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Nocodazole, an anti-mitotic drug, is a rapidly-reversible inhibitor of microtubule polymerization which inhibits Abl, Abl(E255K) and Abl(T315I)with theIC50 value of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively[1].

In vitro: Nocodazolewas a high-affinity ligand for the cancer-related kinases including Abl phosphorylated, c-Kit, BRAF, and MEK with the Kd values of 0.091 μM, 1.6 μM, 1.8 μM and 1.6 μM, respectively. In addition, the Kd for Abl(E255K) phosphorylated, Abl(T315I) phosphorylated, BRAF(V600E) and PI3Kγ was 0.12 μM, 0.17 μM, 1.1 μM and 1.5 μM, respectively. In chronic lymphocytic leukemia cells, Nocodazole induced apoptosis. In some human colon carcinoma cells, Nocodazole decrease D apoptosis. Also, Nocodazole inhibited insulin-stimulated glucose transport. Nocodazole impaired the morphology and directionality of migrating medial gan-glionic eminence cells [1]. At high concentrations, Nocodazole rapidly depolymerized microtubules in cells, while low concentrations of Nocodazole inhibited microtubule dynamic instability [2].In SH-SY5Y cells, Nocodazole disrupted microtubules by binding to β-tubulin, prevented the formation of one of the two interchain disulfide linkages and impaired the transport of vesicles. Nocodazole significantly attenuated METH-induced cell death and lysosomal dysfunction [3]. Nocodazole (≥ 50 nM) resulted in a rapid reduction in fibroblast locomotion to a new rate that was maintained for > 2 hours. Nocodazole(100 nM) decreased the rate of locomotion by more than 60%; and 300 nM nocodazole completely stopped cell locomotion[4].

In vivo: In athymic mice bearing COLO 205 tumor xenografts,after 6 wk of treatment with Ketoconazole (50 mg/kg/three times per week)plus Nocodazole (5 mg/kg/three times per week), the antitumor effects of ND were significantly potentiated by KT. The tumor volume and tumor weight of the mice are significantly reduced as compared with those treated with Ketoconazole or Nocodazole alone. Nocodazole treatment in combination with Ketoconazole strongly enhanced apoptosis of COLO 205 tumor xenografts treated with Ketoconazole or Nocodazole alone [5].

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