Catalog No.: PC-63557Not For Human Use, Lab Use Only.
BI 882370 (BI882370, BI-882370) is a highly potent, selective, orally active pan-RAF inhibitor with IC50 of 0.4, 0.8 and 0.6 nM for BRAF V600E, BRAF WT and CRAF, respectively.
BI 882370 (BI882370, BI-882370) is a highly potent, selective, orally active pan-RAF inhibitor with IC50 of 0.4, 0.8 and 0.6 nM for BRAF V600E, BRAF WT and CRAF, respectively.
BI 882370 demonstrates excellent selectivity (>100-fold) against a panel of 253 kinases (The most sensitive kinase CSF1R IC50=39 nM).
BI 882370 binds to the DFG-out (inactive) conformation of the BRAF kinase, unlike vemurafenib and dabrafenib.
BI 882370 reduces p-MEK1/2 and p-ERK1/2 signals in BRAFV600E mutation A375 cells (EC50=0.3 nM), inhibits cell proliferation of a panel BRAF-mutant human melanoma and colorectal cancer cell lines (EC50=1-10 nM).
BI 882370 demonstrates in vivo anti-cancer activity against human melanoma xenografts in nude mice.
