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Luxdegalutamide

Name: Luxdegalutamide
Brand: TargetMol
SKU: T75129
Price: 768 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: ARV-766) Copy Product Info

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Synonyms: ARV-766

Catalog No. T75129 Copy Product Info

Purity: 99.95%

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Luxdegalutamide (ARV-766) is a PROTAC and a protein degrader targeting the androgen receptor, capable of effectively degrading wild-type and drug-resistant mutants including L702H, H875Y, and T878A. With oral bioactivity and cell permeability, this compound is used in castration-resistant prostate cancer research and exhibits significant antitumor activity.

Cas No. 2750830-09-0

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Pack Size	Price	USA Stock	Global Stock
1 mg	$318	In Stock	In Stock
5 mg	$768	In Stock	In Stock
10 mg	Inquiry	In Stock	In Stock
25 mg	Inquiry	In Stock	In Stock
50 mg	Inquiry	Inquiry	Inquiry
100 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:99.95%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Luxdegalutamide (ARV-766) is a PROTAC and a protein degrader targeting the androgen receptor, capable of effectively degrading wild-type and drug-resistant mutants including L702H, H875Y, and T878A. With oral bioactivity and cell permeability, this compound is used in castration-resistant prostate cancer research and exhibits significant antitumor activity.
Targets & IC50	P-gp:> 5 μM (monolayer assay), BCRP:1.55 μM (monolayer assay), BCRP:0.21 μM (vesicle assay), P-gp:0.23 μM (vesicle assay)
In vitro	Methods: Human primary hepatocytes were treated with various concentrations of Luxdegalutamide (0.03–30 μM) for 48 hours, and mRNA expression levels of CYP1A2, 2B6, 2C9, 2C8, and CYP3A4 were detected. Results: Luxdegalutamide induced CYP3A4 and CYP2C8 mRNA expression, but did not induce CYP1A2, 2B6, or 2C9 mRNA expression, indicating that this drug essentially does not cause cytochrome P450 (CYP) and transporter-mediated drug-drug interactions (DDI). [1]
In vivo	Luxdegalutamide (ARV-766) significantly and dose-dependently inhibits tumor growth in mouse LNCaP and VCaP xenograft models.[2]
Synonyms	ARV-766

Chemical Properties

Molecular Weight	807.95
Formula	C₄₅H₅₄FN₇O₆
Cas No.	2750830-09-0
Smiles	O([C@H]1C(C)(C)[C@H](NC(=O)C2=CC=C(C=C2)N3CCC(CN4CCN(CC4)C5=CC(F)=C(C(N[C@@H]6C(=O)NC(=O)CC6)=O)C=C5)CC3)C1(C)C)C7=CC(OC)=C(C#N)C=C7

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 250 mg/mL (309.43 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.2377 mL	6.1885 mL	12.3770 mL	61.8850 mL
5 mM	0.2475 mL	1.2377 mL	2.4754 mL	12.3770 mL
10 mM	0.1238 mL	0.6189 mL	1.2377 mL	6.1885 mL
20 mM	0.0619 mL	0.3094 mL	0.6189 mL	3.0943 mL
50 mM	0.0248 mL	0.1238 mL	0.2475 mL	1.2377 mL
100 mM	0.0124 mL	0.0619 mL	0.1238 mL	0.6189 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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

Keywords

PROTACLuxdegalutamideARV766ARV 766AndrogenReceptorAndrogen Receptor

Related Tags: Luxdegalutamide chemical structure | Luxdegalutamide in vivo | Luxdegalutamide in vitro | Luxdegalutamide formula | Luxdegalutamide molecular weight