EW-7195

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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。

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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 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℃, 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。