Imetelstat - MedKoo Biosciences

Back to products

Browse products

Approved anticancer agents

Anticancer agents in trials

Anticancer agents in preclinical trials

Anticancer molecular libraries

Other drug agents

Drug intermediates

Bio-reagents and biochemicals

MedKoo product information:

Imetelstat

MedKoo Code#: 205489

Name: Imetelstat

CAS#: 868169-64-6

Synonym: Imetelstat, GRN163L.

　

IUPAC/Chemical name:

3'-amino-3'-deoxy-P-thiothymidylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioadenylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioguanylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioguanylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioguanylyl-(3'→5')-3'-amino-3'-deoxy-P-thiothymidylyl-(3'→5')-3'-amino-3'-deoxy-P-thiothymidylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioadenylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioguanylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioadenylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thiocytidylyl-(3'→5')-3'-amino-2',3'-dideoxy-P-thioadenylyl-(3'→5')-3'-amino-2',3'-dideoxyadenosine 5'-{O-[2-hydroxy-3-(hexadecanoylamino)propyl] hydrogen phosphorothioate.

Chemical structure:

Theoretical analysis:

C₁₄₈H₂₁₁N₆₈O₅₃P₁₃S₁₃

Availability and price:

This agent is not in stock, which may be available through custom synthesis.

To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

Information about this agent

Imetelstat sodium is the sodium salt of imetelstat, a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a "telomerase template antagonist"), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer: Geron.

References

1: Tokcaer-Keskin Z, Dikmen ZG, Ayaloglu-Butun F, Gultekin S, Gryaznov SM, Akcali KC. The effect of telomerase template antagonist GRN163L on bone-marrow-derived rat mesenchymal stem cells is reversible and associated with altered expression of cyclin d1, cdk4 and cdk6. Stem Cell Rev. 2010 Jun;6(2):224-33. PubMed PMID: 20180048.

2: Röth A, Harley CB, Baerlocher GM. Imetelstat (GRN163L)--telomerase-based cancer therapy. Recent Results Cancer Res. 2010;184:221-34. Review. PubMed PMID: 20072842.

3: Goldblatt EM, Gentry ER, Fox MJ, Gryaznov SM, Shen C, Herbert BS. The telomerase template antagonist GRN163L alters MDA-MB-231 breast cancer cell morphology, inhibits growth, and augments the effects of paclitaxel. Mol Cancer Ther. 2009 Jul;8(7):2027-35. Epub 2009 Jun 9. PubMed PMID: 19509275.

4: Shammas MA, Koley H, Bertheau RC, Neri P, Fulciniti M, Tassone P, Blotta S, Protopopov A, Mitsiades C, Batchu RB, Anderson KC, Chin A, Gryaznov S, Munshi NC. Telomerase inhibitor GRN163L inhibits myeloma cell growth in vitro and in vivo. Leukemia. 2008 Jul;22(7):1410-8. Epub 2008 May 1. PubMed PMID: 18449204; PubMed Central PMCID: PMC3155939.

5: Gryaznov SM, Jackson S, Dikmen G, Harley C, Herbert BS, Wright WE, Shay JW. Oligonucleotide conjugate GRN163L targeting human telomerase as potential anticancer and antimetastatic agent. Nucleosides Nucleotides Nucleic Acids. 2007;26(10-12):1577-9. PubMed PMID: 18066830.

6: Jackson SR, Zhu CH, Paulson V, Watkins L, Dikmen ZG, Gryaznov SM, Wright WE, Shay JW. Antiadhesive effects of GRN163L--an oligonucleotide N3'->P5' thio-phosphoramidate targeting telomerase. Cancer Res. 2007 Feb 1;67(3):1121-9. PubMed PMID: 17283146.

7: Gomez-Millan J, Goldblatt EM, Gryaznov SM, Mendonca MS, Herbert BS. Specific telomere dysfunction induced by GRN163L increases radiation sensitivity in breast cancer cells. Int J Radiat Oncol Biol Phys. 2007 Mar 1;67(3):897-905. Epub 2006 Dec 15. PubMed PMID: 17175117.

8: Hochreiter AE, Xiao H, Goldblatt EM, Gryaznov SM, Miller KD, Badve S, Sledge GW, Herbert BS. Telomerase template antagonist GRN163L disrupts telomere maintenance, tumor growth, and metastasis of breast cancer. Clin Cancer Res. 2006 May 15;12(10):3184-92. PubMed PMID: 16707619.

9: Gellert GC, Dikmen ZG, Wright WE, Gryaznov S, Shay JW. Effects of a novel telomerase inhibitor, GRN163L, in human breast cancer. Breast Cancer Res Treat. 2006 Mar;96(1):73-81. Epub 2005 Dec 1. PubMed PMID: 16319992.

10: Dikmen ZG, Gellert GC, Jackson S, Gryaznov S, Tressler R, Dogan P, Wright WE, Shay JW. In vivo inhibition of lung cancer by GRN163L: a novel human telomerase inhibitor. Cancer Res. 2005 Sep 1;65(17):7866-73. PubMed PMID: 16140956.

11: Djojosubroto MW, Chin AC, Go N, Schaetzlein S, Manns MP, Gryaznov S, Harley CB, Rudolph KL. Telomerase antagonists GRN163 and GRN163L inhibit tumor growth and increase chemosensitivity of human hepatoma. Hepatology. 2005 Nov;42(5):1127-36. PubMed PMID: 16114043.

Contact MedKoo:

Email: sales@medkoo.com

(Keyword; CAS#; MedKoo code#)