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 30 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 MVzGeY5kfGmxbjDBd5NigQ>? MX:1JO69VQ>? M2\nVVQ5KGh? M4DHfGROW09? M2qzdoJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> NV3HUmQyOjV7NUS5O|Q>
LoVo  NWPOSph7TnWwY4Tpc44hSXO|YYm= MVu1JO69VQ>? M3nJbVQ5KGh? MkPkSG1UVw>? NVHwT5VK[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o MlHNNlU6PTR7N{S=
HN5 M{ntTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XWbFczKGh? MYfFR|UxRTNwOEGgxtEhOS57OTFOwG0> M3KyOFI2QDFyMEGw
Cal33 MmjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrjUVdrPzJiaB?= NHXTfpNGSzVyPUOuN|chyrFiMD63OUDPxE1? M3TtTVI2QDFyMEGw
UM-22B M3vkN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr2U3V7PzJiaB?= NGXEZ4dGSzVyPUKuOlYhyrFiMD6yOEDPxE1? NFXzeGEzPThzMECxNC=>
686LN NHziXIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSwbow3PzJiaB?= MnS0SWM2OD1{LkC1JOKyKDFwM{Og{txO NYjF[W9EOjV6MUCwNVA>
UM SCC-1 NV\RW4RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fCWFczKGh? MlvDSWM2OD1zLk[3JOKyKDBwNEKg{txO M1rDPFI2QDFyMEGw
UM-22A Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi5[IE4OiCq MYHFR|UxRTFwM{KgxtEhOC5|OTFOwG0> NU\yZoVzOjV6MUCwNVA>
OSC19 MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TuRVczKGh? NUTMNoR4TUN3ME2xMlI3KMLzIECuNlAh|ryP NEPuXG8zPThzMECxNC=>
PCI-52 NVjaU|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITPNHk4OiCq NUXoWmVkTUN3ME2xMlAxKMLzIECuNFkh|ryP M4rDVlI2QDFyMEGw
PCI-15B MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1exV|czKGh? NIHiSnFGSzVyPUCuPVkhyrFiMT63OEDPxE1? NV3o[45wOjV6MUCwNVA>
UMSCC-1 NFzGc2dHfW6ldHnvckBCe3OjeR?= NUPp[XFUOC5yMEC1MVEvPiEQvF2= NGDYXnUzPCCq MnLTZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFjVV4QzPThzMECxNC=>
Cal33 M2W0SmZ2dmO2aX;uJGF{e2G7 MWOwMlAxODVvMz64JO69VQ>? NVTT[4xZOjRiaB?= NUHieYJZ[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NULifFkyOjV6MUCwNVA>
HH5 MkXTSpVv[3Srb36gRZN{[Xl? MViwMlAxODVvMz64JO69VQ>? NX[2eXJ[OjRiaB?= NUHOTHZJ[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYCyOVgyODBzMB?=
UM-22A NWrEeVFiTnWwY4Tpc44hSXO|YYm= MXmwMlAxODVvMT62JO69VQ>? MWKyOEBp NWH0SY1l[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mke1NlU5OTByMUC=
A1847 NUPKUZp[TnWwY4Tpc44hSXO|YYm= MkPDNE4xPS1zMDFOwG0> MmHSNlQhcA>? M3Xa[WROW00EoB?= MXXy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NYDTdHV5OjV4NE[wNVU>
OVCAR-5 Mn;ISpVv[3Srb36gRZN{[Xl? Mo\ZNE4xPS1zMDFOwG0> NXjZcI53OjRiaB?= NEOyPHFFVVORwrC= M3;tOpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NEPhWJgzPTZ2NkCxOS=>
OVCAR-8 M2TiZ2Z2dmO2aX;uJGF{e2G7 NGm1OosxNjB3LUGwJO69VQ>? MkXTNlQhcA>? M3;OSGROW00EoB?= MnzEdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MYiyOVY1PjBzNR?=
MOVCAR-5447 MXTGeY5kfGmxbjDBd5NigQ>? NIm4do0xNjB3LUGwJO69VQ>? M1HpXFI1KGh? MVnEUXNQyqB? NIDtblRz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NHLaVHozPTZ2NkCxOS=>
MOVCAR-5009 NHW3[41HfW6ldHnvckBCe3OjeR?= NGXGO3cxNjB3LUGwJO69VQ>? NGfwU2EzPCCq MliySG1UV8Li M1Xh[JJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MWOyOVY1PjBzNR?=
A1847 NY\KcZFlS2WubDDWbYFjcWyrdImgRZN{[Xl? M3rpfFAvODVvMUCg{txO NFPyPWk4OiCq M3u0fWROW09? MmnadoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MV2yOVY1PjBzNR?=
OVCAR-5 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmnUNE4xPS1zMDFOwG0> MY[3NkBp Mo\lSG1UVw>? MlLzdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NFj3ZlYzPTZ2NkCxOS=>
OVCAR-8  NUjDZpBwS2WubDDWbYFjcWyrdImgRZN{[Xl? MUSwMlA2NTFyIN88US=> NXTENnFGPzJiaB?= NFHuXIlFVVOR NVHuS3NUemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> M2rEWlI2PjR4MEG1
OVCAR-5  MkLvRZBweHSxc3nzJGF{e2G7 M1\3cVAvPS9zL{Wg{txO NFnqNGI1QCCq NVTMfmRlTE2VTx?= NUf1O2RWcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> NWXKbot7OjV4NE[wNVU>
OVCAR-8  NIfUdG1CeG:ydH;zbZMhSXO|YYm= MV2wMlUwOS93IN88US=> M{e3W|Q5KGh? M4rDU2ROW09? MUHpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w MV:yOVY1PjBzNR?=
AKRSL NEf3SlBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIjFVJE4OiCq NF\GWpJKSzVy78{eNVAh|ryP MnX2NlU2ODR4M{W=
PALJDL MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIW3RWw4OiCq NFzk[JdKSzVyPUKuOEDPxE1? MUCyOVUxPDZ|NR?=
MO4 MVTGeY5kfGmxbjDBd5NigQ>? NVjjOIVLOC53L{GvOUDPxE1? NHjxblA3KGh? M4TMNIlvcGmkaYTzJHAuW1SDVEOg[ZhxemW|c3nvcuKh NYnhWZRIOjVzNEm1N|U>
DU145  MkX5SpVv[3Srb36gRZN{[Xl? MonjNE0zODBibl2= M{\lc|EhcMLi NEDwflh{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NF\UTlAzPDV5N{m0Ni=>
DU145  M{L2Z2Z2dmO2aX;uJGF{e2G7 MkD3PFAxKG6P M1vRflczKGh? NUjJS2tPe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 MVKyOFU4Pzl2Mh?=
CWR22Rv1 M{G3UmZ2dmO2aX;uJGF{e2G7 M1ja[VgxOCCwTR?= NFuxV5E4OiCq Mny4d5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 NWLQSnMzOjR3N{e5OFI>
N592 M1jQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPSTWM2OD1yLki0JO69VQ>? MmH1NlQyPTh5MEG=
H82 NHHJR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfZcos3UUN3ME2xMlM4KM7:TR?= M37nRVI1OTV6N{Cx
GLC4 NHPsT2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFwN{mg{txO NHSwT3QzPDF3OEewNS=>
H526 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fvWWlEPTB;Mz6wPEDPxE1? NEH4UmMzPDF3OEewNS=>
H1173 M3W2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULKbWpiUUN3ME2yMlM6KM7:TR?= NI\ESo8zPDF3OEewNS=>
DMS114 NVrDT2ZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TnSGlEPTB;MD63N{DPxE1? MojsNlQyPTh5MEG=
NCI-N592 NGXCUZRHfW6ldHnvckBCe3OjeR?= Mlv5NE4{NzFxMzFOwG0> NVezcpZvOjRiaB?= NEjncGlqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NELsUXUzPDF3OEewNS=>
GLC4 M1[zc2Z2dmO2aX;uJGF{e2G7 M4riUVAvOy9zL{Og{txO MXuyOEBp MojnbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MYKyOFE2QDdyMR?=
NCI-H82 MoTKSpVv[3Srb36gRZN{[Xl? NX;uSIx{OC5|L{GvN{DPxE1? NI\E[WYzPCCq M1XnNIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NVXTbnFMOjRzNUi3NFE>
NCI-N592 NFThSVdCeG:ydH;zbZMhSXO|YYm= NF23em0xNjNxMT:zJO69VQ>? NEDrdXA1QCCq NXrWNYNEcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NHXRbFYzPDF3OEewNS=>
GLC4 M{DLNmFxd3C2b4Ppd{BCe3OjeR?= MXewMlMwOS9|IN88US=> MX60PEBp M1LDeolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M1HufFI1OTV6N{Cx
NCI-H82 NXjiTFBRSXCxcITvd4l{KEG|c3H5 M121TlAvOy9zL{Og{txO Ml7DOFghcA>? MXjpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NHyzPVQzPDF3OEewNS=>
CWR22Rv1  MUPBdI9xfG:|aYOgRZN{[Xl? NWTaNHo1UUN3ME2wMlQ5OiEQvF2= NFfXToozOzl2MkC5OS=>
CWR22Pc MlHwRZBweHSxc3nzJGF{e2G7 NEL1W41KSzVyPUCuOFM5KM7:TR?= MoTxNlM6PDJyOUW=
PC-3 M{eyeGFxd3C2b4Ppd{BCe3OjeR?= NHL0VGdKSzVyPUGuO|U2KM7:TR?= Ml3SNlM6PDJyOUW=
DU145 Mln6RZBweHSxc3nzJGF{e2G7 MoHsTWM2OD1|LkWxO{DPxE1? NYCwUIVsOjN7NEKwPVU>
RC165N M2PEV2Fxd3C2b4Ppd{BCe3OjeR?= M4exZ2lEPTB;Mj6wPFMh|ryP MV6yN|k1OjB7NR?=
ARPE19 NH:xRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnxSG1UVw>? NHXQSHRKSzVyPUK0MlM5KM7:TR?= NX;xSWpXOjN3M{G5NlE>
HEK293 NEfL[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvESG1UVw>? NHzpVYVKSzVyPUiuOlch|ryP NEjSVo4zOzV|MUmyNS=>
KCNR M3jacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfyOWVKTE2VTx?= MY\JR|UxRTBwNE[g{txO NYqzToEzOjN3M{G5NlE>
SY5Y MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTEUXNQ NGDPcZRKSzVyPUCuN|Yh|ryP MXeyN|U{OTl{MR?=
BE2 M1TURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\re2dFVVOR NH7ISYdKSzVyPUCuO|Eh|ryP NEnMOHUzOzV|MUmyNS=>
AS MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PBe2ROW09? NWq0cpV1UUN3ME2xMlU{KM7:TR?= M3\mPVI{PTNzOUKx
NGP MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX5bFlwTE2VTx?= MojFTWM2OD1yLkW2JO69VQ>? NF\tUGszOzV|MUmyNS=>
IMR32 MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LnN2ROW09? NVfOOGJ4UUN3ME2wMlY3KM7:TR?= M3nxR|I{PTNzOUKx
LAN5 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXNTVZXTE2VTx?= NVLNTotFUUN3ME2xMlA1KM7:TR?= MVSyN|U{OTl{MR?=
RH18 NEXvOHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPPSG1UVw>? M17WWmlEPTB;MT60NkDPxE1? M3HuRVI{PTNzOUKx
RH30 NEDrO4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPObYJ5TE2VTx?= NInuRVNKSzVyPUGuNlUh|ryP M2[2WlI{PTNzOUKx
RH17 NXTsbFJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vue2ROW09? MXjJR|UxRTJwNUGg{txO MnGyNlM2OzF7MkG=
RH28 MmDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Lt[mROW09? MV\JR|UxRTRwMkig{txO M3XFVVI{PTNzOUKx
RH36 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUeyOFlrTE2VTx?= MWrJR|UxRTVwM{eg{txO MWmyN|U{OTl{MR?=
RH41 Mm\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPJclRXTE2VTx?= MUDJR|UxRTBwNEig{txO MUGyN|U{OTl{MR?=
RD NGHUXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13QPWROW09? MoHqTWM2OD12LkOyJO69VQ>? Mk\NNlM2OzF7MkG=
TC32 NVGye457T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrEPIxFVVOR MkfxTWM2OD1|Lki1JO69VQ>? Mn7jNlM2OzF7MkG=
TC71 M33iSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrmSG1UVw>? NXXSRXRlUUN3ME20MlM{KM7:TR?= NHvhfHMzOzV|MUmyNS=>
KCNR MknzRZBweHSxc3nzJGF{e2G7 NYjiWnZSOC53L{GuNE8zNjVizszN Mn\NNlQhcA>? NGr0PYlFVVOR NVO0[GZLcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NXrVTXc2OjN3M{G5NlE>
SY5Y MUDBdI9xfG:|aYOgRZN{[Xl? MknLNE42NzFwMD:yMlUh|ryP NETuVoEzPCCq MWPEUXNQ M3nsb4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NF64UVQzOzV|MUmyNS=>
Rh18 M{HtdGFxd3C2b4Ppd{BCe3OjeR?= MojMNE42NzFwMD:yMlUh|ryP NFvr[YYzPCCq M2fufWROW09? M3XXdolv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NWPkWXB5OjN3M{G5NlE>
TC32 NX\NVJM{SXCxcITvd4l{KEG|c3H5 MnfDNE42NzFwMD:yMlUh|ryP Mnv1NlQhcA>? M{j2dGROW09? NFq4[VVqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MkXzNlM2OzF7MkG=
KCNR NYPMR|VDTnWwY4Tpc44hSXO|YYm= NH7oXHIxNjVxMT6wM|IvPS93IN88US=> Ml7vNlQhcA>? MkX6SG1UVw>? M1TLN4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u Mn\ONlM2OzF7MkG=
SY5Y MnzNSpVv[3Srb36gRZN{[Xl? NIi4PW4xNjVxMT6wM|IvPS93IN88US=> MYiyOEBp NEL0U49FVVOR Ml\WbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NFHHZ28zOzV|MUmyNS=>
Rh18 NXnZNG5[TnWwY4Tpc44hSXO|YYm= NETvb2sxNjVxMT6wM|IvPS93IN88US=> NIjKbVUzPCCq NIS3PZRFVVOR NYXaZoNLcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> M170cFI{PTNzOUKx
TC32 M4nQNGZ2dmO2aX;uJGF{e2G7 NYDXfGNbOC53L{GuNE8zNjVxNTFOwG0> NW\jWXo5OjRiaB?= MYfEUXNQ MkjvbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MkXzNlM2OzF7MkG=
TPC-1 M2LlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSxJOK2VQ>? MYKwMVQh\A>? MkD5SG1UVw>? Ml3KbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? NGD6NlgzOzB3NkS5PS=>
MZ-CRC1  M2LRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm1NUDDvU1? MoPLNE02KGR? NUHuPIlvTE2VTx?= M130PYlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MoL4NlMxPTZ2OUm=
TT  NEflTFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrufnpxOSEEtV2= M{XZNlAuPCCm MV\EUXNQ NI\PfZNqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MnO5NlMxPTZ2OUm=
TPC-1 NWnmNGpzTnWwY4Tpc44hSXO|YYm= NV3ndYhiOSEEtV2= M{LVelczKGh? NWfXZok2TE2VTx?= M4P3U4lv\HWlZYOgS|Eh[myxY3vh[4U> M{[2TVI{ODV4NEm5
MZ-CRC1  NI\Zbo5HfW6ldHnvckBCe3OjeR?= Ml7jNUDDvU1? M17tUFczKGh? NWX5U29MTE2VTx?= MVfpcoR2[2W|IFexJIJtd2OtYXfl NWXSb5lwOjNyNU[0PVk>
TT  M1LjO2Z2dmO2aX;uJGF{e2G7 NUfCR5ZPOSEEtV2= Ml;UO|IhcA>? MnPkSG1UVw>? M1PCfIlv\HWlZYOgS|Eh[myxY3vh[4U> MnWzNlMxPTZ2OUm=
MZ-CRC1  MYHBdI9xfG:|aYOgRZN{[Xl? Ml3mNUDDvU1? MWS0PEBp NYDU[FJwTE2VTx?= MnvabY5lfWOnczDhdI9xfG:|aYO= Mni5NlMxPTZ2OUm=
TT  NEWyeFhCeG:ydH;zbZMhSXO|YYm= MUKxJOK2VQ>? Ml;2OFghcA>? M1nTbGROW09? NHnMfXZqdmS3Y3XzJIFxd3C2b4Ppdy=> NX7Mfnh3OjNyNU[0PVk>
HD-LM2 MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVWwZmJuPzMkgJno Mn[4SG1UVw>? M{\acmlEPTB;Nz64OFQh|ryP MX2yNlgzQTB7NB?=
L-428 M3mzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;4OVcz6oDLaB?= NUHoTlVsTE2VTx?= NV7SUJFrUUN3ME23Mlk1PyEQvF2= MkWyNlI5OjlyOUS=
KM-H2 NX;Yeog6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLQTllEPzMkgJno MUHEUXNQ MV7JR|UxRTFwM{C4JO69VQ>? M{W1PVIzQDJ7MEm0
L-540 NFzx[pNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz3cZZ6PzMkgJno NWPmV2RXTE2VTx?= NYD2XotRUUN3ME24MlIyPiEQvF2= MU[yNlgzQTB7NB?=
HD-LM2 NEDQ[mRHfW6ldHnvckBCe3OjeR?= NYKzTI03OC5zL{CuOU8yNzVizszN NIDydpI4OuLCiXi= NVHzSmRxTE2VTx?= M2nUR4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MlfuNlI5OjlyOUS=
L-428 NV\TT3VHTnWwY4Tpc44hSXO|YYm= MXOwMlEwOC53L{GvOUDPxE1? MlHyO|LjiImq MVHEUXNQ NUfSfZF1cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NGW3fmozOjh{OUC5OC=>
KM-H2 MlTqSpVv[3Srb36gRZN{[Xl? MYCwMlEwOC53L{GvOUDPxE1? M4TINlcz6oDLaB?= MYjEUXNQ NUjWfFdXcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? M{LaZlIzQDJ7MEm0
L-540 M{TwTmZ2dmO2aX;uJGF{e2G7 M4fRblAvOS9yLkWvNU82KM7:TR?= NXPXXWJVPzMkgJno MYPEUXNQ MXXpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NGXGb2kzOjh{OUC5OC=>
HD-LM2 NHPuWlNCeG:ydH;zbZMhSXO|YYm= NVjjVHY4OS93IN88US=> NI\YeHc4OuLCiXi= NILVXmFFVVOR NVq3[lk5cW6mdXPld{BieG:ydH;zbZM> MWqyNlgzQTB7NB?=
L-428 NXLiO2V3SXCxcITvd4l{KEG|c3H5 M3jETFEwPSEQvF2= M{PtZlcz6oDLaB?= NX3T[XRQTE2VTx?= Mmi4bY5lfWOnczDhdI9xfG:|aYO= MYeyNlgzQTB7NB?=
KM-H2 NIH3WG5CeG:ydH;zbZMhSXO|YYm= M3iwZlEwPSEQvF2= MkD3O|LjiImq M1fPV2ROW09? NUjXdWlQcW6mdXPld{BieG:ydH;zbZM> MkLzNlI5OjlyOUS=
L-540 MoLGRZBweHSxc3nzJGF{e2G7 NFTC[3AyNzVizszN MXu3NwKBkWh? NXLiWHUxTE2VTx?= M{nK[olv\HWlZYOgZZBweHSxc3nz NEHYRZUzOjh{OUC5OC=>
U251-MG NF\KemxHfW6ldHnvckBCe3OjeR?= MXixJOK2VQ>? Ml3nNE0yPiCq MmX5bY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NITDOHYzOjB{N{[5NS=>
U87-MG NVXjTJFHTnWwY4Tpc44hSXO|YYm= NXznV|FtOSEEtV2= MmS5NE0yPiCq MmLObY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NUmzVHVUOjJyMke2PVE>
4C8 NGXZNW1HfW6ldHnvckBCe3OjeR?= MXOxJOK2VQ>? NELqOJYxNTF4IHi= NFHxVnBqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MnT2NlIxOjd4OUG=
U251-MG NGLlVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP3NlFFOS9zMDFCuW0> M2LmXFI1NzR6L{eyJIg> M4fQd4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO MXOyNlAzPzZ7MR?=
U87-MG MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPwV5pmOS9zMDFCuW0> MWCyOE81QC95MjDo NYT6WVNScW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NXj1N3FjOjJyMke2PVE>
4C8 NIG1W3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULqTpFtOS9zMDFCuW0> M2\UTFI1NzR6L{eyJIg> NH\qboxqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NHTBbVAzOjB{N{[5NS=>
U266 NHHFfnhCeG:ydH;zbZMhSXO|YYm= NFLtNWMxNjVvMjFOwG0> NFXNSm41QC95MjDo MnHWbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M2TFc|IyOTZ2NUG3
Kms.11 NHez[ldCeG:ydH;zbZMhSXO|YYm= MX2wMlUuOiEQvF2= NWfTe3p4PDhxN{KgbC=> NFvjd29qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NXTPWnZVOjFzNkS1NVc>
8226 NHP1N|NCeG:ydH;zbZMhSXO|YYm= NHHmW5cxNjVvMjFOwG0> NWntNnhkPDhxN{KgbC=> M3HwXIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NHLrTG0zOTF4NEWxOy=>

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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

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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