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LAQ824

Cat. No. M1747
LAQ824 Structure
Synonym:

NVP-LAQ824

Size Price Availability Quantity
10mg USD 260 In stock
50mg USD 780 In stock
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Quality Control
Biological Activity

LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase (HDAC) inhibitor with an IC50 of 0.032 μM. NVP-LAQ824 also inhibited patient MM cell growth in a dose- and time-dependent manner. NVP-LAQ824-induced apoptotic signaling includes up-regulation of p21, caspase cascade activation, and poly (adenosine diphosphate [ADP]) ribose (PARP) cleavage.

Protocol
Cell Experiment
Cell lines HCT116, H1299, PC-3, DU145 and MDA435 cells
Preparation method Monolayer Growth Inhibition Assay. Cell proliferation was measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay) as described previously (29) . The CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay was performed according to the manufacturer’s protocol. The average background value (treatment with medium alone) was subtracted from each experimental well; triplicate values were averaged for each compound dilution. The following formulas were used to calculate the percentage of growth: The “% Growth” was plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.
Concentrations 0~10 μM
Incubation time 72 hr
Animal Experiment
Animal models HCT116 cells tumor-bearing mice
Formulation dissolved in DMSO to create a stock solution, which was further diluted just before dosing with D5W to a final DMSO concentration of 10%.
Dosages once daily, 5 days/week, for a total of 15 doses.
Administration i.v. injection into the tail vein
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 379.459
Formula C22H25N3O3
CAS Number 404951-53-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Histone deacetylase inhibition increases levels of choline kinase α and phosphocholine facilitating noninvasive imaging in human cancers.
Beloueche-Babari M et al. Cancer Res. 2012 Feb 15;72(4):990-1000. PMID: 22194463.

Histone deacetylase inhibitor LAQ824 augments inflammatory responses in macrophages through transcriptional regulation of IL-10.
Wang H et al. J Immunol. 2011 Apr 1;186(7):3986-96. PMID: 21368229.

The deacetylase inhibitor LAQ824 induces notch signalling in haematopoietic progenitor cells.
Schwarz K et al. Leuk Res. 2011 Jan;35(1):119-25. PMID: 20674020.

Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824).
Cho YS et al. J Med Chem. 2010 Apr 8;53(7):2952-63. PMID: 20205394.

Enhanced antitumor activity induced by adoptive T-cell transfer and adjunctive use of the histone deacetylase inhibitor LAQ824.
Vo DD et al. Cancer Res. 2009 Nov 15;69(22):8693-9. PMID: 19861533.

The histone deacetylase inhibitors LAQ824 and LBH589 do not require death receptor signaling or a functional apoptosome to mediate tumor cell death or therapeutic efficacy.
Ellis L et al. Blood. 2009 Jul 9;114(2):380-93. PMID: 19383971.

Selective growth inhibition of tumor cells by a novel histone deacetylase inhibitor, NVP-LAQ824.
Atadja P, et al. Cancer Res. 2004 Jan 15;64(2):689-95. PMID: 14744786.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LAQ824, NVP-LAQ824 supplier, HDAC, inhibitors

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