FTI 277

Key Product Details

Product Description

FTI 277 is a 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 activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.

Product Specifications for FTI 277

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for FTI 277

The following data is based on the product molecular weight 561.64.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.05 mM	35.61 mL	178.05 mL	356.10 mL
0.25 mM	7.12 mL	35.61 mL	71.22 mL
0.5 mM	3.56 mL	17.80 mL	35.61 mL
2.5 mM	0.71 mL	3.56 mL	7.12 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 5 publications citing the usage of this product.

• Sun Antitumour efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Tax. and gemcit. Cancer Res. 1999 PMID: 10519405
• Lerner Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem.
• Lerner Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling inducing cytoplasic accumulation of inactive Ras-Raf complexes. J.Biol.Chem. 1995 PMID: 7592920

Product Documents for FTI 277