Irinotecan (CPT-11)

製品コードS1198 バッチS119808

化学情報

	Synonyms	(+)-Irinotecan,CPT-11	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₃H₃₈N₄O₆
	分子量	586.68	CAS No.	97682-44-5
Solubility (25°C)*	体外	DMSO	25 mg/mL (42.61 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Irinotecanは、LoVo細胞およびHT-29細胞に対するTopoisomerase I阻害剤であり、IC50値はそれぞれ15.8 μMおよび5.17 μMです。
in vitro	Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. This compound 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 this chemical is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. The lactone E-ring of this compound 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 this agent to SN-38. At equal concentrations of this drug and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from this compound in both tumour and normal tissue. It is also converted to SN-38 in intestines, plasma and tumor tissues. This agent is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38.
in vivo	In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. A single dose of this compound 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.
特徴	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LoVo and HT-29 cells
	濃度	0 μM -100 μM
	反応時間	48 hours
	実験の流れ	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 this compound or this chemical concentrations responsible for 50% growth inhibition as compared with cells incubated without this compound or this chemical.
動物実験	動物モデル	Female nude mice with COLO 320 and WiDr xenografts
	投薬量	20 mg/kg
	投与方法	Administered via i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/11914913/
https://pubmed.ncbi.nlm.nih.gov/16842384/
https://pubmed.ncbi.nlm.nih.gov/15182436/

https://pubmed.ncbi.nlm.nih.gov/9649129/
https://pubmed.ncbi.nlm.nih.gov/9033637/
https://pubmed.ncbi.nlm.nih.gov/21046105/
https://pubmed.ncbi.nlm.nih.gov/16317751/

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カスタマーフィードバック

: , , Biomaterials, 2015, 72:74-89.

: Data independently produced by Dr. Edita Aksamitiene from Thomas Jefferson University, , Dr. Mikhail Menshikov of Cardiology Research Center

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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