|
|
| | 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]- Basic information |
| | 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]- Chemical Properties |
| 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 |
| | 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]- Usage And Synthesis |
| 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 |
| | 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]- Preparation Products And Raw materials |
|