EW-7195

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EW-7195 

EW-7195 是一种有效的、选择性 ALK5 (TGFβR1) 抑制剂，IC50 为 4.83 nM。EW-7195 对 ALK5 的选择性是 p38α 的 300 多倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移。

EW-7195

EW-7195 Chemical Structure

CAS No. : 1352609-28-9

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生物活性

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 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[1].

IC50 & Target[1]

ALK5

4.83 nM (IC50)

p38α

1.5 μM (IC50)

体外研究
(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[1].
EW-7195 (0.5-1 µM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MMTV/c-Neu mice[1]
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)[1]
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.

分子量

406.44

Formula

C23H18N8
CAS 号

1352609-28-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Park CY, et al. EW-7195, a novel inhibitor of ALK5 kinase inhibits EMT and breast cancer metastasis to lung. Eur J Cancer. 2011;47(17):2642-2653.

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