JNJ-63576253 (TRC-253)

Catalog No.S9900 Batch:S990001

Technical Data

Formula	C₂₃H₂₂ClF₃N₆O₂S
Molecular Weight	538.97	CAS No.	2110428-64-1
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (185.53 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

In vivo

JNJ-63576253 causes tumor growth inhibition in an enzalutamide-resistant LNCaP F877 L xenograft model. <a class="sref" href="#s_ref">[1]</a>

Protocol (from reference)

Cell Assay:^{<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 Study:^{<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.

Cell Assay:^{<a class="sref" href="#s_ref">[1]</a>}

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 Study:^{<a class="sref" href="#s_ref">[1]</a>}

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

References

[1] Jonathan R Branch, et al. Mol Cancer Ther. 2021 May;20(5):763-774.

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SHIPPING AND STORAGE
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