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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: ≥98.0%
- CAS 番号: 2084107-15-1
- 分子式: C35H33F2N5O6
- 分子量:657.66
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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
化学情報
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CAS 番号 2084107-15-1
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性状 Solid
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分子量 657.66
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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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