货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V45054-1mg	≥98%	￥8990.00 V45054-1mg ￥8990.00 3-5天	0 货期：3-5天	-	-	-	-
V45054-5mg	≥98%	￥19800.00 V45054-5mg ￥19800.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V45054-1mg

≥98%

￥8990.00

货期：3-5天

V45054-5mg

≥98%

￥19800.00

货期：3-5天

产品描述：

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. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体外研究：

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.
ARD-61 (0.001-100 μM; for 7?days) has IC50 values of 235?nM and 121?nM in the MDA-MB-453 and HCC1428 cell lines, which have the highest AR expression, respectively. ARD-61 demonstrates partial cell growth inhibition, delivering IC50 values of 39, 147, and 380?nM, respectively, in the MCF-7, BT-549 and MDA-MB-415 cell lines, which have a moderate level of AR protein.
ARD-61 (25-100000 nM; 6-72 h) induces G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines.
ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 and HCC1428 cell lines.
ARD-61 (0.01-1000 nM; 6 h) is highly potent and effective in reducing AR protein levels. ARD-61 (0.01-1000 nM; 24 h) reduces the level of PR protein with a DC50 value of 0.15?nM in the T47D cells. ARD-61 has no obvious effect on ER and GR proteins.
ARD-61 (1?μM; for 24?h) effectively inhibits Wnt/β-catenin and MYC signaling pathways. ARD-61 (1-1000?nM; for 24?h) not only decreases both phosphorylated HER2 and HER3, but also un-phosphorylated HER2 and HER3 proteins.
Efficient knock-down of VHL completely blocks AR degradation induced by ARD-61 (100?nM; 24 h) in both MDA-MB-453 and MCF-7 cell lines.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	0.913 ml	4.563 ml	9.126 ml
5 mM	0.183 ml	0.913 ml	1.825 ml
10 mM	0.091 ml	0.456 ml	0.913 ml
50 mM	0.018 ml	0.091 ml	0.183 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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