WRG-28
- Product Name
- WRG-28
- CAS No.
- 1913291-02-7
- Chemical Name
- WRG-28
- Synonyms
- WRG-28;WRG-28, 10 mM in DMSO;WRG-28 (DDR2 inhibitor WRG-28;N-Ethyl-4-[[(3-oxo-3H-phenoxazin-7-yl)oxy]methyl]benzenesulfonamide;Benzenesulfonamide, N-ethyl-4-[[(3-oxo-3H-phenoxazin-7-yl)oxy]methyl]-;WRG28,4T1 breast cancer cells,WRG-28,joint destruction,breast cancer,Discoidin Domain Receptor,BT549,CAFs,HEK293,Inhibitor,inhibit,rheumatoid arthritis,WRG 28
- CBNumber
- CB45848795
- Molecular Formula
- C21H18N2O5S
- Formula Weight
- 410.44
- MOL File
- 1913291-02-7.mol
WRG-28 Property
- Boiling point:
- 603.4±65.0 °C(Predicted)
- Density
- 1.38±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 15.62 mg/mL (38.06 mM)
- pka
- 11.55±0.50(Predicted)
- form
- Solid
- color
- Pink to red
N-Bromosuccinimide Price
- Product number
- CS-0078189
- Product name
- WRG-28
- Purity
- 99.42%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0078189
- Product name
- WRG-28
- Purity
- 99.42%
- Packaging
- 10mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0078189
- Product name
- WRG-28
- Purity
- 99.42%
- Packaging
- 25mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0078189
- Product name
- WRG-28
- Purity
- 99.42%
- Packaging
- 50mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- CS-0078189
- Product name
- WRG-28
- Purity
- 99.42%
- Packaging
- 100mg
- Price
- $1650
- Updated
- 2021/12/16
WRG-28 Chemical Properties,Usage,Production
Uses
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].
Biological Activity
WRG-28 is a potent, selective and extracellularly acting allosteric inhibitor of discoidin domain receptor 2 (DDR2) th at potently inhibits invasion and migration in mice model of breast cancer. WRG-28 inhibits metastatic breast tumor cell colonization in the lungs.
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].
| 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. |
IC 50
DDR2: 230 nM (IC50)
References
[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. DOI:10.1073/pnas.1805020115
[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. DOI:10.1002/art.41205
WRG-28 Preparation Products And Raw materials
Raw materials
Preparation Products
WRG-28 Suppliers
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 021-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2989
- Advantage
- 58
- Tel
- 010-50973130 18101056239
- 3193328036@qq.com
- Country
- China
- ProdList
- 29760
- Advantage
- 68
- Tel
- 400-6387771-6039 18920764717
- sales@heowns.com
- Country
- China
- ProdList
- 23771
- Advantage
- 60
- Tel
- 0755-23251735 13302967066
- sales@geneseqtools.com
- Country
- China
- ProdList
- 1420
- Advantage
- 58
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- 86-571-88216897,88216896 13588875226
- Fax
- 86-571-88216895
- sales@hzclap.com
- Country
- CHINA
- ProdList
- 6312
- Advantage
- 58
- Tel
- 021-58521787 17701827760
- starpharmsh@gmail.com
- Country
- China
- ProdList
- 292
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 88888888888
- hongquchem@qq.com
- Country
- China
- ProdList
- 5132
- Advantage
- 58