Sunitinib

Catalog No.S7781 Synonyms: SU11248

Sunitinib Chemical Structure

Molecular Weight(MW): 398.47

Sunitinib 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.

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Cited by 89 Publications

Purity & Quality Control

Choose Selective PDGFR Inhibitors

Biological Activity

Description Sunitinib 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.
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
human SW756 cell M2rTXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHjTY5pcWKrdHnvckBw\iCqdX3hckBUXzd3NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlE{PTFizszN MWPTRW5ITVJ?
human EoL-1-cell cell M1\wcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYDJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjZ2ZT2wOi=> NGXtcIRUSU6JRWK=
human MV-4-11 cell NH7jVXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1zx[GlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjd{IH7N M2nUUnNCVkeHUh?=
human MV411 cells MoDoVJJwdGmoZYLheIlwdiCjc4PhfS=> NXvkbFVUPDhiaB?= M2DLbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0NVEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygbYM2OD1|IH7N MlnONlQ6ODR7NkG=
3T3 cells NEHM[npHfW6ldHnvckBie3OjeR?= NWn0[2JTUW6qaXLpeIlwdiCxZjDQSGdHNWmwZIXj[YQhSnKmVTDpcoNwenCxcnH0bY9vKGmwIEPUN{Bk\WyuczD3bZRpKDBwMTWgZo93cW6nIIPldpVuKGGuYoXtbY4tKEmFNUC9O{BvVQ>? NFyxW|IyOjZ2NkCxPS=>
HEK293 cells MmrZSpVv[3Srb36gZZN{[Xl? MWTCbY5lcW6pIHHm[olvcXS7IITvJGZNXDNiY3H0ZYx6fGmlIHTvcYFqdiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGK7IHPvcZBmfGm2aY\lJIJqdmSrbnegZZN{[XluIFvkQVAvPDdibl2= MX[xPVc2PDF7OR?=
human MDA-MB-435 cells Ml3oR5l1d3SxeHnjxsBie3OjeR?= M{Kxe|IhcA>? MnzYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygTWM2OD17Lkegcm0> MWCyOFg6ODZ3Mh?=
human RS4-11 cells M4T5VmZ2dmO2aX;uJIF{e2G7 NUDWTnZ6UW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHXs[YN1em:laHXtbYx2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3ME25Mlkhdk1? M{fwNVE6PjV2NEC4
HUVEC MVPDfZRwfG:6aXRCpIF{e2G7 M{jYS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiXVlXDMEBKSzVyPUGxMlghdk1? NETKZ5ozPDh7ME[1Ni=>
human Kasumi-1 cells MmriSpVv[3Srb36gZZN{[Xl? MmLjTY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEujc4XtbU0yKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNTDuUS=> NV7L[YFTOjB6M{OwN|k>
human NOS-1 cell NVTWc3hDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF3C[oRKdmirYnn0bY9vKG:oIHj1cYFvKE6RUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvOyCwTR?= Ml3XV2FPT0WU
mouse triple negative 4T1 cells NWPWbZNOS3m2b4TvfIlkyqCjc4PhfS=> NGDkcXJEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UB1emmybHWgcoVo[XSrdnWgOHQyKGOnbHzzMEBKSzVyPUG2JI5O M2PVelI1QDlyNkWy
human RS4-11 cells NIPJPFFHfW6ldHnvckBie3OjeR?= NVrCXml7UW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNjDuUS=> NFWyWXYzODh|M{CzPS=>
human MOLM13 cells M3q2S2N6fG:2b4jpZ:Kh[XO|YYm= NYn3eHBPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVU:OTUGzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTdwNzDuUS=> M37rNlI2ODh7OEGw
human U251 cells Ml\3SpVv[3Srb36gZZN{[Xl? NE\6RZVKdmirYnn0bY9vKG:oIG\FS2ZTOiCrbjDoeY1idiCXMkWxJINmdGy|IHL5JJBpd3OyaH;0fZJwe2mwZTDFUGlUSSxiSVO1NF0yQC57IH7N MkPUNlQ6ODB6NkW=
NIH3T3 cells MVvGeY5kfGmxbjDhd5NigQ>? NHHuN2YyKGh? M37uVmlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKEuGUjDrbY5ie2ViZYjwdoV{e2WmIHnuJG5KUDOWMzDj[YxteyC5aYToJFQhfU1iQnnveIlvNUGqeD3BSWVGYU[ITF\BMYFucWSnIHH0JIFu[mmnboSgeIVueGW{YYT1doUh\m:{IEGgbJI> NFnIO3oyPjF4MkCwPC=>
MDA-MB-231 cells NG\5S4dEgXSxdH;4bYPDqGG|c3H5 M3TiWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJRzcXCuZTDu[YdifGm4ZTDNSGEuVUJvMkOxJINmdGy|LDDJR|UxRTJ{LkOgcm0> MYOyOFg6ODZ3Mh?=
MCF7 cells NXPpV5lyS3m2b4TvfIlkyqCjc4PhfS=> NV7YU5A1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTVJvcH;zbZRqfmViTVPGO{Bk\WyuczygTWM2OD1{Nz6xJI5O NVG5O3N1OjR6OUC2OVI>
human CGTH-W-1 cell NILwO45Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvQTRibl2= MlXEV2FPT0WU
human MONO-MAC-6 cell NHXCWppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjNRVVQUW6qaXLpeIlwdiCxZjDoeY1idiCPT17PMW1CSy14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{OuPEBvVQ>? Mn\qV2FPT0WU
human HL60 cells Mor2R5l1d3SxeHnjxsBie3OjeR?= MUm0PEBp MlnIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUO2Mlghdk1? NVrkdmR{OjVyOEm4NVA>
human TT cells M3vWRXBzd2yrZnXyZZRqd25iYYPzZZk> NEnJRWY4OiCq MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSWIHPlcIx{KHC{ZYTy[YF1\WRiZn;yJFczKGi{czDmc4xtd3enZDDifUBkd22yb4Xu[E14[XOqb4X0JI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NECgcm0> M{XjOlI1QTB2OU[x
human THP1 cells MWHDfZRwfG:6aXRCpIF{e2G7 NYG2OlNSPDhiaB?= NI\WU3ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUFBzIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFUvPyCwTR?= NHfXUVAzPTB6OUixNC=>
3T3 cells MkfDSpVv[3Srb36gZZN{[Xl? NVftblE5UW6qaXLpeIlwdiCxZjDWZZNkfWyjcjDlcoRwfGinbHnhcEBoem:5dHig[oFkfG:{IILlZ4VxfG:{IHnuJFNVOyClZXzsd{whUUN3ME21NEBvVQ>? NUC2OldiOTJ4NE[wNVk>
human ALL-PO cell MmjkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE[wd4VKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc6Njh7IH7N NGDlVnhUSU6JRWK=
human SH-SY5Y cells M4OxWGZ2dmO2aX;uJIF{e2G7 MmjpTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iU1itV3k2YSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVA:QDNwMTDuUS=> MnLNNlQ5QTB4NUK=
human U251 cells MkTOSpVv[3Srb36gZZN{[Xl? M{jBZVYxKG2rboO= MnXkTY5pcWKrdHnvckBw\iCSRFfGVk1j\XSjIHnuJIh2dWGwIGWyOVEh[2WubIOgZ49ueG:3bnSgdJJmfHKnYYTl[EBnd3JiNkCgcYlvKGKnZn;y[UBRTEeILVLCJJN1cW23bHH0bY9vKG[xcjCxNEBucW6|IHL5JJBpd3OyaH;0fZJwe2mwZTDFUGlUSSCleYTvZoxwfCCvZYToc4QtKEmFNUC9PFMvOSCwTR?= NWWzVGh6OjV6OEK1NVk>
human NKM-1 cell M4\rfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH\qRVRKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVgvPTJibl2= NGn0VmhUSU6JRWK=
human HAEC cells MlfvVJJwdGmoZYLheIlwdiCjc4PhfS=> M3;WdFczKGh? NWXlTHpvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIRWVEKGOnbHzzJIV5eHKnc4PpcochXkWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkGg{txO NVPOeZk{OjJ2NES2O|k>
HUVEC cell MXHGeY5kfGmxbjDhd5NigQ>? MonTNlQhcA>? Mlr6TY5pcWKrdHnvckBw\iCYRVfGMWEhcW6mdXPl[EBJXV[HQzDj[YxtKHOycn;1eIlv\yCjZoTldkAzPCCqcoOgZpkh[W6paX;n[Y5me2m|IHHzd4F6NCCLQ{WwQVAvOTJizszN M1z5VlIyPzRzMkS5
human A431 cells M1XoOmZ2dmO2aX;uJIF{e2G7 MV62NEBucW6| Mk\HTY5pcWKrdHnvckBw\iCHR1\SJIlvKGi3bXHuJGE1OzFiY3XscJMh[2:vcH;1coQheHKndILlZZRm\CCob4KgOlAhdWmwIHLl[o9z\SCHR1[gd5RqdXWuYYTpc44h\m:{IEGwJI1qdnNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCKGO7dH;icI91KG2ndHjv[EwhUUN3ME2xO|IvOSCwTR?= NFT1eYwzPTh6MkWxPS=>
Sf9 cells NXPjVpk6TnWwY4Tpc44h[XO|YYm= M2rQdmlvcGmkaYTpc44hd2ZiR2PUMZRi\2enZDDWSWdHWiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNVg2KM7:TR?= NGLiWGQyQTh3NEC1NS=>
human HT-29 cells M1\CTnBzd2yrZnXyZZRqd25iYYPzZZk> NG\BeWw4OiCq MlGzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDlfJBz\XO|aX7nJHZGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XoxvJygTWM2OD1yLkOzJO69VQ>? MWCyNlQ1PDZ5OR?=
human KM12 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO1NFE1KM7:TR?= NY\1W3U3W0GQR1XS
human TE-15 cell NEfSOpJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61NFc3OSEQvF2= NH;lOpBUSU6JRWK=
human 697 cell NVTtZXN3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnP1TY5pcWKrdHnvckBw\iCqdX3hckA3QTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[xOFI2KM7:TR?= NGnxVm1USU6JRWK=
human CAKI-1 cells M3XNNnBzd2yrZnXyZZRqd25iYYPzZZk> NXXRdFhZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDRWtKNTFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlY{KM7:TR?= MmXSNlI2PjB4Mke=
human MOLT-16 cell M3XTXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2LkfmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjNzM{Kg{txO MlHnV2FPT0WU
human GB-1 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M362TWlvcGmkaYTpc44hd2ZiaIXtZY4hT0JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|ExOjNizszN M3znTnNCVkeHUh?=
human TE-12 cell NIjIWVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64NFQ2PSEQvF2= NVnOXXlRW0GQR1XS
human NCI-H3122 cells NGHIfmJRem:uaX\ldoF1cW:wIHHzd4F6 NGH5U3E4OiCq Mm\2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg{KM7:TR?= M2\tVlI1QTB2OU[x
human ES6 cell NGfv[XpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXyZ5RKdmirYnn0bY9vKG:oIHj1cYFvKEWVNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVgyODZizszN NWnoVmZ6W0GQR1XS
human NCI-H526 cells NUjHeJN3WHKxbHnm[ZJifGmxbjDhd5NigQ>? Mlu0O|IhcA>? NHvtXVRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4xOSEQvF2= NXSzW3RpOjR7MES5OlE>
human LC-2-ad cell MlnRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLFTY5pcWKrdHnvckBw\iCqdX3hckBNSy1{LXHkJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTRyNzFOwG0> NF3nTJpUSU6JRWK=
human BL-70 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlW1TY5pcWKrdHnvckBw\iCqdX3hckBDVC15MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNVE5PDZizszN M4\CdnNCVkeHUh?=
human ETK-1 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6yPFU5KM7:TR?= NHe2[IRUSU6JRWK=
human SW620 cells NYPWW5FHWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUj0e2FJPDhiaB?= M1e4UGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1zLkOg{txO NYDofFM1OjJ3NkC2Nlc>
IM9 cells MXTDfZRwfG:6aXRCpIF{e2G7 NXnWTW9ZS3m2b4TvfIlkcXS7IHHnZYlve3RiSH;tc{B{[XCrZX7zJEhpfW2jbjmgTW06KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1zLkO1JO69VQ>? NUXL[|cxW0GQR1XS
human A4-Fuk cell NH\J[ZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{j4ZmlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjN2MUSxJO69VQ>? M17OXXNCVkeHUh?=
human SR cell M131fWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVPZU2N{UW6qaXLpeIlwdiCxZjDoeY1idiCVUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVQ2PzJizszN NETQVXZUSU6JRWK=
human A3-KAW cell M2Pubmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWOyfXo6UW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiaXO1NF0yNjZ{NUS2JO69VQ>? M2XLd3NCVkeHUh?=
human KS-1 cell MlPsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHnS3dUUW6qaXLpeIlwdiCxZjDoeY1idiCNUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43QTJ2NzFOwG0> M2q4NXNCVkeHUh?=
human CTV-1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKGi3bXHuJGNVXi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlc2OSEQvF2= MYDTRW5ITVJ?
human LB1047-RCC cell M{jWfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojWTY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS56MU[yOEDPxE1? M3vDSXNCVkeHUh?=
human MEG-01 cell NYGwXoxNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJG1GTy1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFM2PjNizszN NVvwXVBNW0GQR1XS
human TE-11 cell M4rCTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64N|k5PSEQvF2= NWPZWItxW0GQR1XS
human CMK cell M4nYU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGXOdo9KdmirYnn0bY9vKG:oIHj1cYFvKEOPSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVU2OTdizszN NIi1VoRUSU6JRWK=
human NB1 cell NHrYRVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5DOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOU[xNVch|ryP M1G5fnNCVkeHUh?=
human MDA-MB-435 cells Mke1VJJwdGmoZYLheIlwdiCjc4PhfS=> NF;mc3g1QCCq M3TtS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCJSU2yJO69VQ>? MU[yNlU3ODZ{Nx?=
human MCF7 cells NGLBW|dRem:uaX\ldoF1cW:wIHHzd4F6 NF3qd3M1QCCq M324cWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTJizszN NXnoRpdNOjJ3NkC2Nlc>
human A549 cells M1fiR2N6fG:2b4jpZ:Kh[XO|YYm= MkS1O|IhcA>? NFXYfYtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi52NDFOwG0> M4LHS|I{PjB{NESx

... 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
  • Formulation: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • 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.
7mg/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 SU11248

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04115189 Not yet recruiting Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer October 7 2019 --
NCT04033991 Not yet recruiting Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 2019 --
NCT03900793 Recruiting Drug: Losartan|Drug: Sunitinib Osteosarcoma University of Colorado Denver|National Cancer Institute (NCI) August 22 2019 Phase 1
NCT03846128 Not yet recruiting Biological: blood sample Metastatic Kidney Cancer University Hospital Rouen August 2019 --
NCT03905889 Suspended Drug: Abemaciclib|Drug: Sunitinib Renal Cell Carcinoma Metastatic Milton S. Hershey Medical Center|Eli Lilly and Company June 5 2019 Phase 1
NCT03916458 Not yet recruiting -- Carcinoma Renal Cell Pfizer April 18 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID