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 42 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 Ml7YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1f3N2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d5NU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU4yOzVzIN88US=> Mmj4V2FPT0WU
human EoL-1-cell cell NWHERnU4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml\wTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS54NHWtNFY> NVvaPZd5W0GQR1XS
human MV-4-11 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MorkTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPzJibl2= MYTTRW5ITVJ?
human MV411 cells NXXLfppqWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGqxVng1QCCq MmPIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= MX6yOFkxPDl4MR?=
3T3 cells M2\4bWZ2dmO2aX;uJIF{e2G7 NFnsUlhKdmirYnn0bY9vKG:oIGDES2YucW6mdXPl[EBDemSXIHnuZ49zeG:{YYTpc44hcW5iM2SzJINmdGy|IIfpeIghOC5zJTDic5ZqdmVic3XyeY0h[WykdX3pckwhUUN3ME23JI5O M{LkNlEzPjR4MEG5
HEK293 cells NY\0R5d6TnWwY4Tpc44h[XO|YYm= MYrCbY5lcW6pIHHm[olvcXS7IITvJGZNXDNiY3H0ZYx6fGmlIHTvcYFqdiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGK7IHPvcZBmfGm2aY\lJIJqdmSrbnegZZN{[XluIFvkQVAvPDdibl2= NUPZcWg5OTl5NUSxPVk>
human MDA-MB-435 cells M3TmeWN6fG:2b4jpZ:Kh[XO|YYm= MmXpNkBp NYTwSnptS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{whUUN3ME25Mlchdk1? M{LkSFI1QDlyNkWy
human RS4-11 cells Ml:3SpVv[3Srb36gZZN{[Xl? MlziTY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hWlN2LUGxJINmdGy|IHHmeIVzKDJiaILzJIJ6KGWuZXP0do9kcGWvaXz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD17Lkmgcm0> M{XXSlE6PjV2NEC4
HUVEC MkmyR5l1d3SxeHnjxsBie3OjeR?= Mo\hR5l1d3SxeHnjbZR6KGGpYXnud5QhUFWYRVOsJGlEPTB;MUGuPEBvVQ>? NYLhOlBuOjR6OUC2OVI>
human Kasumi-1 cells NVrUZ2V5TnWwY4Tpc44h[XO|YYm= NGT6TlZKdmirYnn0bY9vKG:oIHOtT4l1KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iS3HzeY1qNTFiY3XscJMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBKSzVyPUG1JI5O NIq4WGkzODh|M{CzPS=>
human NOS-1 cell M{fDPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuN{BvVQ>? M1TvcHNCVkeHUh?=
mouse triple negative 4T1 cells M2rVXGN6fG:2b4jpZ:Kh[XO|YYm= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTD0dolxdGVibnXnZZRqfmViNGSxJINmdGy|LDDJR|UxRTF4IH7N M4jyWlI1QDlyNkWy
human RS4-11 cells MXLGeY5kfGmxbjDhd5NigQ>? MlHKTY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hWlN2LUGxJINmdGy|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPiCwTR?= M2LuZVIxQDN|MEO5
human MOLM13 cells MoLjR5l1d3SxeHnjxsBie3OjeR?= NWS2[mE3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVU:OTUGzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTdwNzDuUS=> MWWyOVA5QThzMB?=
human U251 cells NH;yOHFHfW6ldHnvckBie3OjeR?= MoHITY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2EtKEmFNUC9NVgvQSCwTR?= MoniNlQ6ODB6NkW=
NIH3T3 cells NX\PRWtETnWwY4Tpc44h[XO|YYm= NIH1PYUyKGh? MnrrTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4hU0SUIHvpcoF{\SCneIDy[ZN{\WRiaX6gUmlJO1R|IHPlcIx{KHerdHigOEB2VSCEaX;0bY4uSWi6LVHFSWV[Tk[ORlGtZY1q\GViYYSgZY1jcWWwdDD0[Y1x\XKjdIXy[UBnd3JiMTDodi=> MknNNVYyPjJyMEi=
MDA-MB-231 cells NGTLWWxEgXSxdH;4bYPDqGG|c3H5 NGTmUmhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckB1emmybHWgcoVo[XSrdnWgUWRCNU2ELUKzNUBk\WyuczygTWM2OD1{Mj6zJI5O Mn7UNlQ5QTB4NUK=
MCF7 cells NUH5cY1lS3m2b4TvfIlkyqCjc4PhfS=> NFHSe5dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBGWi2yb4PpeIl3\SCPQ1[3JINmdGy|LDDJR|UxRTJ5LkGgcm0> M2PvUlI1QDlyNkWy
human CGTH-W-1 cell MlrLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHvTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjl2IH7N NXfQfZhtW0GQR1XS
human MONO-MAC-6 cell MmDQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnXVTY5pcWKrdHnvckBw\iCqdX3hckBOV06RLV3BR{03KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwODDuUS=> MkPKV2FPT0WU
human HL60 cells NYC4O2I4S3m2b4TvfIlkyqCjc4PhfS=> NHqwVGk1QCCq M2fLcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2zOk45KG6P NFTW[VgzPTB6OUixNC=>
human TT cells MontVJJwdGmoZYLheIlwdiCjc4PhfS=> M{DucVczKGh? NILoOlRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTUJINmdGy|IIDy[ZRz\WG2ZXSg[o9zKDd{IHjyd{Bnd2yub4fl[EBjgSClb33wc5Vv\C25YYPoc5V1KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? MlvNNlQ6ODR7NkG=
human THP1 cells NV7wNFlGS3m2b4TvfIlkyqCjc4PhfS=> NEHuSWM1QCCq NYrKdFlYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2Njdibl2= MVuyOVA5QThzMB?=
3T3 cells M{LTb2Z2dmO2aX;uJIF{e2G7 M4TxXmlvcGmkaYTpc44hd2ZiVnHzZ5Vt[XJiZX7kc5Rp\WyrYXyg[5Jwf3SqIH\hZ5RweiC{ZXPldJRweiCrbjCzWFMh[2WubIOsJGlEPTB;NUCgcm0> Mkn2NVI3PDZyMUm=
human ALL-PO cell M4LFRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4G0[2lvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|kvQDlibl2= MUPTRW5ITVJ?
human SH-SY5Y cells Mn3vSpVv[3Srb36gZZN{[Xl? MmG1TY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iU1itV3k2YSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVA:QDNwMTDuUS=> MnvLNlQ5QTB4NUK=
human U251 cells M1jJfGZ2dmO2aX;uJIF{e2G7 M17PeVYxKG2rboO= MV7Jcohq[mm2aX;uJI9nKFCGR1\SMYJmfGFiaX6gbJVu[W5iVUK1NUBk\WyuczDjc41xd3WwZDDwdoV1emWjdHXkJIZweiB4MDDtbY4h[mWob4LlJHBFT0ZvQlKgd5RqdXWuYYTpc44h\m:{IEGwJI1qdnNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCKGO7dH;icI91KG2ndHjv[EwhUUN3ME24N{4yKG6P M4fmc|I2QDh{NUG5
human NKM-1 cell NGPLOJhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFPsVoRKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVgvPTJibl2= M3vmfXNCVkeHUh?=
human HAEC cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 Ml\FO|IhcA>? Mn7QRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQVXDJINmdGy|IHX4dJJme3OrbnegWmVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjFizszN M3nOV|IzPDR2Nke5
HUVEC cell M4fNS2Z2dmO2aX;uJIF{e2G7 MWWyOEBp MkLRTY5pcWKrdHnvckBw\iCYRVfGMWEhcW6mdXPl[EBJXV[HQzDj[YxtKHOycn;1eIlv\yCjZoTldkAzPCCqcoOgZpkh[W6paX;n[Y5me2m|IHHzd4F6NCCLQ{WwQVAvOTJizszN MUKyNVc1OTJ2OR?=
human A431 cells MXnGeY5kfGmxbjDhd5NigQ>? MWW2NEBucW6| NIfwPYZKdmirYnn0bY9vKG:oIFXHSnIhcW5iaIXtZY4hSTR|MTDj[YxteyClb33wc5Vv\CCycnX0doVifGWmIH\vdkA3OCCvaX6gZoVnd3KnIFXHSkB{fGmvdXzheIlwdiCob4KgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RibXX0bI9lNCCLQ{WwQVE4Oi5zIH7N M3Swc|I2QDh{NUG5
Sf9 cells Mo[1SpVv[3Srb36gZZN{[Xl? M1LqcWlvcGmkaYTpc44hd2ZiR2PUMZRi\2enZDDWSWdHWiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNVg2KM7:TR?= M4\MS|E6QDV2MEWx
human HT-29 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 Mln4O|IhcA>? NF75b2NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIV5eHKnc4PpcochXkWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3Ojef-8kEBKSzVyPUCuN|Mh|ryP MXGyNlQ1PDZ5OR?=
human KM12 cell NGm5OotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1S3T2lvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|UxOTRizszN NXHVfpdLW0GQR1XS
human TE-15 cell NIDZRYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61NFc3OSEQvF2= M1vwb3NCVkeHUh?=
human 697 cell NXvxWZFDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF[zWJJKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlE1OjVizszN NX7aeVFvW0GQR1XS
human CAKI-1 cells NXP0emFYWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYXrR3AySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDRWtKNTFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlY{KM7:TR?= MYOyNlU3ODZ{Nx?=
human MOLT-16 cell NUPDSnVIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUfZTFZmUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54M{GzNkDPxE1? M17u[XNCVkeHUh?=
human GB-1 cell NW\yfIVwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NY\wVJpzUW6qaXLpeIlwdiCxZjDoeY1idiCJQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OTB{MzFOwG0> MlHNV2FPT0WU
human TE-12 cell MmHlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4T0[GlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgxPDV3IN88US=> M3izb3NCVkeHUh?=
human NCI-H3122 cells NUj0RW1MWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV63NkBp NEn5[YxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvQDNizszN NYTLW2poOjR7MES5OlE>
human ES6 cell M3fqdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPRSG9kUW6qaXLpeIlwdiCxZjDoeY1idiCHU{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk5OTB4IN88US=> MoC2V2FPT0WU
human NCI-H526 cells M3vGSnBzd2yrZnXyZZRqd25iYYPzZZk> NHzadIc4OiCq NUDlbmh2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDV{NjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvODFizszN MXeyOFkxPDl4MR?=
human LC-2-ad cell NFe3TVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHfITJFKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUKtZYQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjFzNEC3JO69VQ>? M3;Ec3NCVkeHUh?=
human BL-70 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEnjZVhKdmirYnn0bY9vKG:oIHj1cYFvKEKOLUewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTh2NjFOwG0> MnvGV2FPT0WU
human ETK-1 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWLMSXlnUW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjh3ODFOwG0> NVLRR4RVW0GQR1XS
human SW620 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 MojUOFghcA>? M4PiOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1zLkOg{txO NV7icGUxOjJ3NkC2Nlc>
IM9 cells NIjOPIdEgXSxdH;4bYPDqGG|c3H5 NH\MTG9EgXSxdH;4bYNqfHliYXfhbY5{fCCKb33vJJNieGmnboOgLIh2dWGwKTDJUVkh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[nliTWTUJIF{e2G7LDDJR|UxRTFwM{Wg{txO NFXOR3NUSU6JRWK=
human A4-Fuk cell MoTYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H589yNKEmFNUC9NU4{PDF2MTFOwG0> NUnPUohkW0GQR1XS
human SR cell NGS5dWJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWO5fXBCUW6qaXLpeIlwdiCxZjDoeY1idiCVUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVQ2PzJizszN MmL0V2FPT0WU
human A3-KAW cell M17HfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3lR4pYUW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiaXO1NF0yNjZ{NUS2JO69VQ>? MlLhV2FPT0WU
human KS-1 cell M{\RZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHac2ZOUW6qaXLpeIlwdiCxZjDoeY1idiCNUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43QTJ2NzFOwG0> NGq1VZFUSU6JRWK=
human CTV-1 cell MmPsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4T6TWlvcGmkaYTpc44hd2ZiaIXtZY4hS1SYLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlczPzVzIN88US=> NVvyOItnW0GQR1XS
human LB1047-RCC cell M161Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWD4XFF{UW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64NVYzPCEQvF2= MVnTRW5ITVJ?
human MEG-01 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1jKW2lvcGmkaYTpc44hd2ZiaIXtZY4hVUWJLUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU45OzV4MzFOwG0> MnnMV2FPT0WU
human TE-11 cell NXj5Spp3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MknDTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFM6QDVizszN NUXqNoJtW0GQR1XS
human CMK cell M1L5dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXEd4xuUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2PTF5IN88US=> MkjHV2FPT0WU
human NB1 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NG\qeJFKdmirYnn0bY9vKG:oIHj1cYFvKE6EMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVYyOTdizszN M{\nO3NCVkeHUh?=
human MDA-MB-435 cells NYjuXGQ3WHKxbHnm[ZJifGmxbjDhd5NigQ>? M1nOUlQ5KGh? NYHpbYFvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJQVIh|ryP NUPaRm5QOjJ3NkC2Nlc>
human MCF7 cells M1fLVHBzd2yrZnXyZZRqd25iYYPzZZk> MVK0PEBp NUXYcldnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTB;MjFOwG0> M3y2dFIzPTZyNkK3
human A549 cells NFPIeFNEgXSxdH;4bYPDqGG|c3H5 NF;lWVA4OiCq MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9Nk41PCEQvF2= MV:yN|YxOjR2MR?=

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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

Molarity Calculator

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

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Dilution Calculator

Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03862768 Not yet recruiting Gastrointestinal Stromal Tumors|Surgery Shanghai Zhongshan Hospital July 2019 Not Applicable
NCT03862768 Not yet recruiting Gastrointestinal Stromal Tumors|Surgery Shanghai Zhongshan Hospital July 2019 Not Applicable
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03673501 Recruiting Gastrointestinal Stromal Tumors Deciphera Pharmaceuticals LLC February 11 2019 Phase 3
NCT03641326 Recruiting Gliosarcoma|Central Nervous System Sarcoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 21 2019 Phase 2

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