Pazopanib HCl (GW786034 HCl)

Catalog No.S1035

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.

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Cited by 11 Publications

3 Customer Reviews

  • 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.
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 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml3RbY5pcWKrdIOgeIhmKF[HR1[tbY5lfWOnZDDwdo9tcW[ncnH0bY9vKG:oIFjVWmVEew>? NUPTPWRCOTh4MkCzPFI>
HUVEC NXH2d|M3U2mwYYPlJIF{e2G7 NYjPNG1GcW6qaXLpeJMhXkWJRj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDWSWdHWi1{IHnuJGhWXkWFIHPlcIx{KHerdHigZY4hUUN3MDDv[kDjkLx6IH7N M37Vb|E5PjJyM{iy
MM M1XUT2tqdmG|ZTDhd5NigQ>? NHvZXYFqdmirYnn0d{BXTUeILXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIH\seFE> MXOxO|E3PDN|Mh?=
MM.1S MkfwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYGxNEDPxGdxbVy= NVr2bVV{cW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= MVexO|E3PDN|Mh?=
MM.1R NGXzT4JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{jaUVExKM7:Zz;tUC=> NVjCeXd6cW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= NGi1NY0yPzF4NEOzNi=>
RPMI NHv2fZZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkXDNVAh|rypL33M NFfLe5ZqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= MlzCNVcyPjR|M{K=
Dox40 M1nQeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIfFXYsyOCEQvHevcWw> NUHDNGdHcW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= NVjJXVc4OTdzNkSzN|I>
INA-6 NFrOZlRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2[3c|ExKM7:Zz;tUC=> MX3pcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? MljRNVcyPjR|M{K=
OPM2 NHPjRm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnLlNVAh|rypL33M NWLBZoFZcW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= MWWxO|E3PDN|Mh?=
U266 NHniPHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml:2NVAh|rypL33M M4TyPYlvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq MUixO|E3PDN|Mh?=
MM.1S NIrsXIxkgXSxdH;4bYNqfHliYYPzZZk> MlTPNlAh|rypL33M MkjwbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= NXrmVJlJOTdzNkSzN|I>
MM.1R NIPCUYZkgXSxdH;4bYNqfHliYYPzZZk> M{\PdVIxKM7:Zz;tUC=> NVzTbpZLcW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> MYCxO|E3PDN|Mh?=
RPMI MnvtZ5l1d3SxeHnjbZR6KGG|c3H5 Mn3XNlAh|rypL33M NIrkbIxqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs M3Xab|E4OTZ2M{Oy
Dox40 MV\jfZRwfG:6aXPpeJkh[XO|YYm= MU[yNEDPxGdxbVy= M1P4RYlvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= M2WzV|E4OTZ2M{Oy
INA-6 MUXjfZRwfG:6aXPpeJkh[XO|YYm= MYmyNEDPxGdxbVy= NF30SGVqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs NH7yTFIyPzF4NEOzNi=>
OPM2 M3i1U4N6fG:2b4jpZ4l1gSCjc4PhfS=> MlvQNlAh|rypL33M NFTWXVdqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs Mki2NVcyPjR|M{K=
U266 NIq0PINkgXSxdH;4bYNqfHliYYPzZZk> NV7w[m4xOjBizsznM41N M2DYcIlvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= MmCyNVcyPjR|M{K=
MM.1S M1n4NmZ2dmO2aX;uJIF{e2G7 NHuzRXR{fXCycnXzd4V{KF[HR1[tTY5lfWOnZDDFcoRwfGinbHnhcEBE\WyuIGDyc4xq\mW{YYTpc44h[W6mIF3p[5JifGmxbj6= MlLrNVcyPjR|M{K=
MM.1R MVjGeY5kfGmxbjDhd5NigQ>? M3frbZN2eHC{ZYPz[ZMhXkWJRj3JcoR2[2WmIFXu[I91cGWuaXHsJGNmdGxiUILvcIln\XKjdHnvckBidmRiTXnndoF1cW:wLh?= NEnadGUyPzF4NEOzNi=>
Dox40 MX\GeY5kfGmxbjDhd5NigQ>? MVHzeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? M4npV|E4OTZ2M{Oy
OPM2 MkX3SpVv[3Srb36gZZN{[Xl? NID1NoF{fXCycnXzd4V{KF[HR1[tTY5lfWOnZDDFcoRwfGinbHnhcEBE\WyuIGDyc4xq\mW{YYTpc44h[W6mIF3p[5JifGmxbj6= NEHOZ3AyPzF4NEOzNi=>
HBMEC MlL5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH;n[WN,OTBizszN NW\EXodGTE2VTx?= M3;yUWlEPTB;MTFOwG0> MoDSNlExQDF4NU[=
HBMEC NVTWRVFXTnWwY4Tpc44h[XO|YYm= NVS1UHBKhjFizszN MUXEUXNQ MmnkZYJzd2ejdHXzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiVlXHSnIzKHerdHig[Il{enWydHnvckBw\iCmb4fud5Rz\WGvIGDMR:6{OQ>? M3rnTFIyODhzNkW2
HBMEC M4XYdmZ2dmO2aX;uJIF{e2G7 NEXxRYF,OSEQvF2= NI\PbmZFVVOR MkHk[Il{enWydIOgeIhmKFKjcz3SZYYuTVKNIIDheIh4[XlidHjyc5VocCCmZXPy[YF{\WRicHjvd5Bpd3K7bHH0[YQhVUWNMT:yJIFv\CCHUluxM|I> M2e4d|IyODhzNkW2
HBMEC MlPOSpVv[3Srb36gZZN{[Xl? M36xZ54zOCEQvF2= NHTISYFFVVOR NUnkW|Nb\Gm|coXweJMhPTBnIH;mJJR2[mViZn;ycYF1cW:wIHH0JFEh|ryP MYeyNVA5OTZ3Nh?=
MDA-MB-231 NGjjZ2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVH+NVAh|ryP NHTnNoJFVVOR MkS5TWM2OD13IN88US=> MWmyNVA5OTZ3Nh?=
MDA-MB-231 MVXGeY5kfGmxbjDhd5NigQ>? NV\sb5pzOC53IN88US=> NHn4fFFFVVOR NFn1[2dqdmirYnn0d{B1cGViRWLLNU8zKHOrZ37hcIlv\yCyYYToe4F6 M2LzOVIyODhzNkW2
MDA-MB-231 NGS4TmNHfW6ldHnvckBie3OjeR?= MoT1OUDPxE1? NIjKZY5FVVOR Ml;QbY5lfWOnczDhJINmdGxvY4njcIUh[XK{ZYP0 MkP6NlExQDF4NU[=
J82 MX3jfZRwfG:6aXPpeJkh[XO|YYm= MorlglExKM7:TR?= NXfP[GxKTE2VTx?= NVPEV4VDUUN3ME2yOE42PyEQvF2= M1\TR|IyPTJ7OUCw
T24 M{ewdoN6fG:2b4jpZ4l1gSCjc4PhfS=> MX;+NVAh|ryP NGm4eINFVVOR NITsSJVKSzVyPUWyMlQ2KM7:TR?= NXftZYtnOjF3Mkm5NFA>
HT1376 MXfjfZRwfG:6aXPpeJkh[XO|YYm= MU\+NVAh|ryP MYPEUXNQ NWfQPZJuUUN3ME2yPE4zOSEQvF2= MmjCNlE2Ojl7MEC=
RT4 M2HKNoN6fG:2b4jpZ4l1gSCjc4PhfS=> M1z2Vp4yOCEQvF2= NEjWWmZFVVOR NF;0WlhKSzVyPUWuNVQh|ryP NVPxNGxJOjF3Mkm5NFA>
CRL1749 M1XaUYN6fG:2b4jpZ4l1gSCjc4PhfS=> NWnkXpVRhjFyIN88US=> NFzPe2pFVVOR MoX4TWM2OD1{Mj62PUDPxE1? M3myVlIyPTJ7OUCw
HTB9 M13HToN6fG:2b4jpZ4l1gSCjc4PhfS=> NITNNXh,OTBizszN MXPEUXNQ NV\J[5ltUUN3ME2xNU45PCEQvF2= NX7hc3MxOjF3Mkm5NFA>
Sup M{ToXIN6fG:2b4jpZ4l1gSCjc4PhfS=> NILm[4V,OTBizszN MnHISG1UVw>? NFruN4RKSzVyPUWzMlMzKM7:TR?= MnH1NlE2Ojl7MEC=
HTB3 NVztcJlC[3m2b4TvfIlkcXS7IHHzd4F6 NVqyemNLhjFyIN88US=> Mn\xSG1UVw>? MYrJR|UxRTF2LkG2JO69VQ>? M334elIyPTJ7OUCw
CEC MV\GeY5kfGmxbjDhd5NigQ>? NWnwb5JZhjFyIN88[{9uVA>? MVjEUXNQ NXrqU|RQ\G:5bj3y[Yd2dGG2ZYOgWmVITiCuZY\lcJM> Ml3RNlE3OjB6MkK=
RPE MWXGeY5kfGmxbjDhd5NigQ>? NF\V[JR,OTBizsznM41N M4GybWROW09? MVTkc5dvNXKnZ4XsZZRmeyCYRVfGJIxmfmWucx?= MV[yNVYzODh{Mh?=
CEC NVfKb2RtTnWwY4Tpc44h[XO|YYm= M1vNeJ42KM7:Zz;tUC=> MUfEUXNQ NG[5RWhjdG:la4Og[Y5ld3SqZXzpZYwh[2WubDDtbYdz[XSrb36= MoS5NlE3OjB6MkK=
5637 NF;1PZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV\vRWxNTE2VTx?= NIPlPZVKSzVyPUG1MlDjiIoQvF2= NXnL[5g5OjN6OEe2NFU>
J82 NHHq[o9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2[4T2ROW09? Mmj1TWM2OD1zOD605qCK|ryP NXHHWnhtOjN6OEe2NFU>
5637 NXezWVlNSXW2b4DoZYd6KGG|c3H5 Mkm5NlAh|ryP M{\0ZmROW09? M3TQdZRzcWepZYLzJJRp\SCjdYTvdIhi\2mlIIDyc4Nme3N? NHq3WlczOzh6N{[wOS=>
J82 NVnKNnFtSXW2b4DoZYd6KGG|c3H5 M1;jS|IxKM7:TR?= NHnsfYxFVVOR NHfte2d1emmpZ3Xyd{B1cGViYYX0c5Bp[WerYzDwdo9k\XO| MViyN|g5PzZyNR?=
5637 MnnPSpVv[3Srb36gZZN{[Xl? MX[yNEDPxE1? MmjuSG1UVw>? MXTpcoR2[2W|IHz5d49{d22jbD3k[ZBmdmSnboSgcoVkem:|aYO= M4\WblI{QDh5NkC1
J82 MXLGeY5kfGmxbjDhd5NigQ>? M13iTlIxKM7:TR?= NVrX[FZoTE2VTx?= M17meYlv\HWlZYOgcJl{d3OxbXHsMYRmeGWwZHXueEBv\WO{b4Ppdy=> MXqyN|g5PzZyNR?=
5637 M{jifmZ2dmO2aX;uJIF{e2G7 NFe1WVczOCEQvF2= NGX4bpNFVVOR MlzqbY5lfWOnczDsfZNwe2:vZTDhcJRmemG2aX;uJIFv\CCrbnjpZol1eyCFQjDhZ5Rqfmm2eR?= M2K3WlI{QDh5NkC1
J82 NU\4SpN5TnWwY4Tpc44h[XO|YYm= MmDtNlAh|ryP NVr1V3RqTE2VTx?= MV3pcoR2[2W|IHz5d49{d22nIHHseIVz[XSrb36gZY5lKGmwaHnibZR{KEOEIHHjeIl3cXS7 NUnhPFdGOjN6OEe2NFU>
KATO-II Mn;yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MljDOUDPxE1? MYXEUXNQ MlnEZoxw[2u|IIDyc4xq\mW{YYTpc44> NXfEWpZVOjV{NEm1OVc>
OCUM-2M NWftXVE3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWC1JO69VQ>? MYPEUXNQ NX3Hd3JN[myxY3vzJJBzd2yrZnXyZZRqd25? NX7ROWJUOjV{NEm1OVc>
SNU-16 NEftVWNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1q2ZlUh|ryP NHHEOZZFVVOR NUjFPVVV[myxY3vzJJBzd2yrZnXyZZRqd25? MlH2NlUzPDl3NUe=
HSC-39 NFXtVolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{XRdlUh|ryP MmPTSG1UVw>? MXPicI9kc3NicILvcIln\XKjdHnvci=> M3HpVlI2OjR7NUW3
KATO-II M2K1doN6fG:2b4jpZ4l1gSCjc4PhfS=> MVH+NVAh|ryP NFfJcJZFVVOR MX7JR|UxRTBwMTD0c{AzNjBizsztc4wwVA>? NXPqOXlmOjV{NEm1OVc>
OCUM-2M NYrjfGxu[3m2b4TvfIlkcXS7IHHzd4F6 MXn+NVAh|ryP NX7XR2Q2TE2VTx?= NIDqN5BKSzVyPUCuNUB1dyB{LkCg{txud2xxTB?= MnrCNlUzPDl3NUe=
SNU-16 NVTC[Y1j[3m2b4TvfIlkcXS7IHHzd4F6 NX3mU|JbhjFyIN88US=> M{T0fGROW09? MoTpTWM2OD1yLkGgeI8hOi5yIN88cY9tN0x? NUnKN2h7OjV{NEm1OVc>
HSC-39 NEjhfoRkgXSxdH;4bYNqfHliYYPzZZk> M3K3T54yOCEQvF2= NV;HeJhUTE2VTx?= NVu3[WdZUUN3ME2wMlEhfG9iMj6wJO69dW:uL1y= MYKyOVI1QTV3Nx?=
NIH 3T3 MoLES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYnlNG9ShjFyIN88US=> NEDoboNFVVOR MlP3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W6mIHPvcI9vgSCob4LtZZRqd25? M4K5TFI2OjR7NUW3
KATO-III MWrGeY5kfGmxbjDhd5NigQ>? M3z6dVEh|ryP MnPDSG1UVw>? NELrcHdqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MYGyOVI1QTV3Nx?=
OCUM-2M NH;lN5dHfW6ldHnvckBie3OjeR?= MXuxJO69VQ>? M3LkWmROW09? NVjydYlxcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> NYfmWmk1OjV{NEm1OVc>
KATO-III NWTZdYpbSXCxcITvd4l{KGG|c3H5 MWixJO69VQ>? NVPUblNWTE2VTx?= NHXlbphqdmS3Y3XzJIFxd3C2b4Ppdy=> MWOyOVI1QTV3Nx?=
OCUM-2M M1;TdmFxd3C2b4Ppd{Bie3OjeR?= MkntNUDPxE1? NIjKZZFFVVOR M371RYlv\HWlZYOgZZBweHSxc3nz MlLVNlUzPDl3NUe=
KATO-III NWi2clVTTnWwY4Tpc44h[XO|YYm= NUH1enJGOSEQvF2= M3HhW2ROW09? NGjTOVFqdmirYnn0d{BHT0[UMjDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0he2mpbnHsbY5oKG2xbHXjeYxmew>? MkTRNlUzPDl3NUe=

... 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
  • Formulation: --
  • 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

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
NCT02979899 Completed Biological: TRC105|Drug: Votrient Advanced Angiosarcoma Tracon Pharmaceuticals Inc. February 13 2017 Phase 3

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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID