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编 号:F715380
分子式:C30H35F3N6O3
分子量:584.63
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生物活性:
ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

体外研究:
ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively).ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM.ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively.ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line.
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