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 19 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 NInJWlFHfW6ldHnvckBCe3OjeR?= M{nBTVUh|ryP MkPDOFghcA>? NELoSHpFVVOR M4\sS4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> M3\DWFI2QTV2OUe0
LoVo  MlLGSpVv[3Srb36gRZN{[Xl? MXO1JO69VQ>? NYf6S5ltPDhiaB?= MYPEUXNQ NWfjdo5W[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NIrMd2szPTl3NEm3OC=>
HN5 NYHFSI1KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK3NkBp NV3MNlVETUN3ME2zMlgyKMLzIEGuPVkh|ryP NYnzTWpJOjV6MUCwNVA>
Cal33 Mn7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{izdVczKGh? MXrFR|UxRTNwM{egxtEhOC55NTFOwG0> M{LuclI2QDFyMEGw
UM-22B M2XmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vvclczKGh? NVXLTopNTUN3ME2yMlY3KMLzIECuNlQh|ryP NFXTbHczPThzMECxNC=>
686LN Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX6R|dqPzJiaB?= NYfXOFN5TUN3ME2yMlA2KMLzIEGuN|Mh|ryP MnTQNlU5OTByMUC=
UM SCC-1 MoHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW1Nox7PzJiaB?= M1;qVmVEPTB;MT62O{DDuSByLkSyJO69VQ>? M3TC[|I2QDFyMEGw
UM-22A Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX23NkBp NU\1b4FLTUN3ME2xMlMzKMLzIECuN|kh|ryP NWrRVnNKOjV6MUCwNVA>
OSC19 MoDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml74O|IhcA>? MorkSWM2OD1zLkK2JOKyKDBwMkCg{txO NH\sWo0zPThzMECxNC=>
PCI-52 MmOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDmO|IhcA>? MYDFR|UxRTFwMECgxtEhOC5yOTFOwG0> MWKyOVgyODBzMB?=
PCI-15B NXjlVZQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXu3NkBp M4nzXWVEPTB;MD65PUDDuSBzLke0JO69VQ>? NUfvVldKOjV6MUCwNVA>
UMSCC-1 MVzGeY5kfGmxbjDBd5NigQ>? M2PIfFAvODByNT2xMlYh|ryP NYfBdWE2OjRiaB?= MY\hZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NEG5fHYzPThzMECxNC=>
Cal33 MojBSpVv[3Srb36gRZN{[Xl? MoraNE4xODB3LUOuPEDPxE1? MYeyOEBp MUfhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NV34SG1tOjV6MUCwNVA>
HH5 NX3zd4lzTnWwY4Tpc44hSXO|YYm= MV2wMlAxODVvMz64JO69VQ>? NXHLW2pbOjRiaB?= MWHhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NX\OXXdoOjV6MUCwNVA>
UM-22A NVvhOpF{TnWwY4Tpc44hSXO|YYm= NGDy[ZkxNjByMEWtNU43KM7:TR?= NGnZdHIzPCCq NE[4N5Ni[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHPEbGgzPThzMECxNC=>
A1847 NWfGdWdNTnWwY4Tpc44hSXO|YYm= M2H3eVAvODVvMUCg{txO NIjIUpMzPCCq M2KzPWROW00EoB?= NHG4cWVz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M2HDclI2PjR4MEG1
OVCAR-5 Ml6zSpVv[3Srb36gRZN{[Xl? M3jvUlAvODVvMUCg{txO NF3DfXQzPCCq MnP0SG1UV8Li NGT5eGhz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MmDQNlU3PDZyMUW=
OVCAR-8 NHe4dm1HfW6ldHnvckBCe3OjeR?= MYWwMlA2NTFyIN88US=> NHuwdoMzPCCq MWnEUXNQyqB? NYfTR2lPemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NXfYVo1pOjV4NE[wNVU>
MOVCAR-5447 NF2xU2pHfW6ldHnvckBCe3OjeR?= M{\WXlAvODVvMUCg{txO NF3NXVUzPCCq M3jKTWROW00EoB?= NGrtOZlz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M1HLUVI2PjR4MEG1
MOVCAR-5009 M1zDTmZ2dmO2aX;uJGF{e2G7 NX63ZmpSOC5yNT2xNEDPxE1? NIC1Z2EzPCCq MoLwSG1UV8Li NGHseppz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NYi0TmdnOjV4NE[wNVU>
A1847 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH6xVHYxNjB3LUGwJO69VQ>? NVq2eohOPzJiaB?= Mk\sSG1UVw>? MXvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M3nNZVI2PjR4MEG1
OVCAR-5 NVXEZmxHS2WubDDWbYFjcWyrdImgRZN{[Xl? M3m1Z|AvODVvMUCg{txO MUG3NkBp M2H4eWROW09? MkjYdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NHjSOI4zPTZ2NkCxOS=>
OVCAR-8  M{ixfGNmdGxiVnnhZoltcXS7IFHzd4F6 NFfa[ZoxNjB3LUGwJO69VQ>? M33JbFczKGh? M17ncWROW09? M4\0e5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN M3rLVlI2PjR4MEG1
OVCAR-5  NXPwV3RJSXCxcITvd4l{KEG|c3H5 NHLESVgxNjVxMT:1JO69VQ>? MYG0PEBp NFLDZ5lFVVOR M1fEb4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MVqyOVY1PjBzNR?=
OVCAR-8  MknsRZBweHSxc3nzJGF{e2G7 NF\XVVgxNjVxMT:1JO69VQ>? MlHPOFghcA>? MkPTSG1UVw>? MkOwbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= M4\xSlI2PjR4MEG1
AKRSL MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFfHR5k4OiCq M3XremlEPTExvK6xNEDPxE1? NGfjZpYzPTVyNE[zOS=>
PALJDL NUjrO|FVS2WubDDWbYFjcWyrdImgRZN{[Xl? MnzLO|IhcA>? MkfmTWM2OD1{LkSg{txO M1XFVVI2PTB2NkO1
MO4 MmK0SpVv[3Srb36gRZN{[Xl? NFHxSnUxNjVxMT:1JO69VQ>? NVq3NFVPPiCq NV3TUlJKcW6qaXLpeJMhWC2VVFHUN{BmgHC{ZYPzbY9vyqB? MW[yOVE1QTV|NR?=
DU145  NGDPOotHfW6ldHnvckBCe3OjeR?= MoG0NE0zODBibl2= M2fJRlEhcMLi NIjE[IJ{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NHj6cZYzPDV5N{m0Ni=>
DU145  NFz6fXpHfW6ldHnvckBCe3OjeR?= MmmxPFAxKG6P MYG3NkBp NH2yW4d{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= MlvTNlQ2Pzd7NEK=
CWR22Rv1 MUTGeY5kfGmxbjDBd5NigQ>? MYm4NFAhdk1? MXm3NkBp NEnoU4J{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NIjRd4gzPDV5N{m0Ni=>
N592 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M16wPGlEPTB;MD64OEDPxE1? NEju[IMzPDF3OEewNS=>
H82 M170fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\pUXZtUUN3ME2xMlM4KM7:TR?= NXXyU|VqOjRzNUi3NFE>
GLC4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHVTWM2OD1zLke5JO69VQ>? NGPCT3gzPDF3OEewNS=>
H526 M4nGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLp[3FqUUN3ME2zMlA5KM7:TR?= NX;uT29vOjRzNUi3NFE>
H1173 M3:4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUT5bYREUUN3ME2yMlM6KM7:TR?= NVvFSVhLOjRzNUi3NFE>
DMS114 NVnCTpdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHa[XlKSzVyPUCuO|Mh|ryP M1PPNFI1OTV6N{Cx
NCI-N592 MVTGeY5kfGmxbjDBd5NigQ>? MWGwMlMwOS9|IN88US=> NHfLWJIzPCCq NUDKZ2IycW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NUOzbIZROjRzNUi3NFE>
GLC4 NYKybGJsTnWwY4Tpc44hSXO|YYm= NGDIZYgxNjNxMT:zJO69VQ>? MnflNlQhcA>? NGTQZ|RqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NHHqPI8zPDF3OEewNS=>
NCI-H82 NUmxZpRYTnWwY4Tpc44hSXO|YYm= MknKNE4{NzFxMzFOwG0> NULpRmlnOjRiaB?= NGm1ZlBqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MknSNlQyPTh5MEG=
NCI-N592 NXW2SpNSSXCxcITvd4l{KEG|c3H5 M2XNdFAvOy9zL{Og{txO MW[0PEBp MmDDbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MlrsNlQyPTh5MEG=
GLC4 NWnwNXg3SXCxcITvd4l{KEG|c3H5 MmjrNE4{NzFxMzFOwG0> MnfsOFghcA>? NWi3XW9HcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MlrkNlQyPTh5MEG=
NCI-H82 NHn4SGtCeG:ydH;zbZMhSXO|YYm= NHX1c40xNjNxMT:zJO69VQ>? MkLlOFghcA>? M1HoTIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M1:3b|I1OTV6N{Cx
CWR22Rv1  MXzBdI9xfG:|aYOgRZN{[Xl? MVnJR|UxRTBwNEiyJO69VQ>? M{S0OFI{QTR{MEm1
CWR22Pc M3zpfWFxd3C2b4Ppd{BCe3OjeR?= NV3RTY82UUN3ME2wMlQ{QCEQvF2= MlW1NlM6PDJyOUW=
PC-3 MVvBdI9xfG:|aYOgRZN{[Xl? NIn5UFJKSzVyPUGuO|U2KM7:TR?= M3;VbFI{QTR{MEm1
DU145 MlfIRZBweHSxc3nzJGF{e2G7 NFe1b49KSzVyPUOuOVE4KM7:TR?= M{\sSVI{QTR{MEm1
RC165N M4rFOWFxd3C2b4Ppd{BCe3OjeR?= MYfJR|UxRTJwMEizJO69VQ>? MWOyN|k1OjB7NR?=
ARPE19 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrEbW1VTE2VTx?= MUHJR|UxRTJ2LkO4JO69VQ>? NVfBUJNtOjN3M{G5NlE>
HEK293 M3m4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHON|hFVVOR MW\JR|UxRThwNkeg{txO Ml:1NlM2OzF7MkG=
KCNR M{fIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVL3bHdMTE2VTx?= MYrJR|UxRTBwNE[g{txO MX:yN|U{OTl{MR?=
SY5Y M{nR[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu2VG1ZTE2VTx?= M323WWlEPTB;MD6zOkDPxE1? NV;BU3R3OjN3M{G5NlE>
BE2 MmPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnEUXNQ NXr1SZlPUUN3ME2wMlcyKM7:TR?= NVT2SWpbOjN3M{G5NlE>
AS M4nmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX33VWpZTE2VTx?= M4nvSWlEPTB;MT61N{DPxE1? Mke4NlM2OzF7MkG=
NGP NWHmWVAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\KdWROW09? NVK0[ZZ4UUN3ME2wMlU3KM7:TR?= NWLiSoRVOjN3M{G5NlE>
IMR32 M37admdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXkWWVbTE2VTx?= MoDrTWM2OD1yLk[2JO69VQ>? M3fJU|I{PTNzOUKx
LAN5 NYjWdmNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorXSG1UVw>? MorTTWM2OD1zLkC0JO69VQ>? M3PlZVI{PTNzOUKx
RH18 NHXPdolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjEUXNQ NFvGfI5KSzVyPUGuOFIh|ryP NGPXc|UzOzV|MUmyNS=>
RH30 NHizSHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUmwNlVlTE2VTx?= Mo\UTWM2OD1zLkK1JO69VQ>? M1fsTlI{PTNzOUKx
RH17 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XKbmROW09? Mn2wTWM2OD1{LkWxJO69VQ>? NWPvVW91OjN3M{G5NlE>
RH28 NWnJSFZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfPSG1UVw>? NF3KdW9KSzVyPUSuNlgh|ryP NVy5fopHOjN3M{G5NlE>
RH36 Ml\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvEUXNQ NHnMcllKSzVyPUWuN|ch|ryP MXyyN|U{OTl{MR?=
RH41 M4G2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml20SG1UVw>? M1nv[GlEPTB;MD60PEDPxE1? MV:yN|U{OTl{MR?=
RD NUnZTWZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4q5bWROW09? NX\IRohUUUN3ME20MlMzKM7:TR?= M2rlR|I{PTNzOUKx
TC32 NWXiUVhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXWUIpFVVOR MXfJR|UxRTNwOEWg{txO NXn2UXNGOjN3M{G5NlE>
TC71 NV:xOGRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnkO3lFVVOR NEfLTY9KSzVyPUSuN|Mh|ryP NGD1UGczOzV|MUmyNS=>
KCNR M1XoTmFxd3C2b4Ppd{BCe3OjeR?= NGL1cpoxNjVxMT6wM|IvPSEQvF2= NGjZd4wzPCCq MknKSG1UVw>? MoTrbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NWGzW5NYOjN3M{G5NlE>
SY5Y MlrlRZBweHSxc3nzJGF{e2G7 NUGy[pV4OC53L{GuNE8zNjVizszN M4XPcVI1KGh? MYfEUXNQ NULkdZZxcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NFzBS5EzOzV|MUmyNS=>
Rh18 M{nCWGFxd3C2b4Ppd{BCe3OjeR?= NHG3WGMxNjVxMT6wM|IvPSEQvF2= NYO2WnU5OjRiaB?= MUHEUXNQ MXHpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MVuyN|U{OTl{MR?=
TC32 NXHWb5B1SXCxcITvd4l{KEG|c3H5 MWGwMlUwOS5yL{KuOUDPxE1? NEjTe4czPCCq M2DIc2ROW09? NU[2bXZHcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NVy2WmU{OjN3M{G5NlE>
KCNR NEe3VYNHfW6ldHnvckBCe3OjeR?= NXu1fItTOC53L{GuNE8zNjVxNTFOwG0> MViyOEBp MmPjSG1UVw>? M3:0[YlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NG\NOIkzOzV|MUmyNS=>
SY5Y M4TE[WZ2dmO2aX;uJGF{e2G7 NFKzSlYxNjVxMT6wM|IvPS93IN88US=> M3fRelI1KGh? MYLEUXNQ Ml3GbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NYPmNoI2OjN3M{G5NlE>
Rh18 NGjYSnJHfW6ldHnvckBCe3OjeR?= MkPLNE42NzFwMD:yMlUwPSEQvF2= NVW0Vm82OjRiaB?= NXf3eGlGTE2VTx?= MYDpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= M2ntbFI{PTNzOUKx
TC32 M4jPNWZ2dmO2aX;uJGF{e2G7 NWrzWmJjOC53L{GuNE8zNjVxNTFOwG0> MkXZNlQhcA>? M4jm[mROW09? NGi3ZWZqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NYnlU25WOjN3M{G5NlE>
TPC-1 MmLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PkXFEhyrWP Mkj5NE01KGR? NX72UFN{TE2VTx?= NWLhTnZicW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOiCmIITy[YF1dWWwdB?= M3u4NFI{ODV4NEm5
MZ-CRC1  MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTwSoozOSEEtV2= M4XvN|AuPSCm MV;EUXNQ NWjTXmpUcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= M4HMWFI{ODV4NEm5
TT  MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOxJOK2VQ>? NWO1SJVFOC12IHS= M1\xT2ROW09? MWTpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 MUGyN|A2PjR7OR?=
TPC-1 NHPnOZdHfW6ldHnvckBCe3OjeR?= MVGxJOK2VQ>? MlvtO|IhcA>? Ml;NSG1UVw>? NIrscWlqdmS3Y3XzJGcyKGKub3PrZYdm NUS3[|NKOjNyNU[0PVk>
MZ-CRC1  MXzGeY5kfGmxbjDBd5NigQ>? MXuxJOK2VQ>? MUe3NkBp NITWb3NFVVOR MmjtbY5lfWOnczDHNUBjdG:la3Hn[S=> M2PsXFI{ODV4NEm5
TT  M3LGNmZ2dmO2aX;uJGF{e2G7 NYjubFgzOSEEtV2= MXi3NkBp M3S3OGROW09? NYHET2RHcW6mdXPld{BIOSCkbH;jb4Fo\Q>? NV31OVRtOjNyNU[0PVk>
MZ-CRC1  Mli3RZBweHSxc3nzJGF{e2G7 M1zVNFEhyrWP M1zKXVQ5KGh? MYrEUXNQ NW\UWYZqcW6mdXPld{BieG:ydH;zbZM> NHjUeYEzOzB3NkS5PS=>
TT  MUDBdI9xfG:|aYOgRZN{[Xl? NIDTcVIyKML3TR?= NHLLfWc1QCCq Mlj2SG1UVw>? M2CwOolv\HWlZYOgZZBweHSxc3nz M1SzU|I{ODV4NEm5
HD-LM2 Ml7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYKxO3VJPzMkgJno MVLEUXNQ NXKw[5d6UUN3ME23Mlg1PCEQvF2= M4nVT|IzQDJ7MEm0
L-428 Mln6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFG3eHE4OuLCiXi= MVXEUXNQ MlzwTWM2OD15Lkm0O{DPxE1? MmfFNlI5OjlyOUS=
KM-H2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjtcVZ{PzMkgJno NYjpbFQ{TE2VTx?= NVe1fYpDUUN3ME2xMlMxQCEQvF2= MXmyNlgzQTB7NB?=
L-540 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYS3NwKBkWh? M4XaVWROW09? MWTJR|UxRThwMkG2JO69VQ>? NYDUVo5LOjJ6MkmwPVQ>
HD-LM2 NHnLVHlHfW6ldHnvckBCe3OjeR?= NWq2RWJGOC5zL{CuOU8yNzVizszN NILM[|g4OuLCiXi= MULEUXNQ NHuySINqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? M4fNUlIzQDJ7MEm0
L-428 MX3GeY5kfGmxbjDBd5NigQ>? MUCwMlEwOC53L{GvOUDPxE1? M1XKZ|cz6oDLaB?= NWjmXW9mTE2VTx?= M4TzbIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MmHQNlI5OjlyOUS=
KM-H2 M2C4RmZ2dmO2aX;uJGF{e2G7 MV[wMlEwOC53L{GvOUDPxE1? M1:xcVcz6oDLaB?= NE[zXldFVVOR MY\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MmrPNlI5OjlyOUS=
L-540 MmPQSpVv[3Srb36gRZN{[Xl? NFK4eY8xNjFxMD61M|EwPSEQvF2= MUC3NwKBkWh? MoPJSG1UVw>? MnfKbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NULpTYNjOjJ6MkmwPVQ>
HD-LM2 MXXBdI9xfG:|aYOgRZN{[Xl? MoPBNU82KM7:TR?= M2XU[|cz6oDLaB?= NYfPWWJ1TE2VTx?= M1fIVolv\HWlZYOgZZBweHSxc3nz NV3NU3k3OjJ6MkmwPVQ>
L-428 NUX0XY9USXCxcITvd4l{KEG|c3H5 NHvqdoYyNzVizszN MkL6O|LjiImq NGHwZ3pFVVOR M2C3RYlv\HWlZYOgZZBweHSxc3nz NFj4b2MzOjh{OUC5OC=>
KM-H2 NV3hU2tESXCxcITvd4l{KEG|c3H5 MWSxM|Uh|ryP MV[3NwKBkWh? Mn3pSG1UVw>? NYftXW02cW6mdXPld{BieG:ydH;zbZM> NGe0WmYzOjh{OUC5OC=>
L-540 M{PoZ2Fxd3C2b4Ppd{BCe3OjeR?= NWjXPFFSOS93IN88US=> M{mzTFcz6oDLaB?= MYnEUXNQ M16yV4lv\HWlZYOgZZBweHSxc3nz M4HnclIzQDJ7MEm0
U251-MG M4nDdmZ2dmO2aX;uJGF{e2G7 MV2xJOK2VQ>? M{PSWVAuOTZiaB?= M3XmVYlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? M{nYb|IzODJ5Nkmx
U87-MG MX7GeY5kfGmxbjDBd5NigQ>? M3HEU|EhyrWP M3zzbFAuOTZiaB?= NXzDZZBqcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w M3T6RVIzODJ5Nkmx
4C8 MlTtSpVv[3Srb36gRZN{[Xl? NUDYUnlIOSEEtV2= M{\DN|AuOTZiaB?= MlKwbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MlLHNlIxOjd4OUG=
U251-MG M4rlZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPrNU8yOCEEtV2= NYjqUYR{OjRxNEivO|IhcA>? M1jwd4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO MWWyNlAzPzZ7MR?=
U87-MG MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqxM|ExKML3TR?= NFzoUHUzPC92OD:3NkBp NIXKNpdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MVqyNlAzPzZ7MR?=
4C8 NIm2[W5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XZ[FEwOTBiwsXN NUT1NJU6OjRxNEivO|IhcA>? MYfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> M1XBNVIzODJ5Nkmx
U266 MmPRRZBweHSxc3nzJGF{e2G7 Mn3jNE42NTJizszN NGfXPWE1QC95MjDo MYTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NGjOWoYzOTF4NEWxOy=>
Kms.11 NILBPVZCeG:ydH;zbZMhSXO|YYm= NXX2OYI4OC53LUKg{txO NY\qfo5EPDhxN{KgbC=> MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MoLRNlEyPjR3MUe=
8226 MnXTRZBweHSxc3nzJGF{e2G7 Ml32NE42NTJizszN NImwOlk1QC95MjDo MUDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NFrl[4gzOTF4NEWxOy=>

... Click to View More Cell Line Experimental Data

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

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    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

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01219543 Terminated Solid Tumour|Advanced Solid Malignancies|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma|EGFR and/or ROS Mutant NSCLC|Lung Metastasis Carcinoma|Gastric Cancer AstraZeneca November 2010 Phase 1
NCT01219543 Terminated Solid Tumour|Advanced Solid Malignancies|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma|EGFR and/or ROS Mutant NSCLC|Lung Metastasis Carcinoma|Gastric Cancer AstraZeneca November 2010 Phase 1
NCT01112397 Terminated Solid Malignancies AstraZeneca April 2010 Phase 1
NCT01112397 Terminated Solid Malignancies AstraZeneca April 2010 Phase 1
NCT00910728 Completed Primary Myelofibrosis (PMF)|Post-Polycythaemia Vera|Essential Thrombocythaemia Myelofibrosis AstraZeneca|University of Texas|New York City Hoffman Center|Gustave Roussy Cancer Campus Grand Paris May 2009 Phase 1
NCT00910728 Completed Primary Myelofibrosis (PMF)|Post-Polycythaemia Vera|Essential Thrombocythaemia Myelofibrosis AstraZeneca|University of Texas|New York City Hoffman Center|Gustave Roussy Cancer Campus Grand Paris May 2009 Phase 1

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.

  • * Indicates a Required Field

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID