Irinotecan

別名：(+)-Irinotecan,CPT-11

製品コード：S1198 純度：99.99%

Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

CAS No. 97682-44-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 40500	国内在庫あり
100mg	JPY 29500	国内在庫あり
1g	JPY 145500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（42）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

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シグナル伝達経路

Topoisomeraseシグナル伝達経路

Topoisomerase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	活性情報	PMID
HCT116	cytotoxicity assay	10 μM	ID50=540 nM	11965362
VM46	cytotoxicity assay	10 μM	ID50=220 nM	11965362
MCF-7ADR	cytotoxicity assay	10 μM	ID50>500 nM	11965362
RPMI8402	cytotoxicity assay	100 μM	IC50=570 nM	12747798
A-549	cytotoxicity assay	~20 μM	IC50=6.528 μM	18207748
LOVO	cytotoxicity assay	~20 μM	IC50=9.015 μM	18207748
MCF7	cytotoxicity assay	~20 μM	IC50=17.403 μM	18207748
Hep G2	Growth inhibitory assay	~10 μM	IC50=5.94 μM	19796956
Hep 3B	Growth inhibitory assay	~10 μM	IC50=4.73 μM	19796956
Hep 2.2.	Growth inhibitory assay	~10 μM	IC50>10 μM	19796956
KB	cytotoxicity assay	~20 μM	IC50=9.83 μM	22079254
KB-vin	cytotoxicity assay	~20 μM	IC50>20 μM	22079254
L1210	cytotoxicity assay		IC50=1.2 µM	1846923
LS174T	Growth inhibitory assay		IC50=1.16 μM	18479118
KB3-1	cytotoxicity assay		IC50=0.68 μM	18771930
KBV-1	cytotoxicity assay		IC50=40 μM	18771930
KBH5.0	cytotoxicity assay		IC50=7.4 μM	18771930
A549	cytotoxicity assay		IC50=4.61 μM	20371183
MDA-MB-435	cytotoxicity assay		IC50=1.14 μM	20371183
LOVO	cytotoxicity assay		IC50=4.99 μM	20371183
MDA-MB-435	cytotoxicity assay		IC50=17 μM	20942490
NCI60	Growth inhibitory assay		GI50=14.1254 μM	21035334
H460	cytotoxicity assay		IC50=0.015 μM	21341674
PC-3	cytotoxicity assay		IC50=0.22 μM	21341674
HT29	cytotoxicity assay		IC50=0.004 μM	21341674
SK-MEL-2	cytotoxicity assay		IC50=0.1 μM	21341674
A375	cytotoxicity assay		IC50=0.004 μM	21341674
Malme-3M	cytotoxicity assay		IC50=0.2 μM	21341674
DU 145	cytotoxicity assay		IC50=0.2 μM	21341674
LNCaP	cytotoxicity assay		IC50=0.009 μM	21341674
IGROV-1	cytotoxicity assay		IC50=0.03 μM	21341674
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生物活性

製品説明

Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

特性

Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.

Targets

Topo I ^[1]
(LoVo, HT-29 cells)

In Vitro
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]
細胞実験	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 Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38.

In Vivo
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]
動物実験	動物モデル	Female nude mice with COLO 320 and WiDr xenografts
	投与量	20 mg/kg
	投与経路	Administered via i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05854498	Recruiting	Metastatic Colorectal Cancer	University of Wisconsin Madison\|Ipsen	October 13 2023	Phase 2
NCT05732129	Not yet recruiting	Homologous Recombination Deficiency Alterations Metastatic Colorectal Cancer	Fudan University	March 1 2023	Phase 2
NCT05731518	Recruiting	Small Cell Lung Cancer	Biocity Biopharmaceutics Co. Ltd.	February 23 2023	Phase 1\|Phase 2
NCT06003998	Recruiting	Colorectal Cancer\|Peritoneal Metastases	Catharina Ziekenhuis Eindhoven	December 27 2022	Phase 2
NCT05277766	Recruiting	Peritoneal Carcinomatosis\|Peritoneal Metastases\|Colorectal Cancer\|Small Bowel Cancer\|Appendix Cancer\|Gastric Cancer\|Pancreatic Cancer\|Bile Duct Cancer	University Hospital Ghent\|Kom Op Tegen Kanker\|University Ghent	November 21 2022	Phase 1
NCT05379790	Recruiting	Gastric Cancer\|Peritoneal Metastases	Erasmus Medical Center	May 25 2022	Phase 1

参考
[1] Pavillard V, et al. Cancer Chemother Pharmacol. 2002, 49(4), 329-335. [2] Tobin P, et al. Br J Clin Pharmacol. 2006, 62(1), 122-129. [3] Shingyoji M, et al. Cancer Sci. 2004, 95(6), 537-540. [4] van Ark-Otte J, et al. Br J Cancer. 1998, 77(12), 2171-2176. [5] Jansen WJ, et al. Int J Cancer. 1997, 70(3):335-340. [6] Na YS, et al. Cancer Chemother Pharmacol. 2011, 68(2), 389-398. [7] Wagner LM, et al. Pediatr Blood Cancer. 2007, 48(2), 132-139. + 展開

参考

+ 展開

化学情報

分子量	586.68	化学式	C₃₃H₃₈N₄O₆
CAS No.	97682-44-5	SDF	Download Irinotecan SDFをダウンロードする
Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 25 mg/mL ( (42.61 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	7%DMSO 1 93%Corn oil	2.1mg/ml (3.58mM)	Taking the 1 mL working solution as an example, add 70 μL of 30 mg/ml clear DMSO stock solution to 930 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	6.0mg/ml (10.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.5mg/ml (0.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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