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. 2019 May;16(2):234–246. doi: 10.20892/j.issn.2095-3941.2018.0284

1.

Fifteen radiosensitisers identified for BRAF-mutant cells

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