Irinotecan (CPT-11) HCl Trihydrate

製品コード:S2217

For research use only.

Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.

Irinotecan (CPT-11) HCl Trihydrate化学構造

CAS No. 136572-09-3

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 33500
JPY 13600
JPY 36800
JPY 78100

代表番号: 03-5615-9297|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(74)

製品安全説明書

Topoisomerase阻害剤の選択性比較

相関Topoisomerase製品

生物活性

製品説明 Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.
特性 Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
ターゲット
Topo I [1]
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Hep3B NFLDbplCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEGxTFI4OiCqcoO= NV\VOnYySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZA{SiClZXzsd{Bi\nSncjC3NkBpenNiYomgXHRVKGG|c3H5MEBIUTVyIE2gOE44OyEQvF2u NVHDb3E1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3PVY6PTZpPkG5O|k3QTV4PD;hQi=>
HepG2 MkL4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGXsWlc4OiCqcoO= M12yPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGjUWEBie3OjeTygS2k2OCB;IEWuPVQh|ryPLh?= M2rCSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{m2PVU3Lz5zOUe5Olk2PjxxYU6=
NCI60 NIG5[oJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGj0TFFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBPS0l4MDDj[YxteyCkeTDTRnIh[XO|YYmsJGdKPTBiPTCxOE4yOjV2IN88UU4> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTB|NUOzOEc,OjFyM{WzN|Q9N2F-
Hep3B NUjlXZBOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHzJTIU4OiCqcoO= M1fBRWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhmeDOEIHPlcIx{KGGodHXyJFczKGi{czDifUBZXFRiYYPzZZktKEeLNUCgQUA1Njd|IN88UU4> MnP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{myOVQoRjJ{MEe5NlU1RC:jPh?=
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BT-12 M2HNXJFJXFNiYYPzZZk> MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? Ml:zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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TC32 NGnOSGlyUFSVIHHzd4F6 M37NepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KE:{dHjv[49v[WxiM1Sgeoli[mmuaYT5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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アッセイ
Methods Test Index PMID
Western blot AMPK / p-AMPK / mTOR / p-mTOR / p70S6K / p-p70S6K ; NFκB p65 / phospho-NFκB p65 / NFκB p50 / IκBα / p27Kip1 ; TopI / pAKT / pMEK / pERK / p-p38 MAPK / pJNK2 25973791 22206574 29237470
Immunofluorescence NFκB 22206574
Growth inhibition assay Cell viability 25973791
体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験:

[1]

  • 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.

動物試験:

[5]

  • 動物モデル:Female nude mice with COLO 320 and WiDr xenografts.
  • 投薬量:20 mg/kg
  • 投与方法:Intraperitoneal injection

溶解度 (25°C)

体外

化学情報

分子量 677.18
化学式

C33H38N4O6.HCl.3H2O

CAS No. 136572-09-3
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl

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。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05277766 Not yet recruiting Drug: PIPAC with Nal-IRI 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 September 2022 Phase 1
NCT05379790 Recruiting Drug: Irinotecan|Drug: CAPOX Gastric Cancer|Peritoneal Metastases Erasmus Medical Center May 25 2022 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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