GGTI-2154

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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

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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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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.

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