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.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 3031514-44-7
- Formula: C85H116F3N19O15
- Molecular Weight:1700.94
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Storage:
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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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CAS No. 3031514-44-7
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Appearance Solid
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Molecular Weight 1700.94
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Formula C85H116F3N19O15
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Color White to off-white
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 |
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