2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. 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.

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

YM580

YM580 Chemical Structure

CAS No. : 262295-11-4

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YM580 Related Antibodies

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Description

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[1].

IC50 & TargetAndrogen Receptor

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)

In Vitro

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.

YM580 Related Antibodies
Parmacokinetics
Species Dose Route Note Cmax AUC0-t T1/2 CL
Rat[1] 3 nM p.o. plasma 702 ng/mL 21952 ng·h/mL 12.5 h 133 mL/h/kg
Rat[1] 3 nM p.o. prostate 1561 ng/mL 43215 h·ng/g 11.2 h 68.3 mL/h/kg
In Vivo

YM580 (0.3-30 mg/kg; p.o.; daily; 15 days) reduces ventral prostate weight and exhibits antiandrogenic effect in mature intact male Wistar rats[1].

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

Animal Model: Mature intact male Wistar rats (10-week-old)[1]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: p.o.; daily; 15 days
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.
Molecular Weight

471.41

Formula

C21H19F6N5O
CAS No.
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
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
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YM580 Related Classifications

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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:

YM580262295-11-4YM 580YM-580Androgen ReceptorARestrogen receptors αprogesterone receptorsventral prostatemature intact ratsWistar ratsAR/CHO#3 cellsprostate cancerglucocorticoid receptorsInhibitorinhibitorinhibit

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