瓦特拉尼碱 - CAS:212141-54-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	瓦特拉尼碱
英文名称:	Vatalanib free base
别名:	瓦他拉尼碱 N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
CAS No:	212141-54-3	分子式:	C₂₀H₁₅ClN₄	分子量:	346.82
CAS No:	212141-54-3
分子式:	C₂₀H₁₅ClN₄
分子量:	346.82
MDL:	MFCD08458963

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V10010 瓦特拉尼碱 ≥98%(HPLC) (psaitong)

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包装规格：

10mg 100mg in glass bottle

溶解性：

溶于DMSO

产品描述：

基本信息

产品编号：V10010
产品名称：Vatalanib free base
CAS:	212141-54-3	储存条件	粉末	-20℃	四年
分子式：	C20H15ClN4		溶于液体	-80℃	两年
分子量	346.82
化学名：	N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
Solubility (25°C)	体外	DMSO	50mg/mL (144.17 mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内	现配现用
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.8834mL	14.4171mL	28.8342mL
5mM	0.5767mL	2.8834mL	5.7668mL
10mM	0.2883mL	1.4417mL	2.8834mL

生物活性

产品描述	一种VEGFR2/KDR的抑制剂，IC50：37nM。
靶点/IC₅₀	VEGFR2 37nM (IC50)
体外研究	Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270nM, 730nM and 580nM, respectively. Vatalanib shows the antiproliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1nM, and dosedependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2
体内研究	Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes.

推荐实验方法(仅供参考)

激酶实验：

Each GST-fused kinase is incubated under optimized buffer conditions. ATP in a total volume of 30μL in the presence or absence of a test substance (Vatalanib) for 10 min at ambient temperature. The reaction is stopped by adding 10μL of 250mM EDTA.

细胞实验:

Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin. After 24h, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50ng/mL), bFGF (0.5ng/mL), or FCS (5%), in the presence or absence of Vatalanib. As a control, wells without growth factor are also included. After 24h of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3' 5,5'-tetramethylbenzidine substrate.

动物实验:

A porous Teflon chamber (volume, 0.5mL) is filled with 0.8% w/v agar containing heparin (20units/mL) with or without growth factor (3μg/mL human VEGF, 2μg/mL human PDGF) is implanted s.c. on the dorsal flank of C57/C6 mice. The mice are treated with Vatalanib (12.5, 25 or 50 mg/kg dihydrochloride p.o. once daily) or vehicle (water) starting 1 day before implantation of the chamber and continuing for 5 days after. At the end of treatment, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is carefully removed and weighed, and the blood content is assessed by measuring the hemoglobin content of the tissue.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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