| Identification | Back Directory | [Name]
4H-1-Benzopyran-4-one, 8-[(3,5-dimethyl-1H-pyrazol-4-yl)oxy]-5,7-dihydroxy-2-[4-[4-(2-pyridinyl)-1-piperazinyl]phenyl]- | [CAS]
2410534-62-0 | [Synonyms]
DC-U4106
4H-1-Benzopyran-4-one, 8-[(3,5-dimethyl-1H-pyrazol-4-yl)oxy]-5,7-dihydroxy-2-[4-[4-(2-pyridinyl)-1-piperazinyl]phenyl]- | [Molecular Formula]
C29H27N5O5 | [MOL File]
2410534-62-0.mol | [Molecular Weight]
525.56 |
| Chemical Properties | Back Directory | [Boiling point ]
787.6±60.0 °C(Predicted) | [density ]
1.414±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: Slightly soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
5.92±0.40(Predicted) | [color ]
Yellow to brown |
| Hazard Information | Back Directory | [Uses]
DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer[1]. | [in vivo]
DC-U4106 (intraperitoneal injection, 5 mg/kg or 20 mg/kg, every 2 days, 14 days) inhibits the proliferation of tumors and no significantly effects on body weight, organ morphology and structure in BALB/c nude mice[1]. | Animal Model: | BALB/c nude mice[1] | | Dosage: | 5 mg/kg , 20 mg/kg | | Administration: | Intraperitoneal injection, Every 2 days, 14 days | | Result: | Inhibited tumor growth significantly at a concentration of 20 mg/kg. |
| [References]
[1] Yucheng Tian, et al. Discovery of Potent Small-Molecule USP8 Inhibitors for the Treatment of Breast Cancer through Regulating ERα Expression. J Med Chem. 2022 Jul 5. DOI:10.1021/acs.jmedchem.2c00013 |
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