AZD1480

For research use only.

Catalog No.S2162

78 publications

AZD1480 Chemical Structure

CAS No. 935666-88-9

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 78 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 MWLGeY5kfGmxbjDBd5NigQ>? NHjzVJU2KM7:TR?= MmrnOFghcA>? MkTvSG1UVw>? M13Ud4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> M3LGNVI2QTV2OUe0
LoVo  MVrGeY5kfGmxbjDBd5NigQ>? Mmm1OUDPxE1? MlzFOFghcA>? NFX5PFdFVVOR M1y4T4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> NXniRWt2OjV7NUS5O|Q>
HN5 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHrO|IhcA>? NWnXNI1jTUN3ME2zMlgyKMLzIEGuPVkh|ryP NH\TWpEzPThzMECxNC=>
Cal33 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO2bGY4OiCq NXfMb5VmTUN3ME2zMlM4KMLzIECuO|Uh|ryP NH35TnozPThzMECxNC=>
UM-22B MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi3NkBp M3XCUmVEPTB;Mj62OkDDuSByLkK0JO69VQ>? NF7RTFQzPThzMECxNC=>
686LN M33XRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfkO|IhcA>? MXXFR|UxRTJwMEWgxtEhOS5|MzFOwG0> NX:xdYFEOjV6MUCwNVA>
UM SCC-1 NW\kSVJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzEO|IhcA>? NY\jSXhlTUN3ME2xMlY4KMLzIECuOFIh|ryP MVmyOVgyODBzMB?=
UM-22A MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr5O|IhcA>? NEjnSXNGSzVyPUGuN|IhyrFiMD6zPUDPxE1? NVnJW4p[OjV6MUCwNVA>
OSC19 NE\GdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ew[VczKGh? NEL6Nm5GSzVyPUGuNlYhyrFiMD6yNEDPxE1? M3fG[VI2QDFyMEGw
PCI-52 M4ixfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLoO|IhcA>? NWf1S2tlTUN3ME2xMlAxKMLzIECuNFkh|ryP MYqyOVgyODBzMB?=
PCI-15B NE\ZTnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH6d|N6PzJiaB?= NV:2UJh6TUN3ME2wMlk6KMLzIEGuO|Qh|ryP NWqwcnJDOjV6MUCwNVA>
UMSCC-1 NG\IZodHfW6ldHnvckBCe3OjeR?= MmnkNE4xODB3LUGuOkDPxE1? NXXQZXdGOjRiaB?= M{Gz[IFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWOyOVgyODBzMB?=
Cal33 M36wTGZ2dmO2aX;uJGF{e2G7 NHy2bmgxNjByMEWtN{45KM7:TR?= MoW5NlQhcA>? MmjCZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M37Hb|I2QDFyMEGw
HH5 NFnmNnFHfW6ldHnvckBCe3OjeR?= NYH5T2pqOC5yMEC1MVMvQCEQvF2= NIDBV48zPCCq MXThZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NV6wSHd5OjV6MUCwNVA>
UM-22A NGLvbnNHfW6ldHnvckBCe3OjeR?= NHm5fHMxNjByMEWtNU43KM7:TR?= M1\UUlI1KGh? MWDhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGXrWZIzPThzMECxNC=>
A1847 M1HkSGZ2dmO2aX;uJGF{e2G7 MU[wMlA2NTFyIN88US=> NX3PPYtROjRiaB?= NVvJWY9QTE2VT9Mg MXzy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NW\OWHFzOjV4NE[wNVU>
OVCAR-5 M{HIZ2Z2dmO2aX;uJGF{e2G7 MYGwMlA2NTFyIN88US=> MViyOEBp M13QOmROW00EoB?= MXHy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MlLlNlU3PDZyMUW=
OVCAR-8 Mn\XSpVv[3Srb36gRZN{[Xl? MUiwMlA2NTFyIN88US=> MXGyOEBp M3zROGROW00EoB?= M{CyUZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MmLINlU3PDZyMUW=
MOVCAR-5447 MXnGeY5kfGmxbjDBd5NigQ>? MkfsNE4xPS1zMDFOwG0> MkfYNlQhcA>? MnzJSG1UV8Li MVvy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NFnr[3MzPTZ2NkCxOS=>
MOVCAR-5009 M{nCemZ2dmO2aX;uJGF{e2G7 NIPBU5kxNjB3LUGwJO69VQ>? M3PqcFI1KGh? NFT0dGtFVVORwrC= NIPDU25z\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MkHhNlU3PDZyMUW=
A1847 M2\GbmNmdGxiVnnhZoltcXS7IFHzd4F6 NGnFTGcxNjB3LUGwJO69VQ>? NWXleWxGPzJiaB?= MnPvSG1UVw>? MX;y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M3TWe|I2PjR4MEG1
OVCAR-5 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{\wTFAvODVvMUCg{txO Mlm1O|IhcA>? M3vsXWROW09? M4\4ZpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MkHhNlU3PDZyMUW=
OVCAR-8  NGK2W3JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Ml75NE4xPS1zMDFOwG0> MV63NkBp Mn;YSG1UVw>? MoDrdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NGGwRpgzPTZ2NkCxOS=>
OVCAR-5  Mo\oRZBweHSxc3nzJGF{e2G7 NIHmUWUxNjVxMT:1JO69VQ>? MYW0PEBp NY\LW|dyTE2VTx?= NUXIXoVwcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> MkPBNlU3PDZyMUW=
OVCAR-8  MnrpRZBweHSxc3nzJGF{e2G7 NXzyfFZrOC53L{GvOUDPxE1? M2HWR|Q5KGh? NWfON5NPTE2VTx?= MUTpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w MVeyOVY1PjBzNR?=
AKRSL NFPZXmVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVfrVmFpPzJiaB?= MWnJR|Ux97zgMUCg{txO NWLUZ|Y3OjV3MES2N|U>
PALJDL NGHGRndE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M171SlczKGh? MlS3TWM2OD1{LkSg{txO M{DpXFI2PTB2NkO1
MO4 M4rFVWZ2dmO2aX;uJGF{e2G7 NYG2b4xkOC53L{GvOUDPxE1? NHHuWWQ3KGh? M163O4lvcGmkaYTzJHAuW1SDVEOg[ZhxemW|c3nvcuKh MYSyOVE1QTV|NR?=
DU145  NUXBcVVmTnWwY4Tpc44hSXO|YYm= M3\NZVAuOjByIH7N NUXvSGlGOSCqwrC= MYfzeZBxemW|c3XzJGlNNTZvYXP0bZZifGWmIGP0ZZQ{KGGwZDDFVmsyNzJic3nncoFtcW6p NImyb2gzPDV5N{m0Ni=>
DU145  M{fQZWZ2dmO2aX;uJGF{e2G7 NF;rdZM5ODBibl2= MYG3NkBp MlXZd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 MlnvNlQ2Pzd7NEK=
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N592 Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDyTWM2OD1yLki0JO69VQ>? Mmj0NlQyPTh5MEG=
H82 M4T6RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\qTWM2OD1zLkO3JO69VQ>? MoXINlQyPTh5MEG=
GLC4 M1\hO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PyPWlEPTB;MT63PUDPxE1? NH:5S3EzPDF3OEewNS=>
H526 MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTNwMEig{txO NX\mO2djOjRzNUi3NFE>
H1173 M{DYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DYOmlEPTB;Mj6zPUDPxE1? NHrHTowzPDF3OEewNS=>
DMS114 NFP1NXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwN{Og{txO Mk\vNlQyPTh5MEG=
NCI-N592 MWnGeY5kfGmxbjDBd5NigQ>? NITmZlcxNjNxMT:zJO69VQ>? M3HVXVI1KGh? MlXUbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MVOyOFE2QDdyMR?=
GLC4 MnTNSpVv[3Srb36gRZN{[Xl? NIniT|UxNjNxMT:zJO69VQ>? M2TIUlI1KGh? MX3pcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> MXmyOFE2QDdyMR?=
NCI-H82 M{DGUWZ2dmO2aX;uJGF{e2G7 MkPVNE4{NzFxMzFOwG0> NUDudYYzOjRiaB?= NG\XeXVqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NXzFc4JXOjRzNUi3NFE>
NCI-N592 M4r0cWFxd3C2b4Ppd{BCe3OjeR?= NYW0TVlIOC5|L{GvN{DPxE1? NVzEdW1wPDhiaB?= M37TVolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NYnXd|JIOjRzNUi3NFE>
GLC4 M1LYd2Fxd3C2b4Ppd{BCe3OjeR?= NVuwTJg6OC5|L{GvN{DPxE1? MY[0PEBp MVHpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NXTrc3FsOjRzNUi3NFE>
NCI-H82 MV;BdI9xfG:|aYOgRZN{[Xl? NFe1WJQxNjNxMT:zJO69VQ>? M2OxRlQ5KGh? MXrpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NXT3[IJ6OjRzNUi3NFE>
CWR22Rv1  M2\WV2Fxd3C2b4Ppd{BCe3OjeR?= NHrKUXZKSzVyPUCuOFgzKM7:TR?= NXK3TnY3OjN7NEKwPVU>
CWR22Pc NIPZfWVCeG:ydH;zbZMhSXO|YYm= M3fCUGlEPTB;MD60N|gh|ryP MlPWNlM6PDJyOUW=
PC-3 NF[4[VBCeG:ydH;zbZMhSXO|YYm= M1O0VmlEPTB;MT63OVUh|ryP MYCyN|k1OjB7NR?=
DU145 NWq2RVRDSXCxcITvd4l{KEG|c3H5 MlTGTWM2OD1|LkWxO{DPxE1? MkDXNlM6PDJyOUW=
RC165N MXLBdI9xfG:|aYOgRZN{[Xl? MlTVTWM2OD1{LkC4N{DPxE1? NYqzRXcyOjN7NEKwPVU>
ARPE19 NH7yc2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjrbJpnTE2VTx?= Ml7RTWM2OD1{ND6zPEDPxE1? NUPpSIh[OjN3M{G5NlE>
HEK293 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HJeGROW09? M1XmSmlEPTB;OD62O{DPxE1? M2q5XlI{PTNzOUKx
KCNR NH\SXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHEUXNQ MoC5TWM2OD1yLkS2JO69VQ>? Ml\5NlM2OzF7MkG=
SY5Y NF3ocYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;ifmROW09? NHnDW5VKSzVyPUCuN|Yh|ryP M3OzV|I{PTNzOUKx
BE2 NUS3PYhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[0SG1UVw>? MXTJR|UxRTBwN{Gg{txO MVSyN|U{OTl{MR?=
AS M1TVXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHEV4Z2TE2VTx?= MYTJR|UxRTFwNUOg{txO NIH5XHQzOzV|MUmyNS=>
NGP Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHOSG1UVw>? MlTnTWM2OD1yLkW2JO69VQ>? Mlz1NlM2OzF7MkG=
IMR32 M3vWXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO1SG1UVw>? M{XabmlEPTB;MD62OkDPxE1? NVnQRYFNOjN3M{G5NlE>
LAN5 NWPWSWxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrEUXNQ NH\RUIxKSzVyPUGuNFQh|ryP NFXh[WMzOzV|MUmyNS=>
RH18 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7EUXNQ M3XNNmlEPTB;MT60NkDPxE1? NHXz[5EzOzV|MUmyNS=>
RH30 MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PBdGROW09? NIXxdJpKSzVyPUGuNlUh|ryP MlTQNlM2OzF7MkG=
RH17 NXL4doVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjEUXNQ NVW0fnVRUUN3ME2yMlUyKM7:TR?= NEX6ZXczOzV|MUmyNS=>
RH28 M1LTdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULvVnIyTE2VTx?= NF3XOlJKSzVyPUSuNlgh|ryP M3G3WVI{PTNzOUKx
RH36 NX3uXHVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfEUXNQ M1TY[WlEPTB;NT6zO{DPxE1? MUSyN|U{OTl{MR?=
RH41 NW\tV41{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PVU2ROW09? NGS4RpZKSzVyPUCuOFgh|ryP MV[yN|U{OTl{MR?=
RD M1P4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzXbmUxTE2VTx?= NYjwclhYUUN3ME20MlMzKM7:TR?= NH3tNoEzOzV|MUmyNS=>
TC32 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPPSG1UVw>? MnPtTWM2OD1|Lki1JO69VQ>? M4r0fVI{PTNzOUKx
TC71 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH6SG1UVw>? NUPnOm9OUUN3ME20MlM{KM7:TR?= NX;Re|M2OjN3M{G5NlE>
KCNR MVvBdI9xfG:|aYOgRZN{[Xl? NITLR|kxNjVxMT6wM|IvPSEQvF2= NInSd4wzPCCq NFnXWYhFVVOR MUPpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MYCyN|U{OTl{MR?=
SY5Y NHnHeI5CeG:ydH;zbZMhSXO|YYm= NXjI[nhPOC53L{GuNE8zNjVizszN MXOyOEBp MYPEUXNQ M3rNW4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MWSyN|U{OTl{MR?=
Rh18 MUXBdI9xfG:|aYOgRZN{[Xl? MnjNNE42NzFwMD:yMlUh|ryP MYqyOEBp NFf1fohFVVOR MYnpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MkfQNlM2OzF7MkG=
TC32 NGLYNHpCeG:ydH;zbZMhSXO|YYm= MoLFNE42NzFwMD:yMlUh|ryP M3\x[FI1KGh? MX;EUXNQ NX7uNYN2cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NXLQcXRHOjN3M{G5NlE>
KCNR NIe0WopHfW6ldHnvckBCe3OjeR?= NFHVR|IxNjVxMT6wM|IvPS93IN88US=> MXKyOEBp NEeySGdFVVOR NXj1coNEcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MoXMNlM2OzF7MkG=
SY5Y MoLUSpVv[3Srb36gRZN{[Xl? Mlq4NE42NzFwMD:yMlUwPSEQvF2= NHjBNmYzPCCq M{HX[WROW09? M2PlTYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NWD3T252OjN3M{G5NlE>
Rh18 MWLGeY5kfGmxbjDBd5NigQ>? NIDSfoQxNjVxMT6wM|IvPS93IN88US=> M2fkXlI1KGh? M4Hse2ROW09? MVzpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= M4DySlI{PTNzOUKx
TC32 NEDnO3NHfW6ldHnvckBCe3OjeR?= M4jWS|AvPS9zLkCvNk42NzVizszN NHTDZ4MzPCCq MVrEUXNQ MXLpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= Mn3nNlM2OzF7MkG=
TPC-1 NEHGV5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHJOGExOSEEtV2= M3PPdlAuPCCm MoXTSG1UVw>? MUTpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 NYPJVVc1OjNyNU[0PVk>
MZ-CRC1  NIPQUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXYWVAyKML3TR?= MlfTNE02KGR? MY\EUXNQ MWPpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 MYOyN|A2PjR7OR?=
TT  M1LKdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoOyNUDDvU1? NFfQSXgxNTRiZB?= NIi5[GNFVVOR NID1d|BqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MlzQNlMxPTZ2OUm=
TPC-1 NH7VN5dHfW6ldHnvckBCe3OjeR?= NXKxb4pQOSEEtV2= NGHTdpc4OiCq MXXEUXNQ M1XSXIlv\HWlZYOgS|Eh[myxY3vh[4U> MXGyN|A2PjR7OR?=
MZ-CRC1  NUjhcGhTTnWwY4Tpc44hSXO|YYm= NFjk[GgyKML3TR?= MVK3NkBp NHexPYpFVVOR NHniTnlqdmS3Y3XzJGcyKGKub3PrZYdm NXPzRY9TOjNyNU[0PVk>
TT  MVLGeY5kfGmxbjDBd5NigQ>? MUCxJOK2VQ>? Mk\OO|IhcA>? MVfEUXNQ Ml7EbY5lfWOnczDHNUBjdG:la3Hn[S=> M{PGRlI{ODV4NEm5
MZ-CRC1  MU\BdI9xfG:|aYOgRZN{[Xl? NEfGOmkyKML3TR?= NX;H[48{PDhiaB?= M2fTdGROW09? NXzheJo{cW6mdXPld{BieG:ydH;zbZM> NH3rclczOzB3NkS5PS=>
TT  NWnCSVlOSXCxcITvd4l{KEG|c3H5 M{fFOlEhyrWP NW\3UGVYPDhiaB?= NF7lcGFFVVOR NFjCU5JqdmS3Y3XzJIFxd3C2b4Ppdy=> NGDFb5IzOzB3NkS5PS=>
HD-LM2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\MO|LjiImq NG\M[W1FVVOR M1zZOGlEPTB;Nz64OFQh|ryP NYPuRVg5OjJ6MkmwPVQ>
L-428 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUji[WJQPzMkgJno MYXEUXNQ NVO5ZlNiUUN3ME23Mlk1PyEQvF2= MUKyNlgzQTB7NB?=
KM-H2 MnXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnKVFdLPzMkgJno M1\HTWROW09? M2W5cWlEPTB;MT6zNFgh|ryP NILCWnUzOjh{OUC5OC=>
L-540 MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVO3NwKBkWh? MUnEUXNQ Mkj3TWM2OD16LkKxOkDPxE1? NF;yeJQzOjh{OUC5OC=>
HD-LM2 MYfGeY5kfGmxbjDBd5NigQ>? M{LudFAvOS9yLkWvNU82KM7:TR?= MVe3NwKBkWh? MmHoSG1UVw>? NXn3OYpycW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NHLnenczOjh{OUC5OC=>
L-428 NFe0[|RHfW6ldHnvckBCe3OjeR?= NXLCWFRKOC5zL{CuOU8yNzVizszN M3S5NVcz6oDLaB?= NWjRbJpMTE2VTx?= MoW2bY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NXPMNpdpOjJ6MkmwPVQ>
KM-H2 M3zFS2Z2dmO2aX;uJGF{e2G7 Mmf5NE4yNzBwNT:xM|Uh|ryP Mne0O|LjiImq NV3BN3p[TE2VTx?= NVLkSoh7cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NHuxPYMzOjh{OUC5OC=>
L-540 MoDUSpVv[3Srb36gRZN{[Xl? M3HRPVAvOS9yLkWvNU82KM7:TR?= NUDoWmZ{PzMkgJno MkXtSG1UVw>? NIf6[I1qdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NWm5UJBvOjJ6MkmwPVQ>
HD-LM2 M4TQdmFxd3C2b4Ppd{BCe3OjeR?= M3nzSFEwPSEQvF2= Ml\WO|LjiImq NFG5VlJFVVOR MmPrbY5lfWOnczDhdI9xfG:|aYO= Mn\INlI5OjlyOUS=
L-428 M4rOV2Fxd3C2b4Ppd{BCe3OjeR?= MmHLNU82KM7:TR?= NGnE[2I4OuLCiXi= MUXEUXNQ M{TO[4lv\HWlZYOgZZBweHSxc3nz NXzwN5lpOjJ6MkmwPVQ>
KM-H2 M3;SWmFxd3C2b4Ppd{BCe3OjeR?= NV\sdGNyOS93IN88US=> NX7FSY9xPzMkgJno NWDK[HZKTE2VTx?= NX;wT3hWcW6mdXPld{BieG:ydH;zbZM> NGfHd5ozOjh{OUC5OC=>
L-540 NUjHWY9JSXCxcITvd4l{KEG|c3H5 NHHVUJkyNzVizszN NFvKO5M4OuLCiXi= NVP1UY5PTE2VTx?= NU\6ZoFUcW6mdXPld{BieG:ydH;zbZM> NI\tWZMzOjh{OUC5OC=>
U251-MG MlXKSpVv[3Srb36gRZN{[Xl? NVL5U3lROSEEtV2= MnHQNE0yPiCq NFvvTI5qdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NY\Rb4I1OjJyMke2PVE>
U87-MG MW\GeY5kfGmxbjDBd5NigQ>? MUSxJOK2VQ>? NYDMe3Q1OC1zNjDo M1fpOYlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? M2f2bVIzODJ5Nkmx
4C8 MWTGeY5kfGmxbjDBd5NigQ>? NFXMdGUyKML3TR?= NYfWNVVVOC1zNjDo NHnvXVZqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NXO1UWlZOjJyMke2PVE>
U251-MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[xM|ExKML3TR?= MkHyNlQwPDhxN{KgbC=> NEPtc3ZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NXfKb4FrOjJyMke2PVE>
U87-MG NVT3clJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf4V4QyNzFyINM1US=> M3P5N|I1NzR6L{eyJIg> NXvmXpdxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? Mk\2NlIxOjd4OUG=
4C8 MnrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPjNU8yOCEEtV2= MmG0NlQwPDhxN{KgbC=> NHPGNnBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MknwNlIxOjd4OUG=
U266 NGHtNYdCeG:ydH;zbZMhSXO|YYm= MYSwMlUuOiEQvF2= NHjkeFk1QC95MjDo M3;pZYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M{XpcFIyOTZ2NUG3
Kms.11 NV;5dlQzSXCxcITvd4l{KEG|c3H5 M4jkS|AvPS1{IN88US=> NWD5XZQ{PDhxN{KgbC=> M1Xwfolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NV\0OYl1OjFzNkS1NVc>
8226 NV7Ybop5SXCxcITvd4l{KEG|c3H5 MoHLNE42NTJizszN NVHaUnNtPDhxN{KgbC=> NVfiTmJtcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NULGZlg4OjFzNkS1NVc>

... 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 CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F

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 ()
% 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):
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    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