Raptinal showed complete cytochrome c release within 30 minutes and caspase-3 activation within one hour of exposure (10 µM). Despite its general cytotoxicity in both cancer and non-cancer cell cultures (Cell death induction EC50?= 0.6-3.4 µM in 24 hr), no hematologic toxicity was observed 7 days following single 60 mg/kg i.v. dosing in mice. Studies show that daily i.p. injection (20 mg/kg) is efficacious in suppressing murine B16-F10 melanoma and 4T1 breast cancer expansion in vivo (by ~60% and 50% in 6 days, respectively).
Biochem/physiol Actions
Raptinal is a cell-permeable bifluorene-dicarbaldehyde compound that acts as a rapid activator of mitochondrial pathway-mediated intrinsic apoptosis.