Remarks: PLX4032 is a highly selective inhibitor of BRAF kinase activity, with an IC50 of 44 nmol/L against V600E-mutant BRAF. [1] BRAFV600E cancer-causing mutation occurs in most melanomas and about eight percent of all solid tumors. [2]
BRAF mutant melanoma cell strains were highly sensitive to PLX4032 with IC50 in the nM range (60¨C450 nM), whereas BRAF wild-type cells were resistant, with IC50 2.4 ¦ÌM or above.
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