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MK-0731 

Cat. No. M30678
MK-0731  Structure
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Biological Activity

MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy.

Chemical Information
Molecular Weight 459.5
Formula C25H28F3N3O2
CAS Number 845256-65-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Umar Faruk Mansoor, et al. Bioorg Med Chem. Discovery of novel spiro 1,3,4-thiadiazolines as potent, orally bioavailable and brain penetrant KSP inhibitors

[2] Ajmal Khan, et al. Chemistry. Palladium-catalyzed enantioselective decarboxylative cycloaddition of vinylethylene carbonates with isocyanates

[3] Kyle Holen, et al. Invest New Drugs. A phase I trial of MK-0731, a kinesin spindle protein (KSP) inhibitor, in patients with solid tumors

[4] Christopher D Cox, et al. Anticancer Agents Med Chem. Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs

[5] Christopher D Cox, et al. J Med Chem. Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory can䲧癐

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Keywords: MK-0731  supplier, Kinesin, inhibitors, activators

 
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