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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
Aurora A Inhibitor I 是一种有效且高度选择性的 Aurora A 抑制剂,IC50 为 3.4 nM。
Cas No.1158838-45-9
化学名N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]anilino]-5-fluoropyrimidin-4-yl]amino]benzamide
Canonical SMILESCCN1CCN(CC1)C(=O)CC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=C(C=C4)C(=O)NC5=CC=CC=C5Cl)F
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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.