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ARD-2128

Catalog No. T39695 CAS 2222111-87-5

ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) degrader of the androgen receptor (AR), effectively diminishing AR protein levels, suppressing AR-regulated gene expression in tumor tissues, and inhibiting tumor growth without evident toxicity. This compound holds promise for prostate cancer research.

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ARD-2128, CAS 2222111-87-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 228.00
2 mg	In stock	$ 342.00
5 mg	In stock	$ 578.00
10 mg	In stock	$ 833.00
25 mg	In stock	$ 1,270.00
50 mg	In stock	$ 1,690.00
100 mg	In stock	$ 2,290.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) degrader of the androgen receptor (AR), effectively diminishing AR protein levels, suppressing AR-regulated gene expression in tumor tissues, and inhibiting tumor growth without evident toxicity. This compound holds promise for prostate cancer research.
Targets&IC50	LNCaP cells:5 μM (IC50), VCaP:4 nM (IC50)
In vitro	ARD-2128 exhibits high potency and efficacy in suppressing the growth of both VCaP and LNCaP cell lines, with IC50 values of 4 nM and 5 nM, respectively [1]. Notably, in the VCaP cell line treated with ARD-2128 at concentrations of 1, 10, 100, and 1000 nM for 24 hours, there is a significant decrease in AR protein levels, with reductions of more than 50% observed at 1 nM and over 90% degradation at concentrations of 10, 100, and 1000 nM [1]. This finding is further corroborated by a Cell Viability Assay [1], which demonstrates that ARD-2128 effectively diminishes AR protein levels and facilitates AR degradation in the VCaP cell line under the specified conditions.
In vivo	ARD-2128 administered orally at a dosage of 20 mg/kg effectively lowers AR protein levels in mice within 24 hours, as per reference [1]. When given daily at doses ranging from 10 to 40 mg/kg for 21 days, the compound demonstrates notable antitumor effects in the VCaP xenograft mouse model, inhibiting tumor growth by 46% to 69% [1]. Pharmacokinetic analysis reveals that a 5 mg/kg oral dosage yields a maximum concentration (C max) of 1304 ng/mL, an area under the curve (AUC 0-t) of 22361 ng h/mL, and a half-life (t 1/2) of 18.8 hours [1]. The study, using SCID and Male ICR mice, indicates that ARD-2128, with oral bioavailability of 67%, effectively reduces AR protein levels and suppresses AR-regulated gene activity in tumor tissues. It thus inhibits tumor growth in mice without observable toxicity.

Molecular Weight	820.37
Formula	C45H50ClN7O6
CAS No.	2222111-87-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (121.90 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Transcription Factor-Targeted Compound Library Nuclear Receptor Compound Library Bioactive Compound Library Anti-Prostate Cancer Compound Library Endocrinology-Hormone Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

ARD-2128 2222111-87-5 Endocrinology/Hormones Androgen Receptor orally AR-regulated bioavailable inhibit Inhibitor prostate ARD2128 cancer tumor ARD 2128 PROTACs inhibitor

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