MK-8033 (hydrochloride)

MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron) ), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) [1][2].

Product Specifications

CAS Number

[1283000-43-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

C-Met/HGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/MK-8033-hydrochloride.html

Concentration

10mM

Purity

99.86

Solubility

DMSO : 5.88 mg/mL (ultrasonic) |H2O : 7.14 mg/mL (ultrasonic)

Smiles

O=S(CC1=CC=C2C(C(C3=CC(C4=CN(C)N=C4)=CN=C3C=C2)=O)=C1)(NCC5=NC=CC=C5)=O.Cl

Molecular Formula

C25H22ClN5O3S

Molecular Weight

507.99

Precautions

H302, H315, H319, H335

References & Citations

[1]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 state of c-Met. J Med Chem. 2013 Mar 28;56 (6) :2294-310.|[2]Bhardwaj V, et al. C-Met inhibitor MK-8003 radiosensitizes c-Met-expressing non-small-cell lung cancer cells with radiation-induced c-Met-expression. J Thorac Oncol. 2012 Aug;7 (8) :1211-7.|[3]Chandrani Chattopadhyay, et al. Simultaneous inhibition of the HGF/MET and Erk1/2 pathways affect uveal melanoma cell growth and migration. PLoS One. 2014 Feb 13;9 (2) :e83957.