Tivozanib (AV-951)

For research use only. Not for use in humans.

目录号:S1207 别名: KRN-951

Tivozanib (AV-951) Chemical Structure

Molecular Weight(MW): 454.86

Tivozanib (AV-951)是一种有效的,选择性VEGFR抑制剂,作用于VEGFR1/2/3时,IC50分别为0.21 nM/0.16 nM/0.24 nM,也抑制PDGFR和c-Kit,作用于FGFR-1, Flt3, c-Met EGFR和IGF-1R活性较弱。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1963.28 现货
RMB 977.17 现货
RMB 1415.05 现货
RMB 4648.03 现货
RMB 8165.43 现货
RMB 13980.33 现货
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客户使用Selleck生产的Tivozanib (AV-951)发表文献16篇:

客户使用该产品的6个实验数据:

  • On-chip angiogenesis assay. Fluorescence imaging of Tg(fli1a:EGFP) embryos at 64 hpf. Transgenic embryos were arrayed and immobilized at 16 hpf and continuously perfused with E3 media containing vehicle control (dimethyl sulfoxide) or selected small-molecule antiangiogenic drugs (Sunitinib and Tivozanib). Right panel: microscopic visualization of patterns of ISV. White arrows: normal ISV growth; blue arrows: partial ISV growth inhibition; and red arrows; complete ISV growth inhibition.

    Cytometry A 2014 85(6), 537-47. Tivozanib (AV-951) purchased from Selleck.

  • After serum-starvation for 24 h, the MCF7 cells were co-treated with 10 nM TPA and the indicated doses VEGFR inhibitor, Tivozanib, for 24 h. The levels of fibronectin, p-PKC-α, p-ERK, p-AKT, t-AKT and β-actin protein expression were analyzed by western blotting. The levels of fibronectin mRNA were analyzed by real-time PCR. The results are representative of three independent experiments. The values shown are the means ±SEM. * P < 0.05, ** P < 0.01 vs. control. # P < 0.05, ## P < 0.01 vs. TPA-treated cells. Con: control. LY: LY294002, U: UO126, Go: Go6983, Akt IV: Akt IV inhibitor.

    Cell Physiol Biochem 2013 32(5), 1541-50. Tivozanib (AV-951) purchased from Selleck.

  •  

    Reversal effect of Tivozanib on the sensitivity of HEK/ABCB1 cells to vincrstine. The figure showes the survival curves of cells at different concentrations of vincristine with or without Tivozanib. Cell viability was determined by MTT Assay. HEK293 is human embryonic kidney cell line while HEK/ABCB1 is ABCB1-transfected cell line. Verapamil was used as a positive control of ABCB1 inhibitor.

    Tivozanib (AV-951) purchased from Selleck.

  •  

    Figure 7 shows the effect of Tivozanib on the accumulation of [3H]-mitoxantrone. The accumulation of [3H]-mitoxantrone in empty vector transfected HEK293/pcDNA3.1, ABCG2 vector transfected wild-type ABCG2-482-R2, mutant ABCG2-482-G2 and mutant ABCG2-482-T7 cells was measured by the Accumulation Assays. Columns are the mean of triplicate determinations; bars, SD. *P<0.05, **P<0.01 versus the control group. Fumitremorgin C (FTC) was used as a positive control of ABCG2 inhibitor.

    Tivozanib (AV-951) purchased from Selleck.

  • Effects of VEGFR inhibitor tivozanib treatment on ALP activity (A, 48 h after loading), Runx2 (B, 6 h after loading) and Col-1 (C, 48 h after loading) mRNA expression (the amount of decrease compared to untreated groups and the significant difference were marked, *p < 0.05).

    Arch Biochem Biophys, 2016, 607:37-43. Tivozanib (AV-951) purchased from Selleck.

  • Biol Open, 2018, 7(6). Tivozanib (AV-951) 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 Tivozanib (AV-951)是一种有效的,选择性VEGFR抑制剂,作用于VEGFR1/2/3时,IC50分别为0.21 nM/0.16 nM/0.24 nM,也抑制PDGFR和c-Kit,作用于FGFR-1, Flt3, c-Met EGFR和IGF-1R活性较弱。Phase 3。
靶点
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
EphB2 [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
PDGFRα [1]
(Cell-free assay)
6.5 nM 15 nM 24 nM 30 nM 40 nM
体外研究

AV-951 也抑制PDGFRß和c-Kit的磷酸化作用,IC50 分别为1.72nm 和1.63nM。AV-951阻断VEGF依赖的MAPK活性和内皮细胞增殖。[1]AV-951是新型喹啉-尿素派生物。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNuIFnDOVA:OC5|ODFOwG0> MXWyOFU5OzN3Nx?=

... Click to View More Cell Line Experimental Data

体内研究 活体研究显示AV-951降低移植瘤微血管密度和抑制移植瘤VEGFR-2磷酸化作用水平,尤其当AV-951浓度为1mg/kg (口服处理)。在无胸腺鼠中AV-951几乎抑制全部的移植瘤生长,肿瘤生长抑制率(TGI)>85%。[1]AV-951作用于人类移植瘤模型包括肺, 胸腺, 结肠, 卵巢, 胰脏和前列腺癌,显示出抗癌活性。[2]鼠类腹膜弥散肿瘤模型研究显示AV-951可延长肿瘤携带鼠的寿命。[3]

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

激酶实验:

加入1 μmol/L ATP进行无细胞激酶实验,分四组进行,测定AV-951作用于重组受体和非受体酪氨酸激酶的IC50值。用于细胞实验,细胞在含0.5% FBS的培养基中饥饿过夜。加入AV-951或0.1% DMSO,温育1小时,然后在37oC下加入同源配体诱导。诱导受体磷酸化持续5分钟。加溶解buffer(包含1% NP40, 0.5%脱氧胆酸钠, 0.1% SDS, 100 μg/mL苯甲磺酰氟, 1 mmol/L Na3VO4,及溶在PBS中的3% 抑肽酶)溶解细胞。然后加入合适的抗体进行免疫沉淀反应,及加入磷酸酪氨酸进行免疫印迹。分析回归曲线计算IC50值。
细胞实验:[1]
- 合并
  • Cell lines: 人类脐静脉内皮细胞(HUVEC) 和正常人类皮肤成纤维细胞
  • Concentrations: 1 μM
  • Incubation Time: 15分钟
  • Method: 癌细胞接种在96孔板上,在含10% FBS的培养基上培养24小时。加入AV-951,温育72小时。使用WST-1试剂探测细胞活力。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 无胸腺鼠(RH-rnu/rnu)
  • Dosages: 1 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 20 mg/mL (43.96 mM)
Water Insoluble
Ethanol 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):
2% DMSO+30% PEG 300+ddH2O
1mg/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 454.86
化学式

C22H19ClN4O5

CAS号 475108-18-0
储存条件 粉状
溶于溶剂
别名 KRN-951

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(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
NCT03136627 Active not recruiting Drug: Tivozanib|Drug: Nivolumab Carcinoma Renal Cell AVEO Pharmaceuticals Inc.|Bristol-Myers Squibb March 22 2017 Phase 1|Phase 2
NCT01853644 Active not recruiting Drug: Tivozanib Recurrent Epithelial Ovarian Cancer|Recurrent Fallopian Tube Cancer|Recurrent Primary Peritoneal Cancer Northwestern University|National Comprehensive Cancer Network June 6 2013 Phase 2
NCT01834183 Withdrawn Drug: Tivozanib|Drug: Gemcitabine Renal Cell Carcinoma Dana-Farber Cancer Institute June 2013 Phase 2
NCT01807156 Terminated Drug: Tivozanib Hepatocellular Cancer Emory University|AVEO Pharmaceuticals Inc. March 2013 Phase 2
NCT01769885 Withdrawn Drug: tivozanib|Procedure: therapeutic conventional surgery Stage II Renal Cell Cancer|Stage III Renal Cell Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|AVEO Pharmaceuticals Inc. March 14 2013 Not Applicable

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Would you please provide a little bit more detail regarding how to prepare the Tivozanib for in vivo treatment and the storage condition?

  • 回答:

    For in vivo formula, we recommend to use 2% DMSO+30% PEG 300+ddH2O up to 1mg/mL. Once dissolved it in solution, please make small aliquots and store them at -80C up to 6 months without repeated thawing and refreezing.

VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID