TRC253

Product Name: TRC253
CAS No.: 2110426-27-0
Chemical Name: TRC253
Synonyms: TRC253;186378;CS-2727;JNJ63576253 free base;JNJ-63576253 free base, 10 mM in DMSO;5-(8-oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile;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,resistant,TRC 253,JNJ63576253,TRC-253,CRPC,JNJ63576253 free base,wild-type,prostate,cancer,castration,androgen,LNCaP,Androgen Receptor,Inhibitor,inhibit,JNJ 63576253,mutant
CBNumber: CB63371325
Molecular Formula: C23H21F3N6O2S
Formula Weight: 502.51
MOL File: 2110426-27-0.mol

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TRC253 Property

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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Hazard and Precautionary Statements (GHS)

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TRC253 Chemical Properties,Usage,Production

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%), C_max (0.66 μM) and AUC_last (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.: T_1/2=5.99 h; CL=15.0 mL/min/kg; Vdss=6.11 L/kg. P.o.: F=45%; C_max=0.66 μM; AUC_last=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

TRC253 Preparation Products And Raw materials

Raw materials

Preparation Products

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TRC253 Suppliers

China 33 United States 3 Global 36

ChemShuttle, Inc.

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Finetech Industry Limited

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2110426-27-0, TRC253Related Search:

JNJ-10229570 JNJ0966 JNJ-38158471 N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine 3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine JNJ-7706621 JNJ 63533054 JNJ-26481585 N-(4-chloropyridin-3-yl)-4-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)Methyl)piperazine-1-carboxaMide JNJ 31020028 JNJ-632 2-(4-Chlorophenoxy)-2-methyl-N-[5-[(methylsulfonyl)amino]tricyclo[3.3.1.13,7]dec-2-yl]-propanamide

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

2110426-27-0