货号:A266441
同义名:
2'-Deoxy-5-Fluorocytidine; FCdR
5-Fluoro-2'-deoxycytidine是一种 DNMT 抑制剂,通过与 DNMT 活性位点中的半胱氨酸残基形成共价键进行作用。


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| 产品名称 | DNA Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 6-Thioguanine | ✔ | 98% | |||||||||||||||||
| Zebularine | ✔ | 98% | |||||||||||||||||
| Procainamide HCl | ✔ | 99% | |||||||||||||||||
| 5-Azacytidine | ✔ | 95% | |||||||||||||||||
| Decitabine | ✔ | 99% | |||||||||||||||||
| SGI-1027 |
++
DNMT3A, IC50: 7.5 μM DNMT1, IC50: 6 μM |
99%+ | |||||||||||||||||
| RG108 |
+++
DNA methyltransferase, IC50: 115 nM |
99%+ | |||||||||||||||||
| Guadecitabine sodium | ✔ | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | 5-Fluoro-2'-deoxycytidine is a fluoropyrimidine nucleoside analogue and a DNMT inhibitor. 5-Fluoro-2'-deoxycytidine is a tumour-selective prodrug of 5-fluoro-2′-dUMP[1][2]. |
| Concentration | Treated Time | Description | References | |
| KYSE150 | 1 μM | 72 h | FCdR inhibited KYSE150 cell proliferation with a survival rate of about 30%. | Springerplus. 2012 Dec;1(1):65 |
| U2OS | 1 μM | 72 h | FCdR inhibited U2OS cell proliferation with a survival rate of about 80%. | Springerplus. 2012 Dec;1(1):65 |
| HEPG2 | 1 μM | 72 h | FCdR inhibited HEPG2 cell proliferation with a survival rate of about 40%. | Springerplus. 2012 Dec;1(1):65 |
| dCMPD-/TK- double mutant S-49 cells | 1 μM | Evaluate the inhibitory effect of 5-Fluoro-2'-deoxycytidine on cells lacking both dCMP deaminase and thymidine kinase, showing significantly reduced toxicity. | Proc Natl Acad Sci U S A. 1982 Nov;79(21):6419-23 | |
| dCMPD- mutant S-49 cells | 3 nM | Evaluate the inhibitory effect of 5-Fluoro-2'-deoxycytidine on cells lacking dCMP deaminase, showing reduced toxicity. | Proc Natl Acad Sci U S A. 1982 Nov;79(21):6419-23 | |
| dCK- mutant S-49 cells | 20 nM | Evaluate the inhibitory effect of 5-Fluoro-2'-deoxycytidine on cells lacking deoxycytidine kinase, showing reduced toxicity. | Proc Natl Acad Sci U S A. 1982 Nov;79(21):6419-23 | |
| TK- mutant S-49 cells | 10 nM | Evaluate the inhibitory effect of 5-Fluoro-2'-deoxycytidine on cells lacking thymidine kinase, showing reduced toxicity. | Proc Natl Acad Sci U S A. 1982 Nov;79(21):6419-23 | |
| S49 mouse lymphoma cells | 2 nM | Evaluate the inhibitory effect of 5-Fluoro-2'-deoxycytidine on cell growth, showing it primarily acts by inhibiting thymidylate synthetase. | Proc Natl Acad Sci U S A. 1982 Nov;79(21):6419-23 | |
| Caki-1 PBRM1-/- | 10uM | 72 h | To screen for synthetic lethal drugs in PBRM1-deficient renal cancer cells | Front Oncol. 2022 Jun 3;12:870229 |
| Caki-1 PBRM1+/+ | 10uM | 72 h | To screen for synthetic lethal drugs in PBRM1-deficient renal cancer cells | Front Oncol. 2022 Jun 3;12:870229 |
| Human ependymoma PDX | 8.3 nM | 72 h | To evaluate the inhibitory effect of FdCyd on human ependymoma PDX cell proliferation, showing an EC50 of 8.3 nM. | J Neurooncol. 2016 Jan;126(2):225-34 |
| Human G3 medulloblastoma PDX (TB-12-5950) | 1 nM | 72 h | To evaluate the inhibitory effect of FdCyd on human G3 medulloblastoma PDX cell proliferation, showing an EC50 of 1 nM. | J Neurooncol. 2016 Jan;126(2):225-34 |
| Mouse choroid plexus carcinoma (CPC) | 5.6 nM | 72 h | To evaluate the inhibitory effect of FdCyd on choroid plexus carcinoma cell proliferation, showing an EC50 of 5.6 nM. | J Neurooncol. 2016 Jan;126(2):225-34 |
| Mouse ependymoma (EP) | 4 nM | 72 h | To evaluate the inhibitory effect of FdCyd on ependymoma cell proliferation, showing an EC50 of 4 nM. | J Neurooncol. 2016 Jan;126(2):225-34 |
| Mouse G3 medulloblastoma (Myc1) | 1.7 nM | 72 h | To evaluate the inhibitory effect of FdCyd on G3 medulloblastoma cell proliferation, showing an EC50 of 1.7 nM. | J Neurooncol. 2016 Jan;126(2):225-34 |
| Administration | Dosage | Frequency | Description | References | ||
| CD1 nude mice | G3 medulloblastoma, ependymoma, and choroid plexus carcinoma models | Intravenous injection | 6 mg/kg | 5 days treatment followed by 2 days off for 2 weeks for a 4-week cycle | To evaluate the in vivo efficacy of FdCyd and THU combination therapy in G3 medulloblastoma, ependymoma, and choroid plexus carcinoma models, showing no significant tumor growth inhibition. | J Neurooncol. 2016 Jan;126(2):225-34 |
| BALB/c nude mice | 786-O PBRM1+/+ and PBRM1-/-#1 xenograft model | Oral | 25mg/kg | Daily for 21 days | To evaluate the synthetic lethal effect of Fdcyd in PBRM1-deficient renal cancer | Front Oncol. 2022 Jun 3;12:870229 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
4.08mL 0.82mL 0.41mL |
20.39mL 4.08mL 2.04mL |
40.78mL 8.16mL 4.08mL |
|
| CAS号 | 10356-76-0 |
| 分子式 | C9H12FN3O4 |
| 分子量 | 245.21 |
| SMILES Code | O=C1N=C(N)C(F)=CN1[C@@H]2O[C@H](CO)[C@@H](O)C2 |
| MDL No. | MFCD00077348 |
| 别名 | 2'-Deoxy-5-Fluorocytidine; FCdR; FdCyd; Ro-5-1090; NSC-48006; 5-fluoro-2(')-deoxycytidine |
| 运输 | 蓝冰 |
| InChI Key | IDYKCXHJJGMAEV-RRKCRQDMSA-N |
| Pubchem ID | 515328 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(203.91 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 15 mg/mL(61.17 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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