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编 号:F293116
分子式:C24H28N4O3
分子量:420.5
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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.

体内研究:
GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-ν-Ha-Ras transgenic mice.GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%.Animal Model:MMTV-v-Ha-ras transgenic mice bearing mammary carcinoma
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.

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