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 70 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Topoisomerase Products |
---|
ICRF-193
ICRF-193 is an TopoII inhibitor. |
Topoisomerase II inhibitor 15
Topoisomerase II inhibitor 15 is a Topoisomerase II inhibitor. |
Topoisomerase II inhibitor 13
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. |
ICRF-196
ICRF-196 is an racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193. |
Cholesteryl hemisuccinate
Cholesteryl hemisuccinate is a with hepatoprotective an anticancer activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.