Ketodarolutamide-d6
Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells. Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs. Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer.
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- Formule: C19H11D6ClN6O2
- Masse moléculaire:402.87
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Masse moléculaire 402.87
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Formule C19H11D6ClN6O2
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SMILES
ClC1=C(C=CC(C2=NN(C([2H])([2H])C(C([2H])([2H])[2H])([2H])NC(C3=NNC(C(C)=O)=C3)=O)C=C2)=C1)C#N
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Synonyms
BAY 1896953-d6; ORM-15341-d6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (248.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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.
Pureté et documentation
Références
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4822 mL | 12.4110 mL | 24.8219 mL | 62.0548 mL |
| 5 mM | 0.4964 mL | 2.4822 mL | 4.9644 mL | 12.4110 mL | |
| 10 mM | 0.2482 mL | 1.2411 mL | 2.4822 mL | 6.2055 mL | |
| 15 mM | 0.1655 mL | 0.8274 mL | 1.6548 mL | 4.1370 mL | |
| 20 mM | 0.1241 mL | 0.6205 mL | 1.2411 mL | 3.1027 mL | |
| 25 mM | 0.0993 mL | 0.4964 mL | 0.9929 mL | 2.4822 mL | |
| 30 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0685 mL | |
| 40 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5514 mL | |
| 50 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.2411 mL | |
| 60 mM | 0.0414 mL | 0.2068 mL | 0.4137 mL | 1.0342 mL | |
| 80 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7757 mL | |
| 100 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6205 mL |
Ketodarolutamide-d6 Related Classifications
HY-19337S1 Related Classifications
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Keywords
- Ketodarolutamide-d6
- BAY 1896953-d6
- ORM-15341-d6
- Isotope-Labeled Compounds
- Androgen Receptor
- androgen receptor (AR) antagonist
- nonsteroidal high-affinity competitive full antagonist
- inhibits testosterone-induced AR nuclear translocation
- suppresses AR-dependent cell proliferation
- antitumor activity
- AR-HEK293 cells
- U2-OS cells
- HS-HEK293 cells
- LNCaP cells
- VCaP cells
- DU-145 cells
- H1581 cells
- castrated male nude mice
- orthotopic VCaP tumor-bearing nude mice
- BalbC mice
- prostate cancer
- castration-resistant prostate cancer (CRPC)
- Inhibitor
- inhibitor
- inhibit