JNJ-63576253

JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).

Product information

CAS Number: 2110428-64-1

Molecular Weight: 538.97

Formula: C23H22ClF3N6O2S

Chemical Name: 5-{8-oxo-5-[6-(piperidin-4-yloxy)pyridin-3-yl]-6-sulfanylidene-5,7-diazaspiro[3.4]octan-7-yl}-3-(trifluoromethyl)pyridine-2-carbonitrile hydrochloride

Smiles: Cl.N#CC1=NC=C(C=C1C(F)(F)F)N1C(=O)C2(CCC2)N(C1=S)C1=CN=C(C=C1)OC1CCNCC1

InChiKey: QDINJYHLAKIZLE-UHFFFAOYSA-N

InChi: InChI=1S/C23H21F3N6O2S.ClH/c24-23(25,26)17-10-15(13-29-18(17)11-27)31-20(33)22(6-1-7-22)32(21(31)35)14-2-3-19(30-12-14)34-16-4-8-28-9-5-16;/h2-3,10,12-13,16,28H,1,4-9H2;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (463.85 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM. JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min.

In Vivo:

JNJ-63576253 (30 mg/kg; p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice. JNJ-63576253 (30 mg/kg; p.o. once daily for 10 days) inhibits the five androgen sensitive organs (ASOs) under stimulation by testosterone propionate (TP) in mice. JNJ-63576253 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (45%), Cmax (0.66 μM) and AUClast (4.9 μg•h/mL) in mice. JNJ-63576253 (2 mg/kg; i.v.) exhibits reasonable half-life (5.99 h), CL (15.0 mL/min/kg) and Vdss (6.11 L/kg) in mice.

Products are for research use only. Not for human use.