Table 1.
Fusion | Mutation | ROS1 Domain | Entrectinib IC50 (nmol/L) |
---|---|---|---|
CD74-ROS1 | - | 19.4 ± 2.3 | |
CD74-ROS1 | V1979A | Kinase | 7.3 ± 1.1 |
CD74-ROS1 | L1982F | Kinase | 5.2 ± 0.3 |
CD74-ROS1 | S1986T | Kinase | 5.3 ± 0.9 |
CD74-ROS1 | F2004C | Kinase | 177 ± 9.8 |
CD74-ROS1 | Q2012K | Kinase | 19.7 ± 3.8 |
CD74-ROS1 | G2032R | Kinase | > 2000 |
CD74-ROS1 | D2033N | Kinase | 21.4 ± 4.2 |
CD74-ROS1 | M2073T | Kinase | 11.4 ± 1.0 |
CD74-ROS1 | D2113G | Kinase | 21.4 ± 2.9 |
CD74-ROS1 | I2239* | C-term truncation | 10.6 ± 0.6 |
EZR-ROS1 | - | 5.2 ± 0.9 | |
EZR-ROS1 | A1924_I1934del | Juxtamembrane | 3.4 ± 0.2 |
EZR-ROS1 | F2004C | Kinase | 79.2 ± 7.9 |
EZR-ROS1 | G2032R | Kinase | 767.0 ± 26.3 |
EZR-ROS1 | D2113N | Kinase | 15.9 ± 2.1 |