NMS-P715

SKU: orb1940780

Description

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.

Key Properties

• CAS Number: 1202055-32-0
• MW: 676.745
• Purity: >98% (HPLC)
• Formula: C₃₅H₃₉F₃N₈O₃
• SMILES: CCc1cccc(CC)c1NC(=O)c1nn(C)c-2c1CCc1cnc(Nc3ccc(cc3OC(F)(F)F)C(=O)NC3CCN(C)CC3)nc-21
• Target: Casein Kinase
• Solubility: In Vitro: DMSO : 2 mg/mL (2.96 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Casein Kinase