ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM. ARN-509 inhibits AR nuclear translocation and AR binding to androgen response elements and, unlike bicalutamide, does not exhibit agonist properties in the context of AR overexpression. ARN-509 displayed dose-proportional pharmacokinetics, and demonstrated pharmacodynamic and antitumor activity across all dose levels tested. ARN-509 is currently in a Phase I clinical trial.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer.
Rathkopf DE, et al. J Clin Oncol. 2013 Oct 1;31(28):3525-30. PMID: 24002508.
|Related Androgen Receptor Products|
Nandrolone phenylpropionate (NPP) is an anabolic-androgenic steroid. The low androgenicity and enhanced anabolic activity of NPP has shown to positively influence calcium metabolism and to increase bone mass in osteoporosis.
Testosterone is normally present in the circulation of both men and women. Due to the dynamic regulation of endogenous testosterone production, including the acute effects of competition and exercise, testosterone concentrations may vary considerably within and among individuals.
Testosterone phenylpropionate is a synthetic anabolic-androgenic steroid (AAS) and an androgen ester.
Testosterone Isocaproate help in increasing the body weight and will also help in gaining the strength and also help in losing fat in the body and gives an increase in libido, red blood cells, stamina and quick recovery after heavy training.
Androcur-treatment abolished testosterone-reduced cAMP, coupled with a changed expressional milieu of cAMP signaling elements. Results from in vitro experiments suggest that some of these effects are testosterone-AR dependent, while others could be due to disturbed LH and/or other signals.
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