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.

For research use only. We do not sell to patients.

MK-0731 Chemical Structure

MK-0731 Chemical Structure

CAS No. : 845256-65-7

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Based on 1 publication(s) in Google Scholar

MK-0731 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (108.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1763 mL 10.8814 mL 21.7628 mL
5 mM 0.4353 mL 2.1763 mL 4.3526 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1763 mL 10.8814 mL 21.7628 mL 54.4070 mL
5 mM 0.4353 mL 2.1763 mL 4.3526 mL 10.8814 mL
10 mM 0.2176 mL 1.0881 mL 2.1763 mL 5.4407 mL
15 mM 0.1451 mL 0.7254 mL 1.4509 mL 3.6271 mL
20 mM 0.1088 mL 0.5441 mL 1.0881 mL 2.7203 mL
25 mM 0.0871 mL 0.4353 mL 0.8705 mL 2.1763 mL
30 mM 0.0725 mL 0.3627 mL 0.7254 mL 1.8136 mL
40 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3602 mL
50 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0881 mL
60 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6801 mL
100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5441 mL
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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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