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 9 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 MlzlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH\M[WdqdmirYnn0d{B1cGViVlXHSk1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gTHVXTUO| M3nnOlE5PjJyM{iy
HUVEC MV;LbY5ie2ViYYPzZZk> NYPqdmtEcW6qaXLpeJMhXkWJRj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDWSWdHWi1{IHnuJGhWXkWFIHPlcIx{KHerdHigZY4hUUN3MDDv[kDjkLx6IH7N M33aOlE5PjJyM{iy
MM MlT1T4lv[XOnIHHzd4F6 MXPpcohq[mm2czDWSWdHNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKG[udEG= MXmxO|E3PDN|Mh?=
MM.1S MofpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUnySnVqOTBizsznM41N M1rOOYlvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq NHL1Xm4yPzF4NEOzNi=>
MM.1R NV;NOHlHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVfSTnhyOTBizsznM41N MUDpcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? NH\KZlAyPzF4NEOzNi=>
RPMI MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn2zNVAh|rypL33M MVrpcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? NF;YSYQyPzF4NEOzNi=>
Dox40 NETtbYpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEDtXIMyOCEQvHevcWw> NFPIU5dqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= NUPDXW5HOTdzNkSzN|I>
INA-6 M3SzXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEPEepIyOCEQvHevcWw> NH\DVY9qdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= M3HEO|E4OTZ2M{Oy
OPM2 NXWyUYlxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXSxNEDPxGdxbVy= NXKzZXJ6cW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= M361bVE4OTZ2M{Oy
U266 MnLoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYqxNEDPxGdxbVy= MorGbY5pcWKrdIOgUW0hS2WubDDHdo94fGh? Ml3sNVcyPjR|M{K=
MM.1S NYXPVnBH[3m2b4TvfIlkcXS7IHHzd4F6 MoThNlAh|rypL33M NH7W[mJqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs Mmq5NVcyPjR|M{K=
MM.1R NID1codkgXSxdH;4bYNqfHliYYPzZZk> M3\EelIxKM7:Zz;tUC=> MmrrbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= Mnr2NVcyPjR|M{K=
RPMI M3rRcIN6fG:2b4jpZ4l1gSCjc4PhfS=> NU[x[nNZOjBizsznM41N NXGxUo9bcW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> M36yelE4OTZ2M{Oy
Dox40 MXzjfZRwfG:6aXPpeJkh[XO|YYm= Mk\RNlAh|rypL33M M3\VS4lvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= M13oblE4OTZ2M{Oy
INA-6 NHSyfFdkgXSxdH;4bYNqfHliYYPzZZk> M{TJblIxKM7:Zz;tUC=> M4nYVolvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= NYrhelJ7OTdzNkSzN|I>
OPM2 Mmi0Z5l1d3SxeHnjbZR6KGG|c3H5 NX72XmxoOjBizsznM41N NVu1em9jcW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> MW[xO|E3PDN|Mh?=
U266 NELKelhkgXSxdH;4bYNqfHliYYPzZZk> M4faOlIxKM7:Zz;tUC=> NGLT[5NqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs NEHBdHAyPzF4NEOzNi=>
MM.1S NIi1eINHfW6ldHnvckBie3OjeR?= NWLw[VhDe3WycILld5NmeyCYRVfGMWlv\HWlZXSgSY5ld3SqZXzpZYwhS2WubDDQdo9tcW[ncnH0bY9vKGGwZDDNbYdz[XSrb36u MWKxO|E3PDN|Mh?=
MM.1R MliwSpVv[3Srb36gZZN{[Xl? MU\zeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? MoqzNVcyPjR|M{K=
Dox40 MYrGeY5kfGmxbjDhd5NigQ>? MorCd5VxeHKnc4Pld{BXTUeILVnu[JVk\WRiRX7kc5Rp\WyrYXygR4VtdCCScn;sbYZmemG2aX;uJIFv\CCPaXfyZZRqd25w Ml\GNVcyPjR|M{K=
OPM2 M3fCPGZ2dmO2aX;uJIF{e2G7 Mmfrd5VxeHKnc4Pld{BXTUeILVnu[JVk\WRiRX7kc5Rp\WyrYXygR4VtdCCScn;sbYZmemG2aX;uJIFv\CCPaXfyZZRqd25w MoTHNVcyPjR|M{K=
HBMEC MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVy2fmIxhjFyIN88US=> Ml7xSG1UVw>? M1\NeGlEPTB;MTFOwG0> M{HyblIyODhzNkW2
HBMEC MV3GeY5kfGmxbjDhd5NigQ>? M1vQZp4yKM7:TR?= MVXEUXNQ M1L5SoFjem:pYYTld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIG\FS2ZTOiC5aYToJIRqe3K3cITpc44hd2ZiZH;3cpN1emWjbTDQUGPPuzF? MYiyNVA5OTZ3Nh?=
HBMEC MULGeY5kfGmxbjDhd5NigQ>? NGTpT3Z,OSEQvF2= MmDmSG1UVw>? NW\pd4hj\Gm|coXweJMhfGinIGLhd{1T[WZvRWLLJJBifGi5YYmgeIhzd3WpaDDk[YNz\WG|ZXSgdIhwe3Cqb4L5cIF1\WRiTVXLNU8zKGGwZDDFVmsyNzJ? MoLFNlExQDF4NU[=
HBMEC MlrUSpVv[3Srb36gZZN{[Xl? NX3tSmxthjJyIN88US=> NXftWZc{TE2VTx?= NInacJFlcXO{dYD0d{A2OCVib3[geJVj\SCob4LtZZRqd25iYYSgNUDPxE1? NH7JUoEzOTB6MU[1Oi=>
MDA-MB-231 MlzWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml\LglExKM7:TR?= M4rVNGROW09? NF7iR4tKSzVyPUWg{txO NUC2Soo2OjFyOEG2OVY>
MDA-MB-231 M{X3ZmZ2dmO2aX;uJIF{e2G7 M1XRZVAvPSEQvF2= M1ywe2ROW09? MXPpcohq[mm2czD0bIUhTVKNMT:yJJNq\26jbHnu[{Bx[XSqd3H5 M4PBbFIyODhzNkW2
MDA-MB-231 NUDoenRUTnWwY4Tpc44h[XO|YYm= NVHFdpJ6PSEQvF2= NH\IZpJFVVOR NHTBZ3RqdmS3Y3XzJIEh[2WubD3jfYNt\SCjcoLld5Q> NHvLemkzOTB6MU[1Oi=>
J82 NFnwOWhkgXSxdH;4bYNqfHliYYPzZZk> NHnWcWJ,OTBizszN MnHHSG1UVw>? M1\3e2lEPTB;MkSuOVch|ryP MmfDNlE2Ojl7MEC=
T24 NHz0ToRkgXSxdH;4bYNqfHliYYPzZZk> NWnZ[nBJhjFyIN88US=> MmjUSG1UVw>? MXPJR|UxRTV{LkS1JO69VQ>? M2D6R|IyPTJ7OUCw
HT1376 MV\jfZRwfG:6aXPpeJkh[XO|YYm= NVv5dWQ2hjFyIN88US=> MoDtSG1UVw>? MYDJR|UxRTJ6LkKxJO69VQ>? M1P3W|IyPTJ7OUCw
RT4 NIHSVI9kgXSxdH;4bYNqfHliYYPzZZk> M3nyd54yOCEQvF2= NVPue2o3TE2VTx?= MnTtTWM2OD13LkG0JO69VQ>? MVWyNVUzQTlyMB?=
CRL1749 MXzjfZRwfG:6aXPpeJkh[XO|YYm= Ml;NglExKM7:TR?= NX3NRXJyTE2VTx?= NHzrT5NKSzVyPUKyMlY6KM7:TR?= MUSyNVUzQTlyMB?=
HTB9 M2DsdYN6fG:2b4jpZ4l1gSCjc4PhfS=> M1vnNJ4yOCEQvF2= MnXFSG1UVw>? NXKxWYo4UUN3ME2xNU45PCEQvF2= MYmyNVUzQTlyMB?=
Sup NWnHbFMz[3m2b4TvfIlkcXS7IHHzd4F6 NGqzdId,OTBizszN MWXEUXNQ MmnvTWM2OD13Mz6zNkDPxE1? MVOyNVUzQTlyMB?=
HTB3 NFHVSFNkgXSxdH;4bYNqfHliYYPzZZk> NWTuWZB7hjFyIN88US=> MVnEUXNQ NUXrVVRlUUN3ME2xOE4yPiEQvF2= NV3MW|lkOjF3Mkm5NFA>
CEC NEO2cm9HfW6ldHnvckBie3OjeR?= M{XHXp4yOCEQvHevcWw> MnS5SG1UVw>? NV3jVHoy\G:5bj3y[Yd2dGG2ZYOgWmVITiCuZY\lcJM> Mn3DNlE3OjB6MkK=
RPE MYjGeY5kfGmxbjDhd5NigQ>? MWH+NVAh|rypL33M NV3RboZzTE2VTx?= NV3uSlBs\G:5bj3y[Yd2dGG2ZYOgWmVITiCuZY\lcJM> MmntNlE3OjB6MkK=
CEC NUe2fnB6TnWwY4Tpc44h[XO|YYm= MXX+OUDPxGdxbVy= MYHEUXNQ MY\icI9kc3NiZX7kc5Rp\WyrYXygZ4VtdCCvaXfyZZRqd25? NGH1NowzOTZ{MEiyNi=>
5637 M1\mfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVXEUXNQ M4C2SWlEPTB;MUWuNQKBkc7:TR?= NWOydXRTOjN6OEe2NFU>
J82 M1naU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUnEUXNQ MUjJR|UxRTF6LkVihKnPxE1? M1PhdlI{QDh5NkC1
5637 NXvvdY9iSXW2b4DoZYd6KGG|c3H5 MmDXNlAh|ryP MU\EUXNQ M17yOJRzcWepZYLzJJRp\SCjdYTvdIhi\2mlIIDyc4Nme3N? NWTqR|FIOjN6OEe2NFU>
J82 MYXBeZRweGijZ4mgZZN{[Xl? M4HtO|IxKM7:TR?= NH[3VIRFVVOR MYT0dolo\2W{czD0bIUh[XW2b4DoZYdq[yCycn;j[ZN{ MXKyN|g5PzZyNR?=
5637 NV\qUopOTnWwY4Tpc44h[XO|YYm= NWW2[Xc1OjBizszN MWnEUXNQ MmG4bY5lfWOnczDsfZNwe2:vYXyt[IVx\W6mZX70JI5m[3Kxc3nz NEDlUoYzOzh6N{[wOS=>
J82 NYPpbmlMTnWwY4Tpc44h[XO|YYm= NIDK[mkzOCEQvF2= NXPiS4lYTE2VTx?= MYHpcoR2[2W|IHz5d49{d22jbD3k[ZBmdmSnboSgcoVkem:|aYO= NH:xXWMzOzh6N{[wOS=>
5637 M4\MPGZ2dmO2aX;uJIF{e2G7 M4HHZVIxKM7:TR?= M{juXmROW09? MVfpcoR2[2W|IHz5d49{d22nIHHseIVz[XSrb36gZY5lKGmwaHnibZR{KEOEIHHjeIl3cXS7 MY[yN|g5PzZyNR?=
J82 MYPGeY5kfGmxbjDhd5NigQ>? MWGyNEDPxE1? NX3DdHY{TE2VTx?= NXHBclRmcW6mdXPld{BtgXOxc3;t[UBidHSncnH0bY9vKGGwZDDpcohq[mm2czDDRkBi[3Srdnn0fS=> M4nVNFI{QDh5NkC1
KATO-II NXzz[JJFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWHBboVGPSEQvF2= NFnHe|BFVVOR NF\BN|RjdG:la4OgdJJwdGmoZYLheIlwdg>? M3HyOlI2OjR7NUW3
OCUM-2M Ml[yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1fQUFUh|ryP M2nYTGROW09? MmXBZoxw[2u|IIDyc4xq\mW{YYTpc44> NYnXdZhOOjV{NEm1OVc>
SNU-16 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoTpOUDPxE1? NHrtdZFFVVOR MUficI9kc3NicILvcIln\XKjdHnvci=> Mm\WNlUzPDl3NUe=
HSC-39 NXPpXWF6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXe1JO69VQ>? NIq4RpBFVVOR MlPJZoxw[2u|IIDyc4xq\mW{YYTpc44> MmPpNlUzPDl3NUe=
KATO-II NHvSNIVkgXSxdH;4bYNqfHliYYPzZZk> NHG0Wm5,OTBizszN MkfaSG1UVw>? NFfx[pZKSzVyPUCuNUB1dyB{LkCg{txud2xxTB?= NGTQ[2UzPTJ2OUW1Oy=>
OCUM-2M Mn;DZ5l1d3SxeHnjbZR6KGG|c3H5 NVrtdlYyhjFyIN88US=> NFq1TnpFVVOR NGi5cFBKSzVyPUCuNUB1dyB{LkCg{txud2xxTB?= NWLsbIpUOjV{NEm1OVc>
SNU-16 MV7jfZRwfG:6aXPpeJkh[XO|YYm= MofyglExKM7:TR?= NH\XRYtFVVOR Mo\2TWM2OD1yLkGgeI8hOi5yIN88cY9tN0x? NFjZcWczPTJ2OUW1Oy=>
HSC-39 M3jWU4N6fG:2b4jpZ4l1gSCjc4PhfS=> MknqglExKM7:TR?= M{DM[2ROW09? M17DOGlEPTB;MD6xJJRwKDJwMDFOwI1wdC:O M{PSZ|I2OjR7NUW3
NIH 3T3 M1SxdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnrBglExKM7:TR?= NXjE[XczTE2VTx?= MlLNbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W6mIHPvcI9vgSCob4LtZZRqd25? MUeyOVI1QTV3Nx?=
KATO-III Mn:ySpVv[3Srb36gZZN{[Xl? NE[wZ2UyKM7:TR?= MUXEUXNQ NEOzO3BqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 NGXLWoMzPTJ2OUW1Oy=>
OCUM-2M MXXGeY5kfGmxbjDhd5NigQ>? MWGxJO69VQ>? NEG5VFNFVVOR NY\Bbm9lcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MojMNlUzPDl3NUe=
KATO-III NX7Hb25XSXCxcITvd4l{KGG|c3H5 MmHqNUDPxE1? M3rpWWROW09? Mn:wbY5lfWOnczDhdI9xfG:|aYO= M{\iZlI2OjR7NUW3
OCUM-2M NYTqRmN7SXCxcITvd4l{KGG|c3H5 NE\2[GkyKM7:TR?= NFi4c5JFVVOR NUHCW|FGcW6mdXPld{BieG:ydH;zbZM> MoXwNlUzPDl3NUe=
KATO-III MX\GeY5kfGmxbjDhd5NigQ>? M4m1T|Eh|ryP MlvOSG1UVw>? NVizT5JJcW6qaXLpeJMhTkeIUkKgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKHOrZ37hcIlv\yCvb3zlZ5Vt\XN? MV[yOVI1QTV3Nx?=

... 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]

+ Expand
  • 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]

+ Expand
  • 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