ARD-2128

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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-2128  纯度: 99.04%

ARD-2128 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂。ARD-2128 可有效降低 AR 蛋白并抑制肿瘤组织中 AR 调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。ARD-2128 作用在前列腺癌的研究上。

ARD-2128

ARD-2128 Chemical Structure

CAS No. : 2222111-87-5

规格 价格 是否有货 数量
5 mg ￥7000 In-stock
10 mg ￥11500 In-stock
50 mg   询价  
100 mg   询价  

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ARD-2128 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer[1].

IC50 & Target

IC50: 4 nM (VCaP), 5 μM (LNCaP)[1]
体外研究
(In Vitro)

ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values of 4 nM and 5 nM, respectively[1].
ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell[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 Line: VCaP cell
Concentration: 1, 10, 100, and 1000 nM
Incubation Time: 24 hours
Result: Reduces the AR protein level and achieves the AR degradation.

体内研究
(In Vivo)

ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours[1].
ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice[1].
ARD-2128 (5mg/kg; p.o.) treatment shows the Cmax, AUC0-t and t1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively[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.

Animal Model: SCID mice[1]
Dosage: 20 mg/kg
Administration: Oral
Result: Reducing the level of AR protein in mice after 24 hours.
Animal Model: SCID mice[1]
Dosage: 10, 20, and 40 mg/kg
Administration: P.o.; daily for 21 days
Result: Inhibits tumor growth by 46, 69, and 63%, respectively.
Animal Model: Male ICR Mice[1]
Dosage: 5 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: The Cmax, AUC0-t and t1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.

分子量

820.37

Formula

C45H50ClN7O6
CAS 号

2222111-87-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (121.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2190 mL 6.0948 mL 12.1896 mL
5 mM 0.2438 mL 1.2190 mL 2.4379 mL
10 mM 0.1219 mL 0.6095 mL 1.2190 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00882.

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