TP-008
Based on 1 Customer Validation
TP-008, a chemical probe, is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
For research use only. We do not sell to patients.
- Purity: 99.42%
- CAS No.: 1976038-41-1
- Formula: C20H15ClFN5O2
- Molecular Weight:411.82
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: ALK 5[1]
TP-008 at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC50 value of 2.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:50, 150 and 500 mg/kg
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Administration:Oral administation; 50, 150 and 500 mg/kg; 5 days
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Result:Induced cardiovalvulopathy in both the medium and high dose animal groups.
Chemical Information
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CAS No. 1976038-41-1
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Appearance Solid
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Molecular Weight 411.82
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Formula C20H15ClFN5O2
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Color White to off-white
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SMILES
O=C(N)CN(C1=C2C=CN=C1)C(N2C3=CC(C4=CC(Cl)=CC=C4F)=NC=C3C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 9.6 mg/mL (23.31 mM; Need ultrasonic and warming; 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. 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. 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 (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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. 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 | 2.4282 mL | 12.1412 mL | 24.2825 mL | 60.7061 mL |
| 5 mM | 0.4856 mL | 2.4282 mL | 4.8565 mL | 12.1412 mL | |
| 10 mM | 0.2428 mL | 1.2141 mL | 2.4282 mL | 6.0706 mL | |
| 15 mM | 0.1619 mL | 0.8094 mL | 1.6188 mL | 4.0471 mL | |
| 20 mM | 0.1214 mL | 0.6071 mL | 1.2141 mL | 3.0353 mL |