TP-5801
Based on 1 Customer Validation
TP-5801 is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor 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: 98.55%
- CAS 番号: 2574474-81-8
- 分子式: C24H31BrN8O
- 分子量:527.46
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
生物活性
IC50: 1.40 nM (TNK1)[1]
TP-5801 (10 pM-10 μM; 72 h) treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) inhibits TNK1-dependent L540 cell growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:10 pM-10 μM
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Incubation Time:72 hours
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Result:Inhibited TNK1-driven cell growth with IC50s of 76.78 and 36.95 nM against WT TNK1 and AAA mutant cells, respectively. Inhibited BCR-ABL-driven and IL-3-driven Ba/F3 cell growth with IC50s of 8.5 and 1.2 μM, respectively.
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Cell Line:L540 cells
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Concentration:1, 10, 100, and 1000 nM
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Incubation Time:10 days
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Result:Inhibited TNK1-dependent L540 cell growth at low nM level.
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD/SCID mice injected with Ba/F3 luc cells expressing TNK1 AAA[1]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg; once
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Result:Showed no signs of toxicity and significantly prolonged lifespan.
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Animal Model:NOD/SCID mice implanted subcutaneously with Ba/F3 luc cells expressing TNK1 AAA or BCR-ABL[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; 50 mg/kg; once daily; 7 days
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Result:Reduced phospho-STAT3 in TNK1-driven xenografts at 2 hours post-treatment, and tumor burden in mice xenografted.
化学情報
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CAS 番号 2574474-81-8
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性状 Solid
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分子量 527.46
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分子式 C24H31BrN8O
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Color Light yellow to green yellow
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SMILES
CN1CCN(C2=C(C)C=C(NC3=NC=C(Br)C(NC4=CC=CN=C4N(C)C)=N3)C(OC)=C2)CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 16.67 mg/mL (31.60 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (sealed storage, away from moisture and light). 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 | 1.8959 mL | 9.4794 mL | 18.9588 mL | 47.3970 mL |
| 5 mM | 0.3792 mL | 1.8959 mL | 3.7918 mL | 9.4794 mL | |
| 10 mM | 0.1896 mL | 0.9479 mL | 1.8959 mL | 4.7397 mL | |
| 15 mM | 0.1264 mL | 0.6320 mL | 1.2639 mL | 3.1598 mL | |
| 20 mM | 0.0948 mL | 0.4740 mL | 0.9479 mL | 2.3698 mL | |
| 25 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8959 mL | |
| 30 mM | 0.0632 mL | 0.3160 mL | 0.6320 mL | 1.5799 mL |