TL4830031|cas:2084107-15-1|西域试剂

TL4830031,98.0%

产品编号：Bellancom-150041| CAS NO：2084107-15-1| 分子式：C₃₅H₃₃F₂N₅O₆| 分子量：657.66

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-150041		￥9800.00	杭州北京（现货）
Bellancom-150041		￥15000.00	杭州北京（现货）

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TL4830031

产品介绍

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。

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.

体外研究

TL4830031 (compound 8i) binds to Axl with a K_d value of 1.1 nM. TL4830031 exhibits a 25 fold less potency against Mer with a K_d value of 25 nM, while it is much less potent to Tyro3 with a K_d value of 750 nM.
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.
TL4830031 (0-5000 nM; 4 h) reverses the expression of the EMT markers induced by TGF-β1 in MDA-MB-231 cells.
TL4830031 (0-5000 nM; 24 h) suppresses migration and invasion of MDA-MB-231 cells.

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

Western Blot Analysis

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

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.
TL4830031 (2.5-50 mg/kg; p.o. and i.v.; SD rats) exhibits reasonable pharmacokinetic (PK) properties with an AUC_0-∞ value of 25944.7 μg/mL·h and a T_1/2 value of 5.68 h at an oral dose of 25 mg/kg. The C_max (2386.9 µg/L=3.6 µM) occurred at 4.0 h postdose.

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

Animal Model:	ICR mice
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

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)
AUC_0-∞ (μg/mL·h)	25944.7	20680.6
C_max (ng/mL)	2386.9	4358.2
T_1/2 (h)	5.68	4.26
T_max (h)	4.0
CLz (L/h/kg)		0.12
BA (%)	12.5

体内研究

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

Animal Model:	ICR mice
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

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)
AUC_0-∞ (μg/mL·h)	25944.7	20680.6
C_max (ng/mL)	2386.9	4358.2
T_1/2 (h)	5.68	4.26
T_max (h)	4.0
CLz (L/h/kg)		0.12
BA (%)	12.5

体内研究

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

Animal Model:	ICR mice
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

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)
AUC_0-∞ (μg/mL·h)	25944.7	20680.6
C_max (ng/mL)	2386.9	4358.2
T_1/2 (h)	5.68	4.26
T_max (h)	4.0
CLz (L/h/kg)		0.12
BA (%)	12.5

性状

Solid

溶解性数据

In Vitro:

DMSO : 2.38 mg/mL (3.62 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)

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	---	---	---
10 mM	---	---	---

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式