Description
An Mps1/TTK inhibitor (IC50 = 0.182 µM); selective for Mps1/TTK over a panel of 59 additional kinases (IC50s = >5 µM for all); accelerates mitosis, reducing the length of mitosis by approximately 3-fold, in U2OS cells; induces aneuploidy and apoptosis in A2780 ovarian cancer cells at 1 µM, as well as inhibits proliferation in a panel of 127 cancer cell lines (IC50s = 0.192-10 µM); reduces tumor growth in an A2780 mouse xenograft model at 90 mg/kg per day
Formal name: N-(2,6-diethylphenyl)-4,5-dihydro-1-methyl-8-[[4-[[(1-methyl-4-piperidinyl)amino]carbonyl]-2-(trifluoromethoxy)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Synonyms:
Molecular weight: 676.7
CAS: 1202055-32-0
Purity: ≥95%
Formulation: A solid