient小鼠 Dosages: 30 mg/kg Administration: 口服 |
参考文献: |
1. Ong CC, 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, 17:59. 2. Kosoff RE, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Blood. 2015, 125(19):2995-3005. 3. Alexander B. Koval, et al. An optimized synthesis of the potent and selective Pak1 inhibitor FRAX-1036. Tetrahedron Letters. 2016, 57(3):449-451. 4. Chow HY, et al. Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget. 2015, 6(4): 1981-1994. |
溶解性: |
soluble in 4-Methylpyridine |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.93 ml |
9.652 ml |
19.303 ml |
5 mM |
0.386 ml |
1.93 ml |
3.861 ml |
10 mM |
0.193 ml |
0.965 ml |
1.93 ml |
50 mM |
0.039 ml |
0.193 ml |
0.386 ml |
|
注意: |
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