FTI 277Cat No.
2407
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Price and Availability |
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Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl ]methionine methyl ester trifluoroacetate salt |
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Biological Activity
Prodrug form of FTI 276 (Cat. No. 2406) that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific actvation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.Technical Data
M.Wt:The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.
Resources
Certificate of Analysis / MSDS
References
Lerner et al (1995) Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem. 10 26770. Lerner et al (1995) Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling inducing cytoplasic accumulation of inactive Ras-Raf complexes. J.Biol.Chem. 270 26802. Sun et al (1999) Antitumour 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. 59 4919.If you know of a useful citation for this product please let us know.
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Keywords: FTI 277, Prodrug, FTI, 276, 2406, farnesyltransferase, FTase, H-Ras, K-Ras, MAPK, anti-proliferative, antiproliferative, tumour, tumor, FTI277
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