Luxdegalutamide
| CAS号 | 2750830-09-0 | 货号 | BCP49650 |
| 中文名 | Luxdegalutamide | ||
| 英文名 | Luxdegalutamide | ||
| 中文别名 | |||
| 英文别名 | ARV-766;ARV 766;ARV766; | ||
| 分子式 | C45H54FN7O6 | 分子量 | 807.95 |
| 生物活性 | Luxdegalutamide is an orally bioavailable androgen receptor (AR)-targeted protein degrader, composed of an AR ligand attached to an E3 ligase recognition moiety and utilizing the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon oral administration, luxdegalutamide targets and binds to the AR ligand binding domain on the AR. E3 ligase is then recruited to the AR by the E3 ligase recognition moiety of luxdegalutamide and the AR is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome, and prevents the expression of AR target genes and halts AR-mediated signaling. This inhibits the proliferation of AR-overexpressing tumor cells. In addition, the degradation of the AR releases luxdegalutamide, allowing it to bind to additional AR. AR plays a key role in the proliferation of castration-resistant prostate cancer cells (CRPC). Luxdegalutamide may degrade resistance-driving point mutations of AR, including the L702H mutation associated with treatments including abiraterone. | ||
| 信号通路 | Hormone Pathay Others Pathway | ||
| 靶 点 | Androgen Receptor PROTAC | ||
结构式
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