2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. WRG-28

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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WRG-28 Chemical Structure

WRG-28 Chemical Structure

CAS No. : 1913291-02-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 52 In-stock
5 mg USD 110 In-stock
10 mg USD 180 In-stock
25 mg USD 380 In-stock
50 mg USD 640 In-stock
100 mg USD 1050 In-stock
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Based on 1 publication(s) in Google Scholar

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DDR1 DDR2

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Description

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[1][2].

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.

WRG-28 Related Antibodies

Cell Viability Assay[1]

Cell Line: HEK293 cells (transfected with DDR2-Flag)
Concentration: 0.25, 0.5, 1, 2 µM
Incubation Time: 4 h
Result: Significantly inhibited collagen I-mediated DDR2 tyrosine phosphorylation at 1 or 2µM, and with an IC>sub>50 of 286 nM.

Cell Viability Assay[1]

Cell Line: HEK293 cells (transfected with DDR2-Flag)
Concentration: 1 µM
Incubation Time: 7 h
Result: Inhibited collagen I-mediated ERK activation and SNAIL1 protein stabilization (IC50=286 nM).

Cell Viability Assay[1]

Cell Line: BT549 and 4T1 breast cancer cells (expressing endogenous DDR2)
Concentration: 1 μM
Incubation Time: 48 h
Result: Inhibited DDR2 induced invasion and migration of tumor cells.

Cell Viability Assay[1]

Cell Line: CAF cells (with tumor organoids)
Concentration: 1 μM
Incubation Time: 4 days
Result: Inhibited the activity of DDR2 that supported invasion of primary tumor organoids in CAFs.

Cell Viability Assay[1]

Cell Line: HEK293 cells (expressing DDR2T654I)
Concentration: 0.5, 1 μM
Incubation Time: 4 h
Result: Inhibited phosphorylation of the DDR2T654I mutant in response to collagen I.
In Vivo

WRG-28 (10 mg/kg; i.v.; single) attenuates biochemical signaling of DDR2 in breast tumors in vivo[1].
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.

Animal Model: Female BALB/cJ mice (8-week-old; 4T1-Snail-CBG tumor-bearing mice model)[1].
Dosage: 10 mg/kg
Administration: Intravenous injection, single.
Result: Reduced 60% SNAIL1-clic beetle green (SNAIL1.CBG) level within the tumor in mice.
Animal Model: Female BALB/cJ mice (8-week-old; injected with 4T1 GFP-luc expressing cells)[1].
Dosage: 10 mg/kg
Administration: Intravenous injection, single daily for 7 days.
Result: Reduced lung colonization to a level comparable to shDDR2-depleted cells.
Animal Model: Male DBA/1 mice (8-week-old; CAIA model)[2].
Dosage: 10 mg/kg
Administration: Intravenous injection, single daily for 21 days.
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.
Molecular Weight

410.44

Formula

C21H18N2O5S
CAS No.
Appearance

Solid

Color

Pink to red

SMILES

O=S(C1=CC=C(COC2=CC(OC3=CC(C=CC3=N4)=O)=C4C=C2)C=C1)(NCC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4364 mL 12.1820 mL 24.3641 mL
5 mM 0.4873 mL 2.4364 mL 4.8728 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

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

    Solubility: ≥ 1.56 mg/mL (3.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.56 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.34%

SDS (251 KB)

COA (246 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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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WRG-28 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WRG-281913291-02-7WRG28WRG 28Discoidin Domain Receptorbreast cancerHEK293BT5494T1 breast cancer cellsCAFsrheumatoid arthritisjoint destructionInhibitorinhibitorinhibit

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