| 溶解性 | DMSO 23 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 备注 | XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases. |
| 生化机理 | Description:IC50 Value: 9.9 nM [1]XL388 is a novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitor.in vitro: Compound 28 (XL388) inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates.Furthermore, this compound displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. Oral administration of compound 28 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity [1].in vivo: XL388 resulted in complete inhibition of MCF-7 xenograft tumor growth at both doses, with significant tumor regression of 22% and 40% below pretreatment values at the 50 and 100 mg/kg doses, respectively. Furthermore, 28 does not appear to show significant toxicity. Mice in the 50 mg/kg cohort over the course of the study gained on average 2.2% additional mass, while those in the 100 mg/kg cohort lost on average 2.8% of their body mass [1].Clinical trial: N/A |
| 别名 | Methanone, [7-(6-amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-;Methanone, [7-(6-amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]- |
XL388,mTOR抑制剂
XL388 （订货以英文为准）
编号：X124864
CAS号：1251156-08-7
分子式：C23H22FN3O4S
分子量：455.50
| 产品名称 | XL388 |
| 中文名称 | XL388,mTOR抑制剂 |
| CAS号 | 1251156-08-7 |
| 分子式（M.F.） | C23H22FN3O4S |
| 分子量（M.W.） | 455.50 |
| 储存条件 | -20°C储存 |
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