Name | Karenitecin |
Synonyms | DB 172 BNP 1350 MCC 12824 Cositecan Karenitecin |
CAS | 203923-89-1 |
Molecular Formula | C25H28N2O4Si |
Molar Mass | 448.59 |
Density | 1.29±0.1 g/cm3(Predicted) |
Boling Point | 727.2±60.0 °C(Predicted) |
Solubility | Soluble in DMSO, insoluble in water |
pKa | 11.27±0.20(Predicted) |
Storage Condition | 2-8℃ |
MDL | MFCD09833216 |
In vitro study | 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. |
In vivo study | 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 |