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 Chemical Structure

CAS No. : 2222111-87-5

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5 mg ¥7000 In-stock
10 mg ¥11500 In-stock
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ARD-2128 相关产品


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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]

(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.

(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.








Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
In Vitro: 

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

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


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。

  • [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.