1.
Compound | Effective concentration
in RKO (BRAF mut) (μM) |
Effective concentration
in RKO (BRAF WT) (μM) |
Mechanism of action |
RKO colorectal cancer cells BRAF V600E or WT were screened with 298 approved oncology drugs alone or in combination with irradiation. Radiosensitisation factors were calculated from the ratio of fluorescence of irradiated versus non-irradiated plates. The most significant hits for BRAF-mutant variant RKO cells are shown; each hit has radiosensitisation factor < 1, PFP ≤0.05 and P-values ≤0.05; ‘ns’ indicates that significance was not reached in the BRAF WT cell line for the drug tested. | |||
Dactolisib | 0.016, 0.4 | 0.016 | Dual PI3K/mTOR inhibitor |
Panobinastat | 0.016 | ns | HDAC inhibitor |
Trametinib | 0.016 | 0.016 | MEK inhibitor |
ABT-199 | 0.08 | 0.08 | Bcl-2 inhibitor |
Olaparib | 0.08 | ns | PARP inhibitor |
Tosedostat | 0.08 | ns | Peptidase inhibitor |
AZD 7762 | 0.08 | 0.08 | Chk inhibitor |
Pimasertib | 0.4, 0.08 | 0.08 | MEK inhibitor |
PF477736 | 0.08 | ns | Chk1 inhibitor |
17-AAG | 0.08 | ns | Hsp90 inhibitor |
Doramapimod | 0.08 | ns | p38 MAPK inhibitor |
Danusertib | 0.08 | ns | aurora kinase inhibitor |
Serdametan | 0.4 | 0.4 | MDM2 inhibitor |
Tak-733 | 0.4 | 0.4 | MEK inhibitor |
Auranofin | 0.4 | ns | Gold complex |