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4 nM (Ki of 0
InChi: InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6
InChiKey: ULSSJYNJIZWPSB-CVRXJBIPSA-N
so it has IC50 >1 µM for inhibiting demthylation of H3K4 in U2OS human osteosarcoma cell line and in human breast adenocarcinoma MCF7 tumor cell proliferation assay
resulting in protracted endoplasmic reticulum stress and apoptosis via activation of caspase-3
CFI-402257 - MPS1/TTK inhibitor. CAS# 1610759-22-2 Catalog No.:M6548-2 4 nM (Ki of 0CFI 402257, CAS No. 1610759 22 2, 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).
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