ARD-2128

SKU: orb1303496

Description

ARD-2128 is a potent, orally active PROTAC degrader of the androgen receptor (AR). It effectively reduces AR protein levels, inhibits AR-driven gene expression, and suppresses tumor growth in prostate cancer models, demonstrating utility for both in vitro and in vivo research applications.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2222111-87-5
• MW: 820.37
• Purity: 99.72% (May vary between batches)
• Formula: C₄₅H₅₀ClN₇O₆
• SMILES: O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=C(C2)N4CCC(CN5CCN(CC5)C6=CC=C(C(N[C@@H]7C(C)(C)[C@@H](OC8=CC(Cl)=C(C#N)C=C8)C7(C)C)=O)C=C6)CC4
• Target: Androgen Receptor,PROTACs
• Solubility: DMSO:100 mg/mL (121.9 mM)

Bioactivity

• Target IC50:
  LNCaP cells:5 μM (IC50)|VCaP:4 nM (IC50)
• 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 . 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% . 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 . 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.
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• 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 . 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 . This finding is further corroborated by a Cell Viability Assay , which demonstrates that ARD-2128 effectively diminishes AR protein levels and facilitates AR degradation in the VCaP cell line under the specified conditions.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, orally, Inhibitor, cancer, bioavailable, ARD2128, ARD-2128, ARD 2128, AR-regulated, Androgen Receptor, AndrogenReceptor, prostate, PROTACs, tumor

Compound Identifiers

PubChem CID

140861143