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Archive for March, 2011

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     Acivicin (LKT Cat#: A0934) is a potent anti-cancer agent originally isolated from Streptomyces sviceus.  This heterocyclic analog of L-glutamate is a potential therapeutic in the treatment of a variety of carcinomas, melanomas and leukemia.

 

      Cancer cells, like those in leukemia, have elevated levels of glutamine amidotransferases to help supply the rapidly dividing cells with essential amino acids.  Acivicin irreversibly inhibits the amidotransferase precursors from transforming to the active enzyme.  It accomplishes this through nucleophillic displacement and subsequent trapping of a critical threonine residue in glutamine amidotransferase.

 

     This acivicin mediated inactivation of the enzyme deprives the cancer cells of its supply of essential amino acids and leads to cell death.

 

Specifications

Cas No.
42228-92-2
Product ID
A0934
Product Name
Acivicin
Chemical Name
(2S)-2-amino-2-[(5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl]acetic acid
Synonym
a-Amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid; ACIA
Formula Wt.
178.57
Melting Point
209oC-211oC
Purity
98%
Solubility
Soluble in water. Slightly soluble in methanol, ethanol or chloroform.
Store Temp
-20oC
References
Griffith, O.W. et al. Proc. Natl. Acad. Sci. USA 77:3384 (1980). Earhart, R.H., et al. Adv. Enzyme Regulation. 24:179 (1986). Mukherjee, T. et al. Biochem. Biophys. Res. Commun. 170:426(1982). Graber, R., Losa, G.A. Int. J. Cancer. 62:443-8 (1995).

 


March 9th, 2011
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