Table 4. IC50 determination of pyrrolopyrimidine EGFR inhibitors against osimertinib resistant EGFR-L858R/T790M/C797S a .
Compound | EGFR HTRF IC50 [nM] |
L858R/T790M/C797S | |
29a | 354 ± 110 |
29b | 406 ± 139 |
29c | 110 ± 36 |
29d | 803 ± 434 |
29e | 768 ± 10 |
29f | >20 000 |
29g | 555 ± 139 |
29h | 356 ± 79 |
29i | 249 ± 67 |
29j | 22 ± 17 |
29k | 243 ± 132 |
29l | 2343 ± 952 |
19a | 50 ± 19 |
19b | 113 ± 47 |
19c | 21 ± 7 |
19d | 9.4 ± 1.5 |
19e | 49 ± 35 |
19f | 19 ± 11 |
19g | 8.6 ± 3.2 |
19h | 8.5 ± 3.7 |
19i | 2061 ± 359 |
Gefitinib | 250 ± 23 |
Afatinib | 25 ± 17 |
WZ4002 | 452 ± 189 |
Rociletinib | 541 ± 119 |
Osimertinib | 116 ± 15 |
EGF816 | 398 ± 105 |
Staurosporine | 1.5 ± 0.0 |
aValues are the mean ± SD of three independent measurements in duplicates.