Tivozanib

别名: AV-951, KRN-951 中文名称:替沃扎尼

Tivozanib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。

Tivozanib Chemical Structure

Tivozanib Chemical Structure

CAS: 475108-18-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1963.28 现货
5mg RMB 977.17 现货
10mg RMB 1415.05 现货
50mg RMB 4648.03 现货
100mg RMB 8165.43 现货
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客户使用Selleck的Tivozanib发表文献35

产品质控

批次: 纯度: 99.64%
99.5

Tivozanib相关产品

相关信号通路图

VEGFR抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MCF7 cells Proliferation assay Antiproliferative activity against human MCF7 cells, IC50=0.38 μM 24583357
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Tivozanib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)
点击更多
6.5 nM 15 nM 24 nM 30 nM 40 nM
体外研究(In Vitro)
体外研究活性 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]
激酶实验 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 细胞系 人类脐静脉内皮细胞(HUVEC) 和正常人类皮肤成纤维细胞
浓度 1 μM
孵育时间 15分钟
方法 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。
体内研究(In Vivo)
体内研究活性 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]
动物实验 Animal Models 无胸腺鼠(RH-rnu/rnu)
Dosages 1 mg/kg
Administration 口服处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04645160 Recruiting
Cholangiocarcinoma|Bile Duct Neoplasm|Biliary Tract Malignancy
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
March 4 2022 Phase 1|Phase 2
NCT03136627 Completed
Carcinoma Renal Cell
AVEO Pharmaceuticals Inc.|Bristol-Myers Squibb
March 22 2017 Phase 1|Phase 2
NCT01853644 Completed
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
Renal Cell Carcinoma
Dana-Farber Cancer Institute
June 2013 Phase 2
NCT01807156 Terminated
Hepatocellular Cancer
Emory University|AVEO Pharmaceuticals Inc.
March 2013 Phase 2

化学信息&溶解度

分子量 454.86 分子式

C22H19ClN4O5

CAS号 475108-18-0 SDF Download Tivozanib SDF
Smiles CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 20 mg/mL ( 43.96 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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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.

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