Tasquinimod

Catalog No.S7617 Synonyms: ABR-215050

Tasquinimod Chemical Structure

Molecular Weight(MW): 406.36

Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.

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Biological Activity

Description Tasquinimod 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]

+ Expand
  • Animal Models: Mice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts.
  • Formulation: Water
  • 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 individually and in order:
5% DMSO+30% PEG 300+ddH2O
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
Synonyms ABR-215050

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Clinical Trial Information

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NCT02396368 Withdrawn Prostate Cancer|Bone-only Metastatic Castration-Resistant Prostate Cancer (CRPC) Sidney Kimmel Comprehensive Cancer Center March 2015 Phase 1
NCT02159950 Completed Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|Active Biotech AB January 2015 Phase 2
NCT02057666 Terminated Asian Chemo-naïve Patients With Metastatic Castrate-resistant Prostate Cancer Ipsen January 2014 Phase 3
NCT01732549 Terminated Metastatic Castrate Resistant Prostate Cancer Ipsen January 2013 Phase 2
NCT01743469 Active, not recruiting Advanced or Metastatic Hepatocellular Cancer|Advanced or Metastatic Ovarian Cancer|Metastatic Renal Cell Cancer|Advanced or Metastatic Gastric Carcinoma Ipsen December 2012 Phase 2
NCT01513733 Completed Prostate Cancer Andrew J. Armstrong, MD|Duke University January 2012 Phase 1

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID