TL4830031
Based on 1 Customer Validation
TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.
For research use only. We do not sell to patients.
- Purity: ≥98.0%
- CAS No.: 2084107-15-1
- Formula: C35H33F2N5O6
- Molecular Weight:657.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Axl |
TL4830031 (compound 8i) binds to Axl with a Kd value of 1.1 nM. TL4830031 exhibits a 25 fold less potency against Mer with a Kd value of 25 nM, while it is much less potent to Tyro3 with a Kd value of 750 nM[1].
TL4830031 (0-5000 nM; 4 h; MDA-MB-231 cells) inhibits the phosphorylation of Axl (pAxl (Tyr702)) and the downstream Akt(pAkt(Thr308)) in a dose-dependent manner[1].
TL4830031 (0-5000 nM; 4 h) reverses the expression of the EMT markers induced by TGF-β1 in MDA-MB-231 cells[1].
TL4830031 (0-5000 nM; 24 h) suppresses migration and invasion of MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 8, 40, 200, 1000 and 5000 nM
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Incubation Time:4 hours
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Result:Inhibited the phosphorylation of Axl (pAxl (Tyr702)) and the downstream Akt (pAkt(Thr308)) at a low concentration.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 40, 200, 1000 and 5000 nM
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Incubation Time:4 hours
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Result:Increased the expression of epithelial marker E-cadherin and decreased the expression of mesenchymal marker N-cadherin in MDA-MB-231 cells.
TL4830031 (2.5-50 mg/kg; p.o. and i.v.; SD rats) exhibits reasonable pharmacokinetic (PK) properties with an AUC0-∞ value of 25944.7 μg/mL·h and a T1/2 value of 5.68 h at an oral dose of 25 mg/kg. The Cmax (2386.9 µg/L=3.6 µM) occurred at 4.0 h postdose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[1]
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Dosage:0, 50, 100, 200, 400, 600 and 800 mg/kg
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Administration:Oral administration; daily, for 7 days
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Result:Had toxicity to liver and kidney at 200 mg/kg, 400 mg/kg and 800 mg/kg administration.
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Animal Model:SD rats[1]
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Dosage:2.5 and 25 mg/kg
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Administration:Oral administration (2.5 mg/kg) and intravenous injection (25 mg/kg)
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Result:
1.19 Administration p.o. (25 mg/kg) i.v. (2.5 mg/kg) AUC0-∞ (μg/mL·h) 25944.7 20680.6 Cmax (ng/mL) 2386.9 4358.2 T1/2 (h) 5.68 4.26 Tmax (h) 4.0 CLz (L/h/kg) 0.12 BA (%) 12.5
Chemical Information
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CAS No. 2084107-15-1
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Appearance Solid
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Molecular Weight 657.66
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Formula C35H33F2N5O6
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Color White to off-white
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SMILES
O=C(C1=CN2C3=C(CCC2C)C(N4CCC(CC4)O)=C(F)C=C3C1=O)NC5=CC=C(C(F)=C5)OC6=NC=NC7=C6C=C(OC)C(OC)=C7
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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 : 2.38 mg/mL (3.62 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; 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)
- Korean - KR (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 | 1.5205 mL | 7.6027 mL | 15.2054 mL | 38.0136 mL |
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