Pivanex
(Synonyms: AN-9; Pivalyloxymethyl butyrate) 目录号 : GC68474Pivanex (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
Cas No.:122110-53-6
Sample solution is provided at 25 µL, 10mM.
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.
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 |
General tips | 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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