Tasquinimod

Catalog No.S7617 Synonyms: ABR-215050

For research use only.

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

Tasquinimod Chemical Structure

CAS No. 254964-60-8

Selleck's Tasquinimod has been cited by 13 publications

Purity & Quality Control

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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 (from reference)

Animal Research:

[2]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 406.36
Formula

C20H17F3N2O4

CAS No. 254964-60-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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