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ODM-201 Sale

(Synonyms: 达洛鲁胺,ODM-201; BAY-1841788) 目录号 : GC11386

An androgen receptor antagonist

ODM-201 Chemical Structure

Cas No.:1297538-32-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥987.00
现货
5mg
¥861.00
现货
10mg
¥1,313.00
现货
50mg
¥3,392.00
现货

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Sample solution is provided at 25 µL, 10mM.

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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.

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1 mg 5 mg 10 mg
1 mM 2.5072 mL 12.536 mL 25.0721 mL
5 mM 0.5014 mL 2.5072 mL 5.0144 mL
10 mM 0.2507 mL 1.2536 mL 2.5072 mL
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