MK8033 HCL

This product is for research use only, not for human use. We do not sell to patients.

MK8033 HCL
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Size Price Stock
100mg$2050Check With Us
250mg$3150Check With Us
500mg$4725Check With Us

Cat #: V4304 CAS #: 1283000-43-0 Purity ≥ 98%

Description: MK-8033 HCl is a novel, potent, selective, ATP competitive small-molecule, dual inhibitor of c-Met/Ron (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.

References: Northrup AB, et al, Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated 

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Molecular Weight (MW)507.99
Molecular FormulaC25H22ClN5O3S
CAS No.1283000-43-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SynonymsMK-8033; MK8033; MK 8033
ProtocolIn VitroMK-8033 hydrochloride binds more tightly to phosphorylated c-Met (Kd: 3.2 nM) than to its unphosphorylated counterpart (Kd: 10.4 nM), and inhibits oncogenic c-Met activation loop mutants with IC50s ranging from 0.6 to 1 nM. MK-8033 hydrochloride (1-10 μM, 72 h) inhibits GTL-16 cell proliferation (IC50: 0.58 μM). MK-8033 hydrochloride (1 μM, 2 h) inhibits phosphorylation of Y1349 of c-Met (IC50: 0.03 μM) in the c-Met dependent gastric cancer cell line GTL-16. MK-8033 hydrochloride (Compound 11r, 10 μM) displayed 31% inhibition of CYP3A4 (cytochrome P450 3A4).
In VivoMK-8033 hydrochloride exhibits moderate clearance (t1/2: 0.8 h for rats, 3.1 h for dog) and favorable bioavailability (35% for rats, 33% for dog). MK-8033 hydrochloride (Compound 11r, oral administration, 3-100 mg/kg, twice daily for 21 days) inhibits tumor growth in GTL-16 c-Met amplified gastric tumor xenografts.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.9685 mL9.8427 mL19.6854 mL39.3709 mL
5mM0.3937 mL1.9685 mL3.9371 mL7.8742 mL
10mM0.1969 mL0.9843 mL1.9685 mL3.9371 mL
20mM0.0984 mL0.4921 mL0.9843 mL1.9685 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
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.