ODM-201 (BAY-1841788, Darolutamide) | AR antagonist

Chemical Structure : ODM-201

CAS No.: 1297538-32-9

ODM-201 (BAY-1841788;Darolutamide)

Catalog No.: PC-45113Not For Human Use, Lab Use Only.

ODM-201 (BAY-1841788, Darolutamide) is a potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM.

Packing	Price	Stock
5 mg	$58	In stock
10 mg	$98	In stock
25 mg	$158	In stock
50 mg	$258	In stock
100 mg	$398	In stock
250 mg		Get quote

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Biological Activity

ODM-201 (BAY-1841788, Darolutamide) is a potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM.
ODM-201 inhibits wtAR/AR(F876L) with IC50 of 65/66 nM respectively, weak inhibition on AR(W741L) and AR(T877A).
ODM-201 inhibits the nuclear translocation of AR and more efficaciously than enzalutamide or ARN-509 in VCaP cell line proliferation assay。
ODM-201 reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model.

Physicochemical Properties

M.Wt	398.8462
Formula	C19H19ClN6O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 44 mg/mL
Chemical Name/SMILES	1H-Pyrazole-3-carboxamide, N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-

References

1. Moilanen AM, et al. Sci Rep. 2015 Jul 3;5:12007.

2. Fizazi K, et al. Lancet Oncol. 2014 Aug;15(9):975-85.

3. Cancer Discov. 2014 Sep;4(9):OF10.