Table 1 Cell viability IC50 values for nine KIT-inhibitor TKIs in GIST cell lines
GIST CELL LINE | KIT MUTATION | IMATINIB | SUNITINIB | REGORAFENIB | SORAFENIB | NILOTINIB | PONATINIB | MASITINIB | DASATINIB | DOVITINIB |
|---|---|---|---|---|---|---|---|---|---|---|
GIST-T1 | Ex 11 | 4.5 | 5 | 35 | 30 | 15 | 4 | 15 | 4 | 4 |
GIST430 | Ex 11 | 35 | 10 | 150 | 40 | 50 | 5 | 30 | 10 | 50 |
GIST882 | Ex 13 | 300 | 70 | 800 | 300 | 350 | 50 | 350 | 150 | 500 |
GIST430/654 | Ex 11 + Ex 13 (V654A) | 2500 | 45 | 2000 | 800 | 850 | 100 | 3500 | 1000 | 250 |
GIST-T1/670 | Ex 11 + Ex 14 (T670I) | >10,000 | 30 | 60 | 150 | 5000 | 5 | 10000 | n.r. | 200 |
GIST-T1/816 | Ex 11 + Ex 17 (D816E) | 1500 | >10,000 | 550 | 650 | 500 | 40 | 6500 | 300 | 6000 |
GIST-T1/820 | Ex 11 + Ex 17 (D820A) | 1500 | >10,000 | 600 | 600 | 400 | 25 | 3000 | 90 | 1200 |
GIST-T1/829 | Ex 11 + Ex 18 (A829P) | 3000 | 10000 | 2500 | 1500 | 650 | 25 | >10,000 | 70 | 1500 |
GIST48B | KIT-independent | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | 1500 | >10,000 | >10,000 | 750 |
GIST226 | KIT-independent | >10,000 | >10,000 | >10,000 | >10,000 | 8000 | 6000 | >10,000 | >10,000 | >10,000 |
