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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3 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.

    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 NEXyOpdHfW6ldHnvckBCe3OjeR?= MUG1JO69VQ>? NYHkXotzPDhiaB?= MUTEUXNQ MYricI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= Mnz0NlU6PTR7N{S=
LoVo  NUiwd2VTTnWwY4Tpc44hSXO|YYm= MYC1JO69VQ>? M2ftU|Q5KGh? M2XWSmROW09? MmTlZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n M1HVfVI2QTV2OUe0
HN5 NHTOdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfEO|IhcA>? MWrFR|UxRTNwOEGgxtEhOS57OTFOwG0> NGCyW5UzPThzMECxNC=>
Cal33 M{nhZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXu3NkBp MoDNSWM2OD1|LkO3JOKyKDBwN{Wg{txO NH;TPGgzPThzMECxNC=>
UM-22B NIKwN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PaSVczKGh? MnzRSWM2OD1{Lk[2JOKyKDBwMkSg{txO NWO1WGtOOjV6MUCwNVA>
686LN M1zo[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK3NkBp NHTybWJGSzVyPUKuNFUhyrFiMT6zN{DPxE1? M4K0d|I2QDFyMEGw
UM SCC-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWriVGN3PzJiaB?= MV\FR|UxRTFwNkegxtEhOC52MjFOwG0> MmnFNlU5OTByMUC=
UM-22A MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLZO|IhcA>? MVLFR|UxRTFwM{KgxtEhOC5|OTFOwG0> MXGyOVgyODBzMB?=
OSC19 NX7tOnlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\me|czKGh? M3LW[2VEPTB;MT6yOkDDuSByLkKwJO69VQ>? NXeyZo9HOjV6MUCwNVA>
PCI-52 NX3HO|BPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDJO|IhcA>? NH;uNJlGSzVyPUGuNFAhyrFiMD6wPUDPxE1? NW\zRndFOjV6MUCwNVA>
PCI-15B Mm\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\kRVczKGh? MnXDSWM2OD1yLkm5JOKyKDFwN{Sg{txO NHP0c5gzPThzMECxNC=>
UMSCC-1 NHe1OIlHfW6ldHnvckBCe3OjeR?= M4fVdlAvODByNT2xMlYh|ryP MmPRNlQhcA>? MVfhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NUO4ZoVkOjV6MUCwNVA>
Cal33 MYXGeY5kfGmxbjDBd5NigQ>? NYTGbpFjOC5yMEC1MVMvQCEQvF2= NXXPcHR1OjRiaB?= NUXsUGU6[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFza[pAzPThzMECxNC=>
HH5 NXq1OGhjTnWwY4Tpc44hSXO|YYm= M2LsSlAvODByNT2zMlgh|ryP M4qw[|I1KGh? M{nHPYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHvJSVIzPThzMECxNC=>
UM-22A MUPGeY5kfGmxbjDBd5NigQ>? M{fzXlAvODByNT2xMlYh|ryP NILJfpkzPCCq NVzTVIdz[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXnONlhtOjV6MUCwNVA>
A1847 MnjzSpVv[3Srb36gRZN{[Xl? NFP0eWgxNjB3LUGwJO69VQ>? M2fLWlI1KGh? MVfEUXNQyqB? NUfkTlZ3emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NXftdFRpOjV4NE[wNVU>
OVCAR-5 NHjLSo1HfW6ldHnvckBCe3OjeR?= MU[wMlA2NTFyIN88US=> MkPUNlQhcA>? MVnEUXNQyqB? NWn4XIhyemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NU[1XWFSOjV4NE[wNVU>
OVCAR-8 MVvGeY5kfGmxbjDBd5NigQ>? NXLENY5lOC5yNT2xNEDPxE1? NYfJPHE5OjRiaB?= MkC2SG1UV8Li NUixSZJwemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MUCyOVY1PjBzNR?=
MOVCAR-5447 NWHLU4x7TnWwY4Tpc44hSXO|YYm= Mn;CNE4xPS1zMDFOwG0> NEDaOVYzPCCq MWLEUXNQyqB? MV;y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MnHFNlU3PDZyMUW=
MOVCAR-5009 NXjnTZpVTnWwY4Tpc44hSXO|YYm= M2rT[VAvODVvMUCg{txO MkC1NlQhcA>? M{LRU2ROW00EoB?= NHTFN2dz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NVi4eGJDOjV4NE[wNVU>
A1847 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NITZOlYxNjB3LUGwJO69VQ>? NHrGblM4OiCq MlGzSG1UVw>? M1LETJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MYGyOVY1PjBzNR?=
OVCAR-5 Mo\pR4VtdCCYaXHibYxqfHliQYPzZZk> MYKwMlA2NTFyIN88US=> M3:ydVczKGh? NHfY[HBFVVOR MnS0doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MWCyOVY1PjBzNR?=
OVCAR-8  NXvpTXFTS2WubDDWbYFjcWyrdImgRZN{[Xl? NGTiN5QxNjB3LUGwJO69VQ>? NF[5O4Y4OiCq NELIUmFFVVOR MVPy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= NWXsSY5YOjV4NE[wNVU>
OVCAR-5  MUTBdI9xfG:|aYOgRZN{[Xl? MnnTNE42NzFxNTFOwG0> MnzNOFghcA>? M{Tkb2ROW09? NEfzO2lqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u Mm\GNlU3PDZyMUW=
OVCAR-8  MWnBdI9xfG:|aYOgRZN{[Xl? M1qwbVAvPS9zL{Wg{txO NXi4UJg3PDhiaB?= M4TYXWROW09? MVjpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w NGjJbmYzPTZ2NkCxOS=>
AKRSL MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYHhN2Z{PzJiaB?= MVXJR|Ux97zgMUCg{txO MVOyOVUxPDZ|NR?=
PALJDL NHLvdmpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1TJUlczKGh? NF6wb|BKSzVyPUKuOEDPxE1? MoWwNlU2ODR4M{W=
MO4 NULDRXdFTnWwY4Tpc44hSXO|YYm= NFe0XGcxNjVxMT:1JO69VQ>? MkHQOkBp M1Xo[YlvcGmkaYTzJHAuW1SDVEOg[ZhxemW|c3nvcuKh M1nzfVI2OTR7NUO1
DU145  NYPuSJduTnWwY4Tpc44hSXO|YYm= NVX2eY5XOC1{MECgcm0> M3jYOVEhcMLi M1HR[pN2eHC{ZYPz[ZMhUUxvNj3hZ5RqfmG2ZXSgV5RifDNiYX7kJGVTUzFxMjDzbYdv[Wyrbne= M1jsXFI1PTd5OUSy
DU145  NWnGUWpCTnWwY4Tpc44hSXO|YYm= MlvrPFAxKG6P Mn7xO|IhcA>? NX;3[Idle3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 NE\vN40zPDV5N{m0Ni=>
CWR22Rv1 NHztZXJHfW6ldHnvckBCe3OjeR?= MVu4NFAhdk1? NGLBeYo4OiCq Mo\Od5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 MVOyOFU4Pzl2Mh?=
N592 NUfhV3dxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7KTWM2OD1yLki0JO69VQ>? NHXDPJozPDF3OEewNS=>
H82 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPMTWM2OD1zLkO3JO69VQ>? NETiOVUzPDF3OEewNS=>
GLC4 NF:xeFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnkTWM2OD1zLke5JO69VQ>? NHKwfVUzPDF3OEewNS=>
H526 Mm\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDDTWM2OD1|LkC4JO69VQ>? NVH0OldVOjRzNUi3NFE>
H1173 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXpUohyUUN3ME2yMlM6KM7:TR?= MmnZNlQyPTh5MEG=
DMS114 NXfDPYU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni5TWM2OD1yLkezJO69VQ>? M4DhNVI1OTV6N{Cx
NCI-N592 NIXQdlhHfW6ldHnvckBCe3OjeR?= NVrqV5prOC5|L{GvN{DPxE1? MkjvNlQhcA>? NWj1epl5cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NHztPVEzPDF3OEewNS=>
GLC4 NIC2SldHfW6ldHnvckBCe3OjeR?= NW\ZN5V2OC5|L{GvN{DPxE1? Mm[xNlQhcA>? NWXjUG5RcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NVjjdnVGOjRzNUi3NFE>
NCI-H82 MkD6SpVv[3Srb36gRZN{[Xl? MoDZNE4{NzFxMzFOwG0> NEXFfVczPCCq M17nTolv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MYeyOFE2QDdyMR?=
NCI-N592 M2jkNmFxd3C2b4Ppd{BCe3OjeR?= NYTuNWI5OC5|L{GvN{DPxE1? NELYW3M1QCCq NW\j[XR1cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NYWyeYFQOjRzNUi3NFE>
GLC4 NYLFXlhNSXCxcITvd4l{KEG|c3H5 MUKwMlMwOS9|IN88US=> M4XGdFQ5KGh? NHfSfnJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NGLERmQzPDF3OEewNS=>
NCI-H82 NVrpbFBLSXCxcITvd4l{KEG|c3H5 MV6wMlMwOS9|IN88US=> NEDhR2c1QCCq NWXHfXlRcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MYWyOFE2QDdyMR?=
CWR22Rv1  MWrBdI9xfG:|aYOgRZN{[Xl? M37NSmlEPTB;MD60PFIh|ryP NIW1ZYEzOzl2MkC5OS=>
CWR22Pc M2nON2Fxd3C2b4Ppd{BCe3OjeR?= MWfJR|UxRTBwNEO4JO69VQ>? MX[yN|k1OjB7NR?=
PC-3 NVHOR4w6SXCxcITvd4l{KEG|c3H5 NYewdI0{UUN3ME2xMlc2PSEQvF2= MXWyN|k1OjB7NR?=
DU145 M3;HbGFxd3C2b4Ppd{BCe3OjeR?= NFe2OINKSzVyPUOuOVE4KM7:TR?= NXfBT3Z[OjN7NEKwPVU>
RC165N NIH2fXpCeG:ydH;zbZMhSXO|YYm= MWnJR|UxRTJwMEizJO69VQ>? M1y4ZlI{QTR{MEm1
ARPE19 M1HqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O4WmROW09? MVvJR|UxRTJ2LkO4JO69VQ>? NEPVcoQzOzV|MUmyNS=>
HEK293 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\BZ5VFVVOR MVPJR|UxRThwNkeg{txO NH7OZmQzOzV|MUmyNS=>
KCNR MoDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jybWROW09? NIPjc5pKSzVyPUCuOFYh|ryP MXyyN|U{OTl{MR?=
SY5Y MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrEUXNQ MoTlTWM2OD1yLkO2JO69VQ>? Mn;rNlM2OzF7MkG=
BE2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPBO|VUTE2VTx?= M1O1[GlEPTB;MD63NUDPxE1? NILZSHMzOzV|MUmyNS=>
AS NW\Qd2VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXryW45STE2VTx?= M3O0ZWlEPTB;MT61N{DPxE1? MlLyNlM2OzF7MkG=
NGP NX\6Z2JpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmxSG1UVw>? MYnJR|UxRTBwNU[g{txO NGHqeHUzOzV|MUmyNS=>
IMR32 M3PpTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\OSG1UVw>? NFy0[phKSzVyPUCuOlYh|ryP NGLiVogzOzV|MUmyNS=>
LAN5 MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfDTm9FVVOR MnTVTWM2OD1zLkC0JO69VQ>? MUSyN|U{OTl{MR?=
RH18 M1zVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrRSG1UVw>? MUPJR|UxRTFwNEKg{txO NWXY[WNqOjN3M{G5NlE>
RH30 M3\BeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PIO2ROW09? MVXJR|UxRTFwMkWg{txO MmDaNlM2OzF7MkG=
RH17 M2P0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvhdVlMTE2VTx?= MVvJR|UxRTJwNUGg{txO Ml7ONlM2OzF7MkG=
RH28 M{PlU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4OzfmROW09? MX3JR|UxRTRwMkig{txO NFj1NWYzOzV|MUmyNS=>
RH36 M3\rUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnRSG1UVw>? NVLacnJUUUN3ME21MlM4KM7:TR?= MX6yN|U{OTl{MR?=
RH41 NVHZWm9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HJZ2ROW09? NHX6XVdKSzVyPUCuOFgh|ryP NYHtVIlIOjN3M{G5NlE>
RD MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXP[G9FVVOR M1TnWWlEPTB;ND6zNkDPxE1? NUPwc|QzOjN3M{G5NlE>
TC32 NGXPUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\UbolFVVOR NWHsSWZwUUN3ME2zMlg2KM7:TR?= Mne1NlM2OzF7MkG=
TC71 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jHbmROW09? MXjJR|UxRTRwM{Og{txO MkK4NlM2OzF7MkG=
KCNR MWjBdI9xfG:|aYOgRZN{[Xl? NIHjd4oxNjVxMT6wM|IvPSEQvF2= MV6yOEBp M2fOO2ROW09? NHzTTppqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MoTsNlM2OzF7MkG=
SY5Y M1jJ[GFxd3C2b4Ppd{BCe3OjeR?= M1flWVAvPS9zLkCvNk42KM7:TR?= NX[zZYJ2OjRiaB?= M{X5N2ROW09? MmnSbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NUWwO5U4OjN3M{G5NlE>
Rh18 NXTlNlNYSXCxcITvd4l{KEG|c3H5 NG\BVGkxNjVxMT6wM|IvPSEQvF2= NFmwVIczPCCq MYTEUXNQ M4S1T4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NXrFOlhMOjN3M{G5NlE>
TC32 MVjBdI9xfG:|aYOgRZN{[Xl? MYWwMlUwOS5yL{KuOUDPxE1? M{\5WVI1KGh? NV;KfFllTE2VTx?= NYTtUopCcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NVrVS45mOjN3M{G5NlE>
KCNR M{i4[mZ2dmO2aX;uJGF{e2G7 NGTmdXMxNjVxMT6wM|IvPS93IN88US=> MUKyOEBp MojzSG1UVw>? MmrXbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NYnmfY9pOjN3M{G5NlE>
SY5Y MnPmSpVv[3Srb36gRZN{[Xl? NYj3U45qOC53L{GuNE8zNjVxNTFOwG0> Mn\ONlQhcA>? NH22eZRFVVOR MUDpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= M4SyflI{PTNzOUKx
Rh18 M4jwUmZ2dmO2aX;uJGF{e2G7 NW[1doZOOC53L{GuNE8zNjVxNTFOwG0> MXeyOEBp MmnBSG1UVw>? MnzlbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NVn5[o9TOjN3M{G5NlE>
TC32 MYrGeY5kfGmxbjDBd5NigQ>? MVmwMlUwOS5yL{KuOU82KM7:TR?= M1zGNFI1KGh? M1jvNmROW09? MkXMbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= Mn3LNlM2OzF7MkG=
TPC-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HrRlEhyrWP M17GelAuPCCm NVvRWWp5TE2VTx?= NEHPZoxqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAzKGRidILlZZRu\W62 NVrNUHNYOjNyNU[0PVk>
MZ-CRC1  NXLm[|U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIOySWIyKML3TR?= M1vZbVAuPSCm M2PjW2ROW09? NFvPXW5qdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MXyyN|A2PjR7OR?=
TT  NHvmNYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUn3bHpIOSEEtV2= MVmwMVQh\A>? M1XDSWROW09? NF\pXo1qdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 Mle0NlMxPTZ2OUm=
TPC-1 MlLWSpVv[3Srb36gRZN{[Xl? MVWxJOK2VQ>? MoeyO|IhcA>? MYHEUXNQ MWPpcoR2[2W|IFexJIJtd2OtYXfl MUCyN|A2PjR7OR?=
MZ-CRC1  M{P5emZ2dmO2aX;uJGF{e2G7 MYKxJOK2VQ>? MoS4O|IhcA>? NUX2cHlzTE2VTx?= NGK4THNqdmS3Y3XzJGcyKGKub3PrZYdm M2XX[lI{ODV4NEm5
TT  NFG3V|FHfW6ldHnvckBCe3OjeR?= MmrPNUDDvU1? NWPQVolsPzJiaB?= NXLIS5BWTE2VTx?= M2e4XYlv\HWlZYOgS|Eh[myxY3vh[4U> NYf4b|NPOjNyNU[0PVk>
MZ-CRC1  NYnXfYw6SXCxcITvd4l{KEG|c3H5 MnnjNUDDvU1? NX;3SHF2PDhiaB?= MmqzSG1UVw>? NYWxXZZ7cW6mdXPld{BieG:ydH;zbZM> NFWwc|czOzB3NkS5PS=>
TT  NEflboJCeG:ydH;zbZMhSXO|YYm= M4LZUVEhyrWP MV60PEBp NV3XeZU3TE2VTx?= Mli1bY5lfWOnczDhdI9xfG:|aYO= MXKyN|A2PjR7OR?=
HD-LM2 Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEexfWg4OuLCiXi= MmDCSG1UVw>? NHzGe5RKSzVyPUeuPFQ1KM7:TR?= NV\Kd3JYOjJ6MkmwPVQ>
L-428 MkTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm3O4lWPzMkgJno NVe4NmdWTE2VTx?= M1vidWlEPTB;Nz65OFch|ryP NWe2WWQ3OjJ6MkmwPVQ>
KM-H2 MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX23NwKBkWh? NEjXNGZFVVOR MU\JR|UxRTFwM{C4JO69VQ>? NHPoO2IzOjh{OUC5OC=>
L-540 NGXEV5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfxWY44OuLCiXi= NEXFdmNFVVOR M4D0bGlEPTB;OD6yNVYh|ryP MW[yNlgzQTB7NB?=
HD-LM2 M3\1O2Z2dmO2aX;uJGF{e2G7 M{Hzb|AvOS9yLkWvNU82KM7:TR?= NIruR|I4OuLCiXi= NHjUb|hFVVOR MVfpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MlPPNlI5OjlyOUS=
L-428 MnTzSpVv[3Srb36gRZN{[Xl? M{H4T|AvOS9yLkWvNU82KM7:TR?= MWC3NwKBkWh? NV7NZ4ZLTE2VTx?= M{HCS4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MW[yNlgzQTB7NB?=
KM-H2 M2niNGZ2dmO2aX;uJGF{e2G7 M4L2ZVAvOS9yLkWvNU82KM7:TR?= NHHUUYU4OuLCiXi= MXjEUXNQ MnW3bY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MlHGNlI5OjlyOUS=
L-540 NVjpdmlUTnWwY4Tpc44hSXO|YYm= NXXnZYFFOC5zL{CuOU8yNzVizszN NUG2c|NVPzMkgJno NHvuToZFVVOR M2e4fIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MneyNlI5OjlyOUS=
HD-LM2 MWXBdI9xfG:|aYOgRZN{[Xl? NHfHSIYyNzVizszN M133dFcz6oDLaB?= NVTQXWxvTE2VTx?= NITHcWxqdmS3Y3XzJIFxd3C2b4Ppdy=> M{nOTFIzQDJ7MEm0
L-428 M3XXTGFxd3C2b4Ppd{BCe3OjeR?= NHWwdmoyNzVizszN NEe2TW84OuLCiXi= NHryXIxFVVOR MXzpcoR2[2W|IHHwc5B1d3Orcx?= M2j2WVIzQDJ7MEm0
KM-H2 MVfBdI9xfG:|aYOgRZN{[Xl? M3T6PFEwPSEQvF2= M4myWVcz6oDLaB?= NHLaOFJFVVOR MmjObY5lfWOnczDhdI9xfG:|aYO= NHS3PFMzOjh{OUC5OC=>
L-540 NH;S[2RCeG:ydH;zbZMhSXO|YYm= NHnPRoQyNzVizszN Ml3vO|LjiImq NFjqdJFFVVOR MlK0bY5lfWOnczDhdI9xfG:|aYO= NWTNTnBPOjJ6MkmwPVQ>
U251-MG NIGwd5VHfW6ldHnvckBCe3OjeR?= NGC3R5kyKML3TR?= NInaWoMxNTF4IHi= M1nwdolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? Ml7pNlIxOjd4OUG=
U87-MG MlHaSpVv[3Srb36gRZN{[Xl? MWmxJOK2VQ>? NVjjPI04OC1zNjDo NV62[o1VcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MXyyNlAzPzZ7MR?=
4C8 MkHaSpVv[3Srb36gRZN{[Xl? MXKxJOK2VQ>? M1H4e|AuOTZiaB?= MXHpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> Mni1NlIxOjd4OUG=
U251-MG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\kNU8yOCEEtV2= NH\uVnQzPC92OD:3NkBp NXvMNlNYcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MWqyNlAzPzZ7MR?=
U87-MG MkWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlO4NU8yOCEEtV2= NV71dZBpOjRxNEivO|IhcA>? MYDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NGr6UZkzOjB{N{[5NS=>
4C8 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVqydWRIOS9zMDFCuW0> MnnJNlQwPDhxN{KgbC=> MYfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> Mlu1NlIxOjd4OUG=
U266 M1zT[mFxd3C2b4Ppd{BCe3OjeR?= MWSwMlUuOiEQvF2= NF3oeFg1QC95MjDo NIX1cZJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MoX1NlEyPjR3MUe=
Kms.11 NHXP[m5CeG:ydH;zbZMhSXO|YYm= NHnBcnIxNjVvMjFOwG0> NWWzcos2PDhxN{KgbC=> MX7pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MYmyNVE3PDVzNx?=
8226 NV\0WWs3SXCxcITvd4l{KEG|c3H5 NF6zfXExNjVvMjFOwG0> NVfuUINXPDhxN{KgbC=> NXTYfHZFcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MkDZNlEyPjR3MUe=

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
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