An androgen receptor antagonist (Ki = 11 nM); inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs (IC50s = 65

ODM-201 – 10 mg

Brand:
Cayman
CAS:
1297538-32-9
Storage:
-20
UN-No:
Non-Hazardous - /

ODM-201 is an androgen receptor (AR) antagonist (Ki = 11 nM).{42404} It inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs (IC50s = 65, 66, 1,500, and 1,782 nM for wild-type, ARF876L, ARW741L, and ART877A, respectively). ODM-201 prevents androgen-induced AR nuclear translocation in AR-overexpressing HS-HEK293 and LNCaP cells and suppresses androgen-induced proliferation of VCaP cells (IC50 = 230 nM). In vivo, ODM-201 (50 mg/kg per day) reduces tumor growth in a VCaP castrated mouse xenograft model. It also inhibits tumor growth without increasing serum testosterone levels in a VCaP intact mouse xenograft model.  

 

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SKU: 25643 - 10 mg Category:

Description

An androgen receptor antagonist (Ki = 11 nM); inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs (IC50s = 65, 66, 1,500, and 1,782 nM for wild-type, ARF876L, ARW741L, and ART877A, respectively); prevents androgen-induced AR nuclear translocation in AR-overexpressing HS-HEK293 and LNCaP cells; suppresses androgen-induced proliferation of VCaP cells (IC50 = 230 nM); reduces tumor growth in a VCaP castrated mouse xenograft model at 50 mg/kg per day; inhibits tumor growth without increasing serum testosterone levels in a VCaP intact mouse xenograft model ,

Formal name: N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide

Synonyms:  BAY 1841788

Molecular weight: 398.9

CAS: 1297538-32-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens

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