Tasquinimod

For research use only.

Catalog No.S7617 Synonyms: ABR-215050

12 publications

Tasquinimod Chemical Structure

CAS No. 254964-60-8

Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.

Selleck's Tasquinimod has been cited by 12 publications

1 Customer Review

  • Western blot images suggested inhibition of HDAC4 increased the expression of NOX4 and MMP-9, and treatment with 10 μM SCM-198 reduced the raised levels of NOX4 and MMP-9.

    Oxid Med Cell Longev, 2017, doi: 10.1155/2017/7150376 . Tasquinimod purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
Targets
HDAC4 [1]
In vitro

Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. [1] Tasquinimod also targets infiltrating myeloid cells, and modulates local tumour immunity by blocking the interaction between S100A9 and its ligands receptor of advanced glycation end products and Toll-like receptor 4. [3]

In vivo Tasquinimod (30 mg/kg/d p.o.) shows anti-angiogenic activity and thus causes tumor growth inhibition in mice bearing human and rodent prostate cancer models. [2]

Protocol

Animal Research:

[2]

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  • Animal Models: Mice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts.
  • Dosages: ~30 mg/kg/d
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (199.33 mM)
Ethanol 11 mg/mL warmed (27.06 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
8mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 406.36
Formula

C20H17F3N2O4

CAS No. 254964-60-8
Storage powder
in solvent
Synonyms ABR-215050
Smiles CN1C2=C(C(=CC=C2)OC)C(=C(C1=O)C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02396368 Withdrawn Drug: Tasquinimod|Radiation: Radium 223 Prostate Cancer|Bone-only Metastatic Castration-Resistant Prostate Cancer (CRPC) Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins March 2015 Phase 1
NCT02057666 Terminated Drug: Tasquinimod|Drug: Placebo Prostatic Neoplasms Castration-Resistant Ipsen January 2014 Phase 3
NCT01732549 Terminated Drug: Tasquinimod|Drug: Placebo Metastatic Castrate Resistant Prostate Cancer Ipsen January 2013 Phase 2
NCT01234311 Completed Drug: tasquinimod|Drug: Placebo Prostate Cancer Active Biotech AB March 2011 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID