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GGTI-2154
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GGTI-2154图片
CAS NO:251577-10-3
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
GGTI-2154 是一种有效和选择性的 geranylgeranyltransferase I (GGTase I) 抑制剂,IC50 值为 21 nM。GGTI-2154 对 GGTase I 的选择性是 FTase (IC50=5600 nM) 的 200 倍以上。GGTI-2154 可用于癌症的研究。
Cas No.251577-10-3
分子式C24H28N4O3
分子量420.5
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer[1][2].

GGTI-2154 inhibits the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL, with an IC50 of 21 nM[1].

GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-Ν-Ha-Ras transgenic mice[2].GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%[1].

[1]. Sun J, et, al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26.
[2]. Sun J, et, al. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice. Cancer Res. 2003 Dec 15;63(24):8922-9.