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| 品牌 | absin | CAS | 1352608-82-2 |
|---|---|---|---|
| 分子式 | C22H18FN7 | 纯度 | 98% |
| 分子量 | 399.42 | 货号 | abs47028325 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a highly potent, selective | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
EW-7197 1352608-82-2
| 产品描述 | |
| 描述 | EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | Vactosertib |
| 外观 | White to Light Yellow Solid |
| 可溶性/溶解性 | DMSO : 60 mg/mL (150.22 mM) |
| 生物活性 | |
| 靶点 | ALK5；ALK4 |
| In vitro(体外研究) | In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. |
| In vivo(体内研究) | In rats, EW-7197 shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. EW-7197 also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. EW-7197 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. |
| 参考文献 | |
| 参考文献 |
| 研究领域 | |
| 研究领域 | CancerCancer MetabolismResponse to hypoxia MetabolismPathways and ProcessesMetabolism processesHypoxia NeuroscienceDevelopment Stem CellsSignaling PathwaysTGF betaSurface Molecules Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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