Irinotecan (CPT-11)

別名：(+)-Irinotecan,CPT-11

製品コード：S1198 純度：99.99%

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。

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：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（59）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Irinotecan (CPT-11)関連製品

関連ターゲット	Topo I Topo II Topo IV	もっと見る
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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

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
HCT116	cytotoxicity assay	10 μM	ID50=540 nM
VM46	cytotoxicity assay	10 μM	ID50=220 nM
MCF-7ADR	cytotoxicity assay	10 μM	ID50>500 nM
RPMI8402	cytotoxicity assay	100 μM	IC50=570 nM
A-549	cytotoxicity assay	~20 μM	IC50=6.528 μM
LOVO	cytotoxicity assay	~20 μM	IC50=9.015 μM
MCF7	cytotoxicity assay	~20 μM	IC50=17.403 μM
Hep G2	Growth inhibitory assay	~10 μM	IC50=5.94 μM
Hep 3B	Growth inhibitory assay	~10 μM	IC50=4.73 μM
Hep 2.2.	Growth inhibitory assay	~10 μM	IC50>10 μM
KB	cytotoxicity assay	~20 μM	IC50=9.83 μM
KB-vin	cytotoxicity assay	~20 μM	IC50>20 μM
L1210	cytotoxicity assay		IC50=1.2 µM
LS174T	Growth inhibitory assay		IC50=1.16 μM
KB3-1	cytotoxicity assay		IC50=0.68 μM
KBV-1	cytotoxicity assay		IC50=40 μM
KBH5.0	cytotoxicity assay		IC50=7.4 μM
A549	cytotoxicity assay		IC50=4.61 μM
MDA-MB-435	cytotoxicity assay		IC50=1.14 μM
LOVO	cytotoxicity assay		IC50=4.99 μM
MDA-MB-435	cytotoxicity assay		IC50=17 μM
NCI60	Growth inhibitory assay		GI50=14.1254 μM
H460	cytotoxicity assay		IC50=0.015 μM
PC-3	cytotoxicity assay		IC50=0.22 μM
HT29	cytotoxicity assay		IC50=0.004 μM
SK-MEL-2	cytotoxicity assay		IC50=0.1 μM
A375	cytotoxicity assay		IC50=0.004 μM
Malme-3M	cytotoxicity assay		IC50=0.2 μM
DU 145	cytotoxicity assay		IC50=0.2 μM
LNCaP	cytotoxicity assay		IC50=0.009 μM
IGROV-1	cytotoxicity assay		IC50=0.03 μM
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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。

特性

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

Targets

Topo I
(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. 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.
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 this compound or this chemical concentrations responsible for 50% growth inhibition as compared with cells incubated without this compound or this chemical.

In Vivo
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.
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 2026-06-18)
NCT06365008	NOT_YET_RECRUITING	Unresectable/Metastatic Gastric Cancer	Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University	2026-06	PHASE2
NCT07521605	NOT_YET_RECRUITING	Rectal Cancer Patients	Guangdong Provincial People's Hospital	2026-05-20	PHASE2
NCT07381764	NOT_YET_RECRUITING	Metastatic Colorectal Cancer (CRC)	Gruppo Oncologico Italia Meridionale	2026-03-30	PHASE2
NCT07549321	RECRUITING	High-Risk Neuroblastoma	Renaissance Pharma Ltd.	2026-03-30	PHASE2; PHASE3
NCT07585279	NOT_YET_RECRUITING	Metastatic Colorectal Cancer (CRC); Liposomal Irinotecan; Second-Line	Hebei Medical University Fourth Hospital	2026-05-20	PHASE2; PHASE3
NCT06401330	RECRUITING	Stage I Mixed Cell Type Kidney Wilms Tumor; Stage II Mixed Cell Type Kidney Wilms Tumor; Stage III Mixed Cell Type Kidney Wilms Tumor; Stage IV Mixed Cell Type Kidney Wilms Tumor	Children's Oncology Group	2025-04-15	PHASE3

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/ + 展開

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/

+ 展開

化学情報

分子量	586.68	化学式	C₃₃H₃₈N₄O₆
CAS No.	97682-44-5	SDF	Download Irinotecan (CPT-11) 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ケ月-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
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	7%DMSO 1 93%Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.100mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	6.000mg/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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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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