Berubicin (hydrochloride)

Berubicin (RTA 744) hydrochloride is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin hydrochloride inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin hydrochloride exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin hydrochloride can be used in the study of tumors related to the nervous system^{[1][2][3][4][5]}. In Vitro:Berubicin (0.1-10 μM, 0-5 d) hydrochloride is more effective than Doxorubicin (Dox) in inhibiting SH-SY5Y cell growth^[2].
Berubicin (0-10 μM, 0-48 h) hydrochloride induces apoptosis at the lower drug concentrations through caspase-9 and -3-dependent pathways and activating NF-κB, while other mechanisms of cell death may predominate at higher concentrations in SH-SY5Y cells^[2].
Berubicin (0-100 μM, 24 h) hydrochloride inhibits three AML cell lines K562, KBM-3, OCIM2 and KBM-5 cells with IC₅₀s of 0.18, < 0.05, < 0.05 μg/mL and 0.5 μM, and induces cell apoptosis in cultured human acute lymphoblastic leukemia (ALL) CEM cells at 0.05 μM^[3][4].
Berubicin (0-10 μM, 0-8 h) hydrochloride is more active than Dox in inhibiting DNA synthesis (IC₅₀ = 0.2 μM), activating NF-κB and degradation of IkBα of KBM-5 cells^[4].
In Vivo:Berubicin hydrochloride prolongs the survival time of intracranial orthotopic glioma models in mice compared to Temozolomide (HY-17364)^[5].