JNJ-63576253 | AR inhibitor | Probechem Biochemicals

Chemical Structure : JNJ-63576253

CAS No.: 2110428-64-1

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JNJ-63576253 (JNJ63576253, TRC-253)

货号: 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.

规格	价格	库存
10 mg	￥1280	In stock
25 mg	￥1980	In stock
50 mg	￥3580	In stock
100 mg	￥5580	In stock
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	538.974
分子式	C23H22ClF3N6O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

JNJ-63576253 (JNJ63576253, TRC-253)

生物&药学活性

物理化学性质&存储条件

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JNJ-63576253 (JNJ63576253, TRC-253)

生物&药学活性

物理化学性质&存储条件

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