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Panobinostat

Catalog No. T2383 CAS 404950-80-7

Synonyms: NVP-LBH589, LBH589

Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.

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Panobinostat, CAS 404950-80-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 52.00
25 mg	In stock	$ 79.00
50 mg	In stock	$ 107.00
100 mg	In stock	$ 147.00
200 mg	In stock	$ 187.00
500 mg	In stock	$ 383.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.14%

Purity: 99.01%

Purity: 97.2%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.
Targets&IC50	HDAC (MOLT-4 cells):5 nM, HDAC (Reh cells):20 nM
In vitro	METHODS: Thirty-seven lung cancer cell lines were treated with Panobinostat (0-800 nmol/L) for 48-72 h, and cell viability was measured using the MTT. RESULTS: Panobinostat showed potent antiproliferative activity and cytotoxicity against human and mouse lung cancer cell lines. [1] METHODS: Human ALL cells MOLT-4 and Reh were treated with Panobinostat (10-100 nM) for 24-72 h. Apoptosis was detected by Flow Cytometry. RESULTS: Panobinostat induced apoptosis in MOLT-4 and Reh cells in a time- and dose-dependent manner. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, Panobinostat (20 mg/kg) was intraperitoneally injected five times per week for two weeks into SCID mice bearing human SCLC tumors H526, BKT, RG1, or H69. RESULTS: Panobinostat significantly slowed down the in vivo growth of tumors derived from SCLC cells and induced remission. [1] METHODS: To investigate the potential for enhanced recovery of motor function after stroke, Panobinostat (3-10 mg/kg) was administered intraperitoneally to CD-1 mice with stroke every two days for ten days. RESULTS: Neither physical exercise nor the combination of Panobinostat substantially affected motor recovery in mice after stroke.Panobinostat treatment coupled with limited physical rehabilitation is unlikely to provide a therapeutic modality for stroke survivors with motor dysfunction. [3]
Cell Research	Blasts from peripheral blood of 2 patients and from bone marrow of 4 patients were isolated with Ficoll-Hypaque, put in culture at a density of 500?000 cells/mL with RPMI-1640 medium containing 10% fetal bovine serum and 50 units/mL penicillin and streptomycin, and treated with different doses of LBH589 (0-100 μM) for up to 48 hours [1].
Animal Research	AE17 and TC-1 cancer cells (1 × 10^6 cells) were injected into the flanks of adult female C57Bl/6 mice and severe combined immunodeficiency (SCID) mice. M30 (10 × 10^6 cells), A549 (5 × 10^6 cells), H69 (2.5 × 10^6 cells), BK-T (6.5 × 10^6), H526 (10 × 10^6), and RG1 (10 × 10^6) cells were also injected, but in the presence of matrigel (BD Biosciences), into the flanks of SCID mice. There were 5 to 10 mice in each treatment group. The experiments with the A549 and H69 cell lines were repeated to ensure the statistical consistency of the results. Experiments were terminated when the tumors in the control mice had grown to a size that threatened the quality of life of the mice. When tumors reached 100 to 500 mm3, panobinostat was 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 mice received i.p. injections with dextrose 5% in water ("vehicle treatment"). Every tumor was 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 were administered panobinostat as described above. Three days after the initiation of panobinostat, and again 1 wk later, etoposide (40 mg/kg) was administered i.p [3].

Synonyms	NVP-LBH589, LBH589
Molecular Weight	349.43
Formula	C21H23N3O2
CAS No.	404950-80-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 64 mg/mL (183.2 mM)

References and Literature

1. 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. 2. 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. 3. Al Shoyaib A, et al. The Effect of Histone Deacetylase Inhibitors Panobinostat or Entinostat on Motor Recovery in Mice After Ischemic Stroke. Neuromolecular Med. 2021 Dec;23(4):471-484. 4. 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. 5. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity[J]. bioRxiv. 2021 6. Juarez-Mercado K E, Prieto-Martinez F D, Sanchez-Cruz N, et al. DNA Methyltransferase Inhibitors with Novel Chemical Scaffolds[J]. bioRxiv. 2020 7. Juárez-Mercado K E, Prieto-Martínez F D, Sánchez-Cruz N, et al. Expanding the Structural Diversity of DNA Methyltransferase Inhibitors[J]. Pharmaceuticals. 2021, 14(1): 17.

Citations

1. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity. Cancer Immunology Research. 2022, 10(1): 87-107. 2. Wellinger L C, Hogg S J, Newman D M, et al. Bet inhibition enhances TNF-mediated antitumor immunity. Cancer Immunology Research. 2022, 10(1): 87-107 3. Juárez-Mercado K E, Prieto-Martínez F D, Sánchez-Cruz N, et al. Expanding the Structural Diversity of DNA Methyltransferase Inhibitors. Pharmaceuticals. 2021, 14(1): 17. 4. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 5. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library FDA-Approved & Pharmacopeia Drug Library Covalent Inhibitor Library Histone Modification Compound Library

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Keywords

Panobinostat 404950-80-7 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Proteases/Proteasome HIV Protease HDAC Human immunodeficiency virus Histone deacetylases NVP-LBH 589 HIV inhibit Inhibitor NVP-LBH589 LBH-589 LBH589 NVP-LBH-589 LBH 589 inhibitor

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