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  • Apitolisib (GDC-0980, RG7422)

    • GDC-0980;RG7422
    货号: abs813206
    CAS号: 1032754-93-0
    分子式: C23H30N8O3S
    分子量: 498.6
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    货号-规格 货期 价格 数量
    abs813206-5mg 现货 ¥1335.00
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    abs813206-10mg 现货 ¥1940.00
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    abs813206-50mg 现货 ¥5579.00
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    大包装询价
    产品描述
    描述

    Apitolisib (GDC-0980, RG7422)是一种有效的,I型PI3K抑制剂,作用于PI3Kα/β/δ/γ,IC50分别为5 nM/27 nM/7 nM/14 nM,也抑制mTOR,Ki为17 nM,高选择性作用于其他PIKK家族激酶。

    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
    别名
    GDC-0980;RG7422
    可溶性/溶解性
    DMSO : 14.29 mg/mL (28.66 mM; Need ultrasonic)
    生物活性
    靶点
    p110α ,p110δ ,p110γ ,mTOR ,p110β
    In vitro(体外研究)
    GDC-0980 shows the potent and selective inhibitory activities against class I PI3K and mTOR kinase versus a large panel of kinases with Ki of 17 nM for mTOR and IC50 of 5 nM, 27 nM, 7 nM, and 14 nM for PI3Kα, β, δ, and γ, respectively. In vitro, GDC-0980 significantly inhibits cell proliferation in PC3 and MCF7 cells with IC50 of 307 nM and 255 nM, respectively. A recent study shows that GDC-0980 reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50
    In vivo(体内研究)
    In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg. In mice, intravenous GDC-0980 administration at 1 mg/kg leads to low clearance (Clp: 9.2 mL/min/kg, Vss: 1.7 L/kg). While, oral administration at 5 mg/kg in 80% PEG400 and at 50 mg/kg as a crystalline suspension in 0.5% methylcellulose/0.2% Tween-80 also results in favorable pharmacokinetic parameters.
    参考文献
    参考文献
    Preclinical Assessment of the Absorption and Disposition of the Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor GDC-0980 and Prediction of Its Pharmacokinetics and Efficacy in Human.
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