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  4. GGTI-2154

GGTI-2154 是一種有效和選擇性的 geranylgeranyltransferase I (GGTase I) 抑制劑，IC50 值為 21 nM。GGTI-2154 對(duì) GGTase I 的選擇性是 FTase (IC50=5600 nM) 的 200 倍以上。GGTI-2154 可用于癌癥的研究。

在相同的摩爾濃度下，化合物鹽形式與游離形式有相同的生物活性，但鹽形式 GGTI-2154 hydrochloride 通常具有更好的水溶性和穩(wěn)定性。

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GGTI-2154 Chemical Structure

GGTI-2154 Chemical Structure

CAS No. : 251577-10-3

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GGTI-2154 的其他形式現(xiàn)貨產(chǎn)品:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
體外研究
(In Vitro)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)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].

MCE 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 號(hào)
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
GGTI-2154
目錄號(hào)：
HY-16229
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