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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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 MUXGeY5kfGmxbjDBd5NigQ>? MVe1JO69VQ>? MYC0PEBp NIXsbmlFVVOR NEfh[4NjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MWCyOVk2PDl5NB?=
LoVo  NH7vfFlHfW6ldHnvckBCe3OjeR?= Mnu3OUDPxE1? M{jycVQ5KGh? NUTNT2o3TE2VTx?= NGnNWYpjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MYGyOVk2PDl5NB?=
HN5 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV21TI5rPzJiaB?= NHvj[2hGSzVyPUOuPFEhyrFiMT65PUDPxE1? NVznOnlDOjV6MUCwNVA>
Cal33 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr3Tnk4OiCq Ml\YSWM2OD1|LkO3JOKyKDBwN{Wg{txO NUPLTI1[OjV6MUCwNVA>
UM-22B MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHFSJZxPzJiaB?= M1jvTGVEPTB;Mj62OkDDuSByLkK0JO69VQ>? NYD5bWxXOjV6MUCwNVA>
686LN M2TrcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDhSWJUPzJiaB?= NYDxNYFpTUN3ME2yMlA2KMLzIEGuN|Mh|ryP Mk\JNlU5OTByMUC=
UM SCC-1 NXzRPJJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO3NkBp MXzFR|UxRTFwNkegxtEhOC52MjFOwG0> NVjjdGpxOjV6MUCwNVA>
UM-22A NXjpOWZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rxTFczKGh? NInMOIpGSzVyPUGuN|IhyrFiMD6zPUDPxE1? NWiweXhQOjV6MUCwNVA>
OSC19 NGHkbIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX64dZVXPzJiaB?= M3rocGVEPTB;MT6yOkDDuSByLkKwJO69VQ>? MW[yOVgyODBzMB?=
PCI-52 M321TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK3NkBp NGC2UG1GSzVyPUGuNFAhyrFiMD6wPUDPxE1? MUiyOVgyODBzMB?=
PCI-15B NV7DOY1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3lO|IhcA>? M3PnXmVEPTB;MD65PUDDuSBzLke0JO69VQ>? NVLD[oJoOjV6MUCwNVA>
UMSCC-1 NWnrVpVxTnWwY4Tpc44hSXO|YYm= MUWwMlAxODVvMT62JO69VQ>? NY\ySHVGOjRiaB?= MWXhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnHkNlU5OTByMUC=
Cal33 NGnrcppHfW6ldHnvckBCe3OjeR?= Ml7GNE4xODB3LUOuPEDPxE1? Mm[wNlQhcA>? M1;kUIFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkPhNlU5OTByMUC=
HH5 M4frUmZ2dmO2aX;uJGF{e2G7 NFvOdocxNjByMEWtN{45KM7:TR?= NVLxV4lvOjRiaB?= NYrWXmFu[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4TwXVI2QDFyMEGw
UM-22A M4OyRWZ2dmO2aX;uJGF{e2G7 MnzNNE4xODB3LUGuOkDPxE1? MX:yOEBp Mn63ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlzUNlU5OTByMUC=
A1847 NYftWWpQTnWwY4Tpc44hSXO|YYm= M3vWRVAvODVvMUCg{txO NHPaVogzPCCq NYHLXmF2TE2VT9Mg NXjjVZhHemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NF\wS2wzPTZ2NkCxOS=>
OVCAR-5 M37BbGZ2dmO2aX;uJGF{e2G7 NUfWbpBDOC5yNT2xNEDPxE1? NFO1cpgzPCCq NGKyfGxFVVORwrC= NIK0O5hz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M{LjWlI2PjR4MEG1
OVCAR-8 MnjFSpVv[3Srb36gRZN{[Xl? MnfZNE4xPS1zMDFOwG0> M{T3O|I1KGh? M3XYOGROW00EoB?= NFnMfmdz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NHTiTmozPTZ2NkCxOS=>
MOVCAR-5447 MVHGeY5kfGmxbjDBd5NigQ>? NVriPJk5OC5yNT2xNEDPxE1? Mn7DNlQhcA>? MUfEUXNQyqB? M4PCNJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NUWyXIx5OjV4NE[wNVU>
MOVCAR-5009 NXnzXos{TnWwY4Tpc44hSXO|YYm= NGHidVExNjB3LUGwJO69VQ>? MojDNlQhcA>? NIX2cGdFVVORwrC= NH70S21z\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M4HCcVI2PjR4MEG1
A1847 M1nQXWNmdGxiVnnhZoltcXS7IFHzd4F6 NHrBdokxNjB3LUGwJO69VQ>? M3rSfFczKGh? NXTmUJJiTE2VTx?= NFnkellz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NXyw[|EzOjV4NE[wNVU>
OVCAR-5 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHrRTlMxNjB3LUGwJO69VQ>? MoXvO|IhcA>? Mnf3SG1UVw>? MVvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MVyyOVY1PjBzNR?=
OVCAR-8  MnvoR4VtdCCYaXHibYxqfHliQYPzZZk> NGXCNXMxNjB3LUGwJO69VQ>? MnvOO|IhcA>? M{TVOGROW09? MnvmdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NWqwNWRSOjV4NE[wNVU>
OVCAR-5  NWDaOnVUSXCxcITvd4l{KEG|c3H5 NXLYUIlEOC53L{GvOUDPxE1? M2XEfVQ5KGh? NGT0SmhFVVOR NFzHRXlqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u NHzCbZozPTZ2NkCxOS=>
OVCAR-8  MWLBdI9xfG:|aYOgRZN{[Xl? Mkf4NE42NzFxNTFOwG0> NXjQUo1lPDhiaB?= MnuzSG1UVw>? NWLYU2FpcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M2L6N|I2PjR4MEG1
AKRSL NIXxWpZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2jhZ|czKGh? MY\JR|Ux97zgMUCg{txO MoW1NlU2ODR4M{W=
PALJDL MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWHlWnJnPzJiaB?= NUm2[npPUUN3ME2yMlQh|ryP NE\LPWMzPTVyNE[zOS=>
MO4 MkDjSpVv[3Srb36gRZN{[Xl? MYSwMlUwOS93IN88US=> M3X3SlYhcA>? NXS3TW9tcW6qaXLpeJMhWC2VVFHUN{BmgHC{ZYPzbY9vyqB? MWqyOVE1QTV|NR?=
DU145  NEDvR5VHfW6ldHnvckBCe3OjeR?= M{\yTVAuOjByIH7N MkO3NUBpyqB? NE\0fYJ{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n MkfiNlQ2Pzd7NEK=
DU145  NX7Cc3FPTnWwY4Tpc44hSXO|YYm= MnnRPFAxKG6P NEHaeoc4OiCq MkXKd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 NXjqNXJ[OjR3N{e5OFI>
CWR22Rv1 MYDGeY5kfGmxbjDBd5NigQ>? NWDaWYg2QDByIH7N MVG3NkBp NXLIOpR6e3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 NYnjfo1lOjR3N{e5OFI>
N592 M1PWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIC5[FlKSzVyPUCuPFQh|ryP MnvRNlQyPTh5MEG=
H82 NH2xdGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Ky[2lEPTB;MT6zO{DPxE1? MUKyOFE2QDdyMR?=
GLC4 NY[2coRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnvTWM2OD1zLke5JO69VQ>? MWSyOFE2QDdyMR?=
H526 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33DWGlEPTB;Mz6wPEDPxE1? MWqyOFE2QDdyMR?=
H1173 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJwM{mg{txO M2r2bFI1OTV6N{Cx
DMS114 NIXUd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLwTWM2OD1yLkezJO69VQ>? MXGyOFE2QDdyMR?=
NCI-N592 NHjYOFdHfW6ldHnvckBCe3OjeR?= NEDDboIxNjNxMT:zJO69VQ>? MUCyOEBp NGTwWWNqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? M{XuXFI1OTV6N{Cx
GLC4 MlTKSpVv[3Srb36gRZN{[Xl? MnPlNE4{NzFxMzFOwG0> M2jNUlI1KGh? NVPuNlJncW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M1HhbVI1OTV6N{Cx
NCI-H82 M4T6dGZ2dmO2aX;uJGF{e2G7 NUfuOHFrOC5|L{GvN{DPxE1? NEnCV2IzPCCq MUjpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NUPKOnFKOjRzNUi3NFE>
NCI-N592 MmLFRZBweHSxc3nzJGF{e2G7 MoPONE4{NzFxMzFOwG0> M17OeVQ5KGh? MYfpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NHTzV|kzPDF3OEewNS=>
GLC4 MmXaRZBweHSxc3nzJGF{e2G7 M1PKXVAvOy9zL{Og{txO MoK2OFghcA>? MVLpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ M3qyUVI1OTV6N{Cx
NCI-H82 NITGb3VCeG:ydH;zbZMhSXO|YYm= NFvSOVExNjNxMT:zJO69VQ>? M2PKZ|Q5KGh? MnrrbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MXuyOFE2QDdyMR?=
CWR22Rv1  M4ntVmFxd3C2b4Ppd{BCe3OjeR?= NHPhWFRKSzVyPUCuOFgzKM7:TR?= MlvmNlM6PDJyOUW=
CWR22Pc NYfEeYRNSXCxcITvd4l{KEG|c3H5 MkfETWM2OD1yLkSzPEDPxE1? Ml3oNlM6PDJyOUW=
PC-3 M4PzOGFxd3C2b4Ppd{BCe3OjeR?= MoC2TWM2OD1zLke1OUDPxE1? MXuyN|k1OjB7NR?=
DU145 NETieJFCeG:ydH;zbZMhSXO|YYm= MnLNTWM2OD1|LkWxO{DPxE1? M3XMVlI{QTR{MEm1
RC165N NITPcY5CeG:ydH;zbZMhSXO|YYm= MUjJR|UxRTJwMEizJO69VQ>? NXzudnhVOjN7NEKwPVU>
ARPE19 NUfoZnBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\EUXNQ MXTJR|UxRTJ2LkO4JO69VQ>? NXL1T|dtOjN3M{G5NlE>
HEK293 NGDDdG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPEUXNQ M3XybmlEPTB;OD62O{DPxE1? MWGyN|U{OTl{MR?=
KCNR NEnDc5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG1SG1UVw>? NYT2S2NVUUN3ME2wMlQ3KM7:TR?= NFrUU2QzOzV|MUmyNS=>
SY5Y M13OTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfFSoFFVVOR NY\QXGVHUUN3ME2wMlM3KM7:TR?= MoexNlM2OzF7MkG=
BE2 M4qzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHEUXNQ NWW0c3hyUUN3ME2wMlcyKM7:TR?= MV:yN|U{OTl{MR?=
AS NVLhdpRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLGSG1UVw>? M{myPGlEPTB;MT61N{DPxE1? M3LXUlI{PTNzOUKx
NGP M2HRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK5XJVjTE2VTx?= MVrJR|UxRTBwNU[g{txO NIXKcYgzOzV|MUmyNS=>
IMR32 MlPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz6U|hFVVOR NEL1Ro1KSzVyPUCuOlYh|ryP MkS3NlM2OzF7MkG=
LAN5 NHPDeZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHEUXNQ NIPDenZKSzVyPUGuNFQh|ryP NUHyVItCOjN3M{G5NlE>
RH18 M1nUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTiTpJtTE2VTx?= MofNTWM2OD1zLkSyJO69VQ>? MX[yN|U{OTl{MR?=
RH30 NUXufnVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDISG1UVw>? MYTJR|UxRTFwMkWg{txO NYLTfIZDOjN3M{G5NlE>
RH17 NEPBVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHyXXNFVVOR MVLJR|UxRTJwNUGg{txO M{jHelI{PTNzOUKx
RH28 NHrwbXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;ie2ROW09? NYr1OpVnUUN3ME20MlI5KM7:TR?= MnvNNlM2OzF7MkG=
RH36 NI\GepRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\EUXNQ MUHJR|UxRTVwM{eg{txO NXHBUGRiOjN3M{G5NlE>
RH41 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvF[lVFVVOR NFXldVRKSzVyPUCuOFgh|ryP MUCyN|U{OTl{MR?=
RD M2e2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH0SG1UVw>? MWnJR|UxRTRwM{Kg{txO NFzmVmkzOzV|MUmyNS=>
TC32 NXPDZosyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULtdZdzTE2VTx?= M2izO2lEPTB;Mz64OUDPxE1? NX\POJB{OjN3M{G5NlE>
TC71 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPEUXNQ M{PwcmlEPTB;ND6zN{DPxE1? NGLRdmQzOzV|MUmyNS=>
KCNR M1fX[WFxd3C2b4Ppd{BCe3OjeR?= MWCwMlUwOS5yL{KuOUDPxE1? M{PFclI1KGh? NH;ybHhFVVOR NWWzdY5ncW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MnS3NlM2OzF7MkG=
SY5Y NHnFcldCeG:ydH;zbZMhSXO|YYm= NEOwTlUxNjVxMT6wM|IvPSEQvF2= MWCyOEBp M2PXNGROW09? NYjzUll7cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MYWyN|U{OTl{MR?=
Rh18 NX;i[YNrSXCxcITvd4l{KEG|c3H5 NF;yeIoxNjVxMT6wM|IvPSEQvF2= NFLZdpMzPCCq NIjk[49FVVOR NWTDcmtJcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MlXmNlM2OzF7MkG=
TC32 MX3BdI9xfG:|aYOgRZN{[Xl? NVf3Zmt3OC53L{GuNE8zNjVizszN MUSyOEBp NIrE[49FVVOR M4CzW4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= M4XCbFI{PTNzOUKx
KCNR M1jNVmZ2dmO2aX;uJGF{e2G7 MoXSNE42NzFwMD:yMlUwPSEQvF2= MVqyOEBp NWC1TXlLTE2VTx?= MnzpbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= M1TrVVI{PTNzOUKx
SY5Y NX:zSHczTnWwY4Tpc44hSXO|YYm= M1LTWlAvPS9zLkCvNk42NzVizszN NXzQcY1IOjRiaB?= M{fLVmROW09? MknFbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= M{Xp[|I{PTNzOUKx
Rh18 Ml;ESpVv[3Srb36gRZN{[Xl? MUKwMlUwOS5yL{KuOU82KM7:TR?= NUfqd4RMOjRiaB?= NUHVXXF1TE2VTx?= MWLpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NGTFfoUzOzV|MUmyNS=>
TC32 NUGwN4ZITnWwY4Tpc44hSXO|YYm= MWKwMlUwOS5yL{KuOU82KM7:TR?= NH7BXGwzPCCq NWK3dZBbTE2VTx?= MXzpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NIi0UHYzOzV|MUmyNS=>
TPC-1 NYT0TlVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXixJOK2VQ>? M2TzTlAuPCCm NETJVYNFVVOR M17qe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? MoK2NlMxPTZ2OUm=
MZ-CRC1  MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[xJOK2VQ>? M2LreFAuPSCm M2nlVGROW09? NV\UV3ZvcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NGDNRo8zOzB3NkS5PS=>
TT  M1fmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;UelEhyrWP M{LTV|AuPCCm Mof5SG1UVw>? NELQOIhqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MmHoNlMxPTZ2OUm=
TPC-1 MYHGeY5kfGmxbjDBd5NigQ>? NYf0SnhtOSEEtV2= NFWzRnY4OiCq NHnTOphFVVOR M{\rT4lv\HWlZYOgS|Eh[myxY3vh[4U> M3zLXFI{ODV4NEm5
MZ-CRC1  MUPGeY5kfGmxbjDBd5NigQ>? NHvaUoYyKML3TR?= NVjYd4VbPzJiaB?= MXfEUXNQ NX\CRWRpcW6mdXPld{BIOSCkbH;jb4Fo\Q>? M2fMOVI{ODV4NEm5
TT  MnnaSpVv[3Srb36gRZN{[Xl? NFnyd|gyKML3TR?= M2j6TVczKGh? MXHEUXNQ MX\pcoR2[2W|IFexJIJtd2OtYXfl MlHDNlMxPTZ2OUm=
MZ-CRC1  MVfBdI9xfG:|aYOgRZN{[Xl? NFLKVXIyKML3TR?= M2jXTVQ5KGh? NUW3c3NITE2VTx?= NWPoOplwcW6mdXPld{BieG:ydH;zbZM> MVSyN|A2PjR7OR?=
TT  M{PiXmFxd3C2b4Ppd{BCe3OjeR?= NFjXZZQyKML3TR?= MknFOFghcA>? MY\EUXNQ M3PWT4lv\HWlZYOgZZBweHSxc3nz NVnEZWo{OjNyNU[0PVk>
HD-LM2 NVLUPFFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3VXZM4OuLCiXi= M4r5Z2ROW09? MlvkTWM2OD15Lki0OEDPxE1? NFLLcGMzOjh{OUC5OC=>
L-428 NF;PNVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37XUFcz6oDLaB?= M37RPGROW09? M2nhWmlEPTB;Nz65OFch|ryP NYW4[ZJ6OjJ6MkmwPVQ>
KM-H2 NXvJcnZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Htblcz6oDLaB?= Ml3wSG1UVw>? NFS5fZNKSzVyPUGuN|A5KM7:TR?= MYWyNlgzQTB7NB?=
L-540 MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfRV4ZOPzMkgJno MnX3SG1UVw>? NVvG[Wx[UUN3ME24MlIyPiEQvF2= NInu[3czOjh{OUC5OC=>
HD-LM2 NXyydGhbTnWwY4Tpc44hSXO|YYm= M{fzclAvOS9yLkWvNU82KM7:TR?= M3vTUVcz6oDLaB?= MV\EUXNQ NVr5PXJ[cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NV7DZ3JsOjJ6MkmwPVQ>
L-428 NYraZYM1TnWwY4Tpc44hSXO|YYm= NH;vdHUxNjFxMD61M|EwPSEQvF2= NVPZOWRUPzMkgJno NH[ycmZFVVOR M3zlfYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MmGxNlI5OjlyOUS=
KM-H2 Mn\BSpVv[3Srb36gRZN{[Xl? NXzuT2xTOC5zL{CuOU8yNzVizszN MkLqO|LjiImq NIC1VWVFVVOR NV22Rmg3cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MUmyNlgzQTB7NB?=
L-540 NFzSNVRHfW6ldHnvckBCe3OjeR?= MoTLNE4yNzBwNT:xM|Uh|ryP NV3XTYxPPzMkgJno MnzXSG1UVw>? NGX2cFRqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NF3jWHkzOjh{OUC5OC=>
HD-LM2 MkX2RZBweHSxc3nzJGF{e2G7 MWKxM|Uh|ryP NEXmUpI4OuLCiXi= MXTEUXNQ NEPYcnVqdmS3Y3XzJIFxd3C2b4Ppdy=> MX:yNlgzQTB7NB?=
L-428 MUXBdI9xfG:|aYOgRZN{[Xl? MVqxM|Uh|ryP NHm1c|U4OuLCiXi= NWjkbXdqTE2VTx?= M1;odolv\HWlZYOgZZBweHSxc3nz M{Loe|IzQDJ7MEm0
KM-H2 NH3KWZJCeG:ydH;zbZMhSXO|YYm= MkToNU82KM7:TR?= Mm\5O|LjiImq M2DJVGROW09? NVLTfXJDcW6mdXPld{BieG:ydH;zbZM> M4r3bFIzQDJ7MEm0
L-540 NYrsRZh2SXCxcITvd4l{KEG|c3H5 M2GyRlEwPSEQvF2= MVe3NwKBkWh? M4PseWROW09? NU[wd2NjcW6mdXPld{BieG:ydH;zbZM> M4S4NlIzQDJ7MEm0
U251-MG MV;GeY5kfGmxbjDBd5NigQ>? M4H4VlEhyrWP NV7JTZY1OC1zNjDo MlHGbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MnrGNlIxOjd4OUG=
U87-MG MVHGeY5kfGmxbjDBd5NigQ>? MmL5NUDDvU1? M2X6fFAuOTZiaB?= NIfkbHhqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NVPKXYI4OjJyMke2PVE>
4C8 NGLaOWpHfW6ldHnvckBCe3OjeR?= M1zISlEhyrWP M4rzRVAuOTZiaB?= NFP3NJhqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? M2q2ZlIzODJ5Nkmx
U251-MG NGjUNFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2xM|ExKML3TR?= M{HPblI1NzR6L{eyJIg> NUC3NHMycW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MYqyNlAzPzZ7MR?=
U87-MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHpNU8yOCEEtV2= NUO1UVdUOjRxNEivO|IhcA>? M2fBR4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO M{D3blIzODJ5Nkmx
4C8 NFnvenBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPxNU8yOCEEtV2= MXuyOE81QC95MjDo NF3MW2NqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? M3P4ZVIzODJ5Nkmx
U266 MnrTRZBweHSxc3nzJGF{e2G7 MUmwMlUuOiEQvF2= NFzSPW41QC95MjDo MX7pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnHHNlEyPjR3MUe=
Kms.11 NVTBTXFmSXCxcITvd4l{KEG|c3H5 NH65WFYxNjVvMjFOwG0> NVnLVVJ{PDhxN{KgbC=> NIizN41qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MljZNlEyPjR3MUe=
8226 MYfBdI9xfG:|aYOgRZN{[Xl? M4DOW|AvPS1{IN88US=> MYC0PE84OiCq MWLpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NW\tO3RsOjFzNkS1NVc>

... 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]
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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]
+ 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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID