Luxdegalutamide
Based on 3 publication(s) in Google Scholar
Luxdegalutamide (ARV-766) is an orally active PROTAC that induces the degradation of the androgen receptor (AR) via cereblon (CRBN). Luxdegalutamide 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.
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- Purity : 98.99%
- CAS No.: 2750830-09-0
- 화학식: C45H54FN7O6
- 분자량:807.95
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Luxdegalutamide
MoreAll PROTACs Isoforms
More
Biological Activity
제품 설명
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.
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Cell Line:Human hepatocytes
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Concentration:0.03-30 μM
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Incubation Time:48 h
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Result:Didn't induce mRNA expression of CYP1A2, 2B6, and 2C9 but induced mRNA expression of CYP3A4 and CYP2C8.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2750830-09-0
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Appearance Solid
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분자량 807.95
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화학식 C45H54FN7O6
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Color White to off-white
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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
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Synonyms
ARV-766; JSB462
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Anal Chem
Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]2025 Dec 2;97(47):26097-26107. PMID: 41243541 -
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Asian J Androl
2025 Mar 1;27(2):144-155. PMID: 39558858
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 |
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| 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 |
Luxdegalutamide Related Classifications
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