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Proxalutamide

Name: Proxalutamide
Brand: TargetMol
SKU: T15445
Price: 71 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15445Cas No. 1398046-21-3

Alias GT0918

Proxalutamide is a potent antagonist of the androgen receptor (AR).

Proxalutamide

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Purity: 99.11%

Catalog No. T15445Alias GT0918Cas No. 1398046-21-3

Proxalutamide is a potent antagonist of the androgen receptor (AR).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$71	In Stock	In Stock
5 mg	$173	In Stock	In Stock
10 mg	$265	In Stock	In Stock
25 mg	$529	In Stock	In Stock
50 mg	$810	In Stock	In Stock
100 mg	$1,180	In Stock	In Stock
200 mg	$1,580	-	In Stock
1 mL x 10 mM (in DMSO)	$197	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.11%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Proxalutamide is a potent antagonist of the androgen receptor (AR).
In vitro	Proxalutamide inhibits the proliferation of hormone-sensitive CaP cells and more potently inhibits the proliferation of CRPC cells. Proxalutamide inhibits the growth of AR-positive breast cancer cells. Proxalutamide more effectively inhibits androgen binding with AR's ligand-binding domain than Bicalutamide (11.4x) and MDV3100 (3.5x). Proxalutamide displays stronger potency to block AR function of gene transcription than Bicalutamide (~5-10) and MDV3100 (2-5x) while maintaining full antagonism in CRPC cells, in both hormone-sensitive (LNCaP) and CRPC (C4-2) cancer cells. Proxalutamide has minimum effects on the growth of AR-negative CaP cells (PC-3 and DU145), showing it is a selective AR pathway inhibitor. Proxalutamide impairs androgen stimulates AR translocation to cell nuclei hence blocks its binding DNA and shuts down the downstream oncogenic signaling and Proxalutamide also causes AR downregulation in prostate cancer cells [1].
In vivo	The mean Proxalutamide (GT0918) half-life estimate from the pHM-SD tablets (7.9±2.2 h) was similar to that of the conventional tablets (8.4±0.5 h), remaining consistent with the following pharmacokinetic theory: the extent and rate of absorption should not affect elimination. The relative bioavailability (frel) of the pHM-SD tablets is 125.6% of that for the conventional tablets on average, revealing that the bioavailability of the former is higher. The tmax for the pHM-SD and conventional tablets are 0.9±0.4 h and 2.5±1.1 h, respectively, meaning that the pHM-SD tablets dissolve more quickly than the conventional tablets. The mean Cmax and the AUC0-36 are 5.1±2.4 μg/mL and 38.3±8.2 μgh/mL for the pHM-SD tablets versus 3.1±1.5 μg/mL and 42.1±22.3 μgh/mL for conventional tablets, respectively [2].
Synonyms	GT0918

Chemical Properties

Molecular Weight	517.5
Formula	C₂₄H₁₉F₄N₅O₂S
Cas No.	1398046-21-3
Smiles	CC1(C)N(C(=S)N(C1=O)c1ccc(C#N)c(c1F)C(F)(F)F)c1ccc(CCCc2ncco2)nc1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (193.24 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9324 mL	9.6618 mL	19.3237 mL	96.6184 mL
5 mM	0.3865 mL	1.9324 mL	3.8647 mL	19.3237 mL
10 mM	0.1932 mL	0.9662 mL	1.9324 mL	9.6618 mL
20 mM	0.0966 mL	0.4831 mL	0.9662 mL	4.8309 mL
50 mM	0.0386 mL	0.1932 mL	0.3865 mL	1.9324 mL
100 mM	0.0193 mL	0.0966 mL	0.1932 mL	0.9662 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc