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Darolutamide

Catalog No. T6915 CAS 1297538-32-9

Synonyms: ODM-201, BAY-1841788

Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).

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Darolutamide, CAS 1297538-32-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 107.00
10 mg	In stock	$ 169.00
25 mg	In stock	$ 279.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 590.00
500 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.62%

Purity: 99.14%

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Description	Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).
Targets&IC50	Androgen receptor:11 nM(Ki)
In vitro	In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. [1]
In vivo	In mice bearing VCaP xenografts, ODM-201 (50?mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. [1]
Kinase Assay	AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C.
Cell Research	VCaP cells are treated with a submaximal concentration of mibolerone (0.1?nM) and increasing concentrations of test compounds in steroid-free assay medium supplemented with 4?mM GlutaMAX. After a 4-day incubation with the compounds, cell viability is measured using a WST-1 cell proliferation assay. To rule out non-AR –mediated toxicity, AR-negative PC cells (DU-145) and lung cancer cells (H1581) are treated with an increasing concentration of ODM-201, and cell viability is measured as described above.(Only for Reference)

Synonyms	ODM-201, BAY-1841788
Molecular Weight	398.85
Formula	C19H19ClN6O2
CAS No.	1297538-32-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 74 mg/mL (185.5 mM)

Ethanol: 36 mg/mL (90.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Moilanen AM, et al. Sci Rep. 2015, 5:12007. doi: 10.1038/srep12007.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library EMA Approved Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Targeted Therapy Drug Library Transcription Factor-Targeted Compound Library FDA-Approved Drug Library

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Keywords

Darolutamide 1297538-32-9 Endocrinology/Hormones Androgen Receptor Inhibitor ODM-201 ODM201 inhibit BAY1841788 ODM 201 BAY 1841788 BAY-1841788 inhibitor

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