MK-5108 (VX689)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1140 | Check With Us |
| 500mg | $1850 | Check With Us |
| 1g | $2775 | Check With Us |
: Cat #: V0357 CAS #: 1010085-13-8 Purity ≥ 98%
Description: MK-5108 (also known as VX-689) is a novel, specific and ATP-competitive inhibitor of Aurora A kinase with potential anticancer activity.
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| Molecular Weight (MW) | 461.94 |
|---|---|
| Molecular Formula | C22H21ClFN3O3S |
| CAS No. | 1010085-13-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 92 mg/mL (199.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 0.5% methylcellulose+0.2% Tween 80: ~30mg/mL |
| SMILES Code | O=C([C@@]1(CC2=NC(NC3=NC=CS3)=CC=C2)CC[C@H](OC4=CC=CC(Cl)=C4F)CC1)O |
| Synonyms | VX-689; VX689; VX 689; MK5108; MK-5108; MK 5108; VX-689 |
| Protocol | 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. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1648 mL | 10.8239 mL | 21.6478 mL | 43.2957 mL |
| 5mM | 0.4330 mL | 2.1648 mL | 4.3296 mL | 8.6591 mL |
| 10mM | 0.2165 mL | 1.0824 mL | 2.1648 mL | 4.3296 mL |
| 20mM | 0.1082 mL | 0.5412 mL | 1.0824 mL | 2.1648 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.