Imetelstat - CAS 868169-64-6
Catalog number:
868169-64-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
Imetelstat sodium, the sodium salt of imetelstat, is a telomerase inhibitor, also 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.
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Synonyms:
Imetelstat, GRN163L.
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Current Developer:
Geron.
1.Telomerase Inhibitor Imetelstat in Patients with Essential Thrombocythemia.
Baerlocher GM1, Oppliger Leibundgut E, Ottmann OG, Spitzer G, Odenike O, McDevitt MA, Röth A, Daskalakis M, Burington B, Stuart M, Snyder DS. N Engl J Med. 2015 Sep 3;373(10):920-8. doi: 10.1056/NEJMoa1503479.
BACKGROUND: Imetelstat, a 13-mer oligonucleotide that is covalently modified with lipid extensions, competitively inhibits telomerase enzymatic activity. It has been shown to inhibit megakaryocytic proliferation in vitro in cells obtained from patients with essential thrombocythemia. In this phase 2 study, we investigated whether imetelstat could elicit hematologic and molecular responses in patients with essential thrombocythemia who had not had a response to or who had had unacceptable side effects from prior therapies.
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CAS 868169-64-6 Imetelstat

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