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. 2019 Oct 4;10(46):10789–10801. doi: 10.1039/c9sc03445e

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.