GGTI-2154 hydrochloride |
| Catalog No.GC62635 |
El clorhidrato de GGTI-2154 es un inhibidor potente y selectivo de la geranilgeraniltransferasa I (GGTasa I), con una IC50 de 21 nM. El clorhidrato de GGTI-2154 muestra una selectividad de mÁs de 200 veces para la GGTasa I sobre la FTasa (IC50 = 5600 nM). El clorhidrato de GGTI-2154 se puede utilizar para la investigaciÓn del cÁncer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 478908-50-8
Sample solution is provided at 25 µL, 10mM.
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GGTI-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].
GGTI-2154 inhibits the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL, with an IC50 of 21 nM[1].
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].
[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.
[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.
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