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).

• Synonyme(s) : FTI-276, N-[2-phenyl-4-N[2(R)-amino-3-mercaptopropylamino benzoyl]-methionine, TFA
• Formule empirique (notation de Hill) : C₂₁H₂₇N₃O₃S₂
• Poids moléculaire : 433.59
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥90% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic)
• Couleur: white
• Solubilité: DMSO: 25 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
FTase in vitro

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 500 pM against FTase in vitro

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Forme physique

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.

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable