| Identification | Back Directory | [Name]
TRC253 | [CAS]
2110426-27-0 | [Synonyms]
186378
TRC253
CS-2727
JNJ63576253 free base
5-(8-oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile | [Molecular Formula]
C23H21F3N6O2S | [MDL Number]
MFCD31922706 | [MOL File]
2110426-27-0.mol | [Molecular Weight]
502.51 |
| Hazard Information | Back Directory | [Uses]
JNJ-63576253 (TRC-253) free base 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 free base can be used for the research of castration-resistant prostate cancer (CRPC)[1]. | [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[1].
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[1].
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[1].
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[1]. | Animal Model: | Castrated SHO mice with prostate LNCaP SRα F877L tumor[1] | | Dosage: | 30 mg/kg | | Administration: | P.o. once daily for 72 days | | Result: | Inhibited the tumor growth by 87%. |
| Animal Model: | CD-1 male mice[1] | | Dosage: | 2 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) | | Administration: | Intravenous administration and oral administration | | Result: | I.v.: T1/2=5.99 h; CL=15.0 mL/min/kg; Vdss=6.11 L/kg.
P.o.: F=45%; Cmax=0.66 μM; AUClast=4.9 μg?h/mL.
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| [References]
[1] Zhang Z, et, al. Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). J Med Chem. 2021 Jan 28;64(2):909-924. DOI:10.1021/acs.jmedchem.0c01563 |
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| Company Name: |
ChemShuttle, Inc.
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0510-83588313-811 18800520310 |
| Website: |
https://www.jiehuapharma.com/ |
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Cckinase, Inc.
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+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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