JNJ-63576253 (TRC-253)

Catalog No.S9900

For research use only.

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

CAS No. 2110428-64-1

Purity & Quality Control

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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

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>

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>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • 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.

Animal Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Animal Models: Castrated male rats (Sprague Dawley;ages 42–45 days)
  • Dosages: 10, 30, 50 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 538.97
Formula

C23H22ClF3N6O2S

CAS No. 2110428-64-1
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02987829 Completed Drug: TRC253 Metastatic Castrate-resistant Prostate Cancer|Adenocarcinoma Prostate Tracon Pharmaceuticals Inc.|Janssen Pharmaceutica N.V. Belgium May 23 2017 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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