1A-116
作者：齐岳
发布时间：2023-09-13
16:39:32
点击数：
产品名称：1A-116
产品描述：
| 产品描述 | 1A-116 is a specific Rac1 inhibitor. |
| 靶点活性 | antiproliferation:4 µM(F3II cell) |
| 体外活性 | 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[1]. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 μM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 μM)[2]. |
| 体内活性 | Daily treatment of mice with compound 1A-116 at 3mg/kg body weight/day reduces 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 reduces the total lung weight compare to the control group, leading to a total weight similar to the average pulmonary weight of Balb/c mice[2]. |
| 分子量 | 307.31 |
| 分子式 | C16H16F3N3 |
| CAS No. | 1430208-73-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mg/mL (325.40 mM),Need ultrasonic
H2O: < 0.1 mg/mL (insoluble)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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