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  • A66
    • A 66; A-66
    货号: abs810801
    CAS号: 1166227-08-2
    分子式: C17H23N5O2S2
    分子量: 393.53
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810801-5mg 1-2周 ¥1056.00
    - +
    abs810801-10mg 1-2周 ¥1887.00
    - +
    abs810801-50mg 1-2周 ¥8004.00
    - +
    abs810801-100mg 1-2周 ¥11610.00
    - +
    大包装询价
    产品描述
    描述

    A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    中文别名
    A 66; A-66
    外观
    类白色至淡黄色固体
    可溶性/溶解性
    DMSO :79 mg/mL (200.74 mM)

    Ethanol :1 mg/mL (2.54 mM)
    生物活性
    靶点
    p110α,p110γ,p110δ,PI3Kβ
    In vitro(体外研究)
    A66 is a potent inhibitor of the wild-type and oncogenic forms of p110α but not other class-I PI3K isoforms. The p110α-specific inhibitor A66 (0.7 μM) induces a 75-80% reduction in focus formation by the highly transforming iSH2 mutants KS459delN, DKRMNS560del, and K379E. The p110α-specific inhibitor A66 reduced phosphorylation of Akt on T308 by all p85 mutants.
    In vivo(体内研究)
    The optimal dosing strategy for xenograft studies is determined by investigating the drug pharmacokinetics after a dose of 10 mg/kg of body weight by intraperitoneal injection in CD-1 mice. Despite a short half-life of only 0.42 h, the large Cmax (8247 nM) of A66 S that is reached 30 min after dosing ensured that the AUC0-inf (area under the curve from zero time to infinity) (6809 nM•h) is similar to that of BEZ-235 (7333 nM•h), which has a longer half-life of 2.73 h. Furthermore, the A66 on SK-OV-3 tumour tissue is tested using a single dose of 100 mg/kg of body weight to determine whether a long-lasting effect of the drug could be achieved on target tissues. These studies show that A66 causes a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK (extracellular-signal-regulated kinase), at both 1 and 6 h after dosing. Levels of A66 in plasma are determined to be 21.1±1.2 μM and 9.1±1.1 μM at 1 and 6 h after drug injection, whereas levels of A66 in the tumor are 22.7±2.1 μM and 16.0±1.3 μM at the same time points.
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