Pazopanib

For research use only. Not for use in humans.

目录号:S3012 别名: GW786034 中文名称:帕唑帕尼

Pazopanib Chemical Structure

CAS No. 444731-52-6

Pazopanib (GW786034) 是一种新型多靶点的VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms/CSF1R抑制剂,无细胞试验中IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。

规格 价格 库存 购买数量  
RMB 570.03 现货
RMB 1729.32 现货
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客户使用Selleck生产的Pazopanib发表文献60篇:

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Pazopanib (GW786034) 是一种新型多靶点的VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms/CSF1R抑制剂,无细胞试验中IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。
靶点
VEGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
10 nM 30 nM 47 nM 74 nM 84 nM
体外研究

Pazopanib有效抑制VEGF诱导的HUVEC 细胞中VEGFR2磷酸化作用,IC50为8 nM。[1]在所有滑膜肉瘤细胞系,包括SYO-1和HS-SY-II细胞中,Pazopanib表现出剂量依赖性生长抑制作用。SYO-1和HS-SY-II细胞的增殖在1微克/毫升的Pazopanib下被抑制,在5微克/毫升的Pazopanib下被完全废止。Pazopanib引起G1期阻滞,并且因此抑制滑膜肉瘤细胞的生长。与载体处理的细胞相比,Akts,GSK-3β,JNKs,p70 S6 激酶,和mTOR的磷酸化作用在Pazopanib处理的SYO-1细胞中被抑制。[2] Pazopanib在20毫克/毫升和22.5毫克/毫升之间表现出逐渐增加的RPE细胞活性降低。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HT29 cells NEfsRWZRem:uaX\ldoF1cW:wIHHzd4F6 MmPFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVEK5JINmdGy|IHnuJJNmenWvIHPvcpRicW6rbnegcYVlcXWv M2HRWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkKwN|gzLz5zOE[yNFM5OjxxYU6=
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HT-29 MoP4SpVv[3Srb36gZZN{[Xl? M1;JeFE1KHSxIEK0JIhzew>? MX7Jcohq[mm2aX;uJI9nKFKLUFuxJIlvKGi3bXHuJGhVNTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBVVk[jbIDoZU1qdmS3Y3XkJI5m[3KxcITvd4l{KGmwY4XiZZRm\CCob4KgNVQhfG9iMkSgbJJ{KGmwIIDy[ZNmdmOnIH;mJHNu[WNibXnt[ZRq[yCjbnSgfk1XSURvRl3LJIJ6KGOnbHygeIl1\XJiZ3zvMYJie2WmIHz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD1yLki3N:69VQ>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ{MkC5Okc,OzF4MkKwPVY9N2F-
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MC-CAR NYrNd5BvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJG1ENUODUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSwMlI1PzIQvF2= NInoV3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK|5USU6JRWK8M4E,
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GCT M{LJWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3u5dGlvcGmkaYTpc44hd2ZiaIXtZY4hT0OWIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEGuNlYzPs7:TR?= NWPBZVZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
A375 NVHtXGlTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEHueo5KdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20NU42Ozl3zszN NUDkSpU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
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NCI-H2122 Mny0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;YNpNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRzLkm3{txO MnvlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
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8305C M2\yTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYO0cpZIUW6qaXLpeIlwdiCxZjDoeY1idiB6M{C1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ{Njd4N{ZOwG0> M2rXUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
NCI-H1395 MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkfUTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGzPVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC5zMEW1{txO MnXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
EW-16 MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYX6cplRUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjFyOUVOwG0> NXPSUnlvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
T98G NEi0NYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYHQdnRCUW6qaXLpeIlwdiCxZjDoeY1idiCWOUjHJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvPDJ2Nd88US=> M3T4XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
IST-SL2 MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFqxPGVKdmirYnn0bY9vKG:oIHj1cYFvKEmVVD3TUFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC57Mke5{txO NHfkT2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK|5USU6JRWK8M4E,
NCI-H1651 M3KyVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF2wRpRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR3LkmyNFjPxE1? NEPBVnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK|5USU6JRWK8M4E,
COR-L279 M4HXbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWXidXpVUW6qaXLpeIlwdiCxZjDoeY1idiCFT2KtUFI4QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR4LkKwPFHPxE1? Mnv6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
YT M3e0UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJHlVKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDZwNUC2O:69VQ>? NXrCSFduRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
TE-11 NVHIdFZzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFLmTIpKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFYvPzRyNN88US=> M3XVO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
C-33-A MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXrkXYRjUW6qaXLpeIlwdiCxZjDoeY1idiCFLUOzMWEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Pi56MUm3{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|c4PzJxJ{7TRW5ITVJ:L3G+
OVCAR-5 NFjTZmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWjJPJNiUW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk02KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDdwMkOwO:69VQ>? NGK2VYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK|5USU6JRWK8M4E,
PANC-03-27 NIrNe4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXTWSWFSUW6qaXLpeIlwdiCxZjDoeY1idiCSQV7DMVA{NTJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuN|UyO87:TR?= NH61Zms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK|5USU6JRWK8M4E,
CaR-1 M2L1c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;CTY5pcWKrdHnvckBw\iCqdX3hckBE[VJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4MlI1PzUQvF2= MkPhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
SNU-449 MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3ITY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFkvOjJ6Nd88US=> M2nPdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / PUMA ; 

PubMed: 27924057     


The expression of p53 or PUMA by western blotting analysis in HCT-116 cells treated with (left) 20 μM pazopanib for indicated hours or (right) with 1-20 μM pazopanib for 24 hours.

p-Akt / Akt ; 

PubMed: 27924057     


Akt is inhibited after pazopanib treatment in colon cells. The expression of P-Akt (S473) was detected by western blotting in (A) RKO or HT-29 cells after 20 μM pazopanib treatment for indicated times.

27924057
Growth inhibition assay
Cell viability; 

PubMed: 27924057     


Cell viability was analyzed using Cell Counting Kit-8 at 0, 3, 6, 12 and 24 hours after 1, 5, 10, or 20 μM pazopanib treatment in HCT-116 cells. Data represent the mean ± SEM of four independent experiments.

27924057
体内研究 与用载体或10毫克/千克Pazopanib处理的小鼠相比,用30毫克/千克或100毫克/千克Pazopanib处理的小鼠,肿瘤负荷显著降低。Pazopanib治疗具有良好的耐受性,并且每组小鼠的体重差异没有明显不同。[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)

动物实验:

[2]

- 合并
  • Animal Models: 含有SYO-1细胞的免疫缺陷小鼠
  • Dosages: 0 毫克/千克, 10 毫克/千克, 30毫克/千克, 或100 毫克/千克
  • Administration: 口服给药
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 87 mg/mL warmed (198.84 mM)
Water Insoluble
Ethanol Insoluble

* 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 437.52
化学式

C21H23N7O2S

CAS号 444731-52-6
储存条件 粉状
溶于溶剂
别名 GW786034

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、SDS / 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、SDS / 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
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 Recruiting 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
NCT03149120 Withdrawn Biological: Nivolumab|Drug: Pazopanib Soft Tissue Sarcomas NYU Langone Health|Bristol-Myers Squibb August 2017 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

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