Sunitinib

For research use only. Not for use in humans.

目录号:S7781 别名: SU11248

Sunitinib Chemical Structure

Molecular Weight(MW): 398.47

Sunitinib 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。

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100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 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。
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 M370S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPJ[GM4UW6qaXLpeIlwdiCxZjDoeY1idiCVV{e1OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjF|NUGg{txO NH;HOXBUSU6JRWK=
human EoL-1-cell cell NHvDW|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWPL[W5JUW6qaXLpeIlwdiCxZjDoeY1idiCHb1ytNU1k\WyuIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62OIUuODZ? MUPTRW5ITVJ?
human MV-4-11 cell M{PrZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;w[XZKdmirYnn0bY9vKG:oIHj1cYFvKE2YLUStNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ5MjDuUS=> Mm[xV2FPT0WU
human MV411 cells M1jGUnBzd2yrZnXyZZRqd25iYYPzZZk> M1;ONVQ5KGh? NXrnO3ZlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQyOSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBq[zVyPUOgcm0> M4HiWlI1QTB2OU[x
3T3 cells M1vLV2Z2dmO2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36gbY4hO1R|IHPlcIx{KHerdHigNE4yLSCkb4\pcoUhe2W{dX2gZYxjfW2rbjygTWM2OD15IH7N NV7WWllOOTJ4NE[wNVk>
HEK293 cells MlfOSpVv[3Srb36gZZN{[Xl? NYO0WI03SmmwZHnu[{Bi\m[rbnn0fUB1dyCITGSzJINifGGueYTpZ{Bld22jaX6g[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDifUBkd22yZYTpeIl3\SCkaX7kbY5oKGG|c3H5MEBM\D1yLkS3JI5O NVPyNotjOTl5NUSxPVk>
human MDA-MB-435 cells MY\DfZRwfG:6aXRCpIF{e2G7 MnnTNkBp MmL0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygTWM2OD17Lkegcm0> M1PvOFI1QDlyNkWy
human RS4-11 cells NGnxWI5HfW6ldHnvckBie3OjeR?= M4\STmlvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFKVND2xNUBk\WyuczDh[pRmeiB{IHjyd{BjgSCnbHXjeJJw[2inbXnseY1qdmW|Y3XuZ4Uh[XO|YYmsJGlEPTB;OT65JI5O M1fqNVE6PjV2NEC4
HUVEC NX\K[FRLS3m2b4TvfIlkyqCjc4PhfS=> NHLLeotEgXSxdH;4bYNqfHliYXfhbY5{fCCKVW\FR{whUUN3ME2xNU45KG6P MWWyOFg6ODZ3Mh?=
human Kasumi-1 cells NWPDdWloTnWwY4Tpc44h[XO|YYm= Mk\vTY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEujc4XtbU0yKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNTDuUS=> NVjqR5ZyOjB6M{OwN|k>
human NOS-1 cell M1T1c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuN{BvVQ>? MlH0V2FPT0WU
mouse triple negative 4T1 cells M36wdWN6fG:2b4jpZ:Kh[XO|YYm= NHPtRnNEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UB1emmybHWgcoVo[XSrdnWgOHQyKGOnbHzzMEBKSzVyPUG2JI5O MYmyOFg6ODZ3Mh?=
human RS4-11 cells NH;2Z3FHfW6ldHnvckBie3OjeR?= NGHp[JVKdmirYnn0bY9vKG:oIF\MWFMh[XW2b4Doc5NxcG:{eXzheIlwdiCrbjDoeY1idiCUU{StNVEh[2WubIOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxRTF4IH7N MkDxNlA5OzNyM{m=
human MOLM13 cells M3jQUmN6fG:2b4jpZ:Kh[XO|YYm= MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNU2xOOTNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xO{44KG6P MU[yOVA5QThzMB?=
human U251 cells NYfDNoNYTnWwY4Tpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUwhUUN3ME2xPE46KG6P M4LzblI1QTByOE[1
NIH3T3 cells NITHeHdHfW6ldHnvckBie3OjeR?= MlPKNUBp MXzJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBMTFJia3nuZZNmKGW6cILld5Nm\CCrbjDOTWg{XDNiY3XscJMhf2m2aDC0JJVOKEKrb4Tpck1CcHhvQVXFSXlHTkyIQT3hcYll\SCjdDDhcYJq\W62IITlcZBmemG2dYLlJIZweiBzIHjy M3X0dlE3OTZ{MEC4
MDA-MB-231 cells MXnDfZRwfG:6aXRCpIF{e2G7 M{HzdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJRzcXCuZTDu[YdifGm4ZTDNSGEuVUJvMkOxJINmdGy|LDDJR|UxRTJ{LkOgcm0> MWKyOFg6ODZ3Mh?=
MCF7 cells NHHMXGJEgXSxdH;4bYPDqGG|c3H5 MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDFVk1xd3OrdHn2[UBOS0Z5IHPlcIx{NCCLQ{WwQVI4NjFibl2= NW[weFZ6OjR6OUC2OVI>
human CGTH-W-1 cell MkLaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH\hOlJKdmirYnn0bY9vKG:oIHj1cYFvKEOJVFitW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzBwOUSgcm0> NEDMemFUSU6JRWK=
human MONO-MAC-6 cell M1XPSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4DrRmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:QTz3NRWMuPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN|Lkigcm0> MlXhV2FPT0WU
human HL60 cells NVnCcmtNS3m2b4TvfIlkyqCjc4PhfS=> NYPFOoZGPDhiaB?= NUTFW|ZES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVM3Njhibl2= MlPPNlUxQDl6MUC=
human TT cells M4jHZ3Bzd2yrZnXyZZRqd25iYYPzZZk> NIXOVlI4OiCq M{H6TWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVGSgZ4VtdHNicILleJJm[XSnZDDmc5IhPzJiaILzJIZwdGyxd3XkJIJ6KGOxbYDveY5lNXejc3jveZQhdWWjc4Xy[YQh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20NEBvVQ>? MnXnNlQ6ODR7NkG=
human THP1 cells Mon6R5l1d3SxeHnjxsBie3OjeR?= MlvyOFghcA>? MmDsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWGhROSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUS1Mlchdk1? NFfKcYkzPTB6OUixNC=>
3T3 cells MlTwSpVv[3Srb36gZZN{[Xl? NF;1eFZKdmirYnn0bY9vKG:oIG\hd4N2dGG{IHXu[I91cGWuaXHsJIdzd3e2aDDmZYN1d3JicnXj[ZB1d3JiaX6gN3Q{KGOnbHzzMEBKSzVyPUWwJI5O NGfKfZUyOjZ2NkCxPS=>
human ALL-PO cell NHfKdolIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2ftUGlvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|kvQDlibl2= NEXjdGFUSU6JRWK=
human SH-SY5Y cells M3v3T2Z2dmO2aX;uJIF{e2G7 MlvNTY5pcWKrdHnvckBw\iCSRFfGVoJmfGFiaX6gbJVu[W5iU1itV3k2YSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVA:QDNwMTDuUS=> NVvQe5VSOjR6OUC2OVI>
human U251 cells NUnnc2xSTnWwY4Tpc44h[XO|YYm= M2jkNFYxKG2rboO= NVr4eYNTUW6qaXLpeIlwdiCxZjDQSGdHWi2kZYThJIlvKGi3bXHuJHUzPTFiY3XscJMh[2:vcH;1coQheHKndILlZZRm\CCob4KgOlAhdWmwIHLl[o9z\SCSRFfGMWJDKHO2aX31cIF1cW:wIH\vdkAyOCCvaX7zJIJ6KHCqb4PwbI91gXKxc3nu[UBGVEmVQTDjfZRw[myxdDDt[ZRpd2RuIFnDOVA:QDNwMTDuUS=> M3rmUFI2QDh{NUG5
human NKM-1 cell MnTiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLJTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlUzKG6P MlHRV2FPT0WU
human HAEC cells MmP1VJJwdGmoZYLheIlwdiCjc4PhfS=> MYO3NkBp MnTwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQVXDJINmdGy|IHX4dJJme3OrbnegWmVITlJiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjFizszN M2S5RlIzPDR2Nke5
HUVEC cell NXzQeYxMTnWwY4Tpc44h[XO|YYm= NUDrZ3p{OjRiaB?= M3PYO2lvcGmkaYTpc44hd2ZiVlXHSk1CKGmwZIXj[YQhUFWYRVOgZ4VtdCC|cILveZRqdmdiYX\0[ZIhOjRiaILzJIJ6KGGwZ3nv[4Vv\XOrczDhd5NigSxiSVO1NF0xNjF{IN88US=> MUKyNVc1OTJ2OR?=
human A431 cells NVPQT3IzTnWwY4Tpc44h[XO|YYm= Mlr2OlAhdWmwcx?= MWrJcohq[mm2aX;uJI9nKEWJRmKgbY4hcHWvYX6gRVQ{OSClZXzsd{Bkd22yb4Xu[EBxemW2cnXheIVlKG[xcjC2NEBucW5iYnXmc5JmKEWJRjDzeIlufWyjdHnvckBnd3JiMUCgcYlveyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2Eh[3m2b3Lsc5QhdWW2aH;kMEBKSzVyPUG3Nk4yKG6P Mmi1NlU5QDJ3MUm=
Sf9 cells NUTzPFJ[TnWwY4Tpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKEeVVD30ZYdo\WRiVlXHSnIh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD1yLkG4OUDPxE1? MVGxPVg2PDB3MR?=
human HT-29 cells MnrQVJJwdGmoZYLheIlwdiCjc4PhfS=> NG\rTIY4OiCq MkXZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDlfJBz\XO|aX7nJHZGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XoxvJygTWM2OD1yLkOzJO69VQ>? M4nqWlIzPDR2Nke5
human KM12 cell MkDMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX7BdI5uUW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTBzNDFOwG0> NHH3fIxUSU6JRWK=
human TE-15 cell MlrkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\yPWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxPzZzIN88US=> Mn\CV2FPT0WU
human 697 cell MmDaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\PTY5pcWKrdHnvckBw\iCqdX3hckA3QTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[xOFI2KM7:TR?= MoPjV2FPT0WU
human CAKI-1 cells MkfkVJJwdGmoZYLheIlwdiCjc4PhfS=> NGrVVHhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPBT2kuOSClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOlMh|ryP NYrwTYZ2OjJ3NkC2Nlc>
human MOLT-16 cell NVPWVWJTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYGxNVY2UW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54M{GzNkDPxE1? NHLab2dUSU6JRWK=
human GB-1 cell M324c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlfSTY5pcWKrdHnvckBw\iCqdX3hckBISi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63NVAzOyEQvF2= Mn\VV2FPT0WU
human TE-12 cell NVq1WZUyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1jOcWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgxPDV3IN88US=> NEjHS3NUSU6JRWK=
human NCI-H3122 cells MnLBVJJwdGmoZYLheIlwdiCjc4PhfS=> M1[wU|czKGh? MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuPFMh|ryP M1nVbFI1QTB2OU[x
human ES6 cell MnLKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXlemZuUW6qaXLpeIlwdiCxZjDoeY1idiCHU{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk5OTB4IN88US=> M37ET3NCVkeHUh?=
human NCI-H526 cells M1HENXBzd2yrZnXyZZRqd25iYYPzZZk> MXS3NkBp MlLJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFUzPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuNFEh|ryP NETKUmYzPDlyNEm2NS=>
human LC-2-ad cell M3nZNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3kTY5pcWKrdHnvckBw\iCqdX3hckBNSy1{LXHkJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTRyNzFOwG0> M176UHNCVkeHUh?=
human BL-70 cell NEOzZZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlL2TY5pcWKrdHnvckBw\iCqdX3hckBDVC15MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNVE5PDZizszN MnjWV2FPT0WU
human ETK-1 cell M3LvR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3HmU2lvcGmkaYTpc44hd2ZiaIXtZY4hTVSNLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI5PThizszN NFT5TodUSU6JRWK=
human SW620 cells NXfYcJc2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUS0[JY5PDhiaB?= MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5|IN88US=> MmTHNlI2PjB4Mke=
IM9 cells MVTDfZRwfG:6aXRCpIF{e2G7 NIHlPVdEgXSxdH;4bYNqfHliYXfhbY5{fCCKb33vJJNieGmnboOgLIh2dWGwKTDJUVkh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[nliTWTUJIF{e2G7LDDJR|UxRTFwM{Wg{txO Mn65V2FPT0WU
human A4-Fuk cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H589yNKEmFNUC9NU4{PDF2MTFOwG0> M{ixVnNCVkeHUh?=
human SR cell M2X6Rmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHNTKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53NEW3NkDPxE1? MkPsV2FPT0WU
human A3-KAW cell NXLWSWFHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXQV3VKdmirYnn0bY9vKG:oIHj1cYFvKEF|LVvBW{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCrY{WwQVEvPjJ3NE[g{txO NIPyUYhUSU6JRWK=
human KS-1 cell MmrFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGDPV3BKdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY6OjR5IN88US=> NWjDeZZ7W0GQR1XS
human CTV-1 cell MmXYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLQZot6UW6qaXLpeIlwdiCxZjDoeY1idiCFVG[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzJ5NUGg{txO MnLyV2FPT0WU
human LB1047-RCC cell MljVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJGxDOTB2Nz3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjhzNkK0JO69VQ>? NVS4UnZyW0GQR1XS
human MEG-01 cell M1rxR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4L6UWlvcGmkaYTpc44hd2ZiaIXtZY4hVUWJLUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU45OzV4MzFOwG0> MX\TRW5ITVJ?
human TE-11 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGX1OYpKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU45Ozl6NTFOwG0> NFXDeWlUSU6JRWK=
human CMK cell NYDmSWo6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULHPW5UUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2PTF5IN88US=> MnTjV2FPT0WU
human NB1 cell NUD4flViT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nW[GlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT65OlEyPyEQvF2= NEX1WnpUSU6JRWK=
human MDA-MB-435 cells NXTxSlhEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NV;qOopYPDhiaB?= NHPBboFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m9NkDPxE1? NHL0dpozOjV4ME[yOy=>
human MCF7 cells NFLOepdRem:uaX\ldoF1cW:wIHHzd4F6 NIX0flI1QCCq Mnz6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJOVA:OiEQvF2= M4\GZ|IzPTZyNkK3
human A549 cells MkfqR5l1d3SxeHnjxsBie3OjeR?= MlfmO|IhcA>? M{DtSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zNjR2IN88US=> M{e5UlI{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
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(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 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