1158838-45-9Aurora A Inhibitor I

产品属性：

Cas No.1158838-45-9

别名 化学名 N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]anilino]-5-fluoropyrimidin-4-yl]amino]benzamide

化学名

分子式 C31H31ClFN7O2

分子量 588.07

溶解度 ≥ 29.4 mg/mL in DMSO

储存条件 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.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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.