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首页-抗体药物偶连体和PROTACs-PROTAC-Bavdegalutamide
Bavdegalutamide

Chemical Structure : Bavdegalutamide

CAS No.: 2222112-77-6

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Bavdegalutamide (ARV-110, ARV110)

货号: PC-38047Not For Human Use, Lab Use Only.

Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR with DC50 of <1 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR with DC50 of <1 nM.
At the dose of 0.01 nM-300 nM, ARV-110 leads to AR degradation in LNCaP cells in a dose-dependent manner.
In VCaP cells, ARV-110 leads to AR degradation in a time-dependent manner.
ARV-110 suppresses the expression of the AR-target gene PSA. ARV-110 inhibits AR-dependent cell proliferation and induces apoptosis at low nanomolar concentrations.
ARV-110 degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V, and H874V). retains activity even in a high androgen environment (R1881, 100 nM) in VCaP cells.
ARV-110 exhibits a greater than 90% AR degradation in LNCaP, VCaP, and prostate cancer PDX models.
ARV-110 exhibits significant inhibition of tumor growth and AR signaling in vivo.

物理化学性质&存储条件

分子量 812.3
分子式 C41H43ClFN9O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide

参考文献

1. Cancer Discov. 2020 Aug;10(8):1084.

2. Qi SM, et al. Front Pharmacol. 2021 May 7;12:692574.

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