沸点 | ~665.5 °C at 760 mmHg |
熔点 | >240 °C |
折光率 | 1.65 |
溶解性 | 25°C: DMSO |
存贮条件 | 储存温度-20°C |
密度 | 1.3000 |
产品介绍 | Genz-644282是非喜树碱类拓扑异构酶I抑制剂,IC50为1.2 nM,有抗肿瘤活性。 |
生化机理 | Description:IC50 Value: 1.2 nM [1]Genz-644282 [8,9-dimethoxy-5-(2-N-methylaminoethyl)-2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-one] has emerged as a promising candidate of non-Camptothecin topoisomerase I inhibitor for antitumor agents.in vitro: Genz-644282 demonstrated potent cytotoxic activity with a median IC(50) of 1.2?nM (range 0.2-21.9?nM) [1]. Limited cross-resistance to Genz-644282 was also found in the Top1 knockdown colon cancer (HCT116) and breast cancer (MCF7) cell lines and in human adenocarcinoma cells (KB31/KBV1) that overexpress (P-glycoprotein, ABCB1), a member of the ATP-binding cassette family of cell surface transport proteins known to confer MDR [3].in vivo: Genz-644282 at its MTD (4?mg/kg) induced maintained complete responses (MCR) in 6/6 evaluable solid tumor models. At 2?mg/kg Genz-644282 induced CR or MCR in 3/3 tumor models relatively insensitive to topotecan, but there were no objective responses at 1?mg/ |
别名 | Genz644282;Genz 644282;Genz644282;Genz 644282;2,3-Dimethoxy-12-[2-(methylamino)ethyl]benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one |
Genz-644282,Topo I 抑制剂
Genz-644282 (订货以英文为准)
编号:G126864
CAS号:529488-28-6
分子式:C22H21N3O5
分子量:407.42
产品名称 | Genz-644282 |
中文名称 | Genz-644282,Topo I 抑制剂 |
CAS号 | 529488-28-6 |
分子式(M.F.) | C22H21N3O5 |
分子量(M.W.) | 407.42 |
储存条件 | -20°C储存 |
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