Sunitinib (SU11248)

Catalog No.S7781

For research use only.

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.

Sunitinib (SU11248) Chemical Structure

CAS No. 557795-19-4

Selleck's Sunitinib (SU11248) has been cited by 177 publications

Purity & Quality Control

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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 M1jOV2Z2dmO2aX;uJIF{e2G7 MXOyOEBp MnvxTY5pcWKrdHnvckBw\iCYRVfGMWEhcW6mdXPl[EBJXV[HQzDj[YxtKHOycn;1eIlv\yCjZoTldkAzPCCqcoOgZpkh[W6paX;n[Y5me2m|IHHzd4F6NCCLQ{WwQVAvOTJizszN NHfleZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe0NVI1QSd-MkG3OFEzPDl:L3G+
HEK293 MX3GeY5kfGmxbjDhd5NigQ>? M3nJVGJqdmSrbnegZYZncW6rdImgeI8hTkyWMzDjZZRidHm2aXOg[I9u[WmwIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgZ49ueGW2aYTpeoUh[mmwZHnu[{Bie3OjeTygT4QhRSByLkCwNFQ4KM7:TT6= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd3NEG5PUc,OTl5NUSxPVk9N2F-
MV4-11 MmG1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnPnO|IhcHK| M1HMVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSmxVOy2LVFSg[IVx\W6mZX70JIh2dWGwIF3WOE0yOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmei2pbH:vR2NMQCCjc4PhfUwhT0l3MDC9JFAvODBzIN88UU4> M3rWRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
HL60 MkDVRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUS3NkBpenN? NGH1[IVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBk\WyudHn0[ZIu\2yxL1PDT|gh[XO|YYmsJGdKPTBiPTCwMlAxOSEQvF2u MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
BAF3 MoP1SpVv[3Srb36gZZN{[Xl? MlLnO|IhcHK| MnjDTY5pcWKrdHnvckBw\iCWZXyt[pV{\WRiY1vJWEBVPjdySTDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRWY{KGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LXfsc{9ES0t6IHHzd4F6NCCJSUWwJF0hOC5yMEKg{txONg>? NF\SU5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
MV4-11 MnL4R5l1d3SxeHnjbZR6KGG|c3H5 NGfqSnc4OiCqcoO= NXOyZ5ZXS3m2b4TvfIlkcXS7IHHnZYlve3RiRlzUN{1l\XCnbnTlcpQhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjByMzFOwG0v MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3MkWxPEc,OjJ2NUK1NVg9N2F-
MV411 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MofoOFghcHK| MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YNEGxJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCwN{DPxE1w NXnES|IzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFQ6PjFpPkK0PVA1QTZzPD;hQi=>
BA/F3 MlrJSpVv[3Srb36gZZN{[Xl? NVSzd5J5PzJiaILz NEP0[lhKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA1KM7:TT6= MnzLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
MV4-11 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NUDyWYJYPzJiaILz MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6wNFQ{KM7:TT6= M1zP[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{W0NVk6Lz5zOUe1OFE6QTxxYU6=
MV4-11 M2rIO2N6fG:2b4jpZ4l1gSCjc4PhfS=> NFrIXW44OiCqcoO= NV7ic|U5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGlEPTBiPTCwMlAxPDNizszNMi=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
Sf21 NY\meJZITnWwY4Tpc44h[XO|YYm= MnnmOlAhdWmwcx?= M3K2WGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iTj30[ZJucW6jbDDIbZM3NXSjZ3fl[EBMTFJiKEe5NEB1dyCnbnSgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lIyKGmwc3XjeEBk\WyuczDh[pRmeiB4MDDtbY5{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMES3JO69VS5? MofsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEGwNVAoRjNyMkSxNFExRC:jPh?=
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MOLM14 M2DLfWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NI[5[VU4OiCqcoO= MoHTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDGUHQ{NUmWRDDk[ZBmdmSnboSgbJVu[W5iTV;MUVE1KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNE4xODVizszNMi=> M3HT[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
BA/F3 NFvQWo5HfW6ldHnvckBie3OjeR?= M3;vWVczKGi{cx?= NWfhZ|lwUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJHY3PTSDIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyIE2gNE4xODZizszNMi=> NUjWbXlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BAF3 NIHGZ2xHfW6ldHnvckBie3OjeR?= NF2zOWk4OiCqcoO= MWPJcohq[mm2aX;uJI9nKFSnbD3meZNm\CClS1nUJHY2PTmGL2[2OVRCKGSxdXLs[UBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNFYh|ryPLh?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
MDA-MB-468 MYXDfZRwfG:6aXPpeJkh[XO|YYm= NEOz[lZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckB1emmybHWgcoVo[XSrdnWgUWRCNU2ELUS2PEBk\WyuczygTWM2OCB;IECuNFA3OSEQvF2u MlPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
3T3 M{LCUGZ2dmO2aX;uJIF{e2G7 NHfFXpRKdmirYnn0bY9vKG:oIGDES2YucW6mdXPl[EBDemSXIHnuZ49zeG:{YYTpc44hcW5iM2SzJINmdGy|IIfpeIhwfXRiYn;2bY5mKHOncoXtJIFt[nWvaX6sJGlEPTBiPTCwMlAxPyEQvF2u M2H6UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{NkS2NFE6Lz5zMk[0OlAyQTxxYU6=
3T3 MmPpSpVv[3Srb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36gbY4hO1R|IHPlcIx{KHerdHigNE4yLSCkb4\pcoUhe2W{dX2gZYxjfW2rbjygTWM2OCB;IECuNFA4KM7:TT6= NHHBVnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMk[0OlAyQSd-MUK2OFYxOTl:L3G+
3T3 MXrGeY5kfGmxbjDhd5NigQ>? M2eySGlvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckBqdiB|VEOgZ4VtdHNid3n0bEAxNjVnIHLveolv\SC|ZYL1cUBidGK3bXnuMEBKSzVyIE2gNE4xODdizszNMi=> M2joNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{NkS2NFE6Lz5zMk[0OlAyQTxxYU6=
BA/F3 Ml3QSpVv[3Srb36gZZN{[Xl? MYC3NkBpenN? MljmTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiB7IFHZOVAzKHSxIEWwN{BqdnOncoTpc44hdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCwO{DPxE1w NVnsToN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3 NVX2WIMxTnWwY4Tpc44h[XO|YYm= MVS3NkBpenN? MoewTY5pcWKrdHnvckBw\iCNaYSgWlU3OERxVk[1OGEhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCwO{DPxE1w M1HPUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
3T3 NFjjdXhHfW6ldHnvckBie3OjeR?= Mk[zTY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJIlvKDOWMzDj[YxteyC5aYToJFEmKGKxdnnu[UB{\XK3bTDhcIJ2dWmwLDDJR|UxKD1iMD6wNFgh|ryPLh?= M1ntO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{NkS2NFE6Lz5zMk[0OlAyQTxxYU6=
3T3 MXnGeY5kfGmxbjDhd5NigQ>? MmLHTY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJIlvKDOWMzDj[YxteyxiSVO1NEA:KDBwMEC4JO69VS5? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZ2NkCxPUc,OTJ4NE[wNVk9N2F-
MV4-11 Moj1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmDpO|IhcHK| NGn0UGVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4xODlizszNMi=> NH;JWng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW3NFUzPid-MkC1O|A2OjZ:L3G+
MV4-11 MoKwR5l1d3SxeHnjbZR6KGG|c3H5 NHfZeW5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOXjRvMUGgZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4xODlizszNMi=> NH\zUHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEizN|A{QSd-MkC4N|MxOzl:L3G+
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endothelial precursor cells NFLqWZhHfW6ldHnvckBie3OjeR?= NWnoUnFTUW6qaXLpeIlwdiCxZjDlcoRwfGinbHnhcEBkd3KmIHHy[YEh\m:{bXH0bY9vKGmwIHXu[I91cGWuaXHsJJBz\WO3coPvdkBk\WyuczDifUBETDNzIHPvdoQh[XKnYTDk[ZRm[3Srb36gZoF{\WRicHjlco91gXCrYzDkdpVoKGSrc3PveoVzgSCkYYPl[EBie3OjeTygTWM2OCB;IECuNFA6PiEQvF2u M2L3PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEC5OlY3Lz5{MkSwPVY3PjxxYU6=
MDA-MB-435 M2[0WWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3rPVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGlEPTBiPTCwMlAxQTdizszNMi=> MnruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
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MV4-11 MV;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYnURmhpPzJiaILz NWf3SI5pSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjBzIN88UU4> MkTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7M{W3O|IoRjJ7OUO1O|czRC:jPh?=
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MDA-MB-231 M1GxSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVL6OnFQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hfHKrcHzlJI5m\2G2aY\lJG1FSS2PQj2yN|Eh[2WubIOsJGlEPTBiPTCwMlAzOjNizszNMi=> MkPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
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BA/F3 NIHEV41HfW6ldHnvckBie3OjeR?= NGHYSHI4OiCqcoO= MlHRTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVYxKHSxIEW3PEBz\XOrZIXld{khdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCyOEDPxE1w M1O1Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
MV4-11 M3PQfGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUi0PEBpenN? MmnFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjB{NEOg{txONg>? Ml3yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOEm4NVAoRjJ3MEi5PFExRC:jPh?=
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KM-H2 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn;ZTY5pcWKrdHnvckBw\iCqdX3hckBMVS2KMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFQvQTV5NzFOwG0v NEnhPI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OzVxJ{7TRW5ITVJ:L3G+
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Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; p-GSK3β / GSK3β / MYCN ; p-AKT / AKT / p-ERK / ERK 19244102 24759734
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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 --

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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