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344550 Sigma-Aldrich

FTI-276 - Calbiochem

A highly potent and selective CAAX peptidomimetic of the carboxyl terminal of Ras proteins that inhibits farnesyl transferase (FTase) in vitro (IC₅₀ = 500 pM).

Synonym: FTI-276 - Calbiochem, N-[2-phenyl-4-N[2(R)-amino-3-mercaptopropylamino benzoyl]-methionine, TFA

  • Empirical Formula (Hill Notation) C21H27N3O3S2

  • Molecular Weight 433.59

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Properties

Quality Level   100
assay   ≥90% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  desiccated
storage conditions   -20C
color   white
solubility   DMSO: 25 mg/mL
shipped in   ambient

Description

General description

A highly potent and selective CAAX peptidomimetic of the carboxyl terminal of Ras proteins that inhibits farnesyl transferase (FTase) in vitro (IC50 = 500 pM). Inhibits geranylgeranyltransferase I (GGTase I) at much higher concentration (IC50 = 50 nM). Has been shown to selectively block the growth of a human lung carcinoma expressing oncogenic K-Ras in nude mice. Also inhibits oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the Ras oncogene at 20 µM.

Packaging

250 μg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: no

Primary Target
FTase in vitro

Product does not compete with ATP.

Reversible: no

Target IC50: 500 pM against FTase in vitro

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.

Other Notes

Lantry, L.E., et al. 2000. Carcinogenesis21, 113.
Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26802.
Sun, J., et al. 1995. Cancer Res. 55, 4243.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety & Documentation

Safety Information

WGK Germany 
WGK 1
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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