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经验配方 C₂₀H₁₇N₃O₆ 描述 概述 A cell-permeable, non-peptidyl pyrazolylcarbamoyl compound that targets the amphipathic client protein-binding groove of 14-3-3 and effectively competes against cellular pro-apoptotic c-Abl and cell cycle inhibitor protein p27Kip1 (CDK inhibitor 1B) for 14-3-3ς interaction, leading to c-Abl mitochondrial membrane relocation, c-Abl and p27Kip1 nuclear translocation, sub-G1 arrest, enhanced c-Abl cleavage, caspase-9 and -8 activation (24 h 5 µM treatment), and eventual apoptotic cell death in pro-B murine Ba/F3 lines expressing wt, E255K, or T315I Bcr-Abl (LD50 = 0.41, 1.30, 1.47 µM, respectively;). Also demonstrated to exhibit antiproliferative activity against the survival of three primary IM- (Imatinib mesylate; STI571) resistant CD34+ cultures (LD50 = 0.5, 0.7, and 2.5 µM) from CML (chronic myeloid leukemia) patients with T315I Bcr-Abl mutation. 产品目录编号 100082 品牌系列 Calbiochem®
同义词 2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid 参考 参考 Mancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596. 产品信息 形式 Off-white powder Hill配方 C₂₀H₁₇N₃O₆ 化学配方 C₂₀H₁₇N₃O₆ Molar Mass 395.4 结构配方图像 生物信息 纯度 ≥98% by HPLC 理化信息 溶解度 DMSO 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 Regulatory Review
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
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