受注:045-509-1970 |
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Synonyms | EW-7197 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H18FN7 |
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分子量 | 399.42 | CAS No. | 1352608-82-2 | |
Solubility (25°C)* | 体外 | DMSO | 79 mg/mL (197.78 mM) | |
Ethanol | 79 mg/mL (197.78 mM) | |||
Water | Insoluble | |||
* <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. |
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. |
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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] |
キナーゼアッセイ | Protein Kinase Assay | |
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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. |
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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. |
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Data from [Data independently produced by , , Lab Invest, 2017, 97(3):232-242]
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 |
TGFβR-1/ALK5 inhibitor RepSox induces enteric glia-to-neuron transition and influences gastrointestinal mobility in adult mice [ Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4] | PubMed: 35794374 |
Inhibitors of Activin Receptor-like Kinase 5 Interfere with SARS-CoV-2 S-Protein Processing and Spike-Mediated Cell Fusion via Attenuation of Furin Expression [ Viruses, 2022, 14(6)1308] | PubMed: 35746781 |
Dysregulated myokines and signaling pathways in skeletal muscle dysfunction in a cigarette smoke-induced model of chronic obstructive pulmonary disease [ Front Physiol, 2022, 13:929926] | PubMed: 36091368 |
Myostatin/HIF2α-Mediated Ferroptosis is Involved in Skeletal Muscle Dysfunction in Chronic Obstructive Pulmonary Disease [ Int J Chron Obstruct Pulmon Dis, 2022, 17:2383-2399] | PubMed: 36185172 |
Three subtypes of lung cancer fibroblasts define distinct therapeutic paradigms [ Cancer Cell, 2021, S1535-6108(21)00492-X] | PubMed: 34624218 |
Microglial identity and inflammatory responses are controlled by the combined effects of neurons and astrocytes [ Cell Rep, 2021, 34(12):108882] | PubMed: 33761343 |
Facile discovery of a therapeutic agent for NK-mediated synergistic antitumor effects using a patient-derived 3D platform [ Biomater Sci, 2021, 10.1039/d1bm01699g] | PubMed: 34940764 |
Photobiomodulation Promotes Repair Following Spinal Cord Injury by Regulating the Transformation of A1/A2 Reactive Astrocytes [ Front Neurosci, 2021, 15:768262] | PubMed: 34795557 |
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。