SML3584
AZ1
≥98% (HPLC)
别名:
2-[[[5-Bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-ethanol, AZ 1, AZ-1
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关于此项目
经验公式（希尔记法）:
C17H16BrF4NO2
化学文摘社编号:
分子量:
422.21
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
Quality Level
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Maintaining protein stability of ?Np63 via USP28 is required by squamous cancer cells
Cristian Prieto-Garcia, Oliver Hartmann, Michaela Reissland, Fabian Braun, Thomas Fischer
EMBO Molecular Medicine, 12 (2022)
USP28 enables oncogenic transformation of respiratory cells, and its inhibition potentiates molecular therapy targeting mutant EGFR, BRAF and PI3K
Molecular Oncology, 16, 3082-3106 (2022)
Inhibition of USP28 overcomes Cisplatin-resistance of squamous tumors by suppression of the Fanconi anemia pathway
Cell Death and Differentiation, 29, 568-584 (2022)
The deubiquitinase USP25 supports colonic inflammation and bacterial infection and promotes colorectal cancer
Nature cancer, 1, 811-825 (2020)
Deubiquitylase USP25 prevents degradation of BCR-ABL protein and ensures proliferation of Ph-positive leukemia cells
Oncogene, 39, 3867-3878 (2020)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML3584-5MG | 04065269299400 |
| SML3584-25MG | 04065269299394 |
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