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Chemical Structure : MK-8033
CAS No.: 1001917-37-8
Catalog No.: PC-43477Not For Human Use, Lab Use Only.
MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $528 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM.
MK-8033 is >100-fold selective relative to Ron and c-Met inhibition against a panel of 221 kinases.
MK-8033 potently and selectively inhibits growth in c-Met amplified cell lines (GTL-16 proliferation IC50 =582 nM), causes full inhibition of tumor growth in c-Met amplified (GTL-16) subcutaneous tumor xenograft model.
MK-8033 synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth.
| M.Wt | 471.53 | |
| Formula | C25H21N5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 46 mg/mL |
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| Chemical Name/SMILES |
5H-Benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide, 3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)- |
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1. Northrup AB, et al. J Med Chem. 2013 Mar 28;56(6):2294-310.
2. Bhardwaj V, et al. J Thorac Oncol. 2012 Aug;7(8):1211-7.
3. Marchion DC, et al. Oncol Rep. 2013 May;29(5):2011-8.
4. Keedy VL, et al. Invest New Drugs. 2018 Jan 29. doi: 10.1007/s10637-018-0567-z.
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