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AR antagonist

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SI-7276

AR antagonist, >98% (HPLC)

IUPAC Name : (S)-3-(3-Chloro-4-(trifluoromethyl)-1H-indazol-1-yl)-N-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-2-hydroxy-2-methylpropanamide

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Back Order  Estimated to ship on 04 October 2026
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Chemical Properites
Mol. Formula :
C19H12ClF6N5O2
Mol. Weight :
491.78
Appearance :
Solid
Melting Point :
Not available
For Laboratory research use only, not for drug, household or other uses.

Applications : This is a metabolically stable, next‑generation androgen receptor (AR) antagonist emerging from a >50‑compound SAR campaign aimed at improving the unstable first‑in‑class indole antagonist. It retains very high AR antagonistic potency (IC50= 0.021 μM) and achieves marked metabolic stability (t1/2 = 120 min). It demonstrates enhanced in vivo PK and strong antiandrogen efficacy in both Hershberger assays and Enz‑Res LNCaP‑AR xenograft models, positioning it as a potent, drug‑like AR antagonist suitable for further development in resistant prostate cancer.

References : Hwang D-J. et al.: J. Med. Chem., 66(5), 3372-3392, 2023.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.

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