Home Endocrinology & Hormones Androgen Receptor antagonist JNJ-63576253 (TRC-253) For research use only.

JNJ-63576253 (TRC-253)

JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.

JNJ-63576253 (TRC-253) Chemical Structure

JNJ-63576253 (TRC-253) Chemical Structure

CAS No. 2110428-64-1

Purity & Quality Control

Batch: S990001 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.39%
99.39

JNJ-63576253 (TRC-253) Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

Biological Activity

Description JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
Targets
Androgen receptor [1]
(Cell-free assay)
6.9 nM
In vitro
In vitro

JNJ-63576253 can inhibit transcriptional activity in reporter assays, cellular proliferation, and AR downstream target gene expression, as a potent and selective next-generation AR pathway inhibitor. <sup><a class="sref" href="#s_ref">[1]</a></sup>
Cell Research Cell lines HepG2, VCaP, PC3, LNCaP AR/cs, LNCaP F877L
Concentrations 0.0001 μΜ-1.5 μM
Incubation Time 6 h, 24h
Method

LNCaP AR/cs, LNCaP F877L, VCaP, and PC3 are seeded at densities of 5,000 or 250 cells per well into 96-well plates and incubated overnight. Following compound treatment, the cells are incubated for 6 days for assessing proliferation. For transcriptional reporter assays, LNCaP reporter lines are seeded at a density of 10,000 cells per well, incubated overnight, then treated for 24 hours with JNJ-63576253 in the presence of 0.1 nmol/L R1881. After treatment, cells are assayed using the SteadyGlo-luciferase Kit.
In Vivo
In vivo

JNJ-63576253 causes tumor growth inhibition in an enzalutamide-resistant LNCaP F877 L xenograft model. <sup><a class="sref" href="#s_ref">[1]</a></sup>
Animal Research Animal Models Castrated male rats (Sprague Dawley;ages 42–45 days)
Dosages 10, 30, 50 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02987829 Completed
Metastatic Castrate-resistant Prostate Cancer|Adenocarcinoma Prostate
Tracon Pharmaceuticals Inc.|Janssen Pharmaceutica N.V. Belgium
 May 23 2017 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 538.97 Formula

C23H22ClF3N6O2S
CAS No. 2110428-64-1 SDF --
Smiles Cl.FC(F)(F)C1=CC(=CN=C1C#N)N2C(=O)C3(CCC3)N(C2=S)C4=CN=C(OC5CCNCC5)C=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (185.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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