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ODM-201

ODM-201 structure

CAS No:
1297538-32-9
Formula:
C19H19ClN6O2
Chemical Name:
ODM-201
Synonyms:
CS-1565;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;N-[(1S)-2-[3-(3-Chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

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.

ODM-201 Basic Attributes

Molecular Weight：

398.85

EC Number：

829-313-8

Color/Form：

White to Off-White

Characteristics

Density：

1.41±0.1 g/cm3(Predicted)

Melting Point：

169 - 171°C

Boiling Point：

719.5±60.0 °C(Predicted)

PKA：

11.10±0.10(Predicted)

Critical Temperature & Pressure：

-20°C Freezer, Under inert atmosphere

ODM-201 Use and Manufacturing

ODM-201 is a compound being used as a novel next-generation androgen receptor-directed therapy for prostate cancer.

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