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| | 4α-エチル-4β-ヒドロキシ-10-アミノ-3,4,12,14-テトラヒドロ-1H-ピラノ[3',4':6,7]インドリジノ[1,2-b]キノリン-3,14-ジオン 製品概要 |
| 化学名: | 4α-エチル-4β-ヒドロキシ-10-アミノ-3,4,12,14-テトラヒドロ-1H-ピラノ[3',4':6,7]インドリジノ[1,2-b]キノリン-3,14-ジオン | | 英語化学名: | 9-Aminocamptothecin | | 别名: | 4':6,7)indolizino(1,2-B)quinoline-3,14(4H,12H)-dione;4':6,7)indolizino(1,2-B)quinoline-3,14(4H,12H)-dione, 10-amino-4-ethyl-4-hydroxy-, (S)-;CAMPTOTHECIN, 9-AMINO-(RG);(S)-10-AMino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione;(S)-10-Amino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]-indolizino[1,2-b]quinoline-3,14(4H,12H)-di;CAMPTOTHECIN, 9-AMINO-;AMinocaMptothecin;9-AMINO-CAMPTOTHECIN | | CAS番号: | 91421-43-1 | | 分子式: | C20H17N3O4 | | 分子量: | 363.37 | | EINECS: | | | カテゴリ情報: | Pharmaceutical Raw Materials;Alkaloids;Natural Anti-cancer Medical Materials and It's Derivatives | | Mol File: | 91421-43-1.mol | ![4α-エチル-4β-ヒドロキシ-10-アミノ-3,4,12,14-テトラヒドロ-1H-ピラノ[3',4':6,7]インドリジノ[1,2-b]キノリン-3,14-ジオン](CAS/GIF/91421-43-1.gif) |
| | 4α-エチル-4β-ヒドロキシ-10-アミノ-3,4,12,14-テトラヒドロ-1H-ピラノ[3',4':6,7]インドリジノ[1,2-b]キノリン-3,14-ジオン 物理性質 |
| 融点 | 142.0-145.0 °C | | 沸点 | 819.6±65.0 °C(Predicted) | | 比重(密度) | 1.55±0.1 g/cm3(Predicted) | | 貯蔵温度 | 2-8°C(protect from light) | | 溶解性 | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide | | 外見 | powder to crystal | | 酸解離定数(Pka) | 11.23±0.20(Predicted) | | 色 | Light yellow to Yellow to Orange | | Merck | 14,431 | | InChIKey | FUXVKZWTXQUGMW-FQEVSTJZSA-N | | CAS データベース | 91421-43-1(CAS DataBase Reference) |
| RTECS 番号 | UQ0490500 | | HSコード | 29349990 |
| | 4α-エチル-4β-ヒドロキシ-10-アミノ-3,4,12,14-テトラヒドロ-1H-ピラノ[3',4':6,7]インドリジノ[1,2-b]キノリン-3,14-ジオン Usage And Synthesis |
| 外観 | うすい黄色～黄色～黄赤色粉末～結晶 | | 使用 | 9-Amino Camptothecin is a derivative of Camptothecin (C175150), as antitumor agent. | | 定義 | ChEBI: 9-Aminocamptothecin is a pyranoindolizinoquinoline. | | 生物活性 | 9-amino camptothecin is a topoisomerase i inhibitor [1][2].dna topoisomerases relax dna torsional strain generated during replication, transcription, recombination, repair, and chromosome condensation. the relaxation of dna supercoiling by topoisomerase i is enabled by a mechanism of controlled rotation around a transient dna single-strand break. camptothecin (cpt) is isolated from the bark of the chinese tree camptotheca accuminata [3].9-amino camptothecin, a water-soluble camptothecin analogue, is a topoisomerase i inhibitor. in human ht-29 colon adenocarcinoma, 9-amino camptothecin (9-ac) exhibited cytotoxicity with ic50 value of 19 nm. 9-ac also induced dna damage in whole cells and nuclei at a concenstration of 85 nm and 21 nm, respectively [1].9-amino camptothecin had greater activity than camptothecin against human tumour xenografts, including lewis lung carcinoma and b16 melanoma. 9-ac had entered phase ii trials. in patients with advanced solid tumours, 9-amino camptothecin exhibited anti-tumor activity [1][2]. | | 参考文献 | [1]. rothenberg, m.l. topoisomerase i inhibitors: review and update. annals of oncology 8(9), 837-855 (1997).
[2]. dancey j, eisenhauer ea. current perspectives on camptothecins in cancer treatment. br j cancer. 1996 aug;74(3):327-38.
[3]. drwal mn1, agama k, wakelin lp, et al. exploring dna topoisomerase i ligand space in search of novel anticancer agents. plos one. 2011;6(9):e25150. |
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