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 |
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
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 |
搜索质检报告(COA)
搜索MSDS
相关产品