Table 1.

b-AP15 has a potent anti-melanoma effect irrespective of mutational status, gene expression signatures, and acquired drug resistance

b-AP15
TypeMutation(s)ResistanceIC50 (μmol/L)
Cell line
 SBCL2RGPBRAFaNone0.4
 WM793VGPBRAFV600E/PTENaNone0.3
 WM164METBRAFV600E/CDKN2AaNone0.9
 WM266–4METBRAFV600D/PTENaNone0.5
 MeWoMETTP53a/CDKN2Aa/NF1aNone0.7
 HMVIIMETNRASaNone1.8
 501MelMETBRAFV600ENone0.5
 1205luMETBRAFV600E/PTENaNone0.3
 451luMETBRAFV600E/TP53aNone0.9
 451luRMETBRAFV600E/TP53a/?Dabrafenib1.3
 M229METBRAFV600E/PTENaNone0.9
 M229RMETBRAFV600E/PTENa/RTKaVemurafenib0.9
 M238METBRAFV600E/PTENaNone1.6
 M238RMETBRAFV600E/PTENa/RTKaVemurafenib0.4
 M249METBRAFV600E/PTENaNone2.0
 M249RMETBRAFV600E/PTENa/NRASaVemurafenib3.0
 Mel1617METBRAFa/TP53aNone1.4
 Mel1617RMETBRAFa/TP53a/?Vemurafenib0.9
 A375METBRAFV600E/CDKN2AaNone0.6
 A375DRMETBRAFV600E/CDKN2Aa/?Vemurafenib/ERKi1.3
Short-term cultures
 Pt#1MET?None3.4
 Pt#2MET?None1.7
  • NOTE: IC50 (μmol/L) of b-AP15 treatment on melanoma cell proliferation was determined after 48 hours by a MTS conversion assay.

  • Abbreviations: MET, metastasis; RGP, radial growth phase; RTK, receptor tyrosine kinase; VGP, vertical growth phase.

  • aGene mutation or alteration.