HDAC Bcr-Abl

Pivanex (AN9, 200 mg/kg, b.i.d, daily) significantly improves the survival of SMN7 SMA mice. Pivanex (AN9) treatment also marked delays the end stage of disease as defined by the onset of body mass loss. Animal Model: SMN7 SMA mice (SMN2 +/+ ; SMN7 +/+ ; mSmn −/− ). Dosage: 200 mg/kg. Administration: Oral administration, b.i.d, at 09.00 and 17.00 daily. Result: Improved the mean lifespan of treated SMN7 SMA mice by 84.6%. Delayed the onset of body mass loss in SMN7 SMA mice by 94.9%.

Pivanex (100-500 μM) exhibits significant anti-proliferation activity in K562 cells. Pivanex (100-500 μM) also enhances apoptosis and caspase activity in K562 cells. Pivanex (200 μM) induces enhancement in the G2-M phase, a moderate enhancement in the S phase and a slight reduction in G0-G1 of the cell cycle. Pivanex (AN-9) has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines. Cell Viability Assay Cell Line: K562 cells. Concentration: 100-500 μM. Incubation Time: 24 hours. Result: Reduced the number of K562 viable cells significantly. 100 μM Pivanex with 0.125 or 0.25 μM STI571 reduced the number of viable cells synergistically. Apoptosis Analysis Cell Line: K562 cells. Concentration: 100-500 μM. Incubation Time: 6-72 hours. Result: Increased the number of K562 apoptotic cells significantly. Increased the caspase activity in K562 cells significantly after only 4 h of incubation with 500 μM.

Pivanex (AN-9) 是丁酸的衍生物，是口服有效的 HDAC 抑制剂。Pivanex 可下调 bcr-abl 蛋白，增强凋亡 (apoptosis)。Pivanex 具有抗转移和抗血管生成的活性