Chemical Structure : CFI-400936
Catalog No.: PC-21556Not For Human Use, Lab Use Only.
CFI-400936 is a potent, selective Tyrosine Threonine Kinase (TTK, Mps1) inhibitor with IC50 of 3.6 nM.
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CFI-400936 is a potent, selective Tyrosine Threonine Kinase (TTK, Mps1) inhibitor with IC50 of 3.6 nM.
CFI-400936 attenuates cell growth of HCT116 cells with GI50 of 0.10 μM.
CFI-400936 also inhibits the cell growth of A549, MD-MB-468, OVCAR-3 andSW620 cancer cell lines with GI50's of 0.16, 0.66, 1.3, and 0.21, respectively.
CFI-400936 promotes mitotic checkpoint bypass with phospho-histone H3 EC50 values of 0.52 μM, causes massive aneuploidization of cells at 1 μM and cell death.
CFI-400936 (25 mg/kg QD, ip) demonstrated a dose dependent tumor growth inhibition (TGI) of 66% in HCT116 xenografts in SCID mice.
M.Wt | 477.58 | |
Formula | C25H27N5O3S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Radoslaw Laufer, et al. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.
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