Table 2. Antiproliferative Activity of 18k in BaF3, PC9, PC9-EGFRTM2, and H1299 Cell Linesa.
| BaF3 |
||||||
|---|---|---|---|---|---|---|
| IC50 (μM) | EGFRTM1 | EGFRTM2 | parental cells | PC9 | PC9-EGFRTM2 | H1299b |
| 18k | 0.258 ± 0.167 | 0.141 ± 0.081 | 1.691 ± 0.253 | 1.192 ± 0.727 | 0.603 ± 0.294 | 2.115 ± 0.302 |
| brigatinib (9) | 0.286 ± 0.176 | 0.155 ± 0.046 | 4.191 ± 1.614 | 0.829 ± 0.148 | 1.110 ± 0.028 | 1.049 ± 0.160 |
| AZD9291 (5) | 2.893 ± 0.601 | 2.885 ± 0.689 | 4.427 ± 1.162 | 0.011 ± 0.005 | 3.210 ± 0.853 | >10.0 |
a
BaF3-EGFRTM1, BaF3-EGFRTM2, and PC9-EGFRTM2 cell lines were built by Jian Ding’s laboratory, Shanghai Institute of Materia Medica, Chinese Academy of Sciences. PC9-EGFRTM2 cell line was constructed by introducing the T790M/C797S mutant into PC9 (EGFR19Del). Cellular assay was determined using the CCK8 assay.
b
H1299 (EGFRWT) cellular assay was determined using sulforhodamine B (SRB) assay. The data were shown as mean ± SD from at least three independent experiments. TM1, L858R/T790M/C797S; TM2, 19Del/T790M/C797S.