YM580
YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer.
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- No. CAS: 262295-11-4
- Fòrmula: C21H19F6N5O
- Peso molecular:471.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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hAR 4.6 nM (Ki) |
rAR 6.2 nM (Ki) |
rat PR 3300 nM (Ki) |
human GR >100000 nM (Ki) |
human ERα >100000 nM (Ki) |
YM580 potently inhibits AR-mediated transcriptional activation in AR/CHO#3 cells, with an IC50 of 0.11 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mature intact male Wistar rats (10-week-old)[1]
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Dosage:0.3, 1, 3, 10, 30 mg/kg
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Administration:p.o.; daily; 15 days
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Result:Decreased ventral prostate weight in a dose-dependent manner with an ED50 of 2.2 mg/kg/day, and an inhibition rate of 67% at 10 mg/kg/day.
Exerted a maximum antiandrogenic effect comparable to surgical castration at 30 mg/kg/day.
Did not significantly elevate serum testosterone levels across all doses.
Exhibited good peripheral selectivity.
Chemical Information
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No. CAS 262295-11-4
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Peso molecular 471.41
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Fòrmula C21H19F6N5O
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SMILES
C[C@@H]1N(C2=CC(C(F)(F)F)=C(C#N)C=C2)C[C@@H](C)N(C(NC=3C=CC(C(F)(F)F)=NC3)=O)C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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