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经验配方 CAS号 C₂₃H₂₁N₃O₂ 873305-35-2 描述 概述 A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22 nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16 h 800 nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7 nM) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures. Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72 h 8 µM) and in castrated mice in vivo (4 mg/kg/96 h injections on day 7/11/15/19/23/27 post tumor transplant). 产品目录编号 104833 品牌系列 Calbiochem®
同义词 (S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine, Activated Cdc42 Kinase 1 Inhibitor 参考 参考 Mahajan, K., et al. 2012. J. Biol. Chem. 287, 22112.
Mahajan, K., et al. 2012. Am. J. Pathol. 180, 1386.
Mahajan, K., et al. 2010. Prostate 70, 1274.
DiMauro, E.F., et al. 2007. Bioorg. Med. Chem. Lett. 17, 2305.产品信息 CAS号 873305-35-2 形式 Yellow solid Hill配方 C₂₃H₂₁N₃O₂ 化学配方 C₂₃H₂₁N₃O₂ Molar Mass 371.4 可逆 Y 生物信息 主靶 Ack1 主靶IC50 22 nM for Ack1 副靶 Lck, Lyn 纯度 ≥98% by Chiral HPLC
Enantiomeric excess (ee): 98.29% (based on the ee of (S)-(+)-Tetrahydrofurfurylamine, as determined using Chiral HPLC column)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
避免冻结 / 解冻 Avoid freeze/thaw
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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