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Vactosertib HCl salt form · salt · Parent EW-7197 · Synonyms: EW-7197 Hydrochloride | TEW-7197 Hydrochloride

Vactosertib Hydrochloride is a potent, orally active and ATP-competitive activin receptor-like kinase 5 inhibitor.

For research use only. Not for human or veterinary use.

Target TGF-β Receptor
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

Vactosertib HCl structure

CAS No.: 1352610-25-3

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 420.00 BP-01874A-250mg In stock Get quote
500 mg USD 680.00 BP-01874A-500mg In stock Get quote
1 g USD 1,150.00 BP-01874A-1g In stock Get quote
5 g Inquire BP-01874A-5g Inquire Inquire

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Description

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.

Biological activity

In Vitro Vactosertib (10-1000 nM; 30 minutes; 4T1 cells) treatment blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells. Vactosertib suppresses the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells. The IC50 value of Vactosertib on pSmad3 in 4T1 cells is 10-30 nM. Vactosertib abrogates TGFb1-induced tumor cell migration and invasion. TGFβ1 downregulated the mRNA level of CDH1 and upregulated the mRNA levels of FN1, HMGA2 (high-mobility group AT-hook 2), SNAI1, and SNAI2 (Snail family zinc finger 1 and 2, respectively). Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT). In Vivo Vactosertib (40 mg/kg; intraperitoneal injection; every other day; for 10 weeks; MMTV/c-Neu female mice) treatment inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice. Vactosertib also inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, Vactosertib enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice.

Identifiers

SMILES
CC1=CC=CC(C2=C(C3=CN4C(C=C3)=NC=N4)NC(CNC5=CC=CC=C5F)=N2)=N1.Cl
InChIKey
UDRJLVATGDHMJM-UHFFFAOYSA-N

Specifications

MW (average)
435.8850
Formula
C22H19ClFN7
CAS No.
1352610-25-3
Physical state
Solid
Color
light yellow to yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
-20°C, stored under nitrogen, away from moisture

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[1]. Son JY, et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis. Mol Cancer Ther. 2014 Jul;13(7):1704-16.
[2]. Naka K, et al. Novel oral transforming growth factor-β signaling inhibitor EW-7197 eradicates CML-initiating cells. Cancer Sci. 2016 Feb;107(2):140-8.

Same target

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Same research area

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