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Aurora A Inhibitor I
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aurora A Inhibitor I图片
CAS NO:1158838-45-9
规格:98%
分子量:588.07
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Aurora A inhibitor
CAS:1158838-45-9
分子式:C31H31ClFN7O2
分子量:588.07
纯度:98%
存储:Store at -20°C

Background:

IC50: 3.4 nM.


Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A .


Aurora kinases are reported to be required for mitosis and to complete cell division. Because of this, Aurora kinase inhibitors have been investigated extensively as potential anticancer therapeutic agents. The two major Aurora kinases (Aurora A and Aurora B) are closely related in kinase domain sequence (71% identical).


In vitro: Aurora A Inhibitor I was tested against wild-type kinase and two mutants (Aurora A (T217E) and Aurora B (E161T)). The inhibitory potencies of Aurora A Inhibitor I was strongly affected by the single amino acid substitutions. For either Aurora kinase, the presence of threonine allowed potent inhibition, while for glutamic acid variants, there was a approximately 100-fold shift in IC50, which supported the “gating” role for this residue. The Aurora B binding pocket was enlarged by the E161T mutation, while the pocket in Aurora A was closed by the T217E mutation. Aurora A Inhibitor I was exceptionally selective Aurora A inhibitors, as shown by no inhibition on Aurora B or CDKs was observed in cellular assays [1].


In vivo: So far, there is no animal in vivo study reported.


Clinical trial: N/A


Reference:
[1] Aliagas-Martin I,Burdick D,Corson L,Dotson J,Drummond J,Fields C,Huang OW,Hunsaker T,Kleinheinz T,Krueger E,Liang J,Moffat J,Phillips G,Pulk R,Rawson TE,Ultsch M,Walker L,Wiesmann C,Zhang B,Zhu BY,Cochran AG.  A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J Med Chem.2009 May 28;52(10):3300-7.