CGC-11047
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.
1: Dredge K, Kink JA, Johnson RM, Bytheway I, Marton LJ. The polyamine analog PG11047 potentiates the antitumor activity of cisplatin and bevacizumab in preclinical models of lung and prostate cancer. Cancer Chemother Pharmacol. 2009 Dec;65(1):191-5. doi: 10.1007/s00280-009-1105-7. Epub 2009 Aug 15. PubMed PMID: 19685053.
2: Hacker A, Marton LJ, Sobolewski M, Casero RA Jr. In vitro and in vivo effects of the conformationally restricted polyamine analogue CGC-11047 on small cell and non-small cell lung cancer cells. Cancer Chemother Pharmacol. 2008 Dec;63(1):45-53. doi: 10.1007/s00280-008-0706-x. Epub 2008 Feb 27. PubMed PMID: 18301893.
3: Mitchell JL, Thane TK, Sequeira JM, Marton LJ, Thokala R. Antizyme and antizyme inhibitor activities influence cellular responses to polyamine analogs. Amino Acids. 2007 Aug;33(2):291-7. Epub 2007 Apr 6. PubMed PMID: 17410332.
4: Lima e Silva R, Kachi S, Akiyama H, Shen J, Hatara MC, Aslam S, Gong YY, Khu NH, Lauer TW, Hackett SF, Marton LJ, Campochiaro PA. Trans-scleral delivery of polyamine analogs for ocular neovascularization. Exp Eye Res. 2006 Nov;83(5):1260-7. Epub 2006 Sep 6. PubMed PMID: 16950258.
5: Loussouarn G, Marton LJ, Nichols CG. Molecular basis of inward rectification: structural features of the blocker defined by extended polyamine analogs. Mol Pharmacol. 2005 Aug;68(2):298-304. Epub 2005 May 4. PubMed PMID: 15872118.
2: Hacker A, Marton LJ, Sobolewski M, Casero RA Jr. In vitro and in vivo effects of the conformationally restricted polyamine analogue CGC-11047 on small cell and non-small cell lung cancer cells. Cancer Chemother Pharmacol. 2008 Dec;63(1):45-53. doi: 10.1007/s00280-008-0706-x. Epub 2008 Feb 27. PubMed PMID: 18301893.
3: Mitchell JL, Thane TK, Sequeira JM, Marton LJ, Thokala R. Antizyme and antizyme inhibitor activities influence cellular responses to polyamine analogs. Amino Acids. 2007 Aug;33(2):291-7. Epub 2007 Apr 6. PubMed PMID: 17410332.
4: Lima e Silva R, Kachi S, Akiyama H, Shen J, Hatara MC, Aslam S, Gong YY, Khu NH, Lauer TW, Hackett SF, Marton LJ, Campochiaro PA. Trans-scleral delivery of polyamine analogs for ocular neovascularization. Exp Eye Res. 2006 Nov;83(5):1260-7. Epub 2006 Sep 6. PubMed PMID: 16950258.
5: Loussouarn G, Marton LJ, Nichols CG. Molecular basis of inward rectification: structural features of the blocker defined by extended polyamine analogs. Mol Pharmacol. 2005 Aug;68(2):298-304. Epub 2005 May 4. PubMed PMID: 15872118.
| Chemical | |
|---|---|
| CAS Num | 206991-64-2 |
| Chemical Formula | C14H36Cl4N4 |
| Molecular Weight | 402.27444 |
| IUPAC Chemical Name | (Z)-N1,N1'-(but-2-ene-1,4-diyl)bis(N3-ethylpropane-1,3-diamine) tetrahydrochloride |
| Exact Mass | 256.2627 |
| Elemental Analysis | C, 41.80; H, 9.02; Cl, 35.25; N, 13.93 |
| Synonym | CGC 11047; CGC-11047; CGC11047; SL 11047; SL11047; SL-11047; SL 47; PG11047. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | CCNCCCNC/C=C\CNCCCNCC.[H]Cl.[H]Cl.[H]Cl.[H]Cl |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >5 years if stored properly |
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