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经验配方 CAS号 C₃₂H₄₁N₅O₄S₂ 439575-02-7 描述 概述 A cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19 nM; [ATP] = 1 µM) in an ATP-competitive manner by stabilizing ITK activation loop in a substrate-blocking, inactive conformation, inhibiting Fyn, IR, Lck, Btk only at much higher concentrations (IC50 ≥1.1 µM) and exhibiting little or no activity against 14 other kinases (IC50 ≥11 µM). Inhibits ITK-dependent cellular signaling (IC50 <300 nM against αCD3-stimulated PLCγ1 Tyr phosphorylation and Ca2+ mobilization in Jurkat cells) in vitro and alleviate OVA (Cat. No. 32467) challenge-induced airway leukocytes infiltration (ED50 = 25 mg/kg s.c.) in OVA-sensitized mice in vivo. 产品目录编号 419820 品牌系列 Calbiochem®
同义词 BMS509744; EMT Inhibitor, IL-2-Inducible T Cell Kinase Inhibitor, N-(5-(5-(4-Acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenylthio)thiazol-2-yl)-4-((3,3-dimethylbutan-2-ylamino)methyl)benzamide, N-(5-((3-((4-Acetylpiperazin-1-yl)carbonyl)-4-methyl-6-methoxyphenyl)thio)thiazol-2-yl)-4-(N-1,2-dimethylpropylaminomethyl)benzamide 参考 参考 Kutach, A.K., et al. 2010. Chem. Biol. Drug Des. 76, 154.
Das, J., et al. 2006. Bioorg. Med. Chem. Lett. 16, 3706.
Lin, T.A., et al. 2004. Biochemistry 43, 11056.产品信息 CAS号 439575-02-7 形式 Pale yellow powder Hill配方 C₃₂H₄₁N₅O₄S₂ 化学配方 C₃₂H₄₁N₅O₄S₂ Molar Mass 623.8 可逆 Y 结构配方图像 生物信息 主靶 ITK 主靶IC50 19 nM for ITK 纯度 ≥97% 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 -20°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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