| Identification | Back Directory | [Name]
GGTI-2154 | [CAS]
251577-10-3 | [Synonyms]
GGTI-2154
GGTI2154,GGTI 2154
GAJLKAVQYXFCRU-QFIPXVFZSA-N
L-Leucine, N-[[5-[(1H-imidazol-4-ylmethyl)amino]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]- | [Molecular Formula]
C24H28N4O3 | [MDL Number]
MFCD28347816 | [MOL File]
251577-10-3.mol | [Molecular Weight]
420.5 |
| Chemical Properties | Back Directory | [Boiling point ]
699.6±55.0 °C(Predicted) | [density ]
1.233±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [pka]
3.69±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| [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 |
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