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Merck
CN

SML3584

AZ1

≥98% (HPLC)

Synonym(s):

2-[[[5-Bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-ethanol, AZ 1, AZ-1

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About This Item

Empirical Formula (Hill Notation):
C17H16BrF4NO2
CAS Number:
Molecular Weight:
422.21
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

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

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.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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