Tasquinimod

Catalog No.S7617 Batch:S761702

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Technical Data

Formula

C20H17F3N2O4
Molecular Weight 406.36 CAS No. 254964-60-8
Solubility (25°C)* In vitro DMSO 81 mg/mL (199.33 mM)
Ethanol 11 mg/mL (27.06 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)

Cell Assay:

[4]
  • Cell lines

    LNCaP19 cells

  • Concentrations

    10 μM

  • Incubation Time

    72 h

  • Method

    Cells were treated with indicated concentration of drug for 72 h.
Animal Study:

[2]
  • Animal Models

    Mice bearing PC-82 , CWR-22Rv1, LAPC-4, or LNCaP prostate cancer xenografts.

  • Dosages

    ~30 mg/kg/d

  • Administration

    p.o.

Customer Product Validation

, , Oxid Med Cell Longev, 2017, doi: 10.1155/2017/7150376

Selleck's Tasquinimod has been cited by 20 publications

Histone deacetylase inhibitors promote breast cancer metastasis by elevating NEDD9 expression [ Signal Transduct Target Ther, 2023, 8(1):11] PubMed: 36604412
S100A9-CXCL12 activation in BRCA1-mutant breast cancer promotes an immunosuppressive microenvironment associated with resistance to immunotherapy [ Nat Commun, 2022, 13(1):1481] PubMed: 35304461
HDAC5-mediated Smad7 silencing through MEF2A is critical for fibroblast activation and hypertrophic scar formation [ Int J Biol Sci, 2022, 18(15):5724-5739] PubMed: 36263180
The p300/CBP inhibitor A485 normalizes psoriatic fibroblast gene expression in vitro and reduces psoriasis-like skin inflammation in vivo [ J Invest Dermatol, 2022, S0022-202X(22)01937-6] PubMed: 36174717
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147] PubMed: 36371227
Pharmacological and Genetic Inhibition of HDAC4 Alleviates Renal Injury and Fibrosis in Mice [ Front Pharmacol, 2022, 13:929334] PubMed: 35847036
Histone Deacetylase 4 Controls Extracellular Matrix Production in Orbital Fibroblasts from Graves' Ophthalmopathy Patients [ Thyroid, 2021, 10.1089/thy.2020.0948] PubMed: 34235979
In-Depth Immune-Oncology Studies of the Tumor Microenvironment in a Humanized Melanoma Mouse Model [ Int J Mol Sci, 2021, 22(3)E1011] PubMed: 33498319
HDAC3 inhibitor RGFP966 controls bacterial growth and modulates macrophage signaling during Mycobacterium tuberculosis infection [ Tuberculosis (Edinb), 2021, 127:102062] PubMed: 33639591
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.