CFI-400936 | MPS1/TTK inhibitor | Probechem Biochemicals

Chemical Structure : CFI-400936

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CFI-400936 (CFI 400936)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	477.58
分子式	C25H27N5O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(Dimethylamino)-2-(2-ethylphenyl)-N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)acetamide

参考文献

1. Radoslaw Laufer, et al. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.

CFI-400936 (CFI 400936)

生物&药学活性

物理化学性质&存储条件

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CFI-400936 (CFI 400936)

生物&药学活性

物理化学性质&存储条件

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