Aurora A Inhibitor I
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 3.4 nM。
Aurora A Inhibitor I是一种新型的、强效的和选择性的Aurora A抑制剂。
据报道,Aurora激酶是有丝分裂必需的,用于完成细胞分裂。因此,Aurora激酶抑制剂作为潜在的抗癌治疗剂已被广泛研究。两种主要Aurora激酶(Aurora A和Aurora B)的激酶结构域序列密切相关(71%一致)。
体外:检测Aurora A Inhibitor I对野生型激酶和两种突变体(Aurora A(T217E)和Aurora B(E161T))的作用。Aurora A Inhibitor I的抑制能力受单一氨基酸取代强烈影响。对于任一Aurora激酶,苏氨酸的存在使得抑制作用增强,而对于谷氨酸变体,IC50值改变大约100倍,支持了该残基的“门控”作用。Aurora B结合口袋被E161T突变增大,而Aurora A口袋被T217E突变关闭。Aurora A Inhibitor I是特异的选择性Aurora A抑制剂,在细胞试验中对Aurora B或CDKs未观察到抑制作用[1]。
体内:目前尚未收到动物体内研究的报道。
临床试验:N/A。
参考文献:
[1] Aliagas-Martin I,Burdick D,Corson L,Dotson J,Drummond J,Fields C,Huang OW,Hunsaker T,Kleinheinz T,Krueger E,Liang J,μMoffat 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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 588.07 |
Cas No. | 1158838-45-9 |
Formula | C31H31ClFN7O2 |
Solubility | ≥29.4 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]anilino]-5-fluoropyrimidin-4-yl]amino]benzamide |
SDF | Download SDF |
Canonical SMILES | CCN1CCN(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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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