EW-7195
Based on 1 publication(s) in Google Scholar
EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
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- 純度: 98.84%
- CAS 番号: 1352609-28-9
- 分子式: C23H18N8
- 分子量:406.44
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 EW-7195
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生物活性
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ALK5 4.83 nM (IC50) |
p38α 1.5 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.005 μM
Compound: 12z
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Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay
Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay
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[PMID: 24786585] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MMTV/c-Neu mice[1]
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Dosage:40 mg/kg
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Administration:I.p.; three times a week for 3 weeks
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Result:Inhibited the metastasis of breast cancer cells to the lung.
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Animal Model:Balb/c xenograft model (10-weeks-old female Balb/c mice bearing 4T1 cells)[1]
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Dosage:40 mg/kg
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Administration:I.p.; three times a week for 2.5 weeks
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Result:Suppressed a lung metastasis in the Balb/c Xenograft model.
化学情報
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CAS 番号 1352609-28-9
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性状 Solid
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分子量 406.44
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分子式 C23H18N8
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Color Off-white to light yellow
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SMILES
N#CC1=CC=CC(NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Cell Endocrinol
SIK1 drives lipid-induced insulin resistance in skeletal muscle by linking TGFβ1-Smad2/3 activation to PDE4-cAMP dysregulation. [Abstract]2026 Jul:617:112788. PMID: 41856198
溶剤 & 溶解度
DMSO : 50 mg/mL (123.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4604 mL | 12.3019 mL | 24.6039 mL | 61.5097 mL |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9208 mL | 12.3019 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 mL | 6.1510 mL | |
| 15 mM | 0.1640 mL | 0.8201 mL | 1.6403 mL | 4.1006 mL | |
| 20 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 3.0755 mL | |
| 25 mM | 0.0984 mL | 0.4921 mL | 0.9842 mL | 2.4604 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8201 mL | 2.0503 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6151 mL | 1.5377 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4921 mL | 1.2302 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4101 mL | 1.0252 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7689 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6151 mL |