AVN-944 (also known as VX-944) is an orally active, potent, selective, noncompetitive, and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). IMPDH is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. Additionally, AVN-944 acts as an inhibitor of arenavirus RNA synthesis, blocking arenavirus infection. It exhibits broad anti-cancer activities and is applicable to research on multiple myeloma (MM) and acute myeloid leukemia (AML) [1][2][3].
体内研究
AVN-944 (Orally, at doses ranging from 0 to 150 mg/kg, twice daily) significantly prolongs the median survival time of leukemia model mice [2].
体外研究
AVN-944 inhibits the growth of human multiple myeloma (MM) cell lines in a dose-dependent manner, with concentrations ranging from 0 to 1 μM, in a 48-hour period[1].
AVN-944 (800 nM, 0-72 h) triggers apoptosis in MM cell lines via a caspase-independent pathway involving Bax/AIF/Endo G [1].
AVN-944 (0-200 nM) potentiates the cytotoxic effects of Doxorubicin and Melphalan [1].
AVN-944 suppresses the proliferation of human MV-4-11 and murine Ba/F3-Flt3-ITD-dependent cell lines, with IC50 values of 26 and 30 nM, respectively [2].
AVN-944 (0-32 μM, 48 h) exhibits potent activity against arenavirus infection at low doses (7.5 μM) with minimal cytotoxicity [3].
AVN-944 (0-6.4 μM, 48 h) does not affect the viability of peripheral blood mononuclear cells (PBMNCs) [1].
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