Chemical Structure : CFI-400936
CAS No.:
1338793-07-9
CFI-400936
(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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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477.58
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Formula
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C25H27N5O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(Dimethylamino)-2-(2-ethylphenyl)-N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)acetamide
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References
1. Radoslaw Laufer, et al. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.
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