Sunitinib (SU11248)

For research use only. Not for use in humans.

目录号:S7781 中文名称:舒尼替尼

Sunitinib (SU11248) 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  
10mM (1mL in DMSO) RMB 794.43 现货
RMB 811.55 现货
RMB 1624.45 现货
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客户使用Selleck生产的Sunitinib (SU11248)发表文献171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
HUVEC cell MljkSpVv[3Srb36gZZN{[Xl? MVuyOEBp MWfJcohq[mm2aX;uJI9nKF[HR1[tRUBqdmS3Y3XkJGhWXkWFIHPlcIwhe3C{b4X0bY5oKGGodHXyJFI1KGi{czDifUBidmerb3flcoV{cXNiYYPzZZktKEmFNUC9NE4yOiEQvF2= M1rOSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{SxNlQ6Lz5{MUe0NVI1QTxxYU6=
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MV4-11 NVPKe4lJSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MnzzO|IhcHK| MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF\MWFMuUVSGIHTldIVv\GWwdDDoeY1idiCPVkStNVEh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBk\WyudHn0[ZIu\2yxL1PDT|gh[XO|YYmsJGdKPTBiPTCwMlAxOSEQvF2u M{j4cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
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endothelial precursor cells NF7WdYhHfW6ldHnvckBie3OjeR?= M1[2[mlvcGmkaYTpc44hd2ZiZX7kc5Rp\WyrYXygZ49z\CCjcnXhJIZwem2jdHnvckBqdiCnbnTveIhmdGmjbDDwdoVkfXK|b4KgZ4VtdHNiYomgR2Q{OSClb4LkJIFz\WFiZHX0[YN1cW:wIHLhd4VlKHCqZX7veJlxcWNiZIL1[{BlcXOlb4\ldpkh[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwPVYh|ryPLh?= M{LGflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEC5OlY3Lz5{MkSwPVY3PjxxYU6=
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MDA-MB-231 NFnIZ4REgXSxdH;4bYNqfHliYYPzZZk> Mmr4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6geJJqeGynIH7l[4F1cX[nIF3ERU1OSi1{M{GgZ4VtdHNuIFnDOVAhRSByLkCyNlMh|ryPLh?= NXzOZYRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PVA3PTJpPkK0PFkxPjV{PD;hQi=>
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endothelial precursor cells M3LiSWZ2dmO2aX;uJIF{e2G7 NE\nWIhKdmirYnn0bY9vKG:oIHPlcIwhdWmpcnH0bY9vKGmwIHXu[I91cGWuaXHsJJBz\WO3coPvdkBk\WyuczDifUBQemm|IHPlcIwhdWmpcnH0bY9vKGurdDDiZZNm\CCyaHXuc5R6eGmlIHTyeYch\Gm|Y3;2[ZJ6KGKjc3XkJIF{e2G7LDDJR|UxKD1iMUOuOkDPxE1w NFq5Z4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSwPVY3Pid-MkK0NFk3PjZ:L3G+
HepG2 M1m1e2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MWq0PEBpenN? NEPQUHJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxN{43KM7:TT6= NHvq[oY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2OFM1Pyd-MkWwOlQ{PDd:L3G+
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BT549 NH7YXoZEgXSxdH;4bYNqfHliYYPzZZk> MnXFOFghcHK| MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFU1QSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVUvPSEQvF2u NH:5UZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GyPFE4Oyd-MkexNlgyPzN:L3G+
BT549 MkC1R5l1d3SxeHnjbZR6KGG|c3H5 NVriOlhxPDhiaILz MojKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnQ2PDliY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVUvPSEQvF2u MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzZ|OUO2PUc,Ojd4M{mzOlk9N2F-
BT549 MojiR5l1d3SxeHnjbZR6KGG|c3H5 NXrk[lVlPDhiaILz NELGUmREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDV2OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEG1MlU1KM7:TT6= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR2OEmxOkc,Ojd2NEi5NVY9N2F-
CHO K1 MoDLSpVv[3Srb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKG[jc4Sgd49lcXWvIHP1dpJmdnRiKFnOZUkhcW5iQ3jpcoV{\SCKYX3zeIVzKE:4YYL5JEhEUE9rIFuxJINmdGy|IITyZY5{\mWldHXkJJdqfGhiaIXtZY4hVmG4MT61JI1m[XO3cnXkJJV{cW6pIFnvcndwemu|IGH1ZZR1em9iYYX0c41ifGWmIIDheINpKGOuYX3wJJBt[XSob4LtMEBKSzVyIE2gNVUvQDR6OTFOwG0v M3:z[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEi3O|U{Lz5{NUC4O|c2OzxxYU6=
HepG2 M3jESmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MnOyOFghcHK| NF\hNZlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxOk4xPiEQvF2u MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB3N{SyN{c,OjhyNUe0NlM9N2F-
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EHEB MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVTCdJQ4UW6qaXLpeIlwdiCxZjDoeY1idiCHSFXCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{PC5zMUmzJO69VS5? M17hNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU{PS9pPmPBUmdGWjxxYU6=
U-266 NXq5[WI{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWf0b5J{UW6qaXLpeIlwdiCxZjDoeY1idiCXLUK2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOzRwMke4NkDPxE1w NXiyZ|I{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
EW-11 Mni4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\BTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gN|QvPDd{NTFOwG0v MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
TE-9 MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXnsUWNuUW6qaXLpeIlwdiCxZjDoeY1idiCWRT25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{Py5yNECxJO69VS5? NUnIPIxbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
ES3 NEXLRoJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJGVUOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iM{euOVAxPCEQvF2u MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
NCI-H2141 M3LqdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{fiT2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVQyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB|OD6wPFQ{KM7:TT6= MoixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM2Nyd-U1HOS2VTRC:jPh?=
MPP-89 NIrp[5VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MonlTY5pcWKrdHnvckBw\iCqdX3hckBOWFBvOEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQzNjB3OE[g{txONg>? M3TVTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU{PS9pPmPBUmdGWjxxYU6=
SK-MEL-2 MmDsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Oi54NEC1JO69VS5? NXvBd4d2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
LC-1F NHvpPWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoTWTY5pcWKrdHnvckBw\iCqdX3hckBNSy1zRjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFMvOzZ6MjFOwG0v M1HDNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU{PS9pPmPBUmdGWjxxYU6=
NH-12 MnzQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIfud3FKdmirYnn0bY9vKG:oIHj1cYFvKE6KLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Oy57M{W5JO69VS5? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
RKO Mn[5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\BTY5pcWKrdHnvckBw\iCqdX3hckBTU09iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IES0MlEzPTJizszNMi=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|UwLz6VQV7HSXI9N2F-
KM-H2 MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHq4dlJKdmirYnn0bY9vKG:oIHj1cYFvKEuPLViyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1PC57NUe3JO69VS5? NX3rTFdPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTN3Lze+V2FPT0WUPD;hQi=>
SK-UT-1 M4TwSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWLJcohq[mm2aX;uJI9nKGi3bXHuJHNMNVWWLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ6Njh6MkWg{txONg>? MoHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM2Nyd-U1HOS2VTRC:jPh?=

... 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
0.875mg/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 N/A

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、SDS / 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、SDS / 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
NCT04669366 Recruiting Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd. November 25 2020 Phase 2
NCT04115189 Completed Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT03916458 Completed -- Carcinoma Renal Cell Pfizer December 17 2019 --
NCT04175262 Completed Drug: sunitinib Metastatic Renal Cell Carcinoma (mRCC) Pfizer|IMDC group|Analysis Group October 31 2019 --
NCT04033991 Completed Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 27 2019 --

技术支持

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

如果有其他问题,请给我们留言。

  • * 必填项

PDGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID