PROTAC B-Raf degrader 1

2364367-27-9

763.77

DMSO : 25 mg/mL (32.73 mM; Need ultrasonic)

MAPK/ERK Pathway; PROTAC

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf. With anti-cancer activity^[1]. IC50 & Target: B-Raf^[1]. In Vitro: The IC₅₀ values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 uM, 21.21 uM, 18.70 uM, 41.11uM and 22.68 uM, respectively^[1].
PROTAC B-Raf degrader 1 (5 or 10 uM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf^[1].
MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 uM^[1].
PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase^[1].