GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

BAY-1841788 | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K i of 11 nM. Phase 3.
In vitro

In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells.

In vivo

In mice bearing VCaP xenografts, ODM-201 (50\u2009mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth.
Cell Data

cell lines：

Concentrations：~10 μM

Incubation Time：4 days

Powder Purity:≥99%

Specifications

Synonyms

BAY-1841788 | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Androgen Receptor antagonist

Product Properties

• ALogP: 3.034
• hba_count: 3
• HBD Count: 3
• Rotatable Bond: 6

Names and Identifiers

• Isomeric SMILES: C[C@@H](CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
• Molecular Weight: 398.85
• Reaxy-Rn: 23068895
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23068895&ln=

Associated Targets(Human)

AR Tclin Androgen receptor (2 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 80
• DMSO(mM) Max Solubility: 200.5766579
• Water(mg / mL) Max Solubility: ＜1