C127596-5mgCH5132799
面议
- 阿拉丁
- 生产商
- C127596-5mg
- 现货
- 全国
规格 |
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耗材描述
属性
溶解性 |
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存贮条件 | 储存温度-20°C |
描述
应用 | A PI3K and FRAP inhibitor |
产品介绍 | CH5132799是I型PI3K选择性抑制剂,对PI3Kα,PI3Kβ,PI3Kδ和PI3Kγ的IC50分别为0.014,0.12,0.50和0.36 uM,对II和III型PI3k以及mTOR的抑制性较低。 |
生化机理 | CH5132799 selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 0.014, 0.12, 05.0, and 0.36 μM, respectively. CH5132799 shows less inhibition of class II PI3Ks, class III PI3ks, and mTOR. CH5132799 suppresses phosphorylation of treated breast cancer KPL-4 cells, as well as Akt and its direct substrates, PRAS40 and FoxO1/3a. Down stream factors, including S6K, S6 and 4E-BP1, are effectively suppressed. Cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH5132799. In human tumor cell lines with PI3K pathway activation by mutation, CH5132799 shows potent antiproliferative activity [HCT116(CRC): IC50 = 0.20 lM, KPL-4(BC):13 IC50 = 0.032 lM, T-47D(BC): IC50 = 0.056 lM, SK-OV-3(Ovarian): IC50 = 0.12 lM]. |
别名 | CH 5132799;CH-5132799;(5-(7-甲磺酰基-2-(吗啉-4-基)-6,7-二氢-5H-吡咯并(2,3-d)嘧啶-4-基)嘧啶-2-基)胺;;CH 5132799;CH-5132799;(5-(7-methylsulfonyl-2-(morpholin-4-yl)-6,7-dihydro-5h-pyrrolo(2,3-d)pyrimidin-4-yl)pyrimidin-2-yl)amine |
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