2-(4-メチルヘキサヒドロ-1H-1,4-ジアゼピン-1-イル)-N-[(5-メチルピラジン-2-イル)メチル]-5-オキソ-1,11b-ジアザ-7-チア-5H-ベンゾ[c]フルオレン-6-カルボアミド

一般的な説明A cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142 nM in HCT-116), but not Pol II-mediated c-myc transcription, by preventing TAF SL1 and rDNA association). Effectively inhibits Pol I-dependent proliferation among 39 cancer cell lines (IC50<1 μM) in vitro and suppresses A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion in vivo.