Reversine, a synthetic purine analogue(2,6-disubstituted purine), is a potent human A3adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively.
Reversine, an innovative inhibitor of Aurora kinases, prevents colony formation in human acute myeloid leukemia cells. It strongly inhibits Aurora kinases A and B and moderately inhibits Aurora kinase C at a concentration of 0.5 μM. In further testing, Reversine shows an IC50 of 400 nM for Aurora kinase A, 500 nM for B, and 400 nM for C, while showing limited inhibition on other tested kinases. Additionally, the IC50 for MEK1 is >1.5 μM and for muscle myosin is 350 nM[1].
体内研究
The Reversine and Aspirin combination effectively triggers cell cycle arrest and apoptosis. To assess its anti-tumor efficacy, we established a xenograft nude mouse model via subcutaneous injection. Around 16 days post-tumor inoculation, mice implanted with cervical cancer cells experienced a roughly 10% reduction in initial body weight. Nonetheless, tumor growth (tumor weight) was notably diminished, and the survival rate extended in the combination treatment group[2].
体外研究
Reversine, an innovative inhibitor of Aurora kinases, prevents colony formation in human acute myeloid leukemia cells. It strongly inhibits Aurora kinases A and B and moderately inhibits Aurora kinase C at a concentration of 0.5 μM. In further testing, Reversine shows an IC50 of 400 nM for Aurora kinase A, 500 nM for B, and 400 nM for C, while showing limited inhibition on other tested kinases. Additionally, the IC50 for MEK1 is >1.5 μM and for muscle myosin is 350 nM[1].
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