| In Vitro |
SIAIS117 (0-10 μM, 72 h) inhibits SR, H2228, NCI-H69 and NCI-H1688 cell growth, with IC50 values of 1.7, 46, 799, and 259 nM, respectively[1]. SIAIS117 (0-500 nM, 24 h) inhibits the phosphorylation of ALK and STAT3[1]. SIAIS117 inhibits the growth of G1202R-mutant ALK cell line and degrades G1202R-ALK protein[1]. SIAIS117 (100 nM, 24 h) causes sustained degradation of ALK protein in SR cells[1]. Cell Proliferation Assay Cell Line: NSCLC cell line H2228, Small cell lung cancer cell lines (NCI-H69, NCI-H1688)[1] Concentration: 0-10 μM Incubation Time: 72 h Result: Inhibited cell growth with an about two folds lower IC50 value (46 nM) comparing to SIAIS117NC (114 nM). Showed a good growth inhibition effect on NCI-H69 and NCI-H1688 cell line, with IC50 values of 799 and 259 nM, respectively. Western Blot Analysis Cell Line: SR, H2228[1] Concentration: 0, 1, 10, 50, 100, 500 nM Incubation Time: 24 h Result: Inhibited all of the phosphorylation of ALK at 10 nM and inhibited pSTAT3 in SR cell, degraded ALK proteins at the concentration starting from 50 nM in H2228 cell, and significantly downregulated UCK2 and GAK. Caused sustained degradation of ALK protein in SR cells.
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