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CCT251455 

Cat. No. M28331
CCT251455  Structure
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Biological Activity

CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.

Chemical Information
Molecular Weight 503.98
Formula C26H26ClN7O2
CAS Number 1400284-80-1
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kai Chen, et al. J Biomol Struct Dyn. Identification of the hot spot residues for pyridine derivative inhibitor CCT251455 and ATP substrate binding on monopolar spindle 1 (MPS1) kinase by molecular dynamic simulation

[2] Paolo Innocenti, et al. J Med Chem. Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach

[3] Mark D Gurden, et al. Cancer Res. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance

[4] Sébastien Naud, et al. J Med Chem. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)

Related Mps1/TTK Products
Mps1-IN-6

Mps1-IN-6 is a potent Mps1 inhibitor with an IC50 value of 2.596 nM.

RMS-07 

RMS-07 is a covalent Monopolar Spindle Kinase 1 (MPS1/TTK) inhibitor, with an apparent IC50 of 13.1 nM. RMS-07 targets a poorly conserved cysteine in the kinase's hinge region.

NMS-P715 

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: CCT251455  supplier, Mps1/TTK, inhibitors, activators


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