Pazopanib HCl (GW786034 HCl)

For research use only.

Catalog No.S1035

33 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 33 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 NUH5SYFOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF2yfmJqdmirYnn0d{B1cGViVlXHSk1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gTHVXTUO| NVvWTXVvOTh4MkCzPFI>
HUVEC M4TFT2tqdmG|ZTDhd5NigQ>? M{myb4lvcGmkaYTzJHZGT0ZvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiVlXHSnIuOiCrbjDIWXZGSyClZXzsd{B4cXSqIHHuJGlEPTBib3[g5qi9QCCwTR?= MWCxPFYzODN6Mh?=
MM NV:wNo42U2mwYYPlJIF{e2G7 MUPpcohq[mm2czDWSWdHNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKG[udEG= M1n6UlE4OTZ2M{Oy
MM.1S NHSxflFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGf2bGUyOCEQvHevcWw> MX;pcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? Mn\2NVcyPjR|M{K=
MM.1R NHz6[WNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2i1OVExKM7:Zz;tUC=> NWPoUmo4cW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= M3Hr[FE4OTZ2M{Oy
RPMI MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlL2NVAh|rypL33M MYLpcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? NEjKPGkyPzF4NEOzNi=>
Dox40 MmLoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NE\qZ|QyOCEQvHevcWw> NVficINncW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= MXmxO|E3PDN|Mh?=
INA-6 NXjiNVg5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoC5NVAh|rypL33M NY\H[2FRcW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= Mor4NVcyPjR|M{K=
OPM2 M3TI[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHnlflAyOCEQvHevcWw> NUDxTpF[cW6qaXLpeJMhVU1iQ3XscEBIem:5dHi= MnT6NVcyPjR|M{K=
U266 NVfIbJp[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MknpNVAh|rypL33M MlvMbY5pcWKrdIOgUW0hS2WubDDHdo94fGh? NXnyb3ZOOTdzNkSzN|I>
MM.1S NEDBfo5kgXSxdH;4bYNqfHliYYPzZZk> MkHTNlAh|rypL33M NXnvUXE5cW6qaXLpeJMhVU1iQ3XscEBUfXK4aY\hcC=> M1:4[VE4OTZ2M{Oy
MM.1R MYrjfZRwfG:6aXPpeJkh[XO|YYm= M1TKT|IxKM7:Zz;tUC=> Ml3zbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= MWOxO|E3PDN|Mh?=
RPMI NHHWZoZkgXSxdH;4bYNqfHliYYPzZZk> MmfNNlAh|rypL33M MWjpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu Ml7wNVcyPjR|M{K=
Dox40 NFTFR21kgXSxdH;4bYNqfHliYYPzZZk> NXvQT3pzOjBizsznM41N MUPpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu NEP3fJQyPzF4NEOzNi=>
INA-6 M{HxcYN6fG:2b4jpZ4l1gSCjc4PhfS=> MXeyNEDPxGdxbVy= MoKzbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= Mmr3NVcyPjR|M{K=
OPM2 M3rZeIN6fG:2b4jpZ4l1gSCjc4PhfS=> MUOyNEDPxGdxbVy= M{njRolvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= NXXjUHBwOTdzNkSzN|I>
U266 NEHoTo1kgXSxdH;4bYNqfHliYYPzZZk> NX7uSYJ5OjBizsznM41N NIe4WopqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs MnjiNVcyPjR|M{K=
MM.1S NGjDV2VHfW6ldHnvckBie3OjeR?= NXTs[IlSe3WycILld5NmeyCYRVfGMWlv\HWlZXSgSY5ld3SqZXzpZYwhS2WubDDQdo9tcW[ncnH0bY9vKGGwZDDNbYdz[XSrb36u M4jyXFE4OTZ2M{Oy
MM.1R MoX4SpVv[3Srb36gZZN{[Xl? M1XuOZN2eHC{ZYPz[ZMhXkWJRj3JcoR2[2WmIFXu[I91cGWuaXHsJGNmdGxiUILvcIln\XKjdHnvckBidmRiTXnndoF1cW:wLh?= NGS3VIgyPzF4NEOzNi=>
Dox40 MX7GeY5kfGmxbjDhd5NigQ>? NGfkWll{fXCycnXzd4V{KF[HR1[tTY5lfWOnZDDFcoRwfGinbHnhcEBE\WyuIGDyc4xq\mW{YYTpc44h[W6mIF3p[5JifGmxbj6= MVqxO|E3PDN|Mh?=
OPM2 NXnUdGFMTnWwY4Tpc44h[XO|YYm= NVTqbGFbe3WycILld5NmeyCYRVfGMWlv\HWlZXSgSY5ld3SqZXzpZYwhS2WubDDQdo9tcW[ncnH0bY9vKGGwZDDNbYdz[XSrb36u MW[xO|E3PDN|Mh?=
HBMEC MoDaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnHJglExKM7:TR?= NWLUcZc1TE2VTx?= NVG1W2Z3UUN3ME2xJO69VQ>? NVLDS4E{OjFyOEG2OVY>
HBMEC MmmySpVv[3Srb36gZZN{[Xl? NELh[Gx,OSEQvF2= NGfoVItFVVOR M{HEZoFjem:pYYTld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIG\FS2ZTOiC5aYToJIRqe3K3cITpc44hd2ZiZH;3cpN1emWjbTDQUGPPuzF? M{XMc|IyODhzNkW2
HBMEC M2LOR2Z2dmO2aX;uJIF{e2G7 NWXkZpU6hjFizszN NHX2ZXpFVVOR MXTkbZNzfXC2czD0bIUhWmG|LWLh[k1GWkticHH0bJdigSC2aILveYdpKGSnY4LlZZNm\CCyaH;zdIhwenmuYYTl[EBOTUtzL{KgZY5lKEWUS{GvNi=> NWq5cFFbOjFyOEG2OVY>
HBMEC MWjGeY5kfGmxbjDhd5NigQ>? MkHYglIxKM7:TR?= NISzTW5FVVOR MlPi[Il{enWydIOgOVAmKG:oIIT1ZoUh\m:{bXH0bY9vKGG2IEGg{txO MVOyNVA5OTZ3Nh?=
MDA-MB-231 NIHCRZdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlXpglExKM7:TR?= NF;4OYJFVVOR MkHwTWM2OD13IN88US=> NWXuRVZsOjFyOEG2OVY>
MDA-MB-231 NWnaR3BxTnWwY4Tpc44h[XO|YYm= NV7TSVNLOC53IN88US=> MlXkSG1UVw>? Mof2bY5pcWKrdIOgeIhmKEWUS{GvNkB{cWewYXzpcocheGG2aIfhfS=> NGDjSZczOTB6MU[1Oi=>
MDA-MB-231 M4D0WmZ2dmO2aX;uJIF{e2G7 NFn3U5k2KM7:TR?= NX3nNYV2TE2VTx?= M2\sUYlv\HWlZYOgZUBk\WyuLXP5Z4xmKGG{cnXzeC=> NX\uOG5bOjFyOEG2OVY>
J82 NFfmbnlkgXSxdH;4bYNqfHliYYPzZZk> M2nQXJ4yOCEQvF2= MYTEUXNQ NV7CRXdqUUN3ME2yOE42PyEQvF2= M{LsfFIyPTJ7OUCw
T24 NEK0XmtkgXSxdH;4bYNqfHliYYPzZZk> NXrXOY1ZhjFyIN88US=> MkXpSG1UVw>? M1PlOmlEPTB;NUKuOFUh|ryP MXmyNVUzQTlyMB?=
HT1376 NWLaeGNj[3m2b4TvfIlkcXS7IHHzd4F6 Mnj3glExKM7:TR?= NH[xRotFVVOR MXzJR|UxRTJ6LkKxJO69VQ>? MknrNlE2Ojl7MEC=
RT4 M3LrZoN6fG:2b4jpZ4l1gSCjc4PhfS=> MkD6glExKM7:TR?= M{\3NmROW09? NHTsV4ZKSzVyPUWuNVQh|ryP NISyU4ozOTV{OUmwNC=>
CRL1749 MoPOZ5l1d3SxeHnjbZR6KGG|c3H5 NHTLU5V,OTBizszN M{nIVGROW09? MXvJR|UxRTJ{Lk[5JO69VQ>? NG\0O2ozOTV{OUmwNC=>
HTB9 MU\jfZRwfG:6aXPpeJkh[XO|YYm= NGj1[nl,OTBizszN NEnPdllFVVOR NELJ[W9KSzVyPUGxMlg1KM7:TR?= NVvVeolIOjF3Mkm5NFA>
Sup MYjjfZRwfG:6aXPpeJkh[XO|YYm= NGfORmt,OTBizszN NVj0U21sTE2VTx?= NVXNXZl6UUN3ME21N{4{OiEQvF2= NUXRbGhoOjF3Mkm5NFA>
HTB3 MYrjfZRwfG:6aXPpeJkh[XO|YYm= MoL4glExKM7:TR?= NWe0NohETE2VTx?= MYTJR|UxRTF2LkG2JO69VQ>? MUCyNVUzQTlyMB?=
CEC NF7HSFBHfW6ldHnvckBie3OjeR?= NFizflR,OTBizsznM41N NX3iRlVxTE2VTx?= M{DHWoRwf25vcnXneYxifGW|IG\FS2YhdGW4ZXzz M4KwfFIyPjJyOEKy
RPE NFHaUHhHfW6ldHnvckBie3OjeR?= NHLH[WF,OTBizsznM41N NV:2Noc1TE2VTx?= MmTP[I94di2{ZXf1cIF1\XNiVlXHSkBt\X[nbIO= NHjueHAzOTZ{MEiyNi=>
CEC MWTGeY5kfGmxbjDhd5NigQ>? MYX+OUDPxGdxbVy= MVfEUXNQ NWW4eFNG[myxY3vzJIVv\G:2aHXsbYFtKGOnbHygcYloemG2aX;u MWWyNVYzODh{Mh?=
5637 M2TyV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoLySG1UVw>? MUnJR|UxRTF3LkFihKnPxE1? NHzKfY4zOzh6N{[wOS=>
J82 NV7XOZptT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVrEUXNQ NV75Oo4zUUN3ME2xPE416oDLzszN NEiye2YzOzh6N{[wOS=>
5637 M1G0dmF2fG:yaHHnfUBie3OjeR?= NXzB[mRyOjBizszN MoX2SG1UVw>? MVT0dolo\2W{czD0bIUh[XW2b4DoZYdq[yCycn;j[ZN{ M2WyVlI{QDh5NkC1
J82 NHH5VZRCfXSxcHjh[5kh[XO|YYm= MkfYNlAh|ryP MWHEUXNQ M3uwTZRzcWepZYLzJJRp\SCjdYTvdIhi\2mlIIDyc4Nme3N? MXuyN|g5PzZyNR?=
5637 NXPoPWQ6TnWwY4Tpc44h[XO|YYm= MmPUNlAh|ryP MUjEUXNQ M2HMXIlv\HWlZYOgcJl{d3OxbXHsMYRmeGWwZHXueEBv\WO{b4Ppdy=> NVPVZ|JXOjN6OEe2NFU>
J82 NUPub5c4TnWwY4Tpc44h[XO|YYm= M3nGT|IxKM7:TR?= M3f5bWROW09? MUDpcoR2[2W|IHz5d49{d22jbD3k[ZBmdmSnboSgcoVkem:|aYO= MnjNNlM5QDd4MEW=
5637 NHm4RYtHfW6ldHnvckBie3OjeR?= MUCyNEDPxE1? M13tUGROW09? MoTHbY5lfWOnczDsfZNwe2:vZTDhcJRmemG2aX;uJIFv\CCrbnjpZol1eyCFQjDhZ5Rqfmm2eR?= M1XPU|I{QDh5NkC1
J82 M3rDTGZ2dmO2aX;uJIF{e2G7 M1raPFIxKM7:TR?= MY\EUXNQ Ml:3bY5lfWOnczDsfZNwe2:vZTDhcJRmemG2aX;uJIFv\CCrbnjpZol1eyCFQjDhZ5Rqfmm2eR?= M3PoeVI{QDh5NkC1
KATO-II MlOwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEnuWoQ2KM7:TR?= MmnySG1UVw>? NFzuXYdjdG:la4OgdJJwdGmoZYLheIlwdg>? MUGyOVI1QTV3Nx?=
OCUM-2M MoqyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVW1JO69VQ>? M2DlSGROW09? NXO4boZD[myxY3vzJJBzd2yrZnXyZZRqd25? MVOyOVI1QTV3Nx?=
SNU-16 MlP6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYi1JO69VQ>? MVPEUXNQ NWDBWJBL[myxY3vzJJBzd2yrZnXyZZRqd25? M3jXfVI2OjR7NUW3
HSC-39 NHWz[5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NULHOmpqPSEQvF2= NHj1[YFFVVOR MYXicI9kc3NicILvcIln\XKjdHnvci=> MnriNlUzPDl3NUe=
KATO-II MY\jfZRwfG:6aXPpeJkh[XO|YYm= MmnpglExKM7:TR?= NWjPOHlETE2VTx?= NGf1PI5KSzVyPUCuNUB1dyB{LkCg{txud2xxTB?= NWC2V|BUOjV{NEm1OVc>
OCUM-2M M{Hv[IN6fG:2b4jpZ4l1gSCjc4PhfS=> NGPYUnd,OTBizszN MYHEUXNQ M{TiR2lEPTB;MD6xJJRwKDJwMDFOwI1wdC:O MoW3NlUzPDl3NUe=
SNU-16 MnntZ5l1d3SxeHnjbZR6KGG|c3H5 NGHnXGh,OTBizszN NYDnO5NZTE2VTx?= M2LDN2lEPTB;MD6xJJRwKDJwMDFOwI1wdC:O NHjVdlEzPTJ2OUW1Oy=>
HSC-39 MXnjfZRwfG:6aXPpeJkh[XO|YYm= MnizglExKM7:TR?= MojFSG1UVw>? NF;PTotKSzVyPUCuNUB1dyB{LkCg{txud2xxTB?= NITkb2YzPTJ2OUW1Oy=>
NIH 3T3 NGHQTWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFXRNIl,OTBizszN NVq3fWs{TE2VTx?= MmPPbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W6mIHPvcI9vgSCob4LtZZRqd25? NH[2c2UzPTJ2OUW1Oy=>
KATO-III NFrYVHVHfW6ldHnvckBie3OjeR?= NFzkOlIyKM7:TR?= MkixSG1UVw>? MnTxbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= NYHsb29oOjV{NEm1OVc>
OCUM-2M MYfGeY5kfGmxbjDhd5NigQ>? MonmNUDPxE1? NFvJWmhFVVOR M{Lp[Ilv\HWlZYOgZ4VtdC2leXPs[UBienKnc4S= MkXpNlUzPDl3NUe=
KATO-III MVfBdI9xfG:|aYOgZZN{[Xl? M3\jbFEh|ryP M3vCZmROW09? MVHpcoR2[2W|IHHwc5B1d3Orcx?= MVmyOVI1QTV3Nx?=
OCUM-2M MnH6RZBweHSxc3nzJIF{e2G7 NXewR4x4OSEQvF2= Mn3qSG1UVw>? NFG5ZZpqdmS3Y3XzJIFxd3C2b4Ppdy=> MVmyOVI1QTV3Nx?=
KATO-III NXXTd|FCTnWwY4Tpc44h[XO|YYm= M3nsRVEh|ryP M1\CemROW09? NHyxS5RqdmirYnn0d{BHT0[UMjDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0he2mpbnHsbY5oKG2xbHXjeYxmew>? M3nOSVI2OjR7NUW3

... 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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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
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

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