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MedKoo Cat#: 202151 | Name: Panobinostat
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Panobinostat, also known as NVP LBH-589 or LBH-589, is a cinnamic hydroxamic acid analogue with potential antineoplastic activity. Panobinostat selectively inhibits histone deacetylase (HDAC), inducing hyperacetylation of core histone proteins, which may result in modulation of cell cycle protein expression, cell cycle arrest in the G2/M phase and apoptosis. In addition, this agent appears to modulate the expression of angiogenesis-related genes, such as hypoxia-inducible factor-1alpha (HIF-1a) and vascular endothelial growth factor (VEGF), thus impairing endothelial cell chemotaxis and invasion. On 2/23/2015, it received FDA accelerated approval for use in patients with multiple myeloma who had received at least 2 previous treatments, including bortezomib and an immunomodulatory agent.

Chemical Structure

Panobinostat
Panobinostat
CAS#404950-80-7 (free base)

Theoretical Analysis

MedKoo Cat#: 202151

Name: Panobinostat

CAS#: 404950-80-7 (free base)

Chemical Formula: C21H23N3O2

Exact Mass: 349.1790

Molecular Weight: 349.43

Elemental Analysis: C, 72.18; H, 6.63; N, 12.03; O, 9.16

Price and Availability

Size Price Availability Quantity
25mg USD 150.00 Ready to ship
50mg USD 250.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,650.00 Ready to ship
1g USD 2,950.00 Ready to ship
2g USD 5,250.00 Ready to ship
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Related CAS #
960055-56-5 (lactate) 404950-80-7 (free base) 960055-50-9 (acetate) 960055-60-1 (mesylate) 960055-54-3 (fumarate) 960055-57-6 (maleate)
Synonym
LBH589; LBH 589; LBH-589; NVP-LBH589; NVP-LBH 589; Panobinostat; trade name Farydak;
IUPAC/Chemical Name
(2E)-N-hydroxy-3-[4-({[2-(2-methyl-1H-indol-3-yl)ethyl]amino}methyl)phenyl]acrylamide
InChi Key
FPOHNWQLNRZRFC-ZHACJKMWSA-N
InChi Code
InChI=1S/C21H23N3O2/c1-15-18(19-4-2-3-5-20(19)23-15)12-13-22-14-17-8-6-16(7-9-17)10-11-21(25)24-26/h2-11,22-23,26H,12-14H2,1H3,(H,24,25)/b11-10+
SMILES Code
O=C(NO)/C=C/C1=CC=C(CNCCC2=C(C)NC3=C2C=CC=C3)C=C1
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Panobinostat has been found to synergistically act with sirolimus to kill pancreatic cancer cells in the laboratory in a Mayo Clinic study. In the study, investigators found that this combination destroyed up to 65 percent of cultured pancreatic tumor cells. The finding is significant because the three cell lines studies were all resistant to the effects of chemotherapy – as are many pancreatic tumors. see http://en.wikipedia.org/wiki/Panobinostat.      
Biological target:
Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay.
In vitro activity:
Two model human Ph(-) ALL cell lines (T-cell MOLT-4 and pre-B-cell Reh) were treated with LBH589 and evaluated for biologic and gene expression responses. Low nanomolar concentrations (IC(50): 5-20 nM) of LBH589 induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation. LBH589 treatment increased mRNA levels of proapoptosis, growth arrest, and DNA damage repair genes including FANCG, FOXO3A, GADD45A, GADD45B, and GADD45G. The most dramatically expressed gene (up to 45-fold induction) observed after treatment with LBH589 is GADD45G. LBH589 treatment was associated with increased histone acetylation at the GADD45G promoter and phosphorylation of histone H2A.X. Furthermore, treatment with LBH589 was active against cultured primary Ph(-) ALL cells, including those from a relapsed patient, inducing loss of cell viability (up to 70%) and induction of GADD45G mRNA expression (up to 35-fold). Thus, LBH589 possesses potent growth inhibitory activity against including Ph(-) ALL cells associated with up-regulation of genes critical for DNA damage response and growth arrest. These findings provide a rationale for exploring the clinical activity of LBH589 in the treatment of patients with Ph(-) ALL. Reference: Blood. 2008 May 15;111(10):5093-100. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/18349321/ Reference: Mol Cancer Ther. 2009 Aug;8(8):2221-31. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3605895/
In vivo activity:
In lung cancer and mesothelioma animal models, panobinostat significantly decreased tumor growth by an average of 62% when compared with vehicle control. Panobinostat was equally effective in immunocompetent and severe combined immunodeficiency mice, indicating that the inhibition of tumor growth by panobinostat was not due to direct immunologic effects. Panobinostat was, however, particularly effective in small cell lung cancer (SCLC) xenografts, and the addition of the chemotherapy agent etoposide augmented antitumor effects. Protein analysis of treated tumor biopsies revealed elevated amounts of cell cycle regulators such as p21 and proapoptosis factors, such as caspase 3 and 7 and cleaved poly[ADP-ribose] polymerase, coupled with decreased levels of antiapoptotic factors such as Bcl-2 and Bcl-X(L). These studies together suggest that panobinostat may be a useful adjunct in the treatment of thoracic malignancies, especially SCLC. Reference: Mol Cancer Ther. 2009 Aug;8(8):2221-31. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/19671764/ Reference: Retrovirology. 2016 May 21;13(1):36. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4875645/
Solvent mg/mL mM
Solubility
DMSO 33.0 94.40
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 349.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Crisanti MC, Wallace AF, Kapoor V, Vandermeers F, Dowling ML, Pereira LP, Coleman K, Campling BG, Fridlender ZG, Kao GD, Albelda SM. 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. doi: 10.1158/1535-7163.MCT-09-0138. Epub 2009 Aug 11. PMID: 19671764; PMCID: PMC3605895. 2. Scuto A, Kirschbaum M, Kowolik C, Kretzner L, Juhasz A, Atadja P, Pullarkat V, Bhatia R, Forman S, Yen Y, Jove R. 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. doi: 10.1182/blood-2007-10-117762. Epub 2008 Mar 18. PMID: 18349321; PMCID: PMC2384136. 3. Crisanti MC, Wallace AF, Kapoor V, Vandermeers F, Dowling ML, Pereira LP, Coleman K, Campling BG, Fridlender ZG, Kao GD, Albelda SM. 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. doi: 10.1158/1535-7163.MCT-09-0138. Epub 2009 Aug 11. PMID: 19671764; PMCID: PMC3605895. 4. Tsai P, Wu G, Baker CE, Thayer WO, Spagnuolo RA, Sanchez R, Barrett S, Howell B, Margolis D, Hazuda DJ, Archin NM, Garcia JV. In vivo analysis of the effect of panobinostat on cell-associated HIV RNA and DNA levels and latent HIV infection. Retrovirology. 2016 May 21;13(1):36. doi: 10.1186/s12977-016-0268-7. PMID: 27206407; PMCID: PMC4875645.
In vitro protocol:
1. Crisanti MC, Wallace AF, Kapoor V, Vandermeers F, Dowling ML, Pereira LP, Coleman K, Campling BG, Fridlender ZG, Kao GD, Albelda SM. 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. doi: 10.1158/1535-7163.MCT-09-0138. Epub 2009 Aug 11. PMID: 19671764; PMCID: PMC3605895. 2. Scuto A, Kirschbaum M, Kowolik C, Kretzner L, Juhasz A, Atadja P, Pullarkat V, Bhatia R, Forman S, Yen Y, Jove R. 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. doi: 10.1182/blood-2007-10-117762. Epub 2008 Mar 18. PMID: 18349321; PMCID: PMC2384136.
In vivo protocol:
1. Crisanti MC, Wallace AF, Kapoor V, Vandermeers F, Dowling ML, Pereira LP, Coleman K, Campling BG, Fridlender ZG, Kao GD, Albelda SM. 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. doi: 10.1158/1535-7163.MCT-09-0138. Epub 2009 Aug 11. PMID: 19671764; PMCID: PMC3605895. 2. Tsai P, Wu G, Baker CE, Thayer WO, Spagnuolo RA, Sanchez R, Barrett S, Howell B, Margolis D, Hazuda DJ, Archin NM, Garcia JV. In vivo analysis of the effect of panobinostat on cell-associated HIV RNA and DNA levels and latent HIV infection. Retrovirology. 2016 May 21;13(1):36. doi: 10.1186/s12977-016-0268-7. PMID: 27206407; PMCID: PMC4875645.
1: Zheng B, Cui D, Deng B, Long W, Ye G, Zhang S, Zeng J. Form-deprivation myopia promotes sclera M2-type macrophages polarization in mice. Biochem Biophys Res Commun. 2024 Aug 6;737:150490. doi: 10.1016/j.bbrc.2024.150490. Epub ahead of print. PMID: 39146710. 2: Ling L, Kim M, Soper A, Kovarova M, Spagnuolo RA, Begum N, Kirchherr J, Archin N, Battaglia D, Cleveland D, Wahl A, Margolis DM, Browne EP, Garcia JV. Analysis of the effect of HDAC inhibitors on the formation of the HIV reservoir. mBio. 2024 Aug 13:e0163224. doi: 10.1128/mbio.01632-24. Epub ahead of print. PMID: 39136440. 3: Bhutkar S, Yadav A, Patel H, Barot S, Patel K, Dukhande VV. Synergistic Efficacy of CDK4/6 Inhibitor Abemaciclib and HDAC Inhibitor Panobinostat in Pancreatic Cancer Cells. Cancers (Basel). 2024 Jul 30;16(15):2713. doi: 10.3390/cancers16152713. PMID: 39123441; PMCID: PMC11311278. 4: Lopes N, Salta S, Flores BT, Miranda-Gonçalves V, Correia MP, Gigliano D, Guimarães R, Henrique R, Jerónimo C. Anti-tumour activity of Panobinostat in oesophageal adenocarcinoma and squamous cell carcinoma cell lines. Clin Epigenetics. 2024 Aug 3;16(1):102. doi: 10.1186/s13148-024-01700-3. PMID: 39097736; PMCID: PMC11297794. 5: Yavari S, Naseroleslami M, Peymani M, Yekani F, Khayam Nekouei N. Investigation of SPOCD1 as A Suitable Diagnostic and Prognostic Biomarker in Various Common Cancer Types: Bioinformatics and Practical Analysis. Cell J. 2024 Jul 13;26(5):309-319. doi: 10.22074/cellj.2024.2022401.1506. PMID: 39066595. 6: Alrasheed MA, Alamer KA, Albishi M, Alsuhibani AA, Almohammed OA, Alwhaibi A, Almajed AN, Guo JJ. Descriptive Analysis of Adverse Events Reported for New Multiple Myeloma Medications Using FDA Adverse Event Reporting System (FAERS) Databases from 2015 to 2022. Pharmaceuticals (Basel). 2024 Jun 21;17(7):815. doi: 10.3390/ph17070815. PMID: 39065666; PMCID: PMC11279559. 7: Chen HO, Cui YC, Lin PC, Chiang JH. An Innovative Multi-Omics Model Integrating Latent Alignment and Attention Mechanism for Drug Response Prediction. J Pers Med. 2024 Jun 27;14(7):694. doi: 10.3390/jpm14070694. PMID: 39063948; PMCID: PMC11277895. 8: Okabe S, Tanaka Y, Moriyama M, Gotoh A. Inhibition of glutaminolysis alone and in combination with HDAC inhibitor has anti-myeloma therapeutic effects. Cancer Drug Resist. 2024 Jun 24;7:25. doi: 10.20517/cdr.2024.35. PMID: 39050886; PMCID: PMC11267151. 9: Amani MS, Peymani M. Investigating the impact of SMAD2 and SMAD4 downregulation in colorectal cancer and their correlation with immune markers, prognosis, and drug resistance and sensitivity. Mol Biol Rep. 2024 Jul 22;51(1):831. doi: 10.1007/s11033-024-09697-x. PMID: 39037563. 10: Liu H, Xu L, Yue S, Su H, Chen X, Liu Q, Li H, Liang H, Chen X, He J, Ding Z, Zhang B. Targeting N4-acetylcytidine suppresses hepatocellular carcinoma progression by repressing eEF2-mediated HMGB2 mRNA translation. Cancer Commun (Lond). 2024 Jul 19. doi: 10.1002/cac2.12595. Epub ahead of print. PMID: 39030964. 11: Ge P, Wang Z, Wang W, Gao Z, Li D, Guo H, Qiao S, Dang X, Yang H, Wu Y. Identifying drug candidates for pancreatic ductal adenocarcinoma based on integrative multiomics analysis. J Gastrointest Oncol. 2024 Jun 30;15(3):1265-1281. doi: 10.21037/jgo-23-985. Epub 2024 Jun 27. PMID: 38989421; PMCID: PMC11231868. 12: Miladinovic M, Reinhardt D, Hasle H, Goemans BF, Tomizawa D, Hitzler J, Klusmann JH. Guideline for treating relapsed or refractory myeloid leukemia in children with Down syndrome. Pediatr Blood Cancer. 2024 Sep;71(9):e31141. doi: 10.1002/pbc.31141. Epub 2024 Jul 4. PMID: 38965693. 13: Yamada M, Ikeda S, Kuroki W, Iwama S, Takahashi Y, Kitadate A, Tagawa H, Takahashi N. Comprehensive analysis of microRNAs modulated by histone deacetylase inhibitors identifies microRNA-7-5p with anti-myeloma effect. Int J Hematol. 2024 Jul 2. doi: 10.1007/s12185-024-03812-1. Epub ahead of print. PMID: 38954186. 14: Ismael A, Robinette AJ, Huric L, Schuetz J, Dona K, Benson D, Cocucci E, Cottini F. CREB1 promotes expression of immune checkpoint HLA-E leading to immune escape in multiple myeloma. Leukemia. 2024 Aug;38(8):1777-1786. doi: 10.1038/s41375-024-02303-w. Epub 2024 Jun 20. PMID: 38902472; PMCID: PMC11286514. 15: Hara H, Manome A, Kamiya T. Panobinostat, a Histone Deacetylase Inhibitor, Reduces LPS-Induced Expression of Inducible Nitric Oxide Synthase in Rat Immortalized Microglia HAPI Cells. Biol Pharm Bull. 2024;47(6):1196-1203. doi: 10.1248/bpb.b24-00111. PMID: 38897970. 16: Rode S, Kaur H, Rani R, Lonare S, Sharma M, Tomar S, Kumar P, Roy P, Sharma AK. Deciphering the drug delivery potential of Type1 lipid transfer protein from Citrus sinensis for enhancing the therapeutic efficacy of drugs. Biochem Biophys Res Commun. 2024 Sep 17;725:150253. doi: 10.1016/j.bbrc.2024.150253. Epub 2024 Jun 11. PMID: 38880080. 17: Zhang Y, Wong CH, Hui CWC, Tse T, Yeung V, Cheung K, Tao Q, Loong HH. Synergistic activities of Panobinostat and doxorubicin in soft tissue sarcomas. Biomed Pharmacother. 2024 Jul;176:116895. doi: 10.1016/j.biopha.2024.116895. Epub 2024 Jun 14. PMID: 38876055. 18: Victorelli FD, Lutz-Bueno V, Santos KP, Wu D, Sturla SJ, Mezzenga R. Cubosomes functionalized with antibodies as a potential strategy for the treatment of HER2-positive breast cancer. J Colloid Interface Sci. 2024 Nov;673:291-300. doi: 10.1016/j.jcis.2024.06.091. Epub 2024 Jun 11. PMID: 38875795. 19: Valdez BC, Tsimberidou AM, Yuan B, Nieto Y, Baysal MA, Chakraborty A, Andersen CR, Andersson BS. Synergistic cytotoxicity of histone deacetylase and poly-ADP ribose polymerase inhibitors and decitabine in pancreatic cancer cells: Implications for novel therapy. Oncotarget. 2024 Jun 3;15:361-373. doi: 10.18632/oncotarget.28588. PMID: 38829622; PMCID: PMC11146633. 20: Li C, Yi Y, Ouyang Y, Chen F, Lu C, Peng S, Wang Y, Chen X, Yan X, Xu H, Li S, Feng L, Xie X. TORSEL, a 4EBP1-based mTORC1 live-cell sensor, reveals nutrient-sensing targeting by histone deacetylase inhibitors. Cell Biosci. 2024 Jun 1;14(1):68. doi: 10.1186/s13578-024-01250-4. PMID: 38824577; PMCID: PMC11143692.

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