EW-7195,99.20%

产品编号:Bellancom-18766| CAS NO:1352609-28-9| 分子式:C23H18N8| 分子量:406.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-18766
4000.00 杭州 北京(现货)
Bellancom-18766
6800.00 杭州 北京(现货)
Bellancom-18766
13500.00 杭州 北京(现货)

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EW-7195

产品介绍 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。
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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 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.
体内研究

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.

西域 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.
性状Solid
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (123.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4604 mL 12.3019 mL 24.6039 mL
5 mM 0.4921 mL 2.4604 mL 4.9208 mL
10 mM 0.2460 mL 1.2302 mL 2.4604 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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