Chemical Name : PLX-4032(RG7204)/PLX4032
CAS : 1029872-54-5
Synonyms: N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
Solubility:DMSO
Storage:at -20℃ 2 years
Biologieal
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 (60–450 nM), whereas BRAF wild-type cells were resistant, with IC50 2.4 μM or above. [3]
Reference
[1] Elisa Sala1 et al. Mol Cancer Res. 2008 May; 6(5):751-9
[2] http://www.medicalnewstoday.com/articles/152309.php
[3] Ruth Halaban et al. Pigment Cell Melanoma Res. 2010 April; 23(2): 190-200