MK-8033 Inhibitor CAS No. 1196681-38-5

Cat. No.	Name	Size	Price
KI2821	MK-8033	5 mg	$988
	MK-8033	10 mg	$1508
	MK-8033	20 mg	$2028
	MK-8033	50 mg	$3588
	MK-8033	1 g	$15080

Chemical Characteristic

Product Name	MK-8033
CAS No.	1196681-38-5
Molecular Weight	471.54
Formula	C₂₅H₂₁N₅O₃S
Chemical Name	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
Smiles	C(S(=O)(=O)NCc1ccccn1)c1ccc2c(c(=O)c3c(ncc(c3)c3cnn(c3)C)cc2)c1
Chemical Structure

Biological activities

MK-8033 is a dual c-Met/Ron inhibitor. The IC50s against c-Met and Ron are 1 and 7 nM, respectively. In a BIAcore-based direct binding assay, MK-8033 binds 3-fold more tightly to phosphorylated c-Met kinase domain (Kd= 3.2 nM) than to its unphosphorylated counterpart (Kd= 10.4 nM). MK-8033 is a weak inhibitor of cytochrome P450s at high μM concentrations. In vitro, MK-8033 inhibits the growth of GTL-16 with an IC50 of 580 nM. MK-8033 also potently inhibits c-Met/HGF-dependent cellular phenotypes in vitro. In human GTL-16 cMet amplified gastric tumor xenografts in CD1-nude mice, MK-8033 (100 mg/kg) achieves significant tumor inhibition in vivo.^[1]

References

[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, 56 (6): 2294-2310.

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