2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Metabolic Enzyme/Protease
  3. Kinesin Apoptosis Lipoxygenase
  4. MK-0731

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.

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MK-0731 Chemical Structure

MK-0731 Chemical Structure

CAS No. : 845256-65-7

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MK-0731 Related Antibodies

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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].

IC50 & Target[1]

KSP

2.2 nM (IC50)

In Vitro

MK-0731 (0.415-300 nM; 48 h) induces apoptosis in A2780 cells with an EC50 of 2.7 nM[1].
MK-0731 displays little affinity for binding to the hERG channel (IC50=20.5 μM)[1].
MK-0731 has the ability to induce a mitotic block with an IC50 of 19 nM in cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MK-0731 Related Antibodies

Apoptosis Analysis[1]

Cell Line: A2780 cells
Concentration: 0.415-300 nM
Incubation Time: 48 h
Result: Induced apoptosis with an EC50 of 2.7 nM.
In Vivo

MK-0731 (40 mg/kg/day; sc; for 11 days) inhibits the growth of KB-v tumors that highly overexpress Pgp, whereas Paclitaxel (HY-B0015) has no effect[1].
MK-0731 (2.5, 5, 10, 20, and 40 mg/kg/day; minipump) exhibits a dose-proportional increase in both exposure and mitotic arrest in tumors in A2780-xenografted mice[1].
MK-0731 (1 mg/kg/day; iv) has a T1/2 of 1 hours, a CL of 66 mL/min•kg, and a Vss of 3 L/kg for rats[1].
Pharmacokinetic Parameters of MK-0731 in rats[1].

rat iv (1 mg/kg) dog iv (0.4 mg/kg) rhesus iv (0.4 mg/kg)
T1/2 (h) 1 2 1
CL (mL/min/kg) 66.7 15.1 23.1
Vss (L/kg) 3.0 1.6 2.3

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice for the dual flank xenograft KB-3-1 and KB-v-1 cells[1]
Dosage: 40 mpk
Administration: SC; qd×1; for 11 days
Result: Inhibited the growth of KB-v tumors that highly overexpress Pgp, whereas Paclitaxel (20 mpk; qd×5) had no effect.
Clinical Trial
Molecular Weight

459.50

Formula

C25H28F3N3O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    formulated as a solution in acidified saline at pH 4.0, 100 μL

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Purity & Documentation
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MK-0731 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-0731845256-65-7MK0731MK 0731KinesinApoptosisLipoxygenaseLOXnon-competitiveallosterickinesin spindle proteinmitotic arrestantitumorA2780mitotic blockInhibitorinhibitorinhibit

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