Irinotecan

ArtNr	S1198-5000
Hersteller	Selleckchem
CAS-Nr.	97682-44-5
Menge	5 g
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 200 mg 5 g
Kategorie	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Colorectal Cancer
Typ	Inhibitors
Specific against	other
Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	(+)-Irinotecan,CPT-11
Similar products	Irinotecan
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	586, 68
Administration	Administered via i.p.
Animal Models	Female nude mice with COLO 320 and WiDr xenografts
Cell lines	LoVo and HT-29 cells
Clinical Trials	Irinotecan has entered in a phase II clinical trial in the treatment of non-small cell lung cancer.
Concentrations	0 uM -100 uM
Dosages	20 mg/kg
Formulation	0.9% NaCl
IC50	15.8 uM, 15.8 uM, 15.8 uM, 15.8 uM, 15.8 uM, 15.8 uM
In vitro	Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. [1] The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue. [2] Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. [3] Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38. [4]
In vivo	In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. [5] A single dose of Irinotecan significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group shows significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group. [6]
Incubation Time	48 hours
Method	Exponentially growing cells (LoVo and HT-29 cells) are seeded in 20 cm2 Petri dishes with an optimal cell number for each cell line (2, 104 for LoVo cells, 105 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 Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38.
Solubility (25C)	DMSO 10 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Features	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.

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