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
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About This Item
Empirical Formula (Hill Notation):
C21H27N3O3S2
Molecular Weight:
433.59
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
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
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.
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
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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