AZD1480

For research use only.

Catalog No.S2162

58 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 58 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 M1fjemZ2dmO2aX;uJGF{e2G7 MoKzOUDPxE1? NUnrZll4PDhiaB?= MYDEUXNQ NVe2eYdl[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NFXlUIQzPTl3NEm3OC=>
LoVo  NGTLS|JHfW6ldHnvckBCe3OjeR?= MUK1JO69VQ>? MXW0PEBp MX3EUXNQ M37lNYJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MUiyOVk2PDl5NB?=
HN5 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHJNIU4OiCq MUTFR|UxRTNwOEGgxtEhOS57OTFOwG0> MX6yOVgyODBzMB?=
Cal33 NXfuV3VsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW2VGk4OiCq NEXB[IxGSzVyPUOuN|chyrFiMD63OUDPxE1? NIfhcXgzPThzMECxNC=>
UM-22B NGL4OFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2qxVlczKGh? NH\wRXpGSzVyPUKuOlYhyrFiMD6yOEDPxE1? M2S3VFI2QDFyMEGw
686LN NX;XRYh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PKVlczKGh? Mlq3SWM2OD1{LkC1JOKyKDFwM{Og{txO MknhNlU5OTByMUC=
UM SCC-1 M3jZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu3NkBp NVrYSFg{TUN3ME2xMlY4KMLzIECuOFIh|ryP NVXQZ2RCOjV6MUCwNVA>
UM-22A MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnMSFE4OiCq NF\heINGSzVyPUGuN|IhyrFiMD6zPUDPxE1? NHGxO5QzPThzMECxNC=>
OSC19 M{HmfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T3[lczKGh? NYHj[nk3TUN3ME2xMlI3KMLzIECuNlAh|ryP MY[yOVgyODBzMB?=
PCI-52 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO3NkBp NG\ZOIlGSzVyPUGuNFAhyrFiMD6wPUDPxE1? M1SzU|I2QDFyMEGw
PCI-15B NXfMOFNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjPO|IhcA>? NXftdGF1TUN3ME2wMlk6KMLzIEGuO|Qh|ryP NVW3[GRTOjV6MUCwNVA>
UMSCC-1 MlTQSpVv[3Srb36gRZN{[Xl? NYPJPIltOC5yMEC1MVEvPiEQvF2= M4XwZ|I1KGh? M1fZRYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NInHTWQzPThzMECxNC=>
Cal33 MWnGeY5kfGmxbjDBd5NigQ>? M1juO|AvODByNT2zMlgh|ryP NIDVbXIzPCCq MUDhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NVriN|FHOjV6MUCwNVA>
HH5 M3XjXGZ2dmO2aX;uJGF{e2G7 MkLXNE4xODB3LUOuPEDPxE1? MmLGNlQhcA>? NHvVVmti[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4fvSlI2QDFyMEGw
UM-22A NYDMOmFjTnWwY4Tpc44hSXO|YYm= Mmq5NE4xODB3LUGuOkDPxE1? NWTPSpdbOjRiaB?= NGXLfJdi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2T2bFI2QDFyMEGw
A1847 NV;LeodqTnWwY4Tpc44hSXO|YYm= MV6wMlA2NTFyIN88US=> NX3r[JlFOjRiaB?= NYTIbpBxTE2VT9Mg MUTy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NGnme3MzPTZ2NkCxOS=>
OVCAR-5 NWLxVGRDTnWwY4Tpc44hSXO|YYm= M1\JNlAvODVvMUCg{txO NGfmUXAzPCCq NELvdnBFVVORwrC= M17xWpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MYOyOVY1PjBzNR?=
OVCAR-8 NWPMdIhVTnWwY4Tpc44hSXO|YYm= M4rneFAvODVvMUCg{txO MmHMNlQhcA>? NVy5NVhYTE2VT9Mg M136ZpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MoXUNlU3PDZyMUW=
MOVCAR-5447 NF;HXXZHfW6ldHnvckBCe3OjeR?= NX7INmNOOC5yNT2xNEDPxE1? M17iZ|I1KGh? MkXwSG1UV8Li Mm\TdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NHnoPWUzPTZ2NkCxOS=>
MOVCAR-5009 MVjGeY5kfGmxbjDBd5NigQ>? NXflSVNoOC5yNT2xNEDPxE1? MUeyOEBp NYLndVlTTE2VT9Mg MljEdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MUeyOVY1PjBzNR?=
A1847 Mn;mR4VtdCCYaXHibYxqfHliQYPzZZk> MlXhNE4xPS1zMDFOwG0> M3PXN|czKGh? NEfpWJJFVVOR MmW1doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MofMNlU3PDZyMUW=
OVCAR-5 M{DrU2NmdGxiVnnhZoltcXS7IFHzd4F6 Mne1NE4xPS1zMDFOwG0> MorJO|IhcA>? M2Kw[2ROW09? NFK4VFNz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MVqyOVY1PjBzNR?=
OVCAR-8  MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGHOSJMxNjB3LUGwJO69VQ>? M3XjXFczKGh? NG\v[ZZFVVOR NGDpT4tz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MkjqNlU3PDZyMUW=
OVCAR-5  MmLRRZBweHSxc3nzJGF{e2G7 MlPYNE42NzFxNTFOwG0> NGfvXI81QCCq MV;EUXNQ M1u3b4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MmTxNlU3PDZyMUW=
OVCAR-8  M3zDZWFxd3C2b4Ppd{BCe3OjeR?= MW[wMlUwOS93IN88US=> MXq0PEBp NV2xTFNSTE2VTx?= MV;pcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w NFfENpQzPTZ2NkCxOS=>
AKRSL M1T6cGNmdGxiVnnhZoltcXS7IFHzd4F6 NHj5V2Y4OiCq NEjoXWJKSzVy78{eNVAh|ryP MlvQNlU2ODR4M{W=
PALJDL NUX4foZMS2WubDDWbYFjcWyrdImgRZN{[Xl? MUW3NkBp NWLO[mhxUUN3ME2yMlQh|ryP M3nPOVI2PTB2NkO1
MO4 NUjrNXRqTnWwY4Tpc44hSXO|YYm= M4ruZVAvPS9zL{Wg{txO M4Kzb|YhcA>? MVPpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> NXS4T5hROjVzNEm1N|U>
DU145  NFHrZmtHfW6ldHnvckBCe3OjeR?= NUfuSGx3OC1{MECgcm0> NGHXbYEyKGkEoB?= NYDJOphCe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> MViyOFU4Pzl2Mh?=
DU145  MUTGeY5kfGmxbjDBd5NigQ>? MWe4NFAhdk1? MnjkO|IhcA>? MmnYd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 MXiyOFU4Pzl2Mh?=
CWR22Rv1 MlXQSpVv[3Srb36gRZN{[Xl? NH[5emw5ODBibl2= MXK3NkBp NGDvTXR{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NWDWWmNSOjR3N{e5OFI>
N592 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwOESg{txO NH\XfXIzPDF3OEewNS=>
H82 MmXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFwM{eg{txO M3PXSFI1OTV6N{Cx
GLC4 NVjlfZdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwN{mg{txO NG[3bWszPDF3OEewNS=>
H526 NIDqNWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfI[GhFUUN3ME2zMlA5KM7:TR?= NVLCZ|R{OjRzNUi3NFE>
H1173 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jhTWlEPTB;Mj6zPUDPxE1? M37qdFI1OTV6N{Cx
DMS114 M1nx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwN{Og{txO MWeyOFE2QDdyMR?=
NCI-N592 NG\z[3lHfW6ldHnvckBCe3OjeR?= MkXnNE4{NzFxMzFOwG0> NWLuTWNTOjRiaB?= NIryWVhqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? M3zkVlI1OTV6N{Cx
GLC4 M3TPcmZ2dmO2aX;uJGF{e2G7 NFHRXGIxNjNxMT:zJO69VQ>? NYDE[pk{OjRiaB?= NGjZW4lqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MmiyNlQyPTh5MEG=
NCI-H82 M2HmXGZ2dmO2aX;uJGF{e2G7 M4XMVVAvOy9zL{Og{txO NYr6dYVOOjRiaB?= NUHBOZA1cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M4e0eVI1OTV6N{Cx
NCI-N592 NFzHb|lCeG:ydH;zbZMhSXO|YYm= M2Ptb|AvOy9zL{Og{txO M4DCdFQ5KGh? NYXXe2x4cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MUiyOFE2QDdyMR?=
GLC4 NInMPY1CeG:ydH;zbZMhSXO|YYm= Ml\ONE4{NzFxMzFOwG0> MVS0PEBp NF;leG9qdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MYqyOFE2QDdyMR?=
NCI-H82 MWDBdI9xfG:|aYOgRZN{[Xl? MkjWNE4{NzFxMzFOwG0> MVW0PEBp MVjpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MnrGNlQyPTh5MEG=
CWR22Rv1  MojPRZBweHSxc3nzJGF{e2G7 NW\XNWppUUN3ME2wMlQ5OiEQvF2= M4PWW|I{QTR{MEm1
CWR22Pc Ml25RZBweHSxc3nzJGF{e2G7 NG[zOo9KSzVyPUCuOFM5KM7:TR?= MYCyN|k1OjB7NR?=
PC-3 M{G2[mFxd3C2b4Ppd{BCe3OjeR?= MlLkTWM2OD1zLke1OUDPxE1? NHeyPGozOzl2MkC5OS=>
DU145 M1nTTWFxd3C2b4Ppd{BCe3OjeR?= M3O5RmlEPTB;Mz61NVch|ryP MkDYNlM6PDJyOUW=
RC165N M1izU2Fxd3C2b4Ppd{BCe3OjeR?= MkDRTWM2OD1{LkC4N{DPxE1? MnXDNlM6PDJyOUW=
ARPE19 MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7EUXNQ MVnJR|UxRTJ2LkO4JO69VQ>? Ml3CNlM2OzF7MkG=
HEK293 M2Hzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzFTHRFVVOR MYPJR|UxRThwNkeg{txO M2TiflI{PTNzOUKx
KCNR NUDrTFdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHEUXNQ NILVWoFKSzVyPUCuOFYh|ryP M{DS[|I{PTNzOUKx
SY5Y MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnMUo84TE2VTx?= MlLFTWM2OD1yLkO2JO69VQ>? M{PGelI{PTNzOUKx
BE2 NVjzS4RmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWCxTox3TE2VTx?= MknITWM2OD1yLkexJO69VQ>? MlzLNlM2OzF7MkG=
AS NHu5Z4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrySG1UVw>? MULJR|UxRTFwNUOg{txO NGn3dIQzOzV|MUmyNS=>
NGP MkXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjEUXNQ NEf3c3hKSzVyPUCuOVYh|ryP MV[yN|U{OTl{MR?=
IMR32 NH62XoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjFPFVFVVOR MniwTWM2OD1yLk[2JO69VQ>? M3TTWlI{PTNzOUKx
LAN5 MlLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjMOmljTE2VTx?= M1nKfWlEPTB;MT6wOEDPxE1? NEjXVGozOzV|MUmyNS=>
RH18 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7CVodFVVOR NYnKRYVEUUN3ME2xMlQzKM7:TR?= NXyyZpY4OjN3M{G5NlE>
RH30 MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTxSG1UVw>? NGPWNWtKSzVyPUGuNlUh|ryP M3H0NlI{PTNzOUKx
RH17 NU\WdGFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGSzVG1FVVOR NVO3Z|JpUUN3ME2yMlUyKM7:TR?= MkH1NlM2OzF7MkG=
RH28 MoLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXySG1UVw>? NYPYWVlDUUN3ME20MlI5KM7:TR?= MYGyN|U{OTl{MR?=
RH36 NGfFN|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLEUXNQ MlvxTWM2OD13LkO3JO69VQ>? NEPpWpozOzV|MUmyNS=>
RH41 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTaXnZjTE2VTx?= Ml\YTWM2OD1yLkS4JO69VQ>? NXTVUGlXOjN3M{G5NlE>
RD M1TjSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn4[HV4TE2VTx?= MmPCTWM2OD12LkOyJO69VQ>? MoHoNlM2OzF7MkG=
TC32 M4HrbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm3b5h2TE2VTx?= NFrqTINKSzVyPUOuPFUh|ryP MVOyN|U{OTl{MR?=
TC71 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33ycWROW09? NGLNcZlKSzVyPUSuN|Mh|ryP NYH5[4RNOjN3M{G5NlE>
KCNR NYOyV|hNSXCxcITvd4l{KEG|c3H5 NX3YcmM6OC53L{GuNE8zNjVizszN M3f5UVI1KGh? NWHVNYZtTE2VTx?= NWDycllLcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MoO3NlM2OzF7MkG=
SY5Y M33JOWFxd3C2b4Ppd{BCe3OjeR?= M4rjZVAvPS9zLkCvNk42KM7:TR?= M4jsSFI1KGh? MUTEUXNQ M3f1TIlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NF;0cZUzOzV|MUmyNS=>
Rh18 Mor1RZBweHSxc3nzJGF{e2G7 MlfKNE42NzFwMD:yMlUh|ryP MWKyOEBp NYPHRWJ1TE2VTx?= MVLpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MoDsNlM2OzF7MkG=
TC32 MXTBdI9xfG:|aYOgRZN{[Xl? M4frPVAvPS9zLkCvNk42KM7:TR?= NI[3NI8zPCCq MnfXSG1UVw>? MV\pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NHewS2UzOzV|MUmyNS=>
KCNR NVrNSXB5TnWwY4Tpc44hSXO|YYm= NYrENmRmOC53L{GuNE8zNjVxNTFOwG0> NV;Rb|RwOjRiaB?= Mn\lSG1UVw>? NUP5T5VlcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NHq1[ZQzOzV|MUmyNS=>
SY5Y NXrOZ5V3TnWwY4Tpc44hSXO|YYm= MUewMlUwOS5yL{KuOU82KM7:TR?= M4i5NFI1KGh? NUXLUIxTTE2VTx?= NYnLXmpUcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NWSydGdoOjN3M{G5NlE>
Rh18 MW\GeY5kfGmxbjDBd5NigQ>? NULTVXQ{OC53L{GuNE8zNjVxNTFOwG0> NXzYbHR[OjRiaB?= M37pWGROW09? M3HTV4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NX\icXZ[OjN3M{G5NlE>
TC32 MlHZSpVv[3Srb36gRZN{[Xl? NVzKSm1mOC53L{GuNE8zNjVxNTFOwG0> MknuNlQhcA>? Ml;RSG1UVw>? NUG0U4FycW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MmnxNlM2OzF7MkG=
TPC-1 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\sfXEyKML3TR?= NGHnOW8xNTRiZB?= NH7ncYZFVVOR MXXpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 MViyN|A2PjR7OR?=
MZ-CRC1  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvaUIV6OSEEtV2= M4jYcVAuPSCm M{CzV2ROW09? M1LEN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NH;4XWkzOzB3NkS5PS=>
TT  MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT5eFYyKML3TR?= NH7ic40xNTRiZB?= MXPEUXNQ NHLrV2hqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 M{\ZS|I{ODV4NEm5
TPC-1 M1;3OWZ2dmO2aX;uJGF{e2G7 NFvJV|AyKML3TR?= M3fDTlczKGh? NH\ZboNFVVOR Mn3pbY5lfWOnczDHNUBjdG:la3Hn[S=> MUWyN|A2PjR7OR?=
MZ-CRC1  MVvGeY5kfGmxbjDBd5NigQ>? M{[zcFEhyrWP MV63NkBp MXTEUXNQ M3zPZYlv\HWlZYOgS|Eh[myxY3vh[4U> NFSxeIczOzB3NkS5PS=>
TT  M4nlZmZ2dmO2aX;uJGF{e2G7 NYXWenVTOSEEtV2= M3[wPFczKGh? M{[4OWROW09? NXTuZoJ[cW6mdXPld{BIOSCkbH;jb4Fo\Q>? MkDQNlMxPTZ2OUm=
MZ-CRC1  MmjFRZBweHSxc3nzJGF{e2G7 MVWxJOK2VQ>? NHGxSo01QCCq MV7EUXNQ MmC3bY5lfWOnczDhdI9xfG:|aYO= NInlPFUzOzB3NkS5PS=>
TT  MljrRZBweHSxc3nzJGF{e2G7 M122PVEhyrWP M2\uRlQ5KGh? NGDkdY1FVVOR MknvbY5lfWOnczDhdI9xfG:|aYO= NWf4[3dYOjNyNU[0PVk>
HD-LM2 NYX4VVZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHob3U4OuLCiXi= NU\Z[WJxTE2VTx?= M3XLdWlEPTB;Nz64OFQh|ryP NUnN[|J2OjJ6MkmwPVQ>
L-428 NYDpbmJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3HOno4OuLCiXi= NFzLU2dFVVOR NX3JT2tUUUN3ME23Mlk1PyEQvF2= Ml:4NlI5OjlyOUS=
KM-H2 NUfhOlBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK3NwKBkWh? MX\EUXNQ NEjZVZFKSzVyPUGuN|A5KM7:TR?= MWiyNlgzQTB7NB?=
L-540 M3jo[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWO3NwKBkWh? M{DoVWROW09? MWDJR|UxRThwMkG2JO69VQ>? NETWW2czOjh{OUC5OC=>
HD-LM2 Mm\HSpVv[3Srb36gRZN{[Xl? NF7TR4IxNjFxMD61M|EwPSEQvF2= MV:3NwKBkWh? M{XLN2ROW09? Mn7ObY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MWeyNlgzQTB7NB?=
L-428 MlTpSpVv[3Srb36gRZN{[Xl? M4TZeFAvOS9yLkWvNU82KM7:TR?= NX7aOWp{PzMkgJno NX3ybYp{TE2VTx?= MofkbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NGHIUXozOjh{OUC5OC=>
KM-H2 M13Jd2Z2dmO2aX;uJGF{e2G7 M3LJWlAvOS9yLkWvNU82KM7:TR?= NF\xVVA4OuLCiXi= MnjISG1UVw>? MmribY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> M{PGPVIzQDJ7MEm0
L-540 Mn63SpVv[3Srb36gRZN{[Xl? M3:xc|AvOS9yLkWvNU82KM7:TR?= NHHFXIk4OuLCiXi= NX;lU3BxTE2VTx?= MY\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> Mn72NlI5OjlyOUS=
HD-LM2 NXrk[mhGSXCxcITvd4l{KEG|c3H5 MVKxM|Uh|ryP MnLCO|LjiImq NWrNV|JxTE2VTx?= M3HnOolv\HWlZYOgZZBweHSxc3nz NV3jPGN3OjJ6MkmwPVQ>
L-428 MlzxRZBweHSxc3nzJGF{e2G7 NX;mZ|NCOS93IN88US=> Mn20O|LjiImq MmXlSG1UVw>? NX73XIpxcW6mdXPld{BieG:ydH;zbZM> M3TPcVIzQDJ7MEm0
KM-H2 NVu2e4VVSXCxcITvd4l{KEG|c3H5 MWGxM|Uh|ryP NF3FXYU4OuLCiXi= MmS1SG1UVw>? NXT1T45scW6mdXPld{BieG:ydH;zbZM> NXfk[nBROjJ6MkmwPVQ>
L-540 NYixb3Q3SXCxcITvd4l{KEG|c3H5 MWGxM|Uh|ryP MYG3NwKBkWh? M1LLWWROW09? MkPLbY5lfWOnczDhdI9xfG:|aYO= M4fyNFIzQDJ7MEm0
U251-MG M{Dje2Z2dmO2aX;uJGF{e2G7 MkHoNUDDvU1? MWCwMVE3KGh? NEK5NVJqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? Mlu0NlIxOjd4OUG=
U87-MG MYrGeY5kfGmxbjDBd5NigQ>? MVixJOK2VQ>? MYKwMVE3KGh? MmDjbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MWmyNlAzPzZ7MR?=
4C8 MYXGeY5kfGmxbjDBd5NigQ>? NW\vd|VyOSEEtV2= M4K4RVAuOTZiaB?= MVjpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> M2rjSVIzODJ5Nkmx
U251-MG MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHNcphROS9zMDFCuW0> MWSyOE81QC95MjDo M4e4TolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NVjRfHRQOjJyMke2PVE>
U87-MG M3XjUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFOydWYyNzFyINM1US=> MWCyOE81QC95MjDo MX3pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NGDTXGkzOjB{N{[5NS=>
4C8 NUHSXVdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHYNU8yOCEEtV2= M4jpcVI1NzR6L{eyJIg> NFr0T3NqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? M4\mZ|IzODJ5Nkmx
U266 MlHJRZBweHSxc3nzJGF{e2G7 NUXRe|Q4OC53LUKg{txO Mo\sOFgwPzJiaB?= M4PNcYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Mmi0NlEyPjR3MUe=
Kms.11 NGrFVlJCeG:ydH;zbZMhSXO|YYm= Ml;6NE42NTJizszN NHXmN5c1QC95MjDo NYG3Ums1cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M{nnfFIyOTZ2NUG3
8226 MYTBdI9xfG:|aYOgRZN{[Xl? MkfPNE42NTJizszN M2XmdVQ5Nzd{IHi= MUPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M37jVFIyOTZ2NUG3

... 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)
  • 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

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)

  • Mass
    Concentration
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    Molecular Weight

*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 )

  • C1
    V1
    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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