Table 2 IC50s and maximal inhibition
From: Adaptive Darwinian off-target resistance mechanisms to selective RET inhibition in RET driven cancer
Treatment | BaF3 derived cell line | |||||
|---|---|---|---|---|---|---|
RET(898_901del)/ETV6-NTRK3 | RET(898_901del)/ETV6-NTRK3/EML4-ALK | RET(898_901del)/ETV6-NTRK3 + EML4-ALK | ||||
IC50 (nM) | aMaximal inhibition (%) | IC50 (nM) | Maximal inhibition (%)a | IC50 (nM) | Maximal inhibition (%)a | |
Selpercatinib | 290.6 | 55.9 | 1592 | 15.3 | 6268.0 | 40.5 |
Larotrectinib | 4300.0 | 27.7 | 421.8 | 58.4 | 1745.0 | 16.5 |
Entrectinib | 225.4 | 87.7 | 54.2 | 100.0 | 203.6 | 89.2 |
Selpercatinib (100 nM) +larotrectinb | 10.0 | 100.0 | 54.5 | 93.9 | 49.6 | 61.4 |
Selpercatinib (100 nM) +entrectinib | 1.8 | 100.0 | 14.2 | 100.0 | 8.5 | 100.0 |
