NMS-P715 - 99%, high purity , CAS No.1202055-32-0

Item Number

N648450

• Synonyms: MPS1 Inhibitor | NMS-P715 | (N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide)
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: NMS-P715 is a selective, ATP-competitive inhibitor of MPS1 , with an IC 50 of 182 nM.
• Storage Temp: Protected from light,Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Note: 2mg，100mg卖完停产，不再备货

Product Description

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1 , with an IC 50 of 182 nM.

In Vitro

NMS-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 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:Mps1 182 nM (IC 50 ) CK2 5.7 μM (IC 50 ) MELK 6.01 μM (IC 50 ) NEK6 6.02 μM (IC 50 )