CH5132799

CH5132799 (订货以英文为准)

编号:C127596
CAS号:1007207-67-1
分子式:C15H19N7O3S
分子量:377.42
货号 品牌 包装 目录价 您的价格 库存 数量 购买
C127596-25mg 阿拉丁 25mg ¥965.90
C127596-5mg 阿拉丁 5mg ¥383.90
C127596-100mg 阿拉丁 100mg ¥2470.90
C127596-1mg 阿拉丁 1mg ¥263.90
C127596-50mg 阿拉丁 50mg ¥1544.90
C127596-10mg 阿拉丁 10mg ¥612.90
产品名称 CH5132799
中文名称 CH5132799
CAS号 1007207-67-1
分子式(M.F.) C15H19N7O3S
分子量(M.W.) 377.42
储存条件 -20°C储存
溶解性DMSO 12 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件储存温度-20°C
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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