An androgen receptor antagonist
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ARN-509

Item No. 17132

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[7-[6-cyano-5-(trifluoromethyl)-3-pyridinyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide
CAS Number
956104-40-8
Synonyms
  • JNJ-56021927
Molecular Formula
C21H15F4N5O2S
Formula Weight
477.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.1 mg/mlEthanol: 2 mg/ml
λmax
246 nm
SMILES
S=C(N(C1=CC(F)=C(C(NC)=O)C=C1)C2(CCC2)C3=O)N3C4=CN=C(C#N)C(C(F)(F)F)=C4
InChi Code
InChI=1S/C21H15F4N5O2S/c1-27-17(31)13-4-3-11(8-15(13)22)30-19(33)29(18(32)20(30)5-2-6-20)12-7-14(21(23,24)25)16(9-26)28-10-12/h3-4,7-8,10H,2,5-6H2,1H3,(H,27,31)
InChi Key
HJBWBFZLDZWPHF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Cayman Chemical
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    Product Description

    ARN-509 is an antagonist of the androgen receptor (IC50 = 16 nM).1 It binds the receptor but does not cause nuclear localization or DNA binding.1 ARN-509 is orally bioavailable and, at 30 mg/kg/d, suppresses tumor growth in a mouse model of castration-resistant prostate cancer.1 This compound can be used to study androgen signaling in vitro and in vivo and has potential applications in certain types of cancer.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Clegg, N.J., Wongvipat, J., Joseph, D.J., et al. ARN-509: A novel antiandrogen for prostate cancer treatment. Cancer Res. 72(6), 1494-1503 (2012).

    2. Gupta, E., Guthrie, T., and Tan, W. Changing paradigms in management of metastatic Castration Resistant Prostate Cancer (mCRPC). BMC Urol. 14, 55 (2014).