EW-7195

CAS: 1352609-28-9 货号: E654953 分子式: C23H18N8 分子量: 406.44
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
E654953-1ml
期货 Stock Image
¥4,400.90
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概述


EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC 50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α . EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung

In Vitro

EW7195 inhibits the EMT, motility, and invasiveness of breast cancer cells in vitro. EW-7195 efficiently blocks TGF-β1-induced phosphorylation of Smad2 followed by the nuclear translocation of Smad2/3. EW-7195 blocks TGF-β1-induced mesenchymal morphology. EW-7195 inhibits TGF-β-induced transcriptional activation. EW-7195 (0.5-1 µM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EW7195 (40 mg/kg; i.p.; three times a week for 3/2.5 weeks) inhibits lung metastasis development in both 4T1 orthotopic xenograft and MMTV/cNeu transgenic mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MMTV/c-Neu mice Dosage: 40 mg/kg Administration: I.p.; three times a week for 3 weeks Result: Inhibited the metastasis of breast cancer cells to the lung. Animal Model: Balb/c xenograft model (10-weeks-old female Balb/c mice bearing 4T1 cells) Dosage: 40 mg/kg Administration: I.p.; three times a week for 2.5 weeks Result: Suppressed a lung metastasis in the Balb/c Xenograft model.

IC50& Target:ALK5 4.83 nM (IC 50 ) p38α 1.5 μM (IC 50 )

规格

规格或纯度
10mM in DMSO
英文名称
EW-7195
生化机理
EW-7195 是一种强效、选择性 ALK5(TGFβR1)抑制剂,其 IC 50 为 4.83 nM。与 p38α 相比,EW-7195 对 ALK5 的选择性大于 300 倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮细胞向间质转化(EMT)和乳腺癌的发生。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
分子量
406.44

高级数据

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