GGTI-2154 hydrochloride

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GGTI-2154 hydrochloride Basic information
Product Name:GGTI-2154 hydrochloride
Synonyms:GGTI-2154 hydrochloride;L-Leucine, N-[[5-[(1H-imidazol-4-ylmethyl)amino]-2′-methyl[1,1′-biphenyl]-2-yl]carbonyl]-, monohydrochloride
CAS:478908-50-8
MF:
MW:456.97
EINECS:
Product Categories:
Mol File:478908-50-8.mol
GGTI-2154 hydrochloride Structure
GGTI-2154 hydrochloride Chemical Properties
form Solid
color White to off-white
Safety Information
MSDS Information
GGTI-2154 hydrochloride Usage And Synthesis
UsesGGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 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[1][2].
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].

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.
References[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. PMID:10519405
[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. PMID:14695209
GGTI-2154 hydrochloride Preparation Products And Raw materials
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