名称 | XL388 |
描述 | XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases. |
激酶实验 | Determination of Enzyme IC50 Values: IC50 values are determined using a 10 concentration point, non-radioactive, functional assay that employs a fluorescence-based, coupled-enzyme format, according to the manufacturer's protocol (Z'-LYTE@biochemical assay). Kinase selectivity is determined using both the Z'-LYTE@ and Adapta@ kinase assay format. |
体外活性 | In vitro, XL388 inhibited the activity of solid and hematopoietic tumor cell lines as well as the proliferation of MCF-7 cell line (IC50: 1.37 μM). xL388 inhibited mTORC1 phosphorylation of p70S6K (T389) in MCF-7 cells (IC50: 94 nM). xL388 inhibited the phosphorylation of mTORC2 by AKT (S473) (IC50 : 350 nM). |
体内活性 | In vitro, XL388 inhibited the activity of solid and hematopoietic tumor cell lines as well as the proliferation of MCF-7 cell line (IC50: 1.37 μM). xL388 inhibited mTORC1 phosphorylation of p70S6K (T389) in MCF-7 cells (IC50: 94 nM). xL388 inhibited the phosphorylation of mTORC2 by AKT (S473) (IC50 : 350 nM). |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 22 mg/mL (48.3 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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关键字 | inhibit | XL388 | Mammalian target of Rapamycin | XL-388 | Inhibitor | mTOR | XL 388 |
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