产品说明书
1A-116
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同义名 : | - |
| CAS号 : | 1430208-73-3 | |
| 货号 : | A724348 | |
| 分子式 : | C16H16F3N3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 307.31 | |
| MDL号 : | MFCD31619254 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(341.67 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | As a small GTPase, Rac1 switches between active and inactive states at various subcellular locations that include the plasma membrane, nucleus and mitochondria. Once activated, Rac1 interacts with a range of effectors that then mediate various biological functions[1]. 1A-116 is a specific Rac1 inhibitor[2]. 1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305[2]. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 µM. A-116 also dramatically impaired Rac1 activation at low micromolar range (1 µM)[3]. Daily treatment of mice with compound 1A-116 at 3mg/kg reduced about 60% the formation of total metastatic lung colonies. A significant antitumor activity is obtained for macronodules (more than 1 mm in diameter) by treatment with 1A-116 in this highly aggressive breast cancer model. The treatment with 1A-116 reduced the total lung weight compare to the control group, leading to a total weight similar to the average pulmonary weight of Balb/c mice[3]. | ||
| 作用机制 | Several hydrogen bonds are established between the guanidine nitrogen atoms and residues Asp57 and Ser71. Moreover, pi-stacking interactions are observed between the methylated aromatic ring of the 1A-116 and the aromatic ring of Trp56. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.25mL 0.65mL 0.33mL |
16.27mL 3.25mL 1.63mL |
32.54mL 6.51mL 3.25mL |
| 参考文献 |
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