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.
For research use only. We do not sell to patients.
- Purity: 98.55%
- CAS No.: 2574474-81-8
- Formula: C24H31BrN8O
- Molecular Weight:527.46
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Storage:
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)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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.
Chemical Information
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CAS No. 2574474-81-8
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Appearance Solid
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Molecular Weight 527.46
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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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 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 |
TP-5801 Related Classifications
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