A dual inhibitor of c-Met and Ron
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MK-8033

Item No. 43662

Technical Information
Formal Name
3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide
CAS Number
1001917-37-8
Molecular Formula
C25H21N5O3S
Formula Weight
Purity
≥98%
A solid
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=C2)C3=CC(C4=CN(C)N=C4)=CN=C3C=CC1=CC=C2C[S](NCC5=CC=CC=N5)(=O)=O
InChi Code
InChI=1S/C25H21N5O3S/c1-30-15-20(13-28-30)19-11-23-24(27-12-19)8-7-18-6-5-17(10-22(18)25(23)31)16-34(32,33)29-14-21-4-2-3-9-26-21/h2-13,15,29H,14,16H2,1H3
InChi Key
VMJFTOSOFDEKTM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MK-8033 is a dual inhibitor of c-Met and Ron (IC50s = 1 and 7 nM, respectively).1 It reduces phosphorylated c-Met levels in GTL-16 gastric cancer cells (IC50 = 0.03 µM) and inhibits the proliferation of the same cells (IC50 = 0.58 µM). It induces apoptosis in and reduces the migration of OMM2.5, Mel202, and Mel285 uveal melanoma cells at 2.5 µM.2 MK-8033 (10-100 mg/kg, p.o.) reduces tumor volume in a GTL-16 mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Northrup, A.B., Katcher, M.H., Altman, M.D., 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. 56(6), (2013).

    2. Chattopadhyay, C., Grimm, E.A., and Woodman, S.E. Simultaneous inhibition of the HGF/MET and Erk1/2 pathways affect uveal melanoma cell growth and migration. PLoS One. 9(2), (2014).