上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
ARD-61
ARD-61 是一种高效、特异的 PROTAC 雄激素受体 (AR) 降解剂。ARD-61 有效且有效地诱导 AR+ 癌细胞系中的 AR 和孕酮受体 (PR) 降解。ARD-61 诱导细胞凋亡,也可有效抑制小鼠 MDA-MB-453 异种移植模型中的肿瘤生长。
ARD-61 Chemical Structure
CAS No. : 2316837-08-6
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生物活性 |
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
ARD-61 binds to AR protein through its AR antagonist portion and von Hippel-Lindau (VHL)/cullin 2 E3 ligase through its VHL ligand portion to recruit AR protein to cullin 2 for ubiquitination, followed by proteasome-dependent AR degradation[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay[1]
Cell Cycle Analysis[1]
Apoptosis Analysis[1]
Western Blot Analysis[1]
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体内研究 (In Vivo) |
ARD-61 (25, 50 mg/kg/day; ip; for 75 days) effectively inhibits tumor growthin the MDA-MB-453 xenograft tumor model in male SCID mice[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
1095.78 |
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Formula |
C61H71ClN8O7S |
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CAS 号 |
2316837-08-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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