EW-7197
- CAS No.
- 1352608-82-2
- Chemical Name:
- EW-7197
- Synonyms
- EW-7197;EW-7179;CPD3325;CS-2288;CS-2287;TEW-7197;NOV-1301;CPD3325-A5;Vactosertib;EW-7197 (EW7197
- CBNumber:
- CB42729651
- Molecular Formula:
- C22H18FN7
- Molecular Weight:
- 399.42
- MDL Number:
- MFCD28348363
- MOL File:
- 1352608-82-2.mol
- MSDS File:
- SDS
| Melting point | >85oC (dec.) |
|---|---|
| Density | 1.40±0.1 g/cm3(Predicted) |
| storage temp. | Refrigerator |
| solubility | DMSO (Slightly), Methanol (Slightly) |
| pka | 8.51±0.10(Predicted) |
| form | Solid |
| color | Pale Yellow to Light Yellow |
| FDA UNII | 6T4O391P5Y |
| NCI Drug Dictionary | vactosertib |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
EW-7197 price More Price(26)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 19231 | EW-7197 ≥98% | 1352608-82-2 | 1mg | $121 | 2024-03-01 | Buy |
| Cayman Chemical | 19231 | EW-7197 ≥98% | 1352608-82-2 | 5mg | $230 | 2024-03-01 | Buy |
| Cayman Chemical | 19231 | EW-7197 ≥98% | 1352608-82-2 | 10mg | $362 | 2024-03-01 | Buy |
| TRC | E950000 | EW7197 | 1352608-82-2 | 100mg | $945 | 2021-12-16 | Buy |
| AK Scientific | 2408AH | EW-7197 | 1352608-82-2 | 100mg | $967 | 2021-12-16 | Buy |
EW-7197 Chemical Properties,Uses,Production
Description
EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM). It also inhibits ALK2 and ALK4 at nanomolar concentrations. EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice. It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells. EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.
Description
EW-7197 is a novel ALK-5 kinase inhibitor as well as TGF-β Type I Receptor Kinase Inhibitor. Study has shown that it can potently inhibit the breast to lung metastasis. Mice study has demonstrated that EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice and 4T1 orthotopic-grafted mice. EW-7197 also inhibited the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, EW-7197 enhanced cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. It can also inhibit hepatic, renal, and pulmonary fibrosis by blocking TGF-β/Smad and ROS signaling. Therefore, it is a potential antitumor reagent.
Uses
EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor.
in vitro
ew-7197 inhibited alk5 with ic50 value of 0.013 μm in a kinase assay and with ic50 values of 0.0165 and 0.0121 μm in hacat stable cells and 4t1 stable cells, respectively, in a luciferase assay. selectivity profiling of ew-7197 using a panel of protein kinases revealed that it is a highly selective alk5/alk4 inhibitor [1].
in vivo
ew-7197 inhibited smad/tgf-βsignaling, invasion, cell migration, and lung metastasis in mmtv/c-neu mice and 4t1 orthotopic–grafted mice. ew-7197 inhibited the epithelial-to-mesenchymal transition in both tgf-β-treated breast cancer cells and 4t1 orthotopic–grafted mice as well[2].
IC 50
0.013 μm
References
Park, S. A., et al. "EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-β/Smad and ROS signaling." Cellular & Molecular Life Sciences 72.10(2015):2023-2039.
Kim, Min Jin, et al. "TGF-β Type I Receptor Kinase Inhibitor EW-7197 Suppresses Cholestatic Liver Fibrosis by Inhibiting HIF1α-Induced Epithelial Mesenchymal Transition." Cellular Physiology & Biochemistry International Journal of Experimental Cellular Physiology Biochemistry & Pharmacology 38.2(2016):571.
Son, J. Y., et al. "EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis." Molecular Cancer Therapeutics13.7(2014):1704.
EW-7197 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Accela ChemBio Inc. | (+1)-858-699-3322 | info@accelachem.com | United States | 19965 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29016 | 58 |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9635 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| Supplier | Advantage |
|---|---|
| ATK CHEMICAL COMPANY LIMITED | 60 |
| Accela ChemBio Inc. | 58 |
| Hubei xin bonus chemical co. LTD | 58 |
| BOC Sciences | 58 |
| Career Henan Chemica Co | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 58 |
| Dideu Industries Group Limited | 58 |
| Finetech Industry Limited | 58 |
| InvivoChem | 58 |
| LEAP CHEM CO., LTD. | 58 |