| Identification | Back Directory | [Name]
L778123 | [CAS]
253863-00-2 | [Synonyms]
L-778123HCl
L-778123 (hydrochloride)
L-778123;L 778123;L778123
L778123; L-778123; L 778123; L778,123; L-778,123; L 778,123 HCL; L-778123 HYDROCHLORIDE
4-[[5-[[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl]imidazol-1-yl]methyl]benzonitrile,hydrochloride
4-((5-((4-(3-Chlorophenyl)-3-oxo-1-piperazinyl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile hydrochloride
4-[[5-[[4-(3-Chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]benzonitrile monohydrochloride | [Molecular Formula]
C22H21Cl2N5O | [MOL File]
253863-00-2.mol | [Molecular Weight]
442.341 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 12.5 mg/ml; DMSO: 12.5 mg/ml; Ethanol: 10 mg/ml | [form ]
A crystalline solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively. | [Definition]
ChEBI: L-778,123 hydrochloride is the hydrochloride salt of L-778,123. It is a dual inhibitor of FPTase and GGPTase-I (IC50 of 2nM and 98nm, respectively) and exhibits anti-cancer properties. It has a role as an antineoplastic agent, an EC 2.5.1.58 (protein farnesyltransferase) inhibitor, an EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor and a radiosensitizing agent. It contains a L-778,123 (free base). | [in vivo]
L-778123 (50 mg/kg/day, infusion, 7 days) hydrochloride inhibits both HDJ2 and Rap1A prenylation in PBMCs of dogs, but without inhibition in Ki-Ras prenylation[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. PMID:12479371
[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. DOI:10.5681/apb.2013.012
[3] Fredrick O. Onono, et al. The Farnesyltransferase Inhibitor (FTI) L-778,123 Displays Promising Anti-Leukemia Activity. Blood (2008); 112 (11): 2627.
[4] Si MS, et al. Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123. Invest New Drugs. 2005 Jan;23(1):21-9. DOI:10.1023/B:DRUG.0000047102.26698.08 |
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