merck millipore,默克密理愽
  • merck millipore,默克密理博,526529,PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

  • merck millipore,默克密理博,526529,PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

    产品名称：PIM-Kinase Inhibitor X, CX-6258 - Calbiochem
    产品型号：526529
    The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

    merck millipore,默克密理博,526529,PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

  • 产品介绍
  • merck millipore,默克密理博,526529,PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

    重要规格表

    经验配方
    C₂₆H₂₄ClN₃O₃•HCl
    描述
    概述 An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC50 = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; Ki = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC80 > 500 nM). Shown to arrest the proliferation of several human cancer cells (IC50 = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser112, 4E-BP1-Ser65 and Thr37/46 with an IC50 of ~ 1.0 µM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat.No.324380) and paclitaxel (Cat.No.580555) toxicity in PC3 cells.
    产品目录编号 526529
    品牌系列 Calbiochem®
    同义词 (E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl
    参考
    参考 Haddach, M., et al. 2012. ACS Med. Chem. Lett. 3, 135.
    产品信息
    形式 Orange powder
    Hill配方 C₂₆H₂₄ClN₃O₃•HCl
    Molar Mass 498.4
    吸湿 Hygroscopic
    可逆 Y
    结构配方图像
    生物信息
    主靶 PIM Kimases
    主靶IC50 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3
    副靶 Flt3
    纯度 ≥99% by HPLC
    理化信息
    细胞可渗透 Y
    溶解度 DMSO
    储存和货运信息
    货运代码 Ambient Temperature Only
    毒性 Standard Handling
    储存 +2°C to +8°C
    避光 Protect from light
    吸湿 Hygroscopic
    无需冷冻 No
    特殊指南 Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
    包装信息
    惰性气体下包装 Packaged under inert gas

    merck millipore,默克密理博,526529,PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

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