Home Angiogenesis HDAC inhibitor Tasquinimod For research use only.

Tasquinimod

Synonyms: ABR-215050

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

Tasquinimod Chemical Structure

Tasquinimod Chemical Structure

CAS No. 254964-60-8

Purity & Quality Control

Tasquinimod Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Biological Activity

Description Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
Targets
HDAC4 [1]
In vitro
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]
Cell Research Cell lines LNCaP19 cells
Concentrations 10 μM
Incubation Time 72 h
Method

Cells were treated with indicated concentration of drug for 72 h.
In Vivo
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]
Animal Research Animal Models Mice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts.
Dosages ~30 mg/kg/d
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02396368 Withdrawn
Prostate Cancer|Bone-only Metastatic Castration-Resistant Prostate Cancer (CRPC)
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins
 March 2015 Phase 1
NCT02057666 Terminated
Prostatic Neoplasms Castration-Resistant
Ipsen
 January 2014 Phase 3
NCT01732549 Terminated
Metastatic Castrate Resistant Prostate Cancer
Ipsen
 January 2013 Phase 2
NCT01234311 Completed
Prostate Cancer
Active Biotech AB
 March 2011 Phase 3

Chemical Information & Solubility

Molecular Weight 406.36 Formula

C20H17F3N2O4
CAS No. 254964-60-8 SDF Download Tasquinimod SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (199.33 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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.

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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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