Art. -Nr.: HY-138641

Bavdegalutamide

(Synonyms: ARV-110)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986)).
(Pink: Androgen Receptor ligand (HY-168299); Blue: Cereblon ligand (HY-W093272); Black: linker (HY-W091986)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.99%
CAS. Nr.: 2222112-77-6
Formel: C₄₁H₄₃ClFN₉O₆
Molecular Weight:812.29

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Bavdegalutamide Chemical Structure

CAS. Nr.: 2222112-77-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986))^[1]. (Pink: Androgen Receptor ligand (HY-168299); Blue: Cereblon ligand (HY-W093272); Black: linker (HY-W091986)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	3.9 μM Compound: ARV110	Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38512060]
CWR22R	IC₅₀	316 nM Compound: ARV-110	Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
CWR22R	IC₅₀	316 nM Compound: ARV-110	Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
LNCaP	IC₅₀	124 nM Compound: ARV-110	Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
LNCaP	IC₅₀	124 nM Compound: ARV-110	Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
LNCaP	IC₅₀	18.5 nM Compound: 5; ARV-110	Growth inhibition in human LNCaP cells assessed as reduction in cell viability Growth inhibition in human LNCaP cells assessed as reduction in cell viability	[PMID: 37683104]
LNCaP	IC₅₀	32 nM Compound: 11; ARV-110	Growth inhibition in human LNCaP cells incubated for 4 days by WST-8 assay Growth inhibition in human LNCaP cells incubated for 4 days by WST-8 assay	[PMID: 37382562]
LNCaP	IC₅₀	33.1 nM Compound: 8; ARV-110	Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability by WST-8 assay Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability by WST-8 assay	[PMID: 34473519]
VCaP	IC₅₀	125 nM Compound: ARV-110	Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
VCaP	IC₅₀	16.2 nM Compound: 5; ARV-110	Growth inhibition in human VCaP cells Growth inhibition in human VCaP cells	[PMID: 37683104]
VCaP	IC₅₀	219 nM Compound: ARV-110	Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
VCaP	IC₅₀	30.4 nM Compound: 8; ARV-110	Growth inhibition of human VCaP cells assessed as cell viability by WST-8 assay Growth inhibition of human VCaP cells assessed as cell viability by WST-8 assay	[PMID: 34473519]
VCaP	IC₅₀	41 nM Compound: 11; ARV-110	Growth inhibition in human VCaP cells incubated for 4 days by WST-8 assay Growth inhibition in human VCaP cells incubated for 4 days by WST-8 assay	[PMID: 37382562]

In Vitro

Bavdegalutamide completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC₅₀) < 1 nM^[1].
Bavdegalutamide (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner^[1].
Bavdegalutamide (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner^[2].
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^[2].
Bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2222112-77-6
Appearance Solid
Molecular Weight 812.29
Formel C₄₁H₄₃ClFN₉O₆
Color Light yellow to yellow
SMILES

O=C(C1=NN=C(N2CCC(CN3CCN(C4=CC5=C(C(N(C(CC6)C(NC6=O)=O)C5=O)=O)C=C4F)CC3)CC2)C=C1)N[C@H]7CC[C@H](OC8=CC=C(C#N)C(Cl)=C8)CC7
Synonyms

ARV-110
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (8)

All WBBio/Physico-chemical Assay

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Journal Impact Factor

Clin Cancer Res

Clinical Context Shapes the Relationship between Genomic Alterations and Response to AR Inhibitors and Chemotherapy in Metastatic Prostate Cancer. [Abstract]

2025 Apr 14. PMID: 40227200

Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2025 Apr 14. [Abstract]

Trends toward increased PI3K–AKT signaling were observed in LNCaP cells treated with ARV-110, a PROTAC-based AR degrader.
Anal Chem

Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]

2025 Dec 2;97(47):26097-26107. PMID: 41243541

Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Anal Chem. 2025 Dec 2;97(47):26097-26107. [Abstract]

Calculated Acidic Methine pK_a, and Measured Half-Lives for PROTACs (ARV-110, compound 19) at 37℃ (Mean ± SD, n = 3) in 0.1 M Phosphate Buffer (D2O, pD 7.8).
Pharmaceutics

CC-90009, a Cereblon E3 Ligase Modulator, Exhibits Antiviral Efficacy Against JEV In Vitro and In Vivo via Targeted Degradation of GSPT1 and Viral NS5 Protein. [Abstract]

2025 Nov 27;17(12):1524. PMID: 41471039
Pharmaceutics

Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol. [Abstract]

2024 Nov 22;16(12):1499. PMID: 39771478

Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2024 Nov 22;16(12):1499. [Abstract]

XRPD measurements of ARV-110 are crystalline, PVA 4-88, a physical mixture, and milled VCM discs. The y-axis represents an offset.
Pharmaceutics

Use of Poly(vinyl alcohol) in Spray-Dried Dispersions: Enhancing Solubility and Stability of Proteolysis Targeting Chimeras. [Abstract]

2024 Jul 11;16(7):924. PMID: 39065621

Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2024 Jul 11;16(7):924. [Abstract]

X-ray powder diffractograms of the PROTAC ARV-110 and the physical mixture (PM) of ARV-110 with PVA containing 30% drug load as well as the spray-dried dispersion (SDD) of ARV-110 with PVA containing 30% drug load at t = 0 and after storage for 4 weeks at 5 °C (t = 4 W 5 °C).

Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2024 Jul 11;16(7):924. [Abstract]

Scanning electron microscopy images of the PROTAC ARV-110 and the physical mixture (PM) of ARV-110 with PVA containing 30% drug load as well as the spray-dried dispersion (SDD) of ARV-110 with PVA containing 30% drug load at 5000× magnification.
Drug Metab Dispos

Applications of contemporary tools to measure plasma protein binding of targeted protein degraders. [Abstract]

2025 May;53(5):100066. PMID: 40286535
Arch Biochem Biophys

Chemical degrader enhances the treatment of androgen receptor-positive triple-negative breast cancer. [Abstract]

2022 May 30;721:109194. PMID: 35337811
Research Square Print

November 18th, 2022

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 26.67 mg/mL (32.83 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2311 mL

6.1554 mL

12.3109 mL

5 mM

0.2462 mL

1.2311 mL

2.4622 mL

10 mM

0.1231 mL

0.6155 mL

1.2311 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.79 mg/mL (0.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.79 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (12.31 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]. Taavi K Neklesa,et al. ARV-110: an oral androgen receptor PROTAC degrader for prostate cancer. GU ASCO 2019

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2311 mL	6.1554 mL	12.3109 mL	30.7772 mL
	5 mM	0.2462 mL	1.2311 mL	2.4622 mL	6.1554 mL
	10 mM	0.1231 mL	0.6155 mL	1.2311 mL	3.0777 mL
	15 mM	0.0821 mL	0.4104 mL	0.8207 mL	2.0518 mL
	20 mM	0.0616 mL	0.3078 mL	0.6155 mL	1.5389 mL
	25 mM	0.0492 mL	0.2462 mL	0.4924 mL	1.2311 mL
	30 mM	0.0410 mL	0.2052 mL	0.4104 mL	1.0259 mL

Keywords

Bavdegalutamide

8 Cited Publications

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Bavdegalutamide

PROTAC Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Bavdegalutamide

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bavdegalutamide

PROTAC Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Bavdegalutamide

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bavdegalutamide Related Classifications

HY-138641 Related Classifications