L-778123
L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively[1][2].
Product Specifications
CAS Number
183499-57-2
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.html
Purity
99.92
Solubility
1 M HCl : ≥ 100 mg/mL|DMSO : 20 mg/mL (ultrasonic; adjust pH to 2 with 1 M HCl)
Smiles
N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1
Molecular Formula
C22H20ClN5O
Molecular Weight
405.88
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
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Citation 01
ACS Nano. 2025 Aug 12;19 (31) :28644-28659.|bioRxiv. 2025 Jul 29.|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.
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