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).
别名:
FTI-276, N-[2-phenyl-4-N[2(R)-amino-3-mercaptopropylamino benzoyl]-methionine, TFA
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
Quality Level
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
FTase in vitro
Product does not compete with ATP.
Reversible: no
Target IC50: 500 pM against FTase in vitro
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
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.
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
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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