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MK-8033 是ATP竞争性c-Met/Ron双重抑制剂,对野生型c-Met的IC50为1 nM,对c-Met N1100Y的IC50为2.0 nM。
中文别名:
3-(1-甲基-1H-吡唑-4-基)-5-氧代-N-(2-吡啶甲基)-5H-苯并[4,5]环己烯并[1,2-B]吡啶-7-甲磺酰胺
物化属性:
密度:1.39
沸点:761.011 °C at 760 mmHg
闪光点:414.045 °C
PSA:115.22000
LOGP:4.63500
[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
[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.
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