CAS NO: | 183499-57-2 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Cas No. | 183499-57-2 |
Canonical SMILES | ClC1=CC(N2C(CN(CC3=CN=CN3CC4=CC=C(C#N)C=C4)CC2)=O)=CC=C1 |
分子式 | C22H20ClN5O |
分子量 | 405.9 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml,Ethanol: 10 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50= 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50= 98 nM).1It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner.Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50= 0.81 μM).2 1.Lobell, R.B., Liu, D., Buser, C.A., et al.Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-IMol. Cancer Ther.1(9)747-758(2002) 2.Si, M.-S., Reitz, B.A., and Borie, D.C.Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123Invest New Drugs23(1)21-29(2005) |