Irinotecan

別名:(+)-Irinotecan,CPT-11

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

Irinotecan化学構造

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
JPY 29500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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現在のバッチを見る: 純度: 99.99%
99.99

Irinotecan関連製品

Topoisomerase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 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
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

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

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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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)

mg/kg g μL

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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