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ODM-201

Catalog No.
A8452
new-generation androgen receptor inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$132.00
In stock
5mg
$120.00
In stock
10mg
$190.00
In stock
50mg
$450.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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:
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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt398.85
Cas No.1297538-32-9
FormulaC19H19ClN6O2
Solubility≥19.95mg/mL in DMSO
Chemical NameN-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
SDFDownload SDF
Canonical SMILESN#CC1=C(Cl)C=C(C2=NN(C[[email protected]](C)NC(C3=NNC(C(O)C)=C3)=O)C=C2)C=C1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

ODM-201