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MK-0731

Chemical Structure : MK-0731

CAS No.: 845256-65-7

MK-0731 (MK0731)

Catalog No.: PC-62338Not For Human Use, Lab Use Only.

MK-0731 is a potent, selective kinesin spindle protein (KSP) inhibitor with IC50 of 2.2 nM, cell EC50 of 5.3 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MK-0731 is a potent, selective kinesin spindle protein (KSP) inhibitor with IC50 of 2.2 nM, cell EC50 of 5.3 nM; dispalys >20,000-fold selectivity for KSP over a panel of eight related kinesins (CENP-E, MKLP-1, Kif3A, Kif1B, uKHC, nKHC, KIF14, and MCAK); induces a mitotic block with an IC50 of 19 nM in cells that are refractory to paclitaxel due to P-gp overexpression; induces dose-dependent mitotic arrest in tumors and inhibits tumor growth in mouse xenograft.

Solid Tumors

Discontinued

Physicochemical Properties

M.Wt 459.513
Formula C25H28F3N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-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

References

1. Cox CD, et al. J Med Chem. 2008 Jul 24;51(14):4239-52.

2. Cox CD, et al. Anticancer Agents Med Chem. 2010 Nov 1;10(9):697-712.

3. Holen K, et al. Invest New Drugs. 2012 Jun;30(3):1088-95.

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