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
| 生物活性 | Pivanex (AN-9), a derivative of Butyric acid, is an orally activeHDACinhibitor. Pivanex down-regulatesbcr-ablprotein and enhancesapoptosis. Pivanex has antimetastic and antiangiogenic properties[1]. |
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体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | 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%.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(494.44 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.36 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.36 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (12.36 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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