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NVP-LBH589 (Panobinostat) | HDAC inhibitor

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Price:
$129.00
Catalog #:
C5245-5
Quantity:


Product Description

LBH589, a hydroxamate analog, is a broad-spectrum HDAC inhibitor. It has been shown to increase acetylation of core histones (H3 and H4) and nonhistone proteins (alpha-tublin, HSP90), leading to the modulation of gene expression (p21, FOXO3A, GADD45A, aromatase, etc) and protein activity involved in cell growth and survival pathways1-4. LBH589 induces apoptosis in MOLT-4 and Reh cells with IC50 between 5 to 20nM1. In lung cancer and mesothelioma animal models, LBH589 markedly decreased tumor growth by 62% when compared with the vehicle control5. The anti-tumor activity of LBH589 has also been demonstrated in many other cancer cell lines, including multiple myeloma, NSCLC and castrate-resistant prostate cancer cell lines. LBH589 is under clinical trials to evaluate its effects in conjunction with chemotherapy and/or targeted therapy in multiple cancer types.


Technical information:

Chemical Formula:   C21H23N3O2
CAS #:   404950-80-7
Molecular Weight:   349.43
Purity:   >98%
Appearance:   White solid
Chemical Name:   (2E)-N-hydroxy-3-[4-({[2-(2-methyl-1H-indol-3-yl)ethyl]amino}methyl)phenyl]acrylamide
Solubility:   Up to 50 mM in DMSO

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

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. Chen, S. et al.The HDAC inhibitor LBH589 (panobinostat) is an inhibitory modulator of aromatase gene expression. Proc Natl Acad Sci U S A 2010 Jun 15; 107(24) :11032-7.
3. George, P., et al. "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 105: 1768-1776 (2005).
4. Qian, D.Z., et al. "Targeting tumor angiogenesis with histone deacetylase inhibitors: the hydroxamic acid derivative LBH589." Clin. Cancer Res. 12: 634-642 (2006).
5. 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.

Other Information:

Product Specification (pdf)
MSDS (pdf)

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