JNJ63576253

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 是一种临床阶段雄激素受体拮抗剂，用于治疗 F877L 突变型和野生型去势抵抗性前列腺癌 (mCRPC)。

JNJ-63576253 is a Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

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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.

TRC-253

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor

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2110428-64-1

538.97

C23H22ClF3N6O2S

>98% (HPLC)

DMSO: 200mg/mL?(371.08 mM);H2O: insoluble

N#CC1=NC=C(N(C2=O)C(N(C3=CC=C(OC4CCNCC4)N=C3)C52CCC5)=S)C=C1C(F)(F)F.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years