FTI 276

Discontinued Product

Unfortunately FTI 276 (Cat. No. 2406) has been withdrawn from sale for commercial reasons.
Cat.No. 2406 - FTI 276 | C21H27N3O3S2.C2HF3O2 | CAS No. 1217471-51-6
Description: Farnesyltransferase (FTase) inhibitor; antitumor
Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine trifluoroacetate salt
Purity: ≥95% (HPLC)

Biological Activity

Ras CAAX peptidomimetic, a selective inhibitor of farnesyltransferase (FTase) that displays > 100-fold selectivity over geranylgeranyltransferase I (GGTase I) (IC50 values are 0.5 and 50 nM respectively). Blocks growth of human lung carcinoma expressing oncogenic K-Ras in nude mice.

Technical Data

M. Wt 547.61
Formula C21H27N3O3S2.C2HF3O2
Storage Store at -80°C
Purity ≥95% (HPLC)
CAS Number 1217471-51-6
PubChem ID 395753
Smiles SC[C@H](N)CNC1=CC=C(C(N[C@H]([C@](O)=O)CCSC)=O)C(C2=CC=CC=C2)=C1.FC(F)(C(O)=O)F

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

All Tocris products are intended for laboratory research use only.

Preparing Stock Solutions

The following data is based on the product molecular weight 547.61. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.83 mL 9.13 mL 18.26 mL
5 mM 0.37 mL 1.83 mL 3.65 mL
10 mM 0.18 mL 0.91 mL 1.83 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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Product Datasheets

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References are publications that support the products' biological activity.

Sun et al (1995) Ras CAAX peptidomimetic FTI 276 selectively blocks tumour growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion. Cancer Res. 55 4243 PMID: 7671229

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

Lerner et al (1995) Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem. 10 26770 PMID:

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Keywords: FTI 276, supplier, Ras, CAAX, peptidomimetic, inhibitors, inhibits, farnesyltransferase, FTase, geranylgeranyltransferase, GGTase, carcinoma, K-Ras, tumour, tumor, FTI276, Protein, Prenyltransferases, Post-translational, Modifications, Protein, Prenyltransferases, Tocris Bioscience

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