GS-9219 - CAS 859209-74-8
Catalog number: 859209-74-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
GS-9219 is a prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations.
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GS 9219; GS-9219; GS9219.
Current Developer:
Gilead Sciences
1.Targeting DNA repair in chronic lymphocytic leukemia cells with a novel acyclic nucleotide analogue, GS-9219.
Tsai CY1, Ray AS, Tumas DB, Keating MJ, Reiser H, Plunkett W. Clin Cancer Res. 2009 Jun 1;15(11):3760-9. doi: 10.1158/1078-0432.CCR-08-2848. Epub 2009 May 12.
PURPOSE: GS-9219 is a cell-permeable prodrug of the acyclic nucleotide analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG); the incorporation of the active metabolite PMEG diphosphate (PMEGpp) into DNA results in DNA chain termination due to the lack of a 3'-hydroxyl moiety. We hypothesized that the incorporation of PMEGpp into DNA during repair resynthesis would result in the inhibition of DNA repair and the accumulation of DNA breaks in chronic lymphocytic leukemia (CLL) cells that would activate signaling pathways to cell death.
2.Mutations in adenosine deaminase-like (ADAL) protein confer resistance to the antiproliferative agents N6-cyclopropyl-PMEDAP and GS-9219.
Frey CR1, Andrei G, Votruba I, Cannizzaro C, Han B, Fung W, Hung M, Liu X, Geleziunas R, Fiten P, Opdenakker G, Snoeck R, Cihlar T. Anticancer Res. 2013 May;33(5):1899-912.
BACKGROUND/AIM: GS 9219 is a double prodrug of antiproliferative nucleotide analog 9-(2-Phosphonylmethoxyethyl)guanine (PMEG), with potent in vivo efficacy against various hematological malignancies. This study investigates the role of adenosine deaminase-like (ADAL) protein in the intracellular activation of GS-9219.
3.GS-9219/VDC-1101--a prodrug of the acyclic nucleotide PMEG has antitumor activity in spontaneous canine multiple myeloma.
Thamm DH1, Vail DM, Kurzman ID, Babusis D, Ray AS, Sousa-Powers N, Tumas DB. BMC Vet Res. 2014 Jan 25;10:30. doi: 10.1186/1746-6148-10-30.
BACKGROUND: Multiple myeloma (MM) is an important human and canine cancer for which novel therapies remain necessary. VDC-1101 (formerly GS-9219), a novel double prodrug of the anti-proliferative nucleotide analog 9-(2-phosphonylmethoxyethyl) guanine (PMEG), possesses potent cytotoxic activity in vitro in human lymphoblasts and leukemia cell lines and in vivo in spontaneous canine lymphoma. Given the similarity in lineage between lymphoma and MM, we hypothesized that VDC-1101 would be active against MM.
4.Assessment of GS-9219 in a pet dog model of non-Hodgkin's lymphoma.
Vail DM1, Thamm DH, Reiser H, Ray AS, Wolfgang GH, Watkins WJ, Babusis D, Henne IN, Hawkins MJ, Kurzman ID, Jeraj R, Vanderhoek M, Plaza S, Anderson C, Wessel MA, Robat C, Lawrence J, Tumas DB. Clin Cancer Res. 2009 May 15;15(10):3503-10. doi: 10.1158/1078-0432.CCR-08-3113. Epub 2009 May 5.
PURPOSE: To assess, in dogs with naturally occurring non-Hodgkin's lymphoma, pharmacokinetics, safety, and activity of GS-9219, a prodrug of the nucleotide analogue 9-(2-phosphonylmethoxyethyl) guanine (PMEG), which delivers PMEG and its phosphorylated metabolites to lymphoid cells with preferential cytotoxicity in cells with a high proliferation index such as lymphoid malignancies.
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CAS 859209-74-8 GS-9219

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