Pazopanib HCl (GW786034 HCl)

For research use only. Not for use in humans.

目录号：S1035 中文名称：盐酸帕佐帕尼

Pazopanib HCl (GW786034 HCl) Chemical Structure

CAS No. 635702-64-6

Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，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。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1565.32	现货
10mg	RMB 1225.19	现货
25mg	RMB 2231.51	现货
100mg	RMB 3031.75	现货
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客户使用Selleck生产的Pazopanib HCl (GW786034 HCl)发表文献35篇：

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Discov, 2013, 3(6):636-47

PubMed: 23558953 ( click the link to review the publication )

J Clin Endocrinol Metab, 2021, dgab020

PubMed: 33524147 ( click the link to review the publication )

Radiother Oncol, 2021, 157:175-181

PubMed: 33516789 ( click the link to review the publication )

Drug Metab Dispos, 2021, 49(1):53-61

PubMed: 33148688 ( click the link to review the publication )

Cancer Res, 2020, canres.1992.2020

PubMed: 33203698 ( click the link to review the publication )

Cancers (Basel), 2020, 27;12(5)pii: E1087

PubMed: 32349331 ( click the link to review the publication )

Cancers (Basel), 2020, 13;12(2) pii: E436

PubMed: 32069833 ( click the link to review the publication )

Cancers (Basel), 2020, 17;12(1):232

PubMed: 31963500 ( click the link to review the publication )

Cancers (Basel), 2020, 10;12(6):E1519

PubMed: 32531992 ( click the link to review the publication )

J Mater Chem B, 2020, 10.1039/d0tb00724b

PubMed: 32365151 ( click the link to review the publication )

Front Oncol, 2020, 12;10:696

PubMed: 32528877 ( click the link to review the publication )

Biochem Pharmacol, 2020, 182:114227

PubMed: 32966814 ( click the link to review the publication )

Cancer Cell Int, 2020, 19;20:58

PubMed: 32099531 ( click the link to review the publication )

Toxicol In Vitro, 2020, 71:105063

PubMed: 33271325 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00425-8

PubMed: 32886306 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Neoplasia, 2020, 22(10):470-483

PubMed: 32818841 ( click the link to review the publication )

Cell Rep, 2019, 28(9):2331-2344

PubMed: 31461650 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)E1945

PubMed: 31817360 ( click the link to review the publication )

J Pharm Sci, 2019, 108(3):1272-1283

PubMed: 30773203 ( click the link to review the publication )

Nat Commun, 2018, 9(1):358

PubMed: 29367740 ( click the link to review the publication )

Cancers (Basel), 2018, 10(10)E365

PubMed: 30274248 ( click the link to review the publication )
Oncoimmunology, 2018,

PubMed: 30393581 ( click the link to review the publication )

Clin Exp Hypertens, 2018, 40(6):524-533

PubMed: 29172746 ( click the link to review the publication )

Arch Toxicol, 2017, 91(8):2921-2938

PubMed: 28032146 ( click the link to review the publication )

PLoS ONE, 2017,

PubMed: 28945796 ( click the link to review the publication )

J Cell Physiol, 2016, 231(10):2286-302

PubMed: 27187154 ( click the link to review the publication )

Oncotarget, 2016, 7(11):12975-96

PubMed: 26887051 ( click the link to review the publication )

Tissue Cell, 2015, 47(3):301-10

PubMed: 25958163 ( click the link to review the publication )

Oncotarget, 2015, 6(29):27227-38

PubMed: 26317900 ( click the link to review the publication )

Expert Opin Pharmaco, 2014, 15(11):1489-99

PubMed: 24890457 ( click the link to review the publication )

J Virol, 2011, 85(5):2296-303

PubMed: 21177802 ( click the link to review the publication )

Expert Opin Pharmacother, 2011, 12(7):1171-89

PubMed: 21470066 ( click the link to review the publication )

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述

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	点击更多

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
HT-29	NHXPW2tHfW6ldHnvckBie3OjeR?=		MYOxOEB1dyB{NDDodpM>		MUDJcohq[mm2aX;uJI9nKFKLUFuxJIlvKGi3bXHuJGhVNTJ7IHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBVVk[jbIDoZU1qdmS3Y3XkJI5m[3KxcITvd4l{KGmwY4XiZZRm\CCob4KgNVQhfG9iMkSgbJJ{KGmwIIDy[ZNmdmOnIH;mJHNu[WNibXnt[ZRq[yCjbnSgfk1XSURvRl3LJIJ6KGOnbHygeIl1\XJiZ3zvMYJie2WmIHz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD1yLki3N:69VQ>?	M4LBcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkKyNFk3Lz5\|MU[yNlA6PjxxYU6=
HT29	MmP1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?				NWDJV5dDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWFI6KGOnbHzzJIlvKHOncoXtJINwdnSjaX7pcochdWWmaYXt	NFnieIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[yNFM5Oid-MUi2NlA{QDJ:L3G+
HN5	NWm2T3dsSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=				MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxteyCrbjDz[ZJ2dSClb370ZYlvcW6pIH3l[Il2dQ>?	M13vUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkKwN\|gzLz5zOE[yNFM5OjxxYU6=
A375P	M2\5[2FvfGmycn;sbYZmemG2aY\lJIF{e2G7				Mn:1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDM{e1VEBk\WyuczDpckB{\XK3bTDjc451[WmwaX7nJI1m\Gm3bR?=	NEfDR2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[yNFM5Oid-MUi2NlA{QDJ:L3G+
SJ-GBM2	NITHT\|VyUFSVIHHzd4F6				NHfoOWtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=>	Ml\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	M1:wcJFJXFNiYYPzZZk>				NXvq[mFYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	MnPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	MnzJdWhVWyCjc4PhfS=>				NXy5UIhTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	NHu0SG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB-EBc1	M1fkW5FJXFNiYYPzZZk>				MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?=	MkfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Saos-2	NVX4OHhQeUiWUzDhd5NigQ>?				M2XBTZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	M4LI[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	MmGzdWhVWyCjc4PhfS=>				MYHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	MmDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-12	NVviOJlReUiWUzDhd5NigQ>?				MnOxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy\|	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	MVfxTHRUKGG\|c3H5				MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	NGPPclg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh18	NF3yRY9yUFSVIHHzd4F6				NEP2U4JyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?=	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
OHS-50	NWfIVmlpeUiWUzDhd5NigQ>?				NHL1Z\|NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	NVXFOYNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R)	M3nS[JFJXFNiYYPzZZk>				MUHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	MlzGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	Mn;rdWhVWyCjc4PhfS=>				MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{	M1S3TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS	NGjJO5NyUFSVIHHzd4F6				MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDVMVIhV1NiY3XscJM>	NEDJNYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	MlXudWhVWyCjc4PhfS=>				M1PMWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM>	NH74W4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-SH	NIPuNlJyUFSVIHHzd4F6				NUnScIFzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?=	NHzFVHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
HUVEC	M{DtSGZ2dmO2aX;uJIF{e2G7	MV6xNFAhdk1?	M4W2VVIhcHK\|		M2joeGlvcGmkaYTpc44hd2ZiVlXHSk1{fGmvdXzheIVlKF[HR1\SNkBxcG:\|cHjvdplt[XSrb36gbY4hcHWvYX6gTHVXTUNiY3XscJMh[XRiMUCwJI5OKHC{ZXnuZ5Vj[XSnZDDmc5IhOiCqcoOg[o9tdG:5ZXSgZpkhXkWJRjDzeIlufWyjdHnvckBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	NXPDXWpFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3PFczPjJpPkK5O\|g4OjZ{PD;hQi=>
HUVEC	Ml;FRY51cWGwZ3nv[4VvcWNiYYPzZZk>	NVTSSlJbOC5zIIXN	NYXCWpF7PiCqcoO=		MXnBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCrbjDoeY1idiCKVW\FR{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3HwbYxt[XK7LXzpb4UhfHWkdXzhdkBv\XS5b4LrJIZwem2jdHnvckBifCByLkGgeW0h[W[2ZYKgOkBpenNiYomgdIhie2VvY3;ueJJie3RibXnjdo9{[2:yeR?=	NFzt[mI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe4O\|I3Oid-Mkm3PFczPjJ:L3G+
MM	NETm[ndMcW6jc3WgZZN{[Xl?				M3q2VolvcGmkaYTzJHZGT0ZvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiZnz0NS=>	NUfm[ZlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexOlQ{OzJpPkG3NVY1OzN{PD;hQi=>
MM.1S	MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MofHNVAh\|rypL33M			MlTIbY5pcWKrdIOgUW0hS2WubDDHdo94fGh?	M2\BblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MU[0N\|MzLz5zN{G2OFM{OjxxYU6=
MM.1R	NYXJbYdlT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NYfkSVlKOTBizsznM41N			NWHMfpJucW6qaXLpeJMhVU1iQ3XscEBIem:5dHi=	M2XQR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MU[0N\|MzLz5zN{G2OFM{OjxxYU6=
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MEG-01	M3G4NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7				NXvlW\|dkUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01OS54MUG2{txONg>?	NH\ITmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK\|5USU6JRWK8M4E,
NCI-H2122	NWfXfHlMT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=				MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQyNjl5zszNMi=>	M{DZeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
RPMI-2650	NILpSolIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				MYTJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvMk[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ{NjR5OEVOwG0v	M2LZdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
8305C	Mn32S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?				MkW2TY5pcWKrdHnvckBw\iCqdX3hckA5OzB3QzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUSzMlc3PzYQvF2u	MmTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
NCI-H1395	MmDLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?				MWrJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUO5OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjFyNUZOwG0v	NV7acpV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
EW-16	M2L2[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7				NHfydWpKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvOTB7NN88UU4>	NVrKTlNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
T98G	MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?				NGfVfJpKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OE41OjR3zszNMi=>	M2DDcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
IST-SL2	M4jRbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7				NEnlemZKdmirYnn0bY9vKG:oIHj1cYFvKEmVVD3TUFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC57Mke5{txONg>?	MnSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
NCI-H1651	M3;rOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7				NITKXYhKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTR3LkmyNFjPxE1w	M2f2bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
COR-L279	NUT4Z2JkT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=				NULxNZNXUW6qaXLpeIlwdiCxZjDoeY1idiCFT2KtUFI4QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTR4LkKwPFHPxE1w	M2XVUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
YT	NF\Ge29Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=				MmPtTY5pcWKrdHnvckBw\iCqdX3hckB[XCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTR4LkWwOlfPxE1w	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O\|c4PzJxJ{7TRW5ITVJ:L3G+
TE-11	NFnmUZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				Mnq5TY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUS2Mlc1ODUQvF2u	MnPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
C-33-A	NIf4[2xIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				MmfLTY5pcWKrdHnvckBw\iCqdX3hckBENTN\|LVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Ok45OTl5zszNMi=>	NYC0N5pKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd5N{eyM{c,W0GQR1XSQE9iRg>?
OVCAR-5	MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?				MWXJcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20O{4zOzB5zszNMi=>	M33MdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4Pzd5Mj:nQnNCVkeHUkyvZV4>
PANC-03-27	MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?				NXi2VXVSUW6qaXLpeIlwdiCxZjDoeY1idiCSQV7DMVA{NTJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NEeuN\|UyO87:TT6=	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O\|c4PzJxJ{7TRW5ITVJ:L3G+
CaR-1	NYT0ZZFQT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=				MYPJcohq[mm2aX;uJI9nKGi3bXHuJGNiWi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NEiuNlQ4PM7:TT6=	MmjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc4Pzd{Lze+V2FPT0WUPD;hQi=>
SNU-449	NIXncXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				MlvITY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFkvOjJ6Nd88UU4>	NE\MUnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Pzd5N{KvK\|5USU6JRWK8M4E,

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p53 / PUMA; PubMed: 27924057 Oncotarget 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 Oncotarget Akt is inhibited after pazopanib treatment in colon cells. The expression of P-Akt (S473) was detected by western blotting in RKO or HT-29 cells after 20 μM pazopanib treatment for indicated times. p-VEGFR2 / p-c-Kit / p-PDGFRβ / FLT-3 ; PubMed: 19844230 Br J Cancer Inhibition of receptor autophosphorylation by various tyrosine kinase inhibitors. To compare the activities of pazopanib, sunitinib, and sorafenib, we evaluated their inhibitory effects against wild-type VEGFR-2, c-Kit, PDGFR-β, and Flt-3 receptors in HUVEC (for VEGFR-2), NCI-H526 (c-Kit), HFF (PDGFR-β), and RS4;11 (Flt-3). Cells were serum-starved overnight and then treated with DMSO or different concentrations of pazopanib, sunitinib, or sorafenib for 2 h. Cells were then stimulated with respective ligands as described in the cellular autophosphorylation section under Materials and Methods. Total receptor was immunoprecipitated using antireceptor antibodies and phosphorylation was detected using anti-pTyr antibody following western blot analysis.	27924057 19844230
Immunofluorescence	YAP/TAZ; PubMed: 26199863 FEBS Open Bio Dasatinib, fluvastatin, and pazopanib inhibited the nuclear localization of YAP and TAZ. MDA-MB-231 cells were treated with inhibitors for 8 h and YAP and TAZ were visualized by immunofluorescence. (i) Representative images of immunofluorescence. Bar represents 10 μm.	26199863
Growth inhibition assay	Cell viability; PubMed: 27924057 Oncotarget 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]。

激酶实验： ^[1]	- 合并激酶活性测定: 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]	- 合并 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。 (Only for Reference)
动物实验： ^[2]	- 合并 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 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	17 mg/mL (35.86 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)： 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 Download Pazopanib HCl (GW786034 HCl) SDF

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
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

每只动物给药体积

动物数量

只

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，注：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：取 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。

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。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2021-01-06)

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	Recruiting	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

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操作手册

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VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

选择性强的VEGFR抑制剂

Vandetanib (ZD6474) : VEGFR2-selective, IC50=40 nM.
活性最高的VEGFR抑制剂

Cabozantinib (XL184, BMS-907351) : VEGFR2, IC50=0.035 nM.
FDA批准的VEGFR抑制剂

Axitinib : Approved by FDA for Renal Cell Carcinoma.
经典的VEGFR抑制剂

Nintedanib (BIBF 1120) : Potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM. Phase 3.

研究领域

产品类型

定制您的化合物库

Pazopanib HCl (GW786034 HCl)

客户使用Selleck生产的Pazopanib HCl (GW786034 HCl)发表文献35篇：

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Pazopanib HCl (GW786034 HCl) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技术支持

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

相关VEGFR产品