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.
For research use only. We do not sell to patients.
- Formula: C19H11D6ClN6O2
- Molecular Weight:402.87
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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.
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
-
Molecular Weight 402.87
-
Formula C19H11D6ClN6O2
-
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
-
Synonyms
BAY 1896953-d6; ORM-15341-d6
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- 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