产品
编 号：F620782
分子式：C23H21F3N6O2S
分子量：502.51
分子式：C23H21F3N6O2S
分子量：502.51
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CAS No: 2110426-27-0
产品详情
生物活性：
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).
体内研究：
JNJ-63576253 (30 mg/kg; p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice.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.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.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.Animal Model:Castrated SHO mice with prostate LNCaP SRα F877L tumor
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
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.
体外研究：
JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM.JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min.
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).
体内研究：
JNJ-63576253 (30 mg/kg; p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice.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.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.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.Animal Model:Castrated SHO mice with prostate LNCaP SRα F877L tumor
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
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.
体外研究：
JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM.JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min.
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