Bavdegalutamide (Synonyms: ARV-110)

Name: Bavdegalutamide
Brand: MedChemExpress
SKU: HY-138641
Rating: 5.0 (8 reviews)

Cat. No.: HY-138641 Purity: 98.99%: Data Sheet
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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)).

For research use only. We do not sell to patients.

CAS No. : 2222112-77-6

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

8 Publications Citing Use of MCE Bavdegalutamide

Bio/Physico-chemical Assay

: 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.

: 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).

: Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2024 Jul 11;16(7):924.; 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 Nov 22;16(12):1499.; XRPD measurements of ARV-110 are crystalline, PVA 4-88, a physical mixture, and milled VCM discs. The y-axis represents an offset.

: Bavdegalutamide purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2024 Jul 11;16(7):924.; 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

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)).

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

Molecular Weight

812.29

Formula

C₄₁H₄₃ClFN₉O₆

CAS No.

2222112-77-6

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.64%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (243 KB) HNMR (277 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[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

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

Bavdegalutamide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bavdegalutamide2222112-77-6ARV-110ARV110ARV 110PROTACsAndrogen Receptorandrogenreceptorprostatecancermetastaticcastration-resistant prostate cancerInhibitorinhibitorinhibit

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Bavdegalutamide (Synonyms: ARV-110)

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Bavdegalutamide Related Antibodies

8 Publications Citing Use of MCE Bavdegalutamide

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Purity & Documentation

References

Customer Review

Bavdegalutamide Related Antibodies

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Complete Stock Solution Preparation Table

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