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Vactosertib

CAS No. : 1352608-82-2

MCE 站：Vactosertib

产品活性：Vactosertib (EW-7197) 是一种有效的，具有口服活性且具有 ATP 竞争性激活素受体样激酶 5 (ALK5) 抑制剂，IC₅₀ 为 12.9 nM。Vactosertib 还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC₅₀ 为 17.3 nM)。Vactosertib 具有强大的抗转移活性和抗癌作用。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

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.

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