TL4830031
目录号 : GC67878TL4830031 (compound 8i) 是一种喹诺酮类抗生素衍生物，是一种有效的 Axl 抑制剂，其 IC50 值为 26 nM。TL4830031 抑制 Axl 的磷酸化。TL4830031 抑制细胞侵袭和迁移。TL4830031 可用于癌症研究。
Cas No.:2084107-15-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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[1].
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].
Western Blot Analysis[1]
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 0, 8, 40, 200, 1000 and 5000 nM |
| Incubation Time: | 4 hours |
| Result: | Inhibited the phosphorylation of Axl (pAxl (Tyr702)) and the downstream Akt (pAkt(Thr308)) at a low concentration. |
Western Blot Analysis[1]
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 0, 40, 200, 1000 and 5000 nM |
| Incubation Time: | 4 hours |
| Result: | Increased the expression of epithelial marker E-cadherin and decreased the expression of mesenchymal marker N-cadherin in MDA-MB-231 cells. |
TL4830031 (compound 8i) (0-800 mg/kg; p.o.; daily, for 7 d; ICR mice) has toxicity to liver and kidney in ICR mice[1].
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].
| Animal Model: | ICR mice[1] |
| Dosage: | 0, 50, 100, 200, 400, 600 and 800 mg/kg |
| Administration: | Oral administration; daily, for 7 days |
| Result: | Had toxicity to liver and kidney at 200 mg/kg, 400 mg/kg and 800 mg/kg administration. |
| Animal Model: | SD rats[1] | |||||||||||||||||||||
| Dosage: | 2.5 and 25 mg/kg | |||||||||||||||||||||
| Administration: | Oral administration (2.5 mg/kg) and intravenous injection (25 mg/kg) | |||||||||||||||||||||
| Result: |
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[1]. Tan L, et, al. Quinolone antibiotic derivatives as new selective Axl kinase inhibitors. Eur J Med Chem. 2019 Mar 15;166:318-327.
| Cas No. | 2084107-15-1 | SDF | Download SDF |
| 分子式 | C35H33F2N5O6 | 分子量 | 657.66 |
| 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) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5205 mL | 7.6027 mL | 15.2054 mL |
| 5 mM | 0.3041 mL | 1.5205 mL | 3.0411 mL |
| 10 mM | 0.1521 mL | 0.7603 mL | 1.5205 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。