ZM 447439
ZM 447439是一种选择性的，ATP竞争性Aurora A和Aurora B抑制剂，IC50分别为110 nM和130 nM，作用于Aurora A/B比作用于MEK1， Src， Lck选择性高8倍，对CDK1/2/4， Plk1， Chk1等几乎没有作用效果。
ZM 447439 Chemical Structure
CAS: 331771-20-1
产品质控
批次：
纯度：
99.26%
99.26
ZM 447439相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human LoVo cells | Proliferation assay | 72 h | Antiproliferative activity against human LoVo cells after 72 hrs by MTT-based WST8 reagent assay, IC50=1.9 μM | 25270403 | |
| MCF7 cell | Proliferation assay | Antiproliferative activity against MCF7 cell line, IC50=0.198 μM | 16337122 | ||
| human EoL-1-cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.18678 μM | SANGER | ||
| human P12-ICHIKAWA cell | Growth inhibition assay | Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=0.22441 μM | SANGER | ||
| human KARPAS-45 cell | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.38128 μM | SANGER | ||
| human ES3 cell | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50=0.4732 μM | SANGER | ||
| human ES8 cell | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.49806 μM | SANGER | ||
| human TE-11 cell | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50=0.53703 μM | SANGER | ||
| human RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.5544 μM | SANGER | ||
| human MOLT-16 cell | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=0.60961 μM | SANGER | ||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=0.70656 μM | SANGER | ||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.7963 μM | SANGER | ||
| human SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.83635 μM | SANGER | ||
| human BE-13 cell | Growth inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.84418 μM | SANGER | ||
| human MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=0.89978 μM | SANGER | ||
| human NBsusSR cell | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=0.91387 μM | SANGER | ||
| human H9 cell | Growth inhibition assay | Inhibition of human H9 cell growth in a cell viability assay, IC50=0.92979 μM | SANGER | ||
| human A172 cell | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50=0.98411 μM | SANGER | ||
| human ES5 cell | Growth inhibition assay | Inhibition of human ES5 cell growth in a cell viability assay, IC50=1.00248 μM | SANGER | ||
| human SBC-1 cell | Growth inhibition assay | Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=1.03928 μM | SANGER | ||
| human NCI-H209 cell | Growth inhibition assay | Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=1.16602 μM | SANGER | ||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.16798 μM | SANGER | ||
| human NCI-H720 cell | Growth inhibition assay | Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=1.20627 μM | SANGER | ||
| human KE-37 cell | Growth inhibition assay | Inhibition of human KE-37 cell growth in a cell viability assay, IC50=1.21388 μM | SANGER | ||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=1.23155 μM | SANGER | ||
| human IST-SL1 cell | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=1.31727 μM | SANGER | ||
| human SK-NEP-1 cell | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=1.36498 μM | SANGER | ||
| human NOMO-1 cell | Growth inhibition assay | Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=1.36725 μM | SANGER | ||
| human DOHH-2 cell | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=1.40276 μM | SANGER | ||
| human ABC-1 cell | Growth inhibition assay | Inhibition of human ABC-1 cell growth in a cell viability assay, IC50=1.40352 μM | SANGER | ||
| human Ramos-2G6-4C10 cell | Growth inhibition assay | Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=1.40605 μM | SANGER | ||
| human EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50=1.41721 μM | SANGER | ||
| human NB14 cell | Growth inhibition assay | Inhibition of human NB14 cell growth in a cell viability assay, IC50=1.55621 μM | SANGER | ||
| human MOLT-13 cell | Growth inhibition assay | Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=1.56706 μM | SANGER | ||
| human ECC10 cell | Growth inhibition assay | Inhibition of human ECC10 cell growth in a cell viability assay, IC50=1.63353 μM | SANGER | ||
| human LK-2 cell | Growth inhibition assay | Inhibition of human LK-2 cell growth in a cell viability assay, IC50=1.64594 μM | SANGER | ||
| human CTB-1 cell | Growth inhibition assay | Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=1.67082 μM | SANGER | ||
| human NCI-H1581 cell | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=1.6755 μM | SANGER | ||
| human COLO-800 cell | Growth inhibition assay | Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=1.70382 μM | SANGER | ||
| human NB7 cell | Growth inhibition assay | Inhibition of human NB7 cell growth in a cell viability assay, IC50=1.75297 μM | SANGER | ||
| human LAMA-84 cell | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=1.7552 μM | SANGER | ||
| human HCT-116 cells | Growth inhibition assay | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=1.80908 μM | SANGER | ||
| SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=1.8153 μM | SANGER | ||
| human H4 cell | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50=1.81578 μM | SANGER | ||
| human CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=1.83845 μM | SANGER | ||
| human HN cell | Growth inhibition assay | Inhibition of human HN cell growth in a cell viability assay, IC50=1.9251 μM | SANGER | ||
| human L-363 cell | Growth inhibition assay | Inhibition of human L-363 cell growth in a cell viability assay, IC50=1.9512 μM | SANGER | ||
| human NCI-H747 cell | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=2.03353 μM | SANGER | ||
| human A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=2.3669 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | ZM 447439是一种选择性的，ATP竞争性Aurora A和Aurora B抑制剂，IC50分别为110 nM和130 nM，作用于Aurora A/B比作用于MEK1， Src， Lck选择性高8倍，对CDK1/2/4， Plk1， Chk1等几乎没有作用效果。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | ZM-447439是Aurora选择性ATP竞争性抑制剂 | ||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 体外, ZM-447439 选择性抑制重组人类Aurora A和B,IC50分别为110和130 nM,而抑制其他不同结构类型蛋白激酶，包括有丝分裂激酶CDK1和PLK1时，IC50>10 μM。 [1] Aurora 激酶抑制剂, ZM-447439 抑制BON, QGP-1和MIP-101三种细胞系生长，连续处理72小时，IC50分别为3 μM , 0.9 μM 和3 μM，这种作用存在时间和剂量依赖性。此外, ZM-447439通过促进DNA分裂和 caspase 3 和7激活,有效诱导细胞凋亡，且使GEP-NET细胞在G0/G1期和G2/M期停顿。[2] 在小鼠胚胎中, ZM-447439 抑制Aurora 激酶,通过在每个胚胎周期使用不同干扰，调节G2到中期的组蛋白H3 serine 10 (H3S10Ph)而使前两次分裂发生异常。[3] 最新研究显示ZM-447439作用于宫颈癌SiHa细胞，抑制生长和凋亡，且增强化学敏感性。[4] |
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|---|---|---|---|---|
| 激酶实验 | 体外激酶实验 | |||
| 使用杆状病毒表达体系，表达重组Aurora A和B作为氨基末端His6标记融合蛋白。使用Ni-NTA琼脂糖，通过亲和层析纯化Aurora A，使用CM Sepharose Fast Flow，通过离子交换层析纯化Aurora B。1 ng 纯化的重组酶加到反应中，反应中含 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM 肽底物, 10 μM ATP（Aurora A），5 μM ATP（Aurora B）, 和0.2 μCi γ[33P]ATP (比活≥2,500 Ci/mmol), 然后在室温下温育60分钟。加入20% 磷酸反应终止，使用P30硝化纤维过滤器获得产物， 使用Beta 板TM计数器测定33P摄入率。 | ||||
| 细胞实验 | 细胞系 | BON, QGP-1和MIP-101 | ||
| 浓度 | 0到5 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 通过结晶紫染色测评细胞数。细胞接种在96孔板上，与1% 戊二醇混合。细胞用0.1% 结晶紫染色。用水冲洗未结合的染料。用0.2% Triton X-100溶解结合的结晶紫。使用ELISA读数器在570 nm处分析线性增加的细胞数。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p53 / p21 / p-p38 / p38 pHistone H3 / CEM BubR1 / MAD2 / Cyclin B1 |
|
23759594 | |
| Immunofluorescence | p21 p53 Aurora B / Survivin |
|
23759594 | |
化学信息&溶解度
| 分子量 | 513.59 | 分子式 | C29H31N5O4 |
| CAS号 | 331771-20-1 | SDF | Download ZM 447439 SDF |
| Smiles | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)NC(=O)C4=CC=CC=C4)OCCCN5CCOCC5 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 103 mg/mL ( (200.54 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
mg/kg
g
μL
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Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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 ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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。
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