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Irinotecan hydrochloride trihydrate prevents DNA from unwinding by inhibition of topoisomerase 1. Irinotecan (100 mg/kg) significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver in male Wistar rats. Irinotecan (20 mg/kg i.p.) induces tumor growth inhibition of 92% in COLO 320 xenograft mice model. Irinotecan is activated by hydrolysis to SN-38. The inhibition of topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and transcription. Irinotecan is currently in phase 2 clinical trials for the treatment of Non-small Cell Lung Cancer.
| Molecular Weight | 677.18 |
| Formula | C33H38N4O6.HCl.3H2O |
| CAS Number | 136572-09-3 |
| Solubility (25°C) | DMSO 49 mg/mL Water 1 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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