JNJ-63576253

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-63576253 是一种有效的口服活性雄激素受体 (AR) 完全拮抗剂，在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的 IC50 分别为 37 和 54 nM。

JNJ-63576253 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).

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 (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.

TRC253

Endocrinology/Hormones

Androgen Receptor (AR)

androgen receptor

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2110426-27-0

502.51

C23H21F3N6O2S

>98% (HPLC)

DMSO:10 mM

C1CC2(C1)C(=O)N(C(=S)N2C3=CN=C(C=C3)OC4CCNCC4)C5=CC(=C(N=C5)C#N)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years