Catalog No.: PC-20593Not For Human Use, Lab Use Only.
Tagarafdeg (CFT1946, CFT-1946) is a potent, selective CRBN-based PROTAC degrader of mutant BRAF, selectively degrades BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations and the p61-BRAFV600E splice variant, but not WT BRAF and CRAF.
Tagarafdeg (CFT1946, CFT-1946) is a potent, selective CRBN-based PROTAC degrader of mutant BRAF, selectively degrades BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations and the p61-BRAFV600E splice variant, but not WT BRAF and CRAF.
CFT1946 potently degraded BRAFV600E in A375 cells (DC50=14 nM at 24hr), inhibited ERK phosphorylation (IC50=11nM at 24hr) and cell growth (GI50=94nM at 96hr) while having no effect in the mutant KRAS driven cell line HCT116.
CFT1946 (10 mg/kg PO BID) resulted in deeper tumor regressions in A375 xenografts.
CFT1946 degraded BRAFV600E and caused robust tumor growth inhibition in engineered A375-BRAFV600E/NRASQ61K double mutant model of BRAF inhibitor resistance, caused tumor regressions when combined with the MEK inhibitor, trametinib.
CFT1946, but not Encorafenib (Cat. PC-49770), inhibited proliferation of the BRAFG466V heterozygous lung tumor cell line H1666.
