MK-0731 |
Catalog No.GC74159
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 845256-65-7
Sample solution is provided at 25 µL, 10mM.
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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.
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].
MK-0731 (40 mg/kg/day; sc; for 11 days) inhibits the growth of KB-v tumors that highly overexpress Pgp, whereas Paclitaxel 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].
References:
[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-metlpiperidin-4-yl]-2-(droxymetl)-N-metl-2-phenyl-2,5-didro-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.
| Cas No. | 845256-65-7 | SDF | |
| Formula | C25H28F3N3O2 | M.Wt | 459.5 |
| Solubility | DMSO : 50 mg/mL (108.81 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1763 mL | 10.8814 mL | 21.7628 mL |
| 5 mM | 435.3 μL | 2.1763 mL | 4.3526 mL |
| 10 mM | 217.6 μL | 1.0881 mL | 2.1763 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)