Sunitinib

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该产品发表文献37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 NFjhTI5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzV4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNVM2OSEQvF2= MXHTRW5ITVJ?
human EoL-1-cell cell NYe4dpNDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTITY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS54NHWtNFY> M1riWXNCVkeHUh?=
human MV-4-11 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlTHTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPzJibl2= MX\TRW5ITVJ?
human MV411 cells MlnCVJJwdGmoZYLheIlwdiCjc4PhfS=> M1zwVlQ5KGh? MoLmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= NHnhUZEzPDlyNEm2NS=>
3T3 cells M{DpfGZ2dmO2aX;uJIF{e2G7 M1vNeWlvcGmkaYTpc44hd2ZiUFTHSk1qdmS3Y3XkJGJz\FViaX7jc5Jxd3KjdHnvckBqdiB|VEOgZ4VtdHNid3n0bEAxNjFnIHLveolv\SC|ZYL1cUBidGK3bXnuMEBKSzVyPUegcm0> M{exSlEzPjR4MEG5
HEK293 cells MmruSpVv[3Srb36gZZN{[Xl? NWfEZnRISmmwZHnu[{Bi\m[rbnn0fUB1dyCITGSzJINifGGueYTpZ{Bld22jaX6g[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDifUBkd22yZYTpeIl3\SCkaX7kbY5oKGG|c3H5MEBM\D1yLkS3JI5O NGXBWoEyQTd3NEG5PS=>
human MDA-MB-435 cells NYnPdWE4S3m2b4TvfIlkyqCjc4PhfS=> NF;WZ2wzKGh? MmTGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygTWM2OD17Lkegcm0> MnOwNlQ5QTB4NUK=
human RS4-11 cells MnPHSpVv[3Srb36gZZN{[Xl? MX;Jcohq[mm2aX;uJI9nKE[OVEOgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBTWzRvMUGgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\WynY4Tyc4Np\W2rbIXtbY5me2OnbnPlJIF{e2G7LDDJR|UxRTlwOTDuUS=> MYOxPVY2PDRyOB?=
HUVEC M1HFcmN6fG:2b4jpZ:Kh[XO|YYm= MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzygTWM2OD1zMT64JI5O M{[3d|I1QDlyNkWy
human Kasumi-1 cells NFHwOYtHfW6ldHnvckBie3OjeR?= MmrDTY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEujc4XtbU0yKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNTDuUS=> NWnmXJZNOjB6M{OwN|k>
human NOS-1 cell M2GzWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH6wVnNKdmirYnn0bY9vKG:oIHj1cYFvKE6RUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvOyCwTR?= MY\TRW5ITVJ?
mouse triple negative 4T1 cells NF[2XlNEgXSxdH;4bYPDqGG|c3H5 NVf0cFlGS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhfHKrcHzlJI5m\2G2aY\lJFRVOSClZXzsd{whUUN3ME2xOkBvVQ>? M16yUlI1QDlyNkWy
human RS4-11 cells NULCTmdRTnWwY4Tpc44h[XO|YYm= M4qweWlvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFKVND2xNUBk\WyuczDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNuIFnDOVA:OTZibl2= MYeyNFg{OzB|OR?=
human MOLM13 cells Ml2wR5l1d3SxeHnjxsBie3OjeR?= NULUW4JmS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVU:OTUGzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTdwNzDuUS=> MXKyOVA5QThzMB?=
human U251 cells NYfTWVFXTnWwY4Tpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUwhUUN3ME2xPE46KG6P NV\Z[VRFOjR7MEC4OlU>
NIH3T3 cells NFvkfYFHfW6ldHnvckBie3OjeR?= MnfZNUBp MULJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBMTFJia3nuZZNmKGW6cILld5Nm\CCrbjDOTWg{XDNiY3XscJMhf2m2aDC0JJVOKEKrb4Tpck1CcHhvQVXFSXlHTkyIQT3hcYll\SCjdDDhcYJq\W62IITlcZBmemG2dYLlJIZweiBzIHjy NFHnN5IyPjF4MkCwPC=>
MDA-MB-231 cells MoDvR5l1d3SxeHnjxsBie3OjeR?= Ml7CR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6geJJqeGynIH7l[4F1cX[nIF3ERU1OSi1{M{GgZ4VtdHNuIFnDOVA:OjJwMzDuUS=> Ml;LNlQ5QTB4NUK=
MCF7 cells MonhR5l1d3SxeHnjxsBie3OjeR?= NEHw[FhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBGWi2yb4PpeIl3\SCPQ1[3JINmdGy|LDDJR|UxRTJ5LkGgcm0> M2[5R|I1QDlyNkWy
human CGTH-W-1 cell NHu1W4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvQTRibl2= Mo\qV2FPT0WU
human MONO-MAC-6 cell NIfO[HFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoP6TY5pcWKrdHnvckBw\iCqdX3hckBOV06RLV3BR{03KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwODDuUS=> NVPFO41FW0GQR1XS
human HL60 cells M{P0XmN6fG:2b4jpZ:Kh[XO|YYm= NWPVNWU5PDhiaB?= NEX3eFFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9N|YvQCCwTR?= NY\KR21iOjVyOEm4NVA>
human TT cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 NILUZ|M4OiCq M4PLeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVGSgZ4VtdHNicILleJJm[XSnZDDmc5IhPzJiaILzJIZwdGyxd3XkJIJ6KGOxbYDveY5lNXejc3jveZQhdWWjc4Xy[YQh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20NEBvVQ>? MX:yOFkxPDl4MR?=
human THP1 cells M3PjRWN6fG:2b4jpZ:Kh[XO|YYm= MXK0PEBp NHnJNWdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUFBzIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFUvPyCwTR?= NUfyS5Z1OjVyOEm4NVA>
3T3 cells MmfnSpVv[3Srb36gZZN{[Xl? MUfJcohq[mm2aX;uJI9nKF[jc3P1cIFzKGWwZH;0bIVtcWGuIHfyc5d1cCCoYXP0c5IhemWlZYD0c5IhcW5iM2SzJINmdGy|LDDJR|UxRTVyIH7N MXmxNlY1PjBzOR?=
human ALL-PO cell NWTmeHRZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXTJcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUe5Mlg6KG6P Mn\PV2FPT0WU
human SH-SY5Y cells MnXISpVv[3Srb36gZZN{[Xl? NVrNeWVLUW6qaXLpeIlwdiCxZjDQSGdHWmKndHGgbY4hcHWvYX6gV2guW1l3WTDj[YxteyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2Eh[XO|YYmsJGlEPTB;OEOuNUBvVQ>? NVG5PGN5OjR6OUC2OVI>
human U251 cells MkT4SpVv[3Srb36gZZN{[Xl? NWfZPI05PjBibXnudy=> NGeweIJKdmirYnn0bY9vKG:oIGDES2ZTNWKndHGgbY4hcHWvYX6gWVI2OSClZXzsd{Bkd22yb4Xu[EBxemW2cnXheIVlKG[xcjC2NEBucW5iYnXmc5JmKFCGR1[tRmIhe3SrbYXsZZRqd25iZn;yJFExKG2rboOgZpkheGixc4Doc5R6em:|aX7lJGVNUVODIHP5eI9jdG:2IH3leIhw\CxiSVO1NF05Oy5zIH7N MXuyOVg5OjVzOR?=
human NKM-1 cell NGS3fYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnf5TY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlUzKG6P NUTDc2FqW0GQR1XS
human HAEC cells NUXmV4JDWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWm3NkBp NY\XU3lxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIRWVEKGOnbHzzJIV5eHKnc4PpcochXkWJRmKgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkGg{txO NWH0WFlnOjJ2NES2O|k>
HUVEC cell Mn\0SpVv[3Srb36gZZN{[Xl? MmXMNlQhcA>? M3K1V2lvcGmkaYTpc44hd2ZiVlXHSk1CKGmwZIXj[YQhUFWYRVOgZ4VtdCC|cILveZRqdmdiYX\0[ZIhOjRiaILzJIJ6KGGwZ3nv[4Vv\XOrczDhd5NigSxiSVO1NF0xNjF{IN88US=> MmnGNlE4PDF{NEm=
human A431 cells M4nJXWZ2dmO2aX;uJIF{e2G7 NF3GT3E3OCCvaX7z NG\Bco5KdmirYnn0bY9vKG:oIFXHSnIhcW5iaIXtZY4hSTR|MTDj[YxteyClb33wc5Vv\CCycnX0doVifGWmIH\vdkA3OCCvaX6gZoVnd3KnIFXHSkB{fGmvdXzheIlwdiCob4KgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RibXX0bI9lNCCLQ{WwQVE4Oi5zIH7N MYOyOVg5OjVzOR?=
Sf9 cells MXnGeY5kfGmxbjDhd5NigQ>? NGi4Z4hKdmirYnn0bY9vKG:oIFfTWE11[WepZXSgWmVITlJiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{whUUN3ME2wMlE5PSEQvF2= M{DRSVE6QDV2MEWx
human HT-29 cells M4TnVnBzd2yrZnXyZZRqd25iYYPzZZk> Ml;sO|IhcA>? MkW3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDlfJBz\XO|aX7nJHZGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XoxvJygTWM2OD1yLkOzJO69VQ>? NIW5RZozOjR2NE[3PS=>
human KM12 cell NUfXOoJiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVX2VWlJUW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTBzNDFOwG0> M4DacXNCVkeHUh?=
human TE-15 cell M3PmUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnIO4RzUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB5NkGg{txO NU\YVVdGW0GQR1XS
human 697 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\hTY5pcWKrdHnvckBw\iCqdX3hckA3QTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[xOFI2KM7:TR?= MVPTRW5ITVJ?
human CAKI-1 cells MnTUVJJwdGmoZYLheIlwdiCjc4PhfS=> NUHuOphISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDRWtKNTFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlY{KM7:TR?= NFK3T2wzOjV4ME[yOy=>
human MOLT-16 cell NFHmem1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlrLTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OzF|MjFOwG0> MUPTRW5ITVJ?
human GB-1 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVTadYtwUW6qaXLpeIlwdiCxZjDoeY1idiCJQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OTB{MzFOwG0> NYr0eVJ[W0GQR1XS
human TE-12 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkjFTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPFA1PTVizszN NFHB[WZUSU6JRWK=
human NCI-H3122 cells NUmzVFRGWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4jWXFczKGh? MoX2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg{KM7:TR?= MnfNNlQ6ODR7NkG=
human ES6 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TSdWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD65PFExPiEQvF2= M{\BdXNCVkeHUh?=
human NCI-H526 cells NV:2cW42WHKxbHnm[ZJifGmxbjDhd5NigQ>? NULmcXhzPzJiaB?= MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOVI3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6wNUDPxE1? NFvtV|czPDlyNEm2NS=>
human LC-2-ad cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXmTY5pcWKrdHnvckBw\iCqdX3hckBNSy1{LXHkJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOTRyNzFOwG0> NVXmfVliW0GQR1XS
human BL-70 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGJNNTdyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6xNVg1PiEQvF2= MVnTRW5ITVJ?
human ETK-1 cell NUfjVWFST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn3NTY5pcWKrdHnvckBw\iCqdX3hckBGXEtvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlg2QCEQvF2= NXSyPHM3W0GQR1XS
human SW620 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 MkHaOFghcA>? NXzJdIZsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUGuN{DPxE1? NEjyW2MzOjV4ME[yOy=>
IM9 cells M{fqeWN6fG:2b4jpZ:Kh[XO|YYm= NV;NT|NbS3m2b4TvfIlkcXS7IHHnZYlve3RiSH;tc{B{[XCrZX7zJEhpfW2jbjmgTW06KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1zLkO1JO69VQ>? NUeweXZNW0GQR1XS
human A4-Fuk cell NInrXW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{DsUmlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjN2MUSxJO69VQ>? NU\JU3FRW0GQR1XS
human SR cell NYe4cXJJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\hcmlvcGmkaYTpc44hd2ZiaIXtZY4hW1JiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW0OVczKM7:TR?= NFzFOHBUSU6JRWK=
human A3-KAW cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYDKbnM5UW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiaXO1NF0yNjZ{NUS2JO69VQ>? MV7TRW5ITVJ?
human KS-1 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGtUNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLk[5NlQ4KM7:TR?= MWHTRW5ITVJ?
human CTV-1 cell MnPKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYjFU3cxUW6qaXLpeIlwdiCxZjDoeY1idiCFVG[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzJ5NUGg{txO MoW0V2FPT0WU
human LB1047-RCC cell NHPQZlBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEPOUlBKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkixOlI1KM7:TR?= MWLTRW5ITVJ?
human MEG-01 cell M1LxSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWfqXHhSUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjh|NU[zJO69VQ>? MX3TRW5ITVJ?
human TE-11 cell MkKwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64N|k5PSEQvF2= MULTRW5ITVJ?
human CMK cell M4\vbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUW1NVch|ryP NVvF[4dLW0GQR1XS
human NB1 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHraT|FKdmirYnn0bY9vKG:oIHj1cYFvKE6EMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVYyOTdizszN NI\GfI9USU6JRWK=
human MDA-MB-435 cells NUDVb4RyWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVe0PEBp NFzJb4ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m9NkDPxE1? NWSzS|dMOjJ3NkC2Nlc>
human MCF7 cells Mm\QVJJwdGmoZYLheIlwdiCjc4PhfS=> MXu0PEBp M4jBSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTJizszN MorlNlI2PjB4Mke=
human A549 cells MmSwR5l1d3SxeHnjxsBie3OjeR?= M{j0UVczKGh? NGX6cXBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi52NDFOwG0> NE\lZnczOzZyMkS0NS=>

... Click to View More Cell Line Experimental Data

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]
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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]
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  • 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]
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  • 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。
  • Formulation: 以羧甲基纤维素悬浮液或柠檬酸盐缓冲溶液(pH 3.5)形成
  • 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
稳定性 powder
in solvent
别名 SU11248

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 (g) = 浓度 (mol/L) x 体积 (L) 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 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

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操作手册

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PDGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID