WRG-28
Based on 3 publication(s) in Google Scholar
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice.
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- Pureza : 99.76%
- No. CAS: 1913291-02-7
- Fòrmula: C21H18N2O5S
- Peso molecular:410.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) WRG-28
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
DDR2 230 nM (IC50) |
In Vitro
WRG-28 (1, 2 μM; 4 h) blunts collagen I-mediated DDR2 tyrosine phosphorylation and (1 μM; 7 h) ERK activation as well as SNAIL1 protein stabilization in HEK293 cells (expressing DDR2) (IC50=286 nM)[1].
WRG-28 (1 μM; 48 h) blunts tumor cell invasion and migration by inhibiting DDR2 in BT549 and 4T1 breast cancer cells[1].
WRG-28 (1 μM; 4 days) inhibits tumor-promoting effects of CAFs[1].
WRG-28 (0.5, 1 μM; 4 h) maintains inhibitory action toward acquired DDR2 mutations that are resistant to TKIs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells (transfected with DDR2-Flag)
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Concentration:0.25, 0.5, 1, 2 µM
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Incubation Time:4 h
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Result:Significantly inhibited collagen I-mediated DDR2 tyrosine phosphorylation at 1 or 2µM, and with an IC>sub>50 of 286 nM.
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Cell Line:HEK293 cells (transfected with DDR2-Flag)
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Concentration:1 µM
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Incubation Time:7 h
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Result:Inhibited collagen I-mediated ERK activation and SNAIL1 protein stabilization (IC50=286 nM).
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Cell Line:BT549 and 4T1 breast cancer cells (expressing endogenous DDR2)
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Concentration:1 μM
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Incubation Time:48 h
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Result:Inhibited DDR2 induced invasion and migration of tumor cells.
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Cell Line:CAF cells (with tumor organoids)
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Concentration:1 μM
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Incubation Time:4 days
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Result:Inhibited the activity of DDR2 that supported invasion of primary tumor organoids in CAFs.
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Cell Line:HEK293 cells (expressing DDR2T654I)
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Concentration:0.5, 1 μM
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Incubation Time:4 h
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Result:Inhibited phosphorylation of the DDR2T654I mutant in response to collagen I.
In Vivo
WRG-28 (10 mg/kg; i.v.; single daily for 7 days) reduces metastatic lung colonization of breast tumor cells[1].
WRG-28 (10 mg/kg; i.v.; single daily for 21 days) decreases both the inflammatory reaction and joint destruction in mice with collagen antibody-induced arthritis (CAIA)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/cJ mice (8-week-old; 4T1-Snail-CBG tumor-bearing mice model)[1].
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Dosage:10 mg/kg
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Administration:Intravenous injection, single.
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Result:Reduced 60% SNAIL1-clic beetle green (SNAIL1.CBG) level within the tumor in mice.
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Animal Model:Female BALB/cJ mice (8-week-old; injected with 4T1 GFP-luc expressing cells)[1].
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Dosage:10 mg/kg
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Administration:Intravenous injection, single daily for 7 days.
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Result:Reduced lung colonization to a level comparable to shDDR2-depleted cells.
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Animal Model:Male DBA/1 mice (8-week-old; CAIA model)[2].
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Dosage:10 mg/kg
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Administration:Intravenous injection, single daily for 21 days.
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Result:Significantly ameliorated arthritis in the mice (reduced production of IL-15 and Dkk-1), the hind- paw thickness of the mice was also reduced.
Inhibited inflammatory cell infiltration and destruction of cartilage in mouse ankle and serum.
Significantly alleviated bone destruction, reduced the extent of joint space enlargement and bone mineral density, as well as decreased the severity of bone loss.
Chemical Information
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No. CAS 1913291-02-7
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Appearance Solid
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Peso molecular 410.44
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Fòrmula C21H18N2O5S
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Color Orange to red
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SMILES
O=S(C1=CC=C(COC2=CC(OC3=CC(C=CC3=N4)=O)=C4C=C2)C=C1)(NCC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Small
Collagen Signaling via DDR1 Exacerbates Barriers to Macromolecular Drug Delivery in a 3D Model of Pancreatic Cancer Fibrosis. [Abstract]2025 Dec;21(50):e06926. PMID: 41170605 -
Clin Transl Med
DDR2-mediated autophagy inhibition contributes to angiotensin II-induced adventitial remodeling. [Abstract]2025 Jun;15(6):e70361. PMID: 40468620 -
Sci Rep
Preliminary pharmacokinetic investigation of two discoidin domain receptor 2 inhibitors in murine plasma and brain using liquid chromatography-tandem mass spectrometry analysis. [Abstract]2026 Jun 24. PMID: 42342854
Solvente y solubilidad
In Vitro:
DMSO : 10 mg/mL (24.36 mM; Need ultrasonic; 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)
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: ≥ 1 mg/mL (2.44 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Grither WR, et al. Inhibition of tumor-microenvironment interaction and tumor invasion by small-molecule allosteric inhibitor of DDR2 extracellular domain. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7786-E7794. [Content Brief]
[2]. Mu N, et al. Blockade of Discoidin Domain Receptor 2 as a Strategy for Reducing Inflammation and Joint Destruction in Rheumatoid Arthritis Via Altered Interleukin-15 and Dkk-1 Signaling in Fibroblast-Like Synoviocytes. Arthritis Rheumatol. 2020 Jun;72(6):943-956. [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 | 2.4364 mL | 12.1820 mL | 24.3641 mL | 60.9102 mL |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8728 mL | 12.1820 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL | 6.0910 mL | |
| 15 mM | 0.1624 mL | 0.8121 mL | 1.6243 mL | 4.0607 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2182 mL | 3.0455 mL |
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