Vactosertib (TEW-7197)

製品コードS7530 バッチS753006

印刷

化学情報

Synonyms

EW-7197

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₁₈FN₇

分子量

399.42

CAS No.

1352608-82-2

Solubility (25°C)*

体外

DMSO

80 mg/mL (200.29 mM)

Ethanol

80 mg/mL (200.29 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Vactosertib (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
in vitro	In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. ^[1] EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. ^[3]
in vivo	In rats, EW-7197 shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. EW-7197 also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. [1] In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. ^[2] EW-7197 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Protein Kinase Assay
キナーゼアッセイ	A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation.
細胞アッセイ	細胞株	4T1 and MCF10A cells
	濃度	~5 μM
	反応時間	72 hours
	実験の流れ	Cells are seeded in 96 well plate and treated with indicated concentrations of EW-7197 in 0.2% HI-FBS medium for 72 h. Cells are dried after incubation with 10% TCA in media. Then, cells are incubated with 0.4% SRB (Sulforhodamine B) in 1% acetic acid for 30 min. After washing with 1% glacial acetic acid, bounded dye is released in 10 mM Tris buffer (pH 10.5) for 30 min. Absorbance is measured at 570 nm.
動物実験	動物モデル	Mouse B16 melanoma model
	投薬量	2.5 mg/kg daily
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/24786585/
https://pubmed.ncbi.nlm.nih.gov/24127404/
https://pubmed.ncbi.nlm.nih.gov/24817629/

カスタマーフィードバック

: Data from [Data independently produced by , , Lab Invest, 2017, 97(3):232-242]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The TGFβ type I receptor kinase inhibitor vactosertib in combination with pomalidomide in relapsed/refractory multiple myeloma: a phase 1b trial [ Nat Commun, 2024, 15(1):7388]	PubMed: 39191755
Pre-Clinical Assessment of SAR442257, a CD38/CD3xCD28 Trispecific T Cell Engager in Treatment of Relapsed/Refractory Multiple Myeloma [ Cells, 2024, 13(10)879]	PubMed: 38786100
Pre-Clinical Assessment of SAR442257, a CD38/CD3xCD28 Trispecific T Cell Engager in Treatment of Relapsed/Refractory Multiple Myeloma [ Cells, 2024, 13(10)879]	PubMed: 38786100
A Newly Developed Anti-L1CAM Monoclonal Antibody Targets Small Cell Lung Carcinoma Cells [ Int J Mol Sci, 2024, 25(16)8748]	PubMed: 39201435
Targeting TGF beta receptor 1 in head and neck squamous cell carcinoma [ Oral Dis, 2024, 30(3):1114-1127]	PubMed: 37154295
Development of an automated high-content immunofluorescence assay of pSmads quantification: Proof-of-concept with drugs inhibiting the BMP/TGF-β pathways [ Biotechnol J, 2024, 19(9):e2400007]	PubMed: 39295554
p35 is a Crucial Player in NK-cell Cytotoxicity and TGFβ-mediated NK-cell Dysfunction [ Cancer Res Commun, 2023, 3(5):793-806]	PubMed: 37377891
Using TGF-β1 biology in radioiodine refractory differentiated thyroid cancer to re-establish sodium iodide symporter (NIS) expression using engineered [ University of Munich, 2023, ]	PubMed: None
Development of an automated high-content immuno-fluorescence assay of pSmads quantification: proof-of-concept with drugs inhibiting the BMP/TGFbeta pathways [ bioRxiv, 2023, 10.1101/2023.12.14.571626]	PubMed: none
Vactosertib, a novel TGF-β1 type I receptor kinase inhibitor, improves T-cell fitness: a single-arm, phase 1b trial in relapsed/refractory multiple myeloma [ Res Sq, 2023, rs.3.rs-3112163]	PubMed: 37503043

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。