Pazopanib HCl (GW786034 HCl)

For research use only.

Catalog No.S1035

22 publications

Pazopanib HCl (GW786034 HCl) Chemical Structure

CAS No. 635702-64-6

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 22 publications

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 NVvrSGIyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml3TbY5pcWKrdIOgeIhmKF[HR1[tbY5lfWOnZDDwdo9tcW[ncnH0bY9vKG:oIFjVWmVEew>? NU\2fZlZOTh4MkCzPFI>
HUVEC MX\LbY5ie2ViYYPzZZk> NFPKPGZqdmirYnn0d{BXTUeILXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIG\FS2ZTNTJiaX6gTHVXTUNiY3XscJMhf2m2aDDhckBKSzVyIH;mJQKJxDhibl2= MlPiNVg3OjB|OEK=
MM NV:1dZpGU2mwYYPlJIF{e2G7 NWHFVI1xcW6qaXLpeJMhXkWJRj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDmcJQy MYmxO|E3PDN|Mh?=
MM.1S M4T5[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE[3cZkyOCEQvHevcWw> M2XsTYlvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq MnP0NVcyPjR|M{K=
MM.1R MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M37mclExKM7:Zz;tUC=> NHfufJJqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= MkLSNVcyPjR|M{K=
RPMI MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFvNU4YyOCEQvHevcWw> Mm\rbY5pcWKrdIOgUW0hS2WubDDHdo94fGh? MYSxO|E3PDN|Mh?=
Dox40 NF35T2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVqz[VdZOTBizsznM41N M1HMNIlvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq MVGxO|E3PDN|Mh?=
INA-6 MoPCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{XWWFExKM7:Zz;tUC=> MW\pcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? MVOxO|E3PDN|Mh?=
OPM2 NGnKSoJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIPlbZgyOCEQvHevcWw> NGXPNYVqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= MWGxO|E3PDN|Mh?=
U266 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV[xNEDPxGdxbVy= M{LpV4lvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq MXyxO|E3PDN|Mh?=
MM.1S MnS4Z5l1d3SxeHnjbZR6KGG|c3H5 NV7VVVc6OjBizsznM41N MknybY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= MYWxO|E3PDN|Mh?=
MM.1R MYTjfZRwfG:6aXPpeJkh[XO|YYm= NFS2enEzOCEQvHevcWw> MYjpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu MUKxO|E3PDN|Mh?=
RPMI NGTpSW5kgXSxdH;4bYNqfHliYYPzZZk> MmX0NlAh|rypL33M NWPYUFdtcW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> NILXdVcyPzF4NEOzNi=>
Dox40 NF\tfZVkgXSxdH;4bYNqfHliYYPzZZk> MVmyNEDPxGdxbVy= NGj6WZpqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs NVnKWpF[OTdzNkSzN|I>
INA-6 M3fIUIN6fG:2b4jpZ4l1gSCjc4PhfS=> NHzEV4EzOCEQvHevcWw> MlizbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= MVOxO|E3PDN|Mh?=
OPM2 MlTvZ5l1d3SxeHnjbZR6KGG|c3H5 MnXQNlAh|rypL33M M{\sW4lvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= M1fBW|E4OTZ2M{Oy
U266 MUnjfZRwfG:6aXPpeJkh[XO|YYm= M2\kSlIxKM7:Zz;tUC=> NVPOWWk1cW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> MlzONVcyPjR|M{K=
MM.1S MXLGeY5kfGmxbjDhd5NigQ>? NGHqbFd{fXCycnXzd4V{KF[HR1[tTY5lfWOnZDDFcoRwfGinbHnhcEBE\WyuIGDyc4xq\mW{YYTpc44h[W6mIF3p[5JifGmxbj6= MmHYNVcyPjR|M{K=
MM.1R NXHIc4NLTnWwY4Tpc44h[XO|YYm= Mlzzd5VxeHKnc4Pld{BXTUeILVnu[JVk\WRiRX7kc5Rp\WyrYXygR4VtdCCScn;sbYZmemG2aX;uJIFv\CCPaXfyZZRqd25w NV\NNZJpOTdzNkSzN|I>
Dox40 M3q4b2Z2dmO2aX;uJIF{e2G7 MWPzeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? MoruNVcyPjR|M{K=
OPM2 MlP5SpVv[3Srb36gZZN{[Xl? M{C3c5N2eHC{ZYPz[ZMhXkWJRj3JcoR2[2WmIFXu[I91cGWuaXHsJGNmdGxiUILvcIln\XKjdHnvckBidmRiTXnndoF1cW:wLh?= MXixO|E3PDN|Mh?=
HBMEC MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnHdWZ,OTBizszN Mn;DSG1UVw>? NIrjcWVKSzVyPUGg{txO NWHFbJBrOjFyOEG2OVY>
HBMEC NULGdVBkTnWwY4Tpc44h[XO|YYm= NVj5cG5{hjFizszN NYLL[|hzTE2VTx?= M{TNWoFjem:pYYTld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIG\FS2ZTOiC5aYToJIRqe3K3cITpc44hd2ZiZH;3cpN1emWjbTDQUGPPuzF? NV3ERXN3OjFyOEG2OVY>
HBMEC MWjGeY5kfGmxbjDhd5NigQ>? NUniZ|NXhjFizszN M1;hdGROW09? NG[ybZFlcXO{dYD0d{B1cGViUnHzMXJi\i2HUlugdIF1cHejeTD0bJJwfWeqIHTlZ5Jm[XOnZDDwbI9{eGixconsZZRm\CCPRVuxM|Ih[W6mIFXST|EwOg>? NW\rUWJUOjFyOEG2OVY>
HBMEC NYPicVk2TnWwY4Tpc44h[XO|YYm= NVLvcHlJhjJyIN88US=> M3HJ[mROW09? NWXHXZhN\Gm|coXweJMhPTBnIH;mJJR2[mViZn;ycYF1cW:wIHH0JFEh|ryP MUWyNVA5OTZ3Nh?=
MDA-MB-231 NHnsTohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXLPbXdWhjFyIN88US=> M4n6cGROW09? MUjJR|UxRTVizszN MnPoNlExQDF4NU[=
MDA-MB-231 Mmq5SpVv[3Srb36gZZN{[Xl? NV;CUG5qOC53IN88US=> NIf4OmhFVVOR MmjVbY5pcWKrdIOgeIhmKEWUS{GvNkB{cWewYXzpcocheGG2aIfhfS=> NHzrTm4zOTB6MU[1Oi=>
MDA-MB-231 MWDGeY5kfGmxbjDhd5NigQ>? M3K4SlUh|ryP MWHEUXNQ MlfkbY5lfWOnczDhJINmdGxvY4njcIUh[XK{ZYP0 MXWyNVA5OTZ3Nh?=
J82 NW\0OnpM[3m2b4TvfIlkcXS7IHHzd4F6 MXn+NVAh|ryP MlrGSG1UVw>? Mn\STWM2OD1{ND61O{DPxE1? NUP5fYF1OjF3Mkm5NFA>
T24 Mn64Z5l1d3SxeHnjbZR6KGG|c3H5 MmL3glExKM7:TR?= M1ztRWROW09? NEPvRWFKSzVyPUWyMlQ2KM7:TR?= M{OyS|IyPTJ7OUCw
HT1376 MWTjfZRwfG:6aXPpeJkh[XO|YYm= NUPtNXRChjFyIN88US=> NXjCS4tETE2VTx?= MXjJR|UxRTJ6LkKxJO69VQ>? MkDWNlE2Ojl7MEC=
RT4 NITpbVNkgXSxdH;4bYNqfHliYYPzZZk> M2rhV54yOCEQvF2= NYrOO2hWTE2VTx?= MkTxTWM2OD13LkG0JO69VQ>? M3zhWVIyPTJ7OUCw
CRL1749 MYDjfZRwfG:6aXPpeJkh[XO|YYm= MkfRglExKM7:TR?= MVLEUXNQ NV3DZ5MxUUN3ME2yNk43QSEQvF2= NEnwT4wzOTV{OUmwNC=>
HTB9 MnfaZ5l1d3SxeHnjbZR6KGG|c3H5 MVT+NVAh|ryP NGTCb5NFVVOR Ml7lTWM2OD1zMT64OEDPxE1? MYSyNVUzQTlyMB?=
Sup MULjfZRwfG:6aXPpeJkh[XO|YYm= MX3+NVAh|ryP NVPad5F{TE2VTx?= Mki0TWM2OD13Mz6zNkDPxE1? MY[yNVUzQTlyMB?=
HTB3 NXXXenl7[3m2b4TvfIlkcXS7IHHzd4F6 MX\+NVAh|ryP Mn:0SG1UVw>? MnXkTWM2OD1zND6xOkDPxE1? M4HlTlIyPTJ7OUCw
CEC NWCwPFlKTnWwY4Tpc44h[XO|YYm= NW\YfI1HhjFyIN88[{9uVA>? MUDEUXNQ MWrkc5dvNXKnZ4XsZZRmeyCYRVfGJIxmfmWucx?= MVyyNVYzODh{Mh?=
RPE NInmRYdHfW6ldHnvckBie3OjeR?= Ml7EglExKM7:Zz;tUC=> M3Hqc2ROW09? M3j4fYRwf25vcnXneYxifGW|IG\FS2YhdGW4ZXzz MoHONlE3OjB6MkK=
CEC NWf4TmFLTnWwY4Tpc44h[XO|YYm= MWn+OUDPxGdxbVy= NELTfmNFVVOR MkHoZoxw[2u|IHXu[I91cGWuaXHsJINmdGxibXnndoF1cW:w M1nObVIyPjJyOEKy
5637 M{KxTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXPEUXNQ NGXhN|lKSzVyPUG1MlDjiIoQvF2= MlH2NlM5QDd4MEW=
J82 NG\JXmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYDUcmdsTE2VTx?= MkX3TWM2OD1zOD605qCK|ryP NFjqNZAzOzh6N{[wOS=>
5637 NFrHUoxCfXSxcHjh[5kh[XO|YYm= M2HrflIxKM7:TR?= NGTtW2NFVVOR NUPqSmNDfHKrZ3fldpMhfGinIHH1eI9xcGGpaXOgdJJw[2W|cx?= Ml\oNlM5QDd4MEW=
J82 Mn35RZV1d3CqYXf5JIF{e2G7 MkS2NlAh|ryP NWfyUIhkTE2VTx?= MXH0dolo\2W{czD0bIUh[XW2b4DoZYdq[yCycn;j[ZN{ MWqyN|g5PzZyNR?=
5637 M2rNemZ2dmO2aX;uJIF{e2G7 MX[yNEDPxE1? NVj6UXlDTE2VTx?= NEXtU3ZqdmS3Y3XzJIx6e2:|b33hcE1l\XCnbnTlcpQhdmWlcn;zbZM> MmjjNlM5QDd4MEW=
J82 M4DENmZ2dmO2aX;uJIF{e2G7 NFLPWVQzOCEQvF2= NFvETGVFVVOR MYnpcoR2[2W|IHz5d49{d22jbD3k[ZBmdmSnboSgcoVkem:|aYO= MVeyN|g5PzZyNR?=
5637 MUHGeY5kfGmxbjDhd5NigQ>? NIDpdWgzOCEQvF2= M4ryO2ROW09? NXXQV|JKcW6mdXPld{BtgXOxc3;t[UBidHSncnH0bY9vKGGwZDDpcohq[mm2czDDRkBi[3Srdnn0fS=> M4\HU|I{QDh5NkC1
J82 NVP6Tog4TnWwY4Tpc44h[XO|YYm= M3;BT|IxKM7:TR?= NVu5U24xTE2VTx?= MoTDbY5lfWOnczDsfZNwe2:vZTDhcJRmemG2aX;uJIFv\CCrbnjpZol1eyCFQjDhZ5Rqfmm2eR?= MXuyN|g5PzZyNR?=
KATO-II NGO5Z3RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHfEc|U2KM7:TR?= NEjhOoNFVVOR M1jwWYJtd2OtczDwdo9tcW[ncnH0bY9v M{XydlI2OjR7NUW3
OCUM-2M NVLX[GZ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zvXVUh|ryP MVzEUXNQ NVrKNndw[myxY3vzJJBzd2yrZnXyZZRqd25? M{LnR|I2OjR7NUW3
SNU-16 Ml3NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mme1OUDPxE1? Ml\QSG1UVw>? NV7IXlQ{[myxY3vzJJBzd2yrZnXyZZRqd25? MXqyOVI1QTV3Nx?=
HSC-39 MlzNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUHSUoJwPSEQvF2= M{Lzd2ROW09? NYDxV3lH[myxY3vzJJBzd2yrZnXyZZRqd25? MnTyNlUzPDl3NUe=
KATO-II NU\3TlFV[3m2b4TvfIlkcXS7IHHzd4F6 NV\mOZh2hjFyIN88US=> MUXEUXNQ M{PyZmlEPTB;MD6xJJRwKDJwMDFOwI1wdC:O M4TwPVI2OjR7NUW3
OCUM-2M NWO3blNG[3m2b4TvfIlkcXS7IHHzd4F6 NV3xTXNRhjFyIN88US=> NHTTd5FFVVOR NXTGW3ltUUN3ME2wMlEhfG9iMj6wJO69dW:uL1y= M4SyfVI2OjR7NUW3
SNU-16 MorBZ5l1d3SxeHnjbZR6KGG|c3H5 MnvmglExKM7:TR?= NI\iOHhFVVOR M3WyW2lEPTB;MD6xJJRwKDJwMDFOwI1wdC:O MorlNlUzPDl3NUe=
HSC-39 NEK3NHZkgXSxdH;4bYNqfHliYYPzZZk> NFqyeWh,OTBizszN MmS0SG1UVw>? MXrJR|UxRTBwMTD0c{AzNjBizsztc4wwVA>? MlHHNlUzPDl3NUe=
NIH 3T3 M3vHPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MofWglExKM7:TR?= MmX4SG1UVw>? MXzpcohq[mm2czDj[YxtKGe{b4f0bEBidmRiY3;sc456KG[xcn3heIlwdg>? M1[ycFI2OjR7NUW3
KATO-III NIm1SXRHfW6ldHnvckBie3OjeR?= MkPVNUDPxE1? MkXnSG1UVw>? NHnSNndqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MlzUNlUzPDl3NUe=
OCUM-2M M3HrVWZ2dmO2aX;uJIF{e2G7 NUi0WoV2OSEQvF2= M1fXcGROW09? MkDIbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= M3fROlI2OjR7NUW3
KATO-III MV\BdI9xfG:|aYOgZZN{[Xl? NEjOW|IyKM7:TR?= NVi0cJk6TE2VTx?= M13HXYlv\HWlZYOgZZBweHSxc3nz MmG4NlUzPDl3NUe=
OCUM-2M M4\zemFxd3C2b4Ppd{Bie3OjeR?= M3j6PVEh|ryP MULEUXNQ MlzybY5lfWOnczDhdI9xfG:|aYO= NF3XWpozPTJ2OUW1Oy=>
KATO-III NEjkS4ZHfW6ldHnvckBie3OjeR?= MoDnNUDPxE1? M{\VfWROW09? M1;heolvcGmkaYTzJGZITlJ{IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUB{cWewYXzpcochdW:uZXP1cIV{ MlvKNlUzPDl3NUe=

... 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 CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl

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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

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