Pazopanib HCl (GW786034 HCl)

For research use only.

Catalog No.S1035

18 publications

Pazopanib HCl (GW786034 HCl) Chemical Structure

Molecular Weight(MW): 473.98

Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.

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Selleck's Pazopanib HCl (GW786034 HCl) has been cited by 18 publications

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  • IC50 of Pazopanib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. (B): VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined at indicated times in the presence or absence of Pazopanib.

    J Virol, 2011, 85(5): 2296-303. Pazopanib HCl (GW786034 HCl) purchased from Selleck.

  • Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).

    Expert Opin Pharmacother 2014 15(11), 1489-99. Pazopanib HCl (GW786034 HCl) purchased from Selleck.

  • MRC5 non-transformed human lung fibroblasts were infected with influenza viruses (100 multiplicity of infection). Two hours after infection the cells were treated with vehicle control; sorafenib tosylate (2mM); pazopanib (2mM); OSU-03012 (2mM); and AR-13 (2mM). Twenty-four hours after infection the cells are treated with live/dead agent where green cells are viable and cells staining yellow or red are considered dead. Cells are examined at 10 magnification in a Hermes wide-field microscope (n¼3 SEM) P<0.05 less than vehicle control level of virus-mediated cell killing.

    J Cell Physiol, 2016, 231(10):2286-302.. Pazopanib HCl (GW786034 HCl) purchased from Selleck.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
Features A multi-kinase inhibitor.
Targets
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)
10 nM 30 nM 47 nM 74 nM 84 nM
In vitro

Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. [1] Pazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of Pazopanib and is completely abolished at 5 µg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. [2] Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC NIPBfJRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmfhbY5pcWKrdIOgeIhmKF[HR1[tbY5lfWOnZDDwdo9tcW[ncnH0bY9vKG:oIFjVWmVEew>? NFrCRo8yQDZ{MEO4Ni=>
HUVEC NXm0RZpmU2mwYYPlJIF{e2G7 NX60ZlV2cW6qaXLpeJMhXkWJRj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDWSWdHWi1{IHnuJGhWXkWFIHPlcIx{KHerdHigZY4hUUN3MDDv[kDjkLx6IH7N MUexPFYzODN6Mh?=
MM MnPQT4lv[XOnIHHzd4F6 MWHpcohq[mm2czDWSWdHNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKG[udEG= M4XWOVE4OTZ2M{Oy
MM.1S MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHETndKOTBizsznM41N MmrJbY5pcWKrdIOgUW0hS2WubDDHdo94fGh? NV7W[XdoOTdzNkSzN|I>
MM.1R NUHDTnZ1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HJblExKM7:Zz;tUC=> NGHpWotqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= NVHr[4dNOTdzNkSzN|I>
RPMI NGLPdIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYPHT2ZnOTBizsznM41N NEGwdW1qdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= MVixO|E3PDN|Mh?=
Dox40 M17VVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;oOpBYOTBizsznM41N M2rDSIlvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq NFHMbWwyPzF4NEOzNi=>
INA-6 M4Cwfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlLXNVAh|rypL33M Mof0bY5pcWKrdIOgUW0hS2WubDDHdo94fGh? NHPFXokyPzF4NEOzNi=>
OPM2 NXjXU|RWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NW\DeJBwOTBizsznM41N NXX3fYlEcW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= M2q3cFE4OTZ2M{Oy
U266 M{DJXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3u5cFExKM7:Zz;tUC=> NEn5RYxqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= NF\EPXYyPzF4NEOzNi=>
MM.1S MYjjfZRwfG:6aXPpeJkh[XO|YYm= NHH6OYszOCEQvHevcWw> MkDUbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= M{DFblE4OTZ2M{Oy
MM.1R NGPJXpdkgXSxdH;4bYNqfHliYYPzZZk> NVHyeXNJOjBizsznM41N MnfRbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= MnXFNVcyPjR|M{K=
RPMI MXHjfZRwfG:6aXPpeJkh[XO|YYm= NEDKeIczOCEQvHevcWw> MYPpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu NX6wemhKOTdzNkSzN|I>
Dox40 M4fzUoN6fG:2b4jpZ4l1gSCjc4PhfS=> MVeyNEDPxGdxbVy= MlPSbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= MYSxO|E3PDN|Mh?=
INA-6 MnvwZ5l1d3SxeHnjbZR6KGG|c3H5 NVfKOWNYOjBizsznM41N NWn2OpNTcW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> MX2xO|E3PDN|Mh?=
OPM2 M3\5d4N6fG:2b4jpZ4l1gSCjc4PhfS=> NXzh[4N6OjBizsznM41N MVjpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu MVqxO|E3PDN|Mh?=
U266 NVjWPFZm[3m2b4TvfIlkcXS7IHHzd4F6 MWWyNEDPxGdxbVy= Moj6bY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= MUWxO|E3PDN|Mh?=
MM.1S NULmZXpsTnWwY4Tpc44h[XO|YYm= M2\4S5N2eHC{ZYPz[ZMhXkWJRj3JcoR2[2WmIFXu[I91cGWuaXHsJGNmdGxiUILvcIln\XKjdHnvckBidmRiTXnndoF1cW:wLh?= NXvPe3pzOTdzNkSzN|I>
MM.1R MV7GeY5kfGmxbjDhd5NigQ>? MVjzeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? M1XGTVE4OTZ2M{Oy
Dox40 M4rhT2Z2dmO2aX;uJIF{e2G7 MWnzeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? NI\FbVgyPzF4NEOzNi=>
OPM2 NVeyWY1XTnWwY4Tpc44h[XO|YYm= MXTzeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? MXOxO|E3PDN|Mh?=
HBMEC MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXz+NVAh|ryP MmjqSG1UVw>? NH7ldoFKSzVyPUGg{txO MlPBNlExQDF4NU[=
HBMEC M{XU[mZ2dmO2aX;uJIF{e2G7 NHLseI5,OSEQvF2= MkXYSG1UVw>? NI\kSpVi[nKxZ3H0[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDWSWdHWjJid3n0bEBlcXO{dYD0bY9vKG:oIHTve45{fHKnYX2gVGxE|rNz M1\2bFIyODhzNkW2
HBMEC NVX1Omh[TnWwY4Tpc44h[XO|YYm= MoT0glEh|ryP M2fHNGROW09? NF7OWY1lcXO{dYD0d{B1cGViUnHzMXJi\i2HUlugdIF1cHejeTD0bJJwfWeqIHTlZ5Jm[XOnZDDwbI9{eGixconsZZRm\CCPRVuxM|Ih[W6mIFXST|EwOg>? MnHqNlExQDF4NU[=
HBMEC NWC3U5A5TnWwY4Tpc44h[XO|YYm= NEjHfJN,OjBizszN MkfsSG1UVw>? M2nzUIRqe3K3cITzJFUxLSCxZjD0eYJmKG[xcn3heIlwdiCjdDCxJO69VQ>? MYOyNVA5OTZ3Nh?=
MDA-MB-231 M2jZVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX3+NVAh|ryP NGm0d|RFVVOR MYfJR|UxRTVizszN MYOyNVA5OTZ3Nh?=
MDA-MB-231 MmfmSpVv[3Srb36gZZN{[Xl? MV2wMlUh|ryP NGX5eWZFVVOR NHTvXHBqdmirYnn0d{B1cGViRWLLNU8zKHOrZ37hcIlv\yCyYYToe4F6 NYLrWGY2OjFyOEG2OVY>
MDA-MB-231 NXOzb5QxTnWwY4Tpc44h[XO|YYm= M2P6eVUh|ryP NIXPU4JFVVOR MYnpcoR2[2W|IHGgZ4VtdC2leXPs[UBienKnc4S= NVPuZ3ZNOjFyOEG2OVY>
J82 MUHjfZRwfG:6aXPpeJkh[XO|YYm= M{PLOZ4yOCEQvF2= MVLEUXNQ MYPJR|UxRTJ2LkW3JO69VQ>? MlTINlE2Ojl7MEC=
T24 MluyZ5l1d3SxeHnjbZR6KGG|c3H5 NE\NPXl,OTBizszN NHrh[W9FVVOR MWDJR|UxRTV{LkS1JO69VQ>? MmXvNlE2Ojl7MEC=
HT1376 NX24Z3pN[3m2b4TvfIlkcXS7IHHzd4F6 NI[xXll,OTBizszN NFTqfXBFVVOR NGXoV5lKSzVyPUK4MlIyKM7:TR?= MUOyNVUzQTlyMB?=
RT4 M13tcYN6fG:2b4jpZ4l1gSCjc4PhfS=> NYS5XZc3hjFyIN88US=> MW\EUXNQ NED6TXBKSzVyPUWuNVQh|ryP NVvCcnUyOjF3Mkm5NFA>
CRL1749 NWD4ZYpC[3m2b4TvfIlkcXS7IHHzd4F6 NH36bol,OTBizszN MX7EUXNQ MkPDTWM2OD1{Mj62PUDPxE1? M4LkU|IyPTJ7OUCw
HTB9 NWjMbG81[3m2b4TvfIlkcXS7IHHzd4F6 MoT5glExKM7:TR?= NYfiZ25wTE2VTx?= NFHLXIlKSzVyPUGxMlg1KM7:TR?= MUiyNVUzQTlyMB?=
Sup NWr2NYxX[3m2b4TvfIlkcXS7IHHzd4F6 MYX+NVAh|ryP Mm[3SG1UVw>? M3TXNmlEPTB;NUOuN|Ih|ryP NYf3VmNSOjF3Mkm5NFA>
HTB3 M2TTUIN6fG:2b4jpZ4l1gSCjc4PhfS=> MmjIglExKM7:TR?= NYfoZXNuTE2VTx?= NXjVXphSUUN3ME2xOE4yPiEQvF2= Mo[0NlE2Ojl7MEC=
CEC NFy5fY1HfW6ldHnvckBie3OjeR?= MVr+NVAh|rypL33M NWjSUJM{TE2VTx?= MUHkc5dvNXKnZ4XsZZRmeyCYRVfGJIxmfmWucx?= NF3mbngzOTZ{MEiyNi=>
RPE MnLWSpVv[3Srb36gZZN{[Xl? NFfZUJR,OTBizsznM41N M1;HZWROW09? Mmnt[I94di2{ZXf1cIF1\XNiVlXHSkBt\X[nbIO= MkH0NlE3OjB6MkK=
CEC M4rueWZ2dmO2aX;uJIF{e2G7 M3X0SJ42KM7:Zz;tUC=> NWXHNGc1TE2VTx?= Mkj2Zoxw[2u|IHXu[I91cGWuaXHsJINmdGxibXnndoF1cW:w NXv1OlFXOjF4MkC4NlI>
5637 NHLmeWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NE\oXlhFVVOR MVPJR|UxRTF3LkFihKnPxE1? MUSyN|g5PzZyNR?=
J82 NEW3WFlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHP3ZXdFVVOR NUH1RoRsUUN3ME2xPE416oDLzszN NVf3b2FLOjN6OEe2NFU>
5637 Mk\qRZV1d3CqYXf5JIF{e2G7 M1LLWlIxKM7:TR?= NFP3d2xFVVOR MUf0dolo\2W{czD0bIUh[XW2b4DoZYdq[yCycn;j[ZN{ MXuyN|g5PzZyNR?=
J82 NX7IN5hMSXW2b4DoZYd6KGG|c3H5 M4nQNVIxKM7:TR?= M365SmROW09? MWL0dolo\2W{czD0bIUh[XW2b4DoZYdq[yCycn;j[ZN{ MVKyN|g5PzZyNR?=
5637 M4DGOmZ2dmO2aX;uJIF{e2G7 NEjQdXgzOCEQvF2= Ml[xSG1UVw>? MUjpcoR2[2W|IHz5d49{d22jbD3k[ZBmdmSnboSgcoVkem:|aYO= NVXKNHZLOjN6OEe2NFU>
J82 NF7keIlHfW6ldHnvckBie3OjeR?= M{fEe|IxKM7:TR?= MnzqSG1UVw>? MVLpcoR2[2W|IHz5d49{d22jbD3k[ZBmdmSnboSgcoVkem:|aYO= M3;uRVI{QDh5NkC1
5637 MXHGeY5kfGmxbjDhd5NigQ>? NHT6ZZQzOCEQvF2= M{Dw[WROW09? M1rFPIlv\HWlZYOgcJl{d3OxbXWgZYx1\XKjdHnvckBidmRiaX7obYJqfHNiQ1KgZYN1cX[rdIm= M3j0dVI{QDh5NkC1
J82 NHjzeVVHfW6ldHnvckBie3OjeR?= NI\yTpUzOCEQvF2= MYDEUXNQ NH\rZpRqdmS3Y3XzJIx6e2:|b33lJIFtfGW{YYTpc44h[W6mIHnubIljcXS|IFPCJIFkfGm4aYT5 MlfqNlM5QDd4MEW=
KATO-II MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWnYNnhsPSEQvF2= NXjke5hTTE2VTx?= MWPicI9kc3NicILvcIln\XKjdHnvci=> M4TFXVI2OjR7NUW3
OCUM-2M MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILqWnQ2KM7:TR?= MVjEUXNQ MlzNZoxw[2u|IIDyc4xq\mW{YYTpc44> NHWzN|YzPTJ2OUW1Oy=>
SNU-16 M2TiOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnXtOUDPxE1? NXv0dWdMTE2VTx?= MmPTZoxw[2u|IIDyc4xq\mW{YYTpc44> M3rSSFI2OjR7NUW3
HSC-39 NWjrS2tZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHiwfGg2KM7:TR?= NH25NJdFVVOR M2PUToJtd2OtczDwdo9tcW[ncnH0bY9v MYGyOVI1QTV3Nx?=
KATO-II MlPhZ5l1d3SxeHnjbZR6KGG|c3H5 MnTrglExKM7:TR?= MWPEUXNQ M2DpNWlEPTB;MD6xJJRwKDJwMDFOwI1wdC:O M3XvWFI2OjR7NUW3
OCUM-2M NWrHd4tm[3m2b4TvfIlkcXS7IHHzd4F6 NIfoenB,OTBizszN MUXEUXNQ NXjiOJdVUUN3ME2wMlEhfG9iMj6wJO69dW:uL1y= NV60N4ZOOjV{NEm1OVc>
SNU-16 MonvZ5l1d3SxeHnjbZR6KGG|c3H5 NFSzc3p,OTBizszN NVK3[Io4TE2VTx?= NH3y[JJKSzVyPUCuNUB1dyB{LkCg{txud2xxTB?= MUGyOVI1QTV3Nx?=
HSC-39 NHP1bWpkgXSxdH;4bYNqfHliYYPzZZk> MkPPglExKM7:TR?= NImxfVlFVVOR NVPWU|B1UUN3ME2wMlEhfG9iMj6wJO69dW:uL1y= MV:yOVI1QTV3Nx?=
NIH 3T3 NGfEco9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVHBUFlNhjFyIN88US=> M3zrOmROW09? NVTsU|hDcW6qaXLpeJMh[2WubDDndo94fGhiYX7kJINwdG:weTDmc5Ju[XSrb36= NFHwN2czPTJ2OUW1Oy=>
KATO-III MYPGeY5kfGmxbjDhd5NigQ>? MXKxJO69VQ>? M2HkdmROW09? MmS2bY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= MnK4NlUzPDl3NUe=
OCUM-2M M1;DU2Z2dmO2aX;uJIF{e2G7 MlnQNUDPxE1? NUfQfldPTE2VTx?= MWrpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 MV2yOVI1QTV3Nx?=
KATO-III MV3BdI9xfG:|aYOgZZN{[Xl? NYOwdpdsOSEQvF2= NWS3eXVvTE2VTx?= NXvsXYtbcW6mdXPld{BieG:ydH;zbZM> MX:yOVI1QTV3Nx?=
OCUM-2M NHTCe5lCeG:ydH;zbZMh[XO|YYm= NWniOFRLOSEQvF2= M2XyW2ROW09? MlnubY5lfWOnczDhdI9xfG:|aYO= NYLpRZR3OjV{NEm1OVc>
KATO-III M4TTcWZ2dmO2aX;uJIF{e2G7 MVKxJO69VQ>? MY\EUXNQ NEPlXHpqdmirYnn0d{BHT0[UMjDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0he2mpbnHsbY5oKG2xbHXjeYxmew>? M1G0VFI2OjR7NUW3

... 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 RKO or HT-29 cells after 20 μM pazopanib treatment for indicated times.

p-VEGFR2 / p-c-Kit / p-PDGFRβ / FLT-3 ; 

PubMed: 19844230     


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     


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     


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
In vivo The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group. [2]

Protocol

Kinase Assay:

[1]

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Kinase enzyme assays:

VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated Pazopanib in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs.
Cell Research:

[1]

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  • Cell lines: HUVEC cells
  • Concentrations: 0-10 μM
  • Incubation Time: 1 hour
  • Method:

    Phosphorylation of VEGFR2 is assessed in HUVEC stimulated with VEGF. HUVEC are plated in type-I collagen-coated 10 cm plates in Clonetics EGM-MV medium at 1.0-1.5 × 106 cells/plate. After 24 hours, the confluent cells are serum starved overnight by replacing the growth medium with Clonetics EBM medium containing 0.1% BSA, 500 μg/mL hydrocortisone. Cells are treated with Pazopanib at various concentrations for 1 hour, followed by addition of 10 ng/mL VEGF or vehicle for 10 min. Cells are solubilized in lysis buffer. VEGFR2 is immunoprecipitated using antiflk-1 antibody and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Western blotting and detection with antiflk-1 or with antiphosphotyrosine (anti-P-tyr-biotin) antibody. The VEGFR2 phosphorylation level is quantified by densitometry and normalized to the total VEGFR2 level.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Immunodeficient mice bearing SYO-1 cells
  • Dosages: 0 mg/kg, 10 mg/kg, 30 mg/kg, or 100 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 17 mg/mL (35.86 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 473.98
Formula

C21H23N7O2S.HCl

CAS No. 635702-64-6
Storage powder
in solvent
Synonyms N/A
Smiles Cl.C[N]1N=C2C=C(C=CC2=C1C)N(C)C3=NC(=NC=C3)NC4=CC=C(C)C(=C4)[S](N)(=O)=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT03091465 Completed -- Metastatic Renal Cell Carcinoma Spanish Oncology Genito-Urinary Group December 20 2016 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID