L-778123 

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

L-778123 单独使用对 HT-29 和 A549 细胞系没有明显的细胞毒性 (IC₅₀: >100 μM)，但可以与 Doxorubicin (HY-15142A) 产生协同作用，且 IC₅₀s 分别降低为 1.72 和 1.52 μM^[2]。
L-778123 抑制骨髓性白血病细胞细胞系的增殖，IC₅₀ 值为 0.2 μM-1.8 μM，原代样品中的 IC₅₀ 值为 0.1 μM-161.8 μM^[3]。
L-778123 (0-1 μM, 12 小时; 或 5 μM，6 小时) 抑制 HL-60 细胞中的 H-RAS 异戊二烯化，并抑制磷酸化 MEK-1/2 水平 (5 μM，24 小时)^[3]。
L-778123 (0-100 μM，72 小时) 抑制人 PBMC 中的淋巴细胞活化 (标志物: CD71 或 CD25) 和功能^[4]。

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

L-778123 (50 mg/kg/天，输注，7 天) 抑制狗 PBMC 细胞中的 HDJ2 和 Rap1A 异戊烯化，但不抑制 Ki-Ras 异戊烯化^[1]。

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

405.88

C₂₂H₂₀ClN₅O

183499-57-2

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]