• merck millipore,默克密理博,528121,PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem
  • merck millipore,默克密理博,528121,PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem

    产品名称:PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem
    产品型号:528121
    The PI 3-K/PDK-1 Inhibitor, NVP-BAG956, also referenced under CAS 853910-02-8, controls the biological activity of PI 3-K/PDK-1. This small molecule/inhibitor is primarily used for Phosphorylation & D More>>

    merck millipore,默克密理博,528121,PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem

  • 产品介绍
  • merck millipore,默克密理博,528121,PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem

    重要规格表

    经验配方 CAS号
    C₂₈H₂₁N₅853910-02-8
    描述
    概述 A cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC50 >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).
    产品目录编号 528121
    品牌系列 Calbiochem®
    同义词 α,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile , BAG956, PDK1 Inhibitor IV, PI 3-K Inhibitor XVI
    参考
    参考 Marone, R., et al. 2009. Mol. Cancer Res. 7, 601.
    Weisberg, E., et al. 2008. Blood 111, 3723.
    Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.
    产品信息
    CAS号 853910-02-8
    形式 Orange powder
    Hill配方 C₂₈H₂₁N₅
    化学配方 C₂₈H₂₁N₅
    Molar Mass 427.5
    结构配方图像
    生物信息
    纯度 ≥98% by HPLC
    理化信息
    溶解度 DMSO or EtOH
    储存和货运信息
    货运代码 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
    毒性 Standard Handling
    储存 +2°C to +8°C
    避光 Protect from light
    无需冷冻 No
    特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
    包装信息
    惰性气体下包装 Packaged under inert gas

    merck millipore,默克密理博,528121,PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem

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