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ODM-201
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ODM-201图片
CAS NO:1297538-32-9
规格:98%
分子量:398.85
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍

ODM-201(Darolutamide)

new-generation androgen receptor inhibitor
CAS:1297538-32-9
分子式:C19H19ClN6O2
分子量:398.85
纯度:98%
存储:Store at -20°C

Background:

ODM-201 is a new-generation inhibitor of androgen receptor with Ki value of 11 nM [1].

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 [1].

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 [1].

Reference:
[1].Moilanen AM, Riikonen R, Oksala R, et al.? Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Sci Rep, 2015, 5: 12007.