产品
编 号:F488416
分子式:C15H15F3N2O3S
分子量:360.35
产品类型
结构图
CAS No: 868691-50-3
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产品详情
生物活性:
JNJ-26146900 is a potent and orally active androgen receptor antagonist with a Ki value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer.
体内研究:
JNJ-26146900 (10-100 mg/kg; p.o.; 成年雄性 Sprague-Dawley 大鼠) 同样有效地降低腹侧前列腺和肛提肌肌肉的湿重。JNJ-26146900 (30-100 mg/kg; p.o.) 在 Dunning 大鼠模型中防止前列腺肿瘤生长,在 10mg/kg 的剂量下最大限度地抑制生长。 JNJ-26146900 在 CWR22-LD1 小鼠人前列腺癌异种移植模型中显着抑制肿瘤生长。JNJ-26146900 (30 mg/kg; p.o.; 成年雄性 Sprague-Dawley 大鼠) 减少去势诱导的胫骨骨质流失。Animal Model:mature male Sprague-Dawley rats
Dosage:10, 30, 100 mg/kg
Administration:oral gavage; daily, for 6 weeks
Result:Reduced ventral prostate weight.
Animal Model:CWR22-LD1 mouse xenograft model
Dosage:30, 100 mg/kg
Administration:oral gavage; twice per day for 3 weeks
Result:Inhibited tumor growth at 100 mg/kg, reducing mean tumor weight at Day 21 to about 30% of the intact vehicle tumor weight.
体外研究:
JNJ-26146900 与转染到 Cos-7 细胞中的大鼠雄激素受体结合,具有亚微摩尔效力。