Vactosertib is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.
| 説明 | Vactosertib is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity. |
| ターゲット＆IC50 | ALK5:11 nM, ALK4:13 nM |
| In vitro | In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. [1] EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. [3] |
| In vivo | In rats, EW-7197 shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. EW-7197 also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. [1] In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. [2] EW-7197 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. [3] |
| キナーゼ試験 | Protein Kinase Assay: A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation. |
| 細胞研究 | Cells are seeded in 96 well plate and treated with indicated concentrations of EW-7197 in 0.2% HI-FBS medium for 72 h. Cells are dried after incubation with 10% TCA in media. Then, cells are incubated with 0.4% SRB (Sulforhodamine B) in 1% acetic acid for 30 min. After washing with 1% glacial acetic acid, bounded dye is released in 10 mM Tris buffer (pH 10.5) for 30 min. Absorbance is measured at 570 nm. (Only for Reference) |
| 別名 | TEW-7197, EW-7197 |
| 分子量 | 399.42 |
| 分子式 | C22H18FN7 |
| CAS No. | 1352608-82-2 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: <1 mg/mL
Ethanol: 40 mg/mL (100.1 mM)
DMSO: 73 mg/mL (182.8 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
参考文献引用文献
投与量変換You can also refer to dose conversion for different animals. 詳細
In vivo投与量計算 (透明溶液)計算器bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Vactosertib 1352608-82-2 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad antimetastatic invasion Smad TEW7197 Transforming growth factor beta receptors TGFβ migration TGF-β Receptor breast TEW-7197 TEW 7197 inhibit cell EW 7197 cancer EW7197 survival Inhibitor p38α EW-7197 inhibitor
