GGTI-2154

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GGTI-2154 

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。

GGTI-2154

GGTI-2154 Chemical Structure

CAS No. : 251577-10-3

规格 价格 是否有货
5 mg ￥6200 询问价格 & 货期
10 mg ￥9800 询问价格 & 货期

* Please select Quantity before adding items.

GGTI-2154 的其他形式现货产品:

GGTI-2154 hydrochloride

生物活性

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].

IC50 & Target

IC50: 21 nM (GGTase I)[1]
体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MMTV-v-Ha-ras transgenic mice bearing mammary carcinoma[2]
Dosage: 100 mg/kg/day
Administration: S.c. with osmotic mini-pumps for 14 days
Result: Halted the tumors aggressive growth.
Resulted in rapid tumor regression within 3 days of initiation of drug treatment.

分子量

420.50

Formula

C24H28N4O3
CAS 号

251577-10-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务