产品说明书

MK-5108

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Chemical Structure| 1010085-13-8 同义名 : VX-689
CAS号 : 1010085-13-8
货号 : A108356
分子式 : C22H21ClFN3O3S
纯度 : 99%+
分子量 : 461.937
MDL号 : MFCD22124479
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(25.98 mM)，配合低频超声，并水浴加热至45℃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：

IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 26 mg/mL suspension

生物活性
靶点

  • Aurora A

    Aurora A, IC50:0.064 nM
描述 Aurora-A kinase is a one of the key regulators during mitosis progression, whose overexpression is frequently observed in some human cancers, and results in aberrant mitosis leading to chromosomal instability and possibly tumorigenesis. MK-5108 specifically inhibited Aurora-A activity with an IC50 value of 0.064 nM in an ATP-competitive manner. In synchronized HeLa-S3 cells, accumulation of pHH3-positive cells was observed by treatment with MK-5108 at concentrations between 300 nM and 10 μM, suggesting the selective inhibition of Aurora-A. DNA profiles of asynchronously cultured HeLa-S3 cells treated by MK-5108 for 24 h were evaluated by flow cytometry. Consistent with the induction of pHH3-positive cells, MK-5108 induced accumulation of cells in the G2-M phase. After oral administration of MK-5108 at 16 mg/kg with a HeLa-luc xenograft rat model, MK-5108 treatment resulted in the induction of pHH3 in tumor and skin tissues, which started at 2 hours and reached a maximum at 4 hours. Treatments with oral MK-5108 twice daily for 12 days at 15 and 30 mg/kg resulted in significant tumor growth inhibition in SCID mice bearing HCT116 tumors[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.82mL

2.16mL

1.08mL

21.65mL

4.33mL

2.16mL
参考文献

[1]Shan W, Akinfenwa PY, et al. A small-molecule inhibitor targeting the mitotic spindle checkpoint impairs the growth of uterine leiomyosarcoma. Clin Cancer Res. 2012 Jun 15;18(12):3352-65.

[2]Shimomura T, Hasako S, et al. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther. 2010 Jan;9(1):157-66.

[3]Shimomura T, Hasako S, Nakatsuru Y, Mita T, Ichikawa K, Kodera T, Sakai T, Nambu T, Miyamoto M, Takahashi I, Miki S, Kawanishi N, Ohkubo M, Kotani H, Iwasawa Y. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther. 2010 Jan;9(1):157-66. doi: 10.1158/1535-7163.MCT-09-0609. Epub 2010 Jan 6. PMID: 20053775.