ARV-110

SKU: orb1218412

Description

ARV-110 is an oral degrader of androgen receptor PROTAC for prostate cancer treatment.

Key Properties

• CAS Number: 2222112-77-6
• MW: 812.29
• Purity: >98% (HPLC)
• Formula: C₄₁H₄₃ClFN₉O₆
• SMILES: ClC1=CC(O[C@H]2CC[C@@H](CC2)NC(C3=CC=C(N=N3)N4CCC(CC4)CN5CCN(CC5)C6=CC(C(N7C8CCC(NC8=O)=O)=O)=C(C=C6F)C7=O)=O)=CC=C1C#N
• Target: Androgen Receptor (AR)
• Solubility: DMSO:46 mg/mL (56.63 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Bavdegalutamide (oral gavage; 1 mg/kg; QD) exhibits a greater than 90% AR degradation In vivo. In LNCaP, VCaP and prostate cancer patient derived xenograft (PDX) models, Bavdegalutamide also exhibits significant inhibition of tumor growth and AR signaling. Bavdegalutamide (oral gavage; 3 or 10 mpk; 30 days) demonstrates In vivo efficacy and reduction of AR-target gene expression in a long term, castrate, enzalutamide-resistant VCaP tumor model. The TGI are 70% and 60% for 3 mpk and 10 mpk dosage. Respectively.
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• In Vitro:
  Bavdegalutamide completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) < 1 nM. Bavdegalutamide (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner. Bavdegalutamide (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner. Bavdegalutamide (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations. Bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876 L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Androgen Receptor (AR)