CFI-402257 HCl, MPS1/TTK 0099 CC1(C)C2C3=CC=CC=C3C=CC=2[N+](CCCCS([O-])(=O)=O)=C1/C=C/C=C/C=C/C=C1/N(CCCCS([O-])(=O)=O)C2=CC=C3C=CC=CC3=C2C/1(C)C

CC1(C)C2C3=CC=CC=C3C=CC=2[N+](CCCCS([O-])(=O)=O)=C1/C=C/C=C/C=C/C=C1/N(CCCCS([O-])(=O)=O)C2=CC=C3C=CC=CC3=C2C/1(C)C

InChiKey: WCYMJQXRLIDSAQ-UHFFFAOYSA-N

PubMed PMID: 26515592

PubMed Central PMCID: PMC4200330

2-PMPA demonstrates robust efficacy in numerous animal models of neurological disease

CFI-402257 HCl, MPS1/TTK 0099 CC1(C)C2C3=CC=CC=C3C=CC=2[N+](CCCCS([O-])(=O)=O)=C1/C=C/C=C/C=C/C=C1/N(CCCCS([O-])(=O)=O)C2=CC=C3C=CC=CC3=C2C/1(C)CCFI 402257 is an orally bioavailable inhibitor of monopolar spindle 1 (MPS1 TTK) kinase (IC50 = 1. 7 nM). CFI 402257 is selective for MPS1 TTK over a panel of 262 kinases at a concentration of 1 M. CFI 402257 increases aneuploidy in HCT116 cells when used at concentrations greater than 100 nM. It inhibits cell growth in a panel of breast, ovarian, prostate, pancreatic, lung, and colon cancer cell lines (GI50s = 0. 001 1. 3 M). CFI 402257 (6. 5 mg kg)