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MK-0731

CAS No.: 845256-65-7

MK-0731, a synthetic small molecule with potential antineoplastic activity, selectively inhibits kinesin spindle protein
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Description MK-0731, a synthetic small molecule with potential antineoplastic activity, selectively inhibits kinesin spindle protein (KSP), leading to the inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase and apoptosis in tumor cells that overexpress KSP.
molecular weight 459.5
Molecular formula C25H28F3N3O2
CAS 845256-65-7
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: Soluble H2O: Insoluble
References 1. Matthieu, Michel; Dubois, Vincent; Tranchant, Isabelle; Kearsey, Jonathan. Preparation of peptide prodrugs modified with a 1,2,3,4-cyclobutanetetracarboxylic acid derived moiety useful in treatment and diagnosis of tumors and inflammatory diseases. PCT Int. Appl. (2008), 96pp. CODEN: PIXXD2 WO 2008120098 A2 20081009 CAN 149:448733 AN 2008:1210491 2. Matthieu, Michel; Dubois, Vincent; Tranchant, Isabelle; Kearsey, Jonathan. Preparation of peptide prodrugs modified with a 1,2,3,4-cyclobutanetetracarboxylic acid derived moiety useful in treatment and diagnosis of tumors and inflammatory diseases. Eur. Pat. Appl. (2008), 31pp. CODEN: EPXXDW EP 1977765 A1 20081008 CAN 149:448732 AN 2008:1205912 3. Cox, Christopher D.; Coleman, Paul J.; Breslin, Michael J.; Whitman, David B.; Garbaccio, Robert M.; Fraley, Mark E.; Buser, Carolyn A.; Walsh, Eileen S.; Hamilton, Kelly; Schaber, Michael D.; Lobell, Robert B.; Tao, Weikang; Davide, Joseph P.; Diehl, Ronald E.; Abrams, Marc T.; South, Vicki J.; Huber, Hans E.; Torrent, Maricel; Prueksaritanont, Thomayant; Li, Chunze; Slaughter, Donald E.; Mahan, Elizabeth; Fernandez-Metzler, Carmen; Yan, Youwei; Kuo, Lawrence C.; Kohl, Nancy E.; Hartman, George D. 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 Cancer. Journal of Medicinal Chemistry (2008), 51(14), 4239-4252. CODEN: JMCMAR ISSN:0022-2623. CAN 149:191278 AN 2008:779815 4. Javadi, Gary; Karady, Sandor; Maeda, Kenji; Miller, Ross A.; Szumigala, Ronald H. A process for the preparation of 2,2-disubstituted pyrroles. PCT Int. Appl. (2005), 48 pp. CODEN: PIXXD2 WO 2005102996 A2 20051103 CAN 143:440255 AN 2005:1171050