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CCT251455, the mitotic kinase monopolar spindle 1 (MPS1/TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,820 | 8-10 weeks | |
50 mg | $2,380 | 8-10 weeks | |
100 mg | $3,100 | 8-10 weeks |
Description | CCT251455, the mitotic kinase monopolar spindle 1 (MPS1/TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool. |
Targets&IC50 | MPS1:3 nM |
In vitro | CCT251455 is a potent MPS1 inhibitor that exhibits high selectivity across a broad kinase profiling panel and excellent translation of in vitro biochemical potency to cellular potency compared to the isolated MPS1 enzyme (P-MPS1 IC50 of 0.04 μM and HCT116 GI50 of 0.16 μM).[1] |
In vivo | Methods: Mice bearing HCT116 human colon cancer xenografts were treated with CCT251455 (50, 75, and 100 mg/kg, orally, twice daily). Results: CCT251455 was well tolerated at all doses and inhibited MPS1 activity in mice; the observed reduction in phospho-histone H3 inhibition was consistent with the reduction in total plasma and tumor tissue exposure measured in the same experiment. [1] |
Alias | CCT 251455 |
Molecular Weight | 503.98 |
Formula | C26H26ClN7O2 |
Cas No. | 1400284-80-1 |
Smiles | O=C(OC(C)(C)C)N1C=2C=C(N=CC2C=C1C=3C=NN(C3)C)NC=4C=CC(=CC4Cl)C5=CN=CN5C |
Relative Density. | 1.34 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (198.42 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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