YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.IC50 & Target: IC50: 1.5 μM (glucose-regulated protein 78)In Vitro: YUM70 shows selective cytotoxicity for MIA PaCa-2, PANC-1, BxPC-3 cells (IC50=2.8, 4.5, and 9.6 μM, respectively) over normal pancreatic tissue-derived HPNE cells (IC50>30 μM).
YUM70 (5 μM; 24 h) induces endoplasmic reticulum (ER) stress-mediated apoptosis of MIA PaCa-2cells.In Vivo: YUM70 (30 mg/kg; i.p. 5 days a week for 7 weeks) inhibits tumor growth in a MIA PaCa-2 xenograft model.
YUM70 (15 mg/kg; i.v.) exhibits t1/2 (1.40 h), CL (724.04 mL/h/kg), and Vss (1162.73 mL/kg) in mice.
YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t1/2 (2.74 h), and CL (9230.15 mL/h/kg) in mice.