- Min.Order :10 Milligram
- Purity: 98% 99%
- Payment Terms : L/C,D/A,D/P,T/T
Keywords
BAY-1841788 Darolutamide 1297538-32-9
Quick Details
- Appearance:
- Application:androgen receptor
- PackAge: 5mg 10mg 25mg
- ProductionCapacity:|Metric Ton|Day
- Storage: -20℃
- Transportation:by sea or by air
Superiority:
ODM-201 is a new-generation inhibitor of androgen receptor with Ki value of 11 nM.
Androgen receptor is a type of nuclear receptor that is activated by androgen and functions as a DNA-binding transcription factor that regulates gene expression. Activation of androgen receptor (AR) is crucial for prostate cancer growth.
ODM-201 is a high-affinity and potent androgen receptor antagonist. In competitive AR binding assays, ODM-201 exhibited Ki value of 11 nM. In AR-HEK293 cells stably expressing full-length human AR (hAR) and an androgen-responsive luciferase reporter gene construct, ODM-201 and its major metabolite ORM-15341 inhibited AR-mediated transactivation with IC50 values of 26 nM and 38 nM. 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. in AR overexpressing HS-HEK293 cells, ODM-201 inhibited the androgen-induced nuclear translocation of overexpressed AR. In the VCaP cell line with endogenous AR gene amplification and AR overexpression, ODM-201 inhibited androgen-induced cell proliferation with IC50 value of 230 nM.
In castrated male nude mice with subcutaneously injected VCaP cells, orally treatment with ODM-201 (50 mg/kg) once (qd) or twice daily (bid) for 37 days, ODM-201 showed a significant antitumor activity with both doses. There was no sign of treatment-related toxicities. In orthotopic VCaP tumor-bearing intact nude mice, ODM-201 (50 mg/kg, bid) significantly inhibited tumor growth but did not affect the testosterone levels in serum. ODM-201 couldn’t penetrate the blood-brain barrier.
Details:
Yichang shangnuoder Biomedical Technology Co., Ltd. was registered and established in September 2018, located in the national biomedical incubator of Yichang City, Hubei Province (Chengdong u Valley). It is a comprehensive high-tech enterprise integrating R & D, production and sales of pharmaceutical raw materials and intermediates.
The company has a 400 square meter standard chemical synthesis laboratory, advanced production equipment, and a strong R & D team composed of several senior technical researchers with bachelor's degree and master's degree. It has established the "production, teaching and research" cooperation mode with some universities in Yichang, Wuhan and Shanghai. The company is mainly engaged in the R & D and production of new chemical drugs, high-end chemicals and pharmaceutical intermediates, and has applied for 12 patents in key technology fields.
Since its establishment, the company has been adhering to the business philosophy of "innovation driven, efficiency first, professional guidance, first-class service", continuously providing high-quality products and services to customers at home and abroad, providing services throughout Wuhan, Hangzhou, Shanghai, Shenzhen and other regions, accumulating rich business resources. After years of technical development, the company can provide customers with mature and stable high-level pharmaceutical raw materials, intermediate R & D, manufacturing and other professional services.
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