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NMS-P715MPS1 kinase inhibitor

NMS-P715

Catalog No. B5819
Size Price Stock
5mg Please Inquire Please Inquire
25mg Please Inquire Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

NMS-P715

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Chemical Properties

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
Canonical SMILES CCC1=C(/N=C(O)/C(C2=C3C4=NC(NC5=C(OC(F)(F)F)C=C(/C(O)=N/C(CC6)CCN6C)C=C5)=NC=C4CC2)=NN3C)C(CC)=CC=C1
Formula C35H39F3N8O3 M.Wt 676.73
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

Background

NMS-P715 is a potent and selective inhibitor of MPS1 kinase with IC50 value of 8 nM [1].

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 [1].

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 [1]. In human and murine pancreatic ductal adenocarcinoma (PDAC) cells, NMS-P715 inhibited cell growth [2]. 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) [3].

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% [1].

References:
[1].  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.
[2].  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.
[3].  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.