Sunitinib

For research use only.

Catalog No.S7781 Synonyms: SU11248

124 publications

Sunitinib 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.

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Selleck's Sunitinib has been cited by 124 publications

Purity & Quality Control

Choose Selective PDGFR Inhibitors

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
human SW756 cell MnHMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYHRUoxOUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e1OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjF|NUGg{txO M3\YRnNCVkeHUh?=
human EoL-1-cell cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTSTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS54NHWtNFY> M2C3WnNCVkeHUh?=
human MV-4-11 cell NV7MeW9vT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVn1cXJCUW6qaXLpeIlwdiCxZjDoeY1idiCPVj20MVEyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{N{Kgcm0> NVnxU2k{W0GQR1XS
human MV411 cells MlPVVJJwdGmoZYLheIlwdiCjc4PhfS=> M3nJ[FQ5KGh? NV3UXHl[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQyOSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBq[zVyPUOgcm0> MmfhNlQ6ODR7NkG=
3T3 cells M33xZmZ2dmO2aX;uJIF{e2G7 NWPqZmN4UW6qaXLpeIlwdiCxZjDQSGdHNWmwZIXj[YQhSnKmVTDpcoNwenCxcnH0bY9vKGmwIEPUN{Bk\WyuczD3bZRpKDBwMTWgZo93cW6nIIPldpVuKGGuYoXtbY4tKEmFNUC9O{BvVQ>? NF;lSJkyOjZ2NkCxPS=>
HEK293 cells MVfGeY5kfGmxbjDhd5NigQ>? M1;aTGJqdmSrbnegZYZncW6rdImgeI8hTkyWMzDjZZRidHm2aXOg[I9u[WmwIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgZ49ueGW2aYTpeoUh[mmwZHnu[{Bie3OjeTygT4Q:OC52NzDuUS=> NFXhfmgyQTd3NEG5PS=>
human MDA-MB-435 cells MmPlR5l1d3SxeHnjxsBie3OjeR?= NEfXepkzKGh? NUez[oRoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{whUUN3ME25Mlchdk1? MV[yOFg6ODZ3Mh?=
human RS4-11 cells NWDTUIN{TnWwY4Tpc44h[XO|YYm= NWmweI1TUW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHXs[YN1em:laHXtbYx2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3ME25Mlkhdk1? MWOxPVY2PDRyOB?=
HUVEC Mnf3R5l1d3SxeHnjxsBie3OjeR?= NWL6cZU3S3m2b4TvfIlkcXS7IHHnZYlve3RiSGXWSWMtKEmFNUC9NVEvQCCwTR?= MkHPNlQ5QTB4NUK=
human Kasumi-1 cells M4XDb2Z2dmO2aX;uJIF{e2G7 M4HicWlvcGmkaYTpc44hd2ZiYz3LbZQh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNYYP1cYkuOSClZXzsd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGlEPTB;MUWgcm0> NG\uelQzODh|M{CzPS=>
human NOS-1 cell M2SxO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEXFRnBKdmirYnn0bY9vKG:oIHj1cYFvKE6RUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvOyCwTR?= MnflV2FPT0WU
mouse triple negative 4T1 cells M4XEWmN6fG:2b4jpZ:Kh[XO|YYm= MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTD0dolxdGVibnXnZZRqfmViNGSxJINmdGy|LDDJR|UxRTF4IH7N M3\YVVI1QDlyNkWy
human RS4-11 cells MUHGeY5kfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKE[OVEOgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBTWzRvMUGgZ4VtdHNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE3KG6P NULJfnR2OjB6M{OwN|k>
human MOLM13 cells MX;DfZRwfG:6aXRCpIF{e2G7 M3TZeWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1QVE1zMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE4Njdibl2= MUOyOVA5QThzMB?=
human U251 cells NXexdZZJTnWwY4Tpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUwhUUN3ME2xPE46KG6P NGjKfHYzPDlyMEi2OS=>
NIH3T3 cells Mk[2SpVv[3Srb36gZZN{[Xl? M{S4SlEhcA>? MYfJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBMTFJia3nuZZNmKGW6cILld5Nm\CCrbjDOTWg{XDNiY3XscJMhf2m2aDC0JJVOKEKrb4Tpck1CcHhvQVXFSXlHTkyIQT3hcYll\SCjdDDhcYJq\W62IITlcZBmemG2dYLlJIZweiBzIHjy Mmq0NVYyPjJyMEi=
MDA-MB-231 cells MYrDfZRwfG:6aXRCpIF{e2G7 MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjD0dolxdGVibnXnZZRqfmViTVTBMW1DNTJ|MTDj[YxteyxiSVO1NF0zOi5|IH7N NEjmbYkzPDh7ME[1Ni=>
MCF7 cells MV;DfZRwfG:6aXRCpIF{e2G7 MmLQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSXIueG:|aYTpeoUhVUOINzDj[YxteyxiSVO1NF0zPy5zIH7N MnX0NlQ5QTB4NUK=
human CGTH-W-1 cell NYPKfGJDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmPFTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjl2IH7N NXHZd5NRW0GQR1XS
human MONO-MAC-6 cell NIjkdmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJG1QVk9vTVHDMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy56IH7N M4eyRXNCVkeHUh?=
human HL60 cells NEnpNHZEgXSxdH;4bYPDqGG|c3H5 NFP2[nc1QCCq NEf4eWFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9N|YvQCCwTR?= MnK4NlUxQDl6MUC=
human TT cells NEjhSVNRem:uaX\ldoF1cW:wIHHzd4F6 M{XpWFczKGh? MoDtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWVDDj[YxteyCycnX0doVifGWmIH\vdkA4OiCqcoOg[o9tdG:5ZXSgZpkh[2:vcH;1coQuf2G|aH;1eEBu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSwJI5O NXTjWVkyOjR7MES5OlE>
human THP1 cells NXHod5hWS3m2b4TvfIlkyqCjc4PhfS=> NG\WTWc1QCCq NWi5eGd1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2Njdibl2= M{G3flI2ODh7OEGw
3T3 cells NGjDPY5HfW6ldHnvckBie3OjeR?= MoT3TY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKGmwIEPUN{Bk\WyuczygTWM2OD13MDDuUS=> NYnCW21TOTJ4NE[wNVk>
human ALL-PO cell MlLaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVT2W2luUW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04QS56OTDuUS=> NWf3OZoyW0GQR1XS
human SH-SY5Y cells MWHGeY5kfGmxbjDhd5NigQ>? NGfZfJFKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUBie3OjeTygTWM2OD16Mz6xJI5O NH3K[mgzPDh7ME[1Ni=>
human U251 cells MnS1SpVv[3Srb36gZZN{[Xl? NEXt[Vg3OCCvaX7z M4DMUWlvcGmkaYTpc44hd2ZiUFTHSnIu[mW2YTDpckBpfW2jbjDVNlUyKGOnbHzzJINwdXCxdX7kJJBz\XS{ZXH0[YQh\m:{IE[wJI1qdiCkZX\vdoUhWESJRj3CRkB{fGmvdXzheIlwdiCob4KgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RibXX0bI9lNCCLQ{WwQVg{NjFibl2= NWDzXIhKOjV6OEK1NVk>
human NKM-1 cell NH;GZmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUPJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUiuOVIhdk1? MkPWV2FPT0WU
human HAEC cells NFrm[olRem:uaX\ldoF1cW:wIHHzd4F6 MU[3NkBp MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiDRVOgZ4VtdHNiZYjwdoV{e2mwZzDWSWdHWiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOSEQvF2= MXOyNlQ1PDZ5OR?=
HUVEC cell NV;tOWd3TnWwY4Tpc44h[XO|YYm= NUXKZ2tGOjRiaB?= M{\1ZmlvcGmkaYTpc44hd2ZiVlXHSk1CKGmwZIXj[YQhUFWYRVOgZ4VtdCC|cILveZRqdmdiYX\0[ZIhOjRiaILzJIJ6KGGwZ3nv[4Vv\XOrczDhd5NigSxiSVO1NF0xNjF{IN88US=> NFfyN|QzOTd2MUK0PS=>
human A431 cells NXrPSmhXTnWwY4Tpc44h[XO|YYm= Mk\0OlAhdWmwcx?= MoS0TY5pcWKrdHnvckBw\iCHR1\SJIlvKGi3bXHuJGE1OzFiY3XscJMh[2:vcH;1coQheHKndILlZZRm\CCob4KgOlAhdWmwIHLl[o9z\SCHR1[gd5RqdXWuYYTpc44h\m:{IEGwJI1qdnNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCKGO7dH;icI91KG2ndHjv[EwhUUN3ME2xO|IvOSCwTR?= M4qzUVI2QDh{NUG5
Sf9 cells MnKxSpVv[3Srb36gZZN{[Xl? NYX0dWQ{UW6qaXLpeIlwdiCxZjDHV3QufGGpZ3XkJHZGT0[UIHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NE4yQDVizszN M2PmRVE6QDV2MEWx
human HT-29 cells M{GyZXBzd2yrZnXyZZRqd25iYYPzZZk> NVnrPXRYPzJiaB?= MlnrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDlfJBz\XO|aX7nJHZGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XoxvJygTWM2OD1yLkOzJO69VQ>? MYWyNlQ1PDZ5OR?=
human KM12 cell M{e0Vmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXiTY5pcWKrdHnvckBw\iCqdX3hckBMVTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOVAyPCEQvF2= MX7TRW5ITVJ?
human TE-15 cell NV;aUoh6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3L0XmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxPzZzIN88US=> MVXTRW5ITVJ?
human 697 cell NU\xRlU3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYrJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkG0NlUh|ryP NV;iR|kxW0GQR1XS
human CAKI-1 cells NXXOb5pJWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkHyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQVvJMVEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1yLk[zJO69VQ>? NGexXGIzOjV4ME[yOy=>
human MOLT-16 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M173fGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjNzM{Kg{txO MnHRV2FPT0WU
human GB-1 cell NFPybnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGdDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkexNFI{KM7:TR?= MnPQV2FPT0WU
human TE-12 cell NIi1WYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3L2OWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgxPDV3IN88US=> NFPGR2FUSU6JRWK=
human NCI-H3122 cells Mon5VJJwdGmoZYLheIlwdiCjc4PhfS=> MVm3NkBp MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuPFMh|ryP M1jrT|I1QTB2OU[x
human ES6 cell NIr1VHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGVUPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOUixNFYh|ryP MVvTRW5ITVJ?
human NCI-H526 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 NFH0cGg4OiCq MonDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFUzPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuNFEh|ryP MnfENlQ6ODR7NkG=
human LC-2-ad cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIHveFRKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUKtZYQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjFzNEC3JO69VQ>? MWXTRW5ITVJ?
human BL-70 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFWzWnJKdmirYnn0bY9vKG:oIHj1cYFvKEKOLUewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTh2NjFOwG0> NETLR|VUSU6JRWK=
human ETK-1 cell NEn0TJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH7Dbm9KdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zQDV6IN88US=> MVrTRW5ITVJ?
human SW620 cells NX;YTGtNWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFO1U3U1QCCq MmTsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMzFOwG0> MVGyNlU3ODZ{Nx?=
IM9 cells NWfkeYdjS3m2b4TvfIlkyqCjc4PhfS=> MmX6R5l1d3SxeHnjbZR6KGGpYXnud5QhUG:vbzDzZZBq\W6|IDjoeY1idiliSV25JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjN3IN88US=> NF;OOolUSU6JRWK=
human A4-Fuk cell NH;YN3BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NITse3VKdmirYnn0bY9vKG:oIHj1cYFvKEF2LV\1b{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:OS5|NEG0NUDPxE1? NIf6PXBUSU6JRWK=
human SR cell M13S[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MonlTY5pcWKrdHnvckBw\iCqdX3hckBUWiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUS1O|Ih|ryP M1LKN3NCVkeHUh?=
human A3-KAW cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHS2R4hKdmirYnn0bY9vKG:oIHj1cYFvKEF|LVvBW{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCrY{WwQVEvPjJ3NE[g{txO MWLTRW5ITVJ?
human KS-1 cell M2XDUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LMdGlvcGmkaYTpc44hd2ZiaIXtZY4hU1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlkzPDdizszN NEGze5VUSU6JRWK=
human CTV-1 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmTNTY5pcWKrdHnvckBw\iCqdX3hckBEXFZvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO|I4PTFizszN NWX1eG1rW0GQR1XS
human LB1047-RCC cell MmfqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlTOTY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS56MU[yOEDPxE1? M4TvNHNCVkeHUh?=
human MEG-01 cell M4fNRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG[wSWtKdmirYnn0bY9vKG:oIHj1cYFvKE2HRz2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDN3NkOg{txO MlfwV2FPT0WU
human TE-11 cell NELY[41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXnWXGh6UW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDN7OEWg{txO NIj2bHZUSU6JRWK=
human CMK cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF;yeZpKdmirYnn0bY9vKG:oIHj1cYFvKEOPSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVU2OTdizszN NHfJPGRUSU6JRWK=
human NB1 cell MlrZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHj3XlNKdmirYnn0bY9vKG:oIHj1cYFvKE6EMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVYyOTdizszN MlriV2FPT0WU
human MDA-MB-435 cells M4fwcnBzd2yrZnXyZZRqd25iYYPzZZk> NIXGRo01QCCq MnS5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEeLPUKg{txO NXnVb2VnOjJ3NkC2Nlc>
human MCF7 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 MoDpOFghcA>? M1:xN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTJizszN MXqyNlU3ODZ{Nx?=
human A549 cells NFXiWJlEgXSxdH;4bYPDqGG|c3H5 MXG3NkBp NIXt[mJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi52NDFOwG0> M3:1VFI{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
  • 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
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 ()
% DMSO % % Tween 80 % ddH2O
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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)

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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 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 )

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* 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):
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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
NCT03916458 Recruiting -- Carcinoma Renal Cell Pfizer January 21 2020 --
NCT04115189 Active not recruiting Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT04033991 Active not recruiting Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 27 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 Recruiting Drug: Abemaciclib|Drug: Sunitinib Renal Cell Carcinoma Metastatic Milton S. Hershey Medical Center|Eli Lilly and Company June 5 2019 Phase 1

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID