PI-103,PI3K 和 mTOR 抑制剂

PI-103 (订货以英文为准)

编号:P125961
CAS号:371935-74-9
分子式:C19H16N4O3
分子量:348.36
货号 品牌 包装 目录价 您的价格 库存 数量 购买
P125961-10mg 阿拉丁 10mg ¥552.90
P125961-50mg 阿拉丁 50mg ¥1693.90
P125961-100mg 阿拉丁 100mg ¥3211.90
产品名称 PI-103
中文名称 PI-103,PI3K 和 mTOR 抑制剂
CAS号 371935-74-9
分子式(M.F.) C19H16N4O3
分子量(M.W.) 348.36
储存条件 -20°C储存
溶解性Soluble in DMSO (10 mg/ml), DMF (10 mg/ml), 1:2 DMSO:PBS(pH 7.2) (0.25 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.
存贮条件储存温度-20°C
应用An ATP-competitive DNA-PK, PI 3-kinase, and FRAP inhibitor.
产品介绍PI-103是一种多靶点的PI3K抑制剂,对p110α的抑制效果最好,IC50为2 nM (对p110β/δ/γ抑制效果稍弱),也抑制mTORC1/2和DNA-PK ,IC50分别为20 nM/83 nM和8 nM。
备注PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
生化机理PI-103 is a cell-permeable pyridinylfuranopyrimidine compound that acts as an ATP-competitive inhibitor of DNA-PK, PI 3-kinase (Class IA), and FRAP (mTOR) complex 1 and 2. Studies suggest that PI-103 can induce apoptosis and an arrest in the cell cycle by inhibition of the aforementioned proteins. When PI-103 is combined with rapamycin, a prototypic mTORC1 inhibitor, synergistic suppression of AKT and ribosomal S6 protein phosphorylation are observed. In addition, PI-103 has been seen to have nominal effects inhibiting basal Na+ transport, but is very effective in abolishing insulin-induced Na+ absorption in the nephron.
别名PI 103 ; 3-[4-(4-吗啉基吡啶并[3',2',4,5]呋喃并[3,2-d]嘧啶-2-基]苯酚;PI 103;PI103;PI 3-K Inhibitor V;3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol
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