AT13148
规格
| Cas Number | 1056901-62-2 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| Action Type | 抑制剂 |
| Mechanism Of Action | MAP 激酶激活的蛋白激酶 2 抑制剂 |
| 简短描述 | ROCK2 选择性抑制剂 |
| 英文简短描述 | ROCK2 Selective Inhibitors |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | AT13148 是一种口服 ATP 竞争性多AGC 激酶抑制剂，对 Akt1/2/3、p70S6K、PKA 和 ROCKI/II 的 IC50 分别为 38 nM/402 nM/50 nM、8 nM、3 nM 和 6 nM/4 nM。第一阶段 |
| 英文描述 |
Information AT13148 is an oral, ATP-competitive, multi-AGC kinaseinhibitor withIC50of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM forAkt1/2/3,p70S6K,PKA, andROCKI/II, respectively. Phase 1. Targets PKA (Cell-free assay); ROCK2 (Cell-free assay); ROCK1 (Cell-free assay); p70S6K (Cell-free assay); Akt1 (Cell-free assay) 15565,3 nM; 4 nM; 6 nM; 8 nM; 38 nM In vitro AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling. In vivo AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts. Cell Research(from reference) Cell lines：MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines Concentrations：~10 μM Incubation Time：72 hours or 96 hours |