Pazopanib HCl (GW786034 HCl)

目录号:S1035 中文名称:盐酸帕佐帕尼

仅限科研使用

Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。

Pazopanib HCl (GW786034 HCl) Chemical Structure

CAS: 635702-64-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1565.32 现货
RMB 1225.19 现货
RMB 3031.75 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

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客户使用Selleck生产的Pazopanib HCl (GW786034 HCl)发表文献51篇:

产品安全说明书

VEGFR抑制剂选择性比较

相关VEGFR产品

生物活性

产品描述 Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。
特性 Pazopanib是一个多激酶的抑制剂。
靶点
VEGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
FGFR [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
点击更多
10 nM 30 nM 47 nM 74 nM 84 nM
体外研究

在HUVEC细胞中,Pazopanib显著抑制VEGF诱导的VEGFR-2的磷酸化,IC50 为8nM [1]。 在所有滑膜肉瘤细胞系中Pazopanib都表现出了生长抑制作用,包括SYO-1和HS-SY-II细胞,这种抑制具有剂量依赖的特性。1µg/mL Pazopanib就可以抑制SYO-1和HS-SY-II细胞增殖,而5µg/mL Pazopanib可以让它们的增殖彻底受阻。 Pazopanib 会诱导滑膜肉瘤细胞周期停留在 G1期从而抑制它的生长。与对照的细胞相比,经过Pazopanib处理过的 SYO-1细胞中的AKTs, GSK-3β, JNKs, p70 S6激酶以及mTOR的磷酸化都受到了抑制[2]。在20 mg/mL 到 22.5 mg/mL的浓度之间,Pazopanib 使RPE细胞的生存能力逐渐下降[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HT29 NIXHdJlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWMkmgZ4VtdHNiaX6gd4VzfW1iY3;ueIFqdmmwZzDt[YRqfW1? NVXZeoZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2NlA{QDJpPkG4OlIxOzh{PD;hQi=>
HN5 MVrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mk\yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkWgZ4VtdHNiaX6gd4VzfW1iY3;ueIFqdmmwZzDt[YRqfW1? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDZ{MEO4Nkc,OTh4MkCzPFI9N2F-
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BT-12 MmTvdWhVWyCjc4PhfS=> NXnFVoZKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NVPXb|VSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 Ml73dWhVWyCjc4PhfS=> NV3ROlNPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NVO5bYpMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NGLFfGZyUFSVIHHzd4F6 NUXFXYlYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= NYTWUG84RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 MY\xTHRUKGG|c3H5 MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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SK-N-MC NFS5WGVyUFSVIHHzd4F6 NWWxXYRWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NYTNWmNURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Assay
Methods Test Index PMID
Western blot p53 / PUMA p-Akt / Akt p-VEGFR2 / p-c-Kit / p-PDGFRβ / FLT-3 27924057 19844230
Immunofluorescence YAP/TAZ 26199863
Growth inhibition assay Cell viability 27924057
体内研究 与没有经过Pazopanib或者仅用10 mg/kg的Pazopanib治疗的小鼠相比,经过30 mg/kg或者100 mg/kg Pazopanib治疗的小鼠其肿瘤症状明显减轻。Pazopanib治疗耐受性良好,各组小鼠之间体重没有发生明显差异[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]

  • 激酶活性测定:

    通过杆状病毒表达系统纯化人源的VEGFR受体激酶1, 2和3的C端催化活性区域的GST融合蛋白,用这些蛋白在384孔微量滴定板上利用均相时间分辨荧光技术(HTRF)对VEGRF1,2和3的酶活性进行分析。首先将10 μL活化的VEGFR2激酶溶液[终浓度为1nM酶溶于0.1 M HEPES,pH 7.5,包含0.1 mg/mL BSA,300 μM DTT]加入10μL底物溶液[终浓度为360 nM多肽(生物素偶联的aminohexyl-EEEEYFELVAKKKK-NH2),75 μM ATP, 10 μM MgCl2],同时加入1 μL 溶解在DMSO中的Pazopanib。滴定板在室温条件下孵育1小时,然后加入20 μL 100 mM 的EDTA终止反应。终止之后,加入20μL HTRF试剂(终浓度为15 nM 链亲和素偶联的别藻蓝素,用0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5稀释的1 nM铕标记的酪氨酸磷酸化抗体)孵育十分钟以上。使用Wallac Victor的时间分辨荧光仪测定665 nM处的荧光值,时间间隔为50 μs。

细胞实验:

[1]

  • Cell lines: HUVEC细胞
  • Concentrations: 0 μM -10 μM
  • Incubation Time: 1 小时
  • Method:

    检测经过VEGF处理过的HUVEC细胞中VEGFR2的磷酸化水平。细胞按每板100万到150万个的密度培养在铺有I型胶原蛋白的10 cm平板上,培养基选用 Clonetics EGM-MV。培养24小时后, 将原来的培养基换成含有0.1% BSA和500 μg/mL hydrocortisone 的Clonetics EBM 培养基,对细胞进行过夜的血清饥饿处理。然后用不同浓度的 Pazopanib 处理细胞1小时, 随后用10 ng/mL 的VEGF 或者对照物处理细胞10分钟。将细胞溶解在裂解液中。用flk-1的抗体对VEGFR2进行免疫沉淀反应,随后进行SDS-聚丙烯酰胺凝胶电泳,然后用flk-1 或者 antiphosphotyrosine (anti-P-tyr-biotin)的抗体进行蛋白免疫印迹的检测。通过光密度法测量将VEGFR2的磷酸化水平量化并将总的VEGFR2水品标准化。

动物实验:

[2]

  • Animal Models: 携带SYO-1细胞的免疫缺陷小鼠
  • Dosages: 0 mg/kg, 10 mg/kg, 30 mg/kg或100 mg/kg
  • Administration: 口服

溶解度(25°C)

体外

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):
30% PEG400+0.5% Tween80+5% propylene glycol

30 mg/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 473.98
化学式

C21H23N7O2S.HCl

CAS号 635702-64-6
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05180695 Not yet recruiting Drug: Pazopanib|Drug: HDM201 Advanced Soft-tissue Sarcoma|Metastatic Soft-tissue Sarcoma Centre Leon Berard|Novartis|National Cancer Institute France January 2022 Phase 1|Phase 2
NCT04659343 Recruiting Drug: Medical treatment for metastatic renal cell carcinoma Kidney Cancer|Renal Cell Carcinoma Metastatic|Drug Toxicity|Drug Side Effect|Drug Mechanism Frede Donskov|Odense University Hospital|Herlev Hospital|Rigshospitalet Denmark|University of Aarhus November 1 2020 --
NCT03735758 Terminated Drug: pazopanib or guideline conform chemotherapy Soft Tissue Sarcoma Adult GWT-TUD GmbH November 2 2018 Phase 4
NCT03334409 Terminated Drug: Ascorbic Acid|Drug: Pazopanib Hydrochloride Clear Cell Renal Cell Carcinoma|Metastatic Clear Cell Renal Cell Carcinoma|Stage III Renal Cell Cancer AJCC v8|Stage IV Renal Cell Cancer AJCC v7|Unresectable Renal Cell Carcinoma Academic and Community Cancer Research United|National Cancer Institute (NCI) February 16 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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