| Identification | Back Directory | [Name]
NMS-P715 | [CAS]
1202055-32-0 | [Synonyms]
NMS P715; NMS-P 715; NMS P715; NMS-P 715
Monopolar spindle 1,Mps1,NMS P715,NMS-P715,inhibit,NMSP715,Inhibitor,NMS-P-715
1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, N-(2,6-diethylphenyl)-4,5-dihydro-1-methyl-8-[[4-[[(1-methyl-4-piperidinyl)amino]carbonyl]-2-(trifluoromethoxy)phenyl]amino]- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C35H39F3N8O3 | [MOL File]
1202055-32-0.mol | [Molecular Weight]
676.73 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
11.75±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
JFOAJUGFHDCBJJ-UHFFFAOYSA-N | [SMILES]
CN(N=C1C(NC2=C(CC)C=CC=C2CC)=O)C3=C1CCC4=C3N=C(NC5=CC=C(C(NC6CCN(C)CC6)=O)C=C5OC(F)(F)F)N=C4 |
| Hazard Information | Back Directory | [Uses]
NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM. | [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[1]. | [IC 50]
Mps1: 182 nM (IC50); CK2: 5.7 μM (IC50); MELK: 6.01 μM (IC50); NEK6: 6.02 μM (IC50) | [References]
[1] Colombo R, et al. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64. DOI:10.1158/0008-5472.CAN-10-2101
[2] Slee RB, et al. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther. 2014 Feb;13(2):307-315. DOI:10.1158/1535-7163.MCT-13-0324 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|