Bavdegalutamide

SKU: orb1306042

Description

Bavdegalutamide (ARV-110) is an orally bioavailable PROTAC degrader targeting the androgen receptor (AR). It effectively degrades clinically relevant AR mutants, even in high androgen conditions, and is suitable for in vitro and in vivo prostate cancer research, demonstrating a favorable preclinical safety profile.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2222112-77-6
• MW: 812.29
• Purity: 99.96% (May vary between batches)
• Formula: C₄₁H₄₃ClFN₉O₆
• SMILES: O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC(F)=C(C2)N4CCN(CC5CCN(CC5)C6=CC=C(C(N[C@@H]7CC[C@@H](OC8=CC(Cl)=C(C#N)C=C8)CC7)=O)N=N6)CC4
• Target: PROTACs,Androgen Receptor
• Solubility: DMSO:41.67 mg/mL (51.3 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (1.23 mM)

Bioactivity

• In Vivo:
  METHODS: The mean plasma concentration-time profiles of Bavdegalutamide (ARV-110) were measured in rats and mice after intravenous administration of Bavdegalutamide (2 mg/kg, intravenous injection) and (5 mg/kg, oral administration) using the developed LC-MS/MS method. RESULTS: In rats, after intravenous injection of Bavdegalutamide, the calculated total clearance (CL) value was 413.6 ± 31.7 mL/h/kg, and the steady-state (VSS) value (5775 ± 320 mL/kg) indicated that ARV-110 was well distributed in tissues; after oral administration, the peak plasma concentration (Cmax) value was 110.5 ± 9.2 ng/mL, at 5.5 ± 1.9 hours, and the oral bioavailability of ARV-110 in rats was moderate (23.8%); after intravenous administration in mice, the CL value of ARV-110 was lower than the hepatic blood flow rate of mice (90 mL/min/kg), and Bavdegalutamide showed a relatively large VSS value (2366 ± 402.2 mL/kg), indicating that the drug was mainly confined to tissues; after oral administration, the Cmax value was 612.0 ± 88.38 ng/mL. METHODS: Bavdegalutamide (1 mg/kg, orally, once a day) was used to treat xenograft model mice, and the degree of AR degradation and tumor growth in the mice were observed. RESULTS: With over 90% AR degradation in mice, Bavdegalutamide achieved significant inhibition of tumor growth and AR signaling in both intact and castrated conditions.
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• In Vitro:
  Bavdegalutamide (ARV-110) completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) of < 1 nM.

Storage & Handling

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

Alternative Names

ARV 110, ARV110, ARV-110, Bavdegalutamide, androgen, AndrogenReceptor, Androgen Receptor, cancer, castration-resistant prostate cancer, Inhibitor, inhibit, metastatic, prostate, receptor

Compound Identifiers

PubChem CID

134414307