|
受注：045-509-1970 |
技術サポート：[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
|
Synonyms | (+)-Irinotecan,CPT-11 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C33H38N4O6 |
|||
| 分子量 | 586.68 | CAS No. | 97682-44-5 | |
| Solubility (25°C)* | 体外 | DMSO | 25 mg/mL (42.61 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 is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, 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 | Administered via i.p. |
参考
カスタマーフィードバック
-
, , Biomaterials, 2015, 72:74-89.
-
Data independently produced by Dr. Edita Aksamitiene from Thomas Jefferson University, , Dr. Mikhail Menshikov of Cardiology Research Center
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：
| In-situ cryo-immune engineering of tumor microenvironment with cold-responsive nanotechnology for cancer immunotherapy [ Nat Commun, 2023, 14(1):392] | PubMed: 36693842 |
| Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer [ Cell Rep Med, 2023, 4(9):101162] | PubMed: 37597521 |
| Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer [ Cell Rep Med, 2023, S2666-3791(23)00315-4] | PubMed: 37597521 |
| Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance [ EMBO Mol Med, 2023, e16235.] | PubMed: 36652375 |
| TPX2 enhances the transcription factor activation of PXR and enhances the resistance of hepatocellular carcinoma cells to antitumor drugs [ Cell Death Dis, 2023, 14(1):64] | PubMed: 36707511 |
| Spatial and clonality-resolved 3D cancer genome alterations reveal enhancer-hijacking as a potential prognostic marker for colorectal cancer [ Cell Rep, 2023, 42(7):112778] | PubMed: 37453058 |
| Genetic assessment of pathogenic germline alterations in lysosomal genes among Asian patients with pancreatic ductal adenocarcinoma [ J Transl Med, 2023, 21(1):730] | PubMed: 37848935 |
| ATG4B and pS383/392-ATG4B serve as potential biomarkers and therapeutic targets of colorectal cancer [ Cancer Cell Int, 2023, 23(1):63] | PubMed: 37038218 |
| High CD142 Level Marks Tumor-Promoting Fibroblasts with Targeting Potential in Colorectal Cancer [ Int J Mol Sci, 2023, 24(14)11585] | PubMed: 37511344 |
| Dihydroergotamine ameliorates liver fibrosis by targeting transforming growth factor β type II receptor [ World J Gastroenterol, 2023, 29(20):3103-3118] | PubMed: 37346154 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。