SWTX-143
Based on 1 Customer Validation
SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.29%
- CAS 番号: 2766575-48-6
- 分子式: C19H18F3N3O
- 分子量:361.36
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
YAP アイソフォーム固有の製品をすべて表示
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生物活性
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YAP/TAZ-TEAD |
SWTX-143 (5-207 nM, 6 days) inhibits the proliferation of NF2-deficient mesothelioma cells, with IC50 values ranging from 5 to 207 nM[1].
SWTX-143 (12 nM, 24 hours) selectively inhibits TEAD transcription factor activity in HEK293 cells, with an IC50 of 12 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H226, NCI-H2052, Mero-14 (NF2-deficient mesothelioma cell lines)
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Concentration:5 to 207 nM
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Incubation Time:6 days
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Result:Inhibited proliferation in NF2-deficient mesothelioma cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NF2-deficient human mesothelioma (NCI-H226) xenograft BALB/c nude mice model
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Dosage:10, 25, and 50 mg/kg
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Administration:Oral gavage (p.o.), once daily for 19 days
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Result:Had little effect on tumor volume during the first week of dosing; Resulted in significant dose-dependent reduction in tumor volume observed afterward; Led to no significant weight loss at the end of dosing.
化学情報
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CAS 番号 2766575-48-6
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性状 Solid
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分子量 361.36
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分子式 C19H18F3N3O
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Color White to off-white
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SMILES
O=C(C=C)NC1CC2=C(N)C=CC=C2N(C3=CC=C(C(F)(F)F)C=C3)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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (345.92 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 (275 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 | 2.7673 mL | 13.8366 mL | 27.6732 mL | 69.1831 mL |
| 5 mM | 0.5535 mL | 2.7673 mL | 5.5346 mL | 13.8366 mL | |
| 10 mM | 0.2767 mL | 1.3837 mL | 2.7673 mL | 6.9183 mL | |
| 15 mM | 0.1845 mL | 0.9224 mL | 1.8449 mL | 4.6122 mL | |
| 20 mM | 0.1384 mL | 0.6918 mL | 1.3837 mL | 3.4592 mL | |
| 25 mM | 0.1107 mL | 0.5535 mL | 1.1069 mL | 2.7673 mL | |
| 30 mM | 0.0922 mL | 0.4612 mL | 0.9224 mL | 2.3061 mL | |
| 40 mM | 0.0692 mL | 0.3459 mL | 0.6918 mL | 1.7296 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5535 mL | 1.3837 mL | |
| 60 mM | 0.0461 mL | 0.2306 mL | 0.4612 mL | 1.1531 mL | |
| 80 mM | 0.0346 mL | 0.1730 mL | 0.3459 mL | 0.8648 mL | |
| 100 mM | 0.0277 mL | 0.1384 mL | 0.2767 mL | 0.6918 mL |