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| ODM-201 Basic information |
| Product Name: | ODM-201 | | Synonyms: | CS-1565;ODM-201(Darolutamide);N-{(2S)-1-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]propan-2-yl}-5-[(1RS)-1-hydroxyethyl]-1H-pyrazole-3-carboxamide;0DM021;BAY-1841788;ODM-021;0DM021;ODM 021;ODM 021;ODM-021;ODM-201 | | CAS: | 1297538-32-9 | | MF: | C19H19ClN6O2 | | MW: | 398.85 | | EINECS: | 829-313-8 | | Product Categories: | API | | Mol File: | 1297538-32-9.mol |
| ODM-201 Chemical Properties |
| Melting point | 169 - 171°C | | Boiling point | 719.5±60.0 °C(Predicted) | | density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | -20°C Freezer, Under inert atmosphere | | solubility | DMSO (Slightly), Methanol (Slightly) | | pka | 11.10±0.10(Predicted) | | form | Solid | | color | White to Off-White |
| ODM-201 Usage And Synthesis |
| 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.
| | Description | 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. | | Uses | ODM-201 is a compound being used as a novel next-generation androgen receptor-directed therapy for prostate cancer. | | References | Moilanen, Anu Maarit, et al. "Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies." Sci Rep 5.2(2015):12007.
Fizazi, Karim, et al. "ODM-201, a new generation androgen receptor inhibitor for castration-resistant prostate cancer: Preclinical and phase I data." Genitourinary Cancers Symposium of the Conquer-Cancer-Foundation of 2013.
Fizazi, K, et al. "Activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial." Lancet Oncology 5.9(2014):975-85.
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| ODM-201 Preparation Products And Raw materials |
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