溶解性 | DMSO ≥90mg/mL Water ≥1.8mg/mL Ethanol ≥13mg/mL |
存贮条件 | 储存温度-20°C |
密度 | 1.2480 |
产品介绍 | AZD8055是ATP竞争性mTOR抑制剂,IC50为0.8 nM,比对PI3K和ATM/DNA-PK的抑制性强超过1000倍。 |
备注 | AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (?1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1. |
生化机理 | AZD8055 shows low activity (~1,000-fold) against all PI3K isoforms (α, β, γ, δ) and other members of the PI3K-like kinase family (ATM and DNA-PK). AZD8055 inhibits the phosphorylation of mTORC1 (p70S6K and 4E-BP1) as well as phosphorylation of the mTORC2 (Akt) and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 can be fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. AZD8055 potently inhibits proliferation in U87MG, A549 and H838 cells with IC50 of 53, 50 and 20 nM, respectively. AZD8055 also induces autophagy and increased LC3-II levels in H838 and A549 cells [1]. AZD8055 decreases AML blast cell proliferation and cell cycle progression, reduces the clonogenic growth of leukemic progenitors and induces caspase-dependent apoptosis in leukemic cells but not in normal immature CD34+ cells |
别名 | (5-(2,4-二((3S)-3-甲基吗啉-4-基)吡啶并(2,3-d)嘧啶-7-基)-2-甲氧基苯基)甲醇;;AZD8055; AZD 8055;(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol |
AZD8055
AZD8055 (订货以英文为准)
编号:A126366
CAS号:1009298-09-2
分子式:C25H31N5O4
分子量:465.56
产品名称 | AZD8055 |
中文名称 | AZD8055 |
CAS号 | 1009298-09-2 |
分子式(M.F.) | C25H31N5O4 |
分子量(M.W.) | 465.56 |
储存条件 | -20°C储存 |
WGK德国 | 3 |
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