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 58 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 MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHNYPzV4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNVM2OSEQvF2= NWXxbGdFW0GQR1XS
human EoL-1-cell cell NIm3d3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3LXS2lvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNkTlMVA3 Ml[yV2FPT0WU
human MV-4-11 cell MkPPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\xVopKdmirYnn0bY9vKG:oIHj1cYFvKE2YLUStNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ5MjDuUS=> NVvIeHV7W0GQR1XS
human MV411 cells NFXuOVRRem:uaX\ldoF1cW:wIHHzd4F6 MWq0PEBp MmrZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= M{PPU|I1QTB2OU[x
3T3 cells NUDiWHlNTnWwY4Tpc44h[XO|YYm= Mnn2TY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJIlvKDOWMzDj[YxteyC5aYToJFAvOSViYn;2bY5mKHOncoXtJIFt[nWvaX6sJGlEPTB;NzDuUS=> NH7FdYMyOjZ2NkCxPS=>
HEK293 cells M{f4R2Z2dmO2aX;uJIF{e2G7 M3r5[mJqdmSrbnegZYZncW6rdImgeI8hTkyWMzDjZZRidHm2aXOg[I9u[WmwIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomgZ49ueGW2aYTpeoUh[mmwZHnu[{Bie3OjeTygT4Q:OC52NzDuUS=> MYGxPVc2PDF7OR?=
human MDA-MB-435 cells NFTodnVEgXSxdH;4bYPDqGG|c3H5 NETXcYczKGh? NVXpOGdUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{whUUN3ME25Mlchdk1? MVyyOFg6ODZ3Mh?=
human RS4-11 cells MljISpVv[3Srb36gZZN{[Xl? NI\ZVJFKdmirYnn0bY9vKG:oIF\MWFMh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCUU{StNVEh[2WubIOgZYZ1\XJiMjDodpMh[nliZXzlZ5Rzd2OqZX3pcJVucW6nc3PlcoNmKGG|c3H5MEBKSzVyPUmuPUBvVQ>? MYmxPVY2PDRyOB?=
HUVEC M{XP[mN6fG:2b4jpZ:Kh[XO|YYm= MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzygTWM2OD1zMT64JI5O MlOzNlQ5QTB4NUK=
human Kasumi-1 cells NFLs[npHfW6ldHnvckBie3OjeR?= NUDSZmU5UW6qaXLpeIlwdiCxZjDjMWtqfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvhd5VucS1zIHPlcIx{KGK7IGfld5Rmem5iYnzveEBidmGueYPpd{whUUN3ME2xOUBvVQ>? MlL4NlA5OzNyM{m=
human NOS-1 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\LTWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4{KG6P M{LyWXNCVkeHUh?=
mouse triple negative 4T1 cells MX3DfZRwfG:6aXRCpIF{e2G7 M2fsSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJJRzcXCuZTDu[YdifGm4ZTC0WFEh[2WubIOsJGlEPTB;MU[gcm0> M{HZdVI1QDlyNkWy
human RS4-11 cells M{DRT2Z2dmO2aX;uJIF{e2G7 MWLJcohq[mm2aX;uJI9nKE[OVEOgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBTWzRvMUGgZ4VtdHNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE3KG6P MV6yNFg{OzB|OR?=
human MOLM13 cells NG\vcJlEgXSxdH;4bYPDqGG|c3H5 M3vEe2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1QVE1zMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE4Njdibl2= M2SyblI2ODh7OEGw
human U251 cells MYfGeY5kfGmxbjDhd5NigQ>? MofETY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2EtKEmFNUC9NVgvQSCwTR?= NYjPeYJtOjR7MEC4OlU>
NIH3T3 cells MYDGeY5kfGmxbjDhd5NigQ>? MWCxJIg> NFHhcGVKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiCNRGKgb4lv[XOnIHX4dJJme3OnZDDpckBPUUh|VEOgZ4VtdHNid3n0bEA1KHWPIFLpc5Rqdi2DaIitRWVGTVmIRlzGRU1idWmmZTDheEBidWKrZX70JJRmdXCncnH0eZJmKG[xcjCxJIhz M3vjRlE3OTZ{MEC4
MDA-MB-231 cells MX\DfZRwfG:6aXRCpIF{e2G7 M1L1PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJRzcXCuZTDu[YdifGm4ZTDNSGEuVUJvMkOxJINmdGy|LDDJR|UxRTJ{LkOgcm0> MnrvNlQ5QTB4NUK=
MCF7 cells MXHDfZRwfG:6aXRCpIF{e2G7 NXLpU3d7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTVJvcH;zbZRqfmViTVPGO{Bk\WyuczygTWM2OD1{Nz6xJI5O NE\Pc44zPDh7ME[1Ni=>
human CGTH-W-1 cell M2rYemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvQTRibl2= MVjTRW5ITVJ?
human MONO-MAC-6 cell M3ztSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm[2TY5pcWKrdHnvckBw\iCqdX3hckBOV06RLV3BR{03KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwODDuUS=> Mn3jV2FPT0WU
human HL60 cells NVvreZgzS3m2b4TvfIlkyqCjc4PhfS=> NXnXeWNiPDhiaB?= MnnxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUO2Mlghdk1? NIf1[VMzPTB6OUixNC=>
human TT cells Ml:2VJJwdGmoZYLheIlwdiCjc4PhfS=> MV23NkBp NXTHdGI1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUWEBk\WyuczDwdoV1emWjdHXkJIZweiB5MjDodpMh\m:ubH;3[YQh[nliY3;tdI92dmRvd3HzbI92fCCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQxKG6P NUDBcYFsOjR7MES5OlE>
human THP1 cells NInxc3BEgXSxdH;4bYPDqGG|c3H5 NV\LbGk6PDhiaB?= NXvEN5hJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2Njdibl2= Mkj6NlUxQDl6MUC=
3T3 cells M4GzNWZ2dmO2aX;uJIF{e2G7 Mn7JTY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKGmwIEPUN{Bk\WyuczygTWM2OD13MDDuUS=> MmPzNVI3PDZyMUm=
human ALL-PO cell M3TlZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHJT4FKUW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04QS56OTDuUS=> NYm5fFE5W0GQR1XS
human SH-SY5Y cells MWPGeY5kfGmxbjDhd5NigQ>? M3PxZ2lvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[nlicHjvd5Bpd3S7cn;zbY5mKEWOSWPBJIF{e2G7LDDJR|UxRTh|LkGgcm0> NWjLNmpJOjR6OUC2OVI>
human U251 cells M2THVGZ2dmO2aX;uJIF{e2G7 NWrabY04PjBibXnudy=> MYLJcohq[mm2aX;uJI9nKFCGR1\SMYJmfGFiaX6gbJVu[W5iVUK1NUBk\WyuczDjc41xd3WwZDDwdoV1emWjdHXkJIZweiB4MDDtbY4h[mWob4LlJHBFT0ZvQlKgd5RqdXWuYYTpc44h\m:{IEGwJI1qdnNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCKGO7dH;icI91KG2ndHjv[EwhUUN3ME24N{4yKG6P NX:wNnRiOjV6OEK1NVk>
human NKM-1 cell M13EXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH\SW2lKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVgvPTJibl2= M4TlT3NCVkeHUh?=
human HAEC cells M1OybXBzd2yrZnXyZZRqd25iYYPzZZk> M{jjZlczKGh? NFyzOphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjBSWMh[2WubIOg[ZhxemW|c3nu[{BXTUeIUjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMTFOwG0> NH:xOJczOjR2NE[3PS=>
HUVEC cell MXLGeY5kfGmxbjDhd5NigQ>? NGnjWWYzPCCq MXLJcohq[mm2aX;uJI9nKF[HR1[tRUBqdmS3Y3XkJGhWXkWFIHPlcIwhe3C{b4X0bY5oKGGodHXyJFI1KGi{czDifUBidmerb3flcoV{cXNiYYPzZZktKEmFNUC9NE4yOiEQvF2= NVK2d3UyOjF5NEGyOFk>
human A431 cells NXK3bWpCTnWwY4Tpc44h[XO|YYm= MmTlOlAhdWmwcx?= MX7Jcohq[mm2aX;uJI9nKEWJRmKgbY4hcHWvYX6gRVQ{OSClZXzsd{Bkd22yb4Xu[EBxemW2cnXheIVlKG[xcjC2NEBucW5iYnXmc5JmKEWJRjDzeIlufWyjdHnvckBnd3JiMUCgcYlveyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2Eh[3m2b3Lsc5QhdWW2aH;kMEBKSzVyPUG3Nk4yKG6P MUOyOVg5OjVzOR?=
Sf9 cells M2ft[mZ2dmO2aX;uJIF{e2G7 M4DTcWlvcGmkaYTpc44hd2ZiR2PUMZRi\2enZDDWSWdHWiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNVg2KM7:TR?= MlP6NVk5PTRyNUG=
human HT-29 cells MkD6VJJwdGmoZYLheIlwdiCjc4PhfS=> MofrO|IhcA>? MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHX4dJJme3OrbnegWmVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5Nige,:jDDJR|UxRTBwM{Og{txO MVuyNlQ1PDZ5OR?=
human KM12 cell M4DrUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH\JRVBKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2ODF2IN88US=> M2LkVXNCVkeHUh?=
human TE-15 cell M2T1Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{DwU2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxPzZzIN88US=> MmXxV2FPT0WU
human 697 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIS1TZlKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlE1OjVizszN MnTSV2FPT0WU
human CAKI-1 cells M2PpbHBzd2yrZnXyZZRqd25iYYPzZZk> NWLuNYxbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDRWtKNTFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlY{KM7:TR?= MmXaNlI2PjB4Mke=
human MOLT-16 cell NGjMVVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDUS2tKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ|MUOyJO69VQ>? NX\ncVhVW0GQR1XS
human GB-1 cell NUfhUIs3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\3N5NKUW6qaXLpeIlwdiCxZjDoeY1idiCJQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OTB{MzFOwG0> M4e5OXNCVkeHUh?=
human TE-12 cell M4LqTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{H0e2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgxPDV3IN88US=> M3XpSXNCVkeHUh?=
human NCI-H3122 cells Mn[2VJJwdGmoZYLheIlwdiCjc4PhfS=> MXO3NkBp MlnCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg{KM7:TR?= NH7oUWIzPDlyNEm2NS=>
human ES6 cell MoLFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILuWnBKdmirYnn0bY9vKG:oIHj1cYFvKEWVNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVgyODZizszN NGK3R|BUSU6JRWK=
human NCI-H526 cells MnL4VJJwdGmoZYLheIlwdiCjc4PhfS=> MnHjO|IhcA>? M1XPOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg2OjZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlAyKM7:TR?= NGr2VHEzPDlyNEm2NS=>
human LC-2-ad cell NGTW[W9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnjNmZoUW6qaXLpeIlwdiCxZjDoeY1idiCOQz2yMYFlKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5zMUSwO{DPxE1? MV7TRW5ITVJ?
human BL-70 cell MnLUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2TEUGlvcGmkaYTpc44hd2ZiaIXtZY4hSkxvN{CgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlEyQDR4IN88US=> NI\JVI1USU6JRWK=
human ETK-1 cell NWq1TW1{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF23T5BKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zQDV6IN88US=> MYnTRW5ITVJ?
human SW620 cells M3XBe3Bzd2yrZnXyZZRqd25iYYPzZZk> MVS0PEBp M1fwVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1zLkOg{txO NULpbI5VOjJ3NkC2Nlc>
IM9 cells MXvDfZRwfG:6aXRCpIF{e2G7 MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBJd22xIIPhdIlmdnNiKHj1cYFvMSCLTUmgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZpkhVVSWIHHzd4F6NCCLQ{WwQVEvOzVizszN NX\m[JZEW0GQR1XS
human A4-Fuk cell NECxWohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2rlVmlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjN2MUSxJO69VQ>? M13xe3NCVkeHUh?=
human SR cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{nZS2lvcGmkaYTpc44hd2ZiaIXtZY4hW1JiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW0OVczKM7:TR?= NWPhUGFNW0GQR1XS
human A3-KAW cell NImze2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIPPNIpKdmirYnn0bY9vKG:oIHj1cYFvKEF|LVvBW{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCrY{WwQVEvPjJ3NE[g{txO MYLTRW5ITVJ?
human KS-1 cell MkfUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2nTbWlvcGmkaYTpc44hd2ZiaIXtZY4hU1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlkzPDdizszN MkXtV2FPT0WU
human CTV-1 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVP3eW5ZUW6qaXLpeIlwdiCxZjDoeY1idiCFVG[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzJ5NUGg{txO MmTKV2FPT0WU
human LB1047-RCC cell NX:yT457T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXXSGtUUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64NVYzPCEQvF2= M4P5enNCVkeHUh?=
human MEG-01 cell NILuTGxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXW3[GxKUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjh|NU[zJO69VQ>? M3\6SnNCVkeHUh?=
human TE-11 cell M3[3[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEL5[VdKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU45Ozl6NTFOwG0> MWrTRW5ITVJ?
human CMK cell Mn7vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUW1NVch|ryP NVHVWlhkW0GQR1XS
human NB1 cell NHLYfpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojDTY5pcWKrdHnvckBw\iCqdX3hckBPSjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkm2NVE4KM7:TR?= NInIc3lUSU6JRWK=
human MDA-MB-435 cells NFHWOlBRem:uaX\ldoF1cW:wIHHzd4F6 NF;KOYs1QCCq NUK3VY1jSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJQVIh|ryP MXWyNlU3ODZ{Nx?=
human MCF7 cells MkPuVJJwdGmoZYLheIlwdiCjc4PhfS=> M3nYVVQ5KGh? MnHLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJOVA:OiEQvF2= M2K1cFIzPTZyNkK3
human A549 cells NHnwOVBEgXSxdH;4bYPDqGG|c3H5 MV63NkBp NWTrXIlSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJwNESg{txO MVyyN|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]

+ 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:

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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The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID