您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > EW-7195
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
EW-7195
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EW-7195图片
CAS NO:1352609-28-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

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 selectiveALK5(TGFβR1)inhibitor with anIC50of 4.83 nM. EW-7195 has >300-fold selectivity forALK5overp38α. 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].

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].

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

性状

Solid

Formula

C23H18N8

CAS 号

1352609-28-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM2.4604 mL12.3019 mL24.6039 mL
5 mM0.4921 mL2.4604 mL4.9208 mL
10 mM0.2460 mL1.2302 mL2.4604 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。