Panobinostat (LBH589; NVP-LBH589) est un inhibiteur HDAC puissant et oralement non sélectif, et possède des activités antinéoplasiques. Panobinostat induit la production du virus VIH-1 même à une faible concentration de 8 à 31 nM, stimule l'expression du VIH-1 dans les cellules infectées de manière latente. Panobinostat induit l'apoptose et l'autophagie des cellules. Panobinostat peut être utilisé pour l'étude du myélome multiple réfractaire ou en rechute.
Panobinostat (LBH589; NVP-LBH589) ist ein potenter und oral wirksamer, nicht-selektiver HDAC-Inhibitor mit antineoplastischen Aktivitäten. Panobinostat induziert die Produktion des HIV-1 virus selbst im niedrigen Konzentrationsbereich von 8-31 nM und stimuliert die HIV-1-Expression in latent infizierten Zellen. Panobinostat induziert apoptosis und autophagy. Panobinostat kann für die Untersuchung von refraktären oder rezidivierten Multiplen Myelomen verwendet werden.
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.
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Panobinostat Estructura química
No. CAS : 404950-80-7
This product is a controlled substance and not for sale in your territory.
Based on 54 publication(s) in Google Scholar
Other Forms of Panobinostat:
Panobinostat lactate
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Panobinostat-d4
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Panobinostat-d4 hydrochloride
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Panobinostat purchased from MedChemExpress. Usage Cited in:
J Exp Clin Cancer Res. 2022 Nov 11;41(1):321.
[Abstract]
The expression of BRD4 and MYC proteins are each downregulated by JQ1 (0.5 µM; 24 h) or panobinostat (PAN; 10 nM; 24 h) alone, and more profoundly by the combination of these two inhibitors in in MB HD-MB03 and D-283 cells.
Immunoblot analysis for vIL-6, ORF45, or actin is performed on lysates from BCBL-1 cells treated with NaB+TPA, Romidepsin or Panobinostat.
Panobinostat purchased from MedChemExpress. Usage Cited in:
China Biotechnology. 2016, 36(6): 9-17.
The HDAC expression of PC3 cell with different concentration of Panobinostat. (a) HDACs mRNA expression is analyzed by real time PCR (b) HDACs protein expression is analyzed by Western blot.
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Descripciòn
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
IC50 & Target[1][5]
HDAC
HIV-1
In Vitro
Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. 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 NSCLC cell lines with the IC50 ranging from 5 to 100 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Panobinostat Related Antibodies
In Vivo
Panobinosta (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice[2]. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular
349.43
Fòrmula
C21H23N3O2
No. CAS
404950-80-7
Appearance
Solid
Color
Off-white to light yellow
SMILES
O=C(/C=C/C1=CC=C(CNCCC2=C(NC3=C2C=CC=C3)C)C=C1)NO
Envío
Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (286.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.8618 mL
14.3090 mL
28.6180 mL
5 mM
0.5724 mL
2.8618 mL
5.7236 mL
10 mM
0.2862 mL
1.4309 mL
2.8618 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
Protocol 4
Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution
Protocol 5
Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.15 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100.
[Content Brief]
[2]. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31.
[Content Brief]
[3]. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803.
[Content Brief]
[4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147.
[Content Brief]
[5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8.
[Content Brief]
Ensayo celular
[1]
Cells are washed with ice-cold PBS containing 0.1 mM sodium orthovanadate, and total proteins are isolated using RIPA lysis buffer, which includes protease inhibitors (leupeptin, antipain, and aprotinin), 0.5 mM PMSF, and 0.2 mM sodium orthovanadate. Protein amounts are quantified using the Bio-Rad protein assay. Equal amounts of proteins are loaded onto an sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) gel, transferred onto nitrocellulose membrane, and probed with the antibody of interest: mouse monoclonal c-Myc and mouse monoclonal p21 antibodies; rabbit polyclonal phospho-Histone H2A.X, rabbit polyclonal acetyl-Histone H3 (Lys9), and rabbit polyclonal acetyl-Histone H4 (Lys8) antibodies; mouse monoclonal p27/KIP1 antibody; mouse monoclonal anti-β-actin; and mouse monoclonal anti-GADD45G. Membranes are then washed, reprobed with appropriate horseradish peroxidase-conjugated secondary antibodies, and developed with SuperSignal chemiluminescent substrate.
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales
[1]
AE17 and TC-1 cancer cells (1×106 cells) are injected into the flanks of adult female C57Bl/6 mice and severe combined immunodeficiency (SCID) mice. M30 (10×106 cells), A549 (5×106 cells), H69 (2.5×106 cells), BK-T (6.5×106), H526 (10×106), and RG1 (10×106) cells are also injected, but in the presence of matrigel, into the flanks of SCID mice. When tumors reach 100 to 500 mm3, panobinostat is administered via i.p. injections (10-20 mg/kg) on a daily schedule (5-days-on, 2-days-off regimen) for the entire duration of the experiment. Control micereceive i.p. injections with dextrose 5% in water. Every tumor is measured with a caliper 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, and again 1 wk later, etoposide (40 mg/kg) is administered i.p.
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias
[1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100.
[Content Brief]
[2]. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31.
[Content Brief]
[3]. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803.
[Content Brief]
[4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147.
[Content Brief]
[5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8.
[Content Brief]
[1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic 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 with particular 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 either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803.
[4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147.
[5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.8618 mL
14.3090 mL
28.6180 mL
71.5451 mL
5 mM
0.5724 mL
2.8618 mL
5.7236 mL
14.3090 mL
10 mM
0.2862 mL
1.4309 mL
2.8618 mL
7.1545 mL
15 mM
0.1908 mL
0.9539 mL
1.9079 mL
4.7697 mL
20 mM
0.1431 mL
0.7155 mL
1.4309 mL
3.5773 mL
25 mM
0.1145 mL
0.5724 mL
1.1447 mL
2.8618 mL
30 mM
0.0954 mL
0.4770 mL
0.9539 mL
2.3848 mL
40 mM
0.0715 mL
0.3577 mL
0.7155 mL
1.7886 mL
50 mM
0.0572 mL
0.2862 mL
0.5724 mL
1.4309 mL
60 mM
0.0477 mL
0.2385 mL
0.4770 mL
1.1924 mL
80 mM
0.0358 mL
0.1789 mL
0.3577 mL
0.8943 mL
100 mM
0.0286 mL
0.1431 mL
0.2862 mL
0.7155 mL
Panobinostat Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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