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78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 MkjVSpVv[3Srb36gRZN{[Xl? M{XMT|Uh|ryP NF;aOIY1QCCq NIXRcFVFVVOR M2i2O4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MnLwNlU6PTR7N{S=
LoVo  MWTGeY5kfGmxbjDBd5NigQ>? MUG1JO69VQ>? NG\qfnY1QCCq M{[y[GROW09? NXO5dVUy[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o M1vXVFI2QTV2OUe0
HN5 NHqzUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDSO|IhcA>? MVPFR|UxRTNwOEGgxtEhOS57OTFOwG0> NV;TboJvOjV6MUCwNVA>
Cal33 MoDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP6bIxZPzJiaB?= MoTwSWM2OD1|LkO3JOKyKDBwN{Wg{txO MnjWNlU5OTByMUC=
UM-22B MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3rO|IhcA>? NGq4dVRGSzVyPUKuOlYhyrFiMD6yOEDPxE1? NWfkdWlSOjV6MUCwNVA>
686LN MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnoO|IhcA>? NWLTeIh{TUN3ME2yMlA2KMLzIEGuN|Mh|ryP NEfndGszPThzMECxNC=>
UM SCC-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LvR|czKGh? NHXPXJdGSzVyPUGuOlchyrFiMD60NkDPxE1? NYP1TXhHOjV6MUCwNVA>
UM-22A MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLrU5FbPzJiaB?= NW\xe4c1TUN3ME2xMlMzKMLzIECuN|kh|ryP MnLJNlU5OTByMUC=
OSC19 MlfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHvRmJYPzJiaB?= NES1N2lGSzVyPUGuNlYhyrFiMD6yNEDPxE1? MlmzNlU5OTByMUC=
PCI-52 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3OcVU4OiCq NEe0N5JGSzVyPUGuNFAhyrFiMD6wPUDPxE1? NGjzWYQzPThzMECxNC=>
PCI-15B NW\WUGhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjyUpFEPzJiaB?= Mn36SWM2OD1yLkm5JOKyKDFwN{Sg{txO M2PMVFI2QDFyMEGw
UMSCC-1 NEj1UIhHfW6ldHnvckBCe3OjeR?= NImzdIwxNjByMEWtNU43KM7:TR?= M1\JZVI1KGh? MmC2ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWfaNJJJOjV6MUCwNVA>
Cal33 MV7GeY5kfGmxbjDBd5NigQ>? M17IbFAvODByNT2zMlgh|ryP NUPSVmhKOjRiaB?= MmCzZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWLGO4NjOjV6MUCwNVA>
HH5 MXfGeY5kfGmxbjDBd5NigQ>? MnK2NE4xODB3LUOuPEDPxE1? NXHhPGpGOjRiaB?= MknGZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4njW|I2QDFyMEGw
UM-22A MmHQSpVv[3Srb36gRZN{[Xl? NEGydpQxNjByMEWtNU43KM7:TR?= MVGyOEBp MljpZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXOyOVgyODBzMB?=
A1847 NGPaPG1HfW6ldHnvckBCe3OjeR?= MnfMNE4xPS1zMDFOwG0> M{HBTFI1KGh? M3vMdGROW00EoB?= NH21[VBz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MnXUNlU3PDZyMUW=
OVCAR-5 MmPrSpVv[3Srb36gRZN{[Xl? MoLNNE4xPS1zMDFOwG0> MmLFNlQhcA>? MVzEUXNQyqB? MVjy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MXKyOVY1PjBzNR?=
OVCAR-8 NIfScmhHfW6ldHnvckBCe3OjeR?= NEXPT2wxNjB3LUGwJO69VQ>? M1vWN|I1KGh? M{WzN2ROW00EoB?= NEDjVVdz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M1nORlI2PjR4MEG1
MOVCAR-5447 NYXxUGxNTnWwY4Tpc44hSXO|YYm= M2jZfFAvODVvMUCg{txO NGfsNHUzPCCq NInpc2JFVVORwrC= M374VpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MkLGNlU3PDZyMUW=
MOVCAR-5009 MVfGeY5kfGmxbjDBd5NigQ>? NYDwbpJYOC5yNT2xNEDPxE1? MUmyOEBp MmTZSG1UV8Li NWTDOWFMemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MVWyOVY1PjBzNR?=
A1847 NIn6b5pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnfzNE4xPS1zMDFOwG0> NH31WXU4OiCq M4DFNmROW09? NFn3c5lz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NWnuN3Z3OjV4NE[wNVU>
OVCAR-5 MoDmR4VtdCCYaXHibYxqfHliQYPzZZk> MoG2NE4xPS1zMDFOwG0> NF\YVGE4OiCq M{nQXmROW09? MXjy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M1POOVI2PjR4MEG1
OVCAR-8  NV65TlJJS2WubDDWbYFjcWyrdImgRZN{[Xl? NXy5SZdnOC5yNT2xNEDPxE1? MmrxO|IhcA>? NIH6PVVFVVOR MY\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M1fxXlI2PjR4MEG1
OVCAR-5  MYXBdI9xfG:|aYOgRZN{[Xl? NE\TcnIxNjVxMT:1JO69VQ>? MWO0PEBp MVjEUXNQ M1XiXolv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= NWqycJdWOjV4NE[wNVU>
OVCAR-8  NXT0dG9CSXCxcITvd4l{KEG|c3H5 MYqwMlUwOS93IN88US=> MVS0PEBp NIPFeotFVVOR M{jaWIlv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= M2LnZ|I2PjR4MEG1
AKRSL M{nldGNmdGxiVnnhZoltcXS7IFHzd4F6 NWO5V5lTPzJiaB?= M3ntR2lEPTExvK6xNEDPxE1? NHi3U3AzPTVyNE[zOS=>
PALJDL NVL2VJJ4S2WubDDWbYFjcWyrdImgRZN{[Xl? MmXpO|IhcA>? M1GzUWlEPTB;Mj60JO69VQ>? MXGyOVUxPDZ|NR?=
MO4 M1K5TGZ2dmO2aX;uJGF{e2G7 MofMNE42NzFxNTFOwG0> MUe2JIg> NECxOphqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? M3fjN|I2OTR7NUO1
DU145  NGrzcm1HfW6ldHnvckBCe3OjeR?= M2jkNFAuOjByIH7N M4O4U|EhcMLi NWLOOHQye3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> MVSyOFU4Pzl2Mh?=
DU145  Mk\aSpVv[3Srb36gRZN{[Xl? NIrWU3E5ODBibl2= NV\0eWJbPzJiaB?= NYK3cpRUe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 MViyOFU4Pzl2Mh?=
CWR22Rv1 M{[0S2Z2dmO2aX;uJGF{e2G7 M3LQblgxOCCwTR?= MYi3NkBp MWLzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? M3HlR|I1PTd5OUSy
N592 NFr0[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S5SmlEPTB;MD64OEDPxE1? MYeyOFE2QDdyMR?=
H82 M1j6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{OyZWlEPTB;MT6zO{DPxE1? M4PLXVI1OTV6N{Cx
GLC4 NG[zdXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXJTWM2OD1zLke5JO69VQ>? NFvTS3UzPDF3OEewNS=>
H526 NYLITJV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfBVHNKSzVyPUOuNFgh|ryP MkPoNlQyPTh5MEG=
H1173 Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r1fmlEPTB;Mj6zPUDPxE1? NGf6PHgzPDF3OEewNS=>
DMS114 NYHMe2k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XsfGlEPTB;MD63N{DPxE1? NXK3eZk2OjRzNUi3NFE>
NCI-N592 MonUSpVv[3Srb36gRZN{[Xl? M2XHZVAvOy9zL{Og{txO NYjqVmFyOjRiaB?= NIfoTI5qdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MVGyOFE2QDdyMR?=
GLC4 MXPGeY5kfGmxbjDBd5NigQ>? M1f6WlAvOy9zL{Og{txO MlXuNlQhcA>? MnjwbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NYfBZYxOOjRzNUi3NFE>
NCI-H82 MlvCSpVv[3Srb36gRZN{[Xl? MYCwMlMwOS9|IN88US=> NXXKT5d2OjRiaB?= Moj6bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MYSyOFE2QDdyMR?=
NCI-N592 NWLuS2xTSXCxcITvd4l{KEG|c3H5 MkjtNE4{NzFxMzFOwG0> NYjUUYhYPDhiaB?= NHuwV|ZqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MknNNlQyPTh5MEG=
GLC4 MV3BdI9xfG:|aYOgRZN{[Xl? M3uxdlAvOy9zL{Og{txO NHeyU3M1QCCq NXznfZJQcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MUGyOFE2QDdyMR?=
NCI-H82 MkHSRZBweHSxc3nzJGF{e2G7 MnH0NE4{NzFxMzFOwG0> M2jMRVQ5KGh? NYDGR5R3cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NVTOVYFTOjRzNUi3NFE>
CWR22Rv1  M3vUTWFxd3C2b4Ppd{BCe3OjeR?= MYLJR|UxRTBwNEiyJO69VQ>? MXuyN|k1OjB7NR?=
CWR22Pc MmLZRZBweHSxc3nzJGF{e2G7 Mn\KTWM2OD1yLkSzPEDPxE1? M172UlI{QTR{MEm1
PC-3 M2fudWFxd3C2b4Ppd{BCe3OjeR?= NH[0SVFKSzVyPUGuO|U2KM7:TR?= MUiyN|k1OjB7NR?=
DU145 NH31coVCeG:ydH;zbZMhSXO|YYm= M2izN2lEPTB;Mz61NVch|ryP MUGyN|k1OjB7NR?=
RC165N NXG0UWR4SXCxcITvd4l{KEG|c3H5 M1TkfWlEPTB;Mj6wPFMh|ryP NX;SOVlEOjN7NEKwPVU>
ARPE19 NUXnTYlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\EUXNQ MnPNTWM2OD1{ND6zPEDPxE1? MnfsNlM2OzF7MkG=
HEK293 NXfuc29qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkP2SG1UVw>? M2PLOGlEPTB;OD62O{DPxE1? MmX4NlM2OzF7MkG=
KCNR NGLXVlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DRdmROW09? MYXJR|UxRTBwNE[g{txO NH[ze2UzOzV|MUmyNS=>
SY5Y MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPvSWlnTE2VTx?= Ml\OTWM2OD1yLkO2JO69VQ>? NE[3e24zOzV|MUmyNS=>
BE2 M1fZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HvOWROW09? M4G3U2lEPTB;MD63NUDPxE1? Mn7tNlM2OzF7MkG=
AS M2TIb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLEUXNQ M1nYTmlEPTB;MT61N{DPxE1? NWj6c2d1OjN3M{G5NlE>
NGP NXLmSm5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHEPJRFVVOR MWnJR|UxRTBwNU[g{txO M{PhcVI{PTNzOUKx
IMR32 M1XVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PPUGROW09? NXLuOlR5UUN3ME2wMlY3KM7:TR?= MoLPNlM2OzF7MkG=
LAN5 NVLXS3NST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHxUXpyTE2VTx?= M1XrZWlEPTB;MT6wOEDPxE1? M4f2cVI{PTNzOUKx
RH18 M2KwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\mdItFVVOR NYP3SJBiUUN3ME2xMlQzKM7:TR?= MYiyN|U{OTl{MR?=
RH30 NV\kR2JWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK4SG1UVw>? NGjYdYdKSzVyPUGuNlUh|ryP M4Tr[|I{PTNzOUKx
RH17 MkGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DSbWROW09? MoPmTWM2OD1{LkWxJO69VQ>? MUmyN|U{OTl{MR?=
RH28 NIHJ[o5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH2zbVVFVVOR NGj3OnJKSzVyPUSuNlgh|ryP NFjnSYMzOzV|MUmyNS=>
RH36 M3vC[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M165NWROW09? MnraTWM2OD13LkO3JO69VQ>? M4rOdlI{PTNzOUKx
RH41 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoT5SG1UVw>? NGfK[29KSzVyPUCuOFgh|ryP MmPzNlM2OzF7MkG=
RD NYLkOVRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PG[2ROW09? NUnQcYRXUUN3ME20MlMzKM7:TR?= M{PIUVI{PTNzOUKx
TC32 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHEUXNQ NEH5dY1KSzVyPUOuPFUh|ryP M{nPTlI{PTNzOUKx
TC71 NWDmfnJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDEUXNQ MXrJR|UxRTRwM{Og{txO NV\SfZN2OjN3M{G5NlE>
KCNR MWXBdI9xfG:|aYOgRZN{[Xl? MnGwNE42NzFwMD:yMlUh|ryP NF\Rd3kzPCCq NWfOXI04TE2VTx?= MVLpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NULkOWlNOjN3M{G5NlE>
SY5Y MWjBdI9xfG:|aYOgRZN{[Xl? MljINE42NzFwMD:yMlUh|ryP NV3KZohHOjRiaB?= MXfEUXNQ NGT1TXhqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NWT5SYM4OjN3M{G5NlE>
Rh18 NETUTJFCeG:ydH;zbZMhSXO|YYm= NUexcIlnOC53L{GuNE8zNjVizszN MlHONlQhcA>? M{nKbmROW09? MlS4bY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MlXHNlM2OzF7MkG=
TC32 MXXBdI9xfG:|aYOgRZN{[Xl? NVy1fWRXOC53L{GuNE8zNjVizszN M1q1b|I1KGh? MljQSG1UVw>? MYXpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MUSyN|U{OTl{MR?=
KCNR NXW0eWxYTnWwY4Tpc44hSXO|YYm= MYqwMlUwOS5yL{KuOU82KM7:TR?= MnuwNlQhcA>? NGjIdmpFVVOR MU\pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NIixOowzOzV|MUmyNS=>
SY5Y NEjG[XZHfW6ldHnvckBCe3OjeR?= MlT0NE42NzFwMD:yMlUwPSEQvF2= NV\odIVYOjRiaB?= NIO4SFRFVVOR NGrhXHZqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MmfzNlM2OzF7MkG=
Rh18 M4LhZWZ2dmO2aX;uJGF{e2G7 NF;hNWYxNjVxMT6wM|IvPS93IN88US=> Ml:1NlQhcA>? Ml3mSG1UVw>? NEftO5dqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> Mle4NlM2OzF7MkG=
TC32 NIfPRYRHfW6ldHnvckBCe3OjeR?= NGLnVHkxNjVxMT6wM|IvPS93IN88US=> NIjqR5AzPCCq MmHPSG1UVw>? NEHESZZqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NXLYcnpTOjN3M{G5NlE>
TPC-1 M3WwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLDNUDDvU1? M4W5UVAuPCCm M2LRcWROW09? M4HJb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? M2X6fFI{ODV4NEm5
MZ-CRC1  M3rhRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnld5dHOSEEtV2= NWLLfoRtOC13IHS= M4fER2ROW09? NHv2O4tqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 NHm5W5EzOzB3NkS5PS=>
TT  NE[yR|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzxNUDDvU1? NFy0W5cxNTRiZB?= MYHEUXNQ NX:zOlB2cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= M3yySVI{ODV4NEm5
TPC-1 NHW4ZllHfW6ldHnvckBCe3OjeR?= NUDYNWROOSEEtV2= MmPBO|IhcA>? NWT1Nph7TE2VTx?= M{fiPIlv\HWlZYOgS|Eh[myxY3vh[4U> MoHnNlMxPTZ2OUm=
MZ-CRC1  NVThdnNnTnWwY4Tpc44hSXO|YYm= NIPoepoyKML3TR?= NXfZUIZPPzJiaB?= MWnEUXNQ MnqxbY5lfWOnczDHNUBjdG:la3Hn[S=> NWDxSGhJOjNyNU[0PVk>
TT  M3r1SGZ2dmO2aX;uJGF{e2G7 NHm1UIYyKML3TR?= MXO3NkBp NWTFdmxrTE2VTx?= MWrpcoR2[2W|IFexJIJtd2OtYXfl MoiyNlMxPTZ2OUm=
MZ-CRC1  NFfPVpRCeG:ydH;zbZMhSXO|YYm= NITxVFkyKML3TR?= M{L4ZlQ5KGh? MYXEUXNQ NHLOSmFqdmS3Y3XzJIFxd3C2b4Ppdy=> MoXONlMxPTZ2OUm=
TT  NIOyVldCeG:ydH;zbZMhSXO|YYm= NXiwbVVvOSEEtV2= NFvZcog1QCCq M4fVe2ROW09? M1\3Solv\HWlZYOgZZBweHSxc3nz NEHqT3czOzB3NkS5PS=>
HD-LM2 NHvkSIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfleXI4OuLCiXi= MUnEUXNQ M4fPNmlEPTB;Nz64OFQh|ryP M2j1fVIzQDJ7MEm0
L-428 NXPXPHVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvw[FRGPzMkgJno NIT6Zm1FVVOR MVnJR|UxRTdwOUS3JO69VQ>? NUfCRYREOjJ6MkmwPVQ>
KM-H2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jWUlcz6oDLaB?= Mn7PSG1UVw>? MVTJR|UxRTFwM{C4JO69VQ>? NHn0ZmMzOjh{OUC5OC=>
L-540 NXiwcHdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjoUIhKPzMkgJno MXjEUXNQ NWHx[Gs1UUN3ME24MlIyPiEQvF2= MlvINlI5OjlyOUS=
HD-LM2 MX;GeY5kfGmxbjDBd5NigQ>? NVnIcVM1OC5zL{CuOU8yNzVizszN M{jLe|cz6oDLaB?= NXPuO3BXTE2VTx?= NV3vZ2sycW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? M2OxdVIzQDJ7MEm0
L-428 MlLxSpVv[3Srb36gRZN{[Xl? MoG5NE4yNzBwNT:xM|Uh|ryP NYXp[WF4PzMkgJno NIDZ[WFFVVOR MnHJbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NUSyXoZoOjJ6MkmwPVQ>
KM-H2 NU[1doF3TnWwY4Tpc44hSXO|YYm= MoHyNE4yNzBwNT:xM|Uh|ryP NIfGV5Y4OuLCiXi= NWLRdFNDTE2VTx?= MoTCbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MYqyNlgzQTB7NB?=
L-540 NGG0NIxHfW6ldHnvckBCe3OjeR?= M4\WT|AvOS9yLkWvNU82KM7:TR?= NIO1UVA4OuLCiXi= MYDEUXNQ MkTnbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> Mn7rNlI5OjlyOUS=
HD-LM2 MlS5RZBweHSxc3nzJGF{e2G7 MUSxM|Uh|ryP NEi2NoI4OuLCiXi= NYHKXG9XTE2VTx?= NH\4fIVqdmS3Y3XzJIFxd3C2b4Ppdy=> MWeyNlgzQTB7NB?=
L-428 NX3kXHVYSXCxcITvd4l{KEG|c3H5 NFvkZmkyNzVizszN MXi3NwKBkWh? MoLQSG1UVw>? NUW5VXRVcW6mdXPld{BieG:ydH;zbZM> MUiyNlgzQTB7NB?=
KM-H2 MWfBdI9xfG:|aYOgRZN{[Xl? M1HnelEwPSEQvF2= NGTW[nU4OuLCiXi= MW\EUXNQ NGjJeIpqdmS3Y3XzJIFxd3C2b4Ppdy=> MWiyNlgzQTB7NB?=
L-540 NUPwWpMxSXCxcITvd4l{KEG|c3H5 Mn\sNU82KM7:TR?= MkPYO|LjiImq NITjXFBFVVOR MlfIbY5lfWOnczDhdI9xfG:|aYO= NIHHS2wzOjh{OUC5OC=>
U251-MG Mlv3SpVv[3Srb36gRZN{[Xl? M3\EOlEhyrWP M1PTe|AuOTZiaB?= MXPpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MkHPNlIxOjd4OUG=
U87-MG NEnROZJHfW6ldHnvckBCe3OjeR?= NYnabIhkOSEEtV2= NFT6[4gxNTF4IHi= MmXKbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NX;uVJdzOjJyMke2PVE>
4C8 MVLGeY5kfGmxbjDBd5NigQ>? MXWxJOK2VQ>? M3\ZUlAuOTZiaB?= MnzqbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v M3K3dFIzODJ5Nkmx
U251-MG NYLmPGxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nxXlEwOTBiwsXN M2D4UlI1NzR6L{eyJIg> NG\iZm1qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NWDNUZpyOjJyMke2PVE>
U87-MG M3zCU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxM|ExKML3TR?= NEjVRW4zPC92OD:3NkBp Mn\DbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> MkP4NlIxOjd4OUG=
4C8 M4LGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnGVWY6OS9zMDFCuW0> NV3vZoN5OjRxNEivO|IhcA>? M2TGfIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO Mmr3NlIxOjd4OUG=
U266 MUjBdI9xfG:|aYOgRZN{[Xl? M1KwXVAvPS1{IN88US=> MWq0PE84OiCq M4nlXYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NGfodGQzOTF4NEWxOy=>
Kms.11 MmflRZBweHSxc3nzJGF{e2G7 NWD6OmVLOC53LUKg{txO M3jGbFQ5Nzd{IHi= MXnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NVPpepVxOjFzNkS1NVc>
8226 MkiyRZBweHSxc3nzJGF{e2G7 M1;yXVAvPS1{IN88US=> MYG0PE84OiCq MYjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MmjXNlEyPjR3MUe=

... 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