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| 化学名: | ロニダミン | | 英語化学名: | Lonidamine | | 别名: | af1890;1-[(2,4-dichlorophenyl)methyl]indazole-3-carboxylic acid;1H-Indazole-3-carboxylicacid, 1-[(2,4-dichlorophenyl)Methyl]-;1-(2,4-dichlorbenzyl)-indazole-3-carboxylicacid;1-(2,4-dichlorobenzyl)-1h-indazole-3-carboxylicaci;Lonidamine, >=99%;1-(3,4-dichlorobenzyl)-1H-indazole-3-carboxylic acid;DICLONDAZOLIC ACID | | CAS番号: | 50264-69-2 | | 分子式: | C15H10Cl2N2O2 | | 分子量: | 321.16 | | EINECS: | 256-510-0 | | カテゴリ情報: | API;DORIDAMINA;inhibitor;Anti-cancer&immunity | | Mol File: | 50264-69-2.mol |  |
| 融点 | 207-209°C | | 沸点 | 537.9±45.0 °C(Predicted) | | 比重(密度) | 1.4835 (rough estimate) | | 屈折率 | 1.6070 (estimate) | | 貯蔵温度 | Sealed in dry,2-8°C | | 溶解性 | Soluble in DMSO (up to 25 mg/ml). | | 外見 | solid | | 酸解離定数(Pka) | 3.00±0.10(Predicted) | | 色 | White | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. | | InChIKey | WDRYRZXSPDWGEB-UHFFFAOYSA-N | | CAS データベース | 50264-69-2(CAS DataBase Reference) |
| 主な危険性 | T | | Rフレーズ | 60-22-40 | | Sフレーズ | 53-22-36/37/39-45 | | WGK Germany | 3 | | RTECS 番号 | NK7886000 | | HSコード | 29339900 | | 毒性 | LD50 in mice, rats (mg/kg): 900, 1700 orally; 435, 525 i.p. (Heywood) |
| | ロニダミン Usage And Synthesis |
| 効能 | 抗悪性腫瘍薬 | | 説明 | Lonidamine is an antineoplastic agent reportedly effective for the treatment of various
cancers, including lung, breast, prostate and brain tumors. Its clinical effect appears to be
associated with changes in cellular energy metabolism. | | Originator | Angelini (Italy) | | 使用 | contraceptive, spermicidal | | 定義 | ChEBI: A member of the class of indazoles that is 1H-indazole that is substituted at positions 1 and 3 by 2,4-dichlorobenzyl and carboxy groups, respectively. | | brand name | Doridamina | | 生物活性 | Anticancer and antispermatogenic agent in vitro and in vivo . Inhibits cellular energy metabolism in some cells via inhibition of mitochondrial hexokinase. Also blocks CFTR Cl - channels in vitro . | | Biochem/physiol Actions | Inhibits the energy metabolism of neoplastic cells by interfering with hexokinase and disrupting uncoupler-stimulated mitochondrial electron transport; damages cell and mitochondrial membranes. | | 貯蔵 | Room temperature | | 参考文献 | 1) Gatto?et al. (2002),?Recent studies on lonidamine, the lead compound of the antispermatogenic indazol-carboxylic acids; Contraception,?65?277
2) Floridi?et al., (1981),?Effect of Lonidamine on the Energy Metabolism of Ehrlich Ascites Tumor Cells; Cancer Res.,?41?4661
3) Ravagnan?et al. (1999),?Lonidamine triggers apoptosis via a direct, Bcl-2-inhibited effect on the mitochondrial permeability transition pore; Oncogene,?18?2537
4) Ben-Horin?et al. (1995),?Mechanism of Action of the Antineoplastic Drug Lonidamine: 31P and 13C Nuclear Magnetic Resonance Studies; Cancer Res.?55?2814
5) Nath?et al. (2016),?Mechanism of antineoplastic activity of lonidamine; Biochim.Biophys.Acta Reviews on Cancer?1866?151 |
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