Irinotecan HCl Trihydrate

Description

Name: Irinotecan HCl Trihydrate
Brand: Selleckchem
SKU: S2217

Description

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

In vitro

Irinotecan (20 mg/kg i.p.) induces tumor growth inhibition of 92% in COLO 320 xenograft mice model. ^[3]Irinotecan (100 mg/kg) significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver in male Wistar rats. ^[4] Irinotecan (200 mg/kg) induces severe diarrhea and lethality in treated rats. ^[5]

Irinotecan (20 mg/kg i.p.) induces a maximum growth inhibition of 92% on day 42 in COLO 320 xenograft mice model. ^[3] Irinotecan (100 mg/kg) significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver in male Wistar rats. ^[4] Irinotecan (200 mg/kg) induces a 93-100% incidence of severe diarrhea and an 86-100% incidence of lethality in treated rats, while IL-15 (100 mg/kg or 400 mg/kg) protects against CPT-11-induced toxicity. CPT-11 (200 mg/kg) alone produces serious damage to duodenal villi and colonic crypts in rats. ^[5]

Irinotecan is a prodrug which needs to be transformed by carboxylesterases to its active metabolite SN-38.

Irinotecan HCl Trihydrate

Catalog No.S2217

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	LoVo and HT-29 cells
Concentrations	15.8 μM
Incubation Time	24 hours or 40 hours
Method	Exponentially growing cells are seeded in 20 cm² Petri dishes with an optimal cell number for each cell line (2 × 10⁴ for LoVo cells, 1 × 10⁴ for HT-29 cells). They are treated 2 days later with increasing concentrations of irinotecan or SN-38 for one cell doubling time (24 hours for LoVo cells, 40 hours for HT-29 cells). After washing with 0.15 M NaCl, the cells are further grown for two doubling times in normal medium, detached from the support with trypsin-EDTA and counted in a hemocytometer. The IC50 values are then estimated as the drug concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinote

Animal Models	COLO 320 xenograft mice model
Dosages	20 mg/kg
Administration	Intraperitoneal injection
Solubility	30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00004919	Completed	Unspecified Childhood Solid Tumor, Protocol Specific	National Cancer Institute (NCI)	1999-12	Phase 1
NCT00393094	Terminated	High-Grade Gliomas	National Institutes of Health Clinical Center (CC)\|National Cancer Institute (NCI)	2006-09	Phase 2
NCT00483834	Completed	Colorectal Cancer	University Health Network, Toronto\|Hoffmann-La Roche	2006-12	Phase 2
NCT00160875	Completed	Esophageal Cancer	University Health Network, Toronto\|Pfizer	2009-08	Phase 2\|Phase 3
NCT02015754	Not yet recruiting	Colorectal Cancer	Sidney Kimmel Comprehensive Cancer Center	2013-12	Phase 2

Solubility (25°C) *	In vitro	DMSO	100 mg/mL (147 mM)
		Water	1 mg/mL (1 mM)
		Ethanol	7 mg/mL (10 mM)
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.