| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
FdCyd acts as a DNA methyltransferase (DNMT) inhibitor. As a prodrug, it is converted into the cytotoxic drug 5-fluorouracil (5-FU) by intracellular deaminases. 5-FU is then metabolized into active metabolites, including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits thymidylate synthase, reducing thymidine monophosphate production and depleting thymidine triphosphate, thereby inhibiting DNA synthesis and cell division. FUTP competes with uridine triphosphate for RNA incorporation, inhibiting RNA and protein synthesis.
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| ln Vitro |
In vitro studies demonstrate that FdCyd inhibits DNA methyltransferase activity, leading to the reactivation of silenced tumor suppressor genes. The compound's conversion to 5-fluorouracil and its subsequent metabolites results in the inhibition of DNA synthesis, RNA synthesis, and cell division. FdCyd's antimetabolite activity has been characterized in various cancer cell lines, supporting its potential as an antitumor agent.
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| ln Vivo |
FdCyd has been evaluated in vivo in therapeutic trials for various tumors, including lung cancer, breast cancer, head and neck cancer, and bladder cancer. As an antimetabolite composed of fluorinated pyrimidine analogs, it has potential antitumor activity. The compound is currently in clinical trials for breast cancer and other solid tumors. Its in vivo activity is mediated through its conversion to active metabolites that inhibit DNA and RNA synthesis.
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| Enzyme Assay |
Non-cellular enzyme assays for FdCyd involve assessing its inhibition of DNA methyltransferase (DNMT) activity using purified recombinant DNMT enzymes. The enzyme is incubated with a DNA substrate and a methyl donor (S-adenosylmethionine) in the presence of varying concentrations of FdCyd. The incorporation of methyl groups into the DNA substrate is measured using radiolabeled [³H]-SAM or by using a fluorescence-based assay. IC50 values for DNMT inhibition are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for FdCyd involve treating cancer cell lines with the compound and assessing cell viability, proliferation, and DNA methylation status. Cells are treated with varying concentrations of FdCyd for 72 hours, and cell viability is measured using MTT or CellTiter-Glo® assays. The inhibition of DNA methylation is assessed by bisulfite sequencing or methylation-specific PCR (MSP) to detect the reactivation of silenced genes. The induction of apoptosis and cell cycle arrest is evaluated by flow cytometry.
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| Animal Protocol |
In vivo animal experiments with FdCyd are conducted in mouse xenograft models of human tumors. Tumor-bearing mice are treated with FdCyd via intraperitoneal or oral administration, and tumor growth inhibition is monitored. Endpoints include tumor volume measurements, assessment of DNA methylation status in tumor tissue by bisulfite sequencing, and evaluation of pharmacodynamic markers such as the expression of silenced tumor suppressor genes. The compound's pharmacokinetic properties and toxicity are also assessed in these studies.
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| ADME/Pharmacokinetics |
FdCyd has a molecular weight of 245.21 and a molecular formula of C9H12FN3O4. It is a white to off-white solid powder with a melting point of 196°C and a density of 1.8±0.1 g/cm³. The compound has a calculated LogP of -1.61, indicating high hydrophilicity. It is typically stored at -20°C and is soluble in DMSO and other organic solvents. Purity is ≥98%. The compound is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
FdCyd is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. In preclinical and clinical studies, it has been generally well-tolerated at therapeutic doses. As a DNA methyltransferase inhibitor and fluoropyrimidine antimetabolite, it may cause side effects similar to other fluoropyrimidines, including myelosuppression, gastrointestinal toxicity, and mucositis. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
5-Fluoro-2'-deoxycytidine is a white fine powder. (NTP, 1992)
5-Fluoro-2'-deoxycytidine belongs to the pyrimidine class of compounds and is an organohalide. 5-Fluoro-2'-deoxycytidine has been used in therapeutic trials for various tumors, including lung cancer, breast cancer, head and neck cancer, and bladder cancer. 5-Fluoro-2'-deoxycytidine is an antimetabolite composed of fluorinated pyrimidine analogs and has potential antitumor activity. As a prodrug, 5-Fluoro-2'-deoxycytidine is converted into the cytotoxic drug 5-fluorouracil (5-FU) by intracellular deaminases. 5-Fluorouracil (5-FU) is then metabolized into active metabolites, including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits the activity of thymidine synthase, thereby reducing the production of thymidine monophosphate, leading to the depletion of thymidine triphosphate. This inhibits DNA synthesis and cell division. FUTP competes with uridine triphosphate for RNA incorporation, thereby inhibiting RNA and protein synthesis. Other fluorouracil metabolites also incorporate into DNA and RNA, further hindering cell growth. FdCyd (5-Fluoro-2'-deoxycytidine; CAS 10356-76-0) is a fluoropyrimidine nucleoside analog and DNA methyltransferase (DNMT) inhibitor. It is a tumor-selective prodrug that is converted to 5-fluorouracil and active metabolites that inhibit DNA and RNA synthesis. FdCyd has been used in therapeutic trials for various tumors, including lung, breast, head and neck, and bladder cancers. It is currently in clinical trials for breast cancer and other solid tumors. The compound is available from various commercial suppliers for research applications. |
| Molecular Formula |
C9H12FN3O4
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|---|---|
| Molecular Weight |
245.21
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| Exact Mass |
245.081
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| CAS # |
10356-76-0
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| PubChem CID |
515328
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
465.0±55.0 °C at 760 mmHg
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| Melting Point |
196 °C
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| Flash Point |
235.0±31.5 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
-1.61
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
398
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1[C@@H]([C@H](O[C@H]1N2C=C(C(=NC2=O)N)F)CO)O
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| InChi Key |
IDYKCXHJJGMAEV-RRKCRQDMSA-N
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| InChi Code |
InChI=1S/C9H12FN3O4/c10-4-2-13(9(16)12-8(4)11)7-1-5(15)6(3-14)17-7/h2,5-7,14-15H,1,3H2,(H2,11,12,16)/t5-,6+,7+/m0/s1
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| Chemical Name |
4-amino-5-fluoro-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
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| Synonyms |
FdCyd; Ro-5-1090; NSC-48006
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~203.91 mM)
H2O : ~16.67 mg/mL (~67.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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