product name ODM-201
Description: ODM-201 (also known as BAY-1841788) is a novel and potent androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM in competitive AR binding assays. In AR-HEK293 cells stably expressing full-length human AR (hAR) and an androgen-responsive luciferase reporter gene construct. In human U2-OS osteosarcoma cells expressing wtAR or mutant AR(F876L), AR(W741L), or AR(T877A), ODM-201 and ORM-15341 also functioned as full antagonists.
References: Sci Rep. 2015 Jul 3;5:12007.
398.85
Formula
C19H19ClN6O2
CAS No.
1297538-32-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: 38 mg/mL d (95.3 mM)
Solubility (In vivo)
Synonyms
BAY-1841788
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394758
| In Vitro |
In vitro activity: 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. Kinase Assay: 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: 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. |
|---|---|
| In Vivo | In mice bearing VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. |
| Animal model | BALB/c nude male mice bearing VCaP xenografts |
| Formulation & Dosage | Dissolved in Macrocol + propylene glycol +5% glucose (50:30:20, v/v/v); 50 mg/kg; p.o. administration |
| References | Sci Rep. 2015 Jul 3;5:12007. |
Related Posts
product name ODM-201
Description: ODM-201 (also known as BAY-1841788) is a novel and potent androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM in competitive AR binding assays. In AR-HEK293 cells stably expressing full-length human AR (hAR) and an androgen-responsive luciferase reporter gene construct. In human U2-OS osteosarcoma cells expressing wtAR or mutant AR(F876L), AR(W741L), or AR(T877A), ODM-201 and ORM-15341 also functioned as full antagonists.
References: Sci Rep. 2015 Jul 3;5:12007.
398.85
Formula
C19H19ClN6O2
CAS No.
1297538-32-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: 38 mg/mL d (95.3 mM)
Solubility (In vivo)
Synonyms
BAY-1841788
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394758
| In Vitro |
In vitro activity: 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. Kinase Assay: 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: 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. |
|---|---|
| In Vivo | In mice bearing VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. |
| Animal model | BALB/c nude male mice bearing VCaP xenografts |
| Formulation & Dosage | Dissolved in Macrocol + propylene glycol +5% glucose (50:30:20, v/v/v); 50 mg/kg; p.o. administration |
| References | Sci Rep. 2015 Jul 3;5:12007. |