产品说明书

MPI-0479605

Print
Chemical Structure| 1246529-32-7 同义名 : -
CAS号 : 1246529-32-7
货号 : A519540
分子式 : C22H29N7O
纯度 : 99%+
分子量 : 407.512
MDL号 : MFCD28099811
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 10 mg/mL(24.54 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：
生物活性
靶点

  • Kinesin

    Mps1, IC50:1.8 nM
描述 MPI-0479605 is a potent and selective Mps1 inhibitor with IC50 value of 1.8nM. MPI-0479605 triggered the time-dependent degradation of both cyclin B and securin, which normally allow for mitotic exit, as well as a decrease in BubR1 phosphorylation in nocodazole-arrested cells, which led cells exiting mitosis and failure to undergo cytokinesis. MPI-0479605 at concentration>1.67μM blocked apparent autophosphorylation of Mps1 at threonine 676 in HEK293T cells overexpressing Mps1. Cells treated with MPI-0479605 undergo aberrant mitosis, resulting in aneuploidy and formation of micronuclei. In cells with wild-type p53, this promotes the induction of a postmitotic checkpoint characterized by the ATM- and RAD3-related-dependent activation of the p53–p21 pathway. Administration of MPI-0479605 at 30 mg/kg daily or 150 mg/kg every fourth day, i.p., for a period of 21 days, inhibited tumor growth of mice bearing subcutaneous HCT-116 tumor cell xenografts[2].
作用机制 MPI-0479605 is an ATP competitive inhibitor of Mps1.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.54mL

4.91mL

2.45mL
参考文献

[1]Tardif KD, Rogers A, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol Cancer Ther. 2011 Dec;10(12):2267-75.

[2]Tardif KD, Rogers A, Cassiano J, Roth BL, Cimbora DM, McKinnon R, Peterson A, Douce TB, Robinson R, Dorweiler I, Davis T, Hess MA, Ostanin K, Papac DI, Baichwal V, McAlexander I, Willardsen JA, Saunders M, Christophe H, Kumar DV, Wettstein DA, Carlson RO, Williams BL. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol Cancer Ther. 2011 Dec;10(12):2267-75. doi: 10.1158/1535-7163.MCT-11-0453. Epub 2011 Oct 6. PMID: 21980130.