GlpBio

MK-8745

目录号: GC10442纯度: >99.00%
An Aurora A kinase inhibitor
MK-8745
Cas No.: 885325-71-3
规格价格库存数量操作
5mg¥279.00现货
1
10mg¥450.00现货
1
50mg¥1,350.00现货
1
10mM (in 1mL DMSO)¥307.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

MK-8745 is a novel and selective inhibitor of Aurora A with IC50 value of 0.6 nM [1].

Aurora A kinase is a member of mitotic serine/threonine kinases and plays an important role in cellular division by controlling chromatid segregation. It has been reported that abnormal expression of Aurora A is correlated with the high occurrence of cancer and its expression determines cell sensitivity to MK-8745 treatment [1].

MK-8745 is a potent Aurora A inhibitor. When tested with p53-/+ cell lines, MK-8745 treatment induced apoptotic cell death in a p53-dependent manner through inhibiting Aurora A activity [1]. In non-Hodgkin lymphoma (NHL) cell lines, MK-8745 treatment arrested cell cycle in G2/M phase and induced cell death via inhibiting Aurora A kinase [2]. In HCT 116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cell lines, MK-8745 treatment induced cell apoptosis with the percent of 25%, 22%, 25%, and 22%, respectively [3].

In female athymic nude mice model subcutaneous xenografted with HCT116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cells, administration of MK-8745 significantly inhibited tumor growth [3].

References:
[1].  Nair, J.S., A.L. Ho, and G.K. Schwartz, The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. Cell Cycle, 2012. 11(4): p. 807-17.
[2].  Chowdhury, A., S. Chowdhury, and M.Y. Tsai, A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012. 53(3): p. 462-71.
[3].   Shionome, Y., et al., Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One, 2013. 8(1): p. e55457.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Human non-Hodgkin lymphoma cell lines(NHL cell lines)

Preparation method

The solubility of this compound in DMSO is >21.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1μM for 24 h and 48 h

Applications

In NHL cell lines, MK-8745 treatment for 48 h significantly decreased the cell number in TPX2 (targeting protein for Xenopus kinaselike protein 2) knockdown in cells in comparison to control cells. MK-8745 treatment induced an approximately 160-fold increase in cell death by 96 h and led to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in NHL cell lines.
Animal experiment [2]:

Animal models

Female athymic mice at the age of 4 to 5 weeks (HCT116 isogenic cells were transplanted into both flanks of mice)

Dosage form

s.c, 800 nM for 7 to 12 days.

Application

Xenograft experiments indicated that MK-8745 showed anti-tumor activity, however, it did not regress tumors completely, and drug-resistant tumors still remained in mice. Tumor growth of HCT116 Puma(-), HCT116 p21(-), HCT116 Bax(-) and HCT116 Chk2(-) cells was significantly inhibited with MK-8745 in female athymic mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

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

[2]. Shionome, Y., et al. Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One, 2013. 8(1): p. e55457.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
885325-71-3
化学名
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone
SMILES
ClC1=C(F)C(C(N2CCN(CC3=NC(NC4=NC=CS4)=CC=C3)CC2)=O)=CC=C1
分子式
C20H19ClFN5OS
分子量
431.91 g/mol
溶解性
≥ 21.6mg/mL in DMSO
保存条件
Store at -20° C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol