Free shipping on all orders over $ 500
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.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Molecular Weight | 477.43 |
| Formula | C21H15F4N5O2S |
| CAS Number | 956104-40-8 |
| Purity | 99.79% |
| Solubility | DMSO |
| Storage | at -20°C |
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 |
|---|
| Dehydroepiandrosterone
Dehydroepiandrosterone is an effective antiapoptotic factor. |
| ASC-J9
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. |
| GSK-2881078
GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia. GSK 2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. |
| Indacaterol
Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist. |
| Nandrolone phenylpropionate
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.
