JNJ-63576253 (TRC-253) free base 是一种有效和具有口服活性的雄激素受体 (androgen receptor) 的完全拮抗剂，在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的IC50值分别为 37 和 54 nM。JNJ-63576253 free base 可用于去势抵抗性前列腺癌 (CRPC) 的研究。
| 生物活性 | JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist ofandrogen receptor(AR), withIC50s 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 prostatecancer(CRPC)[1]. |
| IC50& Target | IC50: 37 nM (F877L mutant AR in LNCaP cells); 54 nM (wild-type AR in LNCaP cells)[1] |
体外研究
(In Vitro) | JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50of 265 nM[1].
JNJ-63576253 is stable in human liver microsomes, with anT1/2of >180 min[1].
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体内研究
(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 μgoh/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 μgoh/mL. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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