[CAS NO. 1352608-82-2] Vactosertib (TEW-7197)
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PRODUCTS SPECIFICATIONS [1352608-82-2]
Catalog
SLK-S7530
Brand
Selleck
CAS
1352608-82-2
DESCRIPTION [1352608-82-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 399.42 |
| Molecular Formula | C22H18FN7 |
| SMILES | CC1=CC=CC(C2=C(C3=CN4C(C=C3)=NC=N4)N=C(CNC5=CC=CC=C5F)N2)=N1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5036 mL | 12.5182 mL | 25.0363 mL |
| 5 mM | 0.5007 mL | 2.5036 mL | 5.0073 mL |
| 10 mM | 0.2504 mL | 1.2518 mL | 2.5036 mL |
| 50 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL |
Description
Vactosertib (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable inhibitor with of 13 nM and 11 nM, respectively. Phase 1.
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. [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. 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.
References
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