Sunitinib (SU11248)

For research use only.

Catalog No.S7781

171 publications

Sunitinib (SU11248) Chemical Structure

CAS No. 557795-19-4

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.

Selleck's Sunitinib (SU11248) has been cited by 171 publications

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Biological Activity

Description Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Targets
FLT3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cell MUTGeY5kfGmxbjDhd5NigQ>? M2W1cVI1KGh? MV;Jcohq[mm2aX;uJI9nKF[HR1[tRUBqdmS3Y3XkJGhWXkWFIHPlcIwhe3C{b4X0bY5oKGGodHXyJFI1KGi{czDifUBidmerb3flcoV{cXNiYYPzZZktKEmFNUC9NE4yOiEQvF2= M3LqdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{SxNlQ6Lz5{MUe0NVI1QTxxYU6=
HEK293 M323eWZ2dmO2aX;uJIF{e2G7 MljoRolv\GmwZzDh[oZqdmm2eTD0c{BHVFR|IHPheIFtgXSrYzDkc41icW5iZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCkeTDjc41x\XSrdHn2[UBjcW6maX7nJIF{e2G7LDDL[EA:KDBwMECwOFch|ryPLh?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd3NEG5PUc,OTl5NUSxPVk9N2F-
MV4-11 M3rHTWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NITiVGg4OiCqcoO= MlqxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDGUHQ{NUmWRDDk[ZBmdmSnboSgbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNE4xODFizszNMi=> M2H1NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
HL60 NUSzXmtWSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NITq[po4OiCqcoO= NYHvOmtuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNE4xODFizszNMi=> NWe1cY5iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
BAF3 NUf2PWNKTnWwY4Tpc44h[XO|YYm= MX:3NkBpenN? NUL1[mRmUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgZ2tKXCCWNkewTUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNFIh|ryPLh?= Ml\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
MV4-11 NUm1XIhSS3m2b4TvfIlkcXS7IHHzd4F6 M{LSPVczKGi{cx?= NYPLV5RvS3m2b4TvfIlkcXS7IHHnZYlve3RiRlzUN{1l\XCnbnTlcpQhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjByMzFOwG0v MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3MkWxPEc,OjJ2NUK1NVg9N2F-
MV411 NEnB[25CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3HLWFQ5KGi{cx?= MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YNEGxJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCwN{DPxE1w NHTTZ5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOFk3OSd-MkS5NFQ6PjF:L3G+
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MV4-11 M4TKUGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NIHmVlM4OiCqcoO= NInGO|ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldk1jdHWnIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xODR|IN88UU4> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd3NEG5PUc,OTl5NUSxPVk9N2F-
MV4-11 MVnDfZRwfG:6aXPpeJkh[XO|YYm= NFXtOm44OiCqcoO= Mm\rR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzNWKudXWgZZN{[XluIFnDOVAhRSByLkCwOFMh|ryPLh?= M3jRPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NkW0OFA5Lz5zOU[1OFQxQDxxYU6=
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MOLM14 NHzCTXZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUK3NkBpenN? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF\MWFMuUVSGIHTldIVv\GWwdDDoeY1idiCPT1zNNVQh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBk\WyudHn0[ZIu\2yxL1PDT|gh[XO|YYmsJGdKPTBiPTCwMlAxPSEQvF2u MkjKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{e3NFUoRjJ5MEe3O|A2RC:jPh?=
BA/F3 MnTLSpVv[3Srb36gZZN{[Xl? M4nxVFczKGi{cx?= M{TWTGlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKGGwZDDWOlU1SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA3KM7:TT6= NYL5RnN{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
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3T3 MX\GeY5kfGmxbjDhd5NigQ>? M3[3c2lvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckBqdiB|VEOgZ4VtdHNid3n0bI92fCCkb4\pcoUhe2W{dX2gZYxjfW2rbjygTWM2OCB;IECuNFA4KM7:TT6= Mn7kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJ4NE[wNVkoRjF{NkS2NFE6RC:jPh?=
3T3 NWnLdZZNTnWwY4Tpc44h[XO|YYm= MX\Jcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36gbY4hO1R|IHPlcIx{KHerdHigNE4yLSCkb4\pcoUhe2W{dX2gZYxjfW2rbjygTWM2OCB;IECuNFA4KM7:TT6= NUWwPGRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2OFYxOTlpPkGyOlQ3ODF7PD;hQi=>
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3T3 NU\HUGFsTnWwY4Tpc44h[XO|YYm= NF\pdmxKdmirYnn0bY9vKG:oIGDES2YucW6mdXPl[EBDemSXIHnuZ49zeG:{YYTpc44hcW5iM2SzJINmdGy|LDDJR|UxKD1iMD6wNFgh|ryPLh?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZ2NkCxPUc,OTJ4NE[wNVk9N2F-
MV4-11 MUPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NW\YSlk1PzJiaILz Ml7yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFA6KM7:TT6= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV5MEWyOkc,OjB3N{C1NlY9N2F-
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BT549 NV;jT2JMS3m2b4TvfIlkcXS7IHHzd4F6 NHfP[JY1QCCqcoO= MlLkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnQ2PDliY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVUvPSEQvF2u NYfnOm9YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke2N|k{PjlpPkK3OlM6OzZ7PD;hQi=>
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HepG2 NXnoWok2SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NEjI[pM1QCCqcoO= MnPYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMU[uNFYh|ryPLh?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB3N{SyN{c,OjhyNUe0NlM9N2F-
HepG2 MWjDfZRwfG:6aXPpeJkh[XO|YYm= MmDzOFghcHK| MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSBzNj6wOkDPxE1w NICzb4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkCwPVE3PCd-Mk[wNFkyPjR:L3G+
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EW-11 NWL3XXRJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2rIdWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFM1NjR5MkWg{txONg>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
TE-9 NUO2R3ZXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IEO3MlA1ODFizszNMi=> MmDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM2Nyd-U1HOS2VTRC:jPh?=
ES3 NX3pXWVZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2fWRWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCzO{42ODB2IN88UU4> NHHTWVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OzVxJ{7TRW5ITVJ:L3G+
NCI-H2141 M17zWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LCfWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVQyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB|OD6wPFQ{KM7:TT6= M1\te|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU{PS9pPmPBUmdGWjxxYU6=
MPP-89 M{j1WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHXDeIdKdmirYnn0bY9vKG:oIHj1cYFvKE2SUD24PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDJwMEW4OkDPxE1w NYj0[4xFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
SK-MEL-2 MliyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Oi54NEC1JO69VS5? NXHlXoVqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
LC-1F MnH3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGxENTGIIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0N{4{Pjh{IN88UU4> NX3IWFlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
NH-12 M3rDUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoTsTY5pcWKrdHnvckBw\iCqdX3hckBPUC1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFMvQTN3OTFOwG0v Mki4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM2Nyd-U1HOS2VTRC:jPh?=
RKO M1PLcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XQ[2lvcGmkaYTpc44hd2ZiaIXtZY4hWkuRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0OE4yOjV{IN88UU4> Mme4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM2Nyd-U1HOS2VTRC:jPh?=
KM-H2 MkLES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH6zfmFKdmirYnn0bY9vKG:oIHj1cYFvKEuPLViyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1PC57NUe3JO69VS5? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
SK-UT-1 NVW5[FdQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNVWWLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ6Njh6MkWg{txONg>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-ERK / ERK ; 

PubMed: 24759734     


Effect of 72 h treatment with sunitinib on SH-SY5Y, SK N BE(2), SK-N-AS and IMR-32 NB cell lines analyzed by Western blot with pSer(473)Akt, Akt, pThr202/Thr204 Erk1/2 and Erk1/2 antibodies. β-actin was used as a loading control.

p-GSK3β / GSK3β / MYCN ; 

PubMed: 24759734     


Effect of sunitinib on GSK3β phosphorylation and on MYCN total protein in MYCN amplified NB cell lines.

p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 19244102     


Sunitinib reduced Stat3 and Src activity, with no dramatic reduction of AKT, MAPK and JAK signaling in 786-O cells. Tumor cells were treated with sunitinib at indicated concentrations for 2 h (left panels) or 24 h (right panels). Total cell lysates were prepared and western blots were performed using relevant antibodies to detect total protein levels, with β-actin used as the loading control.

24759734 19244102
Growth inhibition assay
Cell viability; 

PubMed: 24369536     


Isolated effects of sunitinib malate on urinary bladder-cancer cell lines viability, assessed by using the MTT assay. The data shown and bars represent the mean values ± SD (SD: standard deviation). *P < 0.05 versus untreated cells.

24369536
In vivo Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol

Kinase Assay:

[1]

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Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research:

[3]

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  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method:

    Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 25 mg/mL warmed (62.73 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
0.875mg/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 398.47
Formula

C22H27FN4O2

CAS No. 557795-19-4
Storage powder
in solvent
Synonyms N/A
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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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
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / 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 )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / 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):
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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
NCT04669366 Recruiting Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd. November 25 2020 Phase 2
NCT04115189 Completed Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT03916458 Completed -- Carcinoma Renal Cell Pfizer December 17 2019 --
NCT04175262 Completed Drug: sunitinib Metastatic Renal Cell Carcinoma (mRCC) Pfizer|IMDC group|Analysis Group October 31 2019 --
NCT04033991 Completed Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 27 2019 --

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

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PDGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID