產品描述: | MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM. |
靶點: |
Aurora A:4 nM (IC50);CaseinKinase;?PKA;?Src;?AuroraKinase |
體內研究: |
In the HCT-116 tumor-bearing mice, MLN8054 treatment inhibits tumor growth dose dependently. MLN8054 is generally well tolerated. MLN8054 also inhibits the growth of the PC-3 tumor xenograft in nude mice. MLN8054 Treatment Results in Inhibition of Aurora A, Accumulation of Mitotic Cells, and Apoptosis in vivo. MLN8054 selectively inhibits Aurora A kinase activity when dosed at 30 mg/kg. At this dose in HCT116 tumor tissue, MLN8054 has been shown to inhibit Aurora A autophosphorylation, and induce an increase in the Aurora B substrate, pHisH3 |
參考文獻: |
1. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. 2. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84. |
溶解性: |
DMSO : 20.83 mg/mL (43.68 mM; ultrasonic and warming and heat to 60°C) |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.097 ml |
10.485 ml |
20.971 ml |
5 mM |
0.419 ml |
2.097 ml |
4.194 ml |
10 mM |
0.21 ml |
1.049 ml |
2.097 ml |
50 mM |
0.042 ml |
0.21 ml |
0.419 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |