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CAS No. : 1202055-32-0
MCE 国际站: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:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Targeted Diversity Library | Highly Selective Inhibitors Library | TC-Mps1-12 | Mps1-IN-1 dihydrochloride | AZ3146 | Mps1-IN-1 | Mps1-IN-3 hydrochloride | Mps1-IN-4 | BOS-172722 | RMS-07 | Mps-BAY2a | MPI-0479605 | Empesertib | BAY1217389 | CCT251455 | Mps1-IN-5 | Mps1-IN-2 | Mps1-IN-6
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