Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively[1].
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 13,000 | |||
5 mg | 在庫あり | ¥ 28,000 | |||
10 mg | 在庫あり | ¥ 45,500 | |||
25 mg | 在庫あり | ¥ 90,500 | |||
50 mg | 在庫あり | ¥ 134,500 | |||
100 mg | 在庫あり | ¥ 192,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 49,000 |
説明 | ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively[1]. |
ターゲット&IC50 | BRD2(2):4.7 nM (Kd), BRD3(2):7.6 nM (Kd), BRD4(2):7.6 nM (Kd), BRD4(1):9.6 nM (Kd), BRD3(1):8.3 nM (Kd), BRD2(1):34 nM (Kd) |
In vitro | ARV-771, utilizing proteolysis-targeting chimera (PROTAC) technology, outperforms BET inhibitors in CRPC cellular models by effectively degrading BRD2/3/4 in 22Rv1 cells with a DC50 of less than 5 nM. This compound also significantly reduces c-MYC protein levels, a key BET protein effector, achieving an IC50 under 1 nM. Demonstrating potent anti-proliferative abilities, ARV-771 impacts 22Rv1, VCaP, and LnCaP95 cell lines, inducing apoptosis and altering cell morphology. Furthermore, treatment with 10 nM of ARV-771 notably suppresses FL-AR and AR-V7 mRNA in VCaP cells and exerts an antiandrogenic influence on several AR-regulated genes within these cells[1]. |
In vivo | Administering daily subcutaneous injections of ARV-771 at a dosage of 10 mg/kg for three days to non-castrated male Nu/Nu mice with AR-V7+ 22Rv1 tumor xenografts resulted in a significant reduction of BRD4 and c-MYC levels in the tumor tissue by 37% and 76%, respectively. Additionally, a notable decrease in AR-V7 levels was observed in the 22Rv1 tumors following the treatment with ARV-771[1]. |
分子量 | 986.64 |
分子式 | C49H60ClN9O7S2 |
CAS No. | 1949837-12-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
You can also refer to dose conversion for different animals. 詳細
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ARV-771 1949837-12-0 Chromatin/Epigenetic Epigenetic Reader Domain inhibit ARV771 PROTACs Inhibitor ARV 771 inhibitor