FTI-2153是一种有效、高度选择性的法尼基转移酶farnesyltransferase(FTase)抑制剂,IC50为1.4nM。FTI-2153有效抑制H-Ras蛋白的加工修饰,IC50值为10nM,是对其抑制活性是对Rap1A蛋白加工的3000多倍。
Cas No. | 344900-92-1 |
Canonical SMILES | CSCC[C@@H](C(OC)=O)NC(C1=CC=C(CNCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O |
分子式 | C25H30N4O3S |
分子量 | 466.6 |
溶解度 | DMSO: 100 mg/mL (214.32 mM) |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity[1]. [1]. Sun J, et al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26. |