| Identification | Back Directory | [Name]
JNJ-26146900 | [CAS]
868691-50-3 | [Synonyms]
JNJ-26146900
1H-Indole-5-carbonitrile, 2-[(1R)-2-(ethylsulfonyl)-1-hydroxy-1-methylethyl]-6-(trifluoromethyl)- | [Molecular Formula]
C15H15F3N2O3S | [MOL File]
868691-50-3.mol | [Molecular Weight]
360.35 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
JNJ-26146900 (10-100 mg/kg; p.o.; mature male Sprague-Dawley rats) reduces the wet weights of both the ventral prostate and levator ani muscle as effectively[1].
JNJ-26146900 (30-100 mg/kg; p.o.) prevents prostate tumor growth in the Dunning rat model, maximally inhibiting growth at a dose of 10mg/kg. JNJ-26146900 inhibits tumor growth significantly in a CWR22-LD1 mouse xenograft model of human prostate cancer[1].
JNJ-26146900 (30 mg/kg; p.o.; mature male Sprague-Dawley rats) reduces castration-induced tibial bone loss[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. |
| [References]
[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. DOI:10.1016/j.jsbmb.2006.07.006 |
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