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 NXfB[29HTnWwY4Tpc44hSXO|YYm= NVPHSpN5PSEQvF2= NW\JRoRFPDhiaB?= NFq0Z21FVVOR MXzicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= M{LYc|I2QTV2OUe0
LoVo  NV\scpd7TnWwY4Tpc44hSXO|YYm= MYK1JO69VQ>? NWHqOGRoPDhiaB?= NIj1SnVFVVOR MYHicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= M{Lae|I2QTV2OUe0
HN5 NISyOVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDLdHo4OiCq Mk\rSWM2OD1|LkixJOKyKDFwOUmg{txO NUjmZZpmOjV6MUCwNVA>
Cal33 MoPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTwO|IhcA>? NInGN2VGSzVyPUOuN|chyrFiMD63OUDPxE1? MWGyOVgyODBzMB?=
UM-22B MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1noZVczKGh? Mn64SWM2OD1{Lk[2JOKyKDBwMkSg{txO NF;HW|AzPThzMECxNC=>
686LN Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIGxV3I4OiCq Mn3XSWM2OD1{LkC1JOKyKDFwM{Og{txO NVXzfGhXOjV6MUCwNVA>
UM SCC-1 NHfoU25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;sRoc4OiCq NWWzbG5tTUN3ME2xMlY4KMLzIECuOFIh|ryP MXuyOVgyODBzMB?=
UM-22A MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\0[lczKGh? NG\CNJRGSzVyPUGuN|IhyrFiMD6zPUDPxE1? M4\sbFI2QDFyMEGw
OSC19 M1jRXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUW3NkBp M{C5UWVEPTB;MT6yOkDDuSByLkKwJO69VQ>? NWHuRZo6OjV6MUCwNVA>
PCI-52 NVjiclh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW0O|IhcA>? NVryOllGTUN3ME2xMlAxKMLzIECuNFkh|ryP NFf0RoEzPThzMECxNC=>
PCI-15B Mk\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[3NkBp Mn[wSWM2OD1yLkm5JOKyKDFwN{Sg{txO NW\RPHRYOjV6MUCwNVA>
UMSCC-1 MWPGeY5kfGmxbjDBd5NigQ>? NF3lVGYxNjByMEWtNU43KM7:TR?= Mnz1NlQhcA>? NVzQdlBF[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M13teFI2QDFyMEGw
Cal33 M3LF[2Z2dmO2aX;uJGF{e2G7 MX[wMlAxODVvMz64JO69VQ>? M{nsNFI1KGh? NYLHSGlG[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXqyOVgyODBzMB?=
HH5 NHfNVZNHfW6ldHnvckBCe3OjeR?= NUnacYF1OC5yMEC1MVMvQCEQvF2= M4OyOFI1KGh? Mme3ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlfzNlU5OTByMUC=
UM-22A MYXGeY5kfGmxbjDBd5NigQ>? MorMNE4xODB3LUGuOkDPxE1? MnnQNlQhcA>? NXLRdHEy[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1;YdlI2QDFyMEGw
A1847 NVS3XmtSTnWwY4Tpc44hSXO|YYm= MVGwMlA2NTFyIN88US=> NYf0TpBLOjRiaB?= MVvEUXNQyqB? NF[zSlZz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MXyyOVY1PjBzNR?=
OVCAR-5 M{XMcWZ2dmO2aX;uJGF{e2G7 MkjaNE4xPS1zMDFOwG0> NX;4R21oOjRiaB?= NVSxS20{TE2VT9Mg NUXSZpZ4emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> Mom5NlU3PDZyMUW=
OVCAR-8 M4XnfWZ2dmO2aX;uJGF{e2G7 MVywMlA2NTFyIN88US=> M1\xVlI1KGh? MYLEUXNQyqB? MmLCdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NIjYbZczPTZ2NkCxOS=>
MOVCAR-5447 NH3m[45HfW6ldHnvckBCe3OjeR?= MWOwMlA2NTFyIN88US=> NFTNdGQzPCCq M3XPSGROW00EoB?= M1Hx[JJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NHnOelgzPTZ2NkCxOS=>
MOVCAR-5009 NXHxXo05TnWwY4Tpc44hSXO|YYm= NEjPS2oxNjB3LUGwJO69VQ>? MnPpNlQhcA>? M1fFfmROW00EoB?= NYnBS4JpemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M{HQdlI2PjR4MEG1
A1847 NYLJTZYzS2WubDDWbYFjcWyrdImgRZN{[Xl? MWiwMlA2NTFyIN88US=> Mom3O|IhcA>? MWTEUXNQ NIH2Uplz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MljlNlU3PDZyMUW=
OVCAR-5 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3TONFAvODVvMUCg{txO NUiySG9vPzJiaB?= NG\4VFZFVVOR NXzJdINMemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NXTJT5FXOjV4NE[wNVU>
OVCAR-8  M3LVNWNmdGxiVnnhZoltcXS7IFHzd4F6 NIHTUGYxNjB3LUGwJO69VQ>? MYi3NkBp Mln2SG1UVw>? NYPvZZU2emWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> M{LPelI2PjR4MEG1
OVCAR-5  MXrBdI9xfG:|aYOgRZN{[Xl? NWXDXZM{OC53L{GvOUDPxE1? NGnvfm01QCCq NEXMS49FVVOR MX3pcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w MUGyOVY1PjBzNR?=
OVCAR-8  NUDIe3lWSXCxcITvd4l{KEG|c3H5 NWTx[mluOC53L{GvOUDPxE1? M1\NS|Q5KGh? MVnEUXNQ M{fqVolv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MkfTNlU3PDZyMUW=
AKRSL M33yNmNmdGxiVnnhZoltcXS7IFHzd4F6 MXe3NkBp MYDJR|Ux97zgMUCg{txO MVGyOVUxPDZ|NR?=
PALJDL M3vQU2NmdGxiVnnhZoltcXS7IFHzd4F6 NIrmSGM4OiCq NXXYVI56UUN3ME2yMlQh|ryP M2HyNFI2PTB2NkO1
MO4 M4HrNGZ2dmO2aX;uJGF{e2G7 M1j5T|AvPS9zL{Wg{txO Mm[wOkBp NFnwWGdqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NF\TVGQzPTF2OUWzOS=>
DU145  MV3GeY5kfGmxbjDBd5NigQ>? Mo\WNE0zODBibl2= MlzHNUBpyqB? M2XpPZN2eHC{ZYPz[ZMhUUxvNj3hZ5RqfmG2ZXSgV5RifDNiYX7kJGVTUzFxMjDzbYdv[Wyrbne= NY\NZo9SOjR3N{e5OFI>
DU145  M3LwWmZ2dmO2aX;uJGF{e2G7 Ml7qPFAxKG6P NWjpOmFUPzJiaB?= M1XoPZN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= M37CXlI1PTd5OUSy
CWR22Rv1 NYDLc2FxTnWwY4Tpc44hSXO|YYm= MonLPFAxKG6P NYT3RoxHPzJiaB?= M364c5N2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= MnvWNlQ2Pzd7NEK=
N592 NEnXTo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwOESg{txO M3\4dFI1OTV6N{Cx
H82 M4WwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPXZ|E4UUN3ME2xMlM4KM7:TR?= NYTSSFVwOjRzNUi3NFE>
GLC4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFwN{mg{txO MlmwNlQyPTh5MEG=
H526 M13XcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTNwMEig{txO MnHuNlQyPTh5MEG=
H1173 NYTyd3JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJwM{mg{txO NGm5XXkzPDF3OEewNS=>
DMS114 NFjQfWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLY[HNKSzVyPUCuO|Mh|ryP NX31To5wOjRzNUi3NFE>
NCI-N592 MojQSpVv[3Srb36gRZN{[Xl? NGnWN|AxNjNxMT:zJO69VQ>? MWqyOEBp MW\pcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> MVqyOFE2QDdyMR?=
GLC4 MnHTSpVv[3Srb36gRZN{[Xl? M1jHVFAvOy9zL{Og{txO NFPNNFEzPCCq MVHpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NYO2OZNbOjRzNUi3NFE>
NCI-H82 NEL1d3ZHfW6ldHnvckBCe3OjeR?= Mof0NE4{NzFxMzFOwG0> MXGyOEBp NGLWNFRqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NGnxNYQzPDF3OEewNS=>
NCI-N592 M1XH[2Fxd3C2b4Ppd{BCe3OjeR?= MkTWNE4{NzFxMzFOwG0> NHjIemU1QCCq M{D5VIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MXKyOFE2QDdyMR?=
GLC4 NHzwVFdCeG:ydH;zbZMhSXO|YYm= M3TlVVAvOy9zL{Og{txO NE\0T2c1QCCq NInjRZVqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MnLrNlQyPTh5MEG=
NCI-H82 M1PvOGFxd3C2b4Ppd{BCe3OjeR?= MYSwMlMwOS9|IN88US=> MYS0PEBp NHLoeFdqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MUCyOFE2QDdyMR?=
CWR22Rv1  NWXQdHNPSXCxcITvd4l{KEG|c3H5 NWrkd4V5UUN3ME2wMlQ5OiEQvF2= MVGyN|k1OjB7NR?=
CWR22Pc M4fCWGFxd3C2b4Ppd{BCe3OjeR?= M{ToNGlEPTB;MD60N|gh|ryP Mnf4NlM6PDJyOUW=
PC-3 MknrRZBweHSxc3nzJGF{e2G7 NGnLW25KSzVyPUGuO|U2KM7:TR?= NFfFUnUzOzl2MkC5OS=>
DU145 M4nr[mFxd3C2b4Ppd{BCe3OjeR?= M17VU2lEPTB;Mz61NVch|ryP NEDiZoMzOzl2MkC5OS=>
RC165N NFn0NpRCeG:ydH;zbZMhSXO|YYm= MVTJR|UxRTJwMEizJO69VQ>? Mle0NlM6PDJyOUW=
ARPE19 NYfsboZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTlSG1UVw>? MV3JR|UxRTJ2LkO4JO69VQ>? NVfWTIN{OjN3M{G5NlE>
HEK293 MkL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPQSG1UVw>? NFjodZNKSzVyPUiuOlch|ryP MYeyN|U{OTl{MR?=
KCNR M1XwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjjUVlFVVOR MXzJR|UxRTBwNE[g{txO NHX2e5EzOzV|MUmyNS=>
SY5Y NYfqeG4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVu1UG5bTE2VTx?= MkDBTWM2OD1yLkO2JO69VQ>? NVzybGlkOjN3M{G5NlE>
BE2 NWH6fIY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInhfnNFVVOR MX3JR|UxRTBwN{Gg{txO NGfGTHkzOzV|MUmyNS=>
AS MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXwOFFFVVOR NWTF[FRIUUN3ME2xMlU{KM7:TR?= MmjBNlM2OzF7MkG=
NGP NH3tTnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e4fWROW09? NVzCclR5UUN3ME2wMlU3KM7:TR?= MV2yN|U{OTl{MR?=
IMR32 M4\CZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLEUXNQ M{jEbGlEPTB;MD62OkDPxE1? MX[yN|U{OTl{MR?=
LAN5 M{XhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX4WWh7TE2VTx?= NHTQU4VKSzVyPUGuNFQh|ryP MlPWNlM2OzF7MkG=
RH18 NHrTOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3lSG1UVw>? M2TLOmlEPTB;MT60NkDPxE1? MXuyN|U{OTl{MR?=
RH30 NHXmO5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjwSG1UVw>? MXTJR|UxRTFwMkWg{txO MW[yN|U{OTl{MR?=
RH17 NXLhUVd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDYSG1UVw>? NFrNNIRKSzVyPUKuOVEh|ryP NVjZcmo5OjN3M{G5NlE>
RH28 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LL[mROW09? MVrJR|UxRTRwMkig{txO M1jBN|I{PTNzOUKx
RH36 M{SzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn30SG1UVw>? NEeyNFJKSzVyPUWuN|ch|ryP M{TBNlI{PTNzOUKx
RH41 M{[2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;oT2ZFVVOR MkXaTWM2OD1yLkS4JO69VQ>? MW[yN|U{OTl{MR?=
RD MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrEUXNQ MnTuTWM2OD12LkOyJO69VQ>? M4jiVVI{PTNzOUKx
TC32 MmD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrQSG1UVw>? Mme2TWM2OD1|Lki1JO69VQ>? MVOyN|U{OTl{MR?=
TC71 M1\qRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXjVo1FVVOR NGXle|BKSzVyPUSuN|Mh|ryP MVeyN|U{OTl{MR?=
KCNR MYLBdI9xfG:|aYOgRZN{[Xl? MV[wMlUwOS5yL{KuOUDPxE1? NFjTUYkzPCCq NFi1[GRFVVOR NXe3XFlWcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NGHtOGMzOzV|MUmyNS=>
SY5Y M1OzWWFxd3C2b4Ppd{BCe3OjeR?= NXnPVYlrOC53L{GuNE8zNjVizszN NVnzc|NKOjRiaB?= NWnk[WQ6TE2VTx?= Mo[1bY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MojwNlM2OzF7MkG=
Rh18 MnHwRZBweHSxc3nzJGF{e2G7 NWi4SoVvOC53L{GuNE8zNjVizszN NG\wZlczPCCq M1\rOGROW09? MkjNbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MmPUNlM2OzF7MkG=
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Rh18 M{[zdmZ2dmO2aX;uJGF{e2G7 NX[2[FdDOC53L{GuNE8zNjVxNTFOwG0> NEjUfJYzPCCq NX7HUXY6TE2VTx?= MY\pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= M2LaT|I{PTNzOUKx
TC32 MmfrSpVv[3Srb36gRZN{[Xl? M2PaOlAvPS9zLkCvNk42NzVizszN MWeyOEBp NVLQVVBxTE2VTx?= MoXhbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NX;iOVV[OjN3M{G5NlE>
TPC-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHmTVhKOSEEtV2= MnrnNE01KGR? MoPiSG1UVw>? NUTC[3dEcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOiCmIITy[YF1dWWwdB?= Mnn6NlMxPTZ2OUm=
MZ-CRC1  NIDBcGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LqNVEhyrWP MVewMVUh\A>? MVvEUXNQ M2D1V4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MXWyN|A2PjR7OR?=
TT  MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGxJOK2VQ>? MlS2NE01KGR? MX;EUXNQ MUTpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 MV[yN|A2PjR7OR?=
TPC-1 M2nHXGZ2dmO2aX;uJGF{e2G7 NIXOZlUyKML3TR?= M1PWSFczKGh? NWPZPVNFTE2VTx?= M3yzXIlv\HWlZYOgS|Eh[myxY3vh[4U> MVSyN|A2PjR7OR?=
MZ-CRC1  NI\EcWxHfW6ldHnvckBCe3OjeR?= MXyxJOK2VQ>? MWm3NkBp M3y1SmROW09? M4rLdYlv\HWlZYOgS|Eh[myxY3vh[4U> M4W0WFI{ODV4NEm5
TT  M{TBc2Z2dmO2aX;uJGF{e2G7 MV6xJOK2VQ>? M33vO|czKGh? NGSyfnZFVVOR NHjtbI1qdmS3Y3XzJGcyKGKub3PrZYdm MnfPNlMxPTZ2OUm=
MZ-CRC1  M1j2cWFxd3C2b4Ppd{BCe3OjeR?= NGrBfmwyKML3TR?= NIrxUIw1QCCq M{e2[WROW09? MoXYbY5lfWOnczDhdI9xfG:|aYO= MYOyN|A2PjR7OR?=
TT  MUTBdI9xfG:|aYOgRZN{[Xl? Ml\nNUDDvU1? M1;XWVQ5KGh? M1\5cWROW09? MXjpcoR2[2W|IHHwc5B1d3Orcx?= M3HYXlI{ODV4NEm5
HD-LM2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXVXW9qPzMkgJno NIPjNFFFVVOR MWTJR|UxRTdwOES0JO69VQ>? MVSyNlgzQTB7NB?=
L-428 NWHSToh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX3Omw4OuLCiXi= MlXxSG1UVw>? M3;OW2lEPTB;Nz65OFch|ryP MUGyNlgzQTB7NB?=
KM-H2 MnPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr6TZFqPzMkgJno NWTYfphkTE2VTx?= NWrCXYhCUUN3ME2xMlMxQCEQvF2= NIDXfHczOjh{OUC5OC=>
L-540 MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXnd5N2PzMkgJno NV20OIFWTE2VTx?= NYriN4RxUUN3ME24MlIyPiEQvF2= MnTiNlI5OjlyOUS=
HD-LM2 NFLVbmlHfW6ldHnvckBCe3OjeR?= NWfwT2JLOC5zL{CuOU8yNzVizszN M1jFPVcz6oDLaB?= NHTTZpVFVVOR NHzNSJpqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? M3y3cFIzQDJ7MEm0
L-428 MXzGeY5kfGmxbjDBd5NigQ>? NH7lPGMxNjFxMD61M|EwPSEQvF2= MWq3NwKBkWh? NW\zRYdNTE2VTx?= MYrpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MYSyNlgzQTB7NB?=
KM-H2 MYPGeY5kfGmxbjDBd5NigQ>? MXqwMlEwOC53L{GvOUDPxE1? NEficXk4OuLCiXi= NX3NfnVqTE2VTx?= NHnl[XNqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NEPzb3MzOjh{OUC5OC=>
L-540 M3G0UmZ2dmO2aX;uJGF{e2G7 MVKwMlEwOC53L{GvOUDPxE1? MljuO|LjiImq M{DQ[mROW09? M{\qSIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MV2yNlgzQTB7NB?=
HD-LM2 MnXZRZBweHSxc3nzJGF{e2G7 NFPzdm0yNzVizszN MmjyO|LjiImq M2DafWROW09? Mn7sbY5lfWOnczDhdI9xfG:|aYO= NHXPVoozOjh{OUC5OC=>
L-428 MWPBdI9xfG:|aYOgRZN{[Xl? Mn2yNU82KM7:TR?= NYLtbYZPPzMkgJno NIK5TG5FVVOR MWnpcoR2[2W|IHHwc5B1d3Orcx?= NHmyTIszOjh{OUC5OC=>
KM-H2 MVfBdI9xfG:|aYOgRZN{[Xl? NHPMSpQyNzVizszN NF\MVXI4OuLCiXi= NEmyXVFFVVOR NEm1OmNqdmS3Y3XzJIFxd3C2b4Ppdy=> NH\JWYgzOjh{OUC5OC=>
L-540 MXjBdI9xfG:|aYOgRZN{[Xl? M3v2NVEwPSEQvF2= M3fofFcz6oDLaB?= NXvlcWxVTE2VTx?= MULpcoR2[2W|IHHwc5B1d3Orcx?= NYfZTm5zOjJ6MkmwPVQ>
U251-MG MU\GeY5kfGmxbjDBd5NigQ>? MlHwNUDDvU1? MlH6NE0yPiCq NGfKXJRqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NEn4UoEzOjB{N{[5NS=>
U87-MG NGLhNG9HfW6ldHnvckBCe3OjeR?= MVKxJOK2VQ>? NGTTeZcxNTF4IHi= NYXzS242cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MUeyNlAzPzZ7MR?=
4C8 MoDOSpVv[3Srb36gRZN{[Xl? MnjPNUDDvU1? MVmwMVE3KGh? MmPqbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MlO1NlIxOjd4OUG=
U251-MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInW[lIyNzFyINM1US=> NX3kfWExOjRxNEivO|IhcA>? NXnzXIs6cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MnrjNlIxOjd4OUG=
U87-MG MnrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonYNU8yOCEEtV2= MUOyOE81QC95MjDo NULlPY9{cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MWiyNlAzPzZ7MR?=
4C8 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK5bmcyNzFyINM1US=> MU[yOE81QC95MjDo NVPubZVkcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MXqyNlAzPzZ7MR?=
U266 Ml7aRZBweHSxc3nzJGF{e2G7 NUTYPWs6OC53LUKg{txO NXPMXnNEPDhxN{KgbC=> NHLJWJBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MX2yNVE3PDVzNx?=
Kms.11 M1;2VGFxd3C2b4Ppd{BCe3OjeR?= M{Li[lAvPS1{IN88US=> MVK0PE84OiCq NHi1SHNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NH\SOZIzOTF4NEWxOy=>
8226 MlLNRZBweHSxc3nzJGF{e2G7 M3y0WVAvPS1{IN88US=> NFnxdIo1QC95MjDo M3fBd4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Mn\oNlEyPjR3MUe=

... 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
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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 )

  • 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