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ARD-2128 

Cat. No.: HY-132292
Handling Instructions

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.

For research use only. We do not sell to patients.

ARD-2128 Chemical Structure

ARD-2128 Chemical Structure

CAS No. : 2222111-87-5

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Description

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].

MCE 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].

MCE 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.
Molecular Weight

820.37

Formula

C₄₅H₅₀ClN₇O₆

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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ARD-2128
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HY-132292
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