Chemical Structure : MK-8033 hydrochloride
CAS No.: 1283000-43-0
货号: PC-43478Not 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.
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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; 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; synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth.
Solid Tumors
Phase 1 Clinical
分子量 | ||
分子式 | C25H22ClN5O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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)-, hydrochloride (1:1) |
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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