Art. -Nr.: HY-10528

Tasquinimod

(Synonyms: ABR-215050)

19 Cited Publications

Kundenbewertung

Based on 19 publication(s) in Google Scholar

Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn²⁺ binding domain of HDAC4 with K_d of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.

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Reinheit: 99.70%
CAS. Nr.: 254964-60-8
Formel: C₂₀H₁₇F₃N₂O₄
Molecular Weight:406.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Tasquinimod Chemical Structure

CAS. Nr.: 254964-60-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC4

10-30 nM (Kd)

Alle HDAC Isoform-spezifische Produkte anzeigen :

In Vitro

Tasquinimod suppresses hypoxia induced decrease in histone acetylation without lowering HDAC expression or directly inhibiting HDAC activity. Tasquinimod binds allosterically within the regulatory Zinc domain of HDAC4 with a K_d of 10-30 nM, which results in inhibition of co-localization of N-CoR/HDAC3, thereby inhibiting deacetylation of histones and HDAC4 client transcription factors, such as HIF-1α. TAMs secrete angiogenic factors like VEGF, FGF, TNF- α, and TGF-β when myeloid-derived suppressor cells differentiate. Tasquinimod can suppress tumor angiogenesis due to inhibition of S100A9/TLR4 dependent MDSCs tumor infiltration and/or to inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α by MDSCs suppressing their differentiation into TAMs.^[1]. Tasquinimod, an orally active quinoline-3-carboxamide, binds with high affinity to HDAC4 and S100A9 in cancer and infiltrating host cells within compromised tumor microenvironment inhibiting adaptive survival pathways needed for an angiogenic response^[2]. At 10 μM Tasquinimod, the TSP1 mRNA expression is elevated at 6 h and peaked after 72 h. Moreover, after 72 h exposure the TSP1 mRNA levels is already elevated at a dose of 1 μM Tasquinimod, indicating that Tasquinimod-induced changes in TSP1 mRNA expression occurrs in a dose range. At higher dose levels (i.e. 50-100 μM) the mRNA levels decline at 72 h, indicating additional drug effects at these concentrations. The up-regulation of TSP1 mRNA in LNCaP cells by Tasquinimod is manifested by an increased expression of TSP1 protein, as shown by western blot analysis of cell lysates prepared from cells cultured for 24 h and 72 h. Accompanied by increased intracellular TSP1 protein levels are also a statistically significant (p<0.05) accumulation of extracellular TSP1 in the cell culture medium detected. The extracellular secretion of TSP1 is time dependent and could clearly be detected after 24 h exposure to Tasquinimod at 10 μM. Also, TSP1 mRNA levels are induced by Tasquinimod at 10 μM in the hormone insensitive cell line LNCaP19 but not in DU145 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The bioavailability and oral absorption of Tasquinimod is excellent when adult male mice (i.e., C57Bl/6J, or athymic nude mice) are given 0.1-30 mg/kg (i.e., 0.2-74 μmoles/kg) via gavage or the drinking water. The potency of Tasquinimod expressed as the daily oral dose of Tasquinimod which inhibits cancer growth by 50% ranges from 0.1-1.0 mg/kg/d (i.e., 0.24-2.40 μmoles/kg/day) against a series (n>5) of human prostate cancer xenografts in immune-deficient mice. Tasquinimod at a chronic dose of 5 mg/kg/day via the drinking water produces > 80% inhibition (p<0.05) of TRAMP-C2 mouse prostate cancer growth in immune-competent syngeneic mice^[2]. Nude mice carrying subcutaneous LNCaP tumors are treated with Tasquinimod for 3 weeks. Exposure to Tasquinimod at 1 mg/kg/day and 10 mg/kg/day started on day 7 after inoculation. There is a statistically significant dose dependent reduction in tumor weight both at 1 mg/kg/day and 10 mg/kg/day compare to the untreated control group 28 days after inoculation (p<0.001), illustrating the anti-tumor effect of Tasquinimod^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 254964-60-8
Appearance Solid
Molecular Weight 406.36
Formel C₂₀H₁₇F₃N₂O₄
Color White to light yellow
SMILES

O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2OC)N(C)C3=CC=C(C(F)(F)F)C=C3
Synonyms

ABR-215050
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (19)

All In Vivo Efficacy StudyFlow Cytometry

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Journal Impact Factor

Cancer Cell

RAF-independent MEK mutations drive refractory histiocytic neoplasms but respond to ERK inhibition. [Abstract]

2025 Oct 23:S1535-6108(25)00406-4. PMID: 41135521
Nat Commun

An HDAC4-specific PROTAC degrader achieves radiation sensitization by enhancing ferroptosis in lung cancer. [Abstract]

2026 May 25. PMID: 42185286
Interdiscip Med

2026 May 18.
Adv Sci (Weinh)

Single Cell RNA Sequencing Identifies a Unique Inflammatory Macrophage Subset as a Druggable Target for Alleviating Acute Kidney Injury. [Abstract]

2022 Feb 3;e2103675. PMID: 35112806

Tasquinimod purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2022 Feb 3;e2103675. [Abstract]

Flow charts of drug treatments in uIRI animal models. V: vehicle; T: Tasquinimod (5 mg/kg, ip); P: Paquinimod (30 mg/kg).

Tasquinimod purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2022 Feb 3;e2103675. [Abstract]

Flow charts of drug treatments in uIRI animal models. V: vehicle; T: Tasquinimod (5 mg/kg, ip); P: Paquinimod (30 mg/kg). Flow cytometry showing the number of kidney Ims.
Cell Death Dis

S100A9 enhances tumor immune suppression and cancer cell survival in small cell lung cancer. [Abstract]

2025 Oct 31;16(1):774. PMID: 41173834

Tasquinimod purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Oct 31;16(1):774. [Abstract]

SBC5 cells were implanted subcutaneously into nude mice (n = 5). Palpable tumors were treated with vehicle control (VC) or Tasquinimod (TQ, 10 mg/kg) for 4 weeks, and tumor volumes were measured externally every week during the Tasquinimod treatment.

Tasquinimod purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Oct 31;16(1):774. [Abstract]

SCLC PDX was inoculated subcutaneously into the flanks of NSG mice. The PDX-bearing mice were treated with vehicle control (VC) or Tasquinimod (TQ, 10 mg/kg). Tumor volumes were measured externally every week, and tumor weight was calculated at the end of the experiment.

Tasquinimod purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Oct 31;16(1):774. [Abstract]

The experimental schema used to test the effects of Tasquinimod (TQ, oral, 10 mg/kg) and Cisplatin (Cis) alone or in combination (i.p. intraperitoneal) on KP1 tumor growth.
Cancer Lett

Coupling HDAC4 with transcriptional factor MEF2D abrogates SPRY4-mediated suppression of ERK activation and elicits hepatocellular carcinoma drug resistance. [Abstract]

2021 Nov 1:520:243-254. PMID: 34339801
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
EMBO J

Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]

2024 Nov;43(21):4954-4983. PMID: 39294473
Respir Res

S100A9 blockade prevents lipopolysaccharide-induced lung injury via suppressing the NLRP3 pathway. [Abstract]

2021 Feb 6;22(1):45. PMID: 33549095
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
J Innate Immun

Macrophage-Biomimetic Nanoparticles Ameliorate Ulcerative Colitis through Reducing Inflammatory Factors Expression. [Abstract]

2022;14(4):380-392. PMID: 34724662
iScience

Neutrophil S100A9 supports M2 macrophage niche formation in granulomas. [Abstract]

2023 Jan 31;26(3):106081. PMID: 36843852
Mol Hum Reprod

Eutopic macrophages facilitate endometriosis progression via ferroptosis-mediated release of S100A9. [Abstract]

2025 Apr 3;31(2):gaaf027. PMID: 40493892
Development

Inhibition of HDAC4 in granulosa cells improved co-cultured oocyte maturation in vitro independent of LH in porcine. [Abstract]

2025 Apr 1;152(7):dev204618. PMID: 40066659
Tissue Cell

Oleic acid inhibits the proliferation, invasion, and migration of tongue squamous cell carcinoma cells under high glucose conditions through S100A9-HK2/PKM2-SOD2 signaling pathway. [Abstract]

2025 Oct:96:103026. PMID: 40582120
bioRxiv

2026 Feb 3.
bioRxiv

2026 Feb 25.
bioRxiv

2025 Aug 25.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 42 mg/mL (103.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4609 mL

12.3044 mL

24.6087 mL

5 mM

0.4922 mL

2.4609 mL

4.9217 mL

10 mM

0.2461 mL

1.2304 mL

2.4609 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline