2'-Deoxy-2'-fluorocytidine
(Synonyms: 2'-脱氧-2-氟胞苷) 目录号 : GC61756
2'-Deoxy-2'-fluorocytidine是一种核苷类似物，是刚果出血热病毒(CCHFV)复制的有效抑制剂。2'-Deoxy-2'-fluorocytidine可与T705协同作用，增强两种化合物对CCHFV复制的抗病毒效力。
Cas No.:10212-20-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
2'-Deoxy-2'-fluorocytidine, an nucleoside analog, is a potent inhibitor of Crimean-Congo hemorrhagic fever virus (CCHFV) replication. 2′-deoxy-2′-fluorocytidine can act synergistically with T705 to increase the potency of both compounds antiviral effects on CCHFV replication[1].
2'-Deoxy-2'-fluorocytidine has antiviral activities, showing 50% effective concentrations (EC50) of 61 nM and 31 nM against CCHFV and CCHFV/ZsG in Huh7 cells, respectively. And it shows a 50% cytotoxicity concentration (CC50) of >50.0 μM in Huh7 cells[1].
[1]. Stephen R Welch, et al. Identification of 2'-deoxy-2'-fluorocytidine as a potent inhibitor of Crimean-Congo hemorrhagic fever virus replication using a recombinant fluorescent reporter virus. Antiviral Res. 2017 Nov;147:91-99.
| Cas No. | 10212-20-1 | SDF | |
| 别名 | 2'-脱氧-2-氟胞苷 | ||
| Canonical SMILES | F[C@H]1[C@@](N2C(N=C(C=C2)N)=O)([H])O[C@@H]([C@H]1O)CO | ||
| 分子式 | C9H12FN3O4 | 分子量 | 245.21 |
| 溶解度 | Water: 5 mg/mL (20.39 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.0781 mL | 20.3907 mL | 40.7814 mL |
| 5 mM | 0.8156 mL | 4.0781 mL | 8.1563 mL |
| 10 mM | 0.4078 mL | 2.0391 mL | 4.0781 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Different Mechanisms of DNA Radiosensitization by 8-Bromoadenosine and 2'-Deoxy-2'-fluorocytidine Observed on DNA Origami Nanoframe Supports
J Phys Chem Lett 2022 May 5;13(17):3922-3928.PMID:PMC9083549DOI:10.1021/acs.jpclett.2c00584.
DNA origami nanoframes with two parallel DNA sequences are used to evaluate the effect of nucleoside substituents on radiation-induced DNA damage. Double strand breaks (DSB) of DNA are counted using atomic force microscopy (AFM), and total number of lesions is evaluated using real-time polymerase chain reaction (RT-PCR). Enhanced AT or GC content does not increase the number of DNA strand breaks. Incorporation of 8-bromoadenosine results in the highest enhancement in total number of lesions; however, the highest enhancement in DSB is observed for 2'-Deoxy-2'-fluorocytidine, indicating different mechanisms of radiosensitization by nucleoside analogues with the halogen substituent on base or sugar moieties, respectively. "Bystander" effects are observed, when the number of DSB in a sequence is enhanced by a substituent in the parallel DNA sequence. The present approach eliminates limitations of previously developed methods and motivates detailed studies of poorly understood conformation or bystander effects in radiation induced damage to DNA.
Identification of 2'-Deoxy-2'-fluorocytidine as a potent inhibitor of Crimean-Congo hemorrhagic fever virus replication using a recombinant fluorescent reporter virus
Antiviral Res 2017 Nov;147:91-99.PMID:29024765DOI:10.1016/j.antiviral.2017.10.008.
Crimean-Congo hemorrhagic fever virus (CCHFV), a tick-borne orthonairovirus, causes a severe hemorrhagic disease in humans (Crimean-Congo hemorrhagic fever, CCHF). Currently, no vaccines are approved to prevent CCHF; treatment is limited to supportive care and the use of ribavirin, the therapeutic benefits of which remain unclear. CCHF is part of WHO's priority list of infectious diseases warranting further research and development. To aid in the identification of new antiviral compounds, we generated a recombinant CCHFV expressing a reporter protein, allowing us to quantify virus inhibition by measuring the reduction in fluorescence in infected cells treated with candidate compounds. The screening assay was readily adaptable to high-throughput screening (HTS) of compounds using Huh7 cells, with a signal-to-noise ratio of 50:1, and Z'-factors > 0.6 in both 96- and 384-well formats. A screen of candidate nucleoside analog compounds identified 2'-Deoxy-2'-fluorocytidine (EC50 = 61 ± 18 nM) as having 200 × the potency of ribavirin (EC50 = 12.5 ± 2.6 μM), as well as 17 × the potency of T-705 (favipiravir), another compound with reported anti-CCHFV activity (EC50 = 1.03 ± 0.16 μM). Furthermore, we also determined that 2'-Deoxy-2'-fluorocytidine acts synergistically with T-705 to inhibit CCHFV replication without causing cytotoxicity. The incorporation of this reporter virus into the high-throughput screening assay described here will allow more rapid identification of effective therapeutic options to combat this emerging human pathogen.
Inhibition of the subgenomic hepatitis C virus replicon in huh-7 cells by 2'-Deoxy-2'-fluorocytidine
Antimicrob Agents Chemother 2004 Feb;48(2):651-4.PMID:14742230DOI:10.1128/AAC.48.2.651-654.2004.
2'-Deoxy-2'-fluorocytidine (FdC) is a potent inhibitor of the hepatitis C virus RNA replicon in culture, and FdC-5'-triphosphate is an effective inhibitor of the NS5B polymerase. Dynamic profiling of cell growth in an antiviral assay showed that FdC caused cytostasis due to an S-phase arrest. These observations demonstrate that FdC treatment is affecting both a viral target and a cellular target.
The use of oligonucleotide probes containing 2'-deoxy-2'-fluoronucleosides for regiospecific cleavage of RNA by RNase H from Escherichia coli
Biochim Biophys Acta 1992 Feb 28;1130(1):41-6.PMID:1371935DOI:10.1016/0167-4781(92)90459-d.
Protected 2'-deoxy-2'-fluorouridine and 2'-Deoxy-2'-fluorocytidine suitable for incorporation into oligonucleotides via the phosphoramidite approach have been prepared. Five modified and two unmodified oligonucleotides have been synthesized to investigate the regiospecific cleavage of a 5S RNA from Escherichia coli by RNase H. In order to show whether the modified oligonucleotides are able to hybridize with the RNA the physico-chemical properties (melting curves, CD spectra) of analogous DNA/oligodeoxyribonucleotide duplexes have been examined. The modified oligonucleotides are shown to form stable duplexes with a DNA-matrix which exist in an A-like form. Two of the modified probes containing four 2'-deoxy-2'-fluorocytidines or two 2'-deoxy-2'-fluorouridines direct the splitting by RNase H of only one phosphodiester bond of the RNA.
Transcription of 2'-deoxy-2'-fluoro-modified and phosphorothioate-modified RNA templates by HIV-1 reverse transcriptase
Anticancer Res 1999 Nov-Dec;19(6B):5419-21.PMID:10697571doi
RNA templates yield the corresponding DNA in the presence of human immunodeficiency virus reverse transcriptase (HIV-1 RT). The purpose of this study was to determine whether RNA that was modified with either 2'-deoxy-2'-fluoro analogs or with internucleotide phosphorothioate linkages could serve as templates for HIV-1 RT. Modified RNA that contained either 2'-deoxy 2'-fluoro pyrimidine nucleoside analogs or internucleotide phosphorothioate diester linkages 5'- to pyrimidine nucleosides were enzymatically synthesized and tested for template activity with recombinant HIV-1 RT. RNA that was modified with either 2'-deoxy-2'-fluorouridine or with internucleotide phosphorothioate linkages 5'- to pyrimidines yielded full length HIV-1 reverse transcription products, with complete fidelity in transcription. RNA that was modified with 2'-Deoxy-2'-fluorocytidine, either alone or in combination with 2'-deoxy-2'-fluorouridine, did not function as templates for HIV-1 RT, under the conditions reported here. The ability of 2'-deoxy-2'-fluoro-modified and phosphorothioate-modified RNA to serve as template for the RNA-dependent DNA polymerase of HIV-1 RT has not hitherto been reported.