|orally available and highly specific CDK4/6 inhibitor|
Sample solution is provided at 25 µL, 10mM.
|Description||LEE011 is an orally available and highly specific inhibitor of CDK4/6.|
|Cas No.||1211441-98-3||SDF||Download SDF|
|Solubility||Limited solubility||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
LEE011 (NVP-LEE011) is a highly specific inhibitor of CDK4/CDK6 and functions via decreasing in phosphorylated RB and FOXM1 . When tested with 17 human neuroblastoma cell lines, 12 of them were sensitive to LEE011 treatment with mean IC50=306±68 nM .
CDK4/6 could increase G1-S phase cell cycle progression and ultimately cellular proliferation via phosphorylating tumor suppressor protein RB. CDK4/6 signaling also could senescence suppression by regulating FOXM1 transcription. Numerous studies have shown that over-expression of CDK4/CDK6 correlated with tumorigenesis and disease progression .
LEE011 is a novel inhibitor for CDK4/CDK6. When subjected to human liposarcoma cell lines, treated with LEE011 could dramatically decrease cell growth via arresting cell cycle G0-G1 . In 12 of 17 human neuroblastoma-derived cell lines, treatment with LEE011 could significantly reduce cell proliferation .
In a mouse model with human liposarcoma xerography, continued treating the mouse with LEE011 orally could inhibit tumor growth or induce regression without detrimental effects on mouse weight . In mice xerography with neuroblastoma cells, treated with LEE011 could inhibit the tumor growth .
1.Zhang, Y.X., et al., Antiproliferative effects of CDK4/6 inhibition in CDK4-amplified human liposarcoma in vitro and in vivo. Mol Cancer Ther, 2014. 13(9): p. 2184-93.
2.Rader, J., et al., Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res, 2013. 19(22): p. 6173-82.
3.Paternot, S., et al., The CDK4/CDK6 inhibitor PD0332991 paradoxically stabilizes activated cyclin D3-CDK4/6 complexes. Cell Cycle, 2014. 13(18): p. 2879-88.
4.Dickson, M.A., Molecular pathways: CDK4 inhibitors for cancer therapy. Clin Cancer Res, 2014. 20(13): p. 3379-83.