Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration.
性状
Solid
IC50 & Target[1][2]
Tublin polymerization; Hedgehog; Parasite
体外研究(In Vitro)
Mebendazole (1 nM-0.1 mM; 72 h) shows inhibition of GL261 mouse glioma cells with IC value of 0.24 μM. Mebendazole (0.1 μM and 1 μM; 24 h) disrupts microtubule polymerization and microtubule structure in 060919 glioblastoma multiforme (GBM) cells.Mebendazole (10 nM-10 μM; 48 h) inhibits Hh signaling and reduces the expression of downstream Hh pathway effectors, by decreasing Gli1 transcript and protein expression in tumor tissues. Mebendazole inhibits Gli1 expression with an IC50 value of 516 nM.Mebendazole (10 nM-10 μM; 48 h) prevents the formation of the primary cilium, and decreases the proliferation and survival of human medulloblastoma cells with constitutive Hh activation.A combination of mebendazole and Vismodegib (HY-10440) achieved additive inhibition of canonical Hh signaling.Mebendazole has effectively
体内研究(In Vivo)
Mebendazole (50 mg/kg; p.o.; once daily for first 20 d and 5 d per week with 2 d off; 45 d) inhibits intracranial tumor growth in the syngeneic GL261 mouse model and 060919 human glioblastoma multiforme (GBM) xenograft mouse model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Bai RY, et al. Antiparasitic mebendazole shows survival benefit in 2 preclinical models of glioblastoma multiforme. Neuro Oncol. 2011 Sep;13(9):974-82. [2]. Larsen AR, et al. Repurposing the antihelmintic mebendazole as a hedgehog inhibitor. Mol Cancer Ther. 2015 Jan;14(1):3-13. [3]. Erdin?ler P, et al. The r
溶解度数据
In Vitro: DMSO : 4.17 mg/mL (14.12 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic) (insoluble)配制储备液