JNJ-26146900

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[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Androgen Receptor

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[1]。

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[1]。 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[1]。 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[1]。 Animal Model: mature male Sprague-Dawley rats[1] 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[1] 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.

[1]. Lanter J, et, al. A selective androgen receptor modulator that reduces prostate tumor size and prevents orchidectomy-induced bone loss in rats. J Steroid Biochem Mol Biol. 2007 Jan;103(1):76-83.