Table 1 Screening of ALK2 inhibitors
HSJD-DIPG-007 | SU-DIPG-IV | HSJD-DIPG-018 | SU-DIPG-VI | QCTB-R059 | |
|---|---|---|---|---|---|
Histone H3 | H3F3A K27M | HIST1H3B K27M | HIST1H3B K27M | H3F3A K27M | H3F3A K27M |
ACVR1 | ACVR1 R206H | ACVR1 G328V | ACVR1 R258G | ACVR1 wild-type | ACVR1 wild-type |
Dorsomorphin | 1.85 ± 0.15 µM | 6.21 ± 0.84 µM | 8.70 ± 0.71 µM | 5.01 ± 0.75 µM | 10.36 ± 1.44 µM |
DMH | >20 µM | >20 µM | >20 µM | >20 µM | >20 µM |
LDN-193189 | 0.70 ± 0.09 µM | 0.80 ± 0.02 µM | 3.16 ± 0.23 µM | 1.10 ± 0.20 µM | 0.89 ± 0.01 µM |
LDN-212854 | 1.25 ± 0.05 µM | 1.30 ± 0.20 µM | 3.22 ± 0.22 µM | 1.70 ± 0.20 µM | 1.70 ± 0.00 µM |
K02288 | 9.10 ± 0.26 µM | >20 µM | 14.34 ± 1.13 µM | >20 µM | >20 µM |
LDN-214117 | 1.57 ± 0.03 µM | 6.23 ± 0.30 µM | 16.38 ± 0.79 µM | 5.83 ± 0.18 µM | 8.27 ± 0.33 µM |
LDN-213844 | 3.67 ± 0.66 µM | 12.79 ± 2.65 µM | 15.44 ± 0.94 µM | 12.70 ± 2.17 µM | >20 µM |
LDN-213819 | 3.27 ± 0.15 µM | 8.03 ± 0.31 µM | 11.18 ± 0.61 µM | 9.87 ± 0.94 µM | 10.99 ± 1.63 µM |
Perhexiline | 4.07 ± 1.31 µM | 4.70 ± 1.01 µM | 6.11 ± 0.12 µM | 4.90 ± 1.08 µM | 5.33 ± 1.07 µM |
Saracatinib | 17.76 ± 0.56 µM | >20 µM | >20 µM | >20 µM | >20 µM |
Momelotinib | 7.32 ± 0.99 µM | 14.23 ± 0.89 µM | 9.50 ± 0.38 µM | 10.42 ± 1.12 µM | 15.94 ± 1.44 µM |
