Home>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>LAQ824 (NVP-LAQ824,Dacinostat)

LAQ824 (NVP-LAQ824,Dacinostat) (Synonyms: Dacinostat, NVP-LAQ824)

Catalog No.GC15114

A hydroxamate-based HDAC inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

LAQ824 (NVP-LAQ824,Dacinostat) Chemical Structure

Cas No.: 404951-53-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$138.00
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10mg
$140.00
In stock
50mg
$336.00
In stock
200mg
$889.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment: [1]

Cell lines

Dexamethasone –sensitive human multiple myeloma (Dex-sensitive MM.1S) cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

20 nM 24-, 48-, or 72-hour

Applications

As an inhibitor of HDAC, LAQ824 induces apoptosis in multiple myeloma cell lines resistant to conventional therapies. In this experiment, Dex or LAQ824 alone produced only 15% and 7% growth inhibition, respectively, but produced 51% inhibition when used in combination.

Animal experiment : [2]

Animal models

Female BALB/c mice administered 32D.p210 leukemic cells via tail vein injection

Dosage form

The mice were given intraperitoneal injection of either 25 mg/kg LAQ824 or D5W vehicle on a daily basis, beginning 3 days after introduction of the leukemic cells.

Applications

Treatment of mice with LAQ824 delayed the onset of symptoms of leukemia and lethality as compared to mice treated with the vehicle control. Median survival times were 20 days in the LAQ824-treated mice and 15.5 days in the vehicle control mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Catley L, Weisberg E, Tai Y T, et al. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood, 2003, 102(7): 2615-2622.

[2] Weisberg E, Catley L, Kujawa J, et al. Histone deacetylase inhibitor NVP-LAQ824 has significant activity against myeloid leukemia cells in vitro and in vivo. Leukemia, 2004, 18(12): 1951-1963.

Background

LAQ824 (also known as NVP-LAQ824 or Dacinostat), a derivative of 4-aminomethylcinnamic hydroxamic acid, is a novel and potent inhibitor of histone deacetylase (HDAC) that inhibits the activity of HDAC with 50% inhibition concentration IC50 value of 0.03 μM. LAQ824 has been found to inhibit the growth of a variety of cancer cell lines, including colon cancer H1299 and HCT116 cells, breast cancer MDA435 cells, prostate cancer DU145 and PC3 cells and non-small cell lung cancer A549 cells, with IC50 value < 1 μM and induce apoptosis in human breast cancer SKBR-3, BT-474 and MB-468 cells. LAQ824 also dose- and time-dependently inhibits the growth of multiple myeloma cells.

Reference

[1].Catley L, Weisberg E, Tai YT, Atadja P, Remiszewski S, Hideshima T, Mitsiades N, Shringarpure R, LeBlanc R, Chauhan D, Munshi NC, Schlossman R, Richardson P, Griffin J, Anderson KC. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. Epub 2003 Jun 19.

Chemical Properties

Cas No. 404951-53-7 SDF
Synonyms Dacinostat, NVP-LAQ824
Chemical Name (E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide
Canonical SMILES C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)C=CC(=O)NO
Formula C22H25N3O3 M.Wt 379.46
Solubility ≥ 17.45 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6353 mL 13.1766 mL 26.3532 mL
5 mM 0.5271 mL 2.6353 mL 5.2706 mL
10 mM 0.2635 mL 1.3177 mL 2.6353 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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