2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Androgen Receptor
  4. Bavdegalutamide

Bavdegalutamide  (Synonyms: ARV-110)

Cat. No.: HY-138641 Purity: 98.76%
SDS COA Handling Instructions

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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)).

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

Bavdegalutamide Chemical Structure

Bavdegalutamide Chemical Structure

CAS No. : 2222112-77-6

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1 mg USD 55 In-stock
5 mg USD 169 In-stock
10 mg USD 250 In-stock
25 mg USD 470 In-stock
50 mg USD 700 In-stock
100 mg USD 1050 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Bavdegalutamide Related Antibodies

Top Publications Citing Use of Products

Customer Validation

These results were obtained using AlphaLISA™ SureFire® Ultra™ assays

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 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].

Cellular Effect
Cell Line Type Value Description References
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
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]
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.

Bavdegalutamide Related Antibodies
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.
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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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)

g

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%

SDS (393 KB)

COA (243 KB) HNMR (277 KB) LCMS (111 KB)

Handling Instructions (2659 KB)
References

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
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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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