Irinotecan
Référence M4465-50mg
Conditionnement : 50mg
Marque : AbMole Bioscience
(+)-Irinotecan; CPT-11; VAL-413
Quality Control & Documentation
Biological Activity
Irinotecan is an inhibitor of Topoisomerase I, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC50s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC50 of 1.3 μM.
Irinotecan (CPT-11, 5 mg/kg) significantly inhibits the growth of tumors by intratumoral injection daily for 5 days, on two consecutive weeks in rats, and such effects also occur via continuous intraperitoneal infusion by osmotic minipump into mice. However, Irinotecan (10 mg/kg) shows no effect on the growth of tumor by i.p. Irinotecan (CPT-11, 100-300 mg/kg, i.p.) apparently suppresses tumor growth of HT-29 xenografts in athymic female mice by day 21.
Product Citations
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Frontiers in Anti-Cancer Drug Discovery. 2015;64-114 .
Concepts of Anticancer Treatment and Pharmacogenomics in Cancer Treatments
Irinotecan purchased from AbMole
Chemical Information
Molecular Weight | 586.68 |
Formula | C33H38N4O6 |
CAS Number | 97682-44-5 |
Solubility (25°C) | DMSO ≥ 20 mg/mL |
Storage | 2-8°C, protect from light, dry, sealed |
Conversion of different model animals based on BSA (PMID: 27057123)
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.
References
[1] Filemon S Dela Cruz, et al. Genome Med. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma
[2] Mei-Yun Huang, et al. Apoptosis. Chemotherapeutic agent CPT-11 eliminates peritoneal resident macrophages by inducing apoptosis
[3] C Morales, et al. J Neurooncol. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor