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MPI-0479605

Cat. No. M2868
MPI-0479605 Structure
Size Price Availability Quantity
5mg USD 240  USD240 In stock
10mg USD 420  USD420 In stock
25mg USD 780  USD780 In stock
50mg USD 1480  USD1480 In stock
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Quality Control & Documentation
Biological Activity

MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.

Chemical Information
Molecular Weight 407.51
Formula C22H29N7O
CAS Number 1246529-32-7
Solubility (25°C) DMSO
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] Joost C M Uitdehaag, et al. Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity

[2] D Vijay Kumar, et al. Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors

[3] Keith D Tardif, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1

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