L-778123 (hydrochloride)

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively.

Product Specifications

CAS Number

[253863-00-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Farnesyl Transferase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/L-778123-hydrochloride.html

Concentration

10mM

Purity

99.85

Solubility

DMSO : ≥ 25 mg/mL|H2O : 25 mg/mL (ultrasonic)

Smiles

N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl

Molecular Formula

C22H21Cl2N5O

Molecular Weight

442.34

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Citation 01

BioRxiv. 2023 Feb 8:2023.02.07.527548.|Cell. 2025 Nov 24:S0092-8674 (25) 01244-9.|Immunity. 2024 May 14;57 (5) :1056-1070.e5.|ACS Nano. 2025 Aug 12;19 (31) :28644-28659.|bioRxiv. 2025 Jul 29.