2-Fluoro-2-deoxyuridine丨CAS 784-71-4

Overview

2-Fluoro-2-deoxyuridine丨CAS 784-71-4 is a chemotherapeutic nucleoside analog used primarily as an antimetabolite. It interferes with DNA synthesis by mimicking natural nucleosides and integrating into DNA, thus halting cell proliferation, especially in rapidly dividing tumor cells. It is also a metabolite and prodrug of 5-fluorouracil (5-FU).

Applications

1. Anticancer Research

Used in preclinical and clinical research for treating cancers such as:

Colorectal cancer

Breast cancer

Head and neck tumors

Functions as a DNA synthesis inhibitor, leading to cytotoxicity in tumor cells.

2. Chemotherapy Agent

2-Fluoro-2-deoxyuridine丨CAS 784-71-4 acts as a prodrug of 5-fluorouracil (5-FU), metabolized into active forms like FdUMP, which inhibit thymidylate synthase, a key enzyme in DNA replication.

Sometimes administered topically or locally, such as in ocular tumors or implants for sustained release.

3. Radiosensitizer

Enhances the effectiveness of radiotherapy by sensitizing cancer cells, particularly in glioblastoma and other aggressive cancers.

4. Antiviral Activity

Studied for its potential antiviral effects against DNA viruses, though less commonly used than for oncology.

5. Research Tool in Molecular Biology

Used in DNA synthesis and repair studies to probe the mechanism of action of thymidylate synthase inhibitors and the incorporation of analogs into DNA.

Benefits

✅ Potent Antimetabolite

Acts quickly and effectively by blocking DNA synthesis, leading to apoptosis of cancer cells.

✅ Selective Toxicity

More toxic to rapidly dividing cells, making it a valuable agent for targeting tumors while sparing most healthy tissues.

✅ Prodrug of 5-FU

Offers an alternative pathway to deliver 5-fluorouracil, often with improved pharmacokinetics or controlled release formulations.

✅ Useful in Localized Treatment

Can be formulated into implants, ointments, or localized delivery systems to reduce systemic toxicity and increase efficacy at tumor sites.

✅ Research Relevance

Frequently used in laboratory settings to study DNA damage, repair mechanisms, and drug resistance in cancer biology.

Summary

2-Fluoro-2-deoxyuridine丨CAS 784-71-4 is a fluorinated nucleoside analog with powerful anticancer activity. By inhibiting DNA synthesis, it serves as a chemotherapy agent, radiosensitizer, and research tool. It is particularly important in the development of thymidylate synthase-targeted therapies and as a metabolic precursor to the widely used drug 5-fluorouracil.