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非西他滨_69123-90-6_产品详情
69123-90-6
  • names:

    Fiacitabine

  • CAS号:

    69123-90-6

    MDL Number: MFCD00868897
  • MF(分子式): C9H11FIN3O4 MW(分子量): 371.1
  • EINECS: Reaxys Number:
  • Pubchem ID:50312 Brand:BIOFOUNT
非西他滨
非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)是选择性HSV DNA复制抑制剂,对HSV1和HSV2的IC50分别为2.5 nM和12.6 nM。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
HCR201065-25mg 25mg 97% ¥ 1995.00 ¥ 1995.00 4-7周
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中文别名 非西他滨(69123-90-6);1-(2-氟-2-脱氧-β-D-阿拉伯呋喃糖基)-5-碘胞嘧啶;2'-脱氧-2'-氟-β-阿拉伯呋喃糖基-5-碘胞嘧啶;2'-氟-5-碘-1-β-D-阿拉伯呋喃糖基胞嘧啶;2'-氟-5-碘-阿拉伯胞嘧啶;2(1H)-嘧啶酮,4-氨基-1-(2-脱氧-2-氟-β-D-阿拉伯呋喃糖基)-5-碘-;FIAC;非卡他滨;盐酸菲西他滨;盐酸菲西他滨,2-(14)C标记;非西他滨(α-D)-异构体;
英文别名 Fiacitabine(69123-90-6); DRG-0077; DRG 0077; DRG0077; FIAC; FOAC; NSC 382097; NSC-382097; NSC382097; Fiacitabine; Fluoroiodoaracytidine. Fluorviodoaracytidine;1-(2-fluoro-2-deoxy-beta-D-arabinofuranosyl)-5-iodocytosine;2'-deoxy-2'-fluoro-beta-arabinofuranosyl-5-iodocytosine;2'-fluoro-5-iodo-1-beta-D-arabinofuranosylcytosine;2'-fluoro-5-iodo-aracytosine;2(1H)-pyrimidinone, 4-amino-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodo-;FIAC;fiacitabine;fiacitabine monohydrochloride;fiacitabine monohydrochloride, 2-(14)C-labeled;fiacitabine, (alpha-D)-isomer;
CAS号 69123-90-6
Inchi InChI=1S/C9H11FIN3O4/c10-5-6(16)4(2-15)18-8(5)14-1-3(11)7(12)13-9(14)17/h1,4-6,8,15-16H,2H2,(H2,12,13,17)/t4-,5+,6-,8-/m1/s1
InchiKey GIMSJJHKKXRFGV-BYPJNBLXSA-N
分子式 Formula C9H11FIN3O4
分子量 Molecular Weight 371.1
溶解度Solubility
性状 No data available
储藏条件 Storage conditions storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)毒理性质:
非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染
Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:非西他滨试剂,非西他滨杂质,非西他滨合成,非西他滨中间体,非西他滨密度,非西他滨溶解度,非西他滨旋光度,非西他滨闪点,非西他滨购买,
产品说明 非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)可以作为中间体及药物杂质使用,该产品非药用,非食用。
Introduction非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)only use for non-medical purposes in industrial or scientific research, and not for clinical diagnosis and treatment of humans or animals.
Application1Fiacitabine是一种嘧啶核苷类似物,对多种疱疹病毒具有活性。菲西他滨在体内转化为三磷酸形式,并抑制病毒DNA聚合酶.
Application2
Application3
非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)药理学:
1、Fiacitabine是一种嘧啶核苷类似物,对多种疱疹病毒具有活性。菲西他滨在体内转化为三磷酸形式,并抑制病毒DNA聚合酶.
2、抗病毒药 用于预防或治疗病毒性疾病的药物。它们可能发挥作用的方式包括通过抑制病毒DNA聚合酶来防止病毒复制。与特定的细胞表面受体结合并抑制病毒渗透或脱壳;抑制病毒蛋白质合成;或阻止病毒组装的后期。
3、抗肿瘤药 抑制或阻止NEOPLASMS增殖的物质。
4、Fiacitabine(NSC 382097; FIAC; FOAC)是选择性抑制单纯疱疹病毒(HSV)DNA复制的药物,HSV1和HSV2的IC50值分别为2.5 nM和12.6 nM。; IC50值:2.5 / 12.6 nM(HSV1 / 2);目标:HSVFIAC以0.0025至0.0126 microM的浓度抑制了1和2型单纯疱疹病毒各种菌株的复制,抑制了90%。细胞毒性是最小的,这是通过用锥虫蓝染料排除诺曼·维罗(Norman Vero),WI-38和NC-37细胞增殖确定的。在4天的试验中,50%的抑制剂量为4至10 microM。FIAC的活性浓度远低于阿拉伯糖基胞嘧啶,碘脱氧尿苷和阿拉伯糖基腺嘌呤。它对1型单纯疱疹病毒的活性略高于无环鸟苷,并且对正常细胞的毒性更高。
Allaudeen HS, et al. Selective inhibition of DNA replication in herpes simplex virus infected cells by 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine. J Biol Chem. 1982 Oct 25;257(20):1
Lopez C, et al. 2'-fluoro-5-iodo-aracytosine, a potent and selective anti-herpesvirus agent. Antimicrob Agents Chemother. 1980 May;17(5):803-6.
Therapeutic gene expression in transduced mesenchymal stem cells can be monitored using a reporter gene Nuclear medicine and biology22796395 2012-11-01
Evaluation of F-18-labeled 5-iodocytidine (18F-FIAC) as a new potential positron emission tomography probe for herpes simplex virus type 1 thymidine kinase imaging Nuclear medicine and biology21982570
Radiosynthesis of F-18 labeled cytidine analog 2'-fluoro-5-iodo-l-beta-d-arabinofuranosylcytosine ([(18)F]FIAC) Applied radiation and isotopes : including data, instrumentation and methods for use in

非西他滨(69123-90-6,Fiacitabine,NSC 382097,FIAC,FOAC)参考文献:
1.Recognition and treatment of shingles.
Nikkels AF1, Piérard GE. Drugs. 1994 Oct;48(4):528-48.

Varicella zoster virus (VZV) is responsible for a primary infection (varicella) followed by a latency, eventually resulting in herpes zoster (shingles). The replication cycle of VZV is normally interrupted after varicella. Consequently, VZV remains dormant in the organism. Reactivation occurs after viraemia, and the development of tissue alterations (skin and viscera) depends on the immunological status of the patient. Diagnosis of herpes zoster relies on clinical recognition and cytological and histological evaluations combined with immunohistochemistry and molecular biology techniques. Treatment of herpes zoster primarily relies upon antiviral drugs and incidentally on immunomodulating agents, specific immunoglobulins, antimicrobial agents, antiviral enzymes and corticosteroids. Drugs with a clinically relevant activity against varicella zoster virus infections include aciclovir, adenosine monophosphate, bromodeoxyuridine, desciclovir, fiacitabine, idoxuridine, interferon-alpha and vidarabine.

2.Particular characteristics of the anti-human cytomegalovirus activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC) in vitro.
Neyts J1, Snoeck R, Balzarini J, De Clercq E. Antiviral Res. 1991 Jul;16(1):41-52.

The acyclic nucleoside phosphonate analogue (S)-1-[3-hydroxy-2-phosphonylmethoxypropyl]cytosine (HPMPC) is a potent and selective inhibitor of human cytomegalovirus (HCMV) replication and DNA synthesis. Unlike 9-(1,3-dihydroxy-2-propoxymethyl)guanine (DHPG), HPMPC inhibits HCMV replication in cell cultures which have been treated with the compound before infection. Upon short-pulse treatment of HCMV-infected cells with HPMPC, a long-lasting antiviral response is obtained. The antiviral activity of HPMPC, unlike the antiviral activity of other cytosine derivatives (i.e. Ara-C, FIAC), is not readily reversed by 2'-deoxycytidine or cytidine. Neutral and alkaline sucrose gradient analysis of HCMV DNA isolated from HPMPC-treated HCMV-infected cell cultures revealed that HPMPC does not cause (detectable) single- or double-strand breakage of HCMV DNA.

3.Radiosynthesis of F-18 labeled cytidine analog 2'-fluoro-5-iodo-l-beta-d-arabinofuranosylcytosine ([(18)F]FIAC).
Wu CY1, Chan PC, Chang WT, Liu RS, Alauddin MM, Wang HE. Appl Radiat Isot. 2009 Jul-Aug;67(7-8):1362-5. doi: 10.1016/j.apradiso.2009.02.083. Epub 2009 Feb 28.

We reported the synthesis of 2'-deoxy-2'-[(18)F]fluoro-5-iodo-1-beta-d-arabinofuranosyl-5-iodo-cytosine ([(18)F]FIAC) with 15-20% radiochemical yield (decay corrected) in 3.5h. 2-deoxy-2-[(18)F]fluoro-1,3,5-tri-O-benzoyl-alpha-d-arabinofuranose was prepared following literature procedures with some modifications (yield>70%). The (18)F-fluorosugar was converted to 1-bromo-(18)F-fluorosugar, and then coupled with 5-iodocytocine silyl ether. A mixture of acetonitrile (ACN) and 1,2-dichloroethane (DCE) were employed to achieve optimum radiochemical yield and acceptable beta-anomer selectivity (alpha/beta=1/3). After hydrolyzed with sodium methoxide, the crude product was purified using HPLC to afford the beta-[(18)F]FIAC with high radiochemical purity (>or=98%).

4.Therapeutic gene expression in transduced mesenchymal stem cells can be monitored using a reporter gene.
Zhang G1, Lan X, Yen TC, Chen Q, Pei Z, Qin C, Zhang Y. Nucl Med Biol. 2012 Nov;39(8):1243-50. doi: 10.1016/j.nucmedbio.2012.06.010. Epub 2012 Jul 15.

AIM: We constructed a recombinant adenovirus construct Ad5-sr39tk-IRES-VEGF(165) (Ad5-SIV) that contained a mutant herpes viral thymidine kinase reporter gene (HSV1-sr39tk) and the human vascular endothelial growth factor 165 (VEGF(165)) gene for noninvasive imaging of gene expression. The recombinant adenovirus Ad5-SIV was transfected into rat bone marrow-derived mesenchymal stem cells (MSCs), and we measured the expression of HSV1-sr39tk and VEGF(165) to evaluate the feasibility of monitoring VEGF(165) expression using reporter gene expression.


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