Vactosertib Hydrochloride

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC 50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 ( IC 50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect 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 IC 50 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: 4T1 cells Concentration: 10 nM, 30 µM, 50 nM, 100 µM, 300 nM, 500 nM, 1000 nM Incubation Time: 30 minutes Result: Blocked the TGFb-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mammary tumor virus (MMTV)/c-Neu female mice (32-week-old) Dosage: 40 mg/kg Administration: Intraperitoneal injection; every other day; for 10 weeks Result: Inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice. IC50& Target:ALK5 12.9 nM (IC 50 )

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