Irofulven is a semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle.
Structure of 158440-71-2
* For research and manufacturing use only. We do not sell to patients.
Size | Price | Stock | Quantity |
---|---|---|---|
5 mg | $1565 | In stock |
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Capabilities & Facilities
NCT Number | Condition Or Disease | Phase | Start Date | Sponsor | Status |
---|---|---|---|---|---|
NCT00033735 | Pancreatic Cancer | Phase 3 | 2012-12-24 | Eisai Inc. | Completed |
NCT00005968 | Melanoma (Skin) | Phase 2 | 2013-05-30 | University of Colorado, Denver | Completed |
NCT00374660 | Liver Cancer | Phase 1 | 2015-07-01 | Eisai Inc. | Unknown Verified June 2015 by Eisai Inc.. Recruitment status was Active, not recruiting |
NCT00124527 | Thyroid Cancer | Phase 2 | 2021-06-16 | Eisai Inc. | Completed |
NCT00003441 | Colorectal Cancer | Phase 2 | 2018-10-25 | M.D. Anderson Cancer Center | Completed |
Irofulven is a semisynthetic DNA-alkylating agent and a potent ADC cytotoxin used as an ADC payload in antibody-drug conjugates. Its cytotoxic mechanism involves alkylation of DNA, leading to DNA strand breaks, inhibition of replication, and induction of apoptosis in proliferating tumor cells. The molecular structure of Irofulven allows conjugation to antibodies via cleavable or non-cleavable linkers, facilitating targeted intracellular delivery in ADC applications.
Within antibody-drug conjugates, Irofulven is covalently attached to monoclonal antibodies using linkers that provide systemic stability and controlled payload release. The ADC remains inactive in circulation and is activated upon internalization into antigen-expressing tumor cells, where enzymatic cleavage releases Irofulven. This targeted delivery ensures cytotoxic activity is confined to tumor cells, minimizing off-target effects while maintaining precise antitumor mechanisms.
Applications of Irofulven include its use in ADCs targeting both solid tumors and hematologic malignancies. Its chemical compatibility with diverse linker chemistries allows optimization of conjugation efficiency, intracellular release kinetics, and pharmacokinetic behavior. Irofulven exhibits defined cytotoxicity in target-expressing cell lines and supports the development of ADCs with controlled DNA-damaging activity for tumor-targeted therapeutic applications.
What is Irofulven?
Irofulven is a DNA-damaging cytotoxin derived from illudin S, used as an ADC payload. It forms covalent adducts with DNA, leading to strand breaks and apoptosis, making it suitable for targeted cancer therapy when conjugated to antibodies.
30/8/2017
We are interested in how Irofulven improves ADC efficacy.
Irofulven enhances ADC therapeutic performance by selectively inducing DNA damage in antigen-expressing cells. Conjugation to antibodies ensures precise delivery, reducing off-target effects and maximizing cytotoxic impact on tumor cells.
12/12/2017
Could you advise which linkers are suitable for Irofulven conjugation?
Irofulven is compatible with cleavable linkers such as peptide-based or disulfide linkers. These linkers enable controlled intracellular release, maintaining ADC stability in circulation while delivering the payload efficiently to target cells.
20/5/2020
Is Irofulven suitable for preclinical ADC studies?
Yes, Irofulven is widely used in preclinical ADC research to evaluate efficacy, cytotoxicity, and pharmacokinetics. It provides critical data for optimizing ADC design, linker selection, and therapeutic performance in early-stage studies.
4/12/2020
Dear team, what handling precautions are necessary for Irofulven?
Due to its potent DNA-damaging properties, Irofulven must be handled with strict safety protocols, including PPE, fume hoods, and controlled waste disposal to prevent accidental exposure during ADC development.
4/8/2022
— Dr. Jason Carter, Senior Scientist (USA)
Irofulven from BOC Sciences arrived with outstanding purity, enabling efficient ADC conjugation.
20/5/2020
— Dr. Richard Brown, Oncology Researcher (USA)
Irofulven from BOC Sciences arrived quickly and with full traceability, which is essential for regulated research projects.
4/8/2022
— Ms. Maria Schneider, Senior Scientist (Germany)
We were able to integrate Irofulven smoothly into our studies thanks to the compound’s high purity and proper documentation.
4/12/2020
— Dr. Andrew Clarke, Project Lead (UK)
The Irofulven compound performed as expected in conjugation studies, and the stability was impressive over extended storage.
30/8/2017
— Mr. Johan Petersen, R&D Chemist (Denmark)
Customer support was excellent, and the Irofulven delivered by BOC Sciences met all our project’s technical requirements.
— Dr. Olivia Martin, Pharmaceutical Scientist (France)
Our lab has sourced Irofulven multiple times from BOC Sciences, and every batch showed consistency, which is invaluable for our ADC pipeline.
12/12/2017
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