GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I) , with an IC 50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer
In Vitro
GGTI-2154 inhibits the transfer of geranylgeranyl from [ 3 H]GGPP to H-Ras CVLL, with an IC 50 of 21 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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% . 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 carcinomaDosage: 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.
