化合物 T15262 T15262

Product Introduction
Bioactivity


英文名: Vactosertib Hydrochloride

描述: Vactosertib Hydrochloride is an orally active and ATP-competitive ALK5 inhibitor (IC50: 12.9 nM). It has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50: 17.3 nM).

体外活性: Vactosertib inhibits the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells (IC50: 10-30 nM for Vactosertib on pSmad3 in 4T1 cells). 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 abrogates TGFb1-induced tumor cell migration and invasion. Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT) [1].

体内活性: Vactosertib inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Vactosertib (40 mg/kg; i.p.; 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 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 50 mg/mL (114.71 mM)
DMSO : 50 mg/mL (114.71 mM)


关键字: EW 7197 Hydrochloride | EW7197 Hydrochloride | TEW 7197 Hydrochloride | Vactosertib Hydrochloride | TEW7197 Hydrochloride

相关产品: CEP-28122 mesylate salt (1022958-60-6 free base) | Vactosertib | TGFBR1-IN-1 | Blu-782 | A 83-01 | R-268712 | SB 525334 | LDN-212854 | 6-Demethoxytangeretin | Repotrectinib

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途