Vactosertib Hydrochloride (Synonyms: EW-7197 Hydrochloride; TEW-7197 Hydrochloride) |
カタログ番号GC37880 |
バクトセルチブ塩酸塩 (EW-7197 塩酸塩) は、12.9 nM の IC50 を有する強力な経口活性の ATP 競合的アクチビン受容体様キナーゼ 5 (ALK5) 阻害剤です。バクトセルチブ塩酸塩は、ナノモル濃度で ALK2 および ALK4 も阻害します (IC50 は 17.3 nM)。バクトセルチブ塩酸塩は強力な抗転移活性と抗がん効果を有します。
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Cas No.: 1352610-25-3
Sample solution is provided at 25 µL, 10mM.
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM. IC50: 12.9 nM (ALK5)[1]
Kinase assays demonstrate that Vactosertib (EW-7197) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM. The IC50 values of Vactosertib against p38a is 1775 nM. Vactosertib also inhibits ACVR1B/ALK4 and the IC50 value against it is determined to be 17.3 nM. Vactosertib blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells, and MDA-MB-231 cells. Vactosertib suppresses the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells[1]. Vactosertib (EW-7197) treatment also dramatically reduces the colony-forming capacity of CML-MPPs in vitro in a dose-dependent manner[2].
Vactosertib (EW-7197; 40 mg/kg) treatment of MMTV/c-Neu transgenic mice significantly reduces lung metastasis by 60% compare with the control. Treatment with Vactosertib decreases the number of metastatic nodules compare with that in the Veh-treated control group by 53% and 68% (5 and 20 mg/kg). Vactosertib (0.625, 1.25, 2.5, or 5 mg/kg; five times/week) inhibits lung metastasis and increases the survival of 4T1-Luc cells, in a dose-dependent manner. Vactosertib also prolongs the survival of BALB/c mice orthotopically bearing 4T1 tumors by 36% at doses of 2.5 and 5 mg/kg[1].
[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.
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