AZD1480

Catalog No.S2162

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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In DMSO USD 130 In stock
USD 100 In stock
USD 170 In stock
USD 570 In stock
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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 MVLGeY5kfGmxbjDBd5NigQ>? NGP1WIU2KM7:TR?= NFWyOIk1QCCq NIrqVnpFVVOR MnnOZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n MXSyOVk2PDl5NB?=
LoVo  MUjGeY5kfGmxbjDBd5NigQ>? NF\wVI82KM7:TR?= MYC0PEBp NIe0[I9FVVOR M1jGNoJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> NXTaWYpSOjV7NUS5O|Q>
HN5 NX3yNXNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HU[|czKGh? MnnwSWM2OD1|LkixJOKyKDFwOUmg{txO MYKyOVgyODBzMB?=
Cal33 M2fVTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13USFczKGh? NI[xcYxGSzVyPUOuN|chyrFiMD63OUDPxE1? Mn65NlU5OTByMUC=
UM-22B Ml\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\lVpA4OiCq NI\IbHhGSzVyPUKuOlYhyrFiMD6yOEDPxE1? M1;yRVI2QDFyMEGw
686LN MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPINY44OiCq MmfXSWM2OD1{LkC1JOKyKDFwM{Og{txO NF7h[3IzPThzMECxNC=>
UM SCC-1 MlLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ztfFczKGh? NYTKNmRuTUN3ME2xMlY4KMLzIECuOFIh|ryP NU\H[HVWOjV6MUCwNVA>
UM-22A MmOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DxUVczKGh? M3;tNmVEPTB;MT6zNkDDuSByLkO5JO69VQ>? NHLtS3ozPThzMECxNC=>
OSC19 MnnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:3NkBp M{fIbmVEPTB;MT6yOkDDuSByLkKwJO69VQ>? NXrqNXNZOjV6MUCwNVA>
PCI-52 M4juWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljNO|IhcA>? MVfFR|UxRTFwMECgxtEhOC5yOTFOwG0> M4\jXlI2QDFyMEGw
PCI-15B Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITC[nc4OiCq MYTFR|UxRTBwOUmgxtEhOS55NDFOwG0> NHnS[|AzPThzMECxNC=>
UMSCC-1 MV;GeY5kfGmxbjDBd5NigQ>? MWewMlAxODVvMT62JO69VQ>? NFn2SWUzPCCq M3LETIFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYSyOVgyODBzMB?=
Cal33 NGn5U2xHfW6ldHnvckBCe3OjeR?= NUXiRVFnOC5yMEC1MVMvQCEQvF2= NV;T[VZ6OjRiaB?= MmrCZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUOyOVgyODBzMB?=
HH5 NXTiTId{TnWwY4Tpc44hSXO|YYm= NGLQfmgxNjByMEWtN{45KM7:TR?= NHntXIgzPCCq MmjaZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHz1cm0zPThzMECxNC=>
UM-22A Mn\qSpVv[3Srb36gRZN{[Xl? NYnndpVNOC5yMEC1MVEvPiEQvF2= NH3sOnEzPCCq NWr0cFBp[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF[0fmUzPThzMECxNC=>
A1847 NH7Od5NHfW6ldHnvckBCe3OjeR?= NITJb3YxNjB3LUGwJO69VQ>? Mn\1NlQhcA>? NYXlTldbTE2VT9Mg NI\QUnBz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M1TSTFI2PjR4MEG1
OVCAR-5 MXPGeY5kfGmxbjDBd5NigQ>? NYPO[JZxOC5yNT2xNEDPxE1? M{[3UVI1KGh? Mof6SG1UV8Li M1fEeJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NXXITGNNOjV4NE[wNVU>
OVCAR-8 NXnNZZNLTnWwY4Tpc44hSXO|YYm= NIHmelIxNjB3LUGwJO69VQ>? MYeyOEBp NWfMeWJyTE2VT9Mg NHXRRpRz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MV2yOVY1PjBzNR?=
MOVCAR-5447 MmrnSpVv[3Srb36gRZN{[Xl? NU\hcIt5OC5yNT2xNEDPxE1? M2LnTVI1KGh? Mkn4SG1UV8Li NEHEdVhz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NUfBUZc{OjV4NE[wNVU>
MOVCAR-5009 MXrGeY5kfGmxbjDBd5NigQ>? MYKwMlA2NTFyIN88US=> MVmyOEBp NVrKTohoTE2VT9Mg MV3y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= Ml2xNlU3PDZyMUW=
A1847 Mm\kR4VtdCCYaXHibYxqfHliQYPzZZk> MorvNE4xPS1zMDFOwG0> MX23NkBp Mn62SG1UVw>? M2TmPZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MWCyOVY1PjBzNR?=
OVCAR-5 NVvmW5Z7S2WubDDWbYFjcWyrdImgRZN{[Xl? MX[wMlA2NTFyIN88US=> NHe3NmY4OiCq NWrrRYo4TE2VTx?= NVHofI9NemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NIjHdWQzPTZ2NkCxOS=>
OVCAR-8  Mk\sR4VtdCCYaXHibYxqfHliQYPzZZk> NFfzS3ExNjB3LUGwJO69VQ>? NHzLV4Y4OiCq MoLhSG1UVw>? M3HCdpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN NWPLPJpWOjV4NE[wNVU>
OVCAR-5  Mm\TRZBweHSxc3nzJGF{e2G7 M3nNUlAvPS9zL{Wg{txO NVLJTW1{PDhiaB?= NXT6PJFyTE2VTx?= MVzpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w MnTLNlU3PDZyMUW=
OVCAR-8  NYG1T2p3SXCxcITvd4l{KEG|c3H5 MWewMlUwOS93IN88US=> Mn\WOFghcA>? Mk\hSG1UVw>? M3zLNIlv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= M4njd|I2PjR4MEG1
AKRSL MoPsR4VtdCCYaXHibYxqfHliQYPzZZk> MnTFO|IhcA>? NX\DXZlpUUN3MP-8olExKM7:TR?= MnTNNlU2ODR4M{W=
PALJDL MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWrnXZhuPzJiaB?= NV:4PXk6UUN3ME2yMlQh|ryP M2nEZVI2PTB2NkO1
MO4 MUfGeY5kfGmxbjDBd5NigQ>? M1zGdFAvPS9zL{Wg{txO MXy2JIg> NIX0b25qdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NUHSN3Z7OjVzNEm1N|U>
DU145  M3fXS2Z2dmO2aX;uJGF{e2G7 NWTrTFNmOC1{MECgcm0> MUCxJIjDqA>? NEP6fGl{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NXO1XlFpOjR3N{e5OFI>
DU145  MYDGeY5kfGmxbjDBd5NigQ>? M{DiTlgxOCCwTR?= MlfwO|IhcA>? MmLLd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 MX:yOFU4Pzl2Mh?=
CWR22Rv1 NX7nSo1rTnWwY4Tpc44hSXO|YYm= MoLQPFAxKG6P MojrO|IhcA>? NE\FdZV{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NUDXbJJkOjR3N{e5OFI>
N592 NXXwfG83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwOESg{txO MVqyOFE2QDdyMR?=
H82 NIfZOpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHNO4ZKSzVyPUGuN|ch|ryP M2\ybFI1OTV6N{Cx
GLC4 MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFwN{mg{txO M3TsRlI1OTV6N{Cx
H526 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTNwMEig{txO MV[yOFE2QDdyMR?=
H1173 Ml[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLxTWM2OD1{LkO5JO69VQ>? MlH1NlQyPTh5MEG=
DMS114 NIXXPXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX1SHlKSzVyPUCuO|Mh|ryP M4jKelI1OTV6N{Cx
NCI-N592 M3LXNGZ2dmO2aX;uJGF{e2G7 NE\TO2ExNjNxMT:zJO69VQ>? NV3aUIlIOjRiaB?= MVXpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NW\WXmtrOjRzNUi3NFE>
GLC4 NXTHeVB3TnWwY4Tpc44hSXO|YYm= M1T3V|AvOy9zL{Og{txO MlvWNlQhcA>? MoLPbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NF7tXG0zPDF3OEewNS=>
NCI-H82 NYjX[GdWTnWwY4Tpc44hSXO|YYm= NFXIUGYxNjNxMT:zJO69VQ>? M{LP[FI1KGh? NXfifmllcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NFrZRoIzPDF3OEewNS=>
NCI-N592 M{mwN2Fxd3C2b4Ppd{BCe3OjeR?= MV2wMlMwOS9|IN88US=> MVi0PEBp MV7pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MnPYNlQyPTh5MEG=
GLC4 NWP5OFRKSXCxcITvd4l{KEG|c3H5 NYfmdnl6OC5|L{GvN{DPxE1? MYW0PEBp MlP1bY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NVfnRpZOOjRzNUi3NFE>
NCI-H82 MW\BdI9xfG:|aYOgRZN{[Xl? M{TyeVAvOy9zL{Og{txO NG\rUGU1QCCq M1zoVolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NXfmfIplOjRzNUi3NFE>
CWR22Rv1  MnjURZBweHSxc3nzJGF{e2G7 NHryNlRKSzVyPUCuOFgzKM7:TR?= MnfjNlM6PDJyOUW=
CWR22Pc MlvoRZBweHSxc3nzJGF{e2G7 NGXsfIhKSzVyPUCuOFM5KM7:TR?= NVXPXXUyOjN7NEKwPVU>
PC-3 NFX5XlhCeG:ydH;zbZMhSXO|YYm= Mlq3TWM2OD1zLke1OUDPxE1? MXyyN|k1OjB7NR?=
DU145 MkjiRZBweHSxc3nzJGF{e2G7 MmW2TWM2OD1|LkWxO{DPxE1? M3e3PFI{QTR{MEm1
RC165N NGfRNWNCeG:ydH;zbZMhSXO|YYm= MUfJR|UxRTJwMEizJO69VQ>? NHLQUWYzOzl2MkC5OS=>
ARPE19 M1nKO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nUXWROW09? MoDBTWM2OD1{ND6zPEDPxE1? NYTnPZM4OjN3M{G5NlE>
HEK293 NUPtXm9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnp[WNUTE2VTx?= NVHQbFZ5UUN3ME24MlY4KM7:TR?= NH3u[JEzOzV|MUmyNS=>
KCNR NU\oSnQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGyVYo5TE2VTx?= NXT0OI1TUUN3ME2wMlQ3KM7:TR?= MYmyN|U{OTl{MR?=
SY5Y NIfRd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfIfnpXTE2VTx?= NWDMRYE1UUN3ME2wMlM3KM7:TR?= NXW1PI1QOjN3M{G5NlE>
BE2 NWG2OIFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX31W441TE2VTx?= NVzvNJAxUUN3ME2wMlcyKM7:TR?= M37ne|I{PTNzOUKx
AS MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzMSG1UVw>? NIOxV4ZKSzVyPUGuOVMh|ryP NWO1W4F4OjN3M{G5NlE>
NGP MoH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnyzSG1UVw>? NXL1OFB3UUN3ME2wMlU3KM7:TR?= NFzLfGgzOzV|MUmyNS=>
IMR32 M4TZc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfS[HZFVVOR NE\3eFlKSzVyPUCuOlYh|ryP MYSyN|U{OTl{MR?=
LAN5 M4f5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\VPZZFVVOR NIXnXYtKSzVyPUGuNFQh|ryP M1;zNFI{PTNzOUKx
RH18 NXK2SVYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7sRpFFVVOR NF;UVmRKSzVyPUGuOFIh|ryP NGLqVlUzOzV|MUmyNS=>
RH30 NGewb2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHn0WY5FVVOR NHvrVGpKSzVyPUGuNlUh|ryP M2L4VlI{PTNzOUKx
RH17 NXPUW4MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\XSG1UVw>? NYLqTZc{UUN3ME2yMlUyKM7:TR?= MofGNlM2OzF7MkG=
RH28 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvkO5VITE2VTx?= NGfoOI1KSzVyPUSuNlgh|ryP MoXmNlM2OzF7MkG=
RH36 M1XIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvTSG1UVw>? M1zmXWlEPTB;NT6zO{DPxE1? NWCxXGQ2OjN3M{G5NlE>
RH41 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXT0dXBMTE2VTx?= MnrmTWM2OD1yLkS4JO69VQ>? MlLaNlM2OzF7MkG=
RD M{XpSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPEUXNQ NX\vSnVWUUN3ME20MlMzKM7:TR?= M1LZWFI{PTNzOUKx
TC32 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3QSG1UVw>? M1jBfGlEPTB;Mz64OUDPxE1? M3;pZlI{PTNzOUKx
TC71 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTEUXNQ MXvJR|UxRTRwM{Og{txO M3HGd|I{PTNzOUKx
KCNR NUfvWGFJSXCxcITvd4l{KEG|c3H5 M4fWXlAvPS9zLkCvNk42KM7:TR?= M1Lwb|I1KGh? MXvEUXNQ NEPuNVlqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MY[yN|U{OTl{MR?=
SY5Y NGrhXHVCeG:ydH;zbZMhSXO|YYm= NILteocxNjVxMT6wM|IvPSEQvF2= M4rNXFI1KGh? NYixR3h2TE2VTx?= NFzzNZhqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NIDqVIUzOzV|MUmyNS=>
Rh18 MXPBdI9xfG:|aYOgRZN{[Xl? NIrKenMxNjVxMT6wM|IvPSEQvF2= MmnwNlQhcA>? M4OxN2ROW09? MVzpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NFzS[lYzOzV|MUmyNS=>
TC32 NH;tZXpCeG:ydH;zbZMhSXO|YYm= MkTSNE42NzFwMD:yMlUh|ryP NFHnS2EzPCCq M3X4RWROW09? MlXwbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NITXXXkzOzV|MUmyNS=>
KCNR NVrpc2ViTnWwY4Tpc44hSXO|YYm= MYewMlUwOS5yL{KuOU82KM7:TR?= NUTUXJZlOjRiaB?= M1LI[mROW09? NUnvfW5HcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> M4Dr[FI{PTNzOUKx
SY5Y M1rvdWZ2dmO2aX;uJGF{e2G7 MWKwMlUwOS5yL{KuOU82KM7:TR?= NGnve4wzPCCq M3G5VGROW09? MWnpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MXGyN|U{OTl{MR?=
Rh18 Mn7MSpVv[3Srb36gRZN{[Xl? NH\STVMxNjVxMT6wM|IvPS93IN88US=> NI\0SVczPCCq Ml7OSG1UVw>? NVm3XYppcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> M3vZeVI{PTNzOUKx
TC32 M2HHemZ2dmO2aX;uJGF{e2G7 MX6wMlUwOS5yL{KuOU82KM7:TR?= M{O3V|I1KGh? MYDEUXNQ NELrU41qdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> M4r0UlI{PTNzOUKx
TPC-1 MlLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxJOK2VQ>? NWLjVnFnOC12IHS= NHfiXVdFVVOR NGPNbXVqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAzKGRidILlZZRu\W62 M1\P[|I{ODV4NEm5
MZ-CRC1  MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOxJOK2VQ>? MkXSNE02KGR? M1S2NWROW09? M1GyOolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NF;GenUzOzB3NkS5PS=>
TT  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ux[|EhyrWP MVGwMVQh\A>? NH[wSIRFVVOR NXS2W5J2cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NHSzb5AzOzB3NkS5PS=>
TPC-1 NIjaSppHfW6ldHnvckBCe3OjeR?= MmKyNUDDvU1? M4f6e|czKGh? M{O1WGROW09? NHq1Z|FqdmS3Y3XzJGcyKGKub3PrZYdm MVyyN|A2PjR7OR?=
MZ-CRC1  MmXFSpVv[3Srb36gRZN{[Xl? NEHFb20yKML3TR?= M1PBOlczKGh? MXHEUXNQ MofNbY5lfWOnczDHNUBjdG:la3Hn[S=> MUKyN|A2PjR7OR?=
TT  M37TV2Z2dmO2aX;uJGF{e2G7 NYXlTFhHOSEEtV2= NVPBcVI2PzJiaB?= M2PtbGROW09? MmjwbY5lfWOnczDHNUBjdG:la3Hn[S=> NIX1R3UzOzB3NkS5PS=>
MZ-CRC1  NF\kWXlCeG:ydH;zbZMhSXO|YYm= NH\hRo4yKML3TR?= Mk\uOFghcA>? MmLLSG1UVw>? MVrpcoR2[2W|IHHwc5B1d3Orcx?= MX6yN|A2PjR7OR?=
TT  NV6zTnh1SXCxcITvd4l{KEG|c3H5 MWOxJOK2VQ>? MlvFOFghcA>? NW[3WIhTTE2VTx?= NXTud3U5cW6mdXPld{BieG:ydH;zbZM> NYDifZp7OjNyNU[0PVk>
HD-LM2 MojmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLkc4h4PzMkgJno M2HofGROW09? NVfkNWljUUN3ME23Mlg1PCEQvF2= MVyyNlgzQTB7NB?=
L-428 NG\1b3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXFflg5PzMkgJno MkTkSG1UVw>? MV\JR|UxRTdwOUS3JO69VQ>? M3OwTVIzQDJ7MEm0
KM-H2 M1ftc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrnenk4OuLCiXi= MmqwSG1UVw>? NXLDepVFUUN3ME2xMlMxQCEQvF2= MVKyNlgzQTB7NB?=
L-540 M1i4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXKc3o4OuLCiXi= NY\WNWNqTE2VTx?= MWPJR|UxRThwMkG2JO69VQ>? NUPDNJBVOjJ6MkmwPVQ>
HD-LM2 NHzjSIFHfW6ldHnvckBCe3OjeR?= NHO2NpQxNjFxMD61M|EwPSEQvF2= NFj1VWc4OuLCiXi= M3nw[2ROW09? MWnpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NGrhc3YzOjh{OUC5OC=>
L-428 MkK0SpVv[3Srb36gRZN{[Xl? M{DDPFAvOS9yLkWvNU82KM7:TR?= NVTJ[G9{PzMkgJno NY[xd|NxTE2VTx?= MXfpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MUGyNlgzQTB7NB?=
KM-H2 MlHDSpVv[3Srb36gRZN{[Xl? NGO1SHkxNjFxMD61M|EwPSEQvF2= MXe3NwKBkWh? NG\aUmRFVVOR MmTjbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NX[2SZpzOjJ6MkmwPVQ>
L-540 NGHwfJNHfW6ldHnvckBCe3OjeR?= NFHiRlAxNjFxMD61M|EwPSEQvF2= NV7zNpF1PzMkgJno MmfzSG1UVw>? MVrpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> M2fab|IzQDJ7MEm0
HD-LM2 NEPkeWlCeG:ydH;zbZMhSXO|YYm= NXjBRoVXOS93IN88US=> M4PuV|cz6oDLaB?= M{DFSGROW09? Mn3QbY5lfWOnczDhdI9xfG:|aYO= MUGyNlgzQTB7NB?=
L-428 NFLYbXhCeG:ydH;zbZMhSXO|YYm= MkXtNU82KM7:TR?= Mk\IO|LjiImq MYHEUXNQ MoLUbY5lfWOnczDhdI9xfG:|aYO= M1q0c|IzQDJ7MEm0
KM-H2 NYrXcnJZSXCxcITvd4l{KEG|c3H5 NWjPUJZJOS93IN88US=> MUC3NwKBkWh? MlPDSG1UVw>? MVzpcoR2[2W|IHHwc5B1d3Orcx?= M4L1OVIzQDJ7MEm0
L-540 M3XBbGFxd3C2b4Ppd{BCe3OjeR?= M2jjXlEwPSEQvF2= NVzsb5ZHPzMkgJno NVzrRWh7TE2VTx?= MoH4bY5lfWOnczDhdI9xfG:|aYO= M1nPb|IzQDJ7MEm0
U251-MG NULJbo0xTnWwY4Tpc44hSXO|YYm= M3G2c|EhyrWP NH36PVYxNTF4IHi= MXzpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> Mo\oNlIxOjd4OUG=
U87-MG MYXGeY5kfGmxbjDBd5NigQ>? NF3i[2YyKML3TR?= NGjXPJkxNTF4IHi= M{XUdYlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? M3m1SVIzODJ5Nkmx
4C8 NF;4VolHfW6ldHnvckBCe3OjeR?= MoCyNUDDvU1? MW[wMVE3KGh? M4rsU4lvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? MVmyNlAzPzZ7MR?=
U251-MG NXHjXIRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHS1RooyNzFyINM1US=> MmLGNlQwPDhxN{KgbC=> M3XoTYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NU\pNGtCOjJyMke2PVE>
U87-MG Mn\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTBNU8yOCEEtV2= NFPmSXczPC92OD:3NkBp M3v2N4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO M{L6O|IzODJ5Nkmx
4C8 NVzR[llXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnONVlrOS9zMDFCuW0> M1;IdFI1NzR6L{eyJIg> MXHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NFrmc3kzOjB{N{[5NS=>
U266 NELGOnJCeG:ydH;zbZMhSXO|YYm= NFPvTlIxNjVvMjFOwG0> MWS0PE84OiCq M3Hkb4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NIDBUHozOTF4NEWxOy=>
Kms.11 NH;JUmtCeG:ydH;zbZMhSXO|YYm= M3nSPVAvPS1{IN88US=> M3nPNVQ5Nzd{IHi= MmnhbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MUGyNVE3PDVzNx?=
8226 NYDJVVU6SXCxcITvd4l{KEG|c3H5 NILhZpYxNjVvMjFOwG0> MkHsOFgwPzJiaB?= NFP0VYZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M3rGTlIyOTZ2NUG3

... 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

Bio Calculators

Molarity Calculator

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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).

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    C8=C7/X C8: LOG(C8):
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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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JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

  • Pan JAK Inhibitor

    Ruxolitinib (INCB018424) : Pan JAK1/2 inhibitor, IC50=3.3 nM/2.8 nM.

  • FDA-approved JAK Inhibitor

    Tofacitinib (CP-690550,Tasocitinib) : Approved by FDA for rheumatoid arthritis (RA).

  • Newest JAK Inhibitor

    XL019 New : Potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2.

  • Classic JAK Inhibitor

    AG-490 (Tyrphostin B42) : Potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 1/2.

Related JAK Products

  • FLLL32 New

    FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.

  • Cerdulatinib (PRT062070, PRT2070) New

    Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

  • Ruxolitinib (INCB018424)

    Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

  • Tofacitinib (CP-690550) Citrate

    Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively.

  • Tofacitinib (CP-690550,Tasocitinib)

    Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.

  • Fedratinib (SAR302503, TG101348)

    Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.

  • Momelotinib (CYT387)

    Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.

  • WP1066

    WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.

    Features:Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.

  • Baricitinib (LY3009104, INCB028050)

    Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID