Irinotecan HCl Trihydrate

製品コードS2217 バッチS221705

印刷

化学情報

Chemical Structure Synonyms CPT-11 HCl Trihydrate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C33H38N4O6.HCl.3H2O
分子量 677.18 CAS No. 136572-09-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (147.67 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 HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively.
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]
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]
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 Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38.
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 Intraperitoneal injection

カスタマーフィードバック

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

Data from [Data independently produced by , , Biomaterials, 2015, 72:74-89]

Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(2):508-520]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Artesunate ameliorates irinotecan-induced intestinal injury by suppressing cellular senescence and significantly enhances anti-tumor activity [ Int Immunopharmacol, 2023, 119:110205] PubMed: 37104917
Cutoff value of IC50 for drug sensitivity in patient-derived tumor organoids in colorectal cancer [ iScience, 2023, 26(7):107116] PubMed: 37426352
The role of pregnane X receptor (PXR-in cancer drug resistance and identification of novel PXR antagonists [ Tübingen, 2023, ] PubMed: None
p53 controls choice between apoptotic and non-apoptotic death following DNA damage [ bioRxiv, 2023, 2023.01.17.524444] PubMed: 36712034
3D imaging analysis on an organoid-based platform guides personalized treatment in pancreatic ductal adenocarcinoma [ J Clin Invest, 2022, 132(24)e151604] PubMed: 36282600
Colorectal Cancer Patient-Derived 2D and 3D Models Efficiently Recapitulate Inter- and Intratumoral Heterogeneity [ Adv Sci (Weinh), 2022, e2201539] PubMed: 35652270
A microfluidic Braille valve platform for on-demand production, combinatorial screening and sorting of chemically distinct droplets [ Nat Protoc, 2022, 10.1038/s41596-022-00740-4] PubMed: 36261631
Targeting BCL-XL in fibrolamellar hepatocellular carcinoma [ JCI Insight, 2022, 7-17e161820] PubMed: 36073545
Assay establishment and validation of a high-throughput organoid-based drug screening platform [ Stem Cell Res Ther, 2022, 13(1):219] PubMed: 35619149
Hepatic ROS Mediated Macrophage Activation Is Responsible for Irinotecan Induced Liver Injury [ Cells, 2022, 11(23)3791] PubMed: 36497051

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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