Table 1 IC50 values (nM) for the mutant EGFR-expressing Ba/F3 cells, PC9 cells or MGH121 cells.

From: Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer

(a ) IC50 values of Ba/F3 cells expressing EGFR-del19 series to EGFR–TKIs

Ba/F3-EGFR-

Gefitinib

Afatinib

Osimertinib

EGF-816

 

Del19

5.9

<0.3

1.7

2.9

 

T790M/del19

5,603

78.2

6.7

18.5

 

C797S/del19

2.7

2.1

513.4

1,241

 

C797S/T790M/del19

2,922

392.7

740.5

1,408

 

Parent(+IL-3)

>10,000

381.3

752.4

–

 

(b ) IC50 values of Ba/F3 cells expressing EGFR-L858R series to EGFR–TKIs

Ba/F3-EGFR-

Gefitinib

Afatinib

Osimertinib

EGF-816

 

L858R

10.4

<0.3

3

7.7

 

T790M/L858R

5,922

39.2

5.8

15.5

 

C797S/L858R

15.5

7.7

1,115

1,659

 

C797S/T790M/L858R

>10,000

804.2

1,171

2,278

 

(c ) IC50 values of PC9 cells to EGFR–TKIs

 

Gefitinib

Afatinib

Osimertinib

  

PC9 parent

16.38

0.638

7.463

  

PC9 T790M

14,684

61.94

11.31

  

PC9 triple

>10,000

1,130

3,461

  

(d ) IC50 values of PC9 cells to ALK–TKIs

 

Brigatinib

AP26113-analog

AZD3463

 

PC9 parent

132.8

46.18

253

 

PC9 T790M

243.8

89.28

378.3

 

PC9 triple

599.2

194.7

622.4

 

(e ) IC50 values of MGH121 cells to EGFR–TKIs

 

Gefitinib

Osimertinib

Brigatinib

 

MGH121-pt

3,228

2.58

155.3

 

MGH121-res2

>10,000

7,155

592.1

 
  1. EGFR, epidermal growth factor receptor; TKIs, tyrosine kinase inhibitors;
  2. (a–b) IC50 values for the Ba/F3 cells expressing EGFR-activating mutations with or without resistant mutations, the del19 series (a) and the L858R series (b), respectively, treated with the indicated EGFR–TKIs. (c–d) IC50 values for PC9 cells (parental, T790M or C797S/T790M/del19-induced) treated with the indicated EGFR–TKIs (c) or ALK–TKIs (d). (e) IC50 values for the MGH121 parental and res-2 cells treated with the indicated TKIs.
Back to article page