Phortress

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 (Cay-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. Phortress rapidly reverts to 5-fluoro 203 in carcinoma cell lines, resulting in significant growth inhibition at nanomolar concentrations. At 20 mg/kg, phortress can suppress the growth of breast and ovarian xenografts in vivo.Formal Name: 2S,6-diamino-N-[4-(5-fluoro-2-benzothiazolyl)-2-methylphenyl]-hexanamide, dihydrochloride. CAS Number: 328087-38-3. Synonyms: NSC 710305. Molecular Formula: C20H23FN4OS . 2HCl. Formula Weight: 459.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 210, 325 nm. SMILES: FC1=CC=C2C(N=C(C3=CC=C(NC([C@@H](N)CCCCN)=O)C(C)=C3)S2)=C1.Cl.Cl. InChi Code: InChI=1S/C20H23FN4OS.2ClH/c1-12-10-13(20-25-17-11-14(21)6-8-18(17)27-20)5-7-16(12)24-19(26)15(23)4-2-3-9-22,,/h5-8,10-11,15H,2-4,9,22-23H2,1H3,(H,24,26),2*1H/t15-,,/m0../s1. InChi Key: QZSMNTOCJVVFEU-CKUXDGONSA-N.