中文名 | Karenitecin |
英文名 | Karenitecin |
别名 | 化合物 T14703 |
英文别名 | DB 172 BNP 1350 MCC 12824 Cositecan Karenitecin |
CAS | 203923-89-1 |
化学式 | C25H28N2O4Si |
分子量 | 448.59 |
密度 | 1.29±0.1 g/cm3(Predicted) |
沸点 | 727.2±60.0 °C(Predicted) |
溶解度 | 溶于DMSO,不溶于水 |
酸度系数 | 11.27±0.20(Predicted) |
存储条件 | 2-8℃ |
MDL号 | MFCD09833216 |
体外研究 | Karenitecin is a topoisomerase I inhibitor, with potent anti-cancer activity. Karenitecin inhibits cell growth of A253 cells with IC 10 , IC 50 , and IC 90 values of 0.01, 0.07, and 0.7 μM after 2 h treatment. Karenitecin induces DNA damage (0.01, 0.07, and 0.7 μM), and increases cyclin E and cdk2 protein expression in A253 cells (0.07, and 0.7 μM). Karenitecin markedly enhances the cyclin B/cdc2-associated kinase activity at low concentration, but slightly suppresses this kinase activity at higher concentration. Karenitecin inhibits several human colon cancer cell lines such as COLO205, COLO320, LS174T, SW1398 and WiDr cells, with IC 50 s of 2.4 nM, 1.5 nM, 1.6 nM, 2.9 nM, and 3.2 nM, respectively. |
体内研究 | Karenitecin shows maximum growth inhibition of 61% on COLO320 cells and 54% on COLO205 colon cancer cells via i.p. administration of 1 mg/kg in mice. Karenitecin (1.0 mg/kg daily × 5 i.p.) significantly suppresses growth inhibition both in the parental Pgp-negative xenografts and in the Pgp-positive xenografts. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.229 ml | 11.146 ml | 22.292 ml |
5 mM | 0.446 ml | 2.229 ml | 4.458 ml |
10 mM | 0.223 ml | 1.115 ml | 2.229 ml |
5 mM | 0.045 ml | 0.223 ml | 0.446 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!