HM90822

HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer^[1]. In Vitro:HM90822 (72 h) induces dose-dependent cell death in human pancreatic cancer cell lines, with IC₅₀ values of 0.142 μM (BxPC-3), 0.164 μM (Panc03.27), 0.324 μM (Panc-1), 5.3 μM (PL45), and 6.7 μM (Capan-1) after 72 h incubation, while Panc08.13, MiaPaCa-2, Capan-2, and AsPC-1 cells are resistant with IC₅₀ values above 37 μM^[1].
HM90822 (0.3-10 μM; 18 h) induces dose-dependent reduction of XIAP and cIAP1 protein expression in sensitive BxPC-3 and Panc-1 human pancreatic cancer cell lines after 18 h incubation, but has no effect on these proteins in resistant MiaPaCa-2 and Capan-2 cells^[1]. In Vivo:HM90822 (150 mg/kg; p.o.; daily; 14 days) reduces the volume of subcutaneous Panc-1 xenografts in female Balb/c nude mice without altering their body weight^[1].
HM90822 (50-200 mg/kg; p.o.; once daily; for 14 consecutive days) exerts anti-tumor effects in female Balb/c nude mice with Panc-1 orthotopic xenografts^[1].