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Vatalanib dihydrochloride

产品编号 T6720 CAS 212141-51-0

别名: CGP-797870 dihydrochloride, ZK-222584 dihydrochloride, Vatalanib 2HCl, PTK787 dihydrochloride, Vatalanib (PTK787) 2HCl, CGP-79787 dihydrochloride, 瓦他拉尼

Vatalanib dihydrochloride (PTK787 dihydrochloride) 是一种VEGFR2/KDR 的抑制剂，其IC50值为37nM。

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Vatalanib dihydrochloride Chemical Structure

Vatalanib dihydrochloride, CAS 212141-51-0

规格	价格/CNY	货期
1 mg	￥ 113	现货
5 mg	￥ 228	现货
10 mg	￥ 372	现货
25 mg	￥ 628	现货
50 mg	￥ 953	现货
100 mg	￥ 1,530	现货
200 mg	￥ 2,280	现货
1 mL * 10 mM (in DMSO)	￥ 253	现货

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其他形式的 Vatalanib dihydrochloride:

Vatalanib free base
现货
Vatalanib succinate
询价

选择批次

纯度: 100%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Vatalanib dihydrochloride (PTK787 dihydrochloride)(IC50=37 nM) is an inhibitor of VEGFR2/KDR. It exhibits less effective against VEGFR1/Flt-1 and 18-fold against VEGFR3/Flt-4.
靶点活性	PDGFRβ:580 nM, VEGFR1/FLT1:77 nM, VEGFR2/KDR:37 nM, VEGFR2/Flk1:270 nM, VEGFR3/FLT4:660 nM
体外活性	Vatalanib inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Moreover, Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently 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. [1] 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. [2]
体内活性	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 (25-100 mg/kg). Within the same dose range, Vatalanib also inhibits the growth and metastases of several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes. [1]
激酶实验	VEGF Receptor Tyrosine Kinase Assays : The in vitro kinase assays are performed in 96-well plates as a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-Sepharose. γ-[33P]ATP is used as the phosphate donor, and poly-(Glu:Tyr 4:1) peptide is used as the acceptor. Recombinant GST-fusion proteins are diluted in 20 mM Tris·HCl (pH 7.5) containing 1–3 mM MnCl2, 3–10 mM MgCl2, 0.25 mg/mL polyethylene glycol 20000, and 1 mM DTT, according to their specific activity. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1–3 mM MnCl2, 3–10 mM MgCl2, 3–8 μg/mL poly-(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT, and 0.2 μCi[γ-33P]ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 minutes at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA. Using a 96-well filter system, half the volume (20 μL) is transferred onto a Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively in 0.5% H3PO4 and then soaked in ethanol. After drying, Microscint cocktail is added, and scintillation counting is performed. IC50s for PTK787/ZK 222584 or SU5416 in these as well as all assays described below are calculated by linear regression analysis of the percentage inhibition.
细胞实验	As a test of the ability of PTK787/ZK 222584 to inhibit a functional response to VEGF, an endothelial cell proliferation assay, based on BrdUrd incorporation is used. Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin and then incubated at 37 °C and 5% CO2 in growth medium. After 24 hours, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of PTK787/ZK 222584. As a control, wells without growth factor are also included. After 24 hours of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 hours before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3′5,5′-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm. (Only for Reference)

别名	CGP-797870 dihydrochloride, ZK-222584 dihydrochloride, Vatalanib 2HCl, PTK787 dihydrochloride, Vatalanib (PTK787) 2HCl, CGP-79787 dihydrochloride, 瓦他拉尼
分子量	419.73
分子式	C20H15ClN4·2HCl
CAS No.	212141-51-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 79 mg/mL (188.2 mM)

H2O: 10 mg/mL (23.82 mM)

Ethanol: 6 mg/mL (14.29 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O / Ethanol	1 mM	2.3825 mL	11.9124 mL	23.8248 mL	59.5621 mL
	5 mM	0.4765 mL	2.3825 mL	4.765 mL	11.9124 mL
	10 mM	0.2382 mL	1.1912 mL	2.3825 mL	5.9562 mL
DMSO / H2O	20 mM	0.1191 mL	0.5956 mL	1.1912 mL	2.9781 mL
DMSO	50 mM	0.0476 mL	0.2382 mL	0.4765 mL	1.1912 mL
DMSO	100 mM	0.0238 mL	0.1191 mL	0.2382 mL	0.5956 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Wood JM, et al. Cancer Res. 2000, 60(8), 2178-2189. 2. Murakami M, et al. Ann Surg Oncol. 2011, 18(2), 589-596.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Vatalanib dihydrochloride 212141-51-0 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors VEGFR PDGFR Inhibitor CGP-797870 dihydrochloride Vascular endothelial growth factor receptor CGP-79787 CGP-797870 Vatalanib PTK787 Dihydrochloride ZK222584 PTK 787 Dihydrochloride PTK-787 Dihydrochloride ZK-222584 dihydrochloride CGP797870 PTK-787 CGP 797870 Dihydrochloride CGP79787 Dihydrochloride ZK-222584 ZK 222584 ZK 222584 Dihydrochloride CGP 79787 ZK-222584 Dihydrochloride PTK 787 CGP 79787 Dihydrochloride CGP797870 Dihydrochloride CGP 797870 Vatalanib 2HCl CGP-797870 Dihydrochloride PTK787 dihydrochloride ZK222584 Dihydrochloride Vatalanib (PTK787) 2HCl PTK787 Vatalanib (PTK787) inhibit CGP-79787 Dihydrochloride Vatalanib Dihydrochloride CGP-79787 dihydrochloride CGP79787 瓦他拉尼 inhibitor

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Vatalanib dihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords