MK-8745 is an aurora A kinase inhibitor with an IC₅₀ of 0.6 nM.

MK-8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK-8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression^[1]. 1 μM of MK-8745 exposure for 24 h induces cell cycle arrest in all NHL cells, with variable degrees of G2/M arrest. Z138C cells are highly sensitive to MK-8745 (1 μ M) treatment and induces an approximate 5.5-fold increase in the G2/M phase cell population by 96 h. MK-8745 treatment inhibits phosphorylation of Aurora-A in Granta 519 and Z138C cells, while Akata and JVM2 has no effect. MK-8745 specifically inhibits Aurora-A specific function. MK-8745 treatment leads to apoptotic cell death^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

431.91

C₂₀H₁₉ClFN₅OS

885325-71-3

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 100 mg/mL (231.53 mM)

* “≥” means soluble, but saturation unknown.

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent.

  [2]. Aparajita Chowdhury et al. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012 Mar, 53(3):462-71.

A total of 10000 cells are plated per well in a 96-well plate and treated with MK-8745 for varying time points starting 24 h after plating. Cell viability is measured by the MTT assay^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent.

  [2]. Aparajita Chowdhury et al. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012 Mar, 53(3):462-71.