Semaxanib (SU5416)

For research use only. Not for use in humans.

目录号:S2845

Semaxanib (SU5416) Chemical Structure

CAS No. 194413-58-6; 204005-46-9

Semaxanib (SU5416)是一种有效的,选择性的VEGFR(Flk-1/KDR)抑制剂,IC50为1.23 μM,作用于VEGFR比作用于PDGFRβ选择性高20倍,对EGFR, InsR和FGFR没有作用活性。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1627.36 现货
RMB 1378.55 现货
RMB 7963.45 现货
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客户使用Selleck生产的Semaxanib (SU5416)发表文献13篇:

客户使用该产品的3个实验数据:

  • Injected tumor cells move to the tail via blood vessels. Tg (flil1:egfp) embryos at 20 hpf were treated with 2 μM SU5416 for 1 hr (+SU5416) to inhibit vasculogenesis24; the control fish were treated with 0.02% DMSO for 1 hr (-SU5416). After 1 hr, SU5416 or DMSO was washed out by changing fish media. At 48 hpf, tfRFP-B16 cells were injected into the pericardium cavity of fish. Representative images show that tumor cells moved to the tail in a drug-free larva, while no tumor cells moved to the tail in a drug-treated larva after new vessels were inhibited by SU5416. Insets are enlarged images from each corresponding tip of the tail indicated by white arrows. Dashed white lines mark extravasated tumor cells at 12 hpi. Vessels are green and tumor cells are red. –SU5416, 6 other larvae exhibit similar behaviors; +SU5416, 3 other larvae exhibit similar behaviors. Scale bars, 500 μm. Insets, 100 μm.

    Sci Rep, 2016, 6:19304. . Semaxanib (SU5416) purchased from Selleck.

  • HUVEC spheroids embedded in fibrin gel were incubated with a pool of PDR vitreous fluid samples (1:4 dilution) in the absence or in the presence of different extracellular pathway. Formation of radially growing sprouts was evaluated after 24 h of incubation. Data are the mean ± S.E.M. of 30 spheroids per experimental point. *p《0.05, **p《0.01 versus PDR vitreous

    Angiogenesis, 2017, 20(4):629-640. Semaxanib (SU5416) purchased from Selleck.

  • VEGFR inhibition mitigates JNA fibroblast-induced tubule formation in HUVECS. (A) HUVEC tubule formation was assessed in the presence of JNA CM or SFM with or without SU5416 or vehicle control (DMSO). The photograph represents characteristic HUVEC tubules in each treatment group. (B) HUVECs were plated on a layer of Matrigel in the presence of SFM or JNA CM and subsequently treated with vehicle control (DMSO) or SU5416 at an IC50 concentration of 1.23µM. After a 6-hour incubation at 37°C, the HUVECs were examined under magnification ×100 and tubule formation and length were assessed using Pipeline software. The experiment was repeated 3 times. CM = conditioned media; DMSO = dimethylsulfoxide; HUVEC = human umbilical vein endothelial cell; IC50 = the dose that is cytotoxic to 50% of the cells treated in vitro; JNA = juvenile nasopharyngeal angiofibroma; SFM = serum-free media.

    Int Forum Allergy Rhinol, 2017, 7(10):973-979. Semaxanib (SU5416) purchased from Selleck.

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Semaxanib (SU5416)是一种有效的,选择性的VEGFR(Flk-1/KDR)抑制剂,IC50为1.23 μM,作用于VEGFR比作用于PDGFRβ选择性高20倍,对EGFR, InsR和FGFR没有作用活性。Phase 3。
靶点
VEGFR2/Flk1 [1]
(Cell-free assay)
1.23 μM
体外研究

在Flk-1过表达的NIH 3T3细胞中,Semaxanib抑制Flk-1受体的VEGF-依赖性磷酸化, IC50为1.04 μM。在NIH 3T3细胞中,Semaxanib抑制PDGF依赖性自身磷酸化,IC50 为20.3 μM。Semaxanib剂量依赖性抑制VEGF和FGF诱发的有丝分裂,IC50分别为0.04和50 μM。Semaxanib的治疗对C6胶质瘤,Calu 6肺癌,A375黑素瘤,A431 鳞状细胞癌,和SF767T 神经胶质瘤细胞(IC50s都大于20 μM)在体外的生长没有影响。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells NIH2WodEgXSxdH;4bYNqfHliYYPzZZk> NW\BbmFlPDhiaB?= MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyPUOuNUBvVQ>? Mlu4NlM4Pzd6OUi=
mouse B16F10 cells M2DidGN6fG:2b4jpZ4l1gSCjc4PhfS=> M2qzZVQ5KGh? MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCNVZHOTBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNEUzhiYYPzZZktKEmFNUC9N{43KG6P NEfpSpkzOzd5N{i5PC=>
human U251 cells NFfLUGtHfW6ldHnvckBie3OjeR?= NUjFfJJlUW6qaXLpeIlwdiCxZjDWSWdHWjJiaX6gbJVu[W5iVUK1NUBk\WyuczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FuIFnDOVA:OTJwOTDuUS=> M4[3dlI1QTByOE[1
human A431 cells Mn\sSpVv[3Srb36gZZN{[Xl? Mnn6RY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{NCCLQ{WwQVAvODh3IN88US=> MXSyNFQxOzZ7Mx?=
CHO cells NH[4W2xHfW6ldHnvckBie3OjeR?= NX;UWnBpUW6qaXLpeIlwdiCxZjDWSWdHWiCrbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25ib3[gbJVu[W5iVnHzZ5Vt[XJiZX7kc5Rp\WyrYXyg[5Jwf3SqIH\hZ5RweiC{ZXPldJRweiB{IDjWSWdHWjJrIITyZY5{\mWldHXkJIlvKEOKTzDj[YxteyxiSVO1NF0xNjh6NDFOwG0> MnPRNVI1Pzd|NUK=
human MCF7 cells MlLzVJJwdGmoZYLheIlwdiCjc4PhfS=> NW\TcnBoPCCmYYnz MnPCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDRiZHH5d{BjgSClb4XseIVzKGOxdX70[ZIhdWW2aH;kMEBKSzVyPUGuPUDPxE1? M{\qO|I{OTJ2MkGz
human SF539 cells M4HRZWZ2dmO2aX;uJIF{e2G7 M3jjNmlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHnuJIh2dWGwIGPGOVM6KGOnbHzzJIJ6KHCqb4PwbI91gXKxc3nu[UBGVEmVQTygTWM2OD1{LkSg{txO NWq5NohnOTl5NEi3PFU>
A431 cells NH7VRYRHfW6ldHnvckBie3OjeR?= NIDnW2JKdmirYnn0bY9vKG:oIG\FS2ZTOiCneIDy[ZN{\WRiaX6gbJVu[W5iQUSzNUBk\WyuczygTWM2OD1zMj65JO69VQ>? MkDwNlA2PThyN{K=
HUVEC cells MmTXVJJwdGmoZYLheIlwdiCjc4PhfS=> M{HwTVczKGh? MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiXVlXDJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgeJJ6eGGwIHLseYUh[XO|YYmsJGdKPTB;MUOuOkDPxE1? M4nST|I3OzF6MEW2
human HMEC1 cells MkX2VJJwdGmoZYLheIlwdiCjc4PhfS=> NWP2T|N7PyCmYYnz MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiPRVOxJINmdGy|IHHmeIVzKDdiZHH5d{BjgSClb4XseIVzKGOxdX70[ZIhdWW2aH;kMEBKSzVyPUG1JO69VQ>? Mki1NlMyOjR{MUO=
human HeLa cells M4f4d3Bzd2yrZnXyZZRqd25iYYPzZZk> M1H6dFQh\GG7cx?= MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KGOxdXz0[ZIh[2:3boTldkBu\XSqb3SsJGlEPTB;MkCg{txO NFj4bWYzOzF{NEKxNy=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-VEGFR2 / VEGFR2 / p-PLCγ1 / PLCγ1 / p-ERK / ERK ; 

PubMed: 21699503     


SU5416 dose-dependently inhibited VEGF-A and bFGF-regulated intracellular signalling in primary endothelial cells. Cells were treated for 7.5 min with VEGF-A or bFGF (25 ng/mL) and processed for immunoblotting using anti-phospho-PLCγ1 (Y783), anti-PLCγ1, anti-phospho-ERK1/2 (T202/Y204), anti-ERK1/2 and anti-α-tubulin antibodies. Data shown are representative of four independent experiments.

21699503
Immunofluorescence
CD31 / OCT-4 / SOX-2 ; 

PubMed: 25665868     


Immunofluorescent detection of Oct-4, Sox-2, or CD31 in vehicle control (top row) and SU5416 treated cells (bottom row). Representative images are from one of three experiments. Scale bar = 70 μm.

25665868
Growth inhibition assay
Cell viability; 

PubMed: 25794107     


MTT assay showed that SU5416 treatment significantly suppressed Daoy cell growth.

25794107
体内研究 Semaxanib剂量相关性抑制A375肿瘤在体内的生长。Semaxanib每天腹腔注射给药,能够抑制>85%的皮下肿瘤的生长,并且没有可检测的毒性。Semaxanib具有广谱的抗肿瘤活性。测试的10种肿瘤细胞系中,Semaxanib显著抑制其中8种(A431,Calu-6,C6,LNCAP,EPH4-VEGF,3T3HER2,488G2M2以及SF763T细胞)的皮下生长,平均死亡率为2.5%。[1] Semaxanib (25毫克/千克/天)显示出强效抗血管生成活性,导致肿瘤微血管系统的总功能性血管密度显著降低。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

生化激酶试验:

将来自3T3 Flk-1细胞的膜溶解后加入聚苯乙烯ELISA平板,平板用能够识别Flk-1的单克隆抗体预涂层。在4 ℃下,裂解物培养过夜,将连续稀释的SU5416加入到免疫定位的受体。为诱导受体的自身磷酸化,将不同浓度的ATP加入到含有连续稀释的SU5416的ELISA孔板。自身磷酸化在室温下进行60分钟,然后加入EDTA停止。单个孔中在Flk-1受体上的磷酸酪氨酸的数量,通过培育免疫定位受体与直接抗磷酸酪氨酸的生物素化的单克隆抗体测定。除去未结合的抗磷酸酪氨酸抗体,将抗生素蛋白共轭的辣根pero-idase H加入到孔中。稳定形式的3,3 9,5,5 9-四甲基联苯胺盐酸盐和H2O2加入孔中,该测定的颜色读数发展30分钟后,用H2SO4停止反应。
细胞实验:[1]
- 合并
  • Cell lines: HUVECs
  • Concentrations: ~100 μM
  • Incubation Time: 2天
  • Method: HUVECs接种在96孔平底平板(1×104 细胞/100 微升/孔)包含0.5%热灭活FBS 的F-12K介质中,并在37 ℃下培养24小时使细胞静止。连续稀释的化合物在含有1% DMSO的培养基中制备,然后加两小时,接着在培养基中加入促有丝分裂浓度的5纳克/毫升或20纳克/毫升的VEGF或者0.25-5纳克/毫升的酸性成纤维细胞生长因子。测定中DMSO的终浓度为0.25%。24小时后,加入[3H] 胸苷(1 μCi/well)或BrdUrd,单层细胞再培育24小时。细胞摄入[3H] 胸苷(1 μCi/well)或BrdUrd的量分别通过液体闪烁计数器或BrdUrd ELISA测定。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 人类黑色素瘤异种移植A375
  • Dosages: 25 毫克/千克
  • Administration: 每天腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 22 mg/mL (92.32 mM)
Ethanol 2 mg/mL (8.39 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40%PEG 300+ 5% Tween80 + ddH2O
0.5mg/mlmg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 238.28
化学式

C15H14N2O

CAS号 194413-58-6; 204005-46-9
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

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 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

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 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00006247 Terminated Drug: semaxanib Brain and Central Nervous System Tumors Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) August 2000 Phase 1
NCT00005642 Completed Drug: semaxanib Unspecified Adult Solid Tumor Protocol Specific Case Comprehensive Cancer Center|National Cancer Institute (NCI) May 2000 Phase 1
NCT00005647 Completed Drug: paclitaxel|Drug: semaxanib Head and Neck Cancer Case Comprehensive Cancer Center|National Cancer Institute (NCI) May 2000 Phase 1

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID