Targefrin
Based on 1 Customer Validation
Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines.
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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: 99.80%
- CAS 番号: 3031514-44-7
- 分子式: C85H116F3N19O15
- 分子量:1700.94
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells[1].
Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC3 cells (starved for 1 h and pre-treated with Targefrin for 20 min, followed by a combination treatment with 2 μg/mL ephrinA1-Fc for 3 h)
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Concentration:0.025, 0.25, 0.5, 1, 2.5, 5, 7.5 and 10 μM
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Incubation Time:20 min
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Result:Effectively antagonized EphA2 degradation induced by the potent ephrinA1-Fc ligand, with an approximate EC50 of ~1.6 μM.
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Cell Line:BxPC3 cells
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Concentration:2, 4, 5 and 10 μM
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Incubation Time:24 h
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Result:Significantly inhibited pancreatic cancer cell migration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nu/nu mice (injected with MIA PaCa-2 cells)[1]
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Dosage:50 mg/kg
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Administration:i.v.; at day 1, 4, 8, 11 and 15
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Result:Both Targefrin-Paclitaxel and Targefrin-dimer-Paclitaxel displayed a significant antitumor effect compared to both the untreated group and the Paclitaxel-treated group.
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Animal Model:Balb/C mice[1]
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Dosage:50 mg/kg
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Administration:IV via tail vein; single dosage
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Result:Cmax ~650 ng/mL after 2 hours from the injection; estimated t1/2 ~15 hr.
化学情報
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CAS 番号 3031514-44-7
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性状 Solid
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分子量 1700.94
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分子式 C85H116F3N19O15
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Color White to off-white
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 100 mg/mL (58.79 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). 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). 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 (282 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). 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 | 0.5879 mL | 2.9396 mL | 5.8791 mL | 14.6978 mL |
| 5 mM | 0.1176 mL | 0.5879 mL | 1.1758 mL | 2.9396 mL | |
| 10 mM | 0.0588 mL | 0.2940 mL | 0.5879 mL | 1.4698 mL | |
| 15 mM | 0.0392 mL | 0.1960 mL | 0.3919 mL | 0.9799 mL | |
| 20 mM | 0.0294 mL | 0.1470 mL | 0.2940 mL | 0.7349 mL | |
| 25 mM | 0.0235 mL | 0.1176 mL | 0.2352 mL | 0.5879 mL | |
| 30 mM | 0.0196 mL | 0.0980 mL | 0.1960 mL | 0.4899 mL | |
| 40 mM | 0.0147 mL | 0.0735 mL | 0.1470 mL | 0.3674 mL | |
| 50 mM | 0.0118 mL | 0.0588 mL | 0.1176 mL | 0.2940 mL |
Targefrin 関連分類
HY-P3717 関連分類
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