产品说明书

Lonidamine

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Chemical Structure| 50264-69-2 同义名 : AF-1890;Diclondazolic Acid;Doridamina;DICA
CAS号 : 50264-69-2
货号 : A339788
分子式 : C15H10Cl2N2O2
纯度 : 99%
分子量 : 321.158
MDL号 : MFCD00866285
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(155.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 7 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

生物活性
描述 Lonidamine is a selective inhibitor that inhibits aerobic glycolysis in murine tumor cells. Lonidamine at a concentration of 0.32mM reduced the respiration of germ cells and submaxillary gland cells by 58%. Treatment of Serotoli’s cells and hepatocytes with lonidamine led to 16% and 6% inhibition of oxygen consumption, respectively. Lonidamine at the same concentration inhibited oxygen consumption of Ehrlich ascites tumor cells and sarcoma 180 cells by 58 and 63%, respectively, but enhanced aerobic glycolysis in normal cells, such as germ cells (57%) and submaxillary gland cells (35%). Lonidamine at a concentration of 20mM reduced the amount of glucose 6-phosphate formed by the mitochondria of Ehrlich ascites tumor cells by >50%.[2] Lonidamine inhibited glioma cell proliferation with an IC50 value of 200μM. Treatment of SNb-19 cells with 100 or 200μM lonidamine resulted in a slight decrease in the S-phase component of the cell cycle (3% and 9%, respectively). The administration of nude mice with lonidamine (160 mg/kg body weight/day) and diazepam (1 mg/kg body weight/day) via intraperitoneal injection for 10 days inhibited the growth of TG-8-OZ glioma xenograft (78% inhibition) 7 days after the treatment.[1]
作用机制 Lonidamine is a derivative of indazole-3-carboxylic acid that affects energy metabolism in tumor cells by inhibiting mitochondria-bound hexokinase and the electron transport chain.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.11mL

0.62mL

0.31mL

15.57mL

3.11mL

1.56mL

31.14mL

6.23mL

3.11mL
参考文献

[1]Miccoli L, Poirson-Bichat F, Sureau F, Bras Gonçalves R, Bourgeois Y, Dutrillaux B, Poupon MF, Oudard S. Potentiation of lonidamine and diazepam, two agents acting on mitochondria, in human glioblastoma treatment. J Natl Cancer Inst. 1998 Sep 16;90(18):1400-6

[2]De Martino C, Battelli T, et al. Effects of Lonidamine on murine and human tumor cells in vitro. A morphological and biochemical study. Oncology. 1984;41 Suppl 1:15-29.

[3]Miccoli L, Poirson-Bichat F, Sureau F, Bras Gonçalves R, Bourgeois Y, Dutrillaux B, Poupon MF, Oudard S. Potentiation of lonidamine and diazepam, two agents acting on mitochondria, in human glioblastoma treatment. J Natl Cancer Inst. 1998 Sep 16;90(18):1400-6

[4]Floridi A, Paggi MG, Marcante ML, Silvestrini B, Caputo A, De Martino C. Lonidamine, a selective inhibitor of aerobic glycolysis of murine tumor cells. J Natl Cancer Inst. 1981 Mar;66(3):497-9