ZM-447439 | Aurora A/B Inhibitor | AmBeed-信号通路专用抑制剂

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ZM-447439 99%+

货号：A107524

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM, 130 nM respectively, > 8 fold selectivity than Aurora C, MEK1, Src.

ZM-447439 化学结构
CAS号：331771-20-1

ZM-447439 3D分子结构
CAS号：331771-20-1

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ZM-447439 纯度/质量文件产品仅供科研

货号：A107524 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

Aurora Kinase 亚型比较

产品名称	Aurora A ↓ ↑	Aurora B ↓ ↑	Aurora C ↓ ↑	其他靶点	纯度
BI-847325	++ Aurora A (Human), IC50: 25 nM	++++ Aurora B (Xenopus laevis), IC50: 3 nM	++ Aurora C (Human), IC50: 15 nM		99%+
CCT 137690	++ Aurora A, IC50: 15 nM	++ Aurora B, IC50: 25 nM	++ Aurora C, IC50: 19 nM		99%+
MK-5108	++++ Aurora A, IC50: 0.064 nM				99%+
KW-2449	+ Aurora A, IC50: 48 nM			FLT3	99%+
Tozasertib	++++ Aurora A, Ki app: 0.6 nM	++ Aurora B, Ki app: 18 nM	+++ Aurora C, Ki app: 4.6 nM	FLT3,Bcr-Abl	99%+
AT9283	++++ Aurora A, IC50: ~3.0 nM	++++ Aurora B, IC50: ~3.0 nM			99%+
MLN8054	+++ Aurora A, IC50: 4 nM	+ Aurora B, IC50: 172 nM			99%+
ZM-447439	+ Aurora A, IC50: 110 nM	+ Aurora B, IC50: 130 nM		Src	99%+
TCS7010	++++ Aurora A, IC50: 3.4 nM				99%+
TAK-901	++ Aurora A-TPX2, IC50: 21 nM	++ Aurora B-INCENP, IC50: 15 nM			99%+
Danusertib	+++ Aurora A, IC50: 13 nM	+ Aurora B, IC50: 79 nM	+ Aurora C, IC50: 61 nM	RET	99%+
MK-8745	++++ Aurora A, IC50: 0.6 nM				99+%
PHA-680632	++ Aurora A, IC50: 27 nM	+ Aurora B, IC50: 135 nM	+ Aurora C, IC50: 120 nM	FLT3	99%+
AMG 900	+++ Aurora A, IC50: 5 nM	+++ Aurora B, IC50: 4 nM	++++ Aurora C, IC50: 1 nM		99%+
Alisertib	++++ Aurora A, IC50: 1.2 nM				99%+
ENMD-2076	+++ Aurora A, IC50: 14 nM	+ Aurora B, IC50: 350 nM		RET,FLT3	98%
JNJ-7706621	+++ Aurora A, IC50: 11 nM	++ Aurora B, IC50: 15 nM			99%+
CYC-116	+++ Aurora A, Ki: 8 nM	+++ Aurora B, Ki: 9 nM		FLT3	99%+
Reversine	+++ Aurora A, IC50: 12 nM	+++ Aurora B, IC50: 13 nM	++ Aurora C, IC50: 20 nM		98%
CCT129202	++ Aurora A, IC50: 42 nM	+ Aurora B, IC50: 198 nM	+ Aurora C, IC50: 227 nM		98%
SNS-314 mesylate	+++ Aurora A, IC50: 9 nM	++ Aurora B, IC50: 31 nM	++++ Aurora C, IC50: 3 nM		99%+
Barasertib-HQPA		++++ Aurora B, IC50: 0.37 nM			99%+
Hesperadin		+ Aurora B (human), IC50: 250 nM			98%
GSK-1070916		++++ Aurora B-INCENP, IC50: 3.5 nM	+++ Aurora C-INCENP, IC50: 6.5 nM	SIK,Tie-2	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ZM-447439 生物活性

靶点

Aurora A

Aurora A, IC50:110 nM
Aurora B

Aurora B, IC50:130 nM

描述

Cells treated with ZM-447439 enter interphase, proceed normally into mitosis, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and the mitotic phosphorylation of histone H3. It prevents chromosome alignment and separation, impairs spindle checkpoint function, and inhibits the kinetochore localization of BubR1, Mad2, and Cenp-E^[1]. The inhibition of Aurora kinases by ZM-447439 reduces the phosphorylation of Ser10 on histone H3 in Hep2 cancer cells. Cells treated with ZM-447439 that are arrested in G2/M phase induce multipolar spindles and accumulate 4N/8N DNA, similar to cells with genetic suppression of Aurora-B. Treatment with ZM-447439 can induce apoptosis. The inhibition of Aurora kinases by ZM-447439 is closely associated with a reduction in the phosphorylation of Akt Ser473 and its substrates GSK3α/β Ser21 and Ser9^[2].

ZM-447439 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A172 cell		Growth inhibition assay		Inhibition of human A172 cell growth in a cell viability assay, IC50=0.98411 μM	SANGER
human A498 cell		Growth inhibition assay		Inhibition of human A498 cell growth in a cell viability assay, IC50=2.3669 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 BE-13 cell		Growth inhibition assay		Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.84418 μM	SANGER

ZM-447439 动物研究

Dose	Mice: 80 mg/kg^[3] (i.p.)
Administration	i.p.

ZM-447439 参考文献

[1]Ditchfield C, et al. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol. 2003 Apr 28;161(2):267-80.

[2]Long ZJ, et al. ZM 447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensionalculture. Cell Cycle. 2008 May 15;7(10):1473-9.

ZM-447439 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL

ZM-447439 技术信息

CAS号	331771-20-1
分子式	C₂₉H₃₁N₅O₄
分子量	513.588

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(48.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

human A172 cell	Growth inhibition assay		Inhibition of human A172 cell growth in a cell viability assay, IC50=0.98411 μM	SANGER
human A498 cell	Growth inhibition assay		Inhibition of human A498 cell growth in a cell viability assay, IC50=2.3669 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 BE-13 cell	Growth inhibition assay		Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.84418 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 COLO-800 cell	Growth inhibition assay		Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=1.70382 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 DOHH-2 cell	Growth inhibition assay		Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=1.40276 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 EM-2 cell	Growth inhibition assay		Inhibition of human EM-2 cell growth in a cell viability assay, IC50=1.41721 μM	SANGER
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 ES3 cell	Growth inhibition assay		Inhibition of human ES3 cell growth in a cell viability assay, IC50=0.4732 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 ES8 cell	Growth inhibition assay		Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.49806 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 H9 cell	Growth inhibition assay		Inhibition of human H9 cell growth in a cell viability assay, IC50=0.92979 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
human HN cell	Growth inhibition assay		Inhibition of human HN cell growth in a cell viability assay, IC50=1.9251 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 KARPAS-45 cell	Growth inhibition assay		Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.38128 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 L-363 cell	Growth inhibition assay		Inhibition of human L-363 cell growth in a cell viability assay, IC50=1.9512 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 LK-2 cell	Growth inhibition assay		Inhibition of human LK-2 cell growth in a cell viability assay, IC50=1.64594 μM	SANGER
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
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 MOLT-16 cell	Growth inhibition assay		Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=0.60961 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 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 NB14 cell	Growth inhibition assay		Inhibition of human NB14 cell growth in a cell viability assay, IC50=1.55621 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 NBsusSR cell	Growth inhibition assay		Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=0.91387 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 NCI-H209 cell	Growth inhibition assay		Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=1.16602 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 NCI-H747 cell	Growth inhibition assay		Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=2.03353 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 NOMO-1 cell	Growth inhibition assay		Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=1.36725 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 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 RKO cell	Growth inhibition assay		Inhibition of human RKO cell growth in a cell viability assay, IC50=0.70656 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 SBC-1 cell	Growth inhibition assay		Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=1.03928 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 SW48 cell	Growth inhibition assay		Inhibition of human SW48 cell growth in a cell viability assay, IC50=1.23155 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 TE-11 cell	Growth inhibition assay		Inhibition of human TE-11 cell growth in a cell viability assay, IC50=0.53703 μM	SANGER
MCF7 cell	Proliferation assay		Antiproliferative activity against MCF7 cell line, IC50=0.198 μM	16337122
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

ZM-447439 99%+

ZM-447439 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

ZM-447439 质控信息

ZM-447439 生物活性

ZM-447439 细胞研究

ZM-447439 动物研究

ZM-447439 参考文献

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ZM-447439 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

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ZM-447439 生物活性

ZM-447439 细胞研究

ZM-447439 动物研究

ZM-447439 参考文献

ZM-447439 实验方案

ZM-447439 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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