MK-5108 [1010085-13-8]
Referencia HY-13252-5mg
embalaje : 5mg
Marca : MedChemExpress
MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.
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MK-5108 Estructura química
No. CAS : 1010085-13-8
This product is a controlled substance and not for sale in your territory.
Based on 3 publication(s) in Google Scholar
Ver todos los productos específicos de isoformas Aurora Kinase:
Descripciòn |
MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM. |
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IC50 & Target[1] |
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In Vitro |
MK-5108 inhibits Aurora-A activity with an IC50 value of 0.064 nM in an ATP-competitive manner. It shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold). MK-5108 also exhibits high selectivity for Aurora-A over other protein kinases. MK-5108 inhibits the growth of 14 cell lines with IC50 values between 0.16 and 6.4 μM[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
MK-5108 treatments at 15 and 30 mg/kg results in significant tumor growth inhibition in the HCT116 tumor model. MK-5108 is well tolerated at both doses, with minimal reduction in body weight. MK-5108 also exhibits significant antitumor activity in nude rats bearing SW48 tumors. MK-5108 at 15 and 45 mg/kg causes dose-dependent tumor growth inhibition with a %T/C of 35% and 7% at day 10, and 58% and 32% at day 27, respectively. MK-5108 is well tolerated in nude rats, with no body weight reduction and moderate effect on blood cells[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Ensayo clínico |
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Peso molecular |
461.94 |
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Fòrmula |
C22H21ClFN3O3S |
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No. CAS |
1010085-13-8 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
FC(C(Cl)=CC=C1)=C1O[C@H](CC2)CC[C@@]2(C(O)=O)CC3=CC=CC(NC4=NC=CS4)=N3 |
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Envío | Room temperature in continental US; may vary elsewhere. |
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Almacenamiento |
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Solvente y solubilidad |
In Vitro:
DMSO : 12.5 mg/mL (27.06 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Pureza y Documentación |
Purity: 99.89% |
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Referencias |
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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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.1648 mL | 10.8239 mL | 21.6478 mL | 54.1196 mL |
5 mM | 0.4330 mL | 2.1648 mL | 4.3296 mL | 10.8239 mL | |
10 mM | 0.2165 mL | 1.0824 mL | 2.1648 mL | 5.4120 mL | |
15 mM | 0.1443 mL | 0.7216 mL | 1.4432 mL | 3.6080 mL | |
20 mM | 0.1082 mL | 0.5412 mL | 1.0824 mL | 2.7060 mL | |
25 mM | 0.0866 mL | 0.4330 mL | 0.8659 mL | 2.1648 mL |
MK-5108 Related Classifications
- Cell Cycle/DNA Damage Epigenetics Autophagy
- Aurora Kinase Autophagy