溶解性 | DMSO 14 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
存贮条件 | 储存温度-20°C |
备注 | PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2. |
生化机理 | PF-04691502 is an ATP-competitive PI3K/mTOR dual inhibitor with IC50 of 32 nM. PF-04691502 is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PF-04691502 inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. PF-04691502 is currently in Phase II clinical trials in patients with recurrent endometrial cancer and Breast Cancer. A Phase II clinical trials in patients with solid tumors has been completed. |
别名 | 2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one;2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
PF-04691502,双重PI 3-K / mTOR抑制剂
PF-04691502 (订货以英文为准)
编号:P126369
CAS号:1013101-36-4
分子式:C22H27N5O4
分子量:425.48
产品名称 | PF-04691502 |
中文名称 | PF-04691502,双重PI 3-K / mTOR抑制剂 |
CAS号 | 1013101-36-4 |
分子式(M.F.) | C22H27N5O4 |
分子量(M.W.) | 425.48 |
储存条件 | -20°C储存 |
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