All AbMole products are for research use only, cannot be used for human consumption.
Vactosertib (EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively.
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. 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.
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. 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. 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.
| Cell Experiment | |
|---|---|
| Cell lines | 4T1 and MCF10A cells |
| Preparation method | 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. |
| Concentrations | ~5 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mouse B16 melanoma model |
| Formulation | Artificial gastric fluid formulation (vehicle; ddH2O 900 mL, conc. HCl 7 mL, NaCl 2.0 g, pepsin 3.2 g). |
| Dosages | 2.5 mg/kg daily |
| Administration | p.o. |
| Molecular Weight | 399.42 |
| Formula | C22H18FN7 |
| CAS Number | 1352608-82-2 |
| Solubility (25°C) | DMSO 79 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related TGF-β Receptor Products |
|---|
| LY2157299
LY2157299 (Galunisertib) is a novel clinically relevant TBRI (ALK5 kinase) inhibitor with IC50 of 56 nM. |
| GW788388
GW788388 is a potent selective inhibitor of TGF-beta type I receptor and ALK5 with IC50 values of 0.093 and 0.018 μM. |
| LY364947
LY364947 is a selective small molecule inhibitor of the TGFβ type I receptor kinase with IC50 of 59 nM. |
| LY2109761
LY2109761 is a novel TGF-β receptor type I and type II dual inhibitor, with Ki values of 38 nM and 300 nM, respectively. |
| SB-525334
SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 of 14.3 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
