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Proxalutamide (GT0918) Androgen Receptor antagonist

Name: Proxalutamide (GT0918)
SKU: S9898
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9898

Proxalutamide (GT0918), a second-generation androgen receptor antagonist, binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.

Chemical Structure

Molecular Weight: 517.50

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S989801 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 98.95%

98.95

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Glucocorticoid Receptor ACE RAAS Opioid Receptor THR PGES Aromatase 5-alpha Reductase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
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Chemical Information, Storage & Stability

Molecular Weight	517.50	Formula	C₂₄H₁₉F₄N₅O₂S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1398046-21-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1(C)N(C(=S)N(C1=O)C2=C(F)C(=C(C=C2)C#N)C(F)(F)F)C3=CN=C(CCCC4=NC=CO4)C=C3

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (193.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.830mg/ml (1.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Androgen Receptor ^[1] (in the AR competive binding assay) 32 nM
In vitro	Proxalutamide (GT0918), a novel 2nd generation AR antagonist, binds to the ligand-binding domain of AR, with an IC50 of 32 nM in the AR competitive binding assays. It can block AR transcriptional activity, reduce AR protein levels, and obviously inhibit PCa growth in vitro. ^[1]
In vivo	Regardless of whether administered by the intragastric or intravenous route, the elimination half-life of Proxalutamide (GT0918) in rats is approximately 2 h. The maximum plasma concentration of this compound can reach 2 μg/mL or higher, and its oral absolute bioavailability is approximately 80%. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/32460179/ [2] https://pubmed.ncbi.nlm.nih.gov/33169448/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04870606	Completed	Efficacy and Safety	Suzhou Kintor Pharmaceutical Inc	March 5 2021	Phase 3
NCT03899467	Completed	Metastatic Castrate Resistant Prostate Cancer (mCRPC)\|Metastatic Hormone-Sensitive Prostate Cancer (mHSPC)	Suzhou Kintor Pharmaceutical Inc	May 30 2019	Phase 2

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