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FTI 276

Cat No. 2406

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Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl ]methionine trifluoroacetate salt

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

Solubility:

Soluble to 10 mM in water

Purity:

>95 %

Storage:

Store at -80°C

CAS No:

[170006-72-1]

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

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

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. 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.

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Keywords: FTI 276, Ras, CAAX, peptidomimetic, inhibitor, farnesyltransferase, FTase, geranylgeranyltransferase, GGTase, carcinoma, K-Ras, tumour, tumor, FTI276