Cat. No. Name Size Price Add Cart
KI2602ARN-50910 mg$432
ARN-50925 mg$864
ARN-50950 mg$1552
ARN-509100 mg$2032
ARN-509200 mg$3250
ARN-509500 mg$6502
ARN-5091 g$10400

Chemical Characteristic

Product NameARN-509
CAS No.956104-40-8
Molecular Weight 477.43
FormulaC21H15F4N5O2S
Chemical Name4-[7-[6-Cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide
SmilesC(=O)(c1c(cc(cc1)N1C2(CCC2)C(=O)N(C1=S)c1cnc(c(c1)C(F)(F)F)C#N)F)NC
Chemical Structure

Biological activities

ARN-509 is a selective and competitive AR inhibitor. ARN-509 inhibits nuclear translocation and DNA binding of the receptor, thereby modulating expression of genes that drive prostate cancer growth.[1] The IC50 of ARN-509 against AR is 16 nM that is 7- to 10-fold greater affinity than the clinically approved antiandrogen, bicalutamide (median IC50 = 160 nM). In vivo, ARN-509 exhibits antitumor activity in a castration-sensitive xenograft model of prostate cancer and antiandrogenic effects in dogs that phenocopy castration.[2]

Protocols

In vivo, ARN-509 is dissolved in DMSO.[2]

References

[1] Zivi A, Changing therapeutic paradigms in castrate-resistant prostate cancer. Clin Genitourin Cancer. 2010, 8(1): 17-22.
[2] Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. 2012, 72 (6): 1494-1503.

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