344550

FTI-276

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(s): FTI-276, N-[2-phenyl-4-N[2(R)-amino-3-mercaptopropylamino benzoyl]-methionine, TFA
• Empirical Formula (Hill Notation): C₂₁H₂₇N₃O₃S₂
• Molecular Weight: 433.59
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥90% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• color: white
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: −20°C

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.

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 Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable