产品描述: Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity. |
靶点:
Topoisomerase I;Topoisomerase |
体外研究:
Karenitecin is a topoisomerase I inhibitor, with potent anti-cancer activity. Karenitecin inhibits cell growth of A253 cells with IC10, IC50, and IC90 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 IC50s 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 |
参考文献:
1. Yin MB, et al. Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. Mol Pharmacol. 2000 Mar;57(3):453-9. 2. Van Hattum AH, et al. New highly lipophilic camptothecin BNP1350 is an effective drug in experimental human cancer. Int J Cancer. 2000 Oct 15;88(2):260-6. |
溶解性:
Soluble in DMSO |
保存条件:
2-8℃ |
配置溶液浓度参考:
|
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 |
50 mM |
0.045 ml |
0.223 ml |
0.446 ml |
|
注意: |
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