Cas No.: | 253863-00-2 |
Chemical Name: | 4-((5-((4-(3-Chlorophenyl)-3-oxo-1-piperazinyl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile hydrochloride |
Synonyms: | 4-((5-((4-(3-Chlorophenyl)-3-oxo-1-piperazinyl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile hydrochloride;4-[[5-[[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl]imidazol-1-yl]methyl]benzonitrile,hydrochloride;L-778,123 hydrochloride;L778123 hydrochloride;L 778123;L-778123 (hydrochloride);L-778123HCL;L-778123 hydrochloride |
SMILES: | N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl |
Formula: | C22H20N5OCl.HCl |
M.Wt: | 442.34104 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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] |
References: | [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. |