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Antitumoral Phortress Small Molecule (Tool Compound)

Info

Catalogue Number 151839
Antigen/Gene or Protein Targets Human derived carcinomas of breast, ovarian and renal origin
Type Antitumoral
Relevance 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.
On Target IC50 IC50 values for MCF-7 and MDA468 cells are 40 nM and 158 nM, respectively
Molecular Formula C20H25Cl2FN4OS
Molecular Weight (g/mol) 459.41
In vivo applications 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.
In vitro applications Induces expression of CYP1A1 and generates adducts in the DNA of sensitive MCF7 and IGROV-1 cells.
Research Area Cancer
Notes Compound available for screening or similar studies. For larger quantities (>20mg) please contact Ximbio.

References: 3 entries

Bradshaw et al. 2009. Pharmacology. 83(2):99-109. PMID: 19088497.

Fichtner et al. 2004. Breast Cancer Res Treat. 87(1):97-107. PMID: 15377855.

Bradshaw et al. 2004. Curr Med Chem. 11(8):1009-21. PMID: 15078163.


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References: 3 entries

Bradshaw et al. 2009. Pharmacology. 83(2):99-109. PMID: 19088497.

Fichtner et al. 2004. Breast Cancer Res Treat. 87(1):97-107. PMID: 15377855.

Bradshaw et al. 2004. Curr Med Chem. 11(8):1009-21. PMID: 15078163.


Add a reference

References: 3 entries

Bradshaw et al. 2009. Pharmacology. 83(2):99-109. PMID: 19088497.

Fichtner et al. 2004. Breast Cancer Res Treat. 87(1):97-107. PMID: 15377855.

Bradshaw et al. 2004. Curr Med Chem. 11(8):1009-21. PMID: 15078163.


Add a reference


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