MK-0731

• UNSPSC Description:

  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[1][2].

• Target Antigen:

  Apoptosis; Kinesin; Lipoxygenase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Cell Cycle/DNA Damage;Cytoskeleton;Metabolic Enzyme/Protease

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/mk-0731.html

• Purity:

  99.85

• Solubility:

  DMSO : 50 mg/mL (ultrasonic)

• Smiles:

  O=C(N(C)[C@@H](CC1)[C@H](F)CN1C)N2[C@@](C3=CC=CC=C3)(CO)C=C(C4=CC(F)=CC=C4F)C2

• Molecular Weight:

  459.50

• References & Citations:

  [1]Christopher D Cox, et al. 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. J Med Chem. 2008 Jul 24;51(14):4239-52.|[2]Kyle Holen, et al. A phase I trial of MK-0731, a kinesin spindle protein (KSP) inhibitor, in patients with solid tumors. Invest New Drugs. 2012 Jun;30(3):1088-95.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Clinical Information:

  Phase 1

• CAS Number:

  845256-65-7