中文名称: 瓦特拉尼碱
英文名称: Vatalanib free base
CAS No: 212141-54-3
分子式: C20H15ClN4
分子量: 346.82
V10010 瓦特拉尼碱 ≥98%(HPLC) (psaitong)
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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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):