Description
Product Description
Fluorouracil (5-FU), CAS 51-21-8, is a fluorinated pyrimidine analog widely applied in laboratory research for DNA replication stress, RNA misincorporation, apoptosis signaling, metabolic activation, and cytotoxic mechanism studies. Its structural similarity to uracil allows incorporation into DNA and RNA, leading to multiple cellular effects that are widely exploited in preclinical models.
Metabolic Activation and Mechanistic Metabolites
FdUMP: Inhibits thymidylate synthase (TS), causing dTMP depletion, DNA synthesis arrest, and DNA strand breaks.
FUTP: Incorporated into RNA, disrupting rRNA, tRNA, and mRNA processing, affecting translation fidelity.
FdUTP: Misincorporated into DNA, triggering mismatch repair and DNA damage signaling.
These metabolites enable 5-FU to serve as a versatile tool for studying DNA replication stress, checkpoint activation, DNA repair pathways (MMR, BER, HR), and apoptotic signaling.
Cellular Stress Responses
5-FU induces S-phase arrest, mitochondrial depolarization, ROS generation, caspase activation, and transcriptional stress. Researchers utilize these responses to examine replication stress, checkpoint activation, and DNA repair fidelity.
Combination and In Vivo Studies
Combination Studies: Paired with kinase inhibitors, nucleoside analogs, or oxidative stress modulators to evaluate synergistic or antagonistic effects.
In Vivo Studies: Applied in preclinical tumor xenografts to assess tumor growth inhibition, apoptosis induction, pharmacokinetics, and enzyme activity.
Product Specifications
| Parameter | Specification / Data |
|---|---|
| Chemical Name / Synonyms | Fluorouracil; 5-FU; Pyrimidine analog; Antimetabolite; C4H3FN2O2 |
| CAS Number | 51-21-8 |
| Molecular Formula | C4H3FN2O2 |
| Molecular Weight | 130.08 g/mol |
| Purity / Assay | ≥99% |
| Appearance | White to off-white crystalline powder |
| Solubility | Soluble in DMSO, ethanol; moderate aqueous solubility |
| Melting Point | 282–283 °C |
| Storage Temperature | 2–8 °C |
| Stability | Stable under refrigeration; protect from light and moisture |
| Analytical Methods | HPLC, MS, NMR verified; batch consistency confirmed |
| Mechanistic Target | Thymidylate synthase, RNA misincorporation, apoptosis induction, S-phase arrest |
| Structural Category | Pyrimidine analog antimetabolite |
| Applications | DNA/RNA synthesis inhibition studies, apoptosis research, cell-cycle regulation, metabolic activation research, drug resistance modeling |
| Batch Consistency | Verified by HPLC, MS, NMR |
| Regulatory Notes | For laboratory research use only |
| Origin | Factory peptide/small-molecule supplier, China peptide manufacturer, OEM & bulk production available |
| Additional Data | SMILES: C1=CN(C=O)C(=O)N=C1F; CoA provided for each batch |
Mechanism of Action
Fluorouracil exerts its preclinical research effects through thymidylate synthase inhibition, RNA misincorporation, and apoptosis induction.
Thymidylate Synthase Inhibition (FdUMP)
FdUMP forms a covalent ternary complex with TS and 5,10-methylenetetrahydrofolate, causing dTMP depletion. This triggers DNA replication arrest, strand breaks, and activation of ATR/ATM signaling, CHK1/CHK2 phosphorylation, and p53-dependent checkpoints.
RNA Misincorporation (FUTP)
FUTP incorporation into RNA disrupts rRNA, tRNA, and mRNA processing, ribosome biogenesis, and translation fidelity. Leads to ribosomal stress and unfolded protein response.
DNA Misincorporation (FdUTP)
FdUTP misincorporation activates DNA repair pathways, replication fork stalling, and apoptosis. Enables study of mismatch repair, base excision repair, and DNA damage signaling.
Apoptosis Induction
Mitochondrial depolarization, cytochrome c release, caspase-3 and -9 activation, and ROS-mediated oxidative stress. Apoptosis occurs via p53-dependent and independent mechanisms.
Drug Resistance Modeling
TS overexpression, increased DPD activity, and altered nucleotide metabolism are explored using 5-FU to understand chemoresistance mechanisms.

Side Effects
In laboratory models, Fluorouracil exhibits dose-dependent cytotoxicity:
Cellular Effects
S-phase arrest and DNA damage accumulation
ROS-mediated oxidative stress
RNA misincorporation disrupting translation and ribosomal function
Apoptotic Pathways
Caspase-3 and -9 activation
Mitochondrial depolarization and cytochrome c release
p53-dependent and independent apoptosis
Metabolic Considerations
DPD activity and nucleotide pool variability influence cytotoxicity
Used to investigate adaptive responses and combination therapy mechanisms
Laboratory Handling
Use PPE, fume hoods, and containment protocols
Strictly for research use; cytotoxic in nature
Keywords
Fluorouracil, 5-FU, pyrimidine analog, antimetabolite, thymidylate synthase inhibitor, DNA synthesis inhibitor, RNA misincorporation, apoptosis research, cytotoxicity studies, cell-cycle regulation, metabolic activation, drug resistance modeling, high-purity research chemical, factory peptide/small-molecule supplier, China peptide manufacturer, OEM & bulk production, laboratory research reagent
Shipping Guarantee
All Fluorouracil shipments of Fluorouracil are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.
Trade Assurance
We Fluorouracil ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.
Payment Support
We Fluorouracil provide flexible and secure global payment options to support international research transactions. Accepted payment methods include PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are protected by industry-standard encryption and verified payment gateways to ensure confidentiality and fund security.
Disclaimer
Fluorouracil is supplied for laboratory research purposes only. It is not intended for human or animal use, diagnostic applications, or clinical treatment. Researchers must follow all institutional and governmental safety guidelines when handling this compound. The supplier assumes no liability for misuse, unauthorized administration, or off-label applications.




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