AZD1480

For research use only.

Catalog No.S2162

60 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 60 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 Mo\HSpVv[3Srb36gRZN{[Xl? NVP2PYlbPSEQvF2= NG\HSGs1QCCq NVfTPVNNTE2VTx?= NEPEOIVjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> Mmj5NlU6PTR7N{S=
LoVo  MkTjSpVv[3Srb36gRZN{[Xl? MlzqOUDPxE1? M3jwN|Q5KGh? MWPEUXNQ M4nZN4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MX:yOVk2PDl5NB?=
HN5 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T2WVczKGh? MmP3SWM2OD1|LkixJOKyKDFwOUmg{txO NXnuSG4zOjV6MUCwNVA>
Cal33 NWDTWWNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vIOVczKGh? M2DRUWVEPTB;Mz6zO{DDuSByLke1JO69VQ>? MX[yOVgyODBzMB?=
UM-22B MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\PUFRXPzJiaB?= NXTmSpU{TUN3ME2yMlY3KMLzIECuNlQh|ryP MnTlNlU5OTByMUC=
686LN M4P3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXsO|IhcA>? MWLFR|UxRTJwMEWgxtEhOS5|MzFOwG0> NFHteHkzPThzMECxNC=>
UM SCC-1 NF\yUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjLem44OiCq NF\hbYJGSzVyPUGuOlchyrFiMD60NkDPxE1? NEOwXFAzPThzMECxNC=>
UM-22A MorHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVq3NkBp M1fP[2VEPTB;MT6zNkDDuSByLkO5JO69VQ>? Mle1NlU5OTByMUC=
OSC19 NHe5O3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n6SlczKGh? NIHFRm5GSzVyPUGuNlYhyrFiMD6yNEDPxE1? NIq5eoUzPThzMECxNC=>
PCI-52 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zaXVczKGh? NHzmSnJGSzVyPUGuNFAhyrFiMD6wPUDPxE1? M2H5XlI2QDFyMEGw
PCI-15B NWTqb3dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnRSoo4OiCq MW\FR|UxRTBwOUmgxtEhOS55NDFOwG0> NW\VRVdDOjV6MUCwNVA>
UMSCC-1 M{jv[mZ2dmO2aX;uJGF{e2G7 NUD1flh{OC5yMEC1MVEvPiEQvF2= MkTVNlQhcA>? MUPhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MXyyOVgyODBzMB?=
Cal33 MknCSpVv[3Srb36gRZN{[Xl? MWGwMlAxODVvMz64JO69VQ>? MmK4NlQhcA>? M2XvT4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1HBWFI2QDFyMEGw
HH5 NXeyeWZzTnWwY4Tpc44hSXO|YYm= MonvNE4xODB3LUOuPEDPxE1? NWnzS4V2OjRiaB?= NEe5TnVi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmfHNlU5OTByMUC=
UM-22A Mn3RSpVv[3Srb36gRZN{[Xl? M3LsRlAvODByNT2xMlYh|ryP MYqyOEBp MXzhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Ml\2NlU5OTByMUC=
A1847 M3viNWZ2dmO2aX;uJGF{e2G7 MWqwMlA2NTFyIN88US=> Mk\qNlQhcA>? MX;EUXNQyqB? NFXoVWRz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NIj5bm8zPTZ2NkCxOS=>
OVCAR-5 NE\KbHhHfW6ldHnvckBCe3OjeR?= M2LLXlAvODVvMUCg{txO M2Hm[FI1KGh? NHvR[WJFVVORwrC= MV3y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NHzxOYEzPTZ2NkCxOS=>
OVCAR-8 NHfHNZVHfW6ldHnvckBCe3OjeR?= M1TF[|AvODVvMUCg{txO NIXROXUzPCCq M{G4SWROW00EoB?= M4fIZZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MUOyOVY1PjBzNR?=
MOVCAR-5447 MXXGeY5kfGmxbjDBd5NigQ>? MVWwMlA2NTFyIN88US=> NHzne4kzPCCq M{GwN2ROW00EoB?= NV76OpZKemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M{DybVI2PjR4MEG1
MOVCAR-5009 MWLGeY5kfGmxbjDBd5NigQ>? NUHwXIFNOC5yNT2xNEDPxE1? MlnqNlQhcA>? M2n3cWROW00EoB?= NGn4NWhz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MV6yOVY1PjBzNR?=
A1847 M1e3OWNmdGxiVnnhZoltcXS7IFHzd4F6 M4THbFAvODVvMUCg{txO MoPaO|IhcA>? M1\4[GROW09? M{S2b5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MmnlNlU3PDZyMUW=
OVCAR-5 MoPjR4VtdCCYaXHibYxqfHliQYPzZZk> M{jw[VAvODVvMUCg{txO NUi1SI1lPzJiaB?= MmewSG1UVw>? MU\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= NHzvc2IzPTZ2NkCxOS=>
OVCAR-8  NF3Fc4FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnvnNE4xPS1zMDFOwG0> NELjOWc4OiCq M{TtTWROW09? M17iV5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MnfFNlU3PDZyMUW=
OVCAR-5  MYHBdI9xfG:|aYOgRZN{[Xl? NET0dHoxNjVxMT:1JO69VQ>? NEG0Spc1QCCq MUDEUXNQ NHLFWnNqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u M4fkSlI2PjR4MEG1
OVCAR-8  NUDrbYRvSXCxcITvd4l{KEG|c3H5 MoDENE42NzFxNTFOwG0> NXLCXI1XPDhiaB?= NEPiXpJFVVOR M2X5[4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MUGyOVY1PjBzNR?=
AKRSL MlnuR4VtdCCYaXHibYxqfHliQYPzZZk> M2r5dVczKGh? Mn;CTWM2OO,:nkGwJO69VQ>? MUmyOVUxPDZ|NR?=
PALJDL NXTRe5FIS2WubDDWbYFjcWyrdImgRZN{[Xl? M17RdlczKGh? NUXwSGtXUUN3ME2yMlQh|ryP MVGyOVUxPDZ|NR?=
MO4 Mn\2SpVv[3Srb36gRZN{[Xl? MXGwMlUwOS93IN88US=> M2TsVlYhcA>? NHfFV5dqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? M37LUVI2OTR7NUO1
DU145  M1jkVWZ2dmO2aX;uJGF{e2G7 NYLmTVJtOC1{MECgcm0> MlzBNUBpyqB? NWP0[Wh3e3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> NX;YXWtLOjR3N{e5OFI>
DU145  Mo\USpVv[3Srb36gRZN{[Xl? MXW4NFAhdk1? NFX6c2s4OiCq NHTnT2F{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= MXGyOFU4Pzl2Mh?=
CWR22Rv1 MlW4SpVv[3Srb36gRZN{[Xl? MV24NFAhdk1? NIXSVVk4OiCq MYPzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? MmPrNlQ2Pzd7NEK=
N592 NWjUW3FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwOESg{txO MkK2NlQyPTh5MEG=
H82 NH7KTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHJTWM2OD1zLkO3JO69VQ>? NWPRd483OjRzNUi3NFE>
GLC4 NUPhd|JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq0[FA2UUN3ME2xMlc6KM7:TR?= NWjvVm9{OjRzNUi3NFE>
H526 MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TYSWlEPTB;Mz6wPEDPxE1? NV\0Vo57OjRzNUi3NFE>
H1173 NIXqbpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzMW5lMUUN3ME2yMlM6KM7:TR?= MV2yOFE2QDdyMR?=
DMS114 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljGTWM2OD1yLkezJO69VQ>? NFftTJYzPDF3OEewNS=>
NCI-N592 MU\GeY5kfGmxbjDBd5NigQ>? M3zWWVAvOy9zL{Og{txO MVmyOEBp NIrJOZBqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? Mki0NlQyPTh5MEG=
GLC4 NFH4fo1HfW6ldHnvckBCe3OjeR?= NV3YNo9[OC5|L{GvN{DPxE1? MU[yOEBp NHTYZ|RqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MmLKNlQyPTh5MEG=
NCI-H82 NIPYOY1HfW6ldHnvckBCe3OjeR?= MYSwMlMwOS9|IN88US=> NVrrOGk2OjRiaB?= NFvmRmtqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NWrje|lsOjRzNUi3NFE>
NCI-N592 MVfBdI9xfG:|aYOgRZN{[Xl? NVLKNoFWOC5|L{GvN{DPxE1? M1\1W|Q5KGh? M1nTNolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NYixWIk1OjRzNUi3NFE>
GLC4 MXfBdI9xfG:|aYOgRZN{[Xl? MlfzNE4{NzFxMzFOwG0> NVPPN2k{PDhiaB?= M2P4Xolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MXuyOFE2QDdyMR?=
NCI-H82 NFPQ[ZlCeG:ydH;zbZMhSXO|YYm= MYGwMlMwOS9|IN88US=> NEiwe4M1QCCq M3\tUolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MmLjNlQyPTh5MEG=
CWR22Rv1  MkK5RZBweHSxc3nzJGF{e2G7 M1jaWmlEPTB;MD60PFIh|ryP M2X0XlI{QTR{MEm1
CWR22Pc MWTBdI9xfG:|aYOgRZN{[Xl? MUDJR|UxRTBwNEO4JO69VQ>? MnHwNlM6PDJyOUW=
PC-3 M{D2UmFxd3C2b4Ppd{BCe3OjeR?= NXTtVndVUUN3ME2xMlc2PSEQvF2= NWfEc5hTOjN7NEKwPVU>
DU145 NUTkbHE1SXCxcITvd4l{KEG|c3H5 Mnr2TWM2OD1|LkWxO{DPxE1? NWfycYNrOjN7NEKwPVU>
RC165N M4L2ZWFxd3C2b4Ppd{BCe3OjeR?= NGjwfoVKSzVyPUKuNFg{KM7:TR?= NEXvU2MzOzl2MkC5OS=>
ARPE19 NYPsdGR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TySGROW09? MUPJR|UxRTJ2LkO4JO69VQ>? M2e5ZVI{PTNzOUKx
HEK293 MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnL2SG1UVw>? NGTrdolKSzVyPUiuOlch|ryP MmCzNlM2OzF7MkG=
KCNR NX3CU5BzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXexe3R6TE2VTx?= MkLITWM2OD1yLkS2JO69VQ>? NEDr[YMzOzV|MUmyNS=>
SY5Y NXzmT25QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX3V|RyTE2VTx?= MoPoTWM2OD1yLkO2JO69VQ>? M{D2SFI{PTNzOUKx
BE2 NYmxWVRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvTSG1UVw>? NHnGe4RKSzVyPUCuO|Eh|ryP NXrxdlB4OjN3M{G5NlE>
AS MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPTe2VFVVOR MoLiTWM2OD1zLkWzJO69VQ>? MVKyN|U{OTl{MR?=
NGP MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTtUmh3TE2VTx?= NETrU3pKSzVyPUCuOVYh|ryP MlLONlM2OzF7MkG=
IMR32 MnfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;EUXNQ NUHQdYl3UUN3ME2wMlY3KM7:TR?= NYT5XmZlOjN3M{G5NlE>
LAN5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TLTWROW09? NITjXYVKSzVyPUGuNFQh|ryP MmL4NlM2OzF7MkG=
RH18 NYryOFZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTXWHBYTE2VTx?= NU\Q[3N7UUN3ME2xMlQzKM7:TR?= NWnhcJJnOjN3M{G5NlE>
RH30 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v5[mROW09? NEjvVnhKSzVyPUGuNlUh|ryP MnTjNlM2OzF7MkG=
RH17 NWfwcFltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH4cndJTE2VTx?= MXjJR|UxRTJwNUGg{txO MmnsNlM2OzF7MkG=
RH28 Mo\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DGbmROW09? MofFTWM2OD12LkK4JO69VQ>? MlfLNlM2OzF7MkG=
RH36 MmHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37mWWROW09? MnPlTWM2OD13LkO3JO69VQ>? M3TBUFI{PTNzOUKx
RH41 NVz5Sml{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTLO5g5TE2VTx?= MXPJR|UxRTBwNEig{txO NXzYS3J2OjN3M{G5NlE>
RD MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrvTmFFVVOR NH3mUo1KSzVyPUSuN|Ih|ryP NULDTW4xOjN3M{G5NlE>
TC32 M4TNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP3eHBFVVOR NETlXJhKSzVyPUOuPFUh|ryP NX7YWnBFOjN3M{G5NlE>
TC71 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe4RmRvTE2VTx?= Mn3vTWM2OD12LkOzJO69VQ>? MljuNlM2OzF7MkG=
KCNR NGS5[49CeG:ydH;zbZMhSXO|YYm= NH[zOHAxNjVxMT6wM|IvPSEQvF2= MUWyOEBp NEPnSWtFVVOR MVfpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 M4jUTVI{PTNzOUKx
SY5Y NHj6S|RCeG:ydH;zbZMhSXO|YYm= NWDpdmFEOC53L{GuNE8zNjVizszN M3TaU|I1KGh? M{HwOWROW09? MnmybY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MkXhNlM2OzF7MkG=
Rh18 M1zrSmFxd3C2b4Ppd{BCe3OjeR?= M1vETFAvPS9zLkCvNk42KM7:TR?= NGfZb|EzPCCq NV;FPI9vTE2VTx?= MUHpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 M3niU|I{PTNzOUKx
TC32 NGXVZVdCeG:ydH;zbZMhSXO|YYm= NYnpd5ZQOC53L{GuNE8zNjVizszN M1T5dVI1KGh? M4XiW2ROW09? NVXSXGlscW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> M1\NVlI{PTNzOUKx
KCNR NXu0bYp5TnWwY4Tpc44hSXO|YYm= MnjTNE42NzFwMD:yMlUwPSEQvF2= NULhZnZGOjRiaB?= MXXEUXNQ Mnm5bY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NYW1O256OjN3M{G5NlE>
SY5Y M1LNdWZ2dmO2aX;uJGF{e2G7 NI\J[VMxNjVxMT6wM|IvPS93IN88US=> NX7hXW9LOjRiaB?= MWPEUXNQ NGDOfo9qdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MofRNlM2OzF7MkG=
Rh18 MkfISpVv[3Srb36gRZN{[Xl? MnXMNE42NzFwMD:yMlUwPSEQvF2= NH\MTWQzPCCq NWHyVFZFTE2VTx?= NGDlfZVqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MYKyN|U{OTl{MR?=
TC32 M4fFS2Z2dmO2aX;uJGF{e2G7 NFzFTlExNjVxMT6wM|IvPS93IN88US=> MkPPNlQhcA>? NWrSOYRpTE2VTx?= MVXpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NFfidFAzOzV|MUmyNS=>
TPC-1 MnrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHTNUDDvU1? MW[wMVQh\A>? NH:4PHdFVVOR MkS2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? NVfISJpJOjNyNU[0PVk>
MZ-CRC1  MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rCe|EhyrWP MViwMVUh\A>? M4jUZWROW09? M2\wdolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MWiyN|A2PjR7OR?=
TT  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvJXY1IOSEEtV2= Mnu5NE01KGR? NX7GR|Y3TE2VTx?= NGfsem1qdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 NWPzdm1IOjNyNU[0PVk>
TPC-1 NFLMRXRHfW6ldHnvckBCe3OjeR?= M3vud|EhyrWP Mn3DO|IhcA>? MnLQSG1UVw>? MnTqbY5lfWOnczDHNUBjdG:la3Hn[S=> NGLaboozOzB3NkS5PS=>
MZ-CRC1  NEjkV3BHfW6ldHnvckBCe3OjeR?= MlP0NUDDvU1? NHvXfIU4OiCq MnrFSG1UVw>? NVjFU3h7cW6mdXPld{BIOSCkbH;jb4Fo\Q>? MnTRNlMxPTZ2OUm=
TT  MX7GeY5kfGmxbjDBd5NigQ>? M1f0c|EhyrWP MV[3NkBp M{TkWWROW09? MoXobY5lfWOnczDHNUBjdG:la3Hn[S=> M{nEclI{ODV4NEm5
MZ-CRC1  M4j5ZWFxd3C2b4Ppd{BCe3OjeR?= MkDuNUDDvU1? NF7yNWM1QCCq NYfRZWNSTE2VTx?= NGDJd2FqdmS3Y3XzJIFxd3C2b4Ppdy=> MojxNlMxPTZ2OUm=
TT  NXvueW1xSXCxcITvd4l{KEG|c3H5 MnfTNUDDvU1? Mm\vOFghcA>? MYPEUXNQ NVjZUGhbcW6mdXPld{BieG:ydH;zbZM> NFr4SGMzOzB3NkS5PS=>
HD-LM2 M4LXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHndpU4OuLCiXi= NEXR[WFFVVOR NEGzNJpKSzVyPUeuPFQ1KM7:TR?= MXqyNlgzQTB7NB?=
L-428 M2S4Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjaRoVvPzMkgJno NUjZRnZGTE2VTx?= Mn7FTWM2OD15Lkm0O{DPxE1? Ml;oNlI5OjlyOUS=
KM-H2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTad2xSPzMkgJno MWHEUXNQ MUDJR|UxRTFwM{C4JO69VQ>? NVzS[Xd1OjJ6MkmwPVQ>
L-540 MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHw[Y84OuLCiXi= M{LJVmROW09? NFvIeXlKSzVyPUiuNlE3KM7:TR?= MnnWNlI5OjlyOUS=
HD-LM2 MXLGeY5kfGmxbjDBd5NigQ>? MWSwMlEwOC53L{GvOUDPxE1? M4fDbVcz6oDLaB?= M2X1fmROW09? MVvpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MmG3NlI5OjlyOUS=
L-428 NVm0cnhSTnWwY4Tpc44hSXO|YYm= M1POe|AvOS9yLkWvNU82KM7:TR?= MmXwO|LjiImq NYflO4F4TE2VTx?= NInFe5RqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NGDSem8zOjh{OUC5OC=>
KM-H2 NYLFNJp{TnWwY4Tpc44hSXO|YYm= NVjpUW9iOC5zL{CuOU8yNzVizszN MXi3NwKBkWh? MVPEUXNQ NU\DTZBPcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NVjGO2pLOjJ6MkmwPVQ>
L-540 MWrGeY5kfGmxbjDBd5NigQ>? NWD3UpBUOC5zL{CuOU8yNzVizszN M12xZ|cz6oDLaB?= M1HUO2ROW09? M1P1U4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v M4XTVlIzQDJ7MEm0
HD-LM2 MoXxRZBweHSxc3nzJGF{e2G7 M2T2R|EwPSEQvF2= MmrwO|LjiImq MojvSG1UVw>? NYLUTIN6cW6mdXPld{BieG:ydH;zbZM> MU[yNlgzQTB7NB?=
L-428 NYrtWVl2SXCxcITvd4l{KEG|c3H5 M4DaXVEwPSEQvF2= NHvGcVI4OuLCiXi= MljHSG1UVw>? M3TqPIlv\HWlZYOgZZBweHSxc3nz MV[yNlgzQTB7NB?=
KM-H2 MlrURZBweHSxc3nzJGF{e2G7 NImzWFYyNzVizszN M13mW|cz6oDLaB?= MlHRSG1UVw>? MX3pcoR2[2W|IHHwc5B1d3Orcx?= NFXnc3czOjh{OUC5OC=>
L-540 M3XESmFxd3C2b4Ppd{BCe3OjeR?= MmXVNU82KM7:TR?= NIPhU4Y4OuLCiXi= M2jpR2ROW09? Ml\ybY5lfWOnczDhdI9xfG:|aYO= M4D2WFIzQDJ7MEm0
U251-MG M2HrVWZ2dmO2aX;uJGF{e2G7 NX\0bG1pOSEEtV2= M4\NN|AuOTZiaB?= MlHKbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MnvKNlIxOjd4OUG=
U87-MG M2jiT2Z2dmO2aX;uJGF{e2G7 NUW2TmxNOSEEtV2= M1j0NFAuOTZiaB?= MUjpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> NFG0cFgzOjB{N{[5NS=>
4C8 NVflSGk5TnWwY4Tpc44hSXO|YYm= MXOxJOK2VQ>? MoniNE0yPiCq M2fLbolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? MknVNlIxOjd4OUG=
U251-MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq0TG0yNzFyINM1US=> M2HZ[|I1NzR6L{eyJIg> MV;pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NXPDWoZxOjJyMke2PVE>
U87-MG NUCzboRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSxM|ExKML3TR?= M1PkdVI1NzR6L{eyJIg> NFzhcYdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NH;jZpAzOjB{N{[5NS=>
4C8 NGn3TI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7sR|MyNzFyINM1US=> MXWyOE81QC95MjDo M3PzV4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO M4fO[FIzODJ5Nkmx
U266 M3fTbmFxd3C2b4Ppd{BCe3OjeR?= M1vRSlAvPS1{IN88US=> MlPqOFgwPzJiaB?= MnvmbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= Mk\nNlEyPjR3MUe=
Kms.11 NEnL[4RCeG:ydH;zbZMhSXO|YYm= M37nXFAvPS1{IN88US=> Mmj2OFgwPzJiaB?= M1vWN4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MmLNNlEyPjR3MUe=
8226 MW\BdI9xfG:|aYOgRZN{[Xl? MlSwNE42NTJizszN M4Kzb|Q5Nzd{IHi= NXfVfpVTcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NEPZRYIzOTF4NEWxOy=>

... 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 ()
% 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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*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