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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4 Customer Reviews

  • bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.

    Nat Cell Biol, 2015, 17(1): 57-67. AZD1480 purchased from Selleck.

    Adipocytes were pre-infected with pAd-Foxc2 or si-Foxc2, and incubated with AZD1480 or not. Figures show protein levels of leptin, IL-6 and TNFα in adipocytes.

    Int J Obes, 2018, 42(2):252-259. AZD1480 purchased from Selleck.

  • A431 cells were treated with ALA-PDT alone or pretreated with 1μM AZD1480 for 1h or pretreated with 1ng/ml OSM for 10 minutes and the protein expression of Bcl-2 and Bax were analyzed by Western Blot.

    Photodiagnosis Photodyn Ther, 2016, 14:119-27. AZD1480 purchased from Selleck.

    HEL cells were treated for 3 hours with the indicated concentrations of AZD1480. AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar  concentrations in intact cells.

     

     

    M.Sc. Karoline Gaebler and Dr. Claude Haan of Université du Luxembour. AZD1480 purchased from Selleck.

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{nlR2Z2dmO2aX;uJGF{e2G7 MkDVOUDPxE1? NHyy[Ws1QCCq NWS0dZRDTE2VTx?= M3n3RYJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MVeyOVk2PDl5NB?=
LoVo  MoDoSpVv[3Srb36gRZN{[Xl? M1Xpc|Uh|ryP M3nZblQ5KGh? NHvZeJVFVVOR NHXJfIpjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> M37aZ|I2QTV2OUe0
HN5 NHnGXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LaNFczKGh? NGLWeGhGSzVyPUOuPFEhyrFiMT65PUDPxE1? MXSyOVgyODBzMB?=
Cal33 NU\OfVFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUizTG5uPzJiaB?= MVXFR|UxRTNwM{egxtEhOC55NTFOwG0> NX\xWodnOjV6MUCwNVA>
UM-22B MlyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS3NkBp MUXFR|UxRTJwNk[gxtEhOC5{NDFOwG0> NGPoWZQzPThzMECxNC=>
686LN MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDObZhoPzJiaB?= NH7mVZJGSzVyPUKuNFUhyrFiMT6zN{DPxE1? MlXLNlU5OTByMUC=
UM SCC-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTRcGlGPzJiaB?= NI[wbnNGSzVyPUGuOlchyrFiMD60NkDPxE1? Mo\1NlU5OTByMUC=
UM-22A NFjBVYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYq3NkBp MkjBSWM2OD1zLkOyJOKyKDBwM{mg{txO MVyyOVgyODBzMB?=
OSC19 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXEe3dUPzJiaB?= MXHFR|UxRTFwMk[gxtEhOC5{MDFOwG0> MnjFNlU5OTByMUC=
PCI-52 M1\sN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3pdYQ4OiCq NH60S3FGSzVyPUGuNFAhyrFiMD6wPUDPxE1? NGG0[oUzPThzMECxNC=>
PCI-15B MoPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLC[pJ[PzJiaB?= NX7nNYd4TUN3ME2wMlk6KMLzIEGuO|Qh|ryP NVO5WIEyOjV6MUCwNVA>
UMSCC-1 MYXGeY5kfGmxbjDBd5NigQ>? M3jUV|AvODByNT2xMlYh|ryP NIPSd3czPCCq MX\hZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFHTfYUzPThzMECxNC=>
Cal33 NHy4TWZHfW6ldHnvckBCe3OjeR?= MmrTNE4xODB3LUOuPEDPxE1? NIrqdFgzPCCq MXvhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NX24cWpSOjV6MUCwNVA>
HH5 M3vLbmZ2dmO2aX;uJGF{e2G7 MYGwMlAxODVvMz64JO69VQ>? NF3RbXIzPCCq NInuUnNi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MofWNlU5OTByMUC=
UM-22A NESxXJJHfW6ldHnvckBCe3OjeR?= NV:yeYR6OC5yMEC1MVEvPiEQvF2= MkLZNlQhcA>? MUDhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MWmyOVgyODBzMB?=
A1847 MnW0SpVv[3Srb36gRZN{[Xl? NVnOPJlTOC5yNT2xNEDPxE1? Mnj6NlQhcA>? MXXEUXNQyqB? M4DIXZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NX6wPHNqOjV4NE[wNVU>
OVCAR-5 NGTLTo9HfW6ldHnvckBCe3OjeR?= NFnHb2IxNjB3LUGwJO69VQ>? NILYWXkzPCCq NHrocmhFVVORwrC= NH3LVlhz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MnfqNlU3PDZyMUW=
OVCAR-8 MUPGeY5kfGmxbjDBd5NigQ>? MU[wMlA2NTFyIN88US=> MXyyOEBp M2LSfWROW00EoB?= M33DV5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NX3m[ld6OjV4NE[wNVU>
MOVCAR-5447 M4Ptb2Z2dmO2aX;uJGF{e2G7 MlfuNE4xPS1zMDFOwG0> NUHYbnRDOjRiaB?= MYDEUXNQyqB? MXjy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MkS1NlU3PDZyMUW=
MOVCAR-5009 MX7GeY5kfGmxbjDBd5NigQ>? NUGyOWtjOC5yNT2xNEDPxE1? MmDyNlQhcA>? MWjEUXNQyqB? MVry[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NVLpbnpGOjV4NE[wNVU>
A1847 M1XBO2NmdGxiVnnhZoltcXS7IFHzd4F6 MXywMlA2NTFyIN88US=> NVzlNWVTPzJiaB?= NXu2PVU4TE2VTx?= NEjZWINz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MVWyOVY1PjBzNR?=
OVCAR-5 M1OwSWNmdGxiVnnhZoltcXS7IFHzd4F6 NGL0NpAxNjB3LUGwJO69VQ>? MVy3NkBp M4rlSWROW09? MWHy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M3i3elI2PjR4MEG1
OVCAR-8  M2\NR2NmdGxiVnnhZoltcXS7IFHzd4F6 NEW4ZmgxNjB3LUGwJO69VQ>? NHjaOYI4OiCq MofnSG1UVw>? NH76ZZBz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NEnufHYzPTZ2NkCxOS=>
OVCAR-5  MWfBdI9xfG:|aYOgRZN{[Xl? NYDEb4p7OC53L{GvOUDPxE1? NVLrSIxXPDhiaB?= Mk\0SG1UVw>? NIXtVIdqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u MoPZNlU3PDZyMUW=
OVCAR-8  NIO1TJBCeG:ydH;zbZMhSXO|YYm= M3zLeVAvPS9zL{Wg{txO NGi2ZZM1QCCq M2LPSGROW09? NXrIWZFbcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> MW[yOVY1PjBzNR?=
AKRSL MkX4R4VtdCCYaXHibYxqfHliQYPzZZk> MUS3NkBp MX7JR|Ux97zgMUCg{txO NH22epEzPTVyNE[zOS=>
PALJDL M1LpSWNmdGxiVnnhZoltcXS7IFHzd4F6 MnywO|IhcA>? MoXiTWM2OD1{LkSg{txO MnKxNlU2ODR4M{W=
MO4 M2q3fmZ2dmO2aX;uJGF{e2G7 M4DxOVAvPS9zL{Wg{txO NU\xO5BLPiCq M{Xjc4lvcGmkaYTzJHAuW1SDVEOg[ZhxemW|c3nvcuKh Mnq0NlUyPDl3M{W=
DU145  NHOzd3FHfW6ldHnvckBCe3OjeR?= MmPBNE0zODBibl2= MVWxJIjDqA>? NFXOXnB{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NY\SdFJ[OjR3N{e5OFI>
DU145  NVjwV2sxTnWwY4Tpc44hSXO|YYm= M3ftWFgxOCCwTR?= MUO3NkBp NFvncXp{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NXiwW45JOjR3N{e5OFI>
CWR22Rv1 NXfV[VlkTnWwY4Tpc44hSXO|YYm= MX64NFAhdk1? M1fwZlczKGh? M{nxU5N2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= M1TDZlI1PTd5OUSy
N592 M2Ptcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwOESg{txO M3\1W|I1OTV6N{Cx
H82 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i3[2lEPTB;MT6zO{DPxE1? MUKyOFE2QDdyMR?=
GLC4 M2j6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW2SFRKSzVyPUGuO|kh|ryP MmPoNlQyPTh5MEG=
H526 NVzV[4JbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnQTWM2OD1|LkC4JO69VQ>? M3\TVVI1OTV6N{Cx
H1173 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\OSG9wUUN3ME2yMlM6KM7:TR?= NEXvOmgzPDF3OEewNS=>
DMS114 NWDqdJc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwN{Og{txO MV6yOFE2QDdyMR?=
NCI-N592 NXLmfWNkTnWwY4Tpc44hSXO|YYm= NXy5dIY6OC5|L{GvN{DPxE1? NEfTeZczPCCq NXTM[HpRcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NYrIXlNyOjRzNUi3NFE>
GLC4 MUDGeY5kfGmxbjDBd5NigQ>? M1\1RlAvOy9zL{Og{txO MU[yOEBp NGP1PIVqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NXr6SpJNOjRzNUi3NFE>
NCI-H82 MnHaSpVv[3Srb36gRZN{[Xl? MnPQNE4{NzFxMzFOwG0> MWOyOEBp MnzPbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 Mke4NlQyPTh5MEG=
NCI-N592 MlvwRZBweHSxc3nzJGF{e2G7 NVzWTG9sOC5|L{GvN{DPxE1? MXu0PEBp M1vVdYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NG\6OoEzPDF3OEewNS=>
GLC4 NGXvNnJCeG:ydH;zbZMhSXO|YYm= NW\OR|FNOC5|L{GvN{DPxE1? Mm[5OFghcA>? MYLpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ M1rONlI1OTV6N{Cx
NCI-H82 Ml7PRZBweHSxc3nzJGF{e2G7 NGfZRWkxNjNxMT:zJO69VQ>? NUfUVXBJPDhiaB?= MmHRbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MWWyOFE2QDdyMR?=
CWR22Rv1  NVu5XZJPSXCxcITvd4l{KEG|c3H5 MXfJR|UxRTBwNEiyJO69VQ>? NWHTO4NuOjN7NEKwPVU>
CWR22Pc M33YfmFxd3C2b4Ppd{BCe3OjeR?= MYrJR|UxRTBwNEO4JO69VQ>? NULoV|NHOjN7NEKwPVU>
PC-3 MnnaRZBweHSxc3nzJGF{e2G7 MUTJR|UxRTFwN{W1JO69VQ>? M4PMelI{QTR{MEm1
DU145 M1rLVWFxd3C2b4Ppd{BCe3OjeR?= M3fX[WlEPTB;Mz61NVch|ryP NXPBOYpXOjN7NEKwPVU>
RC165N NFfWUYpCeG:ydH;zbZMhSXO|YYm= M1rr[GlEPTB;Mj6wPFMh|ryP M4jHWVI{QTR{MEm1
ARPE19 MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInwbWdFVVOR MV7JR|UxRTJ2LkO4JO69VQ>? M1X5XVI{PTNzOUKx
HEK293 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLzSG1UVw>? MnLoTWM2OD16Lk[3JO69VQ>? NFS2cJQzOzV|MUmyNS=>
KCNR M{KwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTEUXNQ MnfDTWM2OD1yLkS2JO69VQ>? NUP1VJNSOjN3M{G5NlE>
SY5Y M33hZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XTUmROW09? M2rXN2lEPTB;MD6zOkDPxE1? NGjMOFUzOzV|MUmyNS=>
BE2 NX3TR3BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf2eYpFVVOR NID6WndKSzVyPUCuO|Eh|ryP MVOyN|U{OTl{MR?=
AS NWTNc4R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPEUXNQ NEC3fIVKSzVyPUGuOVMh|ryP MWmyN|U{OTl{MR?=
NGP M4jUdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrEUXNQ M1\Yd2lEPTB;MD61OkDPxE1? M4Gz[|I{PTNzOUKx
IMR32 MnnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXrSG1UVw>? MXzJR|UxRTBwNk[g{txO MX[yN|U{OTl{MR?=
LAN5 NHGye5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPEUXNQ NGjRToVKSzVyPUGuNFQh|ryP NGLrb3YzOzV|MUmyNS=>
RH18 NUm5TGxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjEUXNQ MX7JR|UxRTFwNEKg{txO NXnHPGF4OjN3M{G5NlE>
RH30 NV3QPWt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vNb2ROW09? NX\3b4l4UUN3ME2xMlI2KM7:TR?= Ml3CNlM2OzF7MkG=
RH17 M{nhWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjBNYFFVVOR M1fwWWlEPTB;Mj61NUDPxE1? NXHaV2YzOjN3M{G5NlE>
RH28 NULITGdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjhSG1UVw>? Mny1TWM2OD12LkK4JO69VQ>? M3LSSVI{PTNzOUKx
RH36 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLXPIZFVVOR MVnJR|UxRTVwM{eg{txO MWCyN|U{OTl{MR?=
RH41 M{LKUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrUSG1UVw>? NVzQbpRUUUN3ME2wMlQ5KM7:TR?= MmnGNlM2OzF7MkG=
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TC71 M1XTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXUT29yTE2VTx?= NF3zSFZKSzVyPUSuN|Mh|ryP NXrQUIdDOjN3M{G5NlE>
KCNR NWHNW45QSXCxcITvd4l{KEG|c3H5 M4K1[lAvPS9zLkCvNk42KM7:TR?= NXHSSZY5OjRiaB?= MlfQSG1UVw>? NIf4S4VqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NYTDW4JHOjN3M{G5NlE>
SY5Y M1j0SWFxd3C2b4Ppd{BCe3OjeR?= NFzKSJUxNjVxMT6wM|IvPSEQvF2= MonHNlQhcA>? NYDLbWJUTE2VTx?= MlvYbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NUDwV4NoOjN3M{G5NlE>
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SY5Y M{TGNmZ2dmO2aX;uJGF{e2G7 MUewMlUwOS5yL{KuOU82KM7:TR?= NXPHWpZNOjRiaB?= Ml;aSG1UVw>? M{L5NYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NGTuVGMzOzV|MUmyNS=>
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TC32 NITue5lHfW6ldHnvckBCe3OjeR?= NXHVUJVDOC53L{GuNE8zNjVxNTFOwG0> MUWyOEBp MmDuSG1UVw>? M4Huc4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u MV:yN|U{OTl{MR?=
TPC-1 M{H4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzwRWYyKML3TR?= NX72ZVFCOC12IHS= MUTEUXNQ M3rOTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? MnrtNlMxPTZ2OUm=
MZ-CRC1  M1vHOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33FbVEhyrWP NFG4fpMxNTViZB?= NGG3THdFVVOR NIXWZ5RqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 M1XLXlI{ODV4NEm5
TT  M37TN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCxJOK2VQ>? MY[wMVQh\A>? MUPEUXNQ MXPpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 NF7mWIgzOzB3NkS5PS=>
TPC-1 Mn\2SpVv[3Srb36gRZN{[Xl? M1XzblEhyrWP NELi[444OiCq Mn7pSG1UVw>? M3W3dYlv\HWlZYOgS|Eh[myxY3vh[4U> MnP6NlMxPTZ2OUm=
MZ-CRC1  NHLyUHNHfW6ldHnvckBCe3OjeR?= MojaNUDDvU1? MV23NkBp NGrZZ5VFVVOR MYPpcoR2[2W|IFexJIJtd2OtYXfl MkH5NlMxPTZ2OUm=
TT  M2\EUmZ2dmO2aX;uJGF{e2G7 MUexJOK2VQ>? MXO3NkBp NHLwZodFVVOR MmDsbY5lfWOnczDHNUBjdG:la3Hn[S=> NXq5PWNEOjNyNU[0PVk>
MZ-CRC1  NGD1WWhCeG:ydH;zbZMhSXO|YYm= NWTBVpBSOSEEtV2= NVHnboFkPDhiaB?= MV;EUXNQ M{nG[olv\HWlZYOgZZBweHSxc3nz MVmyN|A2PjR7OR?=
TT  NELmcnBCeG:ydH;zbZMhSXO|YYm= NUHmOlRnOSEEtV2= M2LsfFQ5KGh? M33LZ2ROW09? MmDObY5lfWOnczDhdI9xfG:|aYO= NFTHdYwzOzB3NkS5PS=>
HD-LM2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L6[|cz6oDLaB?= MWHEUXNQ MYjJR|UxRTdwOES0JO69VQ>? NYW0S4l3OjJ6MkmwPVQ>
L-428 NVPzfHRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDlO|LjiImq NV[wNVdITE2VTx?= NH65fHhKSzVyPUeuPVQ4KM7:TR?= MYeyNlgzQTB7NB?=
KM-H2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzJfVI4OuLCiXi= NFu3R2ZFVVOR MWDJR|UxRTFwM{C4JO69VQ>? M1XXSFIzQDJ7MEm0
L-540 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33xU|cz6oDLaB?= NYDBVGdDTE2VTx?= MVTJR|UxRThwMkG2JO69VQ>? MV2yNlgzQTB7NB?=
HD-LM2 M2LNPWZ2dmO2aX;uJGF{e2G7 NXzxVGszOC5zL{CuOU8yNzVizszN MX:3NwKBkWh? NXqzOoxMTE2VTx?= MnyxbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MWSyNlgzQTB7NB?=
L-428 M3TJfmZ2dmO2aX;uJGF{e2G7 MViwMlEwOC53L{GvOUDPxE1? MV23NwKBkWh? Ml3vSG1UVw>? Mn3HbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MWeyNlgzQTB7NB?=
KM-H2 NFu2WnpHfW6ldHnvckBCe3OjeR?= NVTQ[IFTOC5zL{CuOU8yNzVizszN MoXPO|LjiImq NGnKOHJFVVOR NXzXcIpWcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NGr0b5gzOjh{OUC5OC=>
L-540 MUHGeY5kfGmxbjDBd5NigQ>? M1vFT|AvOS9yLkWvNU82KM7:TR?= MXW3NwKBkWh? MkK0SG1UVw>? NUW0Z28xcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MonzNlI5OjlyOUS=
HD-LM2 MlnORZBweHSxc3nzJGF{e2G7 MkfCNU82KM7:TR?= M3LCXlcz6oDLaB?= M3[1e2ROW09? MV7pcoR2[2W|IHHwc5B1d3Orcx?= NFT6S2czOjh{OUC5OC=>
L-428 NH\wWFZCeG:ydH;zbZMhSXO|YYm= M{K1fVEwPSEQvF2= M2\4XFcz6oDLaB?= M1qyPWROW09? MVnpcoR2[2W|IHHwc5B1d3Orcx?= M{jGNlIzQDJ7MEm0
KM-H2 MWrBdI9xfG:|aYOgRZN{[Xl? Mk\0NU82KM7:TR?= MYG3NwKBkWh? M{jUVmROW09? MVfpcoR2[2W|IHHwc5B1d3Orcx?= MkDnNlI5OjlyOUS=
L-540 M4XYd2Fxd3C2b4Ppd{BCe3OjeR?= NIXwPJgyNzVizszN NI\1SFE4OuLCiXi= MliySG1UVw>? NHLiRmxqdmS3Y3XzJIFxd3C2b4Ppdy=> M2jK[lIzQDJ7MEm0
U251-MG M4HObGZ2dmO2aX;uJGF{e2G7 M1vafVEhyrWP MUKwMVE3KGh? NFvMO4ZqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? M2PVRlIzODJ5Nkmx
U87-MG NH[1bIZHfW6ldHnvckBCe3OjeR?= NI[3ZpAyKML3TR?= Mof4NE0yPiCq NX\JVJJ7cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MXKyNlAzPzZ7MR?=
4C8 M2jJOGZ2dmO2aX;uJGF{e2G7 NXjJZZdUOSEEtV2= M3;STFAuOTZiaB?= M3ziOYlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? MmXONlIxOjd4OUG=
U251-MG NUHOO3loT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWKxM|ExKML3TR?= NX7P[3c2OjRxNEivO|IhcA>? MoHPbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> NUS5Z2VSOjJyMke2PVE>
U87-MG MkXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[xM|ExKML3TR?= M3L0XFI1NzR6L{eyJIg> MVfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MViyNlAzPzZ7MR?=
4C8 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK4cpkyNzFyINM1US=> NGPtVIMzPC92OD:3NkBp M{jTZolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NH[w[I4zOjB{N{[5NS=>
U266 M2TUUWFxd3C2b4Ppd{BCe3OjeR?= NX3XPIs{OC53LUKg{txO NHvROGQ1QC95MjDo M2[wT4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NGHOTIozOTF4NEWxOy=>
Kms.11 NV3L[4I5SXCxcITvd4l{KEG|c3H5 NHzIOHMxNjVvMjFOwG0> NU\s[md2PDhxN{KgbC=> NV31R3N6cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NV:4eWoxOjFzNkS1NVc>
8226 NFrnfY1CeG:ydH;zbZMhSXO|YYm= NYOxcWIyOC53LUKg{txO MXq0PE84OiCq NELzTppqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Ml3iNlEyPjR3MUe=

... 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]
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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]
+ 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:
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
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

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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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID