Ziritaxestat
Based on 7 publication(s) in Google Scholar
Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 1628260-79-6
- Formula: C30H33FN8O2S
- Molecular Weight:588.70
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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) Ziritaxestat
More- Immunity. 2021 Nov 9;54(11):2514-2530.e7. [Abstract]
- EBioMedicine. 2020 Feb;52:102652. [Abstract]
- Pharmacol Res. 2023 Sep:195:106877. [Abstract]
- Cancer Immunol Res. 2026 Jan 21:10.1158/2326-6066.CIR-25-0743. [Abstract]
- RSC Adv. 2026 Apr 7;16(20):18359-18373. [Abstract]
- Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]
- bioRxiv. 2024 Feb 19.
Customer Validation & Images
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
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Flow Cytometry
Biological Activity
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Autotaxin 131 nM (IC50) |
Autotaxin 15 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>15 μM
Compound: GLPG-1690
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Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
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[PMID: 32535330] |
| A549 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
| Hep 3B2 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
| MCF7 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
| MCF7 | IC50 |
8.32 μM
Compound: GLPG-1690
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Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay
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[PMID: 32535330] |
| MDA-MB-231 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
| MDA-MB-231 | IC50 |
6.27 μM
Compound: GLPG-1690
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Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
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[PMID: 32535330] |
| NCI-H1581 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
| NCI-H2228 | IC50 |
>15 μM
Compound: GLPG-1690
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Antiproliferative activity against human NCI-H2228 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H2228 cells measured after 72 hrs by MTT assay
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[PMID: 32535330] |
| NCI-H2228 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
| RAW264.7 | IC50 |
>20 μM
Compound: 4; GLPG1690
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Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 35436669] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1628260-79-6
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Appearance Solid
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Molecular Weight 588.70
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Formula C30H33FN8O2S
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Color White to off-white
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SMILES
N#CC1=C(C2=CC=C(F)C=C2)N=C(N(C3=C(CC)N=C4C(C)=CC(N5CCN(CC(N6CC(O)C6)=O)CC5)=CN43)C)S1
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Synonyms
GLPG1690
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Immunity
Plasmacytoid dendritic cell activation is dependent on coordinated expression of distinct amino acid transporters. [Abstract]2021 Nov 9;54(11):2514-2530.e7. PMID: 34717796
Ziritaxestat purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Nov 9;54(11):2514-2530.e7. [Abstract]
Isolated pDCs were maintained in HPLM ± IL-3 with Ziritaxestat (ZIR; 10-30 μM) o/n then stimulated ± CpG-A for 5 h and probed for: kynurenine uptake, pS6 expression and IFN-α production.
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EBioMedicine
A SNP of bacterial blc disturbs gut lysophospholipid homeostasis and induces inflammation through epithelial barrier disruption. [Abstract]2020 Feb;52:102652. PMID: 32058942 -
Pharmacol Res
ENPP2 inhibitor improves proliferation in AOM/DSS-induced colorectal cancer mice via remodeling the gut barrier function and gut microbiota composition. [Abstract]2023 Sep:195:106877. PMID: 37524154
Ziritaxestat purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Sep:195:106877. [Abstract]
GLPG1690 (Ziritaxestat; 7.5-20 μM; 48 h) treatment significantly increased the percentage of apoptotic cells in HT29 and HCT116 cells.
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Cancer Immunol Res
Ex Vivo Immuno-Oncology Platform Reveals Spatial T Cell Infiltration Patterns Linked to ATR Inhibition Responses in High-Grade Serous Ovarian Cancer. [Abstract]2026 Jan 21:10.1158/2326-6066.CIR-25-0743. PMID: 41563843 -
RSC Adv
A multi-stage computational pipeline and in vitro validation for the discovery of small-molecule translation inhibitors targeting the bacterial ribosome. [Abstract]2026 Apr 7;16(20):18359-18373. PMID: 41953617 -
Cancer Sci
Dual role of autotaxin as novel biomarker and therapeutic target in pancreatic neuroendocrine neoplasms. [Abstract]2023 Dec;114(12):4571-4582. PMID: 37770812
Ziritaxestat purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]
Cell proliferation by ATX inhibitor (GLPG1690, Ziritaxestat; 48 h) in QGP-1 and BON-1. Data represent means of the control group with dimethyl sulfoxide (DMSO) (n = 4) and treatment group with GLPG1690 (n = 4). Daily treatment was GLPG1690 at 10 μmol/L in QGP-1 and BON-1 or equivalent amount of DMSO.
Ziritaxestat purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]
Ziritaxestat (GLPG1690; 10 μM; 24 h) suppressed the migration of BON-1 cells.
Ziritaxestat purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]
Ziritaxestat (GLPG1690; 60 mg/kg; i.p.; once daily for 13 days) attenuated tumor growth in a BON-1 xenograft mouse model.
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Solvent & Solubility
DMSO : 40 mg/mL (67.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (3.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 20 mg/mL (33.97 mM); Suspended solution; Need ultrasonic
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 (273 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Portuguese - PT (643 KB)
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Handling Instructions (2659 KB)
References
[1]. Desroy N, et al. Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis. J Med Chem. 2017 May 11;60(9):3580-3590. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6987 mL | 8.4933 mL | 16.9866 mL | 42.4665 mL |
| 5 mM | 0.3397 mL | 1.6987 mL | 3.3973 mL | 8.4933 mL | |
| 10 mM | 0.1699 mL | 0.8493 mL | 1.6987 mL | 4.2466 mL | |
| 15 mM | 0.1132 mL | 0.5662 mL | 1.1324 mL | 2.8311 mL | |
| 20 mM | 0.0849 mL | 0.4247 mL | 0.8493 mL | 2.1233 mL | |
| 25 mM | 0.0679 mL | 0.3397 mL | 0.6795 mL | 1.6987 mL | |
| 30 mM | 0.0566 mL | 0.2831 mL | 0.5662 mL | 1.4155 mL | |
| 40 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0617 mL | |
| 50 mM | 0.0340 mL | 0.1699 mL | 0.3397 mL | 0.8493 mL | |
| 60 mM | 0.0283 mL | 0.1416 mL | 0.2831 mL | 0.7078 mL |
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