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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-mTOR-XL388
XL388

Chemical Structure : XL388

CAS No.: 1251156-08-7

XL388 (XL-388)

货号: PC-49619Not For Human Use, Lab Use Only.

XL388 (XL-388) is a potent, selective and orally bioavailable mTOR inhibitor with IC50 of 9.9 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

XL388 (XL-388) is a potent, selective and orally bioavailable mTOR inhibitor with IC50 of 9.9 nM.
XL388 displays no significant activity against PI3K members with IC50 of >3 uM.
XL388 inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates.
XL388 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.

物理化学性质&存储条件

分子量 455.50
分子式 C23H22FN3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]methanone

参考文献

1. Takeuchi CS, et al. J Med Chem. 2013 Mar 28;56(6):2218-34.

2. Zhu YR, et al. Oncotarget. 2016 Aug 2;7(31):49527-49538.

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