2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. TL4830031

TL4830031 (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。

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TL4830031 Chemical Structure

TL4830031 Chemical Structure

CAS No. : 2084107-15-1

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规格 价格 是否有货 数量
1 mg ￥3920
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Customer Review

TL4830031 相关抗体

Top Publications Citing Use of Products

查看 TAM Receptor 亚型特异性产品:

查看所有亚型
Axl Mer Tyro3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

Axl

 

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TL4830031 相关抗体:

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.
体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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: 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
分子量

657.66

Formula

C35H33F2N5O6
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 2.38 mg/mL (3.62 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5205 mL 7.6027 mL 15.2054 mL
5 mM --- --- ---
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥98.0%

COA (267 KB) HNMR (309 KB)

产品使用指南 (1538 KB)
参考文献

TL4830031 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5205 mL 7.6027 mL 15.2054 mL 38.0136 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TL48300312084107-15-1TL 4830031TL-4830031TAM ReceptorTyro3AxlMerquinolonesselective inhibitorbreast canceranticancerphosphorylationcell invasioncell migrationInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-150041
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