A lysyl amide prodrug of the benzothiazole 5-fluoro 203

Phortress – 5 mg

Brand:
Cayman
CAS:
328087-38-3
Storage:
-20
UN-No:
Non-Hazardous - /

The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that promotes the expression of phase I and II xenobiotic chemical metabolizing enzyme genes, including the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2. Phortress is a lysyl amide prodrug of the benzothiazole 5-fluoro 203 (Item No. 17677), a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1, which leads to the formation of DNA adducts and cell cycle arrest.{29410,29411} Phortress rapidly reverts to 5-fluoro 203 in carcinoma cell lines, resulting in significant growth inhibition at nanomolar concentrations.{29411} At 20 mg/kg, phortress can suppress the growth of breast and ovarian xenografts in vivo.{29411}  

 

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Description

A lysyl amide prodrug of the benzothiazole 5-fluoro 203, a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1, which leads to the formation of DNA adducts and cell cycle arrest

Formal name: 2S,6-diamino-N-[4-(5-fluoro-2-benzothiazolyl)-2-methylphenyl]-hexanamide, dihydrochloride

Synonyms:  NSC 710305

Molecular weight: 459.4

CAS: 328087-38-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Transcription Factors & Coactivators||Research Area|Cancer|Cell Cycle||Research Area|Cancer|DNA Damage and Repair||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Xenobiotic Sensing

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