JNJ-63576253(TRC-253)
- Product Name
- JNJ-63576253(TRC-253)
- CAS No.
- 2110428-64-1
- Chemical Name
- JNJ-63576253(TRC-253)
- Synonyms
- JNJ63576253 HCl;JNJ-63576253(TRC-253);JNJ-63576253, 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 hydrochloride;TRC-253,mutant,JNJ 63576253,resistant,wild-type,JNJ63576253,TRC 253,prostate,inhibit,Androgen Receptor,castration,cancer,Inhibitor,androgen,CRPC,LNCaP,JNJ-63576253,TRC253
- CBNumber
- CB19383079
- Molecular Formula
- C23H22ClF3N6O2S
- Formula Weight
- 538.97
- MOL File
- 2110428-64-1.mol
JNJ-63576253(TRC-253) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : 250 mg/mL (463.85 mM; Need ultrasonic)
- form
- Solid
- color
- Off-white to light yellow
JNJ-63576253(TRC-253) Chemical Properties,Usage,Production
Biological Activity
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)[1]. JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM[1].JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min[1]. 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].
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.
JNJ-63576253(TRC-253) Preparation Products And Raw materials
Raw materials
Preparation Products
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