Flubendazole

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Chemical Structure| 31430-15-6 同义名 : NSC 313680; Flumoxanal; R-17899; R-17889
CAS号 : 31430-15-6
货号 : A100488
分子式 : C16H12FN3O3
纯度 : 98%
分子量 : 313.28
MDL号 : MFCD00871999
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

IP 2% DMSO+water 0.1 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

生物活性
描述 Flubendazole is a widely used anthelmintic drug belonging to benzimidazole group. The molecular mechanism of action of flubendazole is based on its specific binding to tubulin, which results in disruption of microtubule structure and function, and in the interference with the microtubule-mediated transport of secretory vesicles in absorptive tissues of helminths[3]. In animals, flubendazole has good oral bioavailability from an ASD formulation ranging from 15% in dogs, 27% in rats to more than 100% in jirds. Regarding genotoxicity, flubendazole was negative in the Ames test, but positive in the in vivo micronucleus test[4]. Flubendazole exerts anti-proliferation and pro-apoptosis effects in Glioma through affecting the cell cycle and intrinsic apoptotic signaling[5]. Flubendazole is a novel small molecule inhibitor of not only melanoma growth and spread but also of PD-1(programmed cell death protein-1) and MDSC (myeloid-derived suppressor cell) [6]. Flubendazole inhibited the cell survival of different ESCC (esophageal squamous cell carcinoma) cells and induced cell apoptosis in both EC9706 and TE1 cells. In addition, flubendazole also showed a synergistic effect on ESCC cells when combined with doxorubicin[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.96mL

3.19mL

1.60mL

31.92mL

6.38mL

3.19mL
参考文献

[1]Elissondo M, Dopchiz M, et al. In vitro effects of flubendazole on Echinococcus granulosus protoscoleces. Parasitol Res. 2006 Mar;98(4):317-23.

[2]Moreno L, Alvarez L, et al. Integrated pharmacological assessment of flubendazole potential for use in sheep: disposition kinetics, liver metabolism and parasite diffusion ability. J Vet Pharmacol Ther. 2004 Oct;27(5):299-308.

[3]Čáňová K, Rozkydalová L, Rudolf E. Anthelmintic Flubendazole and Its Potential Use in Anticancer Therapy. Acta Medica (Hradec Kralove). 2017;60(1):5‐11

[4]Lachau-Durand S, Lammens L, van der Leede BJ, et al. Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients. PLoS Negl Trop Dis. 2019;13(1):e0007026. Published 2019 Jan 16

[5]Zhou X, Liu J, Zhang J, Wei Y, Li H. Flubendazole inhibits glioma proliferation by G2/M cell cycle arrest and pro-apoptosis. Cell Death Discov. 2018;4:18. Published 2018 Feb 14

[6]Li Y, Acharya G, Elahy M, Xin H, Khachigian LM. The anthelmintic flubendazole blocks human melanoma growth and metastasis and suppresses programmed cell death protein-1 and myeloid-derived suppressor cell accumulation. Cancer Lett. 2019;459:268‐276

[7]Tao J, Zhao H, Xie X, et al. The anthelmintic drug flubendazole induces cell apoptosis and inhibits NF-κB signaling in esophageal squamous cell carcinoma. Onco Targets Ther. 2019;12:471‐478. Published 2019 Jan 9