JNJ-63576253 (Synonyms: TRC-253) |
| Catalog No.GC62106 |
JNJ-63576253(TRC-253)은 LNCaP 세포에서 F877L 돌연변이 AR 및 야생형 AR에 대해 37 및 54nM의 IC50을 갖는 안드로겐 수용체(AR)의 강력하고 경구 활성인 완전 길항제입니다. JNJ-63576253은 거세저항성 전립선암(CRPC) 연구에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2110428-64-1
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
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