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Pivanex

(Synonyms: AN-9; Pivalyloxymethyl butyrate) 目录号 : GC68474

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

Pivanex Chemical Structure

Cas No.:122110-53-6

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10mg
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100mg
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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

Cas No. 122110-53-6 SDF Download SDF
别名 AN-9; Pivalyloxymethyl butyrate
分子式 C10H18O4 分子量 202.25
溶解度 DMSO : ≥ 100 mg/mL (494.44 mM) 储存条件 Store at -20°C
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1 mM 4.9444 mL 24.7219 mL 49.4438 mL
5 mM 0.9889 mL 4.9444 mL 9.8888 mL
10 mM 0.4944 mL 2.4722 mL 4.9444 mL
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