Panobinostat

Product Description

Panobinostat is a potent pan-histone deacetylase (HDAC) inhibitor (IC₅₀ values = 2.1 - 531 nM). Panobinostat induces histone H3 and H4 acetylation and potently inhibits cell proliferation and cell viability in HH, BT474 and HCT116 cells (IC₅₀ are 1.8, 2.6 and 7.1 nM, respectively) in vitro. It leads to significant tumor regression of up to 94% in an HH CTCL mouse xenograft model. Panobinostat inhibits the DNA binding activity of STAT5 in leukemia cell lines and acts synergistically with 17-AAG (Cat. No. 1515) to induce apoptosis. The compound shows potent antimyeloma activity, including in drug-resistant cell lines. Panobinostat also induces a significant increase in cell-associated unspliced (CA-US) HIV-1 RNA from CD4⁺ T cells and leads to activation of transcription of proviruses. Panobinostat simultaneously suppresses the expression of angiotensin-converting enzyme 2 (ACE2) and ABO in epithelial cell lines. Antimalarial and orally bioavailable.

Solubility

Preparing Stock Solutions for Panobinostat

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.86 mL	14.31 mL	28.62 mL
5 mM	0.57 mL	2.86 mL	5.72 mL
10 mM	0.29 mL	1.43 mL	2.86 mL
50 mM	0.06 mL	0.29 mL	0.57 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Takahashi Histone deacetylase inhibitors suppress ACE2 and ABO simultaneously, suggesting a preventive potential against COVID-19. Sci.Rep. 2021 PMID: 33564039
• Barton Broad activation of latent HIV-1 in vivo. Nat.Commun. 2016 PMID: 27605062
• Maiso The histone deacetylase inhibitor LBH589 is a potent antimyeloma agent that overcomes drug resistance. Cancer Res. 2006 PMID: 16740717
• George Combination of the histone deacetylase inhibitor LBH589 and the hsp90 inhibitor 17-AAG is highly active against human CML-BC cells and AML cells with activating mutation of FLT-3. Blood 2005 PMID: 15514006
• Atadja Development of the pan-DAC inhibitor panobinostat (LBH589): successes and challenges. Cancer Lett. 2009 PMID: 19344997