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NMS-P715

CAS No. : 1202055-32-0

MCE 站：NMS-P715

产品活性：NMS-P715 是一种选择性的，ATP 竞争性的 MPS1 抑制剂，IC₅₀ 值为 182 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：Mps1

In Vitro: NMS-P715 is a selective inhibitor of MPS1, with an IC₅₀ of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC₅₀ 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 EC₅₀ 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.

In Vivo: NMS-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.

相关产品：Anti-Aging Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Bioactive Compound Library Plus  |  Cytoskeleton Compound Library  |  BAY1217389  |  BOS-172722  |  Empesertib  |  MPI-0479605  |  Mps1-IN-3  |  AZ3146  |  Mps1-IN-1  |  Mps1-IN-2  |  TC-Mps1-12  |  CCT251455

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