Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates Bcr-Abl protein and enhances Apoptosis. Pivanex has antimetastic and antiangiogenic properties[1].
Pivanex (100-500 μM) exhibits significant anti-proliferation activity in K562 cells[1].
Pivanex (100-500 μM) also enhances apoptosis and caspase activity in K562 cells[1].
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[1].
Pivanex (AN-9) has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines[2].
Cell Viability Assay[1]
| 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[1]
| 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 (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[3].
| Animal Model: | SMN7 SMA mice (SMN2+/+; SMN7+/+; mSmn-/-)[3]. |
| 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%. |
[1]. Rabizadeh E, et al. Pivanex, a histone deacetylase inhibitor, induces changes in BCR-ABL expression and when combined with STI571, acts synergistically in a chronic myelocytic leukemia cell line. Leuk Res. 2007 Aug;31(8):1115-23. Epub 2007 Jan 30.
[2]. Batova A, et al. The histone deacetylase inhibitor AN-9 has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines. Blood. 2002 Nov 1;100(9):3319-24.
[3]. Edwards JD, et al. Effect of the Butyrate Prodrug Pivaloyloxymethyl Butyrate (AN9) on a Mouse Model for Spinal Muscular Atrophy. J Neuromuscul Dis. 2016 Nov 29;3(4):511-515.