Basic information Safety Supplier Related

TRC253

Basic information Safety Supplier Related

TRC253 Basic information

Product Name:
TRC253
Synonyms:
  • CS-2727
  • 186378
  • 5-(8-oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile
  • TRC253
  • JNJ63576253 free base
  • JNJ 63576253 free base,resistant,TRC 253,JNJ63576253,TRC-253,CRPC,JNJ63576253 free base,wild-type,prostate,cancer,castration,androgen,LNCaP,Androgen Receptor,Inhibitor,inhibit,JNJ 63576253,mutant
  • 2-Pyridinecarbonitrile, 5-[8-oxo-5-[6-(4-piperidinyloxy)-3-pyridinyl]-6-thioxo-5,7-diazaspiro[3.4]oct-7-yl]-3-(trifluoromethyl)-
  • JNJ-63576253 free base, 10 mM in DMSO
CAS:
2110426-27-0
MF:
C23H21F3N6O2S
MW:
502.51
Mol File:
2110426-27-0.mol
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TRC253 Chemical Properties

Boiling point:
672.3±65.0 °C(Predicted)
Density 
1.53±0.1 g/cm3(Predicted)
pka
9.56±0.10(Predicted)
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TRC253 Usage And Synthesis

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.

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

TRC253Supplier

ChemShuttle, Inc.
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0510-83588313-811 18800520310
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sales@chemshuttle.com
Finetech Industry Limited
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027-87465837 19945049750
Email
sales@finetechnology-ind.com
Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Email
sales@zehanbiopharma.com
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Email
3008007409@qq.com
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TRC253(2110426-27-0)Related Product Information