VEGFR-3-IN-1

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VEGFR-3-IN-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2756668-73-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

VEGFR-3-IN-1 是一种有效的高选择性VEGFR3抑制剂，其IC₅₀为 110.4 nM。VEGFR-3-IN-1 通过使 VEGFR3 信号通路失活，显著抑制 VEGF-C 诱导人真皮淋巴管内皮细胞 (HDLEC)、MDA-MB-231 和 MDA-MB-436 细胞的增殖和迁移，并且能有效抑制乳腺癌的生长。

生物活性

VEGFR-3-IN-1 is a potent and selectiveVEGFR3inhibitor with anIC₅₀of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breastcancergrowth^[1].

IC₅₀& Target^[1]

VEGFR3

110.4 nM (IC₅₀)

体外研究
(In Vitro)

VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC₅₀>50 μM), with IC₅₀values of 2.22 and 3.50 μM, respectively^[1].
VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner^[1].

Cell Viability Assay^[1]

Cell Line:	MDA-MB-231 and MDA-MB-436 cells
Concentration:	100 nM
Incubation Time:	48 hours
Result:	Exerted antimigration and antiproliferative activities through targeting VEGFR3 in MDA-MB-231 and MDA-MB-436 cells.

Western Blot Analysis^[1]

Cell Line:	HDLEC cells
Concentration:	10-500 nM
Incubation Time:
Result:	Antilymphangiogenic activities of VEGFR-3-IN-1 by suppressing the expression of VEGFR3.

体内研究
(In Vivo)

VEGFR-3-IN-1 (50, 25 mg/kg; p.o.) reduces the tumor volume, and displays the strongest inhibitory activity in mice, with a growth inhibition rate of 61.9%^[1].
VEGFR-3-IN-1 (10 mg/kg; p.o.) treatment shows the C_max, AUC_0-t, AUC_0-∞and t_1/2values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively^[1].

Animal Model:	Nude mice (carrying xenografted BC)^[1]
Dosage:	50 mg/kg
Administration:	P.o.;once
Result:	Reduced the tumor volume, and displayed the strongest inhibitory activity in mice.

Animal Model:	Sprague-Dawley (SD) rats^[1]
Dosage:	10 mg/kg
Administration:	P.o. (Pharmacokinetic Analysis)
Result:	The C_max, AUC_0-t, AUC_0-∞and t_1/2were 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively.

分子量

616.10

性状

Solid

Formula

C₂₉H₂₉ClF₃N₇OS

CAS 号

2756668-73-0

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

In Vitro:

DMSO : 12.5 mg/mL(20.29 mM;ultrasonic and warming and adjust pH to 6 with HCl and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.6231 mL	8.1156 mL	16.2311 mL
5 mM	0.3246 mL	1.6231 mL	3.2462 mL
10 mM	0.1623 mL	0.8116 mL	1.6231 mL

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。