首页工具

登录

Semaxinib

产品编号 T2064 CAS 204005-46-9

别名: 司马沙尼, SU5416

Semaxinib (SU5416) 是一种选择性的 VEGFR(Flk-1/KDR) 抑制剂，其 IC50=1.23 μM。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Semaxinib Chemical Structure

Semaxinib, CAS 204005-46-9

规格	价格/CNY		货期	数量
5 mg	￥ 498		现货
10 mg	￥ 818		现货
50 mg	￥ 2,515		现货
100 mg	￥ 3,120		现货
1 mL * 10 mM (in DMSO)	￥ 349		现货

大包装超大折扣，点击咨询

其他形式的 Semaxinib:

(Z)-Semaxinib
现货

选择批次

纯度: 99.15%

TargetMol batch loading

更多批次查询请联系客服

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	Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR than PDGFRβ, lack of activity against InsR, EGFR, and FGFR. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature.
靶点活性	VEGFR2:1.23 μM
体外活性	SU5416 inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC50 of 0.04±0.02 μM (n=3). In contrast, SU5416 blocked FGF-dependent mitogenesis of HUVECs with an IC50 of 50 μM (n=10). The selective activity of SU5416 on Flk-1 is supported by the fact that testing of SU5416 using NIH 3T3 cells overexpressing either the EGF or insulin receptors indicated a complete lack of activity (IC50>100 μM). This observation is confirmed by immunoblotting after ligand stimulation. An IC50 of 20.26±5.2 μM (n=7), which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β[1].
体内活性	Daily administration of SU5416 (i.p., 3 mg/kg/day) inhibits the local growth of C6 tumors in the colon. A comparable level of growth inhibition (62% by day 16; P=0.001) is observed for tumors growing in the colon in comparison with ones growing in the hindflank region (54% by day 18; P=0.001). These results indicate that SU5416 could inhibit tumor growth at a site other than the subcutaneous implantation site, where the preexisting vasculature may be different[1]. Daily treatment with SU5416(25 mg/kg) results in a significantly lower tumor growth rate with tumor masses of up to 8% of that present in control animals by day 22 after implantation. Inhibition of tumor growth is clearly preceded by a marked reduction of the tissue area covered by the newly formed glioma microvasculature in the SU5416-treated group, indicating a reduced initial tumor vascularization[2].
激酶实验	Solubilized membranes from 3T3 Flk-1 cells are added to polystyrene ELISA plates that has been precoated with a monoclonal antibody that recognizes Flk-1. After an overnight incubation with lysate at 4°C, serial dilutions of SU5416 are added to the immunolocalized receptor. To induce autophosphorylation of the receptor, various concentrations of ATP are added to the ELISA plate wells containing serially diluted solutions of SU5416. The autophosphorylation is allowed to proceed for 60 min at room temperature and then stopped with EDTA. The amount of phosphotyrosine present on the Flk-1 receptors in the individual wells is determined by incubating the immunolocalized receptor with a biotinylated monoclonal antibody directed against phosphotyrosine. After removal of the unbound anti-phosphotyrosine antibody, avidin-conjugated horseradish peroxidase H is added to the wells. A stabilized form of 3,3′,5,5′-tetramethyl benzidine dihydrochloride and Water2 is added to the wells. The color readout of the assay is allowed to develop for 30 min, and the reaction is stopped with H2SO4. Parallel biochemical kinase assays are performed to measure autophosphorylation on EGFR and fibroblast growth factor receptor[1].
细胞实验	SU5416 is dissolved in DMSO and stored,and then diluted with appropriate media (DMSO<0.5%) before use[1] 3T3Her2 and 488 g2M2 are NIH3T3 fibroblast cell lines engineered to overexpress Her2 and to express human PDGF-BB and human PDGF receptor β.Both cell lines are cultured in DMEM supplemented with 2% CS and 2 mM L-glutamine.C6,Calu 6,A375,A431,and SF767T are plated in their respective growth medium at 2×103 cells/100 μL/well in 96-well,flat-bottomed plates.SU5416 is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture.Cell growth is measured after 96 h using the sulforhodamine B method.IC50s are calculated by curve fitting using four-parameter analysis[1].

别名	司马沙尼, SU5416
分子量	238.28
分子式	C15H14N2O
CAS No.	204005-46-9

存储

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

溶解度

DMSO: 2.38 mg/mL (10 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.1967 mL	20.9837 mL	41.9674 mL	104.9186 mL
	5 mM	0.8393 mL	4.1967 mL	8.3935 mL	20.9837 mL
	10 mM	0.4197 mL	2.0984 mL	4.1967 mL	10.4919 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

X

容积

X

分子量

浓度 (起始)

X

容积 (起始)

=

浓度 (终)

X

容积 (终)

溶液体积

=

质量

/

配液浓度

参考文献

1. Fong TA, et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res, 1999, 59(1), 99-106. 2. Vajkoczy P, et al. Inhibition of tumor growth, angiogenesis, and microcirculation by the novel Flk-1 inhibitor SU5416 as assessed by intravital multi-fluorescence videomicroscopy. Neoplasia, 1999, 1(1), 31-41. 3. Happé, C. M, De Raaf M A , Rol N , et al. Pneumonectomy combined with SU5416 induces severe pulmonary hypertension in rats[J]. American Journal of Physiology - Lung Cellular and Molecular Physiology, 2016, 310(11):L1088-L1097. 4. Huang X, Zhu J, Jiang Y, et al. SU5416 attenuated lipopolysaccharide-induced acute lung injury in mice by modulating properties of vascular endothelial cells[J]. Drug Design, Development and Therapy. 2019, 13: 1763.

文献引用

1. Chen F, Shi Q, Pei F, et al. A systems‐level study reveals host‐targeted repurposable drugs against SARS‐CoV‐2 infection. Molecular Systems Biology. 2021, 17(8): e10239 2. Huang X, Zhu J, Jiang Y, et al. SU5416 attenuated lipopolysaccharide-induced acute lung injury in mice by modulating properties of vascular endothelial cells. Drug Design, Development and Therapy. 2019, 13: 1763 3. Lei W, Xu H, Yao H, et al.5α-Hydroxycostic acid inhibits choroidal neovascularization in rats through a dual signalling pathway mediated by VEGF and angiopoietin 2.Molecular Medicine.2023, 29(1): 1-13. 4. Li M Y, Gao R P, Zhu Q, et al.Skeletal muscle-derived FSTL1 starting up angiogenesis by regulating endothelial junction via activating Src pathway can be upregulated by hydrogen sulfide.American Journal of Physiology-Cell Physiology.2023, 325(5): C1252-C1266.

相关产品

具有相同靶点的化合物

Protein LMWP Vandetanib SU 5402 SCR-1481B1 (Z)-FeCP-oxindole ZM 306416 Regorafenib monohydrate SU5204

相关化合物库

该产品包含在如下化合物库中：

抑制剂库抗癌药物库抗癌临床化合物库激酶抑制剂库药物功能重定位化合物库抗癌活性化合物库抗肺癌化合物库血液病分子库临床期小分子药物库已知活性化合物库

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

g

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

Semaxinib 204005-46-9 Angiogenesis Tyrosine Kinase/Adaptors VEGFR SU-5416 Vascular endothelial growth factor receptor inhibit 司马沙尼 Inhibitor SU5416 SU 5416 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Copyright © 2015-2024 TargetMol Chemicals Inc. All rights reserved. 沪ICP备20019793号-4

沪公网安备 31010602006700号

沪公网安备 31010602006700号

TargetMol Loading

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

陶术生物

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼