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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 100 In stock
USD 170 In stock
USD 570 In stock
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Cited by 49 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 MVrGeY5kfGmxbjDBd5NigQ>? MoTMOUDPxE1? NFruWG41QCCq MlXESG1UVw>? NF;FN5ljdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MkLkNlU6PTR7N{S=
LoVo  MWjGeY5kfGmxbjDBd5NigQ>? NG[yOo42KM7:TR?= M2Cw[VQ5KGh? NWDWdHdsTE2VTx?= NUjaOmd7[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NF[yZnYzPTl3NEm3OC=>
HN5 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzxOmdnPzJiaB?= MUnFR|UxRTNwOEGgxtEhOS57OTFOwG0> NV6yRWRSOjV6MUCwNVA>
Cal33 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HGV|czKGh? MXzFR|UxRTNwM{egxtEhOC55NTFOwG0> MXOyOVgyODBzMB?=
UM-22B MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TSOlczKGh? NWPUNoJUTUN3ME2yMlY3KMLzIECuNlQh|ryP NGThfpAzPThzMECxNC=>
686LN M{PwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVO3NkBp NUn1elRjTUN3ME2yMlA2KMLzIEGuN|Mh|ryP M4\IVlI2QDFyMEGw
UM SCC-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV23NkBp MmTqSWM2OD1zLk[3JOKyKDBwNEKg{txO NGHvemgzPThzMECxNC=>
UM-22A M1P2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoO2O|IhcA>? MlPTSWM2OD1zLkOyJOKyKDBwM{mg{txO MYiyOVgyODBzMB?=
OSC19 NHywNGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\hW3k4OiCq MkPQSWM2OD1zLkK2JOKyKDBwMkCg{txO MVyyOVgyODBzMB?=
PCI-52 NVrDWGxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfKVodGPzJiaB?= MoLaSWM2OD1zLkCwJOKyKDBwMEmg{txO NIfZfpQzPThzMECxNC=>
PCI-15B NXnCXo9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fxSlczKGh? MorqSWM2OD1yLkm5JOKyKDFwN{Sg{txO MmGyNlU5OTByMUC=
UMSCC-1 MlHZSpVv[3Srb36gRZN{[Xl? NVr4c|JXOC5yMEC1MVEvPiEQvF2= NX3zbFJMOjRiaB?= NFK2XGZi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX;yUoQ4OjV6MUCwNVA>
Cal33 MVrGeY5kfGmxbjDBd5NigQ>? M2G5TlAvODByNT2zMlgh|ryP NUPTNHpmOjRiaB?= MlTwZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYqyOVgyODBzMB?=
HH5 MWLGeY5kfGmxbjDBd5NigQ>? NF;VVFcxNjByMEWtN{45KM7:TR?= NVzLVYZTOjRiaB?= NEfjPFJi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2fK[VI2QDFyMEGw
UM-22A NEDucpFHfW6ldHnvckBCe3OjeR?= M{TncFAvODByNT2xMlYh|ryP M3HVXlI1KGh? NGXzVWhi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVmyOVgyODBzMB?=
A1847 MYjGeY5kfGmxbjDBd5NigQ>? NIjUWmExNjB3LUGwJO69VQ>? Mn3ENlQhcA>? M1y2N2ROW00EoB?= NH7yN3lz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MnHpNlU3PDZyMUW=
OVCAR-5 MojHSpVv[3Srb36gRZN{[Xl? NEjjWnMxNjB3LUGwJO69VQ>? MorLNlQhcA>? M1PFPWROW00EoB?= MXzy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= M3Wyd|I2PjR4MEG1
OVCAR-8 M{LmR2Z2dmO2aX;uJGF{e2G7 M3TaWFAvODVvMUCg{txO NVO5UlBCOjRiaB?= M17QTmROW00EoB?= NYLqRpJ2emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NGfOWmkzPTZ2NkCxOS=>
MOVCAR-5447 MmPWSpVv[3Srb36gRZN{[Xl? NV3YR4JrOC5yNT2xNEDPxE1? M3jMOlI1KGh? M4fNRmROW00EoB?= NInsPZdz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NHzNWVUzPTZ2NkCxOS=>
MOVCAR-5009 M{Xa[GZ2dmO2aX;uJGF{e2G7 NXzYVnNUOC5yNT2xNEDPxE1? M4G3NVI1KGh? M{LoXGROW00EoB?= NUnURYJWemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M1HFOVI2PjR4MEG1
A1847 NWPGUmx3S2WubDDWbYFjcWyrdImgRZN{[Xl? NHjsdVAxNjB3LUGwJO69VQ>? M1HFOFczKGh? MV;EUXNQ Mm\SdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= Moe0NlU3PDZyMUW=
OVCAR-5 NXPWO5hSS2WubDDWbYFjcWyrdImgRZN{[Xl? NHLrWlMxNjB3LUGwJO69VQ>? MUG3NkBp MV7EUXNQ MX7y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M1HVXVI2PjR4MEG1
OVCAR-8  NV\lcY82S2WubDDWbYFjcWyrdImgRZN{[Xl? MnHnNE4xPS1zMDFOwG0> M3rTbVczKGh? MWDEUXNQ NY[3UpNjemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MnWwNlU3PDZyMUW=
OVCAR-5  M1XzdGFxd3C2b4Ppd{BCe3OjeR?= MoToNE42NzFxNTFOwG0> MkXuOFghcA>? M2Szc2ROW09? NWGxbYxVcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M4nmbVI2PjR4MEG1
OVCAR-8  NXn4XZVQSXCxcITvd4l{KEG|c3H5 NWWw[oZEOC53L{GvOUDPxE1? M1vuV|Q5KGh? NIPoZnNFVVOR MXnpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w NUG2[25jOjV4NE[wNVU>
AKRSL MmHpR4VtdCCYaXHibYxqfHliQYPzZZk> NE[5NHg4OiCq M4i3OmlEPTExvK6xNEDPxE1? M4LmWlI2PTB2NkO1
PALJDL Mn[xR4VtdCCYaXHibYxqfHliQYPzZZk> M{LaUlczKGh? NF33[2xKSzVyPUKuOEDPxE1? NITnfoQzPTVyNE[zOS=>
MO4 MWrGeY5kfGmxbjDBd5NigQ>? NYfXflRGOC53L{GvOUDPxE1? MlTsOkBp NEW3OoRqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? MViyOVE1QTV|NR?=
DU145  MWXGeY5kfGmxbjDBd5NigQ>? MmH2NE0zODBibl2= MnKzNUBpyqB? NV\v[XZUe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> MVqyOFU4Pzl2Mh?=
DU145  MUPGeY5kfGmxbjDBd5NigQ>? MW[4NFAhdk1? M1e1S|czKGh? M2T6WJN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= M3i5SFI1PTd5OUSy
CWR22Rv1 MUfGeY5kfGmxbjDBd5NigQ>? M33XfVgxOCCwTR?= NGjBTJI4OiCq MkPkd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 M{TjclI1PTd5OUSy
N592 NHT1R5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnWzTWM2OD1yLki0JO69VQ>? MnPVNlQyPTh5MEG=
H82 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv4TWM2OD1zLkO3JO69VQ>? MYiyOFE2QDdyMR?=
GLC4 NIfIUIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFwN{mg{txO M3nO[|I1OTV6N{Cx
H526 NF\Y[IpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWmzZZdOUUN3ME2zMlA5KM7:TR?= Mo\6NlQyPTh5MEG=
H1173 M1nuS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\xVYttUUN3ME2yMlM6KM7:TR?= NGPOXHEzPDF3OEewNS=>
DMS114 M17MTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3ETWM2OD1yLkezJO69VQ>? NHjifVAzPDF3OEewNS=>
NCI-N592 NIHCNFNHfW6ldHnvckBCe3OjeR?= Mm[yNE4{NzFxMzFOwG0> NWC1Rms1OjRiaB?= NHLBXI9qdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NWT1Xld5OjRzNUi3NFE>
GLC4 M1WyeGZ2dmO2aX;uJGF{e2G7 NY[ybHlNOC5|L{GvN{DPxE1? NEjpZ|EzPCCq MmGxbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M1rTSVI1OTV6N{Cx
NCI-H82 M3nzZmZ2dmO2aX;uJGF{e2G7 MVqwMlMwOS9|IN88US=> MnrPNlQhcA>? MnX4bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NWX4UI1UOjRzNUi3NFE>
NCI-N592 MXnBdI9xfG:|aYOgRZN{[Xl? M{PVVFAvOy9zL{Og{txO NYrJS2h5PDhiaB?= MWfpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NIDx[JkzPDF3OEewNS=>
GLC4 NEC4Z5FCeG:ydH;zbZMhSXO|YYm= NFy4SlMxNjNxMT:zJO69VQ>? MmK2OFghcA>? MXTpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MYKyOFE2QDdyMR?=
NCI-H82 NIfIeVdCeG:ydH;zbZMhSXO|YYm= MlrXNE4{NzFxMzFOwG0> NH\mbFE1QCCq M1rpdIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MlrFNlQyPTh5MEG=
CWR22Rv1  MmniRZBweHSxc3nzJGF{e2G7 M1TY[2lEPTB;MD60PFIh|ryP M3;rPFI{QTR{MEm1
CWR22Pc NVjpc20{SXCxcITvd4l{KEG|c3H5 M{DhU2lEPTB;MD60N|gh|ryP M4W2eFI{QTR{MEm1
PC-3 Mki5RZBweHSxc3nzJGF{e2G7 M4X5eWlEPTB;MT63OVUh|ryP NG\BenozOzl2MkC5OS=>
DU145 MnLvRZBweHSxc3nzJGF{e2G7 NWr6OXRXUUN3ME2zMlUyPyEQvF2= M{LyTlI{QTR{MEm1
RC165N NYTwfJN7SXCxcITvd4l{KEG|c3H5 Mkm0TWM2OD1{LkC4N{DPxE1? M1y3OFI{QTR{MEm1
ARPE19 M2\0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHEUXNQ M4XsUmlEPTB;MkSuN|gh|ryP M13HdVI{PTNzOUKx
HEK293 NXjoNZBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jGe2ROW09? MkfaTWM2OD16Lk[3JO69VQ>? NHrzeVAzOzV|MUmyNS=>
KCNR MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37YXGROW09? MnzSTWM2OD1yLkS2JO69VQ>? NX;TeVF4OjN3M{G5NlE>
SY5Y NFzxT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\QdnRUTE2VTx?= MXTJR|UxRTBwM{[g{txO MlfaNlM2OzF7MkG=
BE2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPvRXVFVVOR M4nDfGlEPTB;MD63NUDPxE1? NFq5OGEzOzV|MUmyNS=>
AS MojKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDWbmZFVVOR M{ewd2lEPTB;MT61N{DPxE1? NUfJeGJWOjN3M{G5NlE>
NGP MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;WdYFsTE2VTx?= MkjKTWM2OD1yLkW2JO69VQ>? NEDMR4kzOzV|MUmyNS=>
IMR32 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojHSG1UVw>? MkTYTWM2OD1yLk[2JO69VQ>? M{DOfVI{PTNzOUKx
LAN5 NEnrUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfvPFdFVVOR M2LBe2lEPTB;MT6wOEDPxE1? MnLTNlM2OzF7MkG=
RH18 NWPyU2ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLEUXNQ NYDWephXUUN3ME2xMlQzKM7:TR?= M4jzfVI{PTNzOUKx
RH30 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M123NGROW09? MX;JR|UxRTFwMkWg{txO MlzPNlM2OzF7MkG=
RH17 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi3RYV1TE2VTx?= M2HCNWlEPTB;Mj61NUDPxE1? M3fCdFI{PTNzOUKx
RH28 NXXXOmtkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGO2W2hFVVOR NUXwcYJxUUN3ME20MlI5KM7:TR?= NYTveGlEOjN3M{G5NlE>
RH36 NVfoSo5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7tdGZFVVOR NY\4ZpBwUUN3ME21MlM4KM7:TR?= MWSyN|U{OTl{MR?=
RH41 NHXPTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK1flNFVVOR NEPNPIZKSzVyPUCuOFgh|ryP Mk\CNlM2OzF7MkG=
RD NXPIfHdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXRUmRFVVOR MlfITWM2OD12LkOyJO69VQ>? M4\QTVI{PTNzOUKx
TC32 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;4SG1UVw>? NG\pUHFKSzVyPUOuPFUh|ryP M3XpU|I{PTNzOUKx
TC71 NHSze3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;EUXNQ Mn3vTWM2OD12LkOzJO69VQ>? MXuyN|U{OTl{MR?=
KCNR M3rReWFxd3C2b4Ppd{BCe3OjeR?= MYGwMlUwOS5yL{KuOUDPxE1? MXSyOEBp MVrEUXNQ MljPbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MVWyN|U{OTl{MR?=
SY5Y NUiyOFNvSXCxcITvd4l{KEG|c3H5 NX;OSG9MOC53L{GuNE8zNjVizszN M17Z[|I1KGh? NXTNdJNtTE2VTx?= M3T2d4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NYjNdIxPOjN3M{G5NlE>
Rh18 MoG2RZBweHSxc3nzJGF{e2G7 NVHWVFJlOC53L{GuNE8zNjVizszN Ml\VNlQhcA>? MUTEUXNQ MnvTbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MYOyN|U{OTl{MR?=
TC32 MnjxRZBweHSxc3nzJGF{e2G7 MU[wMlUwOS5yL{KuOUDPxE1? M2HCWFI1KGh? MVjEUXNQ NY[2VIt1cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NXHQTm1ZOjN3M{G5NlE>
KCNR NXy5dJFZTnWwY4Tpc44hSXO|YYm= NXvkOXJMOC53L{GuNE8zNjVxNTFOwG0> NIPocZQzPCCq MXrEUXNQ NVzCbGFXcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MkDINlM2OzF7MkG=
SY5Y NHzUd|FHfW6ldHnvckBCe3OjeR?= MnXHNE42NzFwMD:yMlUwPSEQvF2= M{\uVFI1KGh? NHvnSIpFVVOR NXTtZm9zcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MWKyN|U{OTl{MR?=
Rh18 NEjxPVBHfW6ldHnvckBCe3OjeR?= NWTYfYJoOC53L{GuNE8zNjVxNTFOwG0> MXyyOEBp M4jX[WROW09? NEmySZZqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NWjMXHVTOjN3M{G5NlE>
TC32 MUfGeY5kfGmxbjDBd5NigQ>? MoH6NE42NzFwMD:yMlUwPSEQvF2= MXWyOEBp NUnCTW5TTE2VTx?= M{jo[olvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u Mle1NlM2OzF7MkG=
TPC-1 M2jyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLqe5Y{OSEEtV2= NEPjZYkxNTRiZB?= NWixbnhYTE2VTx?= MVjpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 MmfjNlMxPTZ2OUm=
MZ-CRC1  NVS0[3ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD2NUDDvU1? M{WzNFAuPSCm M{Tx[mROW09? MnnvbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MojINlMxPTZ2OUm=
TT  MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELzNVYyKML3TR?= NVHm[24{OC12IHS= NYTqbZhQTE2VTx?= M{[4RYlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NWLlUlJzOjNyNU[0PVk>
TPC-1 NVLEVG5GTnWwY4Tpc44hSXO|YYm= Mo\kNUDDvU1? MoTiO|IhcA>? Mne0SG1UVw>? MXjpcoR2[2W|IFexJIJtd2OtYXfl Mm[yNlMxPTZ2OUm=
MZ-CRC1  M2\tUWZ2dmO2aX;uJGF{e2G7 MlTTNUDDvU1? NGrm[o44OiCq MUPEUXNQ MYTpcoR2[2W|IFexJIJtd2OtYXfl M3m1Z|I{ODV4NEm5
TT  NGDmSWJHfW6ldHnvckBCe3OjeR?= Ml64NUDDvU1? M4jYZ|czKGh? NUXJepNPTE2VTx?= NYjXZVNJcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MY[yN|A2PjR7OR?=
MZ-CRC1  NFzUbpBCeG:ydH;zbZMhSXO|YYm= MmDUNUDDvU1? NF7MWoo1QCCq MWHEUXNQ NETEV5VqdmS3Y3XzJIFxd3C2b4Ppdy=> MYOyN|A2PjR7OR?=
TT  M3foSWFxd3C2b4Ppd{BCe3OjeR?= NX\2[YVJOSEEtV2= NV3FdnJLPDhiaB?= M3PGSmROW09? NXTGcFc1cW6mdXPld{BieG:ydH;zbZM> NX3weXRVOjNyNU[0PVk>
HD-LM2 NGPmUYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrUN3I4OuLCiXi= MXTEUXNQ MlqwTWM2OD15Lki0OEDPxE1? NIPCPIQzOjh{OUC5OC=>
L-428 M4LhN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLHO|LjiImq NGPE[VRFVVOR MWPJR|UxRTdwOUS3JO69VQ>? MXmyNlgzQTB7NB?=
KM-H2 NV;X[mU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW1RpI4OuLCiXi= M17TSWROW09? NYHzVGJVUUN3ME2xMlMxQCEQvF2= M3G3b|IzQDJ7MEm0
L-540 NUPZOWRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlroO|LjiImq M3zlbGROW09? MX\JR|UxRThwMkG2JO69VQ>? MknZNlI5OjlyOUS=
HD-LM2 M{DyO2Z2dmO2aX;uJGF{e2G7 NVTZdW9UOC5zL{CuOU8yNzVizszN MorGO|LjiImq NWP1RZFYTE2VTx?= M4HPeYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NYfhfYpoOjJ6MkmwPVQ>
L-428 MXzGeY5kfGmxbjDBd5NigQ>? MoTSNE4yNzBwNT:xM|Uh|ryP NX:0d29VPzMkgJno NHTWN5BFVVOR NYKySG9ocW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? M{PmWlIzQDJ7MEm0
KM-H2 NYjWUpNMTnWwY4Tpc44hSXO|YYm= NWPE[plpOC5zL{CuOU8yNzVizszN MlPKO|LjiImq MWLEUXNQ MnzZbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NEnGco0zOjh{OUC5OC=>
L-540 M4jtbWZ2dmO2aX;uJGF{e2G7 MoLENE4yNzBwNT:xM|Uh|ryP NWfOO4k2PzMkgJno M3j1UGROW09? MWXpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NIrheYYzOjh{OUC5OC=>
HD-LM2 NYq4ZY1RSXCxcITvd4l{KEG|c3H5 MlfSNU82KM7:TR?= NYnPe3doPzMkgJno NITBOpNFVVOR M{j2UIlv\HWlZYOgZZBweHSxc3nz NWP2TXdTOjJ6MkmwPVQ>
L-428 MojDRZBweHSxc3nzJGF{e2G7 NITZNXcyNzVizszN NWXZbXZoPzMkgJno Moi0SG1UVw>? M3zMeYlv\HWlZYOgZZBweHSxc3nz M2XpT|IzQDJ7MEm0
KM-H2 NEL3SXpCeG:ydH;zbZMhSXO|YYm= M3\jU|EwPSEQvF2= MV63NwKBkWh? Mmn3SG1UVw>? MkL4bY5lfWOnczDhdI9xfG:|aYO= MkG5NlI5OjlyOUS=
L-540 MmTBRZBweHSxc3nzJGF{e2G7 NXG0eFNROS93IN88US=> M4DMdlcz6oDLaB?= MYjEUXNQ MkLybY5lfWOnczDhdI9xfG:|aYO= M1TQdlIzQDJ7MEm0
U251-MG MkS1SpVv[3Srb36gRZN{[Xl? NEW3cGEyKML3TR?= NGW3dXkxNTF4IHi= NEnQbZhqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MXOyNlAzPzZ7MR?=
U87-MG NW\YS|Q1TnWwY4Tpc44hSXO|YYm= NEDpO2MyKML3TR?= NHnXS4UxNTF4IHi= MnTUbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MWeyNlAzPzZ7MR?=
4C8 MlnDSpVv[3Srb36gRZN{[Xl? NFvJOJYyKML3TR?= NYiw[JI1OC1zNjDo NH;URYNqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MoPONlIxOjd4OUG=
U251-MG NHvDXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPqNU8yOCEEtV2= M4rDZVI1NzR6L{eyJIg> NHXYOmtqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? M{WzVlIzODJ5Nkmx
U87-MG NID5bHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkm2NU8yOCEEtV2= NEnOWYczPC92OD:3NkBp NIPaV4ZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MV2yNlAzPzZ7MR?=
4C8 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmxM|ExKML3TR?= NHnVelYzPC92OD:3NkBp MX3pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MYqyNlAzPzZ7MR?=
U266 NX;MWm9oSXCxcITvd4l{KEG|c3H5 MlrONE42NTJizszN M4G3cFQ5Nzd{IHi= NUK4WXA2cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M1[4UFIyOTZ2NUG3
Kms.11 NIfSOlhCeG:ydH;zbZMhSXO|YYm= MUWwMlUuOiEQvF2= NIjme5I1QC95MjDo MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NGq4THkzOTF4NEWxOy=>
8226 MVHBdI9xfG:|aYOgRZN{[Xl? NXT3UVBvOC53LUKg{txO NX3lVJNzPDhxN{KgbC=> NV;3cVRncW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NHroS3gzOTF4NEWxOy=>

... 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).

The Serial Dilution Calculator Equation

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    C8=C7/X C8: LOG(C8):
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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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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