Tasquinimod

SKU: orb1300548

Description

Tasquinimod (ABR-215050) is an orally active small molecule with antiangiogenic and antitumor properties. It functions as an S100A9 inhibitor and binds the HDAC4 Zn²⁺ domain with high affinity (Kd 10-30 nM). This agent has been investigated in preclinical in vivo models for cancers like prostate carcinoma and in vitro for immunomodulatory effects.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 254964-60-8
• MW: 406.36
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₁₇F₃N₂O₄
• SMILES: COc1cccc2n(C)c(=O)c(C(=O)N(C)c3ccc(cc3)C(F)(F)F)c(O)c12
• Target: HDAC
• Solubility: 2% DMSO+40% PEG300+5% Tween-80+53% Saline:1 mg/mL (2.46 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:9 mg/mL (22.15 mM);DMSO:65 mg/mL (159.96 mM)

Bioactivity

• Target IC50:
  HUVECs:0.500 μM|HDAC4:10-30 nM (Kd)|AhR:1 mM (EC50)
• In Vivo:
  METHODS: Mice were treated with Tasquinimod (ABR-215050) (30 mg/kg), added to the daily drinking water at an early stage after MM cell inoculation, and immune cell populations were studied using flow cytometry. RESULTS Short-term Tasquinimod treatment did not lead to alterations in MM cell homing to the bone marrow, but a significant increase in the total percentage of CD11b cells could be observed, whereas a slight decrease in monocytes and immature myeloid populations (CD11b, Ly6G, Ly6C+-low) was observed, and an increase in macrophage populations (CD11b, F4/80), which showed a more pro-inflammatory phenotype of M1 (MHCII) and the M2 marker CD206. METHODS: SKOV3 or SKOV3/DDP cells were injected into 4-week-old female BALB/c nude mice. Then, 50 mg/kg Tasquinimod was administered every 3 days. finally, changes in tumor diameter and weight were measured, and apoptosis, migration rate, and related expression of Nur77 and Bcl-2 (BH3 structural domain specific) were detected by flow cytometry, scratch assay, and immunofluorescence. RESULTS Tasquinimod significantly reduced tumor diameter, tumor mass, and in vivo HDAC4 levels in mice. Meanwhile, Nur77 and Bcl-2 (BH3 structural domain specific) levels were elevated.
• In Vitro:
  METHODS: Human MM cells (multiple myeloma cells) were treated with increasing concentrations of Tasquinimod (ABR-215050) (10,25 μM) for 24 h, 48 h, 72 h, and 120 h. The effect of Tasquinimod on the value added of human MM cells was observed. RESULTS Tasquinimod inhibited the growth and proliferation of MM cells in vitro. METHODS: SKOV3 and SKOV3/DDP cells were treated with 40 μM tasquinimod, and the expression of histone deacetylase 4 (HDAC4), Nur77, Bcl-2 (BH3 structural domain specific), and caspase-3 were analyzed by Western blot and quantitative real-time polymerase chain reaction (qPCR). RESULTS Cell migration and HDAC4 expression levels were significantly reduced, while Nur77 expression levels were elevated.
• Cell Research:
  Tasquinimod is dissolved in DMSO and stored, and then diluted with appropriate media before use. Two human prostate cancer cell lines, CWR-22RH and LNCaP (ATCC) are both androgen independent, but remain sensitive to androgen stimulation of growth, express PSA and a mutated androgen receptor. The hormone independent cell lines LNCaP19 and DU145 are also tested for TSP1 induction after in vitro exposure to Tasquinimod (0.1-100 μM). CWR-22RH, LNCaP and DU145 are grown in RPMI Medium 1640 containing 10% FCS and L-Glutamine mixture, while LNCAP19 is cultured in RPMI-medium with 10% hormone free (RDCC) FCS.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ABR215050, ABR-215050, ABR 215050, inhibit, HDAC4, HDAC, Inhibitor, Histone deacetylases, Tasquinimod

Compound Identifiers

PubChem CID

54682876