Product Name
Irinotecan hydrochloride
Synonyms
(+)-Irinotecan hydrochloride; CPT-11 hydrochloride; VAL-413
Description
Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
Solubility
DMSO : 125 mg/mL(200.60 mM;Need ultrasonic) H2O : 3.33 mg/mL(5.34 mM;Need ultrasonic)
Source
Plants >Nyssaceae > Camptotheca acuminataDecne.
Storage
4℃, sealed storage, away from moisture
IC50 & Target
Plasmodium Microbial Metabolite
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
O=C(N1CCC(N2CCCCC2)CC1)OC3=CC=C4N=C5C(CN6C(C(COC([C@@]7(CC)O)=O)=C7C=C65)=O)=C(CC)C4=C3.[H]Cl
In Vivo
Irinotecan hydrochloride (CPT-11 hydrochloride, 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. The two groups of Irinotecan (125 mg/kg) plus TSP-1 (10 mg/kg per day) or Irinotecan (150 mg/kg) in combination TSP-1 (20 mg/kg per day) are nearly equally effective and inhibit tumor growth 84% and 89%, respectively, and both are more effective than Irinotecan alone at doses of 250 and 300 mg/kg.
In Vitro
Irinotecan hydrochloride is a topoisomerase I inhibitor. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC50s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC50 of 1.3 μM.