Aurora A Inhibitor I
目录号 : GC13332
A potent and selective inhibitor of Aurora A kinase
Cas No.:1158838-45-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1158838-45-9 | SDF | |
| 化学名 | N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]anilino]-5-fluoropyrimidin-4-yl]amino]benzamide | ||
| 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 | ||
| 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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7005 mL | 8.5024 mL | 17.0048 mL |
| 5 mM | 0.3401 mL | 1.7005 mL | 3.401 mL |
| 10 mM | 0.17 mL | 0.8502 mL | 1.7005 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet