Table 1. Anti-proliferation effect against CHMFL-EGFR-26 against a panel of BaF3 isogenic cell linesa.
Cells (GI50: μM) | CHMFL-EGFR-26 | CHMFL-EGFR-26R | AZD9291 |
---|---|---|---|
Parental BaF3 | >10 | >10 | 1.5 |
BaF3-TEL-EGFR | 5.4 | >10 | 0.3 |
BaF3-TEL-EGFR-C797S | 2.5 | 6.6 | 0.59 |
BaF3-TEL-EGFR-L858R | <0.0003 | >10 | <0.0003 |
BaF3-TEL-EGFR-L858R-C797S | 3.2 | >10 | 0.59 |
BaF3-TEL-EGFR-T790M | <0.0003 | >10 | 0.013 |
BaF3-TEL-EGFR-T790M-C797S | 3.7 | >10 | 0.55 |
BaF3-FL-EGFR-del19 | 0.013 | >10 | 0.001 |
BaF3-FL-EGFR-del19-T790M | <0.0003 | 7.1 | <0.0003 |
BaF3-FL-EGFR-del19-T790M-C797S | 2.1 | 7.3 | 0.2 |
BaF3-FL-EGFR-L858R-T790M | 0.006 | >10 | <0.0003 |
BaF3-FL-EGFR-L858R-T790M-C797S | 0.34 | >10 | 0.31 |
aAll GI50 values were obtained by triplet testing.