Sunitinib

For research use only.

Catalog No.S7781 Synonyms: SU11248

116 publications

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. 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 116 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. 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 NUTWZph{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1j5Z2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d5NU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU4yOzVzIN88US=> NXXWUW53W0GQR1XS
human EoL-1-cell cell MoHnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWDJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjZ2ZT2wOi=> NVPJbYEzW0GQR1XS
human MV-4-11 cell NUmw[pNTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M136TmlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjd{IH7N MlLRV2FPT0WU
human MV411 cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NYnabYtLPDhiaB?= MojQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= M2G2cFI1QTB2OU[x
3T3 cells NUHkTotLTnWwY4Tpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36gbY4hO1R|IHPlcIx{KHerdHigNE4yLSCkb4\pcoUhe2W{dX2gZYxjfW2rbjygTWM2OD15IH7N NWDhWo84OTJ4NE[wNVk>
HEK293 cells MkS5SpVv[3Srb36gZZN{[Xl? M322U2JqdmSrbnegZYZncW6rdImgeI8hTkyWMzDjZZRidHm2aXOg[I9u[WmwIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgZ49ueGW2aYTpeoUh[mmwZHnu[{Bie3OjeTygT4Q:OC52NzDuUS=> MVexPVc2PDF7OR?=
human MDA-MB-435 cells Mnr1R5l1d3SxeHnjxsBie3OjeR?= Ml3NNkBp M{TwSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGlEPTB;OT63JI5O MnnoNlQ5QTB4NUK=
human RS4-11 cells NF;OZYdHfW6ldHnvckBie3OjeR?= NXvnSGJzUW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHXs[YN1em:laHXtbYx2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3ME25Mlkhdk1? NUjVc5ZvOTl4NUS0NFg>
HUVEC MXfDfZRwfG:6aXRCpIF{e2G7 NUfjW4lvS3m2b4TvfIlkcXS7IHHnZYlve3RiSGXWSWMtKEmFNUC9NVEvQCCwTR?= MUeyOFg6ODZ3Mh?=
human Kasumi-1 cells M2\tTmZ2dmO2aX;uJIF{e2G7 Ml\1TY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEujc4XtbU0yKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNTDuUS=> M{jh[FIxQDN|MEO5
human NOS-1 cell NYXpNXJNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYjJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuN{BvVQ>? M4ruZ3NCVkeHUh?=
mouse triple negative 4T1 cells MlviR5l1d3SxeHnjxsBie3OjeR?= M2nXcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJJRzcXCuZTDu[YdifGm4ZTC0WFEh[2WubIOsJGlEPTB;MU[gcm0> Mke0NlQ5QTB4NUK=
human RS4-11 cells MXjGeY5kfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKE[OVEOgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBTWzRvMUGgZ4VtdHNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE3KG6P NVS4fpJ{OjB6M{OwN|k>
human MOLM13 cells M2TSU2N6fG:2b4jpZ:Kh[XO|YYm= NH\sZm1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOV0yPMUOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPy55IH7N M3fUbFI2ODh7OEGw
human U251 cells M{DETmZ2dmO2aX;uJIF{e2G7 NYq3VpB[UW6qaXLpeIlwdiCxZjDWSWdHWjJiaX6gbJVu[W5iVUK1NUBk\WyuczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FuIFnDOVA:OThwOTDuUS=> NG\rT3AzPDlyMEi2OS=>
NIH3T3 cells MXXGeY5kfGmxbjDhd5NigQ>? MYOxJIg> NFfLNoVKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiCNRGKgb4lv[XOnIHX4dJJme3OnZDDpckBPUUh|VEOgZ4VtdHNid3n0bEA1KHWPIFLpc5Rqdi2DaIitRWVGTVmIRlzGRU1idWmmZTDheEBidWKrZX70JJRmdXCncnH0eZJmKG[xcjCxJIhz NV60NpV{OTZzNkKwNFg>
MDA-MB-231 cells NUfHW252S3m2b4TvfIlkyqCjc4PhfS=> MljuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6geJJqeGynIH7l[4F1cX[nIF3ERU1OSi1{M{GgZ4VtdHNuIFnDOVA:OjJwMzDuUS=> M1fMe|I1QDlyNkWy
MCF7 cells NULkPG03S3m2b4TvfIlkyqCjc4PhfS=> M2CweGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGVTNXCxc3n0bZZmKE2FRkegZ4VtdHNuIFnDOVA:OjdwMTDuUS=> MlrsNlQ5QTB4NUK=
human CGTH-W-1 cell NEHrdIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvs[3NKdmirYnn0bY9vKG:oIHj1cYFvKEOJVFitW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzBwOUSgcm0> NFfD[IdUSU6JRWK=
human MONO-MAC-6 cell MonGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG1QVk9vTVHDMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy56IH7N NU\OU|hYW0GQR1XS
human HL60 cells MX\DfZRwfG:6aXRCpIF{e2G7 MoW0OFghcA>? NEi5SoJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9N|YvQCCwTR?= MUOyOVA5QThzMB?=
human TT cells NGC3b4NRem:uaX\ldoF1cW:wIHHzd4F6 MWq3NkBp MkTKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWVDDj[YxteyCycnX0doVifGWmIH\vdkA4OiCqcoOg[o9tdG:5ZXSgZpkh[2:vcH;1coQuf2G|aH;1eEBu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSwJI5O NHPvPJMzPDlyNEm2NS=>
human THP1 cells NUL1e4h[S3m2b4TvfIlkyqCjc4PhfS=> NX;xVHZ3PDhiaB?= NUTQTJNxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2Njdibl2= MX[yOVA5QThzMB?=
3T3 cells NVLuPW9{TnWwY4Tpc44h[XO|YYm= MoKxTY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKGmwIEPUN{Bk\WyuczygTWM2OD13MDDuUS=> NWLMfXJWOTJ4NE[wNVk>
human ALL-PO cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{fiSGlvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|kvQDlibl2= MXjTRW5ITVJ?
human SH-SY5Y cells MX\GeY5kfGmxbjDhd5NigQ>? MnjjTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iU1itV3k2YSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVA:QDNwMTDuUS=> MWmyOFg6ODZ3Mh?=
human U251 cells MkHtSpVv[3Srb36gZZN{[Xl? M2O0S|YxKG2rboO= MlizTY5pcWKrdHnvckBw\iCSRFfGVk1j\XSjIHnuJIh2dWGwIGWyOVEh[2WubIOgZ49ueG:3bnSgdJJmfHKnYYTl[EBnd3JiNkCgcYlvKGKnZn;y[UBRTEeILVLCJJN1cW23bHH0bY9vKG[xcjCxNEBucW6|IHL5JJBpd3OyaH;0fZJwe2mwZTDFUGlUSSCleYTvZoxwfCCvZYToc4QtKEmFNUC9PFMvOSCwTR?= Mn23NlU5QDJ3MUm=
human NKM-1 cell NGLsSZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fOfWlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25PE42OiCwTR?= MYrTRW5ITVJ?
human HAEC cells M4XhOnBzd2yrZnXyZZRqd25iYYPzZZk> MWW3NkBp MlG4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQVXDJINmdGy|IHX4dJJme3OrbnegWmVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjFizszN MUmyNlQ1PDZ5OR?=
HUVEC cell MYXGeY5kfGmxbjDhd5NigQ>? NF[2UoQzPCCq NYDWdoNFUW6qaXLpeIlwdiCxZjDWSWdHNUFiaX7keYNm\CCKVW\FR{Bk\WyuIIPwdo92fGmwZzDh[pRmeiB{NDDodpMh[nliYX7nbY9o\W6nc3nzJIF{e2G7LDDJR|UxRTBwMUKg{txO NWi1eJlZOjF5NEGyOFk>
human A431 cells MV3GeY5kfGmxbjDhd5NigQ>? M4DMWVYxKG2rboO= NWrqZ495UW6qaXLpeIlwdiCxZjDFS2ZTKGmwIHj1cYFvKEF2M{GgZ4VtdHNiY3;tdI92dmRicILleJJm[XSnZDDmc5IhPjBibXnuJIJm\m:{ZTDFS2Yhe3SrbYXsZZRqd25iZn;yJFExKG2rboOgZpkheGixc4Doc5R6em:|aX7lJGVNUVODIHP5eI9jdG:2IH3leIhw\CxiSVO1NF0yPzJwMTDuUS=> M2f3dFI2QDh{NUG5
Sf9 cells MUjGeY5kfGmxbjDhd5NigQ>? NF3KSlFKdmirYnn0bY9vKG:oIFfTWE11[WepZXSgWmVITlJiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{whUUN3ME2wMlE5PSEQvF2= NXHJOI14OTl6NUSwOVE>
human HT-29 cells NHv2TJNRem:uaX\ldoF1cW:wIHHzd4F6 NFj3cW04OiCq M3nNZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOg[ZhxemW|c3nu[{BXTUeIUjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G778{MJGlEPTB;MD6zN{DPxE1? NFHWcpczOjR2NE[3PS=>
human KM12 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TXeGlvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|UxOTRizszN NWHZbYtSW0GQR1XS
human TE-15 cell M3PiS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIjrcFNKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42ODd4MTFOwG0> NHrH[3lUSU6JRWK=
human 697 cell NU\ofFRMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTPRpFKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlE1OjVizszN MmO1V2FPT0WU
human CAKI-1 cells M4i0WHBzd2yrZnXyZZRqd25iYYPzZZk> MkHYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQVvJMVEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1yLk[zJO69VQ>? MWiyNlU3ODZ{Nx?=
human MOLT-16 cell NV3tdYt1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFPhRZhKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ|MUOyJO69VQ>? NGXLUYNUSU6JRWK=
human GB-1 cell NWH5e3h5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXq1NYdKUW6qaXLpeIlwdiCxZjDoeY1idiCJQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OTB{MzFOwG0> NFfwdnZUSU6JRWK=
human TE-12 cell MlP2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{PBdWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgxPDV3IN88US=> NYfwZWJrW0GQR1XS
human NCI-H3122 cells Ml7uVJJwdGmoZYLheIlwdiCjc4PhfS=> MX63NkBp M{\1RWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE45OyEQvF2= NYDMVY9qOjR7MES5OlE>
human ES6 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHifItGUW6qaXLpeIlwdiCxZjDoeY1idiCHU{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk5OTB4IN88US=> M4n0WHNCVkeHUh?=
human NCI-H526 cells NWLvc|h3WHKxbHnm[ZJifGmxbjDhd5NigQ>? NW\MO4JIPzJiaB?= NIPITJFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4xOSEQvF2= NHuzZnYzPDlyNEm2NS=>
human LC-2-ad cell MnLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk[1TY5pcWKrdHnvckBw\iCqdX3hckBNSy1{LXHkJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTRyNzFOwG0> NH;jWYNUSU6JRWK=
human BL-70 cell M2W4TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlXlTY5pcWKrdHnvckBw\iCqdX3hckBDVC15MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNVE5PDZizszN M3jVbXNCVkeHUh?=
human ETK-1 cell NWXiXGtDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjlZVZKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zQDV6IN88US=> MoOxV2FPT0WU
human SW620 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 Mnq4OFghcA>? M4fob2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1zLkOg{txO NX7EflljOjJ3NkC2Nlc>
IM9 cells MoXBR5l1d3SxeHnjxsBie3OjeR?= NUfuZmZzS3m2b4TvfIlkcXS7IHHnZYlve3RiSH;tc{B{[XCrZX7zJEhpfW2jbjmgTW06KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1zLkO1JO69VQ>? NVTZ[Y46W0GQR1XS
human A4-Fuk cell NXL4XY8{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUHJUINQUW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTFwM{SxOFEh|ryP NXHXeHB3W0GQR1XS
human SR cell M3zub2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWPNVYNFUW6qaXLpeIlwdiCxZjDoeY1idiCVUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVQ2PzJizszN NHrY[IVUSU6JRWK=
human A3-KAW cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo\zTY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhcWN3ME2xMlYzPTR4IN88US=> MXjTRW5ITVJ?
human KS-1 cell NU\QephPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF;w[VNKdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY6OjR5IN88US=> NUXjXYxIW0GQR1XS
human CTV-1 cell NX\RVYtHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUPzc256UW6qaXLpeIlwdiCxZjDoeY1idiCFVG[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzJ5NUGg{txO NWqycIZlW0GQR1XS
human LB1047-RCC cell MnXmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKGi3bXHuJGxDOTB2Nz3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjhzNkK0JO69VQ>? Ml7RV2FPT0WU
human MEG-01 cell M4nqTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NITyXGJKdmirYnn0bY9vKG:oIHj1cYFvKE2HRz2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDN3NkOg{txO MonDV2FPT0WU
human TE-11 cell NY\EfnpQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYfJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64N|k5PSEQvF2= NYTRVZZPW0GQR1XS
human CMK cell M1HRZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzJcXd4UW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2PTF5IN88US=> NYjrfWxuW0GQR1XS
human NB1 cell Mn3JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJG5DOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOU[xNVch|ryP NXWyfpo2W0GQR1XS
human MDA-MB-435 cells NWD3UmFXWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml\5OFghcA>? M4rZdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCJSU2yJO69VQ>? MUCyNlU3ODZ{Nx?=
human MCF7 cells M2Hxb3Bzd2yrZnXyZZRqd25iYYPzZZk> NGLLXlY1QCCq NHviO4RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1{IN88US=> MYmyNlU3ODZ{Nx?=
human A549 cells MVjDfZRwfG:6aXRCpIF{e2G7 M4rKWVczKGh? NVTNN3dTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJwNESg{txO MV[yN|YxOjR2MR?=

... 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(C)[NH]C(=C1C)/C=C/2C(=O)NC3=C2C=C(F)C=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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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    C8=C7/X C8: LOG(C8):
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 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

Tel: +1-832-582-8158 Ext:3

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PDGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID