Tasquinimod
Based on 22 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 Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
For research use only. We do not sell to patients.
- Purity : 99.70%
- CAS No.: 254964-60-8
- Formula: C20H17F3N2O4
- Molecular Weight:406.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tasquinimod
More- Cancer Cell. 2025 Oct 23:S1535-6108(25)00406-4. [Abstract]
- Nat Commun. 2026 May 25. [Abstract]
- Interdiscip Med. 2026 May 18.
- Adv Sci (Weinh). 2022 Feb 3;e2103675. [Abstract]
- Cell Death Dis. 2026 May 2;17(1):584.
- Cell Death Dis. 2025 Oct 31;16(1):774. [Abstract]
- Cancer Lett. 2021 Nov 1:520:243-254. [Abstract]
- Oncogene. 2026 Sep 1.
- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- EMBO J. 2024 Nov;43(21):4954-4983. [Abstract]
- Respir Res. 2021 Feb 6;22(1):45. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- J Innate Immun. 2022;14(4):380-392. [Abstract]
- iScience. 2023 Jan 31;26(3):106081. [Abstract]
- Mol Hum Reprod. 2025 Apr 3;31(2):gaaf027. [Abstract]
- Development. 2025 Apr 1;152(7):dev204618. [Abstract]
- Tissue Cell. 2025 Oct:96:103026. [Abstract]
- bioRxiv. 2026 Sep 28.
- bioRxiv. 2026 Feb 3.
- bioRxiv. 2026 Feb 25.
- bioRxiv. 2025 Aug 25.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Flow Cytometry
Biological Activity
Description
IC50 & Target
[1]|
HDAC4 10-30 nM (Kd) |
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 Kd 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
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
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| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 254964-60-8
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Appearance Solid
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Molecular Weight 406.36
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Formula C20H17F3N2O4
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Color White to light yellow
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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
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Synonyms
ABR-215050
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (22)
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Journal Impact Factor
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Most Recent
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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 -
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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.
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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.
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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 -
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Oncogene
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)
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
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 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Isaacs JT, et al. Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Cancer Res. 2013 Feb 15;73(4):1386-99. [Content Brief]
[2]. Isaacs JT, et al. Anti-cancer potency of tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment. Oncotarget. 2014 Sep 30;5(18):8093-106. [Content Brief]
[3]. Olsson A, et al. Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Mol Cancer. 2010 May 17;9:107. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4609 mL | 12.3044 mL | 24.6087 mL | 61.5218 mL |
| 5 mM | 0.4922 mL | 2.4609 mL | 4.9217 mL | 12.3044 mL | |
| 10 mM | 0.2461 mL | 1.2304 mL | 2.4609 mL | 6.1522 mL | |
| 15 mM | 0.1641 mL | 0.8203 mL | 1.6406 mL | 4.1015 mL | |
| 20 mM | 0.1230 mL | 0.6152 mL | 1.2304 mL | 3.0761 mL | |
| 25 mM | 0.0984 mL | 0.4922 mL | 0.9843 mL | 2.4609 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8203 mL | 2.0507 mL | |
| 40 mM | 0.0615 mL | 0.3076 mL | 0.6152 mL | 1.5380 mL | |
| 50 mM | 0.0492 mL | 0.2461 mL | 0.4922 mL | 1.2304 mL | |
| 60 mM | 0.0410 mL | 0.2051 mL | 0.4101 mL | 1.0254 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3076 mL | 0.7690 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2461 mL | 0.6152 mL |
Tasquinimod Related Classifications
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