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. Author manuscript; available in PMC: 2016 Jul 13.
Published in final edited form as: Cancer Cell. 2015 Jul 2;28(1):70–81. doi: 10.1016/j.ccell.2015.05.010

Figure 2. PF-06463922 potently inhibits ALK fusion wild type and mutant-mediated tumor cell survival.

Figure 2

(A–C) Cell viability assays of H3122 EML4-ALKWT (A), H3122 EML4- ALKL1196M (B), H3122 EML4-ALKG1269A (C) cells treated with the indicated doses of crizotinib or PF-06463922 for 72 hours. Cell viability was assayed by Cell-Titer-Glo. For panels A–C, values are presented as mean +/− SEM (n=3) D) IC50 of PF-06463922, crizotinib, ceritinib and alectinib on ALK phosphorylation in H3122 cell lines expressing EML4-ALKWT, EML4-ALKL1196M and EML4-ALKG1269A. Values are presented as mean +/− SEM (n=3–7). E) Cleaved caspase 3/7 induction by PF-06463922 treatment in the three different H3122 cell models. Values are presented as mean +/− SD (n=3). F) Cell viability assay of the alectinib-resistant H3122 cell line (EML4-ALKV1180L) treated with the indicated doses of crizotinib, PF-06463922 or alectinib for 72 hours. Values are presented as mean +/− SEM (n=6) G) Cell survival and ALK phosphorylation IC50s of PF-06463922, crizotinib, ceritinib and alectinib on crizotinib-resistant patient-derived cell line SNU2535 (EML4-ALKG1269A). Values are presented as mean +/− SEM (n=3–14). H) Cell viability assay of ceritinib-resistant patient-derived cell line MGH021-5 (SQSTM1-ALKG1202R) treated with the indicated doses of crizotinib, PF-06463922 or alectinib for 7 days. I) Cell viability assay of alectinib-resistant patient-derived cell line MGH056-1 (EML4-ALKI1171T) treated with the indicated doses of crizotinib, PF-06463922 or alectinib for 72 hours. For panels H and I values are presented as mean +/− SEM (n=3). See also Figure S2.