|NMS-P715MPS1 kinase inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||1202055-34-2||SDF||Download SDF|
|Chemical Name||(Z)-N-(2,6-diethylphenyl)-8-((4-((Z)-hydroxy((1-methylpiperidin-4-yl)imino)methyl)-2-(trifluoromethoxy)phenyl)amino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carbimidic acid|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
NMS-P715 is a potent and selective inhibitor of MPS1 kinase with IC50 value of 8 nM .
Human monopolar spindle 1 (MPS1) kinase is a serine/threonine kinase that plays an important role in spindle assembly checkpoint (SAC) signaling by influencing the stability of the kinetochore-microtubule interaction and controlling chromosome alignment .
NMS-P715 is an orally available, selective and ATP-competitive MPS1 kinase inhibitor. In nocodazole-arrested U2OS cells, NMS-P715 promoted massive SAC override with EC50 value of
65 nM. In U2OS cells overexpressing YFP-α-tubulin, NMS-P715 induced mitotic acceleration and reduced mitotic cells. In nocodazole-arrested HeLa cells with MG132, NMS-P715 leads to complete delocalization of MAD1, MAD2, BUB1, BUB3 and Borealin and also reduced MPS1. In A2780 ovarian cancer cells, NMS-P715 reduced G1 phase, caused a flattening in G2/M phase of the cell cycle and subsequently induced apoptosis . In human and murine pancreatic ductal adenocarcinoma (PDAC) cells, NMS-P715 inhibited cell growth . In glioblastoma (GBM) cells, NMS-P715 increased the radiosensitivity of GBM cells by induction of post-radiation mitotic catastrophe and reduced repair of DNA double strand breaks (DSBs) .
In nude mice bearing human A2780 ovary carcinoma xenograft model, NMS-P715 (90 mg/kg for 7 days) inhibited tumor growth by 53%. In the A375 melanoma xenograft model, NMS-P715 (100 mg/kg for 10 days) inhibited tumor growth by 43% .
. Colombo R, Caldarelli M, Mennecozzi M, et al. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res, 2010, 70(24): 10255-10264.
. Slee RB, Grimes BR, Bansal R, et al. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther, 2014, 13(2): 307-315.
. Maachani UB, Kramp T, Hanson R, et al. Targeting MPS1 Enhances Radiosensitization of Human Glioblastoma by Modulating DNA Repair Proteins. Mol Cancer Res, 2015, 13(5): 852-862.