Pivanex-AN-9-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPivanexCat. No.: HY-120508CAS No.: 122110-53-6Synonyms: AN-9; Pivalyloxymethyl butyrate分式: CHO分量: 202.25作靶点: HDAC; Apoptosis作通路: Cell Cycle/DNA Damage; Epigenetics; Apoptosis储存式: Please store the product under the recommended co

2、nditions inthe COA.溶解性数据体外实验 DMSO : 100 mg/mL (494.44 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.9444 mL 24.7219 mL 49.4438 mL5 mM 0.9889 mL 4.9444 mL 9.8888 mL10 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，并请注意储备液的保存式和期限。体内实验 请根据

3、您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (12.36 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (12.36 m

4、M); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (12.36 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Pivanex (AN-9)丁酸的衍物，HDAC 的抑制剂，具有抗转移和抗管成的活性。Pivanex (AN-9) 可下调bcr-abl 蛋，增强凋亡。体外研究 Pivanex (100-500 M) exhibits significant anti-

5、proliferation activity in K562 cells 1.Pivanex (100-500 M) also enhances apoptosis and caspase activity in K562 cells 1.Pivanex (200 M) induces enhancement in the G2-M phase, a moderate enhancement in the S phase and aslight reduction in G0-G1 of the cell cycle 1.Pivanex (AN-9) has selective toxicit

6、y to acute leukemia and drug-resistant primary leukemia and cancer celllines 2.Cell Viability Assay 1Cell Line: K562 cells.Concentration: 100-500 M.Incubation Time: 24 hours.Result: Reduced the number of K562 viable cells significantly.100 M Pivanex with 0.125 or 0.25 M STI571 reduced the number of

7、viable cellssynergistically.Apoptosis Analysis 1Cell Line: K562 cells.Concentration: 100-500 M.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 with500 M.体内研究Pivanex

8、(AN9, 200 mg/kg, b.i.d, daily) significantly improves the survival of SMN7 SMA mice. AN9 treatmentalso 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

9、.d, at 09.00 and 17.00 daily.Result: Improved the mean lifespan of treated SMN7 SMA mice by 84.6%.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEDelayed the onset of body mass loss in SMN7 SMA mice by 94.9%.REFERENCES1. Rabizadeh E, et al. Pivanex, a histone deacetylase inhibitor, induces changes

10、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 andcancer 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. JNeuromuscul Dis. 2016 Nov 29;3(4):511-515.McePdfHeightCaution: Product has not bee