CGC-11047 - CAS 206991-64-2
Catalog number: 206991-64-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
CGC-11047 is a second generation polyamine analogue, synthesized through the restriction of molecular conformations of parent polyamine compounds, with potential antineoplastic activity. Polyamine analogue PG11047 may displace endogenous polyamines from DNA binding sites, thereby interfering with cell cycle processes dependent upon polyamine binding and function, and resulting in cell-cycle arrest, induction of apoptosis, depletion of polyamines, and interference with gene and ligand-receptor activities involved with cell growth. This agent may exhibit decreased toxicity and enhanced cytotoxicity profiles compared to first-generation polyamine compounds. In tumor cells, there is an increase dependence on polyamines as well as a dysregulated polyamine metabolic pathway resulting in abnormal or sustained tumor growth.
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Synonyms:
CGC 11047; SL 11047; SL 47; CGC-11047; PG11047; SL-11047; 2-
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Current Developer:
Progen Pharmaceuticals Limited
1.In vitro and in vivo effects of the conformationally restricted polyamine analogue CGC-11047 on small cell and non-small cell lung cancer cells.
Hacker A1, Marton LJ, Sobolewski M, Casero RA Jr. Cancer Chemother Pharmacol. 2008 Dec;63(1):45-53. doi: 10.1007/s00280-008-0706-x. Epub 2008 Feb 27.
PURPOSE: Polyamines are essential for normal growth; however, the requirement for, and the metabolism of, polyamines are frequently dysregulated in cancer. Polyamine analogues have demonstrated promising preclinical results in multiple model systems of cancer, but their clinical utility has been limited by apparent toxicity. A representative compound of a new generation of short chain, conformationally restricted polyamine analogues, CGC-11047 has been synthesized and ongoing phase I clinical trials indicate it to be well tolerated at weekly doses of 610 mg (dose escalation is still in progress). Therefore, studies were designed to gain a better understanding of its effects on cellular polyamine biochemistry and efficacy in the treatment of human lung cancer models in vitro and in vivo.
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CAS 206991-64-2 CGC-11047

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