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

Luxdegalutamide  (Synonyms: ARV-766)

Cat. No.: HY-153342 Purity: 98.94% ee.: 98.11%
COA Handling Instructions

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Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer.

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

Luxdegalutamide Chemical Structure

Luxdegalutamide Chemical Structure

CAS No. : 2750830-09-0

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1 mg USD 386 In-stock
5 mg USD 1160 In-stock
10 mg USD 1500 In-stock
25 mg USD 2150 In-stock
50 mg USD 2800 In-stock
100 mg USD 3750 In-stock
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Based on 1 publication(s) in Google Scholar

Luxdegalutamide Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer[1][2].
IC50 & Target

Androgen Receptor[1].
In Vitro

Luxdegalutamide (0.03-30 μM, 48 h) induces the expression of CYP3A4 and CYP2C8 mRNA instead of CYP1A2, 2B6, and 2C9 mRNA, with little effect on cytochrome P450 (CYP) and transporter mediated drug interactions (DDI)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Luxdegalutamide Related Antibodies

RT-PCR[1].

Cell Line: Human hepatocytes
Concentration: 0.03-30 μM
Incubation Time: 48 h
Result: Didn't induce mRNA expression of CYP1A2, 2B6, and 2C9 but induced mRNA expression of CYP3A4 and CYP2C8.
In Vivo

Luxdegalutamide exhibits anti-tumor activity in mouse LNCaP and VCaP xenograft models[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

807.95

Formula

C45H54FN7O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)([C@@H](C1(C)C)NC(C2=CC=C(N3CCC(CC3)CN4CCN(C5=CC(F)=C(C=C5)C(N[C@@H]6C(NC(CC6)=O)=O)=O)CC4)C=C2)=O)[C@@H]1OC7=CC(OC)=C(C=C7)C#N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°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 : 100 mg/mL (123.77 mM; Need ultrasonic; 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 1.2377 mL 6.1885 mL 12.3770 mL
5 mM 0.2475 mL 1.2377 mL 2.4754 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)

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (3.09 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 98.94% ee.: 98.11%

COA (244 KB) HNMR (254 KB) RP-HPLC (266 KB) NP-HPLC (913 KB) LCMS (98 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 1.2377 mL 6.1885 mL 12.3770 mL 30.9425 mL
5 mM 0.2475 mL 1.2377 mL 2.4754 mL 6.1885 mL
10 mM 0.1238 mL 0.6189 mL 1.2377 mL 3.0943 mL
15 mM 0.0825 mL 0.4126 mL 0.8251 mL 2.0628 mL
20 mM 0.0619 mL 0.3094 mL 0.6189 mL 1.5471 mL
25 mM 0.0495 mL 0.2475 mL 0.4951 mL 1.2377 mL
30 mM 0.0413 mL 0.2063 mL 0.4126 mL 1.0314 mL
40 mM 0.0309 mL 0.1547 mL 0.3094 mL 0.7736 mL
50 mM 0.0248 mL 0.1238 mL 0.2475 mL 0.6189 mL
60 mM 0.0206 mL 0.1031 mL 0.2063 mL 0.5157 mL
80 mM 0.0155 mL 0.0774 mL 0.1547 mL 0.3868 mL
100 mM 0.0124 mL 0.0619 mL 0.1238 mL 0.3094 mL
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Luxdegalutamide 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:

Luxdegalutamide2750830-09-0ARV-766ARV766ARV 766PROTACsAndrogen Receptorandrogen receptorPROTACAR mutationprostatic cancerInhibitorinhibitorinhibit

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