L-778123盐酸盐是FPTase和GGPTase-I双重抑制剂,IC50值分别为2nM和98nM。
CAS：253863-00-2
分子式：C22H21Cl2N5O
分子量：442.34
纯度：98%
存储：Store at -20°C

Background:

L-778123 hydrochloride is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.IC50 value: 2 nM [1]Target: FPTasein vitro: L-778123 can completely inhibit Ki-Ras prenylation. [1] L-778123 as a farnesyltransferase inhibitor can have a good cytotoxic activity as a classic anti-cancer agent. [2]in vivo: In the dog model, L-778123 inhibits HDJ2 prenylation and produces measurable, albeit slight (5%), levels of unprenylatedRap1A in PBMCs. [1]

[1]. Lobell RB, et al. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-758. [2]. Ghasemi S, et al. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines. Adv Pharm Bull. 2013;3(1):73-77.