For research use only. Not for therapeutic Use.
Sapacitabine is an orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity. Sapacitabine is hydrolyzed by amidases to the deoxycytosine analogue CNDAC (2/’-Cyano-2/’-deoxyarabinofuranosylcytosine), which is then phosphorylated into the active triphosphate form. As an analogue of deoxycytidine triphosphate, CNDAC triphosphate incorporates into DNA strands during replication, resulting in single-stranded DNA breaks during polymerization due to beta-elimination during the fidelity checkpoint process; cell cycle arrest in the G2 phase and apoptosis ensue. The unmetabolized prodrug may exhibit antineoplastic activity as well.
| Catalog Number | M094000 |
| CAS Number | 151823-14-2 |
| Molecular Formula | C26H42N4O5 |
| Purity | ≥95% |
| Target | Nucleoside Antimetabolite/Analog |
| Storage | Store at -20C |
| Reference | </br>1:HDAC Inhibition Induces MicroRNA-182, which Targets RAD51 and Impairs HR Repair to Sensitize Cells to Sapacitabine in Acute Myelogenous Leukemia. Lai TH, Ewald B, Zecevic A, Liu C, Sulda M, Papaioannou D, Garzon R, Blachly JS, Plunkett W, Sampath D.Clin Cancer Res. 2016 Jul 15;22(14):3537-49. doi: 10.1158/1078-0432.CCR-15-1063. Epub 2016 Feb 8. PMID: 26858310 </br>2:Sapacitabine in the treatment of acute myeloid leukemia. Norkin M, Richards AI.Expert Rev Anticancer Ther. 2015;15(11):1261-6. doi: 10.1586/14737140.2015.1102064. Epub 2015 Nov 2. PMID: 26523431 </br>3:A randomised comparison of the novel nucleoside analogue sapacitabine with low-dose cytarabine in older patients with acute myeloid leukaemia. Burnett AK, Russell N, Hills RK, Panoskaltsis N, Khwaja A, Hemmaway C, Cahalin P, Clark RE, Milligan D.Leukemia. 2015 Jun;29(6):1312-9. doi: 10.1038/leu.2015.38. Epub 2015 Feb 13. PMID: 25676423 </br>4:Profile of sapacitabine: potential for the treatment of newly diagnosed acute myeloid leukemia in elderly patients. Lim MY, Jamieson K.Clin Interv Aging. 2014 May 6;9:753-62. doi: 10.2147/CIA.S39558. eCollection 2014. Review. PMID: 24851045 Free PMC Article</br>5:Improvement of the antitumor activity of poorly soluble sapacitabine (CS-682) by using Soluplus® as a surfactant. Obata T, Suzuki Y, Ogawa N, Kurimoto I, Yamamoto H, Furuno T, Sasaki T, Tanaka M.Biol Pharm Bull. 2014;37(5):802-7. PMID: 24790002 Free Article</br>6:Oral sapacitabine for the treatment of acute myeloid leukaemia in elderly patients: a randomised phase 2 study. Kantarjian H, Faderl S, Garcia-Manero G, Luger S, Venugopal P, Maness L, Wetzler M, Coutre S, Stock W, Claxton D, Goldberg SL, Arellano M, Strickland SA, Seiter K, Schiller G, Jabbour E, Chiao J, Plunkett W.Lancet Oncol. 2012 Nov;13(11):1096-104. doi: 10.1016/S1470-2045(12)70436-9. Epub 2012 Oct 15. PMID: 23075701 Free PMC Article</br>7:Bone Marrow and Peripheral Blood AML Cells Are Highly Sensitive to CNDAC, the Active Form of Sapacitabine. Jagan S, Paganessi LA, Frank RR, Venugopal P, Larson M, Christopherson KW 2nd.Adv Hematol. 2012;2012:727683. doi: 10.1155/2012/727683. Epub 2012 Sep 23. PMID: 23049558 Free PMC Article</br>8:Sapacitabine, the prodrug of CNDAC, is a nucleoside analog with a unique action mechanism of inducing DNA strand breaks. Liu XJ, Nowak B, Wang YQ, Plunkett W.Chin J Cancer. 2012 Aug;31(8):373-80. doi: 10.5732/cjc.012.10077. Epub 2012 Jun 26. PMID: 22739266 Free PMC Article</br>9:Nucleoside and nucleobase analogs in cancer treatment: not only sapacitabine, but also gemcitabine. Muggia F, Diaz I, Peters GJ.Expert Opin Investig Drugs. 2012 Apr;21(4):403-8. doi: 10.1517/13543784.2012.666236. Epub 2012 Mar 9. PMID: 22404148 </br>10:Sapacitabine for cancer. Liu X, Kantarjian H, Plunkett W.Expert Opin Investig Drugs. 2012 Apr;21(4):541-55. doi: 10.1517/13543784.2012.660249. Epub 2012 Feb 14. Review. PMID: 22329458 Free PMC Article |
