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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.
|Storage||Store at -80°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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 will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.05 mM||35.61 mL||178.05 mL||356.1 mL|
|0.25 mM||7.12 mL||35.61 mL||71.22 mL|
|0.5 mM||3.56 mL||17.8 mL||35.61 mL|
|2.5 mM||0.71 mL||3.56 mL||7.12 mL|
References are publications that support the biological activity of the product.
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 PMID: 7592920
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, Tax. and gemcit. Cancer Res. 59 4919 PMID: 10519405
Lerner et al (1995) Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem. 10 26770
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Keywords: FTI 277, FTI 277 supplier, Prodrug, FTI, 276, 2406, farnesyltransferase, FTase, H-Ras, K-Ras, MAPK, anti-proliferative, antiproliferative, tumour, tumor, FTI277, Protein, Prenyltransferases, Post-translational, Modifications, 2407, Tocris Bioscience
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