Vactosertib | EW 7197 | ALK5 Inhibitor | AmBeed-信号通路专用抑制剂

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Vactosertib {[allProObj[0].p_purity_real_show]}

货号：A287741 同义名： EW 7197;TEW-7197

Vactosertib是一种选择性 TGF-β 受体 ALK4 和 ALK5 抑制剂，IC50 分别为 13 nM 和 11 nM。

Vactosertib 化学结构
CAS号：1352608-82-2

Vactosertib 3D分子结构
CAS号：1352608-82-2

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Vactosertib 纯度/质量文件产品仅供科研

货号：A287741 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

转化生长因子-β 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		99%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Vactosertib 生物活性

靶点	TGFβRI/ALK5 ALK5, IC50:11 nM ALK4 ALK4, IC50:13 nM
描述	EW-7197 is a potent and selective ALK5/ALK4 with IC50 values of 13nM/17nM. It inhibited cellular ALK5 activity with IC50 values of 16.5nM and 12.1nM measured by a luciferase assay in HaCaT (3TP-luc) stable cells and 4T1 (3TP-luc) stable cells, respectively^[6]. EW-7197 dose-dependently reduced TGFβ1-induced Smad3 phosphorylation at concentration>30nM in 4T1 cells post 30min, and blocked Smad2/3 nuclear translocation at 1μM. Also it inhibited TGFβ1-induced 4T1 cell migration and invasion as well as inhibited EMT in breast cancer cells. Administration of EW-7197 at doses of 0.625, 1.25, 2.5 and 5mg/kg dose-dependently prolonged the life span of BALB/c 4T1 mice via inhibition of EMT. It inhibited metastasis and enhanced the activity of cytotoxic T lymphocytes in 4T1 orthotopic–grafted mice at dose of 20mg/kg^[7].
作用机制	The [1,2,4]triazolo[1,5-a]pyridin-6-yl moiety of EW-7197 occupies the pocket for adenine ring of ATP and commonly forms a hydrogen bonding with NH of His283 in the backbone of hinge region of ALK5.^[6]

Vactosertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay		Inhibition of human ERG channel expressed in HEK293 cells after 3 to 5.7 mins by whole-cell patch clamp technique, IC50=31.04 μM	24786585
human HaCaT cells		Function assay	24 h	Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=0.0165 μM	24786585
mouse 4T1 cells		Function assay	24 h	Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=0.0121 μM	24786585

Vactosertib 动物研究

Dose

Mice: 2.5 mg/kg^[3] (p.o.); 40 mg/kg^[2] (i.p.) Rat: 20 mg/kg^[4] (p.o.)

Administration

p.o., i.p.

Pharmacokinetics

Animal	Mice^[5]
Dose	10 mg/kg
Administration	p.o.
C_max	625.0 ± 529.7 ng⁄ml
T_1/2	3.26 ± 2.47 h

Vactosertib 参考文献

[1]Jin CH, Krishnaiah M, et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem. 2014 May 22;57(10):4213-38.

[2]Son JY, Park SY, et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis. Mol Cancer Ther. 2014 Jul;13(7):1704-16.

[3]Yoon JH, Jung SM, et al. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol Med. 2013 Nov;5(11):1720-39.

[4]Jun EJ, Park JH, et al. EW-7197, an activin-like kinase 5 inhibitor, suppresses granulation tissue after stent placement in rat esophagus. Gastrointest Endosc. 2017 Jul;86(1):219-228.

[5]Naka K, Ishihara K, et al. Novel oral transforming growth factor-β signaling inhibitor EW-7197 eradicates CML-initiating cells. Cancer Sci. 2016 Feb;107(2):140-8.

[6]Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Lee HJ, Park SJ, Park HJ, Lee K, Sheen YY, Kim DK. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem. 2014 May 22;57(10):4213-38. doi: 10.1021/jm500115w. Epub 2014 May 13. PMID: 24786585.

[7]Son JY, Park SY, Kim SJ, Lee SJ, Park SA, Kim MJ, Kim SW, Kim DK, Nam JS, Sheen YY. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis. Mol Cancer Ther. 2014 Jul;13(7):1704-16. doi: 10.1158/1535-7163.MCT-13-0903. Epub 2014 May 9. PMID: 24817629.

Vactosertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.04mL

5.01mL

2.50mL

Vactosertib 技术信息

CAS号	1352608-82-2
分子式	C₂₂H₁₈FN₇
分子量	399.424

别名	EW 7197;TEW-7197
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(262.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 5%DMSO+40%PEG400+5% tween80+H2O 5 mg/mL clear

Vactosertib {[allProObj[0].p_purity_real_show]}

Vactosertib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Vactosertib 质控信息

Vactosertib 生物活性

Vactosertib 细胞研究

Vactosertib 动物研究

Vactosertib 参考文献

Vactosertib 实验方案

Vactosertib 技术信息

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Vactosertib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Vactosertib 质控信息

Vactosertib 生物活性

Vactosertib 细胞研究

Vactosertib 动物研究

Vactosertib 参考文献

Vactosertib 实验方案

Vactosertib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Vactosertib 纯度/质量文件产品仅供科研