Antitumoral Phortress Small Molecule (Tool Compound)
- Name Malcolm F G Stevens
- Institute University of Nottingham
Tool name: Antitumoral Phortress Small Molecule (Tool Compound)
Molecular formula: C20H25Cl2FN4OS
Tool type: Small molecules
Tool sub-type: Antitumoral
Cancer type: Breast; Ovarian; Renal
Molecular weight of the target: 459.41
Application: Active against breast, ovarian and renal carcinomas. Taken up into sensitive cells followed by aryl hydrocarbon receptor binding and translocation into the nucleus. Requires metabolic activation by cytochrome P450 to generate cytotoxic species. Induces expression of CYP1A1 and generates adducts in the DNA of sensitive MCF7 and IGROV-1 cells.
Description: The Antitumoral Phortress compound is a potential anticancer agent for treatment of human breast carcinoma. Phortress is highly selective for susceptible cancer cells because of its mechanism of action. Following the release of 5F 203 from Phortress, it activates AhR signalling and causes induction of cytochrome P450 activity, which metabolically bioactivates 5F 203 to a cytotoxic species at the tumour site.
Phortress (the dihydrochloride salt of the lysylamide prodrug of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203)) is an experimental antitumour agent with potent and selective activity against human-derived carcinomas of breast, ovarian and renal origin
The mechanism of action of Phortress is distinct from all classes of chemotherapeutic agents currently in the clinic, and involves metabolic activation by cytochrome P450 (CYP) 1A1 to electrophilic species, which generate DNA adducts in sensitive tumours only.
Research area: Cancer; Cell Cycle; Epigenetics & Nuclear Signalling
IC50: IC50 values for MCF-7 and MDA468 cells are 40 nM and 158 nM, respectively
Additional notes: Compound available for screening or similar studies. For larger quantities (>20mg) please contact Ximbio.
Phortress Diode Array
- For Research Use Only
- • Bradshaw et al. 2009. Pharmacology. 83(2):99-109. PMID: 19088497.
- • Preclinical toxicokinetic evaluation of phortress [2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole lysylamide dihydrochloride] in two rodent species.
- • Fichtner et al. 2004. Breast Cancer Res Treat. 87(1):97-107. PMID: 15377855.
- • The experimental antitumor agents Phortress and doxorubicin are equiactive against human-derived breast carcinoma xenograft models.
- • Bradshaw et al. 2004. Curr Med Chem. 11(8):1009-21. PMID: 15078163.
- • The development of the antitumour benzothiazole prodrug, Phortress, as a clinical candidate.