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GSK-1070916

产品编号 T6129 CAS 942918-07-2

别名: GSK-1070916A, GSK1070916

GSK-1070916 (GSK-1070916A) 是一种选择性，ATP 竞争型的极光激酶B/C 抑制剂，Ki 值分别为0.38和1.5 nM。

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GSK-1070916, CAS 942918-07-2

规格	价格/CNY	货期
1 mg	￥ 366	现货
5 mg	￥ 822	现货
10 mg	￥ 1,330	现货
25 mg	￥ 1,970	现货
50 mg	￥ 2,790	现货
100 mg	￥ 4,130	现货
1 mL * 10 mM (in DMSO)	￥ 918	现货

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选择批次

纯度: 98.51%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
靶点活性	Aurora C-INCENP:6.5 nM, Aurora B-INCENP:3.5 nM
体外活性	GSK1070916 selectively inhibits Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM over Aurora A with Ki of 490 nM. Inhibition of Aurora B and Aurora C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively. In addition, GSK1070916 is also a competitive inhibitor with respect to ATP. [1] Human tumor cells treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B. Moreover, GSK1070916 inhibits the proliferation of tumor cells with EC50 values of <10 nM in over 100 cell lines spanning a broad range of tumor types, with a median EC50 of 8 nM. Although GSK1070916 has potent activity against proliferating cells, a dramatic shift in potency is observed in primary, nondividing, normal human vein endothelial cells. Furthermore, GSK1070916-treated cells do not arrest in mitosis but instead fails to divide and become polyploid, ultimately leading to apoptosis. [2] In another study, it is also reported high chromosome number associated with resistance to the inhibition of Aurora B and C suggests cells with a mechanism to bypass the high ploidy checkpoint are resistant to GSK1070916. [3]
体内活性	GSK1070916 (25, 50, or 100 mg/kg) shows dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. [2]
激酶实验	Kinase Assay: The ability of GSK1070916 to inhibit the Aurora enzymes is measured using in vivo kinase assays. The assays measure the ability of Aurora A, Aurora B and Aurora C to phosphorylate a synthetic peptide substrate. Biotin-Ahx-RARRRLSFFFFAKKK-NH2 is used for the Aurora A–TPX2 LEADseekerTM assay and 5FAM-PKAtide is used for the IMAPTM assay for all three Aurora kinases. To take into account time-dependent inhibition of Aurora enzymes, Aurora A–TPX2, Aurora B–INCENP and Aurora C–INCENP are incubated with GSK1070916 at various concentrations for 30 min before the reactions are initiated with the addition of substrates. For the Aurora A LEADseekerTM assay, final assay conditions are 0.5 nM Aurora A–TPX2, 1 μM peptide substrate, 6 mM MgCl2, 1.5 μM ATP, 0.003 μCi/μL [γ-33P] ATP in 50 mM Hepes, pH 7.2, 0.15 mg/mL BSA, 0.01% Tween-20, 5 mM DTT and 25 mM KCl. The reactions are incubated at room temperature (25 °C) for 120 min and terminated by the addition of LEADseekerTM beads in PBS containing EDTA (final concentration 2 mg/mL beads and 25 mM EDTA). The plates are then sealed, and the beads are allowed to settle overnight. Product formation is quantified using a Viewlux Imager. For the IMAPTM assays, Aurora A–TPX2 (final concentration 1 nM), Aurora B–INCENP (final concentration 2 nM) or Aurora C–INCENP (final concentration 2.5 nM) is added to the compound-containing plates in 5 μL of buffer (25 mM Hepes, pH 7.2, for Aurora A, 25 mM Hepes, pH 7.5, for Aurora B and 20 mM Hepes, pH 7.2, for Aurora C) containing 0.15 mg/mL BSA, 0.01% Tween 20 and 25 mM NaCl. This mixture is incubated at room temperature for 30 min. To start the reaction, 5 μL of a substrate solution is added containing the same Hepes buffer as used for the pre-incubation, 25 mM NaCl, MgCl2 (2, 4 and 4 mM for Aurora A, B and C respectively), DTT (4, 4 and 2 mM for Aurora A, B and C respectively), ATP (4, 4 and 10 μM for Aurora A, B and C respectively), 200 nM 5FAM-PKAtide, 0.01% Tween 20 and 0.15 mg/mL BSA. The reactions are incubated at room temperature for 120 min for Aurora A and B and 60 min for Aurora C. These reactions are then terminated by the addition of 10 μL of 1:500 (1:600 for Aurora C) Progressive Binding Reagent in 95% Progressive Binding Buffer A and 5% Progressive Binding Buffer B. Plates are incubated at room temperature for approx. 90–120 min (time allowed for equilibrium to be reached). Plates are read in a Molecular Devices Analyst plate reader in fluorescence polarization mode.
细胞实验	Cells are plated in 96-well plates in the recommended growth media and incubated at 37 °C in 5% CO2 overnight. The following day, the cells are treated with serial dilutions of GSK1070916. At this time, one set of cells is treated with CellTiter-Glo for a time equal to 0 (T = 0) measurement. Following a 6- to 7-d incubation with compound, cell proliferation is measured using the CellTiter-Glo reagent according to the manufacture's recommended protocol. As inhibition of Aurora B induces endomitosis, the degree of which differs depending on the cell type, an extended compound treatment time is required to accurately reflect the effects on cell viability across a large panel of cell lines. For analysis of cell viability, values from wells with no cells are subtracted for background correction and the data plotted as a percent of the DMSO-treated control samples using Microsoft Excel XLfit4 software. The EC50 values represent the concentration of GSK1070916 where 50% maximal effect is observed(Only for Reference)

别名	GSK-1070916A, GSK1070916
分子量	507.63
分子式	C30H33N7O
CAS No.	942918-07-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 102 mg/mL (200.93 mM)

Ethanol: 8 mg/mL(15.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.9699 mL	9.8497 mL	19.6994 mL	49.2485 mL
	5 mM	0.394 mL	1.9699 mL	3.9399 mL	9.8497 mL
	10 mM	0.197 mL	0.985 mL	1.9699 mL	4.9248 mL
DMSO	20 mM	0.0985 mL	0.4925 mL	0.985 mL	2.4624 mL
	50 mM	0.0394 mL	0.197 mL	0.394 mL	0.985 mL
	100 mM	0.0197 mL	0.0985 mL	0.197 mL	0.4925 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Anderson K, et al. Biochem J, 2009, 420(2), 259-265. 2. Hardwicke MA, et al. Mol Cancer Ther, 2009, 8(7),1808-1817. 3. Moy C, et al. J Transl Med, 2011, 9, 110.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GSK-1070916 942918-07-2 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Tie-2 FLT AMPK Aurora Kinase GSK-1070916A Inhibitor GSK1070916 inhibit GSK 1070916 inhibitor

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GSK-1070916

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords