Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC₅₀s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.

Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Reversine is a potent inhibitor of Aurora A and B and is also an inhibitor of Aurora C kinase. Aurora A and B activities are inhibited by 80% and Aurora kinase C by 55%, already at a concentration of 0.5 μM, whereas no inhibition or only modest inhibition is observed on others kinases tested. In a second round of experiments, the IC₅₀ of Reversine is determined on Aurora kinase A to be 400 nM, whereas Aurora kinase B and C IC₅₀ are 500 and 400 nM, respectively. The IC₅₀ is also determined on MEK1 is >1.5 μM and that the IC₅₀ on muscle myosin (an analogue of nonmuscle myosin II) is 350 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

The combination of Reversine and aspirin can more efficiently induce cell cycle arrest and apoptosis. To evaluate the anti-tumor effect of this combination, a xenograft nude mouse model is established by s.c. injection. Mice inoculated with cervical cancer cells have lost about 10 % of their initial body weight by about 16 days after tumor inoculation. However, tumor growth (tumor weight) is reduced and the mice survive longer in the combination group.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

The combination of Reversine and aspirin can more efficiently induce cell cycle arrest and apoptosis. To evaluate the anti-tumor effect of this combination, a xenograft nude mouse model is established by s.c. injection. Mice inoculated with cervical cancer cells have lost about 10 % of their initial body weight by about 16 days after tumor inoculation. However, tumor growth (tumor weight) is reduced and the mice survive longer in the combination group.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . D'Alise AM, et al. Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Mol Cancer Ther. 2008 May;7(5):1140-9.  [Content Brief]

  . Qin HX, et al. Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology. 2013 Aug;65(4):643-53.  [Content Brief]