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119644-22-3
  • names:

    5-chloro-1-((2R,4S,5R)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione

  • CAS号:

    119644-22-3

    MDL Number:
  • MF(分子式): C9H10ClFN2O4 MW(分子量): 264.6374
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Raluridine
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中文别名 5-chloro-1-((2R,4S,5R)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione
英文别名 Raluridine; 935U-83; BW-935U-83; FCU; FddClUrd; DRG-0215.
CAS号 119644-22-3
Inchi InChI=1S/C9H10ClFN2O4/c10-4-2-13(9(16)12-8(4)15)7-1-5(11)6(3-14)17-7/h2,5-7,14H,1,3H2,(H,12,15,16)/t5-,6+,7+/m0/s1
InchiKey WKVDSZYIGHLONN-RRKCRQDMSA-N
分子式 Formula C9H10ClFN2O4
分子量 Molecular Weight 264.6374
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 Raluridine(CAS:119644-22-3):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。
IntroductionRaluridine, also known as 935U-83; DRG-0215; BW-935U-83; FCU; FddClUrd, is a RNA-directed DNA polymerase inhibitor potentially for the treatment of HIV infection. 935U83 inhibited virus growth with an average 50% inhibitory concentration (IC50) of 1.8 microM; corresponding IC50s were 0.10 microM for FLT (3'-deoxy-3'-fluorothymidine) and 0.23, 0.49, and 0.03 microM for the approved agents AZT, ddI (2',3'-dideoxyinosine), and ddC (2',3'-dideoxycytosine), respectively.
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危险性警示
安全声明
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备注
[1]Riddler SA, Wang LH, Bartlett JA, Savina PM, Packard MV, McMahon DK, Blum MR, Dunn JA, Elkins MM, Mellors JW. Safety and pharmacokinetics of 5-chloro-2',3'-dideoxy-3'-fluorouridine (935U83) following oral administration of escalating single doses in human immunodeficiency virus-infected adults. Antimicrob Agents Chemother. 1996 Dec;40(12):2842-7. PubMed PMID: 9124852; PubMed Central PMCID: PMC163633.
[2]Dunn JA, Savina PM. Validation of a high-performance liquid chromatographic-mass spectrometric method for the measurement of 5-chloro-2',3'-dideoxy-3' -fluorouridine (935U83) in human plasma. J Chromatogr B Biomed Appl. 1996 Nov 15;686(2):241-8. PubMed PMID: 8971606.
[3] Sundseth R, Joyner SS, Moore JT, Dornsife RE, Dev IK. The anti-human immunodeficiency virus agent 3'-fluorothymidine induces DNA damage and apoptosis in human lymphoblastoid cells. Antimicrob Agents Chemother. 1996 Feb;40(2):331-5. PubMed PMID: 8834875; PubMed Central PMCID: PMC163111.
[4] Daluge SM, Purifoy DJ, Savina PM, St Clair MH, Parry NR, Dev IK, Novak P, Ayers KM, Reardon JE, Roberts GB, et al. 5-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile. Antimicrob Agents Chemother. 1994 Jul;38(7):1590-603. PubMed PMID: 7526782; PubMed Central PMCID: PMC284598.
[5] Van Aerschot A, Herdewijn P, Balzarini J, Pauwels R, De Clercq E. 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. J Med Chem. 1989 Aug;32(8):1743-9. PubMed PMID: 2754700.
6: Balzarini J, Van Aerschot A, Pauwels R, Baba M, Schols D, Herdewijn P, De Clercq E. 5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of human immunodeficiency virus (HIV): potent and selective anti-HIV activity of 3'-fluoro-2',3'-dideoxy-5-chlorouridine. Mol Pharmacol. 1989 May;35(5):571-7. PubMed PMID: 2725468.
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