中文名: | YM 155;1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(吡嗪-2-基甲基)-4,9-二氢-1H-萘并[2,3-d]咪唑-3-鎓溴化物 |
中文别名: | YM 155; YM-155;4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-d]咪唑鎓溴化物 |
英文名称: | YM155 (Sepantronium Bromide) |
英文别名: | YM155; Sepantronium bromide;YM 155;YM-155;1H-Naphth[2,3-d]imidazolium, 4,9-dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-, bromide;4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium bromide |
CAS No.: | 781661-94-7 |
分子式: | C20H19BrN4O3 |
分子量: | 443.29 |
性状: | 属性溶解性Soluble in water (>89 mg/ml), DMSO (>89 mg/ml), ethanol (>24 mg/ml), DMF (~3 mg/ml), and PBS (pH 7.2) (~10 mg/ml).存贮条件储存温度-20°C描述产品介绍YM155 (Sepantronium Bromide)是一种有效的survivin抑制药,通过抑制Survivin启动子活性而发挥作用,在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM;对SV40启动子活性抑制作用不显著,能够轻微抑制Survivin与XIAP相互作用。用途An inhibitor of survivin expression and apoptosis inducer.生化机理YM155 is a small molecule inhibitor of survivin expression that acts by inhibiting the survivin gene promoter transcription. Shown to induce apoptosis and inhibit tumor growth. |
储存: | 储存温度-20°C |
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用途: | YM155 (YM 155, YM-155) is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity. However, YM155 (YM 155, YM-155) did not significantly inhibit SV40 promoter activity at concentrations up to 30 μM. YM155 (YM 155, YM-155) induced apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nM. In a s.c.xenografted PC-3 tumor model in mice, 3-day continuous infusions of YM155 (YM 155, YM-155) at 3 to 10 mg/kg induced massive tumor regression accompanied by suppression of intratumoral survivin. Pharmacokinetic analyses indicated that YM155 (YM 155, YM-155) is highly distributed to tumors and at concentrations approximately 20-fold higher than those in plasma. [1][2][3] |