Sunitinib

For research use only. Not for use in humans.

目录号:S7781 别名: SU11248

Sunitinib Chemical Structure

CAS No. 557795-19-4

Sunitinib (SU11248) 是一种多靶点 RTK 抑制剂,以VEGFR2(Flk-1)和PDGFRβ为靶点,IC50为80 nM 和 2 nM,对c-Kit也有抑制作用。Sunitinib 还是 IRE1α 的自磷酸化活性的剂量依赖性抑制剂。 舒尼替尼可诱导自噬和细胞凋亡。

规格 价格 库存 购买数量  
RMB 811.55 现货
RMB 1624.45 现货
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客户使用Selleck生产的Sunitinib发表文献118篇:

产品安全说明书

PDGFR抑制剂选择性比较

生物活性

产品描述 Sunitinib (SU11248) 是一种多靶点 RTK 抑制剂,以VEGFR2(Flk-1)和PDGFRβ为靶点,IC50为80 nM 和 2 nM,对c-Kit也有抑制作用。Sunitinib 还是 IRE1α 的自磷酸化活性的剂量依赖性抑制剂。 舒尼替尼可诱导自噬和细胞凋亡。
靶点
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
体外研究

Sunitinib能够有效抑制Kit 和FLT-3。[1] Sunitinib是VEGFR2 (Flk1) 和 PDGFRβ有效的ATP竞争性抑制剂,Ki分别为9 nM 和8 nM,作用于VEGFR2和 PDGFR比作用于FGFR-1,EGFR,Cdk2,Met,IGFR-1,Abl,和src选择性高10倍多。在血清饥饿的表达VEGFR2 或PDGFRβ的NIH-3T3细胞中,Sunitinib抑制VEGF依赖性VEGFR2磷酸化和PDGF依赖性PDGFRβ磷酸化,IC50分别为10 nM和10 nM。对于过表达PDGFRβ或PDGFRα的NIH-3T3细胞,Sunitinib抑制VEGF对其诱导的增殖,IC50 分别为39 nM和69 nM。[2] Sunitinib抑制野生型FLT3,FLT3-ITD,和FLT3-Asp835磷酸化,IC50分别为250 nM,50 nM,和30 nM。Sunitinib抑制MV4;11 和OC1-AML5细胞的增殖,IC50分别为8 nM和14 nM,并以剂量依赖的方式诱导细胞凋亡。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SW756 cell MnTES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4LXb2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d5NU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU4yOzVzIN88US=> MXXTRW5ITVJ?
human EoL-1-cell cell NVn4e2JTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjZ2ZT2wOi=> M1HnUnNCVkeHUh?=
human MV-4-11 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3u3ZmlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjd{IH7N Mk\QV2FPT0WU
human MV411 cells MWDQdo9tcW[ncnH0bY9vKGG|c3H5 NEnifYM1QCCq MoC3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= M2jtVFI1QTB2OU[x
3T3 cells MWPGeY5kfGmxbjDhd5NigQ>? M4G5dmlvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckBqdiB|VEOgZ4VtdHNid3n0bEAxNjFnIHLveolv\SC|ZYL1cUBidGK3bXnuMEBKSzVyPUegcm0> M2HlSVEzPjR4MEG5
HEK293 cells NF3wfHRHfW6ldHnvckBie3OjeR?= NGHzW|dDcW6maX7nJIFn\mmwaYT5JJRwKE[OVEOgZ4F1[Wy7dHnjJIRwdWGrbjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHL5JINwdXCndHn0bZZmKGKrbnTpcoch[XO|YYmsJGtlRTBwNEegcm0> NVnCOW1IOTl5NUSxPVk>
human MDA-MB-435 cells MmG5R5l1d3SxeHnjxsBie3OjeR?= M4PnPFIhcA>? M{TSNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGlEPTB;OT63JI5O M2[x[VI1QDlyNkWy
human RS4-11 cells M2fCNGZ2dmO2aX;uJIF{e2G7 NYLQNoFwUW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHXs[YN1em:laHXtbYx2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3ME25Mlkhdk1? NHLZc4syQTZ3NESwPC=>
HUVEC MorVR5l1d3SxeHnjxsBie3OjeR?= NU\ZOZBRS3m2b4TvfIlkcXS7IHHnZYlve3RiSGXWSWMtKEmFNUC9NVEvQCCwTR?= NEXs[VEzPDh7ME[1Ni=>
human Kasumi-1 cells NXnzUVEzTnWwY4Tpc44h[XO|YYm= MlnzTY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEujc4XtbU0yKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNTDuUS=> NYmx[WVMOjB6M{OwN|k>
human NOS-1 cell NEPmOIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuN{BvVQ>? NVzzSYFSW0GQR1XS
mouse triple negative 4T1 cells MYjDfZRwfG:6aXRCpIF{e2G7 NG\DN|VEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UB1emmybHWgcoVo[XSrdnWgOHQyKGOnbHzzMEBKSzVyPUG2JI5O MnTuNlQ5QTB4NUK=
human RS4-11 cells MWTGeY5kfGmxbjDhd5NigQ>? NX[4NItmUW6qaXLpeIlwdiCxZjDGUHQ{KGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iUmO0MVEyKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNjDuUS=> M1LqelIxQDN|MEO5
human MOLM13 cells NF3rS5FEgXSxdH;4bYPDqGG|c3H5 M2DMcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1QVE1zMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE4Njdibl2= MVqyOVA5QThzMB?=
human U251 cells M{n5emZ2dmO2aX;uJIF{e2G7 M4\LS2lvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKFV{NUGgZ4VtdHNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCNCCLQ{WwQVE5Njlibl2= NIH5O5UzPDlyMEi2OS=>
NIH3T3 cells NGi3eIFHfW6ldHnvckBie3OjeR?= M3T5ZVEhcA>? M{PPSmlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKEuGUjDrbY5ie2ViZYjwdoV{e2WmIHnuJG5KUDOWMzDj[YxteyC5aYToJFQhfU1iQnnveIlvNUGqeD3BSWVGYU[ITF\BMYFucWSnIHH0JIFu[mmnboSgeIVueGW{YYT1doUh\m:{IEGgbJI> MnHZNVYyPjJyMEi=
MDA-MB-231 cells NHLJc25EgXSxdH;4bYPDqGG|c3H5 MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjD0dolxdGVibnXnZZRqfmViTVTBMW1DNTJ|MTDj[YxteyxiSVO1NF0zOi5|IH7N MmrINlQ5QTB4NUK=
MCF7 cells M{fWZWN6fG:2b4jpZ:Kh[XO|YYm= MoGxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSXIueG:|aYTpeoUhVUOINzDj[YxteyxiSVO1NF0zPy5zIH7N NUnSVZpGOjR6OUC2OVI>
human CGTH-W-1 cell M{Xqb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEe4UppKdmirYnn0bY9vKG:oIHj1cYFvKEOJVFitW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzBwOUSgcm0> Mnr0V2FPT0WU
human MONO-MAC-6 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKGi3bXHuJG1QVk9vTVHDMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy56IH7N MWjTRW5ITVJ?
human HL60 cells MWrDfZRwfG:6aXRCpIF{e2G7 NFu0XIg1QCCq NIrJVpZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9N|YvQCCwTR?= M2jQVlI2ODh7OEGw
human TT cells NWDMdI85WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3vaV|czKGh? MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSWIHPlcIx{KHC{ZYTy[YF1\WRiZn;yJFczKGi{czDmc4xtd3enZDDifUBkd22yb4Xu[E14[XOqb4X0JI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NECgcm0> NFWyXlQzPDlyNEm2NS=>
human THP1 cells NXHmTplsS3m2b4TvfIlkyqCjc4PhfS=> MlS0OFghcA>? MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUTHAyKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NEWuO{BvVQ>? MXOyOVA5QThzMB?=
3T3 cells NEDpN21HfW6ldHnvckBie3OjeR?= NGi1OJBKdmirYnn0bY9vKG:oIG\hd4N2dGG{IHXu[I91cGWuaXHsJIdzd3e2aDDmZYN1d3JicnXj[ZB1d3JiaX6gN3Q{KGOnbHzzMEBKSzVyPUWwJI5O MXixNlY1PjBzOR?=
human ALL-PO cell M1HrZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWqyd3hGUW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04QS56OTDuUS=> NV;OSm9RW0GQR1XS
human SH-SY5Y cells NIfM[oVHfW6ldHnvckBie3OjeR?= NVLGRVh1UW6qaXLpeIlwdiCxZjDQSGdHWmKndHGgbY4hcHWvYX6gV2guW1l3WTDj[YxteyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2Eh[XO|YYmsJGlEPTB;OEOuNUBvVQ>? M{\aXlI1QDlyNkWy
human U251 cells MYrGeY5kfGmxbjDhd5NigQ>? MX[2NEBucW6| MX;Jcohq[mm2aX;uJI9nKFCGR1\SMYJmfGFiaX6gbJVu[W5iVUK1NUBk\WyuczDjc41xd3WwZDDwdoV1emWjdHXkJIZweiB4MDDtbY4h[mWob4LlJHBFT0ZvQlKgd5RqdXWuYYTpc44h\m:{IEGwJI1qdnNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCKGO7dH;icI91KG2ndHjv[EwhUUN3ME24N{4yKG6P MUGyOVg5OjVzOR?=
human NKM-1 cell NFPyN2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTSZWtKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVgvPTJibl2= NEf2Z3NUSU6JRWK=
human HAEC cells MmrEVJJwdGmoZYLheIlwdiCjc4PhfS=> MnexO|IhcA>? NY\1OHluSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIRWVEKGOnbHzzJIV5eHKnc4PpcochXkWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkGg{txO MXqyNlQ1PDZ5OR?=
HUVEC cell NF\P[XpHfW6ldHnvckBie3OjeR?= MoXJNlQhcA>? M1q4bWlvcGmkaYTpc44hd2ZiVlXHSk1CKGmwZIXj[YQhUFWYRVOgZ4VtdCC|cILveZRqdmdiYX\0[ZIhOjRiaILzJIJ6KGGwZ3nv[4Vv\XOrczDhd5NigSxiSVO1NF0xNjF{IN88US=> M3niflIyPzRzMkS5
human A431 cells NYnpUYhNTnWwY4Tpc44h[XO|YYm= MoHEOlAhdWmwcx?= M3m5TGlvcGmkaYTpc44hd2ZiRVfGVkBqdiCqdX3hckBCPDNzIHPlcIx{KGOxbYDveY5lKHC{ZYTy[YF1\WRiZn;yJFYxKG2rbjDi[YZwemViRVfGJJN1cW23bHH0bY9vKG[xcjCxNEBucW6|IHL5JJBpd3OyaH;0fZJwe2mwZTDFUGlUSSCleYTvZoxwfCCvZYToc4QtKEmFNUC9NVczNjFibl2= MkjNNlU5QDJ3MUm=
Sf9 cells NUC4cWp5TnWwY4Tpc44h[XO|YYm= Mnu4TY5pcWKrdHnvckBw\iCJU2SteIFo\2WmIG\FS2ZTKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MD6xPFUh|ryP NGX5d5UyQTh3NEC1NS=>
human HT-29 cells NF3YWpBRem:uaX\ldoF1cW:wIHHzd4F6 NWP0[3hYPzJiaB?= MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHX4dJJme3OrbnegWmVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5Nige,:jDDJR|UxRTBwM{Og{txO NUDl[XJ6OjJ2NES2O|k>
human KM12 cell NFzwZmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW\lU3hXUW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTBzNDFOwG0> Mo\EV2FPT0WU
human TE-15 cell M3rVRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnMTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVA4PjFizszN NHPRd3dUSU6JRWK=
human 697 cell M4HlRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MofVTY5pcWKrdHnvckBw\iCqdX3hckA3QTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[xOFI2KM7:TR?= NGDmRpNUSU6JRWK=
human CAKI-1 cells MoLDVJJwdGmoZYLheIlwdiCjc4PhfS=> NHGzblhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPBT2kuOSClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOlMh|ryP NEXYWoIzOjV4ME[yOy=>
human MOLT-16 cell NX;HXJdYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3TQfWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjNzM{Kg{txO NXXxbohPW0GQR1XS
human GB-1 cell M4HJUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1j3SmlvcGmkaYTpc44hd2ZiaIXtZY4hT0JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|ExOjNizszN M{TyTHNCVkeHUh?=
human TE-12 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64NFQ2PSEQvF2= MnHIV2FPT0WU
human NCI-H3122 cells MnXXVJJwdGmoZYLheIlwdiCjc4PhfS=> NWmzOZZRPzJiaB?= MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuPFMh|ryP MVKyOFkxPDl4MR?=
human ES6 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkPNTY5pcWKrdHnvckBw\iCqdX3hckBGWzZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm4NVA3KM7:TR?= NGTDOVRUSU6JRWK=
human NCI-H526 cells MmrVVJJwdGmoZYLheIlwdiCjc4PhfS=> MnzuO|IhcA>? MkSyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFUzPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuNFEh|ryP M2i1eFI1QTB2OU[x
human LC-2-ad cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFmxcIJKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUKtZYQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjFzNEC3JO69VQ>? MoDmV2FPT0WU
human BL-70 cell M4XyUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknwTY5pcWKrdHnvckBw\iCqdX3hckBDVC15MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNVE5PDZizszN MVfTRW5ITVJ?
human ETK-1 cell NU[2Z5lmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6yPFU5KM7:TR?= MkX5V2FPT0WU
human SW620 cells MoTSVJJwdGmoZYLheIlwdiCjc4PhfS=> MmLrOFghcA>? NHS5XotCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOlIxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTB;MT6zJO69VQ>? NIH0ZmMzOjV4ME[yOy=>
IM9 cells MknyR5l1d3SxeHnjxsBie3OjeR?= NF7jSYdEgXSxdH;4bYNqfHliYXfhbY5{fCCKb33vJJNieGmnboOgLIh2dWGwKTDJUVkh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[nliTWTUJIF{e2G7LDDJR|UxRTFwM{Wg{txO NGXmOHVUSU6JRWK=
human A4-Fuk cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H589yNKEmFNUC9NU4{PDF2MTFOwG0> MVLTRW5ITVJ?
human SR cell NUPoZ2NrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfxfY1KdmirYnn0bY9vKG:oIHj1cYFvKFOUIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OFU4OiEQvF2= NXfUNJlMW0GQR1XS
human A3-KAW cell MmTGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBq[zVyPUGuOlI2PDZizszN M3zRNXNCVkeHUh?=
human KS-1 cell MoXpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37XV2lvcGmkaYTpc44hd2ZiaIXtZY4hU1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlkzPDdizszN M1zadnNCVkeHUh?=
human CTV-1 cell NILnSGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJGNVXi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlc2OSEQvF2= NYXrO2UzW0GQR1XS
human LB1047-RCC cell NU\ofHFiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7FZnNOUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64NVYzPCEQvF2= NVvUc5NMW0GQR1XS
human MEG-01 cell MlL4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXe5eGM4UW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjh|NU[zJO69VQ>? NXnWO3hTW0GQR1XS
human TE-11 cell MmnOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\rN2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlg{QTh3IN88US=> NUHCVJRqW0GQR1XS
human CMK cell NWPNcpVpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvyeXVkUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2PTF5IN88US=> M{jhSHNCVkeHUh?=
human NB1 cell NGTKcpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLtO2lKdmirYnn0bY9vKG:oIHj1cYFvKE6EMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVYyOTdizszN NYXj[o9vW0GQR1XS
human MDA-MB-435 cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NXnueFR5PDhiaB?= NUjKbm54SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJQVIh|ryP MljJNlI2PjB4Mke=
human MCF7 cells MnvPVJJwdGmoZYLheIlwdiCjc4PhfS=> NFTnclU1QCCq MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m1NF0zKM7:TR?= NFfGXHQzOjV4ME[yOy=>
human A549 cells Mn;DR5l1d3SxeHnjxsBie3OjeR?= NYGwWmFuPzJiaB?= MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9Nk41PCEQvF2= NWToUmpWOjN4MEK0OFE>

... 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
体内研究 与实质性,选择性抑制VEGFR2 或PDGFR在体内磷酸化与信号传导一致,Sunitinib (20-80 mg/kg/day)对各种肿瘤异种移植模型,包括HT-29,A431,Colo205,H-460,SF763T,C6,A375,或MDA-MB-435表现出广泛有效的剂量依赖性抗肿瘤活性。Sunitinib以80 mg/kg/day的剂量给药21天,导致8只小鼠中6只完全的肿瘤消退,并且在治疗结束后,110天的观察期内肿瘤不会再生。第二轮使用Sunitinib治疗依然能够有效抗肿瘤,但是不能完全恢复到第一轮治疗的情况。Sunitinib治疗导致肿瘤MVD显著下降,在SF763T神经胶质瘤中减少~40%。SU11248治疗导致表达荧光素酶的PC-3M异种移植物额外的肿瘤生长被完全抑制,尽管肿瘤大小没有减少。[2] 在FLT3-ITD 骨髓移植模型中,Sunitinib治疗(20 mg/kg/day)显著抑制皮下MV4;11 (FLT3-ITD)异种移植物的生长,并延长生存。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

生化酪氨酸激酶试验:

Sunitinib作用于VEGFR2 (Flk-1)和PDGFRβ的IC50值使用包含PKT完整胞浆区的谷胱甘肽-S-转移酶融合蛋白测定。生物化学的酪氨酸激酶试验,用来测定VEGFR2 (Flk-1)和PDGFRβ反式磷酸化活性,在多肽底物poly-Glu,Tyr (4:1)预涂层(在PBS中20 μg/well;4 °C下培养过夜)的96微孔板中进行。过量蛋白结合位点通过加入1-5% (w/v) BSA的PBS溶液阻断。纯化的GST融合蛋白在感染杆状病毒的昆虫细胞中产生。将GST-VEGFR2 和GST-PDGFRβ加入微孔板的2倍浓度激酶稀释缓冲液(由100 mM HEPES,50 mM NaCl,40 μM NaVO4,和0.02% (w/v) BSA组成)中。对GST-VEGFR2或GST-PDGFRβ的最终酶浓度为50 ng/mL。随后将25μL稀释的Sunitinib加入每个反应孔中以产生一系列适用于每个酶的抑制剂浓度。激酶反应通过加入不同浓度的ATP MnCl2溶液起始,使ATP浓度跨越酶的Km值,终MnCl2浓度为10 mM。板在室温下培养5-15分钟,然后加入EDTA停止反应。将板用TBST洗涤3次。在TBST(包含0.5% (w/v) BSA,0.025% (w/v)脱脂奶粉,和100 μM NaVO4)中以1:10,000稀释的兔子多克隆抗磷酸酪氨酸抗血清加入孔中,并在37℃下培养1小时。然后将板用TBST洗涤3次,接着加入山羊抗兔抗血清结合的辣根过氧化物酶(在TBST中以1:10,000 稀释)。板在37℃下培养1小时,然后用TBST清洗3次。加入2,2′-azino-di-[3-ethylbenzthiazoline sulfonate]作为底物后,测定每孔中的磷酸酪氨酸酶数量。
细胞实验:[3]
- 合并
  • Cell lines: RS4;11,MV4;11,和 OC1-AML5
  • Concentrations: 溶解于DMSO,终浓度为~10 μM
  • Incubation Time: 24和48小时
  • Method: 加入Sunitinib和FL (50 ng/mL;仅FLT3-WT细胞)之前,细胞在包含0.1% FBS的培养基中饥饿过夜。培养48小时后,使用Alamar Blue法或台盼蓝细胞活性法测定增殖。加入Sunitinib 24小时后,通过蛋白免疫印迹法检测多聚(ADP-核糖)聚合酶(PARP)的裂解或caspase-3水平,以测量细胞凋亡。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 皮下植入HT-29,A431,Colo205,H-460,SF763T,C6,A375,或MDA-MB-435的雌性nu/nu小鼠,和负荷表达荧光素酶的PC-3M肿瘤的雄性nu/nu小鼠。
  • Dosages: ~80 mg/kg
  • Administration: 口服,每天一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 25 mg/mL warmed (62.73 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+corn oil
7mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 398.47
化学式

C22H27FN4O2

CAS号 557795-19-4
储存条件 粉状
溶于溶剂
别名 SU11248

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

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在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID