Pazopanib HCl (GW786034 HCl)

For research use only. Not for use in humans.

目录号:S1035 中文名称:盐酸帕佐帕尼

Pazopanib HCl (GW786034 HCl) Chemical Structure

CAS No. 635702-64-6

Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1565.32 现货
RMB 1225.19 现货
RMB 2231.51 现货
RMB 3031.75 现货
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客户使用Selleck生产的Pazopanib HCl (GW786034 HCl)发表文献33篇:

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。
特性 Pazopanib是一个多激酶的抑制剂。
靶点
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
体外研究

在HUVEC细胞中,Pazopanib显著抑制VEGF诱导的VEGFR-2的磷酸化,IC50 为8nM [1]。 在所有滑膜肉瘤细胞系中Pazopanib都表现出了生长抑制作用,包括SYO-1和HS-SY-II细胞,这种抑制具有剂量依赖的特性。1µg/mL Pazopanib就可以抑制SYO-1和HS-SY-II细胞增殖,而5µg/mL Pazopanib可以让它们的增殖彻底受阻。 Pazopanib 会诱导滑膜肉瘤细胞周期停留在 G1期从而抑制它的生长。与对照的细胞相比,经过Pazopanib处理过的 SYO-1细胞中的AKTs, GSK-3β, JNKs, p70 S6激酶以及mTOR的磷酸化都受到了抑制[2]。在20 mg/mL 到 22.5 mg/mL的浓度之间,Pazopanib 使RPE细胞的生存能力逐渐下降[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGfHfpZqdmirYnn0d{B1cGViVlXHSk1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gTHVXTUO| MnrqNVg3OjB|OEK=
HUVEC NFvPdm5McW6jc3WgZZN{[Xl? NEW5VpNqdmirYnn0d{BXTUeILXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIG\FS2ZTNTJiaX6gTHVXTUNiY3XscJMhf2m2aDDhckBKSzVyIH;mJQKJxDhibl2= NWS3TXk5OTh4MkCzPFI>
MM M4HhOWtqdmG|ZTDhd5NigQ>? MkHObY5pcWKrdIOgWmVITi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCobISx MlTENVcyPjR|M{K=
MM.1S NIO0dmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVzIXFF[OTBizsznM41N MWrpcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? M1u3elE4OTZ2M{Oy
MM.1R M3LPbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXmxNEDPxGdxbVy= MX;pcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? M1i1VlE4OTZ2M{Oy
RPMI NIPEcVlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3\MNlExKM7:Zz;tUC=> MXvpcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? NWTjTWlLOTdzNkSzN|I>
Dox40 M3iybWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHzmVJUyOCEQvHevcWw> MnnCbY5pcWKrdIOgUW0hS2WubDDHdo94fGh? MojENVcyPjR|M{K=
INA-6 NGm4e5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX2xNEDPxGdxbVy= NFnRcJlqdmirYnn0d{BOVSCFZXzsJGdzd3e2aB?= MV:xO|E3PDN|Mh?=
OPM2 MlfGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWrZdmh4OTBizsznM41N MYDpcohq[mm2czDNUUBE\WyuIFfyc5d1cA>? NHLQfXgyPzF4NEOzNi=>
U266 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIfW[48yOCEQvHevcWw> M{DsXolvcGmkaYTzJG1OKEOnbHygS5Jwf3Sq NWDJRmE4OTdzNkSzN|I>
MM.1S NHi3[JNkgXSxdH;4bYNqfHliYYPzZZk> M{fmUlIxKM7:Zz;tUC=> NHLlbZhqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs MU[xO|E3PDN|Mh?=
MM.1R NUDDWnhQ[3m2b4TvfIlkcXS7IHHzd4F6 MXWyNEDPxGdxbVy= MnTpbY5pcWKrdIOgUW0hS2WubDDTeZJ3cX[jbB?= NF;UbWIyPzF4NEOzNi=>
RPMI MVPjfZRwfG:6aXPpeJkh[XO|YYm= MmLxNlAh|rypL33M M1jqb4lvcGmkaYTzJG1OKEOnbHygV5Vzfmm4YXy= NFvneYEyPzF4NEOzNi=>
Dox40 M{LRVYN6fG:2b4jpZ4l1gSCjc4PhfS=> MX:yNEDPxGdxbVy= MXXpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu MojvNVcyPjR|M{K=
INA-6 NEH5Z4pkgXSxdH;4bYNqfHliYYPzZZk> NFfxW|EzOCEQvHevcWw> NGHMOZhqdmirYnn0d{BOVSCFZXzsJHN2en[rdnHs NFTobocyPzF4NEOzNi=>
OPM2 NEnjVVdkgXSxdH;4bYNqfHliYYPzZZk> NH\UR3UzOCEQvHevcWw> MV7pcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu MoX6NVcyPjR|M{K=
U266 MlnZZ5l1d3SxeHnjbZR6KGG|c3H5 MXiyNEDPxGdxbVy= MVPpcohq[mm2czDNUUBE\WyuIGP1dpZqfmGu MXOxO|E3PDN|Mh?=
MM.1S M3rqeWZ2dmO2aX;uJIF{e2G7 MVPzeZBxemW|c3XzJHZGT0ZvSX7keYNm\CCHbnTveIhmdGmjbDDD[YxtKFC{b3zp[oVz[XSrb36gZY5lKE2rZ4LheIlwdi5? NV7iUJBpOTdzNkSzN|I>
MM.1R NV;YeGNYTnWwY4Tpc44h[XO|YYm= M{\C[5N2eHC{ZYPz[ZMhXkWJRj3JcoR2[2WmIFXu[I91cGWuaXHsJGNmdGxiUILvcIln\XKjdHnvckBidmRiTXnndoF1cW:wLh?= MV:xO|E3PDN|Mh?=
Dox40 NF3nRnBHfW6ldHnvckBie3OjeR?= M2T2OZN2eHC{ZYPz[ZMhXkWJRj3JcoR2[2WmIFXu[I91cGWuaXHsJGNmdGxiUILvcIln\XKjdHnvckBidmRiTXnndoF1cW:wLh?= NUPFcoNxOTdzNkSzN|I>
OPM2 M3niTGZ2dmO2aX;uJIF{e2G7 MoHjd5VxeHKnc4Pld{BXTUeILVnu[JVk\WRiRX7kc5Rp\WyrYXygR4VtdCCScn;sbYZmemG2aX;uJIFv\CCPaXfyZZRqd25w MojqNVcyPjR|M{K=
HBMEC M{fGWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4r5NJ4yOCEQvF2= Mki1SG1UVw>? MXrJR|UxRTFizszN MXuyNVA5OTZ3Nh?=
HBMEC MXLGeY5kfGmxbjDhd5NigQ>? NWm0N4trhjFizszN NWDqc4ZOTE2VTx?= NX3sOGtz[WK{b3fheIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gWmVITlJ{IIfpeIgh\Gm|coXweIlwdiCxZjDkc5dve3S{ZXHtJHBNS87|MR?= NFu3W5czOTB6MU[1Oi=>
HBMEC NGrDV|NHfW6ldHnvckBie3OjeR?= NWHuNXc2hjFizszN MWDEUXNQ NVzT[lFv\Gm|coXweJMhfGinIGLhd{1T[WZvRWLLJJBifGi5YYmgeIhzd3WpaDDk[YNz\WG|ZXSgdIhwe3Cqb4L5cIF1\WRiTVXLNU8zKGGwZDDFVmsyNzJ? NWGzRotqOjFyOEG2OVY>
HBMEC M{CyNmZ2dmO2aX;uJIF{e2G7 MkfqglIxKM7:TR?= M3LkTmROW09? MlnY[Il{enWydIOgOVAmKG:oIIT1ZoUh\m:{bXH0bY9vKGG2IEGg{txO NHvUNHQzOTB6MU[1Oi=>
MDA-MB-231 M{TI[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUL+NVAh|ryP NYrpNmhoTE2VTx?= MVzJR|UxRTVizszN M4XCRVIyODhzNkW2
MDA-MB-231 NFHmeWdHfW6ldHnvckBie3OjeR?= NFjhVmYxNjVizszN MYfEUXNQ NYGwVohkcW6qaXLpeJMhfGinIFXST|EwOiC|aXfuZYxqdmdicHH0bJdigQ>? MX6yNVA5OTZ3Nh?=
MDA-MB-231 M3rremZ2dmO2aX;uJIF{e2G7 MoC2OUDPxE1? NEG1[3dFVVOR NVnlXoVscW6mdXPld{BiKGOnbHytZ5lkdGViYYLy[ZN1 MYCyNVA5OTZ3Nh?=
J82 MWjjfZRwfG:6aXPpeJkh[XO|YYm= NEn6dXp,OTBizszN M3nXfWROW09? NFvzRWFKSzVyPUK0MlU4KM7:TR?= NEfEW28zOTV{OUmwNC=>
T24 NYXXenZt[3m2b4TvfIlkcXS7IHHzd4F6 NWnscWE4hjFyIN88US=> Mlz3SG1UVw>? Ml\GTWM2OD13Mj60OUDPxE1? MVmyNVUzQTlyMB?=
HT1376 MnXGZ5l1d3SxeHnjbZR6KGG|c3H5 M3rsVZ4yOCEQvF2= MVLEUXNQ NGXBZWFKSzVyPUK4MlIyKM7:TR?= NYnPXFlmOjF3Mkm5NFA>
RT4 M3zCWoN6fG:2b4jpZ4l1gSCjc4PhfS=> MXj+NVAh|ryP MlvkSG1UVw>? NEHaXFhKSzVyPUWuNVQh|ryP NUn0ZXNrOjF3Mkm5NFA>
CRL1749 MV;jfZRwfG:6aXPpeJkh[XO|YYm= MoTTglExKM7:TR?= NVzEWYZyTE2VTx?= MUXJR|UxRTJ{Lk[5JO69VQ>? NIi1N5QzOTV{OUmwNC=>
HTB9 MlfIZ5l1d3SxeHnjbZR6KGG|c3H5 MYT+NVAh|ryP NVWxUZJpTE2VTx?= M3fMUWlEPTB;MUGuPFQh|ryP MUKyNVUzQTlyMB?=
Sup NUTHU5JV[3m2b4TvfIlkcXS7IHHzd4F6 Mn62glExKM7:TR?= NH;yTIhFVVOR MkLXTWM2OD13Mz6zNkDPxE1? MUSyNVUzQTlyMB?=
HTB3 NXi2WVE5[3m2b4TvfIlkcXS7IHHzd4F6 NE\4b|F,OTBizszN M1n1U2ROW09? M4DqbmlEPTB;MUSuNVYh|ryP MortNlE2Ojl7MEC=
CEC NGXDOZJHfW6ldHnvckBie3OjeR?= M{fRUJ4yOCEQvHevcWw> MXzEUXNQ MXfkc5dvNXKnZ4XsZZRmeyCYRVfGJIxmfmWucx?= NUnPO|E3OjF4MkC4NlI>
RPE MY\GeY5kfGmxbjDhd5NigQ>? Mk\HglExKM7:Zz;tUC=> MYfEUXNQ MmXo[I94di2{ZXf1cIF1\XNiVlXHSkBt\X[nbIO= MkfMNlE3OjB6MkK=
CEC MlrDSpVv[3Srb36gZZN{[Xl? M2LaZZ42KM7:Zz;tUC=> M4jae2ROW09? M17VXIJtd2OtczDlcoRwfGinbHnhcEBk\WyuIH3p[5JifGmxbh?= MlO1NlE3OjB6MkK=
5637 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWPmcItFTE2VTx?= M{f2WWlEPTB;MUWuNQKBkc7:TR?= M1S5[FI{QDh5NkC1
J82 NWKxb215T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{i1SWROW09? NI\GT2pKSzVyPUG4MlTjiIoQvF2= NH3FTYwzOzh6N{[wOS=>
5637 NX\0XlF6SXW2b4DoZYd6KGG|c3H5 Mn3kNlAh|ryP M3zHd2ROW09? MkfveJJq\2encoOgeIhmKGG3dH;wbIFocWNicILvZ4V{ew>? MlvoNlM5QDd4MEW=
J82 NFe5XFFCfXSxcHjh[5kh[XO|YYm= MYOyNEDPxE1? NVfCVHZoTE2VTx?= MoX1eJJq\2encoOgeIhmKGG3dH;wbIFocWNicILvZ4V{ew>? M2Dpb|I{QDh5NkC1
5637 NW\BSVBSTnWwY4Tpc44h[XO|YYm= M{fWTlIxKM7:TR?= M1XoPWROW09? Mn\qbY5lfWOnczDsfZNwe2:vYXyt[IVx\W6mZX70JI5m[3Kxc3nz MmTrNlM5QDd4MEW=
J82 NYXQU2pbTnWwY4Tpc44h[XO|YYm= M2nDOVIxKM7:TR?= NVn4WVJUTE2VTx?= M{HsR4lv\HWlZYOgcJl{d3OxbXHsMYRmeGWwZHXueEBv\WO{b4Ppdy=> Ml7JNlM5QDd4MEW=
5637 MYfGeY5kfGmxbjDhd5NigQ>? Mlz4NlAh|ryP MWLEUXNQ MmDlbY5lfWOnczDsfZNwe2:vZTDhcJRmemG2aX;uJIFv\CCrbnjpZol1eyCFQjDhZ5Rqfmm2eR?= Mn;SNlM5QDd4MEW=
J82 MWjGeY5kfGmxbjDhd5NigQ>? MUeyNEDPxE1? NFPGdnlFVVOR NYmwWZU4cW6mdXPld{BtgXOxc3;t[UBidHSncnH0bY9vKGGwZDDpcohq[mm2czDDRkBi[3Srdnn0fS=> MUiyN|g5PzZyNR?=
KATO-II NFPPS|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXe4doZTPSEQvF2= NILtO5dFVVOR NIX3fmVjdG:la4OgdJJwdGmoZYLheIlwdg>? NYHV[G1{OjV{NEm1OVc>
OCUM-2M NYDlZld5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXHxNmFSPSEQvF2= NIruXpBFVVOR M{DTN4Jtd2OtczDwdo9tcW[ncnH0bY9v M1XsTlI2OjR7NUW3
SNU-16 M2[4bWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWDNbI52PSEQvF2= MV3EUXNQ MVPicI9kc3NicILvcIln\XKjdHnvci=> NVjnWlRzOjV{NEm1OVc>
HSC-39 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDhcpU2KM7:TR?= NUTaZ4E5TE2VTx?= M4j2OoJtd2OtczDwdo9tcW[ncnH0bY9v MViyOVI1QTV3Nx?=
KATO-II MUXjfZRwfG:6aXPpeJkh[XO|YYm= M1TvR54yOCEQvF2= NHrGUlZFVVOR NV2xPGZDUUN3ME2wMlEhfG9iMj6wJO69dW:uL1y= MWiyOVI1QTV3Nx?=
OCUM-2M MmLlZ5l1d3SxeHnjbZR6KGG|c3H5 NXLXTJNxhjFyIN88US=> NYX2bolTTE2VTx?= MXvJR|UxRTBwMTD0c{AzNjBizsztc4wwVA>? MoPqNlUzPDl3NUe=
SNU-16 MoPWZ5l1d3SxeHnjbZR6KGG|c3H5 MnXZglExKM7:TR?= NY\U[IJ2TE2VTx?= NV3Fc482UUN3ME2wMlEhfG9iMj6wJO69dW:uL1y= NEDjS4EzPTJ2OUW1Oy=>
HSC-39 NVTDcIhr[3m2b4TvfIlkcXS7IHHzd4F6 MWH+NVAh|ryP MojZSG1UVw>? MXfJR|UxRTBwMTD0c{AzNjBizsztc4wwVA>? MUCyOVI1QTV3Nx?=
NIH 3T3 M37a[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\tU2x,OTBizszN MUfEUXNQ NITVN|lqdmirYnn0d{Bk\WyuIHfyc5d1cCCjbnSgZ49td267IH\vdo1ifGmxbh?= MVyyOVI1QTV3Nx?=
KATO-III NUDZfmlsTnWwY4Tpc44h[XO|YYm= MkTxNUDPxE1? NH3ROnRFVVOR MXLpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 MUGyOVI1QTV3Nx?=
OCUM-2M MoP4SpVv[3Srb36gZZN{[Xl? MkDmNUDPxE1? Mlm1SG1UVw>? NYHS[FVzcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MYCyOVI1QTV3Nx?=
KATO-III NHrGcY1CeG:ydH;zbZMh[XO|YYm= MV2xJO69VQ>? NVrW[5RiTE2VTx?= NG\wOHRqdmS3Y3XzJIFxd3C2b4Ppdy=> NYDzOoRrOjV{NEm1OVc>
OCUM-2M NWXnU4ppSXCxcITvd4l{KGG|c3H5 M1jTd|Eh|ryP MYTEUXNQ NWryUJk3cW6mdXPld{BieG:ydH;zbZM> MW[yOVI1QTV3Nx?=
KATO-III MkfNSpVv[3Srb36gZZN{[Xl? MUWxJO69VQ>? M{XYbWROW09? M1;0S4lvcGmkaYTzJGZITlJ{IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUB{cWewYXzpcochdW:uZXP1cIV{ MUGyOVI1QTV3Nx?=

... 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
体内研究 与没有经过Pazopanib或者仅用10 mg/kg的Pazopanib治疗的小鼠相比,经过30 mg/kg或者100 mg/kg Pazopanib治疗的小鼠其肿瘤症状明显减轻。Pazopanib治疗耐受性良好,各组小鼠之间体重没有发生明显差异[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

激酶活性测定:

通过杆状病毒表达系统纯化人源的VEGFR受体激酶1, 2和3的C端催化活性区域的GST融合蛋白,用这些蛋白在384孔微量滴定板上利用均相时间分辨荧光技术(HTRF)对VEGRF1,2和3的酶活性进行分析。首先将10 μL活化的VEGFR2激酶溶液[终浓度为1nM酶溶于0.1 M HEPES,pH 7.5,包含0.1 mg/mL BSA,300 μM DTT]加入10μL底物溶液[终浓度为360 nM多肽(生物素偶联的aminohexyl-EEEEYFELVAKKKK-NH2),75 μM ATP, 10 μM MgCl2],同时加入1 μL 溶解在DMSO中的Pazopanib。滴定板在室温条件下孵育1小时,然后加入20 μL 100 mM 的EDTA终止反应。终止之后,加入20μL HTRF试剂(终浓度为15 nM 链亲和素偶联的别藻蓝素,用0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5稀释的1 nM铕标记的酪氨酸磷酸化抗体)孵育十分钟以上。使用Wallac Victor的时间分辨荧光仪测定665 nM处的荧光值,时间间隔为50 μs。
细胞实验:

[1]

- 合并
  • Cell lines: HUVEC细胞
  • Concentrations: 0 μM -10 μM
  • Incubation Time: 1 小时
  • Method:

    检测经过VEGF处理过的HUVEC细胞中VEGFR2的磷酸化水平。细胞按每板100万到150万个的密度培养在铺有I型胶原蛋白的10 cm平板上,培养基选用 Clonetics EGM-MV。培养24小时后, 将原来的培养基换成含有0.1% BSA和500 μg/mL hydrocortisone 的Clonetics EBM 培养基,对细胞进行过夜的血清饥饿处理。然后用不同浓度的 Pazopanib 处理细胞1小时, 随后用10 ng/mL 的VEGF 或者对照物处理细胞10分钟。将细胞溶解在裂解液中。用flk-1的抗体对VEGFR2进行免疫沉淀反应,随后进行SDS-聚丙烯酰胺凝胶电泳,然后用flk-1 或者 antiphosphotyrosine (anti-P-tyr-biotin)的抗体进行蛋白免疫印迹的检测。通过光密度法测量将VEGFR2的磷酸化水平量化并将总的VEGFR2水品标准化。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 携带SYO-1细胞的免疫缺陷小鼠
  • Dosages: 0 mg/kg, 10 mg/kg, 30 mg/kg或100 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 17 mg/mL (35.86 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 473.98
化学式

C21H23N7O2S.HCl

CAS号 635702-64-6
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID