L-778123 dihydrochloride 

L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC₅₀s of 2 nM and 98 nM, respectively^[1][2].

L-778123 dihydrochloride alone does not have obvious cytotoxicity on HT-29 and A549 cell lines (IC₅₀: >100 μM), but can generate synergistic effects with Doxorubicin (HY-15142A), with the decreased IC₅₀s of 1.72 and 1.52 μM respectively^[2].
L-778123 dihydrochloride inhibits myeloid leukemia cell proliferation with IC₅₀ values of 0.2 μM-1.8 μM for cell lines, and 0.1 μM-161.8 μM in primary samples^[3].
L-778123 dihydrochloride (0-1 μM, 12 h; or 5 μM, 6 h) inhibits H-RAS prenylation in HL-60 cells, and inhibits phosphorylated MEK-1/2 level (5 μM, 24 h)^[3].
L-778123 dihydrochloride (0-100 μM, 72 h) inhibits lymphocyte activation (marker: CD71 or CD25) and function in human PBMCs^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

L-778123 dihydrochloride (50 mg/kg/day, infusion, 7 days) inhibits both HDJ2 and Rap1A prenylation in PBMCs of dogs, but without inhibition in Ki-Ras prenylation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

478.80

C₂₂H₂₂Cl₃N₅O

183499-56-1

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]