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Product Name | CFI-402257 |
Description | An orally bioavailable inhibitor of MPS1/TTK (IC50 = 1.7 nM); selective for MPS1/TTK over a panel of 262 kinases at 1 µM; increases aneuploidy in HCT116 cells at >100 nM; inhibits cell growth in a panel of breast, ovarian, prostate, pancreatic, lung, and colon cancer cell lines (GI50s = 0.001-1.3 µM); reduces tumor growth in HCT116 and HT29 mouse xenograft models as well as platinum-resistant and -sensitive high-grade serous ovarian cancer PDX mouse models at 6.5 mg/kg; inhibits CYP2C9 and CYP2C19 (IC50s = 13 and 8 µM, respectively) as well as CYP3A4 metabolism of BFC and DBF (IC50s = 0.51 and 14 µM, respectively) |
Size | 1 mg |
Concentration | n/a |
Applications | n/a |
Other Names | CFI402257 MPS-1 HCT-116 HT-29 CYP-2C9 2C19 3A4 |
Gene, Accession, CAS # | CAS: 1610759-22-2 |
Catalog # | 21960-1 |
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Order / More Info | CFI-402257 from CAYMAN CHEMICAL COMPANY |
Product Specific References | n/a |
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