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Bavdegalutamide

Catalog No. T22263 CAS 2222112-77-6

Synonyms: ARV-110

Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR). Bavdegalutamide can be used in studies about prostate cancer. Bavdegalutamide shows oral activity and selectivity and facilitates the ubiquitination and degradation of AR.

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Bavdegalutamide, CAS 2222112-77-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 85.00
5 mg	In stock	$ 139.00
10 mg	In stock	$ 216.00
25 mg	In stock	$ 424.00
50 mg	In stock	$ 545.00
100 mg	In stock	$ 785.00
200 mg	In stock	$ 1,090.00

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Purity: 99.04%

Purity: 98.32%

Purity: 97.17%

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Description	Bavdegalutamide (ARV-110) is a PROTAC degrader of androgen receptor (AR). Bavdegalutamide can be used in studies about prostate cancer. Bavdegalutamide shows oral activity and selectivity and facilitates the ubiquitination and degradation of AR.
In vitro	Bavdegalutamide effectively degrades AR in all tested cell lines, achieving a 50% degradation concentration (DC50) of <1 nM[1]. In LNCaP cells, Bavdegalutamide induces dose-dependent AR degradation within the concentration range of 0.01 nM to 300 nM[1]. In VCaP cells, a time-dependent AR degradation is observed when treated with Bavdegalutamide at 10 nM for durations ranging from 0.5 to 24 hours[1]. Treatment with Bavdegalutamide at concentrations between 10 nM and 1000 nM results in the suppression of AR-target gene PSA expression, inhibition of AR-dependent cell proliferation, and induction of apoptosis at low nanomolar concentrations[1]. Bavdegalutamide effectively degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V, and H874V) and maintains activity in a high androgen environment (R1881, 100 nM) in VCaP cells[1].
In vivo	Administered through oral gavage at a dose of 1 mg/kg once daily, Bavdegalutamide demonstrates over 90% AR degradation in vivo. In LNCaP, VCaP, and patient-derived xenograft (PDX) models of prostate cancer, Bavdegalutamide significantly inhibits tumor growth and AR signaling[1]. In a long-term, castrate, enzalutamide-resistant VCaP tumor model, oral gavage of Bavdegalutamide at doses of 3 or 10 mpk for 30 days shows in vivo efficacy and reduces AR-target gene expression. The tumor growth inhibition (TGI) is 70% and 60% for 3 mg/kg and 10 mg/kg dosages, respectively[1].

Synonyms	ARV-110
Molecular Weight	812.29
Formula	C41H43ClFN9O6
CAS No.	2222112-77-6

Storage

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

Solubility Information

DMSO: 46 mg/mL (56.63 mM), Sonication is recommended.

References and Literature

1. Taavi Neklesa, et al. ARV-110: An androgen receptor PROTAC degrader for prostate cancer. American Association for Cancer Research. 2018. 78 (13): pp. 5236. 2. Qi SM, et al. PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy. Front Pharmacol. 2021 May 7;12:692574.

Citations

1. Sun R, Yan B, Li H, et al.Androgen receptor variants confer castration resistance in prostate cancer by counteracting antiandrogen-induced ferroptosis.Cancer Research.2023 2. Xiao M, Ha S, Zhu J, et al.Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer.Journal of Medicinal Chemistry.2024

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Compound Library Orally Active Compound Library Bioactive Compound Library Clinical Compound Library Bioactive Compounds Library Max Transcription Factor-Targeted Compound Library

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Keywords

Bavdegalutamide 2222112-77-6 Endocrinology/Hormones Androgen Receptor ARV 110 prostate castration-resistant prostate cancer receptor androgen ARV-110 ARV110 inhibit cancer Inhibitor metastatic inhibitor

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