Bavdegalutamide
产品说明书
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同义名 : | ARV-110 |
| CAS号 : | 2222112-77-6 | |
| 货号 : | A1452141 | |
| 分子式 : | C41H43ClFN9O6 | |
| 纯度 : | 99%+ | |
| 分子量 : | 812.288 | |
| MDL号 : | - | |
| 存储条件： |
Pure form Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(30.78 mM)，配合低频超声，水浴加热至45℃，并调节pH至3，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Protease-targeted chimeras (PROTACs) molecules are bifunctional small molecules that simultaneously bind a target protein and an E3-ubiquitin ligase, thus causing ubiquitination and degradation of the target protein by the proteasome. Like small molecules, PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins[2]. ARV-110, an orally small molecule PROTAC was designed to specifically target Androgen receptor (AR), firstly enters clinical phase I trials for the treatment of metastatic castration-resistant prostate cancer, which turns a new avenue for the development of PROTAC[3]. ARV-110 robustly degrades AR in all cell lines tested, with an observed halfmaximal degradation concentration (DC50) of ~1 nM. ARV-110 treatment leads to highly selective AR degradation, as demonstrated by proteomic studies. In VCaP cells,PROTAC-mediated AR degradation suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations. Further, ARV-110 degrades clinically relevant mutant AR proteins and retains activity in a high androgen environment. In mouse xenograft studies, greater than 90% AR degradation is observed at a 1 mg/kg PO QD dose. Notably, ARV-110 demonstrates in vivo efficacy and reduction of AR-target gene expression in a long term, castrate,enzalutamide-resistant VCaP tumor modelz[4]. Clinical activity for ARV-110 in heavily pretreated patients with mCRPC and suggested enhanced activity in patients with specific molecular profiles, eg, AR T878 and H875 mutations (ARV-110 doses ranged from 35–700 mg QD or 210–420 mg BID)[5]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.23mL 0.25mL 0.12mL |
6.16mL 1.23mL 0.62mL |
12.31mL 2.46mL 1.23mL |
| 参考文献 |
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[1]Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer |