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ALK-IN-21 (Compound B10), a potent ALK inhibitor for ALKG1202R mutation, exhibits remarkable enzymatic inhibitory potency with IC50 values of 4.59 nM, 2.07 nM and 5.95 nM toward ALKWT, ALKL1196M and ALKG1202R, respectively. ALK-IN-21 efficiently inhibits the proliferation of ALK-positive Karpas299 and H2228 cells both with IC50 values of 0.07 μM. ALK-IN-21 can be used for the research of anaplastic large cell lymphoma[1]. | [References]
[1] Xinyue Wang, et al. Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors. Bioorg Med Chem. 2022 Jul 15;66:116794. DOI:10.1016/j.bmc.2022.116794 |
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