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. Author manuscript; available in PMC: 2022 Aug 1.
Published in final edited form as: Mol Cancer Ther. 2021 Dec 14;21(2):336–346. doi: 10.1158/1535-7163.MCT-21-0395

Table 1.

Entrectinib sensitivity in re-engineered Ba/F3 cell lines

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