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FTI-277 hydrochloride

Chemical Structure : FTI-277 hydrochloride

CAS No.: 180977-34-8

FTI-277 hydrochloride (FTI 277)

Catalog No.: PC-44767Not For Human Use, Lab Use Only.

FTI-277 hydrochloride is a peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM.

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Biological Activity

FTI-277 hydrochloride is a peptide mimetic of the C-terminal Cys-Val-Ile-Met of K-Ras4B that potently inhibits FTase (Farnesyltransferase) with IC50 of 0.5 nM.
FTI-277 hydrochloride highly selective for FTase over GGTase I (IC50 = 50 nM).
FTI-277 hydrochloride extremely potent (IC50=100 nM) at inhibiting H-Ras in whole cells.
FTI-277 hydrochloride blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm.

Physicochemical Properties

M.Wt 484.0749
Formula C22H30ClN3O3S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 4.7 mg/mL

Chemical Name/SMILES

L-Methionine, N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester, monohydrochloride (9CI)

References

1. Lerner EC, et al. J Biol Chem. 1995 Nov 10;270(45):26802-6.

2. Bernhard EJ, et al. Cancer Res. 1996 Apr 15;56(8):1727-30.

3. Bolick SC, et al. Leukemia. 2003 Feb;17(2):451-7.

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