Table 3.
Comparison of inhibition of cellular proliferation by ABL1 TKIs (IC50, nM)
| Ba/F3-BCR-ABL1 | DCC-2036 | imatinib | dasatinib | nilotinib | MK-0457 |
|---|---|---|---|---|---|
| Ba/F3 Parent* | 3,500 | >10,000 | 3,800 | 9,500 | 102 |
| Native | 5.4 | 48 | 0.4 | 2.1 | 104 |
| L248R | 51 | >10,000 | 7.3 | 930 | 110 |
| G250E | 98 | 1,900 | 2.8 | 67 | 180 |
| Q252H | 2 | 700 | 0.3 | 5.1 | 130 |
| Y253F | 39 | 2,300 | 2 | 63 | 80 |
| Y253H | 56 | >10,000 | 1 | 120 | 190 |
| E255K | 127 | 6,400 | 8 | 80 | 84 |
| E255V | 150 | >10,000 | 2 | >10,000 | 190 |
| V299L | 6 | 190 | 8 | 10 | 200 |
| T315A | 19 | 536 | 65 | 17 | 88 |
| T315I | 13 | >10,000 | 5,200 | 2,800 | 74 |
| F317L | 36 | 417 | 2.3 | 10 | 84 |
| M351T | 14 | 417 | 1.1 | 4.2 | 65 |
| F359C | 120 | 2,500 | 2.7 | 190 | 130 |
| H396P | 81 | 1,700 | 1.2 | 49 | 160 |
IC50 values were determined as described in Experimental Procedures
*
Determined in the presence of 10 ng/mL IL-3