Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR). Bavdegalutamide can be used in studies about prostate cancer. Bavdegalutamide shows oral activity and selectivity and facilitates the ubiquitination and degradation of AR.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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2 mg | 在庫あり | ¥ 19,500 | |||
5 mg | 在庫あり | ¥ 32,000 | |||
10 mg | 在庫あり | ¥ 49,500 | |||
25 mg | 在庫あり | ¥ 97,500 | |||
50 mg | 在庫あり | ¥ 125,000 | |||
100 mg | 在庫あり | ¥ 180,500 | |||
200 mg | 在庫あり | ¥ 250,500 |
説明 | Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR). Bavdegalutamide can be used in studies about prostate cancer. Bavdegalutamide shows oral activity and selectivity and facilitates the ubiquitination and degradation of AR. |
In vitro | Bavdegalutamide effectively degrades AR in all tested cell lines, achieving a 50% degradation concentration (DC50) of <1 nM[1]. In LNCaP cells, Bavdegalutamide induces dose-dependent AR degradation within the concentration range of 0.01 nM to 300 nM[1]. In VCaP cells, a time-dependent AR degradation is observed when treated with Bavdegalutamide at 10 nM for durations ranging from 0.5 to 24 hours[1]. Treatment with Bavdegalutamide at concentrations between 10 nM and 1000 nM results in the suppression of AR-target gene PSA expression, inhibition of AR-dependent cell proliferation, and induction of apoptosis at low nanomolar concentrations[1]. Bavdegalutamide effectively degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V, and H874V) and maintains activity in a high androgen environment (R1881, 100 nM) in VCaP cells[1]. |
In vivo | Administered through oral gavage at a dose of 1 mg/kg once daily, Bavdegalutamide demonstrates over 90% AR degradation in vivo. In LNCaP, VCaP, and patient-derived xenograft (PDX) models of prostate cancer, Bavdegalutamide significantly inhibits tumor growth and AR signaling[1]. In a long-term, castrate, enzalutamide-resistant VCaP tumor model, oral gavage of Bavdegalutamide at doses of 3 or 10 mpk for 30 days shows in vivo efficacy and reduces AR-target gene expression. The tumor growth inhibition (TGI) is 70% and 60% for 3 mg/kg and 10 mg/kg dosages, respectively[1]. |
別名 | ARV-110 |
分子量 | 812.29 |
分子式 | C41H43ClFN9O6 |
CAS No. | 2222112-77-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 46 mg/mL (56.63 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Bavdegalutamide 2222112-77-6 Endocrinology/Hormones Androgen Receptor ARV 110 prostate castration-resistant prostate cancer receptor androgen ARV-110 ARV110 inhibit cancer Inhibitor metastatic inhibitor