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ARN-509

Cat. No. M2270
ARN-509 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 100 In stock
10mg USD 140 In stock
50mg USD 350 In stock
100mg USD 600 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 477.43
Formula C21H15F4N5O2S
CAS Number 956104-40-8
Purity 99.79%
Solubility DMSO
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ARN-509 supplier, Androgen Receptor, inhibitors

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