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. 2014 Jun 5;5(6):e1278. doi: 10.1038/cddis.2014.241

Table 1. The inhibitory activity of the compounds against RIP3 and Rafs.

Compounds IC50 for RIP3 (μM)
IC50 for Rafs (nM)
  Luminescent assaysa Radioactive assaysa B-Raf B-RafV600E C-Raf Refsb
Dabrafenib 0.25±0.16 0.002 3.2 0.8 5.0 35
AZ628 0.90±0.15 4.48 100 34 29 36
Regorafenib 2.56±1.02 0.95 28 19 c 37
PLX4720 4.72±2.25 1.52 13 38
Vemurafenib 6.73±3.72 14.30 100 31 48 39
Sorafenib 14.52±0.51 NAd 22 40
GDC-0879 NA ND 0.13 41
SB590885 NA ND 0.16 1.72 42
SU11248 NA ND  
Necrostatin-1 NA NA  

Abbreviations: NA, not applicable; ND, not determined; RIP, receptor-interacting protein

a

IC50 values from luminescent assays were presented as mean±S.D. from three independent experiments in our laboratory, whereas the IC50 values from radioactive assays were presented as the mean of two independent experiments performed by the Reaction Biology Corporation

b

References (refs) reporting the IC50 values of Rafs inhibition by the corresponding compounds

c

No data reported

d

No IC50 available at the tested conditions