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Chemical Structure : JNJ-63576253
CAS No.: 2110428-64-1
Catalog No.: PC-72511Not For Human Use, Lab Use Only.
JNJ-63576253 (TRC-253, JNJ63576253) is a next-generation, potent, selective androgen receptor (AR) antagonist (inhibitor) against wild-type AR (IC50=6.9 nM), AR F877L and other clinically detected ligand binding domain (LBD) point mutations.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $358 | In stock | |
| 100 mg | $558 | In stock | |
| 1 g | Get quote |
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JNJ-63576253 (TRC-253, JNJ63576253) is a next-generation, potent, selective androgen receptor (AR) antagonist (inhibitor) against wild-type AR (IC50=6.9 nM), AR F877L and other clinically detected ligand binding domain (LBD) point mutations.
JNJ-63576253 inhibits transcriptional activity in reporter assays, cellular proliferation, and AR downstream target gene expression.
JNJ-63576253 causes tumor growth inhibition (TGI) in an enzalutamide-resistant LNCaP F877 L xenograft model.
JNJ-63576253 displayed an approximately 1,000-fold selectivity versus other nuclear hormone receptors (GR IC50>30 uM).
JNJ-63576253 completely inhibited transiently transfected VP16-AR F877 L with IC50 of 15 nM in HepG2 transcriptional reporter models, JNJ-63576253 completely inhibited AR-mediated transactivation in the presence of 100 pmol/L R1881 (IC50=99 nM).
JNJ-63576253 abrogates cellular proliferation, nuclear translocation, and AR target gene expression in models of human prostate adenocarcinoma.
JNJ-63576253 causes tumor growth inhibition (TGI) in an enzalutamide-resistant LNCaP F877 L xenograft model.
| M.Wt | 538.974 | |
| Formula | C23H22ClF3N6O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-(8-Oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)-picolinonitrile hydrochloride |
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1. Zhang Z, et al. J Med Chem. 2021 Jan 28;64(2):909-924.
2. Branch JR, et al. Mol Cancer Ther. 2021 May;20(5):763-774.
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