产品
编 号:F309576
分子式:C25H27N5O5
分子量:477.51
产品类型
结构图
CAS No: 297730-17-7
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产品详情
生物活性:
AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.
体内研究:
AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice.Animal Model:Balb/c mice (leukemia model, using Ba/F3 cells transduced with an activating human Flt-3 mutation injected into mice)
Dosage:75 or 150 mg/kg
Administration:Orally, twice daily
Result:Provided a significant increase in median survival time. Three of the 12 mice treated with 150 mg/kg AVN-944 were still alive on Day 35 when the study was terminated.
体外研究:
AVN-944 (0-1 μM, 48 h) inhibits growth of human multiple myeloma (MM) cell lines in a dose-dependent manner.AVN-944 (800?nM, 0-72?h) induces apoptosis in MM cell lines via a caspase-independent, Bax/AIF/Endo G pathway.AVN-944 (0-200 nM) enhances the cytotoxicity of Doxorubicin (HY-15142A) and Melphalan (HY-17575).AVN-944 inhibits the proliferation of the human MV-4-11 and murine Ba/F3-Flt3-ITD-dependent cell lines with IC50 values of 26 and 30 nM, respectively. AVN-944 (0-32 μM, 48?h) shows good activity against arenavirus infection at low doses (7.5?μM) with less cytotoxicity.AVN-944 (0-6.4 μM, 48 h) does not reduce the viability of peripheral blood mononuclear cells (PBMNCs).