NMS-P715

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NMS-P715 是一种高选择性和 ATP 竞争性 MPS1 抑制剂（IC50 为 182 nM）。

NMS-P715 is a highly selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).(In Vitro):NMS-P715 (1 μM) inhibits the proliferation of HCT116 cells. And it causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy. NMS-P715 (0.5, 1 μM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation. (In Vivo):NMS-P715 (90 mg/kg, p.o.) is well tolerated and causes no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model.

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.

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.

——

Metabolic Enzyme/Protease

Casein Kinase

Protease

——

——

1202055-32-0

676.745

C35H39F3N8O3

>98% (HPLC)

In Vitro:?DMSO : 2 mg/mL (2.96 mM)

CCc1cccc(CC)c1NC(=O)c1nn(C)c-2c1CCc1cnc(Nc3ccc(cc3OC(F)(F)F)C(=O)NC3CCN(C)CC3)nc-21

——

(-20℃)

With Ice Pack

≥ 2 years