Home>>Signaling Pathways>> Proteases>> Farnesyl Transferase>>L-778123 hydrochloride (L-778,123 hydrochloride)

L-778123 hydrochloride (L-778,123 hydrochloride) Sale

(Synonyms: 4-[[5-[[4-(3-氯苯基)-3-氧代-1-哌嗪基]甲基]-1H-咪唑-1-基]甲基]苯甲腈单盐酸盐,L-778,123 hydrochloride) 目录号 : GC32759

A dual inhibitor of FTase and GGTase I

L-778123 hydrochloride (L-778,123 hydrochloride) Chemical Structure

Cas No.:253863-00-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥932.00
现货
5mg
¥848.00
现货
10mg
¥1,428.00
现货
50mg
¥5,712.00
现货
100mg
¥9,818.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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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).1 It 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 CTLL-2 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)

Chemical Properties

Cas No. 253863-00-2 SDF
别名 4-[[5-[[4-(3-氯苯基)-3-氧代-1-哌嗪基]甲基]-1H-咪唑-1-基]甲基]苯甲腈单盐酸盐,L-778,123 hydrochloride
Canonical SMILES N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl
分子式 C22H21Cl2N5O 分子量 442.34
溶解度 DMSO : ≥ 25 mg/mL (56.52 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2607 mL 11.3035 mL 22.607 mL
5 mM 0.4521 mL 2.2607 mL 4.5214 mL
10 mM 0.2261 mL 1.1304 mL 2.2607 mL
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