Bavdegalutamide
Based on 10 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: Androgen Receptor ligand (HY-168299); Blue: Cereblon ligand (HY-W093272); Black: linker (HY-W091986)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.99%
- CAS No.: 2222112-77-6
- Formule: C41H43ClFN9O6
- Masse moléculaire:812.29
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bavdegalutamide
More- Clin Cancer Res. 2025 Apr 14. [Abstract]
- Anal Chem. 2025 Dec 2;97(47):26097-26107. [Abstract]
- Pharmaceutics. 2025 Nov 27;17(12):1524. [Abstract]
- Pharmaceutics. 2024 Nov 22;16(12):1499. [Abstract]
- Pharmaceutics. 2024 Jul 11;16(7):924. [Abstract]
- Drug Metab Dispos. 2026 Jul 14;54(8):100365.
- Drug Metab Dispos. 2026 Jul 17.
- Drug Metab Dispos. 2025 May;53(5):100066. [Abstract]
- Arch Biochem Biophys. 2022 May 30;721:109194. [Abstract]
- Research Square Print. November 18th, 2022
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
3.9 μM
Compound: ARV110
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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
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[PMID: 38512060] |
| CWR22R | IC50 |
316 nM
Compound: ARV-110
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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
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[PMID: 38477974] |
| CWR22R | IC50 |
316 nM
Compound: ARV-110
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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
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[PMID: 38530938] |
| LNCaP | IC50 |
124 nM
Compound: ARV-110
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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
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[PMID: 38477974] |
| LNCaP | IC50 |
124 nM
Compound: ARV-110
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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
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[PMID: 38530938] |
| LNCaP | IC50 |
18.5 nM
Compound: 5; ARV-110
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Growth inhibition in human LNCaP cells assessed as reduction in cell viability
Growth inhibition in human LNCaP cells assessed as reduction in cell viability
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[PMID: 37683104] |
| LNCaP | IC50 |
32 nM
Compound: 11; ARV-110
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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
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[PMID: 37382562] |
| LNCaP | IC50 |
33.1 nM
Compound: 8; ARV-110
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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
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[PMID: 34473519] |
| VCaP | IC50 |
125 nM
Compound: ARV-110
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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
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[PMID: 38477974] |
| VCaP | IC50 |
16.2 nM
Compound: 5; ARV-110
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Growth inhibition in human VCaP cells
Growth inhibition in human VCaP cells
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[PMID: 37683104] |
| VCaP | IC50 |
219 nM
Compound: ARV-110
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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
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[PMID: 38530938] |
| VCaP | IC50 |
30.4 nM
Compound: 8; ARV-110
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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
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[PMID: 34473519] |
| VCaP | IC50 |
41 nM
Compound: 11; ARV-110
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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
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[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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2222112-77-6
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Appearance Solid
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Masse moléculaire 812.29
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Formule C41H43ClFN9O6
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Color Light yellow to yellow
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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
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Synonyms
ARV-110
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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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.
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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 pKa, 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).
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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.
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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.
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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 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline 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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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.
| 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 |
Bavdegalutamide Related Classifications
HY-138641 Related Classifications
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