中文名: | PP242;2-(4-氨基-1-异丙基-1H-吡唑并[3,4-d]嘧啶-3-基)-1H-吲哚-5-醇 |
中文别名: | PP 242; PP-242;2-(4-氨基-1-异丙基-1H-吡唑并[3,4-d]嘧啶-3-基)-1H-吲哚-5-醇; |
英文名称: | PP242 |
英文别名: | 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol;Torkinib |
CAS No.: | 1092351-67-1 |
分子式: | C16H16N6O |
分子量: | 308.34 |
性状: | 属性溶解性Soluble in DMSO (>10 mg/mL)存贮条件储存温度 2-8°C描述产品介绍Torkinib (PP242)是一种选择性的mTOR抑制剂,IC50为8 nM;靶向作用于mTOR复合体,作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。用途A selective FRAP inhibitor生化机理PP242 has been shown to be a an ATP-competitive mTORC1/mTORC2 (FRAP) inhibitor (IC50 = 8 nM). PP242 is the first selective inhibitor that targets the ATP domain of FRAP. This compound shows selectivity for FRAP over other PI 3K family kinases (IC50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 μM for p110γ, DNA-PK, p110δ, p110α and p110β respectively). Furthermore, PP242 hydrate inhibits both S6K and 4EBP1 phosphorylation this activity displays an overall decrease in cap-dependent protein translation. |
储存: | 储存温度 2-8°C |
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用途: | A selective FRAP inhibitor |