Darolutamide (ODM-201) is a new-generation, potent and selective androgen receptor (AR) inhibitor. Darolutamide inhibits testosterone-induced nuclear translocation of AR. Darolutamide also blocks the activity of the tested mutant ARs arising in response to antiandrogen therapies, including the F876L mutation that confers resistance to enzalutamide and ARN-509. In addition, Darolutamide reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model. Darolutamide overcomes resistance to AR-targeted therapies by antagonizing both overexpressed and mutated ARs.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
|Related Androgen Receptor Products|
Bavdegalutamide (ARV-110) is an oral, specific androgen receptor (AR) PROTAC degrader.
MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
Dehydroepiandrosterone is an effective antiapoptotic factor.
ASC-J9, also known as GO-Y025 and Dimethylcurcumin, suppressesing castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
R1881 (Metribolone) is an orally active, non-aromatisable androgen and anabolic steroid.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.