AZD1480

Catalog No.S2162

AZD1480 Chemical Structure

Molecular Weight(MW): 348.77

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

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In DMSO USD 130 In stock
USD 100 In stock
USD 170 In stock
USD 570 In stock
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Cited by 35 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 NHfMWnhHfW6ldHnvckBCe3OjeR?= Ml2xOUDPxE1? Ml7iOFghcA>? MUHEUXNQ MWLicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= NUTXO5lrOjV7NUS5O|Q>
LoVo  MlnsSpVv[3Srb36gRZN{[Xl? NGmyVXc2KM7:TR?= NHLBb4Y1QCCq Mnz6SG1UVw>? NFzvbXRjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NF34[YMzPTl3NEm3OC=>
HN5 M4q5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn25O|IhcA>? MXzFR|UxRTNwOEGgxtEhOS57OTFOwG0> MXKyOVgyODBzMB?=
Cal33 M{nwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrMSpY4OiCq NVXpXWZrTUN3ME2zMlM4KMLzIECuO|Uh|ryP NXe3TGd7OjV6MUCwNVA>
UM-22B NYDlRZg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rIU|czKGh? Mn3qSWM2OD1{Lk[2JOKyKDBwMkSg{txO NFTQPZIzPThzMECxNC=>
686LN MmHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXzO|IhcA>? MmKzSWM2OD1{LkC1JOKyKDFwM{Og{txO NFvYdFkzPThzMECxNC=>
UM SCC-1 NEC4[4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm3NkBp NFrUdoJGSzVyPUGuOlchyrFiMD60NkDPxE1? MnLiNlU5OTByMUC=
UM-22A M2PUVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGWyUIc4OiCq NXHiNY1HTUN3ME2xMlMzKMLzIECuN|kh|ryP MlnQNlU5OTByMUC=
OSC19 M3jJ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XLVlczKGh? MVjFR|UxRTFwMk[gxtEhOC5{MDFOwG0> M1uwWFI2QDFyMEGw
PCI-52 NFvndItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofPO|IhcA>? NHrPZlFGSzVyPUGuNFAhyrFiMD6wPUDPxE1? MXmyOVgyODBzMB?=
PCI-15B NUTQXHBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXS3NkBp M3O1R2VEPTB;MD65PUDDuSBzLke0JO69VQ>? NXvvPZAxOjV6MUCwNVA>
UMSCC-1 M3;zOmZ2dmO2aX;uJGF{e2G7 MlHoNE4xODB3LUGuOkDPxE1? M1HRdVI1KGh? MUXhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NWXsdmZKOjV6MUCwNVA>
Cal33 M1XNdGZ2dmO2aX;uJGF{e2G7 M3TVWVAvODByNT2zMlgh|ryP NUnqOHdEOjRiaB?= Ml;aZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXqyOVgyODBzMB?=
HH5 NXPke2c{TnWwY4Tpc44hSXO|YYm= MXOwMlAxODVvMz64JO69VQ>? MmXRNlQhcA>? NVvHWoUy[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFPP[pAzPThzMECxNC=>
UM-22A MmPlSpVv[3Srb36gRZN{[Xl? MVuwMlAxODVvMT62JO69VQ>? MlPzNlQhcA>? NHfJb2Ri[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFLQO28zPThzMECxNC=>
A1847 M{fTfWZ2dmO2aX;uJGF{e2G7 MX[wMlA2NTFyIN88US=> NUny[ZNOOjRiaB?= NULWN4pZTE2VT9Mg MV7y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NYfZVIVPOjV4NE[wNVU>
OVCAR-5 M4\ucGZ2dmO2aX;uJGF{e2G7 M1fUbFAvODVvMUCg{txO NH\YVFYzPCCq NY\iVWJ7TE2VT9Mg NWXKeoFSemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NVXK[G9WOjV4NE[wNVU>
OVCAR-8 NV2wbYh7TnWwY4Tpc44hSXO|YYm= NUXYNGNoOC5yNT2xNEDPxE1? NGW1XG0zPCCq Mo\tSG1UV8Li MnrkdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NIG4UJQzPTZ2NkCxOS=>
MOVCAR-5447 M2X5UGZ2dmO2aX;uJGF{e2G7 NG\TWFYxNjB3LUGwJO69VQ>? NFGw[FUzPCCq NWPycppITE2VT9Mg NVTZV2JQemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MmnXNlU3PDZyMUW=
MOVCAR-5009 MV7GeY5kfGmxbjDBd5NigQ>? NXnTTlVIOC5yNT2xNEDPxE1? M{nLcVI1KGh? MmDTSG1UV8Li Mmq3doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MV6yOVY1PjBzNR?=
A1847 MnTvR4VtdCCYaXHibYxqfHliQYPzZZk> NUTrVWh{OC5yNT2xNEDPxE1? MmL3O|IhcA>? M4\lNGROW09? NYTTTG9KemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NHHncWczPTZ2NkCxOS=>
OVCAR-5 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH;Gdo8xNjB3LUGwJO69VQ>? MXi3NkBp M13HTmROW09? MoHMdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MmfuNlU3PDZyMUW=
OVCAR-8  MlSxR4VtdCCYaXHibYxqfHliQYPzZZk> M2LmOVAvODVvMUCg{txO MU[3NkBp M1LBe2ROW09? NUfnSZRyemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> M1nZWVI2PjR4MEG1
OVCAR-5  MlrDRZBweHSxc3nzJGF{e2G7 Ml25NE42NzFxNTFOwG0> MnLDOFghcA>? NGq3N4xFVVOR MoPKbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= MYKyOVY1PjBzNR?=
OVCAR-8  M2jGfWFxd3C2b4Ppd{BCe3OjeR?= MUCwMlUwOS93IN88US=> NFvOVlg1QCCq NYjBfW9ZTE2VTx?= NXPWd|F1cW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M2OwbVI2PjR4MEG1
AKRSL NH7PS3hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUnhVnlJPzJiaB?= NYTJW5hWUUN3MP-8olExKM7:TR?= NGOxcVkzPTVyNE[zOS=>
PALJDL NEDEOnBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX63NkBp NXLoSow6UUN3ME2yMlQh|ryP NF;BbYMzPTVyNE[zOS=>
MO4 MXzGeY5kfGmxbjDBd5NigQ>? NXvQb3VtOC53L{GvOUDPxE1? MUm2JIg> MVTpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> NH2y[JEzPTF2OUWzOS=>
DU145  NWPncmFGTnWwY4Tpc44hSXO|YYm= Mn2yNE0zODBibl2= MXexJIjDqA>? MmHNd5VxeHKnc4Pld{BKVC14LXHjeIl3[XSnZDDTeIF1OyCjbnSgSXJMOS9{IIPp[45idGmwZx?= NGXaRnozPDV5N{m0Ni=>
DU145  MkHISpVv[3Srb36gRZN{[Xl? MmPwPFAxKG6P NFzIV|Q4OiCq MYnzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? NIXlc2MzPDV5N{m0Ni=>
CWR22Rv1 MYHGeY5kfGmxbjDBd5NigQ>? NV;CeYJyQDByIH7N NF3tRlQ4OiCq NFHHcoV{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= M{jRS|I1PTd5OUSy
N592 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PoWGlEPTB;MD64OEDPxE1? MXeyOFE2QDdyMR?=
H82 Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFwM{eg{txO NFHvOpUzPDF3OEewNS=>
GLC4 NXTGW|JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjQTWM2OD1zLke5JO69VQ>? NIO4cFczPDF3OEewNS=>
H526 Mnm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPkb5JqUUN3ME2zMlA5KM7:TR?= NImzS2EzPDF3OEewNS=>
H1173 NIXzdlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJwM{mg{txO NV;R[HBiOjRzNUi3NFE>
DMS114 M1Wwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEf1dnlKSzVyPUCuO|Mh|ryP MmrlNlQyPTh5MEG=
NCI-N592 M{PlR2Z2dmO2aX;uJGF{e2G7 NYW0V3l6OC5|L{GvN{DPxE1? NFvVdHczPCCq MVXpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NVXEUFJnOjRzNUi3NFE>
GLC4 M1q3PGZ2dmO2aX;uJGF{e2G7 NGnCXmYxNjNxMT:zJO69VQ>? M1fDTlI1KGh? NEPnXWZqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MVKyOFE2QDdyMR?=
NCI-H82 NGnB[otHfW6ldHnvckBCe3OjeR?= NGfZVo8xNjNxMT:zJO69VQ>? NYTFXIdNOjRiaB?= NWXkZYpicW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NIDDOlkzPDF3OEewNS=>
NCI-N592 MUDBdI9xfG:|aYOgRZN{[Xl? NUTJOpFuOC5|L{GvN{DPxE1? M13OT|Q5KGh? NYLXW2d[cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MkTVNlQyPTh5MEG=
GLC4 NH\SUlBCeG:ydH;zbZMhSXO|YYm= NHri[5MxNjNxMT:zJO69VQ>? NWjX[JVGPDhiaB?= M1;Ibolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NFXrOYgzPDF3OEewNS=>
NCI-H82 MXrBdI9xfG:|aYOgRZN{[Xl? MXOwMlMwOS9|IN88US=> MYS0PEBp NIDRNZlqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NXzubYZIOjRzNUi3NFE>
CWR22Rv1  MVjBdI9xfG:|aYOgRZN{[Xl? NWHETZlKUUN3ME2wMlQ5OiEQvF2= NHrVOowzOzl2MkC5OS=>
CWR22Pc MkmzRZBweHSxc3nzJGF{e2G7 NGDRXIlKSzVyPUCuOFM5KM7:TR?= NFPwUHEzOzl2MkC5OS=>
PC-3 MXjBdI9xfG:|aYOgRZN{[Xl? M{jvb2lEPTB;MT63OVUh|ryP MmXUNlM6PDJyOUW=
DU145 MlnwRZBweHSxc3nzJGF{e2G7 M4O4TWlEPTB;Mz61NVch|ryP NUnGWXl4OjN7NEKwPVU>
RC165N MoruRZBweHSxc3nzJGF{e2G7 MlLZTWM2OD1{LkC4N{DPxE1? MmjQNlM6PDJyOUW=
ARPE19 NUTmS4Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HzUWROW09? M{XJcmlEPTB;MkSuN|gh|ryP NVLIeGYyOjN3M{G5NlE>
HEK293 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjEUXNQ NVe3bYdwUUN3ME24MlY4KM7:TR?= MVyyN|U{OTl{MR?=
KCNR NFzPOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom5SG1UVw>? NYH0W4dmUUN3ME2wMlQ3KM7:TR?= M2HLeVI{PTNzOUKx
SY5Y MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLFSG1UVw>? MYDJR|UxRTBwM{[g{txO MmPGNlM2OzF7MkG=
BE2 NXXzdGhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\B[mROW09? NVnm[pJkUUN3ME2wMlcyKM7:TR?= MYGyN|U{OTl{MR?=
AS NGTlO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\MeGROW09? M4fC[WlEPTB;MT61N{DPxE1? NUfNOItEOjN3M{G5NlE>
NGP NVf4fI9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIC3c4JFVVOR Ml\GTWM2OD1yLkW2JO69VQ>? M1zXR|I{PTNzOUKx
IMR32 NYXD[XF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfSSG1UVw>? MVXJR|UxRTBwNk[g{txO NXnMOIhTOjN3M{G5NlE>
LAN5 NYTpblh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLEUXNQ NWjaTJdtUUN3ME2xMlA1KM7:TR?= NI\DbIMzOzV|MUmyNS=>
RH18 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTEUXNQ MXTJR|UxRTFwNEKg{txO M2q3OVI{PTNzOUKx
RH30 NV;mcFh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn24SG1UVw>? MnPuTWM2OD1zLkK1JO69VQ>? MlPjNlM2OzF7MkG=
RH17 NYPL[o5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjZW3VFVVOR Mn;6TWM2OD1{LkWxJO69VQ>? NEHOWmgzOzV|MUmyNS=>
RH28 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\PSG1UVw>? MUnJR|UxRTRwMkig{txO NFjk[JEzOzV|MUmyNS=>
RH36 NHi1fmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPoR4VKTE2VTx?= NGnXbopKSzVyPUWuN|ch|ryP M2rTfFI{PTNzOUKx
RH41 NULtV3RmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfJSG1UVw>? Mof4TWM2OD1yLkS4JO69VQ>? NHHRcYMzOzV|MUmyNS=>
RD MlT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy3TpdFVVOR MnvFTWM2OD12LkOyJO69VQ>? MVqyN|U{OTl{MR?=
TC32 MmjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PwOWROW09? M{PrRmlEPTB;Mz64OUDPxE1? MV6yN|U{OTl{MR?=
TC71 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCxSG1UVw>? MXvJR|UxRTRwM{Og{txO M3fqTFI{PTNzOUKx
KCNR NYTWbHZRSXCxcITvd4l{KEG|c3H5 NXzifGQ3OC53L{GuNE8zNjVizszN MWSyOEBp MoHrSG1UVw>? NVXTWoRzcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MnfPNlM2OzF7MkG=
SY5Y MX7BdI9xfG:|aYOgRZN{[Xl? NV;KUZBiOC53L{GuNE8zNjVizszN NUP1[o1ROjRiaB?= MY\EUXNQ MX\pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MYWyN|U{OTl{MR?=
Rh18 NWjWdWZxSXCxcITvd4l{KEG|c3H5 M1jYTlAvPS9zLkCvNk42KM7:TR?= M3TwSFI1KGh? M1jLUGROW09? MYnpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NYq0eWdKOjN3M{G5NlE>
TC32 NY\IOXdYSXCxcITvd4l{KEG|c3H5 M{jUW|AvPS9zLkCvNk42KM7:TR?= NInyRWUzPCCq NGrVS41FVVOR M3\sVIlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NFn1OGwzOzV|MUmyNS=>
KCNR MUfGeY5kfGmxbjDBd5NigQ>? NV7ZPG1wOC53L{GuNE8zNjVxNTFOwG0> NX3MbXZlOjRiaB?= NIGzWYJFVVOR NHvrWYtqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MWOyN|U{OTl{MR?=
SY5Y NHnRbXlHfW6ldHnvckBCe3OjeR?= MXOwMlUwOS5yL{KuOU82KM7:TR?= MWWyOEBp MnLXSG1UVw>? NVHTXlNtcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MUeyN|U{OTl{MR?=
Rh18 M2fQZmZ2dmO2aX;uJGF{e2G7 MU[wMlUwOS5yL{KuOU82KM7:TR?= MkCzNlQhcA>? M4LPOWROW09? MVXpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NV7wbGw1OjN3M{G5NlE>
TC32 NGTXT3hHfW6ldHnvckBCe3OjeR?= Mk\5NE42NzFwMD:yMlUwPSEQvF2= NFHlSIMzPCCq NFrZUnlFVVOR NIizXlNqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> M3vGd|I{PTNzOUKx
TPC-1 M1;Zfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXle|VMOSEEtV2= MVWwMVQh\A>? NHe2OldFVVOR M1TQdolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? NXHkfW9UOjNyNU[0PVk>
MZ-CRC1  MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHyzTGsyKML3TR?= MlrtNE02KGR? NVrUZ5dtTE2VTx?= Ml3wbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? NGjGbYkzOzB3NkS5PS=>
TT  MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3sXoMyKML3TR?= NXHpcWhHOC12IHS= NVy1XY5wTE2VTx?= NV7pOpVscW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= MVyyN|A2PjR7OR?=
TPC-1 MmK1SpVv[3Srb36gRZN{[Xl? NWXBfoFCOSEEtV2= NWHKd4xJPzJiaB?= NYP6[2RGTE2VTx?= NIfZOmlqdmS3Y3XzJGcyKGKub3PrZYdm M2PCNVI{ODV4NEm5
MZ-CRC1  NYC3bWR5TnWwY4Tpc44hSXO|YYm= NEG3bo0yKML3TR?= MVe3NkBp NH2xOnlFVVOR M2j6PIlv\HWlZYOgS|Eh[myxY3vh[4U> MlLLNlMxPTZ2OUm=
TT  NX\NVVZzTnWwY4Tpc44hSXO|YYm= M2HTfVEhyrWP MXi3NkBp M1X5cWROW09? MXnpcoR2[2W|IFexJIJtd2OtYXfl NVT3VGVMOjNyNU[0PVk>
MZ-CRC1  M3z4ZmFxd3C2b4Ppd{BCe3OjeR?= Ml7nNUDDvU1? MkLCOFghcA>? MVfEUXNQ NHrkfIJqdmS3Y3XzJIFxd3C2b4Ppdy=> NXXuR2V1OjNyNU[0PVk>
TT  NVH0emd5SXCxcITvd4l{KEG|c3H5 M1nwbVEhyrWP M3Twd|Q5KGh? MlznSG1UVw>? Mmq3bY5lfWOnczDhdI9xfG:|aYO= NHfvdFMzOzB3NkS5PS=>
HD-LM2 NUHh[HNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ToZlcz6oDLaB?= M13EdWROW09? MlzwTWM2OD15Lki0OEDPxE1? MXeyNlgzQTB7NB?=
L-428 MnHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLDSndYPzMkgJno MYfEUXNQ NEm3UZhKSzVyPUeuPVQ4KM7:TR?= M4CwNVIzQDJ7MEm0
KM-H2 M1LQSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvzO|LjiImq MXLEUXNQ MlfPTWM2OD1zLkOwPEDPxE1? NU\q[VdGOjJ6MkmwPVQ>
L-540 NYnLRmNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\PO|LjiImq NWKwWml4TE2VTx?= MmrhTWM2OD16LkKxOkDPxE1? NXT1SXFoOjJ6MkmwPVQ>
HD-LM2 NUf3SHhxTnWwY4Tpc44hSXO|YYm= M4T6Z|AvOS9yLkWvNU82KM7:TR?= M2HnfVcz6oDLaB?= MkSySG1UVw>? MkjlbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NHHuNXIzOjh{OUC5OC=>
L-428 M4jrTGZ2dmO2aX;uJGF{e2G7 NGm3W|kxNjFxMD61M|EwPSEQvF2= M1TjVFcz6oDLaB?= Ml\oSG1UVw>? NXTpcIsycW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NGPCZVEzOjh{OUC5OC=>
KM-H2 Ml;1SpVv[3Srb36gRZN{[Xl? MojXNE4yNzBwNT:xM|Uh|ryP M{TE[lcz6oDLaB?= MlfwSG1UVw>? MUjpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NUTVXotoOjJ6MkmwPVQ>
L-540 MV\GeY5kfGmxbjDBd5NigQ>? MXiwMlEwOC53L{GvOUDPxE1? M17z[Fcz6oDLaB?= M1zlemROW09? M1j1ZYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MUWyNlgzQTB7NB?=
HD-LM2 M4XqOGFxd3C2b4Ppd{BCe3OjeR?= M1iyWlEwPSEQvF2= M{LYVlcz6oDLaB?= M2PySGROW09? NWP5Zm5WcW6mdXPld{BieG:ydH;zbZM> NHzGW|AzOjh{OUC5OC=>
L-428 MnL0RZBweHSxc3nzJGF{e2G7 NVToPIVXOS93IN88US=> NUf3VnlNPzMkgJno NIPzcW5FVVOR MV;pcoR2[2W|IHHwc5B1d3Orcx?= MX6yNlgzQTB7NB?=
KM-H2 MYfBdI9xfG:|aYOgRZN{[Xl? MmDZNU82KM7:TR?= NIfqTGY4OuLCiXi= Ml62SG1UVw>? MXHpcoR2[2W|IHHwc5B1d3Orcx?= Mkj0NlI5OjlyOUS=
L-540 Mlr4RZBweHSxc3nzJGF{e2G7 NGq4R5YyNzVizszN MkXUO|LjiImq MlvjSG1UVw>? M4PQUYlv\HWlZYOgZZBweHSxc3nz NVfyNZJOOjJ6MkmwPVQ>
U251-MG MlvXSpVv[3Srb36gRZN{[Xl? M1fOUVEhyrWP MWOwMVE3KGh? MWnpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MoHzNlIxOjd4OUG=
U87-MG MlPWSpVv[3Srb36gRZN{[Xl? M{LUTlEhyrWP NWLLUWVYOC1zNjDo M2nHRolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? MX2yNlAzPzZ7MR?=
4C8 M{HZdmZ2dmO2aX;uJGF{e2G7 NHG2Z3oyKML3TR?= NE\NdpQxNTF4IHi= NHrkNnVqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MV2yNlAzPzZ7MR?=
U251-MG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[xM|ExKML3TR?= NWnQ[Yo3OjRxNEivO|IhcA>? NHrv[|VqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NUn0Tmp4OjJyMke2PVE>
U87-MG M{\CWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF76TI8yNzFyINM1US=> MXOyOE81QC95MjDo MlTMbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> M1rkU|IzODJ5Nkmx
4C8 NHrxSolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWxM|ExKML3TR?= NXvTcIw6OjRxNEivO|IhcA>? NVfWcZc6cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MVGyNlAzPzZ7MR?=
U266 NVPtU|g2SXCxcITvd4l{KEG|c3H5 NFn4V3AxNjVvMjFOwG0> Mn7HOFgwPzJiaB?= MlnCbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MX2yNVE3PDVzNx?=
Kms.11 MVrBdI9xfG:|aYOgRZN{[Xl? MViwMlUuOiEQvF2= M1nDZ|Q5Nzd{IHi= NIHx[W9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MYGyNVE3PDVzNx?=
8226 M3jSemFxd3C2b4Ppd{BCe3OjeR?= MYqwMlUuOiEQvF2= M2HpXFQ5Nzd{IHi= M{jzWIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NWn2NJpCOjFzNkS1NVc>

... 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).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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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