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ZM 447439
ZM 447439是一種選擇性的，ATP競爭性Aurora A和Aurora B抑制劑，IC50分別為110 nM和130 nM，作用于Aurora A/B比作用于MEK1， Src， Lck選擇性高8倍，對CDK1/2/4， Plk1， Chk1等幾乎沒有作用效果。
ZM 447439 Chemical Structure
CAS: 331771-20-1
產(chǎn)品質(zhì)控
批次：
純度：
99.26%
99.26
ZM 447439相關(guān)產(chǎn)品
| 相關(guān)靶點 | Aurora A Aurora B Aurora C Aurora B | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Alisertib (MLN8237) Barasertib (AZD1152-HQPA) Tozasertib (VX-680) MLN8054 Hesperadin Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632 SNS-314 CCT137690 GSK1070916 CYC116 TAK-901 CCT129202 SNS-314 Mesylate LY3295668 SP-96 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復(fù)化合物庫 細胞周期化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | ZM 447439是一種選擇性的，ATP競爭性Aurora A和Aurora B抑制劑，IC50分別為110 nM和130 nM，作用于Aurora A/B比作用于MEK1， Src， Lck選擇性高8倍，對CDK1/2/4， Plk1， Chk1等幾乎沒有作用效果。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | ZM-447439是Aurora選擇性ATP競爭性抑制劑 | ||||||||||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 體外, ZM-447439 選擇性抑制重組人類Aurora A和B,IC50分別為110和130 nM,而抑制其他不同結(jié)構(gòu)類型蛋白激酶，包括有絲分裂激酶CDK1和PLK1時，IC50>10 μM。 [1] Aurora 激酶抑制劑, ZM-447439 抑制BON, QGP-1和MIP-101三種細胞系生長，連續(xù)處理72小時，IC50分別為3 μM , 0.9 μM 和3 μM，這種作用存在時間和劑量依賴性。此外, ZM-447439通過促進DNA分裂和 caspase 3 和7激活,有效誘導(dǎo)細胞凋亡，且使GEP-NET細胞在G0/G1期和G2/M期停頓。[2] 在小鼠胚胎中, ZM-447439 抑制Aurora 激酶,通過在每個胚胎周期使用不同干擾，調(diào)節(jié)G2到中期的組蛋白H3 serine 10 (H3S10Ph)而使前兩次分裂發(fā)生異常。[3] 最新研究顯示ZM-447439作用于宮頸癌SiHa細胞，抑制生長和凋亡，且增強化學敏感性。[4] |
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|---|---|---|---|---|
| 激酶實驗 | 體外激酶實驗 | |||
| 使用桿狀病毒表達體系，表達重組Aurora A和B作為氨基末端His6標記融合蛋白。使用Ni-NTA瓊脂糖，通過親和層析純化Aurora A，使用CM Sepharose Fast Flow，通過離子交換層析純化Aurora B。1 ng 純化的重組酶加到反應(yīng)中，反應(yīng)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), 然后在室溫下溫育60分鐘。加入20% 磷酸反應(yīng)終止，使用P30硝化纖維過濾器獲得產(chǎn)物， 使用Beta 板TM計數(shù)器測定33P攝入率。 | ||||
| 細胞實驗 | 細胞系 | BON, QGP-1和MIP-101 | ||
| 濃度 | 0到5 μM | |||
| 孵育時間 | 72小時 | |||
| 方法 | 通過結(jié)晶紫染色測評細胞數(shù)。細胞接種在96孔板上，與1% 戊二醇混合。細胞用0.1% 結(jié)晶紫染色。用水沖洗未結(jié)合的染料。用0.2% Triton X-100溶解結(jié)合的結(jié)晶紫。使用ELISA讀數(shù)器在570 nm處分析線性增加的細胞數(shù)。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p53 / p21 / p-p38 / p38 pHistone H3 / CEM BubR1 / MAD2 / Cyclin B1 |
|
23759594 | |
| Immunofluorescence | p21 p53 Aurora B / Survivin |
|
23759594 | |
化學信息&溶解度
| 分子量 | 513.59 | 分子式 | C29H31N5O4 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 103 mg/mL ( (200.54 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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