L-778123 (hydrochloride)

Names

[ Name ]:
L-778123 (hydrochloride)

[Synonym ]:
Benzonitrile, 4-[[5-[[4-(3-chlorophenyl)-3-oxo-1-piperazinyl]methyl]-1H-imidazol-1-yl]methyl]-, hydrochloride (1:1)
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 hydrochloride (1:1)
Benzonitrile,4-((5-((4-(3-chlorophenyl)-3-oxo-1-piperazinyl)methyl)-1H-imidazol-1-yl)methyl)-,monohydrochloride
4-[(5-{[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl}-1h-imidazol-1-yl)methyl]benzonitrile hydrochloride(1:1)
L 778123
L-778123
L-778123 HCl
L-778123 (hydrochloride)

Biological Activity

[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]

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase

Research Areas >> Cancer

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
698.9ºC at 760 mmHg

[ Molecular Formula ]:
C₂₂H₂₁Cl₂N₅O

[ Molecular Weight ]:
442.341

[ Flash Point ]:
376.5ºC

[ Exact Mass ]:
441.112305

[ PSA ]:
65.16000

[ LogP ]:
4.11018

[ Vapour Pressure ]:
2.22E-19mmHg at 25°C

[ Storage condition ]:
2-8℃

Related Compounds

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