AZD1480

For research use only. Not for use in humans.

Catalog No.S2162

50 publications

AZD1480 Chemical Structure

Molecular Weight(MW): 348.77

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

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Selleck's AZD1480 has been cited by 50 publications

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Description AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.
Targets
JAK2 [1]
(Cell-free assay)
0.26 nM
In vitro

5μM AZD1480 induces G2/M arrest and cell death by inhibiting Aurora kinases. [1] AZD1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 and STAT3 signaling and downstream targets including Cyclin D2 in human multiple myeloma cells. At low micromolar concentrations, AZD1480 blocks cell proliferation and induces apoptosis of myeloma cell lines. [2]AZD1480 effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. [3]AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, and that it is capable of inhibiting STAT3 phosphorylation and tumor growth in a STAT3-dependent manner. AZD1480 inhibits tumor angiogenesis and metastasis in part by affecting the tumor microenvironment. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW620 MnLDSpVv[3Srb36gRZN{[Xl? M3frdVUh|ryP MnzlOFghcA>? MWTEUXNQ MlLIZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n MorINlU6PTR7N{S=
LoVo  NFPUbWRHfW6ldHnvckBCe3OjeR?= M1PyNVUh|ryP Ml7yOFghcA>? MmLOSG1UVw>? NYq5XpBs[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NULQUHQxOjV7NUS5O|Q>
HN5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL4O|IhcA>? M2PCZ2VEPTB;Mz64NUDDuSBzLkm5JO69VQ>? MXOyOVgyODBzMB?=
Cal33 NV;wc5RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjMSWQ4OiCq NWrBOHdRTUN3ME2zMlM4KMLzIECuO|Uh|ryP NUj6eIZ[OjV6MUCwNVA>
UM-22B Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn4e41{PzJiaB?= NIfuW2VGSzVyPUKuOlYhyrFiMD6yOEDPxE1? MVuyOVgyODBzMB?=
686LN MoizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYOwfoN3PzJiaB?= NYLT[Zh[TUN3ME2yMlA2KMLzIEGuN|Mh|ryP MY[yOVgyODBzMB?=
UM SCC-1 NEnUUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mly5O|IhcA>? Mn:0SWM2OD1zLk[3JOKyKDBwNEKg{txO MViyOVgyODBzMB?=
UM-22A MknzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDkS3ZvPzJiaB?= NH22VWVGSzVyPUGuN|IhyrFiMD6zPUDPxE1? M3\pXlI2QDFyMEGw
OSC19 NEXXbphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnkO2I4OiCq NXmwOlZrTUN3ME2xMlI3KMLzIECuNlAh|ryP M2XTRVI2QDFyMEGw
PCI-52 MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf3PXo4OiCq MlHFSWM2OD1zLkCwJOKyKDBwMEmg{txO MWeyOVgyODBzMB?=
PCI-15B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf6TVYyPzJiaB?= MnnBSWM2OD1yLkm5JOKyKDFwN{Sg{txO M1vlblI2QDFyMEGw
UMSCC-1 NHjldm9HfW6ldHnvckBCe3OjeR?= M{DmT|AvODByNT2xMlYh|ryP M{[5fFI1KGh? M2rVT4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkSyNlU5OTByMUC=
Cal33 NU[wWo5kTnWwY4Tpc44hSXO|YYm= M3TWblAvODByNT2zMlgh|ryP MmK2NlQhcA>? NE\QUZNi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NET0PJQzPThzMECxNC=>
HH5 NEHCOppHfW6ldHnvckBCe3OjeR?= NYn2VIlMOC5yMEC1MVMvQCEQvF2= M2jvTFI1KGh? MoT0ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFnYTZYzPThzMECxNC=>
UM-22A NUT1WZdlTnWwY4Tpc44hSXO|YYm= NGXJcnYxNjByMEWtNU43KM7:TR?= MlzaNlQhcA>? NHrMWVdi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4DPVVI2QDFyMEGw
A1847 NX;3U49{TnWwY4Tpc44hSXO|YYm= MoTVNE4xPS1zMDFOwG0> NHrlR4EzPCCq MlfGSG1UV8Li MmLZdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NYDmU|FWOjV4NE[wNVU>
OVCAR-5 MlLGSpVv[3Srb36gRZN{[Xl? M4KyVVAvODVvMUCg{txO M3KwSFI1KGh? M33hbWROW00EoB?= NImzbopz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MUWyOVY1PjBzNR?=
OVCAR-8 Mn3rSpVv[3Srb36gRZN{[Xl? MluxNE4xPS1zMDFOwG0> NH\ZVIozPCCq MVHEUXNQyqB? MWry[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NFLk[nEzPTZ2NkCxOS=>
MOVCAR-5447 MXTGeY5kfGmxbjDBd5NigQ>? M33neFAvODVvMUCg{txO MVqyOEBp NHLoOW5FVVORwrC= MkfidoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M3nkdFI2PjR4MEG1
MOVCAR-5009 M2LsTmZ2dmO2aX;uJGF{e2G7 NGHtbZkxNjB3LUGwJO69VQ>? Mm\5NlQhcA>? NWrE[YZnTE2VT9Mg NVrId3poemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M375OlI2PjR4MEG1
A1847 MkniR4VtdCCYaXHibYxqfHliQYPzZZk> M3f0OlAvODVvMUCg{txO NEfJNZc4OiCq M{fWTmROW09? MmG5doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= M{e0TFI2PjR4MEG1
OVCAR-5 M2nCfWNmdGxiVnnhZoltcXS7IFHzd4F6 Ml\5NE4xPS1zMDFOwG0> NWXGS2dxPzJiaB?= M362bmROW09? NXG1OVVuemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NGTsR5IzPTZ2NkCxOS=>
OVCAR-8  M1TVSmNmdGxiVnnhZoltcXS7IFHzd4F6 MnW0NE4xPS1zMDFOwG0> NVLyU3h1PzJiaB?= M33pS2ROW09? M4S3RZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN M{GxTlI2PjR4MEG1
OVCAR-5  NVnhO3ZMSXCxcITvd4l{KEG|c3H5 M3P6clAvPS9zL{Wg{txO NYm5Z446PDhiaB?= NHO4SHdFVVOR MlvTbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= M3jLXFI2PjR4MEG1
OVCAR-8  MljmRZBweHSxc3nzJGF{e2G7 MUmwMlUwOS93IN88US=> NHroSno1QCCq NWDmUZgzTE2VTx?= NFv4OVVqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u M3;6flI2PjR4MEG1
AKRSL NIrCcXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MW[3NkBp M4jtSWlEPTExvK6xNEDPxE1? NIi3[HgzPTVyNE[zOS=>
PALJDL MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NILEVos4OiCq NYD3XVNIUUN3ME2yMlQh|ryP NULqNZpsOjV3MES2N|U>
MO4 NGTsT4dHfW6ldHnvckBCe3OjeR?= MWSwMlUwOS93IN88US=> NYLzOpBXPiCq MUTpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> MUiyOVE1QTV|NR?=
DU145  MmjYSpVv[3Srb36gRZN{[Xl? MnXqNE0zODBibl2= NYL6c2xmOSCqwrC= NUmxUndCe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> NGXVTmEzPDV5N{m0Ni=>
DU145  M2\zW2Z2dmO2aX;uJGF{e2G7 M2KyXVgxOCCwTR?= MV:3NkBp NFGwR3d{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= MVqyOFU4Pzl2Mh?=
CWR22Rv1 NFv5eFJHfW6ldHnvckBCe3OjeR?= MWC4NFAhdk1? NH35dHA4OiCq NUS2eJRZe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 MYqyOFU4Pzl2Mh?=
N592 NFv0UpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHGU2loUUN3ME2wMlg1KM7:TR?= MYOyOFE2QDdyMR?=
H82 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELUe4VKSzVyPUGuN|ch|ryP NHjjSIczPDF3OEewNS=>
GLC4 M3rl[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq3TWM2OD1zLke5JO69VQ>? MnHHNlQyPTh5MEG=
H526 M{\h[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTNwMEig{txO M3;pU|I1OTV6N{Cx
H1173 Mn3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXsTWM2OD1{LkO5JO69VQ>? MUGyOFE2QDdyMR?=
DMS114 M4jWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwN{Og{txO NWTROmF4OjRzNUi3NFE>
NCI-N592 MVjGeY5kfGmxbjDBd5NigQ>? MWSwMlMwOS9|IN88US=> NYnrelV{OjRiaB?= MnftbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MWOyOFE2QDdyMR?=
GLC4 NVrmNIN3TnWwY4Tpc44hSXO|YYm= NX\wbYZ6OC5|L{GvN{DPxE1? MViyOEBp MVzpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NY\rfpY1OjRzNUi3NFE>
NCI-H82 NUS1V3I{TnWwY4Tpc44hSXO|YYm= Mn3ENE4{NzFxMzFOwG0> MnrnNlQhcA>? M3Wzbolv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Ml3pNlQyPTh5MEG=
NCI-N592 NUPzZppOSXCxcITvd4l{KEG|c3H5 MYSwMlMwOS9|IN88US=> NVfQXWdxPDhiaB?= M2nTUIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NVfnZVZROjRzNUi3NFE>
GLC4 MVjBdI9xfG:|aYOgRZN{[Xl? NUfJTWtpOC5|L{GvN{DPxE1? NEToPI01QCCq NWK4clR3cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= M4\XeFI1OTV6N{Cx
NCI-H82 MnPDRZBweHSxc3nzJGF{e2G7 MYewMlMwOS9|IN88US=> MUe0PEBp NXq1NWplcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NInLfYwzPDF3OEewNS=>
CWR22Rv1  M1H5fWFxd3C2b4Ppd{BCe3OjeR?= Ml3HTWM2OD1yLkS4NkDPxE1? NXvkPHNsOjN7NEKwPVU>
CWR22Pc MULBdI9xfG:|aYOgRZN{[Xl? NHLJTZJKSzVyPUCuOFM5KM7:TR?= NHHiS4szOzl2MkC5OS=>
PC-3 M3rQRWFxd3C2b4Ppd{BCe3OjeR?= MnvHTWM2OD1zLke1OUDPxE1? NUjMUY5yOjN7NEKwPVU>
DU145 NHrPdXRCeG:ydH;zbZMhSXO|YYm= NF;3c41KSzVyPUOuOVE4KM7:TR?= NVu0RoNSOjN7NEKwPVU>
RC165N NID3S3NCeG:ydH;zbZMhSXO|YYm= NX2xdXNnUUN3ME2yMlA5OyEQvF2= NYHWd5JyOjN7NEKwPVU>
ARPE19 NXLpZoc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nkU2ROW09? MWjJR|UxRTJ2LkO4JO69VQ>? M4n0UlI{PTNzOUKx
HEK293 MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPEUXNQ MVXJR|UxRThwNkeg{txO M3fVblI{PTNzOUKx
KCNR NYXZWZpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonqSG1UVw>? NWH2V|RvUUN3ME2wMlQ3KM7:TR?= NE\DemkzOzV|MUmyNS=>
SY5Y MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PX[GROW09? M4LJOmlEPTB;MD6zOkDPxE1? NFj2O|QzOzV|MUmyNS=>
BE2 MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\EUXNQ NHzpRmFKSzVyPUCuO|Eh|ryP M1zKTlI{PTNzOUKx
AS NIG5SnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\wd2dFVVOR M4HFXWlEPTB;MT61N{DPxE1? M1jteFI{PTNzOUKx
NGP NIruXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETNUWFFVVOR MVHJR|UxRTBwNU[g{txO NYrnRYVuOjN3M{G5NlE>
IMR32 M3fveGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPWSG1UVw>? NXzjeVhJUUN3ME2wMlY3KM7:TR?= NIHwXZQzOzV|MUmyNS=>
LAN5 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvEUXNQ Mk\mTWM2OD1zLkC0JO69VQ>? NXHK[pRPOjN3M{G5NlE>
RH18 MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r6UWROW09? MUfJR|UxRTFwNEKg{txO NVP3cW5YOjN3M{G5NlE>
RH30 Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4naXmROW09? M4fSW2lEPTB;MT6yOUDPxE1? MYeyN|U{OTl{MR?=
RH17 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzjN4xJTE2VTx?= NXrielc5UUN3ME2yMlUyKM7:TR?= NYjafmM3OjN3M{G5NlE>
RH28 M1u5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHnN3V[TE2VTx?= Mnf5TWM2OD12LkK4JO69VQ>? MV2yN|U{OTl{MR?=
RH36 M3;WOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjHZVhFVVOR M3;pd2lEPTB;NT6zO{DPxE1? NGrGWpUzOzV|MUmyNS=>
RH41 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITkOZhFVVOR M1[wd2lEPTB;MD60PEDPxE1? NU\CU29EOjN3M{G5NlE>
RD MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\qXGdJTE2VTx?= NIPnPXFKSzVyPUSuN|Ih|ryP MV2yN|U{OTl{MR?=
TC32 NF7KeYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz6W5ZFVVOR M1LWVGlEPTB;Mz64OUDPxE1? NF[5d2QzOzV|MUmyNS=>
TC71 NXnLSYhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PyXWROW09? NUXJTIJTUUN3ME20MlM{KM7:TR?= NVTQO2x7OjN3M{G5NlE>
KCNR NVLkTppGSXCxcITvd4l{KEG|c3H5 M1rSfVAvPS9zLkCvNk42KM7:TR?= MnrhNlQhcA>? MYHEUXNQ NYW3dJpycW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NVf6TWJjOjN3M{G5NlE>
SY5Y M1HSZmFxd3C2b4Ppd{BCe3OjeR?= NYH3O5Z1OC53L{GuNE8zNjVizszN M37nc|I1KGh? NXvtVXhPTE2VTx?= MXvpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NFTFflIzOzV|MUmyNS=>
Rh18 NIjGW4FCeG:ydH;zbZMhSXO|YYm= MX[wMlUwOS5yL{KuOUDPxE1? MkPXNlQhcA>? Mn7lSG1UVw>? NUPJR4E1cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NXzM[IFqOjN3M{G5NlE>
TC32 M4\MbWFxd3C2b4Ppd{BCe3OjeR?= NFL1VHoxNjVxMT6wM|IvPSEQvF2= MUmyOEBp MVPEUXNQ NGToNINqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MkPJNlM2OzF7MkG=
KCNR NGfzUIxHfW6ldHnvckBCe3OjeR?= NV7BTlhROC53L{GuNE8zNjVxNTFOwG0> MYWyOEBp MoTWSG1UVw>? MX\pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NYjWfopYOjN3M{G5NlE>
SY5Y Mm\MSpVv[3Srb36gRZN{[Xl? NWHTRpF4OC53L{GuNE8zNjVxNTFOwG0> MkPINlQhcA>? NGL3emxFVVOR M1m5V4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NE\qTVYzOzV|MUmyNS=>
Rh18 NXrnOolCTnWwY4Tpc44hSXO|YYm= NH3aZnAxNjVxMT6wM|IvPS93IN88US=> NGXlUWczPCCq MnzjSG1UVw>? MYXpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NHu4T|UzOzV|MUmyNS=>
TC32 MUHGeY5kfGmxbjDBd5NigQ>? M2OwNlAvPS9zLkCvNk42NzVizszN MWGyOEBp MXvEUXNQ NXz0XpNjcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NV3LT5pFOjN3M{G5NlE>
TPC-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\WNUDDvU1? M2HnWVAuPCCm NE\ne2dFVVOR M3H3VolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? NUPMbG1kOjNyNU[0PVk>
MZ-CRC1  NUnmPWFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET0NmwyKML3TR?= MYCwMVUh\A>? M1fOcWROW09? M{fZO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NYrDUm43OjNyNU[0PVk>
TT  MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vBeVEhyrWP NICwRWMxNTRiZB?= MWjEUXNQ MknWbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? Mnu2NlMxPTZ2OUm=
TPC-1 M3fZdWZ2dmO2aX;uJGF{e2G7 NHXlSpgyKML3TR?= NXi0[Yl4PzJiaB?= NX7zRnZjTE2VTx?= NW\ZZWp6cW6mdXPld{BIOSCkbH;jb4Fo\Q>? MoLwNlMxPTZ2OUm=
MZ-CRC1  MUTGeY5kfGmxbjDBd5NigQ>? MXGxJOK2VQ>? M4LRfVczKGh? NWXTT5pyTE2VTx?= NXvPW3NJcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MUCyN|A2PjR7OR?=
TT  NEfFTFZHfW6ldHnvckBCe3OjeR?= NIrsfIcyKML3TR?= NVjDcnNVPzJiaB?= MVzEUXNQ NIjIVG9qdmS3Y3XzJGcyKGKub3PrZYdm NXnRWYlsOjNyNU[0PVk>
MZ-CRC1  MkTHRZBweHSxc3nzJGF{e2G7 MnrnNUDDvU1? M{HJNlQ5KGh? M1\MNWROW09? MX3pcoR2[2W|IHHwc5B1d3Orcx?= NIjr[pMzOzB3NkS5PS=>
TT  NHL0Z5dCeG:ydH;zbZMhSXO|YYm= MWCxJOK2VQ>? NYnNRXo5PDhiaB?= M2e3XWROW09? MmPhbY5lfWOnczDhdI9xfG:|aYO= MmfQNlMxPTZ2OUm=
HD-LM2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HtcFcz6oDLaB?= NF\ReFVFVVOR NH\kS3dKSzVyPUeuPFQ1KM7:TR?= NYf5PZdNOjJ6MkmwPVQ>
L-428 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPCdVZPPzMkgJno Ml33SG1UVw>? NIfWXodKSzVyPUeuPVQ4KM7:TR?= M1;rV|IzQDJ7MEm0
KM-H2 M{XmTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXrT5J5PzMkgJno M1vIWGROW09? MVnJR|UxRTFwM{C4JO69VQ>? NWnwblh[OjJ6MkmwPVQ>
L-540 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLlO|LjiImq NGq0RXRFVVOR NEHD[|FKSzVyPUiuNlE3KM7:TR?= MX:yNlgzQTB7NB?=
HD-LM2 MXzGeY5kfGmxbjDBd5NigQ>? Ml:2NE4yNzBwNT:xM|Uh|ryP NW\RcIdKPzMkgJno MUHEUXNQ M3;5fIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NIrjRoQzOjh{OUC5OC=>
L-428 NW\OfGVCTnWwY4Tpc44hSXO|YYm= MUGwMlEwOC53L{GvOUDPxE1? MX63NwKBkWh? NXnGeldITE2VTx?= Ml;pbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NWj5XJpSOjJ6MkmwPVQ>
KM-H2 NX3NVHp{TnWwY4Tpc44hSXO|YYm= MoDXNE4yNzBwNT:xM|Uh|ryP MlXTO|LjiImq NVfofmhiTE2VTx?= NWjJ[FhFcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NGLmbmszOjh{OUC5OC=>
L-540 MoLnSpVv[3Srb36gRZN{[Xl? MmjuNE4yNzBwNT:xM|Uh|ryP MljLO|LjiImq NFfRTY5FVVOR NWj5SlFWcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? M1XWbFIzQDJ7MEm0
HD-LM2 M4f5PGFxd3C2b4Ppd{BCe3OjeR?= M334b|EwPSEQvF2= M1q0fFcz6oDLaB?= MoXaSG1UVw>? NVPlbYtHcW6mdXPld{BieG:ydH;zbZM> NX;pcFZzOjJ6MkmwPVQ>
L-428 M1XrbWFxd3C2b4Ppd{BCe3OjeR?= NXLs[5hqOS93IN88US=> NUT5SYlDPzMkgJno M13WVmROW09? M{\YO4lv\HWlZYOgZZBweHSxc3nz NULIO2hJOjJ6MkmwPVQ>
KM-H2 Mn\QRZBweHSxc3nzJGF{e2G7 MXyxM|Uh|ryP NVnaNZRKPzMkgJno MkjDSG1UVw>? NV3ITnVWcW6mdXPld{BieG:ydH;zbZM> MkW0NlI5OjlyOUS=
L-540 MoW4RZBweHSxc3nzJGF{e2G7 NEPFSFAyNzVizszN M{T0[|cz6oDLaB?= MVfEUXNQ Mni0bY5lfWOnczDhdI9xfG:|aYO= M2XadFIzQDJ7MEm0
U251-MG MWfGeY5kfGmxbjDBd5NigQ>? MWixJOK2VQ>? NUL5cGx5OC1zNjDo MnXkbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MmjENlIxOjd4OUG=
U87-MG NGq3fYJHfW6ldHnvckBCe3OjeR?= M1O3V|EhyrWP M{jUVlAuOTZiaB?= NFXQZoNqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? M1PYOVIzODJ5Nkmx
4C8 MWrGeY5kfGmxbjDBd5NigQ>? MoTsNUDDvU1? MoXaNE0yPiCq NYPrV2JicW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NX3KcZRXOjJyMke2PVE>
U251-MG NFuzV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSxM|ExKML3TR?= M4fHW|I1NzR6L{eyJIg> NEKzOnBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NVToXXoyOjJyMke2PVE>
U87-MG Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[xM|ExKML3TR?= NHHueWIzPC92OD:3NkBp MoHtbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> MVKyNlAzPzZ7MR?=
4C8 M2nTd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxM|ExKML3TR?= NEK2RoczPC92OD:3NkBp MnPtbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> MUCyNlAzPzZ7MR?=
U266 MnGyRZBweHSxc3nzJGF{e2G7 M1P6e|AvPS1{IN88US=> NVHOVGdDPDhxN{KgbC=> MoTUbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NFzZSlkzOTF4NEWxOy=>
Kms.11 NF3WWGxCeG:ydH;zbZMhSXO|YYm= MXqwMlUuOiEQvF2= MkjqOFgwPzJiaB?= NFTJZXpqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NYTscnBZOjFzNkS1NVc>
8226 MVfBdI9xfG:|aYOgRZN{[Xl? NWCyeoZWOC53LUKg{txO NVn5eoNLPDhxN{KgbC=> MYPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NXnZVJVxOjFzNkS1NVc>

... 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
In vivo AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. [1] In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. [3]AZD1480 blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis and metastasis in a human xenograft tumor model. [4] The Jak2 inhibitor, AZD1480, suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity. [5]

Protocol

Kinase Assay:[5]
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kinase assays:

Inhibition studies of AZD1480 are performed using recombinant Jak1, Jak2, or Jak3 under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/ml BSA, and 10 mM MgCl2. Jak3 enzyme is expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes are assayed in the presence of AZD1480 (10 point dose response, in triplicate, from 8.3 μM to 0.3 nM in half-log dilution steps) using 1.5 μM peptide substrate (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 and Jak3: FAM-SRCtide) and screened under their respective ATP Km (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) and approximated physiological ATP concentration of 5 mM. Phosphorylated and unphosphorylated peptides are separated and quantified by a Caliper LC3000 system for calculating percent inhibition.
Cell Research:[4]
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  • Cell lines: Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs
  • Concentrations: ~1 μM
  • Incubation Time: 48 or 24 hours
  • Method: Renca or 786-O cells are suspended in DMEM medium with 5% FBS , and seeded in 96-well plates (5×103 per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 hours. Cell viability is determined by MTS assay. Absorbance at 490 nm is measured with Mikrotek Laborsysteme. Mouse endothelial cells and splenic CD11b+/c- myeloid cells are enriched from tumor-bearing mice,and cultured in 5% FBS RPMI-1640 medium. HUVECs are cultured on collagen 1–coated plates in complete medium. All cells are treated with DMSO and AZD1480 at various doses for 24 hours. Cell viability is determined by counting cell number manually. All the experiments are repeated 3 times.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Female BALB/c and athymic nude (NCR - nu/nu) mice (7–8 weeks old)
  • Formulation: AZD1480 is suspended in water supplemented with 0.5% hypromellose and 0.1% Tween 80.
  • Dosages: Once a day at the dose of 50 mg/kg or twice daily at 30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL warmed (197.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 348.77
Formula

C14H14ClFN8

CAS No. 935666-88-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(NC1=NC=C(Cl)C(=N1)NC2=N[NH]C(=C2)C)C3=NC=C(F)C=N3

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID