Chemical Property of ODM-201
Chemical Property:
- Boiling Point:719.5±60.0 °C(Predicted)
- PKA:11.10±0.10(Predicted)
- PSA：119.62000
- Density:1.41±0.1 g/cm3(Predicted)
- LogP:3.06098
- Storage Temp.:-20°C Freezer, Under inert atmosphere
- Solubility.:DMSO (Slightly), Methanol (Slightly)
- Purity/Quality:
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99% *data from raw suppliers
ODM-201 *data from reagent suppliers
Safty Information:
- Pictogram(s):
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- MSDS Files:
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Useful:
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Description
ODM-201 is a novel androgen receptor (AR) inhibit designed to inhibit the growth of prostate cancer cells through binding to the AR to inhibit the testosterone-induced AR nuclear translocation. It is particularly used in patients with progressive metastatic castration-resistant prostate cancer. It is effective in inhibiting the activity of some mutant ARs emerging during antiandrogen therapies, including the F876L mutation version which is resistant to enzalutamide and ARN-509 (the second-generation antiandrogens).Therefore, it has potential to overcome the resistance issue occurring upon AR-targeted therapies. ODM-201 is an androgen receptor (AR) antagonist (Ki = 11 nM). It inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs (IC50s = 65, 66, 1,500, and 1,782 nM for wild-type, ARF876L, ARW741L, and ART877A, respectively). ODM-201 prevents androgen-induced AR nuclear translocation in AR-overexpressing HS-HEK293 and LNCaP cells and suppresses androgen-induced proliferation of VCaP cells (IC50 = 230 nM). In vivo, ODM-201 (50 mg/kg per day) reduces tumor growth in a VCaP castrated mouse xenograft model. It also inhibits tumor growth without increasing serum testosterone levels in a VCaP intact mouse xenograft model.
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Uses
ODM-201 is a compound being used as a novel next-generation androgen receptor-directed therapy for prostate cancer.
