1. Cell Cycle/DNA Damage Epigenetics Autophagy
  2. HDAC Autophagy
  3. Dacinostat

Dacinostat  (Synonyms: NVP-LAQ824; LAQ824)

Cat. No.: HY-13606 Purity: 98.45%
COA Handling Instructions

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

For research use only. We do not sell to patients.

Dacinostat Chemical Structure

Dacinostat Chemical Structure

CAS No. : 404951-53-7

Size Price Stock Quantity
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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 262 In-stock
Solution
10 mM * 1 mL in DMSO USD 262 In-stock
Solid
5 mg USD 153 In-stock
10 mg USD 238 In-stock
50 mg USD 634 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

IC50 & Target[1][2]

HDAC1

9 nM (IC50)

HDAC

32 nM (IC50)

In Vitro

Dacinostat (NVP-LAQ824) activates p21 promoter, with AC50 of 0.30 μM. NVP-LAQ824 inhibits tumor cell (H1299, HCT116) growth, with IC50s of 150 and 10 nM, respectively. NVP-LAQ824 also shows inhibitory activities against two prostate cancer cell lines (DU145 and PC3) and a breast cancer line (MDA435), with IC50s of 18, 23, 39 nM, respectively. Continuous exposure of NVP-LAQ824 for 72 h produces LD90s of 0.09 M in HCT116 cells and 0.47 M in A549 cells. NVP-LAQ824 treatment of NDHF cells causes the expected G1-S growth arrest in addition to a significant reduction of cells in S-phase and accumulation of cells at the G2-M checkpoint. NVP-LAQ824 induces apoptotic death in human tumor cells. NPV-LAQ824 increases acetylation of histones H3 and H4[1]. Dacinostat inhibits HDAC1 with an IC50 of 9 nM[2]. Dacinostat (10 and 20 nM) suppresses proliferation of AML fusion protein-expressing 32D cells. Dacinostat impairs short-term engraftment potential of leukemic stem cells. Dacinostat exhausts in vitro self-renewal potential of murine AML1/ETO- and PLZF/RARα-positive HSC[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NVP-LAQ824 produces a dose-dependent inhibition of tumor growth, and at 100 mg/kg, its antitumor effect is similar to that of 5-Fluorouracil[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

379.45

Formula

C22H25N3O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NO)/C=C/C1=CC=C(CN(CCO)CCC2=CNC3=C2C=CC=C3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 43 mg/mL (113.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.45%

References
Kinase Assay
[2]

The HDAC enzymatic assay measures compound activity in inhibiting purified HDAC isoforms. HDACs 1, 3, and 6 are immunopurified from 293 cells stably expressing the FLAG-tagged HDAC isoform, whereas HDACs 2, 4, 5, 7, 8, 9, 10, and 11 are purified from the baculovirus expression system. HDAC activity is measured in a fluorescent assay in which deacetylation of the substrate, bis-Boc-(Ac)Lys-rhodamine 110, generates a fluorophore that can be detected on a fluorometric plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cells are plated at 5000−10000 cells per well in 96-well plates and treated with eight serial compound dilutions. Cell viability following 72 h of compound treatment is measured using the CellTiter-Glo or MTS assay. XLfit 4 is used for plotting of the growth curves and calculation of IC50 values[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

The studies are performed on-site, using outbred athymic (nu/nu) female mice. Mice are anesthetized with Metofane, and a cell suspension (100 μL) containing 1×106 HCT116 cells is injected s.c. into the right axillary (lateral) region of each animal. Tumors are allowed to reach the volume of approximately 100-400 mm3. At this point, mice bearing tumors with acceptable morphology (non-necrotic) and of similar size range are selected and distributed into groups of six for the studies. NVP-LAQ824 is dissolved in DMSO to create a stock solution, which is further diluted just before dosing with D5W to a final DMSO concentration of 10%. Tumor-bearing mice are treated with the compound by i.v. injection into the tail vein. NVP-LAQ824 is dosed once daily, 5 days/week, for a total of 15 doses. 5-Fluorouracil is administered at 100 mg/kg in 0.9% saline 1 day/week for a total of three doses. The control groups are treated with the vehicle. Tumors are collected from the animals at the indicated time points[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6354 mL 13.1770 mL 26.3539 mL 65.8848 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL 13.1770 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL 6.5885 mL
15 mM 0.1757 mL 0.8785 mL 1.7569 mL 4.3923 mL
20 mM 0.1318 mL 0.6588 mL 1.3177 mL 3.2942 mL
25 mM 0.1054 mL 0.5271 mL 1.0542 mL 2.6354 mL
30 mM 0.0878 mL 0.4392 mL 0.8785 mL 2.1962 mL
40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6471 mL
50 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3177 mL
60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0981 mL
80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
100 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
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Dacinostat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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