Darolutamide (ODM-201)

Catalog No.S7559 Batch:S755902

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Technical Data

Formula

C19H19ClN6O2
Molecular Weight 398.85 CAS No. 1297538-32-9
Solubility (25°C)* In vitro DMSO 80 mg/mL (200.57 mM)
Ethanol 40 mg/mL (100.28 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
Targets
Androgen receptor [1]
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • Cell lines

    DU-145, H1581, and VCaP cells

  • Concentrations

    ~10 μM

  • Incubation Time

    4 days

  • Method

    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.
Animal Study:[1]
  • Animal Models

    BALB/c nude male mice bearing VCaP xenografts

  • Dosages

    50 mg/kg, bid

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1469]

Selleck's Darolutamide (ODM-201) has been cited by 14 publications

Loss of LCMT1 and biased protein phosphatase 2A heterotrimerization drive prostate cancer progression and therapy resistance [ Nat Commun, 2023, 14(1):5253] PubMed: 37644036
Loss of LCMT1 and biased protein phosphatase 2A heterotrimerization drive prostate cancer progression and therapy resistance [ Nat Commun, 2023, 14(1):5253] PubMed: 37644036
Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer [ Cancer Res, 2023, 83(3):456-470] PubMed: 36469363
Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models [ Pharmacol Res, 2023, 189:106692] PubMed: 36773708
Ferroptosis heterogeneity in triple-negative breast cancer reveals an innovative immunotherapy combination strategy [ Cell Metab, 2022, S1550-4131-2200411-9] PubMed: 36257316
A novel inhibitor of ARfl and ARv7 induces protein degradation to overcome enzalutamide resistance in advanced prostate cancer [ Acta Pharm Sin B, 2022, 12(11):4165-4179] PubMed: 36386477
An oral first-in-class small molecule RSK inhibitor suppresses AR variants and tumor growth in prostate cancer [ Cancer Sci, 2022, 113(5):1731-1738] PubMed: 35118769
Impact of Androgen Receptor Activity on Prostate-Specific Membrane Antigen Expression in Prostate Cancer Cells [ Int J Mol Sci, 2022, 23(3)1046] PubMed: 35162969
Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2 [ Proc Natl Acad Sci U S A, 2020, 202021450] PubMed: 33310900
Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC resistant to Second-Line Antiandrogen Therapy [ Mol Cancer Ther, 2020, molcanther.0417.2020] PubMed: 33277442

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.