SML3584

AZ1

≥98% (HPLC)

• Synonym(s): 2-[[[5-Bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-ethanol, AZ 1, AZ-1
• Empirical Formula (Hill Notation): C₁₇H₁₆BrF₄NO₂
• CAS Number: 2165322-94-9
• Molecular Weight: 422.21
• UNSPSC Code: 12352200
• NACRES: NA.21
• MDL number: MFCD32201047
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: FC1=CC=C(COC2=CC=C(C=C2CNCCO)Br)C=C1C(F)(F)F
• InChI key: ITHSFXDGKQYOED-UHFFFAOYSA-N

Description

Biochem/physiol Actions

AZ1 is a potent and selective dual USP25 & USP28 deubiquitinase (DUBs) inhibitor (USP25/28 IC50 = 0.62/0.7 nM by Ub-Rh110 assay) that induces HCT116 cellular c-Myc degradation (20-100 µM for 3h or 60 µM for 0.3-3h). AZ1 exhibits antiproliferation activity in cancer cultures (IC50 ≤20 µM; HCT116, HT29 and SW480) and anti-tumor efficacy in an orthotopic model of lung SCC tumours in mice in vivo (125 mg/kg or 375 mg/kg i.p. once every three days, 6 injections total).

Potent and selective dual USP25 & USP28 deubiquitinase (DUBs) inhibitor with anti-cancer efficacy in vitro and in vivo.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable