Panobinostat-LBH589-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPanobinostatCat. No.: HY-10224CAS No.: 404950-80-7Synonyms: LBH589; NVP-LBH589分式: CHNO分量: 349.43作靶点: HDAC; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C

2、 1 month溶解性数据体外实验 DMSO : 57 mg/mL (163.12 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8618 mL 14.3090 mL 28.6180 mL5 mM 0.5724 mL 2.8618 mL 5.7236 mL10 mM 0.2862 mL 1.4309 mL 2.8618 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。体内实验请根据您的实验动物和给药式选择适

3、当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清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 (7.15 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 (7.15 mM); Clear so

4、lution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.15 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Panobinostat种选择性组蛋去酰化酶 (HDAC) 抑制剂。IC50 & Target HDAC体外研究 Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and

5、dose-dependentmanner. Panobinosta treatment results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells 1. Panobinostat exhibites potent antiproliferative activity in human NSCLCcell lines with the IC50 ranging from 5 to 100 nM 2.体内研究 Panobinosta (10,

6、20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivomodels. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvestfrom SCID mice 2. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumorbur

7、den, significantly improves TTE and reduces bone density loss in a disseminated multiple myelomamouse model 3.PROTOCOLCell Assay 1 Cells are washed with ice-cold PBS containing 0.1 mM sodium orthovanadate, and total proteins are isolatedusing RIPA lysis buffer, which includes protease inhibitors (le

8、upeptin, antipain, and aprotinin), 0.5 mM PMSF,and 0.2 mM sodium orthovanadate. Protein amounts are quantified using the Bio-Rad protein assay. Equalamounts of proteins are loaded onto an sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) gel, transferred onto nitrocellulose membra

9、ne, and probed with the antibody of interest: mousemonoclonal c-Myc and mouse monoclonal p21 antibodies; rabbit polyclonal phospho-Histone H2A.X, rabbitpolyclonal acetyl-Histone H3 (Lys9), and rabbit polyclonal acetyl-Histone H4 (Lys8) antibodies; mousemonoclonal p27/KIP1 antibody; mouse monoclonal

10、anti-actin; and mouse monoclonal anti-GADD45G.Membranes are then washed, reprobed with appropriate horseradish peroxidase-conjugated secondaryantibodies, and developed with SuperSignal chemiluminescent substrate.MCE has not independently confirmed the accuracy of these methods. They are for referenc

11、e only.Animal AE17 and TC-1 cancer cells (1106 cells) are injected into the flanks of adult female C57Bl/6 mice andAdministration 1 severe combined immunodeficiency (SCID) mice. M30 (10106 cells), A549 (5106 cells), H69 (2.5106cells), BK-T (6.5106), H526 (10106), and RG1 (10106) cells are also injec

12、ted, but in the presence ofmatrigel, into the flanks of SCID mice. When tumors reach 100 to 500 mm3, panobinostat is administered viai.p. injections (10-20 mg/kg) on a daily schedule (5-days-on, 2-days-off regimen) for the entire duration of theexperiment. Control micereceive i.p. injections with de

13、xtrose 5% in water. Every tumor is measured with acaliper at least twice weekly. For evaluation of the effects of combination therapy on SCLC-derived tumors,SCID mice with H69 tumors are administered panobinostat. Three days after the initiation of panobinostat,2/3 Master of Small Molecules 您边的抑制剂师w

14、ww.MedChemEand again 1 wk later, etoposide (40 mg/kg) is administered i.p.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cancer Res. 2016 Dec 1;76(23):7001-7011. PLoS Pathog. 2018 Sep 13;14(9):e1007267. Mol Ther Oncolytics. 2019 Feb 5;12:23

15、5-245. Drug Des Devel Ther. 2018 Apr 30;12:1009-1017. Insect Mol Biol. 2019 Aug 7.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis inPh- acute lymphobla

16、stic leukemia cells. Blood. 2008 May 15;111(10):5093-100.2. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo withparticular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31.3. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with eitherbortezomib or lenalidomide in multiple