Description
NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC 50 of 182 nM.In VitroNMS-P715 is a selective inhibitor of MPS1, with an IC 50 of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC 50 value of 5 µM and only 3 kinases inhibited below 10 µM (CK2, MELK, and NEK6). NMS-P715 promotes massive spindle assembly checkpoint (SAC) override with an EC 50 of 65 nM. NMS-P715 (1 µM) causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy and inhibits the proliferation of HCT116 cells. NMS-P715 (0.5, 1 µM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation. NMS-P715 (1 µM) exhibits bypass of the spindle assembly checkpoint and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. NMS-P715 (0-25 µM) also selectively inhibits growth of PDAC cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoNMS-P715 (10 mg/kg) exhibits an oral bioavailability of 37% and good pharmacokinetic properties in nude mice bearing subcutaneous implanted human tumor cell xenografts. NMS-P715 (90 mg/kg, p.o.) is well tolerated and cuases no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model. NMS-P715 (100 mg/kg, p.o.) inhibits the tumor growth by appr 43% in the A375 melanoma xenograft model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:Mps1 182 nM (IC 50 ) CK2 5.7 µM (IC 50 ) MELK 6.01 µM (IC 50 ) NEK6 6.02 µM (IC 50 )