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MK-8033

Catalog No. TQ0219 CAS 1001917-37-8

MK-8033 is a new and selective dual ATP competitive c-Met/Ron inhibitor (IC50: 1 nM Wt c-Met).

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MK-8033, CAS 1001917-37-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 98.00
2 mg	In stock	$ 145.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 422.00
25 mg	In stock	$ 689.00
50 mg	In stock	$ 981.00
1 mL * 10 mM (in DMSO)	In stock	$ 256.00

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Purity: 97.16%

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Description	MK-8033 is a new and selective dual ATP competitive c-Met/Ron inhibitor (IC50: 1 nM Wt c-Met).
Targets&IC50	c-Met (WT):1 nM (cell free), c-Met (N1100Y):1 nM (cell free)
In vitro	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). Significantly, MK-8033 potently inhibits the kinase activity of three oncogenic c-Met activation loop mutants, Y1230C, Y1230H, and Y1235D (IC50s: 0.6~1 nM at 50 uM ATP) in addition to other c-Met activating mutants N1100Y and M1250T. MK-8033 potently inhibited GTL-16 proliferation (IC50: 582 nM). By contrast, the HCT116 cell line, which does not harbor basal c-Met activation, was not inhibited by MK-8033 (IC50 > 10000 nM) [1]. MK-8033 radiosensitizer the high-c-Met-expressing EBC-1 and H1993 cells but not the low-c-Met-expressing cell lines A549 and H460. However, irradiation of A549 and H460 cells increased the expression of c-Met protein at 30 minutes after the irradiation. Subsequent targeting of this up-regulated c-Met by using MK-8033 followed by a second radiation dose reduced the clonogenic survival of both A549 and H460 cells. MK-8033reduced the levels of radiation-induced phosphorylated (activated) c-Met in A549 cells [2].
In vivo	MK-8033 was orally dosed in GTL-16 tumor xenograft bearing mice. Mice were euthanized 1 h after dosing and tested for p-Met (Y1349) in tumors and MK-8033 concentrations in plasma. At 100 mg/kg, essentially complete inhibition of p-Met (Y1349) was achieved. An in vivo IC50 of 1.3 uM was deduced from the relationship between plasma MK-8033 level and Met pY1349. Dosing at 3, 10, 30, and 100 mg/kg resulted in 22, 18, 57, and 86% tumor growth inhibition, respectively, relative to the tumor from vehicle-treated mice [1].

Molecular Weight	471.53
Formula	C25H21N5O3S
CAS No.	1001917-37-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (97.83 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compound Library Bioactive Compounds Library Max Orally Active Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MK-8033 1001917-37-8 Tyrosine Kinase/Adaptors c-Met/HGFR bladder cancer breast cancer EBC-1 H1993 MK 8033 anti-tumor Inhibitor GTL-16 radiosensitivity Anti-ancer MK8033 NSCLCs inhibit inhibitor

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