Vactosertib - CAS:1352608-82-2

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Vactosertib (Synonyms:EW-7197; TEW-7197)

目录号 : KM12952 CAS No. : 1352608-82-2 纯度 : 98%

Vactosertib (EW-7197) 是一种有效的，具有口服活性且具有 ATP 竞争性激活素受体样激酶 5 (ALK5) 抑制剂，IC₅₀ 为 12.9 nM。Vactosertib 还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC₅₀ 为 17.3 nM)。Vactosertib 具有强大的抗转移活性和抗癌作用。

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25mg		In-stock
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500mg	询价	In-stock

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生物活性

Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC₅₀ of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC₅₀ of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.

体外研究

Vactosertib (10-1000 nM; 30 minutes; 4T1 cells) treatment blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells.
Vactosertib suppresses the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells. The IC₅₀ value of Vactosertib on pSmad3 in 4T1 cells is 10-30 nM.
Vactosertib abrogates TGFb1-induced tumor cell migration and invasion.
TGFβ1 downregulated the mRNA level of CDH1 and upregulated the mRNA levels of FN1, HMGA2 (high-mobility group AT-hook 2), SNAI1, and SNAI2 (Snail family zinc finger 1 and 2, respectively). Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT).

Western Blot Analysis

Cell Line:	4T1 cells
Concentration:	10 nM, 30 µM, 50 nM, 100 µM, 300 nM, 500 nM, 1000 nM
Incubation Time:	30 minutes
Result:	Blocked the TGFb-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner.

体内研究

Vactosertib (40 mg/kg; intraperitoneal injection; every other day; for 10 weeks; MMTV/c-Neu female mice) treatment inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice.
Vactosertib also inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, Vactosertib enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice.

Animal Model:	Mammary tumor virus (MMTV)/c-Neu female mice (32-week-old)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; every other day; for 10 weeks
Result:	Inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice.

分子式

C₂₂H₁₈FN₇

分子量

399.42

CAS号

1352608-82-2

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 : 100 mg/mL (250.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5036 mL	12.5182 mL	25.0363 mL
5 mM	0.5007 mL	2.5036 mL	5.0073 mL
10 mM	0.2504 mL	1.2518 mL	2.5036 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.26 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.26 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

临床试验

科研文献

•Cancers. 2020 Jun 30;12(7):1737.

纯度： 98%

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