TP-5801 TFA
Based on 1 Customer Validation
TP-5801 TFA 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: 99.55%
- Formula: C26H32BrF3N8O3
- Molecular Weight:641.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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) TFA treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) TFA 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) TFA 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 luciferase 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 luciferase 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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Appearance Solid
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Molecular Weight 641.48
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Formula C26H32BrF3N8O3
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Color Light yellow to yellow
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SMILES
OC(C(F)(F)F)=O.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
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : 100 mg/mL (155.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (271 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
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5589 mL | 7.7945 mL | 15.5890 mL | 38.9724 mL |
| 5 mM | 0.3118 mL | 1.5589 mL | 3.1178 mL | 7.7945 mL | |
| 10 mM | 0.1559 mL | 0.7794 mL | 1.5589 mL | 3.8972 mL | |
| 15 mM | 0.1039 mL | 0.5196 mL | 1.0393 mL | 2.5982 mL | |
| 20 mM | 0.0779 mL | 0.3897 mL | 0.7794 mL | 1.9486 mL | |
| 25 mM | 0.0624 mL | 0.3118 mL | 0.6236 mL | 1.5589 mL | |
| 30 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2991 mL | |
| 40 mM | 0.0390 mL | 0.1949 mL | 0.3897 mL | 0.9743 mL | |
| 50 mM | 0.0312 mL | 0.1559 mL | 0.3118 mL | 0.7794 mL | |
| 60 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6495 mL | |
| 80 mM | 0.0195 mL | 0.0974 mL | 0.1949 mL | 0.4872 mL | |
| 100 mM | 0.0156 mL | 0.0779 mL | 0.1559 mL | 0.3897 mL |
TP-5801 TFA Related Classifications
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