MK-0731 (MK0731)

Chemical Structure : MK-0731

CAS No.: 845256-65-7

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货号: PC-62338Not For Human Use, Lab Use Only.

MK-0731 (MK0731) is a potent, selective kinesin spindle protein (KSP, KIF11) inhibitor with IC50 of 2.2 nM, cell EC50 of 5.3 nM.

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生物&药学活性

MK-0731 (MK0731) is a potent, selective kinesin spindle protein (KSP, KIF11) inhibitor with IC50 of 2.2 nM, cell EC50 of 5.3 nM.
MK-0731 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).
MK-0731 induces a mitotic block with an IC50 of 19 nM in cells that are refractory to paclitaxel due to P-gp overexpression.
MK-0731 induces dose-dependent mitotic arrest in tumors and inhibits tumor growth in mouse xenograft.

物理化学性质&存储条件

分子量	459.513
分子式	C25H28F3N3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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.

MK-0731 (MK0731)

生物&药学活性

物理化学性质&存储条件

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MK-0731 (MK0731)

生物&药学活性

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