AZD1480

For research use only. Not for use in humans.

目录号:S2162

AZD1480 Chemical Structure

CAS No. 935666-88-9

AZD1480是一种新型,ATP竞争性的JAK2抑制剂,无细胞试验中IC50为0.26 nM,选择性作用于JAK3和Tyk2,对JAK1的作用较弱。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1071.19 现货
RMB 819.48 现货
RMB 4671.71 现货
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客户使用Selleck生产的AZD1480发表文献85篇:

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 AZD1480是一种新型,ATP竞争性的JAK2抑制剂,无细胞试验中IC50为0.26 nM,选择性作用于JAK3和Tyk2,对JAK1的作用较弱。Phase 1。
特性 AZD1480为治疗多发性骨髓瘤的潜在新型治疗剂。
靶点
JAK2 [1]
(Cell-free assay)
0.26 nM
体外研究

5μM AZD1480诱导细胞周期停在G2/M期,且通过抑制Aurora激酶而诱导细胞死亡。[1]AZD1480是JAK2的有效抑制剂,作用于人类多发性骨髓瘤细胞,可以抑制生长,存活,FGFR3 和 STAT3信号,及下游靶点,包括 Cyclin D2。在低微摩尔浓度时,AZD1480抑制细胞增殖和诱导骨髓瘤细胞系凋亡。[2]AZD1480 作用于人和鼠神经胶质瘤细胞,有效抑制组成型和诱导型JAK1, JAK2, 及STAT-3的磷酸化作用 ,结果导致细胞增殖降低,且诱导凋亡。[3]AZD1480是有效的ATP竞争性的JAK1/2激酶小分子抑制剂,可抑制STAT3磷酸化和肿瘤生长,这种抑制存在STAT3依赖性。AZD1480通过影响肿瘤的微环境而抑制肿瘤血管生成和局部转移。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW620 NFn4OoFHfW6ldHnvckBCe3OjeR?= NWHnRmNwPSEQvF2= MoPwOFghcA>? M2TNc2ROW09? NHTnN4pjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl3NEm3OEc,OjV7NUS5O|Q9N2F-
LoVo  NWn1b3d{TnWwY4Tpc44hSXO|YYm= NX\CbHBEPSEQvF2= NUnqSY9NPDhiaB?= NGexcpVFVVOR NHHSWpVjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MkjHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NUS5O|QoRjJ3OUW0PVc1RC:jPh?=
HN5 M4nkXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWe3NkBp MXPFR|UxRTNwOEGgxtEhOS57OTFOwG0> NXvD[|NIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVAxOTBpPkK1PFExODFyPD;hQi=>
Cal33 M2\iSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LlelczKGh? M3HrTGVEPTB;Mz6zO{DDuSByLke1JO69VQ>? Mn;aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCwNVAoRjJ3OEGwNFExRC:jPh?=
UM-22B Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnqwO|IhcA>? M4TpdGVEPTB;Mj62OkDDuSByLkK0JO69VQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMECxNEc,OjV6MUCwNVA9N2F-
686LN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVW3NkBp NFX0XIpGSzVyPUKuNFUhyrFiMT6zN{DPxE1? NVr5bI5XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVAxOTBpPkK1PFExODFyPD;hQi=>
UM SCC-1 M1X0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj2O|IhcA>? MYfFR|UxRTFwNkegxtEhOC52MjFOwG0> M1G3[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwNFExLz5{NUixNFAyODxxYU6=
UM-22A NHrYXmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\QTFczKGh? MnjGSWM2OD1zLkOyJOKyKDBwM{mg{txO NFL5SIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFAyOCd-MkW4NVAxOTB:L3G+
OSC19 NXXaNWt[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf3ZWE4OiCq MYDFR|UxRTFwMk[gxtEhOC5{MDFOwG0> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMECxNEc,OjV6MUCwNVA9N2F-
PCI-52 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXnR3JRPzJiaB?= NYrDSFh4TUN3ME2xMlAxKMLzIECuNFkh|ryP MmT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCwNVAoRjJ3OEGwNFExRC:jPh?=
PCI-15B MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3nXGM4OiCq NV3jbJVOTUN3ME2wMlk6KMLzIEGuO|Qh|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMECxNEc,OjV6MUCwNVA9N2F-
UMSCC-1 MXPGeY5kfGmxbjDBd5NigQ>? M13XZ|AvODByNT2xMlYh|ryP Mm\FNlQhcA>? MUXhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMECxNEc,OjV6MUCwNVA9N2F-
Cal33 M4\pO2Z2dmO2aX;uJGF{e2G7 NFr0XYwxNjByMEWtN{45KM7:TR?= MXmyOEBp MkPDZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYPNS41bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVAxOTBpPkK1PFExODFyPD;hQi=>
HH5 MlzPSpVv[3Srb36gRZN{[Xl? NGXwXlUxNjByMEWtN{45KM7:TR?= MknNNlQhcA>? NFTEUmZi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4X4d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwNFExLz5{NUixNFAyODxxYU6=
UM-22A NW\kRW9ZTnWwY4Tpc44hSXO|YYm= NETveHoxNjByMEWtNU43KM7:TR?= MnP0NlQhcA>? NHvR[pli[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NELnO5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFAyOCd-MkW4NVAxOTB:L3G+
A1847 MkfLSpVv[3Srb36gRZN{[Xl? MWGwMlA2NTFyIN88US=> NF7KU4EzPCCq MY\EUXNQyqB? MmD0doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NY\1fIRYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OFYxOTVpPkK1OlQ3ODF3PD;hQi=>
OVCAR-5 NH\rcHhHfW6ldHnvckBCe3OjeR?= NW\kVWV4OC5yNT2xNEDPxE1? NWDSdlc1OjRiaB?= NF33emVFVVORwrC= NXPjW3hqemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M4DVRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkS2NFE2Lz5{NU[0OlAyPTxxYU6=
OVCAR-8 M2XIVGZ2dmO2aX;uJGF{e2G7 NUHNTnY3OC5yNT2xNEDPxE1? NGLNdJczPCCq M3XLWGROW00EoB?= M3nONJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NI\vPWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[0OlAyPSd-MkW2OFYxOTV:L3G+
MOVCAR-5447 NW\1dVAyTnWwY4Tpc44hSXO|YYm= NWnnSo0{OC5yNT2xNEDPxE1? MkLWNlQhcA>? NWLrZnZ{TE2VT9Mg NFXFUWJz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NWH4dHJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OFYxOTVpPkK1OlQ3ODF3PD;hQi=>
MOVCAR-5009 M4rqbGZ2dmO2aX;uJGF{e2G7 MnziNE4xPS1zMDFOwG0> NUHjT3dMOjRiaB?= NXjjUHlbTE2VT9Mg MXPy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NVLMboRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OFYxOTVpPkK1OlQ3ODF3PD;hQi=>
A1847 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYPsUlJKOC5yNT2xNEDPxE1? MVO3NkBp M4fKWGROW09? MWjy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= NGPTelY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[0OlAyPSd-MkW2OFYxOTV:L3G+
OVCAR-5 NGGybYlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NULKO5E5OC5yNT2xNEDPxE1? M{HENlczKGh? NXPPeJM4TE2VTx?= MoP0doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= Ml[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NE[wNVUoRjJ3NkS2NFE2RC:jPh?=
OVCAR-8  NYm3ToFVS2WubDDWbYFjcWyrdImgRZN{[Xl? NXzKTXdSOC5yNT2xNEDPxE1? NVHuV|RbPzJiaB?= NFPzb5NFVVOR NWe5TG9MemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NIrpSnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[0OlAyPSd-MkW2OFYxOTV:L3G+
OVCAR-5  M1rURmFxd3C2b4Ppd{BCe3OjeR?= MoDqNE42NzFxNTFOwG0> MnXQOFghcA>? M{DIVWROW09? M3z1eolv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MoHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NE[wNVUoRjJ3NkS2NFE2RC:jPh?=
OVCAR-8  NVP3dGs6SXCxcITvd4l{KEG|c3H5 NIHrfVAxNjVxMT:1JO69VQ>? NFixU3A1QCCq NYPobWR5TE2VTx?= MXzpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w NEXNZ5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[0OlAyPSd-MkW2OFYxOTV:L3G+
AKRSL NGTScm9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVq1WVB4PzJiaB?= NGfBPWFKSzVy78{eNVAh|ryP NXrmN49QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1NFQ3OzVpPkK1OVA1PjN3PD;hQi=>
PALJDL NGLqRnpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUjiWVIxPzJiaB?= MnT0TWM2OD1{LkSg{txO MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTVyNE[zOUc,OjV3MES2N|U9N2F-
MO4 MlLoSpVv[3Srb36gRZN{[Xl? NHfZblQxNjVxMT:1JO69VQ>? NET3elk3KGh? NVrXboZ3cW6qaXLpeJMhWC2VVFHUN{BmgHC{ZYPzbY9vyqB? NYjLOmpqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxOFk2OzVpPkK1NVQ6PTN3PD;hQi=>
DU145  MoLKSpVv[3Srb36gRZN{[Xl? MWWwMVIxOCCwTR?= MXmxJIjDqA>? NXn1WXFWe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> M4jVO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQzLz5{NEW3O|k1OjxxYU6=
DU145  MX7GeY5kfGmxbjDBd5NigQ>? NUXJZlFFQDByIH7N NUPoe2xYPzJiaB?= M{XlPJN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= M1qzWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQzLz5{NEW3O|k1OjxxYU6=
CWR22Rv1 NHrRT3dHfW6ldHnvckBCe3OjeR?= MkDVPFAxKG6P M362cFczKGh? MUjzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0Nkc,OjR3N{e5OFI9N2F-
N592 Mn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjLcHhPUUN3ME2wMlg1KM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3OEewNUc,OjRzNUi3NFE9N2F-
H82 NGPoO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwM{eg{txO NHPxZ5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1PFcxOSd-MkSxOVg4ODF:L3G+
GLC4 MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknRTWM2OD1zLke5JO69VQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3OEewNUc,OjRzNUi3NFE9N2F-
H526 NHq1NI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDQRZZKUUN3ME2zMlA5KM7:TR?= M1rwRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUW4O|AyLz5{NEG1PFcxOTxxYU6=
H1173 NWLJSY4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jRV2lEPTB;Mj6zPUDPxE1? NEfLV4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1PFcxOSd-MkSxOVg4ODF:L3G+
DMS114 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXxToRLUUN3ME2wMlc{KM7:TR?= NFfGZok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1PFcxOSd-MkSxOVg4ODF:L3G+
NCI-N592 NHTYU5RHfW6ldHnvckBCe3OjeR?= M1rlZVAvOy9zL{Og{txO MlrwNlQhcA>? NFKwdYZqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NGfWNnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1PFcxOSd-MkSxOVg4ODF:L3G+
GLC4 NXHYUnIyTnWwY4Tpc44hSXO|YYm= Mn\oNE4{NzFxMzFOwG0> Mk\CNlQhcA>? NWnjNXNpcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MlfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUi3NFEoRjJ2MUW4O|AyRC:jPh?=
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MZ-CRC1  MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxJOK2VQ>? NHOwPZIxNTViZB?= NGDQZVdFVVOR MkjkbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MkfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNU[0PVkoRjJ|MEW2OFk6RC:jPh?=
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MZ-CRC1  NF3qO2xHfW6ldHnvckBCe3OjeR?= Mk\yNUDDvU1? NX2zbmZ{PzJiaB?= MYTEUXNQ MmLIbY5lfWOnczDHNUBjdG:la3Hn[S=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3NkS5PUc,OjNyNU[0PVk9N2F-
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MZ-CRC1  M4LpVGFxd3C2b4Ppd{BCe3OjeR?= M3vOO|EhyrWP M1\wN|Q5KGh? NYXtUmRmTE2VTx?= M{n4Xolv\HWlZYOgZZBweHSxc3nz NH3ZTVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C1OlQ6QSd-MkOwOVY1QTl:L3G+
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HD-LM2 MmXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO3NwKBkWh? NYDqdHhZTE2VTx?= M2nQOmlEPTB;Nz64OFQh|ryP NHPJXHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiyPVA6PCd-MkK4NlkxQTR:L3G+
L-428 M3TNNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fBR|cz6oDLaB?= M3[5NGROW09? NGPCeW9KSzVyPUeuPVQ4KM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh{OUC5OEc,OjJ6MkmwPVQ9N2F-
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L-540 MoXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmCwO|LjiImq MkT1SG1UVw>? MYjJR|UxRThwMkG2JO69VQ>? MofQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MkmwPVQoRjJ{OEK5NFk1RC:jPh?=
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NCI-H1975 NFrHXmFHfW6ldHnvckBie3OjeR?= NIn0XngxNjByMzD0c{A{KHWP MVuyJIhzew>? NFvSSmpKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hVkOLLVixPVc2KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiMD6wNFMhfG9iMzD1UUBi\nSncjCyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NHHXcVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[xOFQxQCd-Mk[2NVQ1ODh:L3G+
HEL 92.1.7 NXS3e28xTnWwY4Tpc44h[XO|YYm= MUKyJIhzew>? M4X5dmlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBJTUxiOUKuNU44KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDTWGFVPSCyaH;zdIhwenmuYYTpc44h[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ Ml;yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4MUS0NFgoRjJ4NkG0OFA5RC:jPh?=
DAOY MlfxdWhVWyCjc4PhfS=> M{ewOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| Mk\SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 Mke1dWhVWyCjc4PhfS=> Mof5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NFvudYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 NGDreFlyUFSVIHHzd4F6 MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NWr2Z4VNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MkDvdWhVWyCjc4PhfS=> MkP4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NEjUSoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 NGPXcGJyUFSVIHHzd4F6 M{TqTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NXnvVIhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 NUTnWWNreUiWUzDhd5NigQ>? M4To[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NX25bJVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 Mn3YdWhVWyCjc4PhfS=> NXjIU25teUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MmnyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH MmnxdWhVWyCjc4PhfS=> MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= MnT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 M1XORpFJXFNiYYPzZZk> MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| Mln5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 M3XHVJFJXFNiYYPzZZk> MnLYdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MljRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 M4PDcJFJXFNiYYPzZZk> MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NGrTeWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MmLldWhVWyCjc4PhfS=> M2fXW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NHSzboY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NGf3RlVyUFSVIHHzd4F6 MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? Mk\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MmHadWhVWyCjc4PhfS=> NWnjd3pseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-JAK2 / JAK2 ; 

PubMed: 22027691     


Cells were treated with AZD1480 for the indicated times, lysed and immunoblotted with the indicated antibodies. 

p-STAT1 / STAT1 / p-STAT5 / STAT5 / p-STAT6 / STAT6 ; 

PubMed: 22829094     


Western blot assay of the four HL cell lines treated with increasing doses of AZD1480 (0.1–5 μM) for 72 h. 

p-ERK / ERK / p-p38 / p38 / SOCS3 / p-SHP2 / SHP2 ; 

PubMed: 22829094     


Representative western blot assay showing increased levels of ERK, p38 and SHP-2 phosphorylation in HD-LM2 and L-428, after treatment for 72 h with increasing doses of AZD1480 (0.1-5 μM). In contrast, L-540 showed a dose-dependent inhibition of ERK and p38 activation without increased SHP-2 phosphorylation. SOCS-3 levels decreased in all the cell lines.

22027691 22829094
Immunofluorescence
pSTAT5; 

PubMed: 30140255     


HepG2 cells were incubated in the presence of Pro-Gly (0.5 mM) and/or AZD1480 (1 μM) for 6 h and phospho-STAT5 translocation to nuclei was detected by ICC. Scale bar, 10 μm. The IP and ICC experiments were conducted independently for 3 times, with 3 replicates each time.

30140255
Growth inhibition assay
Cell proliferation ; 

PubMed: 22027691     


Cells were treated with AZD1480 for the indicated times, and the WST-1 cell proliferation assay performed. The 48 and 72 h time points were statistically significant. Data represent mean ± SD, replicates of three (**, p<0.001; ANOVA). 

Cell viability; 

PubMed: 25855603     


IL-3-independent Ba/F3 cells were treated with increasing concentrations of the JAK inhibitor AZD1480 showing submicromolar inhibition of proliferation.

22027691 25855603
体内研究 AZD1480作用于人类实体瘤模型和多发性骨髓瘤模型,抑制 STAT3磷酸化。[1]在体内, AZD1480抑制皮下移植瘤的生长,且通过抑制STAT3活性提高携带颅内恶性胶质瘤(GBM)的鼠寿命,说明AZD1480抑制JAK/STAT3通路的药理学可以用于研究治疗携带颅内恶性胶质瘤的患者。[3]AZD1480抑制骨髓细胞的肺浸润和肺转移瘤。AZD1480作用于人类移植瘤模型降低血管生成和代谢。[4]AZD1480抑制含有STAT活性的人类实体瘤的生长。[5]

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:[5]
- 合并

激酶实验:

在有buffer(包括50 mM HEPES pH 为7.3, 1 mM DTT, 0.01% Tween-20, 50 µg/ml BSA,及10 mM MgCl2)的条件下,使用重组Jak1, Jak2, 或Jak3进行AZD1480抑制效果研究。在昆虫细胞中,Jak3酶表达为氮端GST融合蛋白,且通过谷胱甘肽亲和及尺寸排除色谱来纯化Jak3酶。加入AZD1480 (10点剂量反应, 重复三次, 8.3 µM 到0.3 nM ),使用1.5 µM 肽底物(Jak1:FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2和Jak3: FAM-SRCtide),及各自ATP Km (Jak1: 55 µM, Jak2: 15 µM, Jak3: 3 µM),ATP浓度为5 mM,进行酶实验。分离磷酸化和未磷酸化的肽段,使用Caliper LC3000系统计算抑制百分率。
细胞实验:[4]
- 合并
  • Cell lines: Renca或786-O细胞,鼠内皮细胞和脾CD11b+/c−骨髓细胞, HUVECs
  • Concentrations: 1 μM
  • Incubation Time: 48或24小时
  • Method: Renca或786-O细胞悬浮在含5%FBS的DMEM培养基中,按每孔5×103个细胞接种在96孔板上,使细胞粘附,实验组用AZD1480,对照组用DMSO,处理48小时。通过MTS实验测定细胞活力。使用Mikrotek Laborsysteme在490nm处测定吸光值。鼠内皮细胞和脾CD11b+/c− 骨髓细胞从携带肿瘤的鼠中富集得到,培养在含5% FBS的RPMI-1640培养基上。HUVECs 培养在胶原1包被的含完全培养基的板上。用DMSO和不同剂量AZD1480处理所有细胞,持续24小时。手动计算细胞数而测定细胞活力。所有实验重复三次。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: 雌性BALB/c和无胸腺鼠(NCR− nu/nu) (7-8周大)
  • Dosages: 每天一次,剂量为50 mg/kg;或者每天两次,剂量为30 mg/kg
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 69 mg/mL warmed (197.83 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):
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/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 348.77
化学式

C14H14ClFN8

CAS号 935666-88-9
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、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

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

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

相关JAK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID