251577-10-3

Name	GGTI-2154
CAS	251577-10-3
Molecular Formula	C24H28N4O3
MDL Number	MFCD28347816
Molecular Weight	420.5
MOL File	251577-10-3.mol

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]-

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Chemical Properties

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

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.

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

Supplier

Dayang Chem (Hangzhou) Co.,Ltd.

Telephone+86-0571-88938639 17705817739

Websitehttps://www.dycnchem.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Chengdu Peter-like Biotechnology Co., Ltd.

Telephone028-81700200 13308200041

Websitehttps://www.weikeqi-biotech.com/

GIHI CHEMICALS CO.,LIMITED

Telephone+86-571-86217390; +8618058761490

Websitehttps://www.gihichem.com/

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