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经验配方 C₃₁H₃₄N₄O₃S 描述 概述 A cell-permeable benzyl ester prodrug form of FTI-2148 (Cat. No. 344557) that preferentially inhibits protein farnesyltransferase activity (IC50 = 530 nM for mammalian and 1.0 µM for P. falciparum) over protein geranylgeranyltransferase-I (IC50 > 10 µM for mammalian) and displays anti-malarial properties. Potently disrupts Ras farnesylation in H-Ras-transformed NIH 3T3 cells (IC50 = 20 nM) and inhibits the growth of P. falciparum in red blood cells (ED50 = 150 nM). Also suppresses parasitemia in P. berghei-infected mice by 46.1% (50 mg/kg, ip) with no apparent toxicity. 产品目录编号 344559 品牌系列 Calbiochem®
同义词 2-(((5-((1H-Imidazol-4-ylmethyl)-amino)-methyl)-2ʹ-methyl-biphenyl-2-carbonyl)-amino)-4-methylsulfanyl-butyric acid benzyl ester 参考 参考 Carrico, D., et al. 2004. Bioorg. Med. Chem. 12, 6517.
Ohkanda, J., et al. 2004. J. Med. Chem. 47, 432.产品信息 具有ATP竞争性 N 形式 White solid Hill配方 C₃₁H₃₄N₄O₃S 化学配方 C₃₁H₃₄N₄O₃S Molar Mass 542.7 可逆 N 结构配方图像 生物信息 主靶 Protein farnesyltransferase (PFTase) 主靶IC50 530 nM for mammalian and 1.0 µM for P. falciparum protein farnesyltransferase activity 纯度 ≥95% by HPLC 理化信息 细胞可渗透 Y 溶解度 DMSO or MeOH 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
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 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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