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AZD8055
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
货号 | CAS号 | 操作 |
---|---|---|
A126366-10mg | 1009298-09-2 | 询价 |
A126366-200mg | 1009298-09-2 | 询价 |
A126366-50mg | 1009298-09-2 | 询价 |
产品介绍
属性
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 |
描述
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信息由上海阿拉丁生化科技股份有限公司为您提供,如您想了解更多关于AZD8055报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途