| Bioactivity | L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM, respectively[1][2]. |
| Invitro | L-778123 dihydrochloride 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 dihydrochloride 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 dihydrochloride (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 dihydrochloride (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. 0 --> L-778123 dihydrochloride 相关抗体: |
| In Vivo | L-778123 dihydrochloride (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. |
| CAS | 183499-56-1 |
| Formula | C22H22Cl3N5O |
| Molar Mass | 478.80 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
L-778123 dihydrochloride
CAS: 183499-56-1 F: C22H22Cl3N5O W: 478.80
L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM, respectively.
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This product is for research use only, not for human use. We do not sell to patients.