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65886-71-7
  • names:

    4-amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one

  • CAS号:

    65886-71-7

    MDL Number:
  • MF(分子式): C8H12N4O5 MW(分子量): 244.20468
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Fazarabine
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中文别名 Fazarabine
英文别名 CCRIS 93; CCRIS-93; CCRIS93; NSC 281272; NSC-281272; NSC281272; Fazarabine. AraAC; Kymarabine
CAS号 65886-71-7
Inchi InChI=1S/C8H12N4O5/c9-7-10-2-12(8(16)11-7)6-5(15)4(14)3(1-13)17-6/h2-6,13-15H,1H2,(H2,9,11,16)/t3-,4-,5+,6-/m1/s1
InchiKey NMUSYJAQQFHJEW-ARQDHWQXSA-N
分子式 Formula C8H12N4O5
分子量 Molecular Weight 244.20468
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 Fazarabine(CAS:65886-71-7):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionFazarabine, also known as Kymarabine, is an orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug.
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[1]Wilhelm M, O'Brien S, Rios MB, Estey E, Keating MJ, Plunkett W, Sorenson M, Kantarjian HM. Phase I study of arabinosyl-5-azacytidine (fazarabine) in adult acute leukemia and chronic myelogenous leukemia in blastic phase. Leuk Lymphoma. 1999 Aug;34(5-6):511-8. PubMed PMID: 10492074.
[2]Goldberg RM, Reid JM, Ames MM, Sloan JA, Rubin J, Erlichman C, Kuffel MJ, Fitch TR. Phase I and pharmacological trial of fazarabine (Ara-AC) with granulocyte colony-stimulating factor. Clin Cancer Res. 1997 Dec;3(12 Pt 1):2363-70. PubMed PMID: 9815635.
[3] Barchi JJ Jr, Cooney DA, Ahluwalia GS, Gharehbaghi K, Covey JM, Hochman I, Paull KD, Jayaram HN. Studies on the mechanism of action of 1-beta-D-arabinofuranosyl-5-azacytosine (fazarabine) in mammalian lymphoblasts. J Exp Ther Oncol. 1996 May;1(3):191-203. PubMed PMID: 9414404.
[4] Manetta A, Blessing JA, Mann WJ, Smith DM. A phase II study of fazarabine (NSC 281272) in patients with advanced squamous cell carcinoma of the cervix. A Gynecologic Oncology Group study. Am J Clin Oncol. 1995 Oct;18(5):439-40. PubMed PMID: 7572764.
[5] Manetta A, Blessing JA, Look KY. A phase II study of fazarabine in patients with advanced ovarian cancer. A Gynecologic Oncology Group study. Am J Clin Oncol. 1995 Apr;18(2):156-7. PubMed PMID: 7534978.
6: Williamson SK, Crowley JJ, Livingston RB, Panella TJ, Goodwin JW. Phase II trial and cost analysis of fazarabine in advanced non-small cell carcinoma of the lung: a Southwest Oncology Group study. Invest New Drugs. 1995;13(1):67-71. PubMed PMID: 7499111.7: Selby GB, Upchurch C, Townsend J, Eyre HJ. A phase II evaluation of fazarabine in high-grade gliomas: a Southwest Oncology Group study. Cancer Chemother Pharmacol. 1994;34(2):179-80. PubMed PMID: 7514963.8: Bernstein ML, Whitehead VM, Grier H, Dubowy R, Land V, Devine S, Murphy S, Kung F. A phase I trial of fazarabine in refractory pediatric solid tumors. A Pediatric Oncology Group study. Invest New Drugs. 1993 Nov;11(4):309-12. PubMed PMID: 7512539.9: Heideman RL, McCully C, Balis FM, Poplack DG. Cerebrospinal fluid pharmacokinetics and toxicology of intraventricular and intrathecal arabinosyl-5-azacytosine (fazarabine, NSC 281272) in the nonhuman primate. Invest New Drugs. 1993 May-Aug;11(2-3):135-40. PubMed PMID: 7505267.10: Ben-Baruch N, Denicoff AM, Goldspiel BR, O'Shaughnessy JA, Cowan KH. Phase II study of fazarabine (NSC 281272) in patients with metastatic colon cancer. Invest New Drugs. 1993 Feb;11(1):71-4. PubMed PMID: 7688714.
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