AZD1480

For research use only.

Catalog No.S2162

67 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 67 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 M{HaZ2Z2dmO2aX;uJGF{e2G7 NXqzc2tTPSEQvF2= MlqxOFghcA>? M{OydWROW09? NWfkenI1[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NHr3PXEzPTl3NEm3OC=>
LoVo  NF;sN|hHfW6ldHnvckBCe3OjeR?= MXq1JO69VQ>? NXPZNphMPDhiaB?= M1T1W2ROW09? NV3RS2FO[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NUDHXHBNOjV7NUS5O|Q>
HN5 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjjWoZOPzJiaB?= NILNNoJGSzVyPUOuPFEhyrFiMT65PUDPxE1? MlLWNlU5OTByMUC=
Cal33 MnSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO3NkBp M2\sWGVEPTB;Mz6zO{DDuSByLke1JO69VQ>? NVjtWpZ3OjV6MUCwNVA>
UM-22B NUnHbYF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf1XJE4OiCq MVTFR|UxRTJwNk[gxtEhOC5{NDFOwG0> M2X4b|I2QDFyMEGw
686LN NFHLc4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXsO|IhcA>? MoPXSWM2OD1{LkC1JOKyKDFwM{Og{txO NUfr[lhyOjV6MUCwNVA>
UM SCC-1 NYm4NpE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m3fFczKGh? MXHFR|UxRTFwNkegxtEhOC52MjFOwG0> M2jmO|I2QDFyMEGw
UM-22A NGHw[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDGeZg2PzJiaB?= Mn;LSWM2OD1zLkOyJOKyKDBwM{mg{txO MkHqNlU5OTByMUC=
OSC19 NY\yNoZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq0O|IhcA>? NFWweZVGSzVyPUGuNlYhyrFiMD6yNEDPxE1? NEP3XlYzPThzMECxNC=>
PCI-52 NFSybFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXQSYo4OiCq M3Lzd2VEPTB;MT6wNEDDuSByLkC5JO69VQ>? MV[yOVgyODBzMB?=
PCI-15B M2LkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHJepc4OiCq MnzKSWM2OD1yLkm5JOKyKDFwN{Sg{txO NHq5[JUzPThzMECxNC=>
UMSCC-1 NFTXe|lHfW6ldHnvckBCe3OjeR?= MlzFNE4xODB3LUGuOkDPxE1? MlHaNlQhcA>? NInkZnVi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3POZVI2QDFyMEGw
Cal33 MoDESpVv[3Srb36gRZN{[Xl? MVuwMlAxODVvMz64JO69VQ>? MmXuNlQhcA>? MnL2ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWqyOVgyODBzMB?=
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UM-22A MlvZSpVv[3Srb36gRZN{[Xl? MlfvNE4xODB3LUGuOkDPxE1? M335eFI1KGh? MoLaZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYCyOVgyODBzMB?=
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OVCAR-5 MnrMSpVv[3Srb36gRZN{[Xl? NW[0NIh1OC5yNT2xNEDPxE1? MmSxNlQhcA>? MV;EUXNQyqB? MUny[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MXSyOVY1PjBzNR?=
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MOVCAR-5447 M1PMR2Z2dmO2aX;uJGF{e2G7 NUG0RZR4OC5yNT2xNEDPxE1? NXXIUIpGOjRiaB?= NXTkb4loTE2VT9Mg MlW0doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MXmyOVY1PjBzNR?=
MOVCAR-5009 MlO1SpVv[3Srb36gRZN{[Xl? MoXkNE4xPS1zMDFOwG0> MojONlQhcA>? NWfDcVFqTE2VT9Mg NHnKZlJz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NWj3N3FYOjV4NE[wNVU>
A1847 M{LpOGNmdGxiVnnhZoltcXS7IFHzd4F6 MW[wMlA2NTFyIN88US=> M1\RNFczKGh? MWrEUXNQ MX\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MmLjNlU3PDZyMUW=
OVCAR-5 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVzwfmNYOC5yNT2xNEDPxE1? Mnj4O|IhcA>? MV;EUXNQ NXHvZZI4emWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NWPRRmNyOjV4NE[wNVU>
OVCAR-8  M{T1TWNmdGxiVnnhZoltcXS7IFHzd4F6 MWKwMlA2NTFyIN88US=> MW[3NkBp NULNXWFRTE2VTx?= NFXzUHRz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NULYdWllOjV4NE[wNVU>
OVCAR-5  NF;4NIJCeG:ydH;zbZMhSXO|YYm= M1K3b|AvPS9zL{Wg{txO MX20PEBp M{nDb2ROW09? NIS0[mZqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u Mn33NlU3PDZyMUW=
OVCAR-8  NGC1dVZCeG:ydH;zbZMhSXO|YYm= M3H5SlAvPS9zL{Wg{txO M{XUfVQ5KGh? MVrEUXNQ Mo[5bY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= MX:yOVY1PjBzNR?=
AKRSL Mm\UR4VtdCCYaXHibYxqfHliQYPzZZk> Mo\FO|IhcA>? MUTJR|Ux97zgMUCg{txO MnviNlU2ODR4M{W=
PALJDL NELFfZpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1P4[VczKGh? M4H4TGlEPTB;Mj60JO69VQ>? M4mwe|I2PTB2NkO1
MO4 NIrBeHlHfW6ldHnvckBCe3OjeR?= NUjscYlqOC53L{GvOUDPxE1? NHnE[po3KGh? NGDzfVhqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NYHzOVJNOjVzNEm1N|U>
DU145  NGLINYRHfW6ldHnvckBCe3OjeR?= MWCwMVIxOCCwTR?= M4TXNFEhcMLi NYXJS|VLe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> NILkZnQzPDV5N{m0Ni=>
DU145  NHLrOlFHfW6ldHnvckBCe3OjeR?= NYTXSXRFQDByIH7N M4nPXFczKGh? M3ezR5N2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NYfy[mI{OjR3N{e5OFI>
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GLC4 MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLSTWM2OD1zLke5JO69VQ>? NYDVOlVrOjRzNUi3NFE>
H526 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PKXmlEPTB;Mz6wPEDPxE1? MV[yOFE2QDdyMR?=
H1173 M1:xXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDPUoJvUUN3ME2yMlM6KM7:TR?= M1PaOlI1OTV6N{Cx
DMS114 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwN{Og{txO M1fC[FI1OTV6N{Cx
NCI-N592 NXO2NoRDTnWwY4Tpc44hSXO|YYm= M3z6SFAvOy9zL{Og{txO NGTHPVMzPCCq NGHCSG1qdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NX\m[ZFWOjRzNUi3NFE>
GLC4 NH[wdXlHfW6ldHnvckBCe3OjeR?= NFT3bmsxNjNxMT:zJO69VQ>? NYXTV5lTOjRiaB?= MVnpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NXHpNnBwOjRzNUi3NFE>
NCI-H82 NYW1[JNrTnWwY4Tpc44hSXO|YYm= NX\aOFZCOC5|L{GvN{DPxE1? NGjQbXkzPCCq M1;DT4lv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MVmyOFE2QDdyMR?=
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GLC4 Mlz3RZBweHSxc3nzJGF{e2G7 NVXIPFdTOC5|L{GvN{DPxE1? M1T6V|Q5KGh? M2K2VYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NHLTbHEzPDF3OEewNS=>
NCI-H82 NV3PbG9vSXCxcITvd4l{KEG|c3H5 M2P3[lAvOy9zL{Og{txO M1;MPFQ5KGh? NIfESWJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NELi[pMzPDF3OEewNS=>
CWR22Rv1  MVnBdI9xfG:|aYOgRZN{[Xl? NFXVfWdKSzVyPUCuOFgzKM7:TR?= MmXENlM6PDJyOUW=
CWR22Pc NWj5SmxISXCxcITvd4l{KEG|c3H5 MlPlTWM2OD1yLkSzPEDPxE1? NV\nUZhqOjN7NEKwPVU>
PC-3 NH;oO|ZCeG:ydH;zbZMhSXO|YYm= MXfJR|UxRTFwN{W1JO69VQ>? MlLzNlM6PDJyOUW=
DU145 Mof3RZBweHSxc3nzJGF{e2G7 NHXnVW1KSzVyPUOuOVE4KM7:TR?= NEe4boczOzl2MkC5OS=>
RC165N MmT6RZBweHSxc3nzJGF{e2G7 NFf0bmJKSzVyPUKuNFg{KM7:TR?= M2G1UFI{QTR{MEm1
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HEK293 MonUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfvSG1UVw>? MU\JR|UxRThwNkeg{txO MWmyN|U{OTl{MR?=
KCNR M2TiNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLwSG1UVw>? NG\2cWpKSzVyPUCuOFYh|ryP MlrtNlM2OzF7MkG=
SY5Y MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnEUXNQ MXXJR|UxRTBwM{[g{txO NHvtWHczOzV|MUmyNS=>
BE2 NIC5fZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2POdmROW09? NVTX[Go6UUN3ME2wMlcyKM7:TR?= MXqyN|U{OTl{MR?=
AS NIXjWo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjS[lNtTE2VTx?= M2PtTGlEPTB;MT61N{DPxE1? MnTqNlM2OzF7MkG=
NGP NF\NTmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PUUWROW09? M1[3dWlEPTB;MD61OkDPxE1? M4\oN|I{PTNzOUKx
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RH36 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\se45FVVOR NX3UU|FnUUN3ME21MlM4KM7:TR?= NYHnV|VQOjN3M{G5NlE>
RH41 M1foN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXjcI0xTE2VTx?= NHXNS2JKSzVyPUCuOFgh|ryP NYTTfm1yOjN3M{G5NlE>
RD MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILlOnpFVVOR MlS5TWM2OD12LkOyJO69VQ>? NYSzXYpLOjN3M{G5NlE>
TC32 M1r5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrEUXNQ MVXJR|UxRTNwOEWg{txO NUTMbYNjOjN3M{G5NlE>
TC71 MonUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrFVmxFVVOR MWPJR|UxRTRwM{Og{txO MmjJNlM2OzF7MkG=
KCNR NVLr[oJnSXCxcITvd4l{KEG|c3H5 M{fwdlAvPS9zLkCvNk42KM7:TR?= NUHLVHd1OjRiaB?= NULMfZlTTE2VTx?= Mn\ZbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MVmyN|U{OTl{MR?=
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TC32 MXvGeY5kfGmxbjDBd5NigQ>? M3m5dVAvPS9zLkCvNk42NzVizszN MlrQNlQhcA>? M3HlR2ROW09? MkTzbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NYnITY1COjN3M{G5NlE>
TPC-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:wUHhtOSEEtV2= NYmy[oliOC12IHS= MUPEUXNQ Mnj1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? MVSyN|A2PjR7OR?=
MZ-CRC1  NXfhW4lzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexJOK2VQ>? MmPaNE02KGR? M{fDemROW09? M3;4OYlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MYqyN|A2PjR7OR?=
TT  M{WxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDkNUDDvU1? M325eVAuPCCm NITiTItFVVOR NEfETJlqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 M1:4e|I{ODV4NEm5
TPC-1 NFTiZo9HfW6ldHnvckBCe3OjeR?= MXSxJOK2VQ>? MWC3NkBp MUTEUXNQ NGPhTXhqdmS3Y3XzJGcyKGKub3PrZYdm M3[2e|I{ODV4NEm5
MZ-CRC1  NVTxUmZCTnWwY4Tpc44hSXO|YYm= MW[xJOK2VQ>? NEPaenU4OiCq M4ixZWROW09? MUjpcoR2[2W|IFexJIJtd2OtYXfl NGrx[HIzOzB3NkS5PS=>
TT  NXTpfZNvTnWwY4Tpc44hSXO|YYm= MXexJOK2VQ>? NFKwfIc4OiCq NI\UfoRFVVOR M2nhWolv\HWlZYOgS|Eh[myxY3vh[4U> M4ns[VI{ODV4NEm5
MZ-CRC1  NHrEc4lCeG:ydH;zbZMhSXO|YYm= M2PocVEhyrWP NXv2VpBbPDhiaB?= MVjEUXNQ M2HN[olv\HWlZYOgZZBweHSxc3nz M1HlNlI{ODV4NEm5
TT  NF3qOnBCeG:ydH;zbZMhSXO|YYm= MYqxJOK2VQ>? NYG2XmJYPDhiaB?= NYr0dZdYTE2VTx?= NEfE[XBqdmS3Y3XzJIFxd3C2b4Ppdy=> MXOyN|A2PjR7OR?=
HD-LM2 M1HXcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj3OlVIPzMkgJno MmTJSG1UVw>? MlT1TWM2OD15Lki0OEDPxE1? NIHiRm4zOjh{OUC5OC=>
L-428 NIXpW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH64VXo4OuLCiXi= NXTN[JZHTE2VTx?= M4rWN2lEPTB;Nz65OFch|ryP MnrPNlI5OjlyOUS=
KM-H2 NX;KRWVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj1bGQ4OuLCiXi= NYHwWYFsTE2VTx?= Ml3tTWM2OD1zLkOwPEDPxE1? MWmyNlgzQTB7NB?=
L-540 Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TFV|cz6oDLaB?= MkPWSG1UVw>? NUOzWGNwUUN3ME24MlIyPiEQvF2= M{XTbVIzQDJ7MEm0
HD-LM2 NWP0[Gd5TnWwY4Tpc44hSXO|YYm= MlrCNE4yNzBwNT:xM|Uh|ryP NHzuRXA4OuLCiXi= MX;EUXNQ M1HXUIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MlLkNlI5OjlyOUS=
L-428 NVziWoQzTnWwY4Tpc44hSXO|YYm= NUjPfpg6OC5zL{CuOU8yNzVizszN NHjmPVM4OuLCiXi= Ml2ySG1UVw>? M3G3UIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v Ml[4NlI5OjlyOUS=
KM-H2 MWnGeY5kfGmxbjDBd5NigQ>? MXewMlEwOC53L{GvOUDPxE1? Mn\EO|LjiImq NWXST2RWTE2VTx?= NXGyTGw2cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MViyNlgzQTB7NB?=
L-540 NXHjRVNqTnWwY4Tpc44hSXO|YYm= M4XCflAvOS9yLkWvNU82KM7:TR?= NWDxSZEyPzMkgJno MnrWSG1UVw>? M3XLTIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MXGyNlgzQTB7NB?=
HD-LM2 MXrBdI9xfG:|aYOgRZN{[Xl? M4L4SlEwPSEQvF2= NETX[nA4OuLCiXi= M2i2O2ROW09? MlO5bY5lfWOnczDhdI9xfG:|aYO= NIDSclkzOjh{OUC5OC=>
L-428 MmnTRZBweHSxc3nzJGF{e2G7 NY\XSmJuOS93IN88US=> Mo\DO|LjiImq NHPLXY9FVVOR MkPxbY5lfWOnczDhdI9xfG:|aYO= MmKwNlI5OjlyOUS=
KM-H2 NWDUbINpSXCxcITvd4l{KEG|c3H5 NIKxeoUyNzVizszN NXPUSGplPzMkgJno NHPJNmtFVVOR NVPTSINLcW6mdXPld{BieG:ydH;zbZM> MWCyNlgzQTB7NB?=
L-540 NYX5UZBGSXCxcITvd4l{KEG|c3H5 NX3xWYY4OS93IN88US=> MYG3NwKBkWh? M1PQV2ROW09? NF30NpFqdmS3Y3XzJIFxd3C2b4Ppdy=> M4G4fFIzQDJ7MEm0
U251-MG NXTofHlvTnWwY4Tpc44hSXO|YYm= NH36OYcyKML3TR?= Ml\sNE0yPiCq NV:xd5A{cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NVTQNWdtOjJyMke2PVE>
U87-MG MUfGeY5kfGmxbjDBd5NigQ>? MWmxJOK2VQ>? NWfLWZBYOC1zNjDo MUHpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MVqyNlAzPzZ7MR?=
4C8 M3jme2Z2dmO2aX;uJGF{e2G7 MV2xJOK2VQ>? MmjnNE0yPiCq NXj6ZXg1cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MVSyNlAzPzZ7MR?=
U251-MG NHT3VWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjEXmdVOS9zMDFCuW0> NETEcnczPC92OD:3NkBp MYLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NV;qUIFpOjJyMke2PVE>
U87-MG MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF21d5UyNzFyINM1US=> NXLHdWFVOjRxNEivO|IhcA>? M{DudIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO M{PBXFIzODJ5Nkmx
4C8 NI\aO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m0bVEwOTBiwsXN NHfUdFkzPC92OD:3NkBp M13LT4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NHTWdVgzOjB{N{[5NS=>
U266 MnHaRZBweHSxc3nzJGF{e2G7 NUDLclZqOC53LUKg{txO M1rNNFQ5Nzd{IHi= M1zrXIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NI\PbHozOTF4NEWxOy=>
Kms.11 MkLkRZBweHSxc3nzJGF{e2G7 Mly3NE42NTJizszN M2\lfFQ5Nzd{IHi= NIjhSIFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NV7wdo1lOjFzNkS1NVc>
8226 NFTKdmNCeG:ydH;zbZMhSXO|YYm= NGfLSmUxNjVvMjFOwG0> M2Dk[FQ5Nzd{IHi= MYHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 Mle4NlEyPjR3MUe=

... 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
    Concentration
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    Molecular Weight

*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