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 NGKzTW1HfW6ldHnvckBCe3OjeR?= MX:1JO69VQ>? MlvUOFghcA>? NYTBV3h1TE2VTx?= NEPsR5ljdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MWiyOVk2PDl5NB?=
LoVo  NIO5S5NHfW6ldHnvckBCe3OjeR?= MmDoOUDPxE1? NETSdFI1QCCq NXjsZlJPTE2VTx?= NHXPeXdjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MofXNlU6PTR7N{S=
HN5 MnzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrsbFNLPzJiaB?= Mn3TSWM2OD1|LkixJOKyKDFwOUmg{txO MoTYNlU5OTByMUC=
Cal33 NETtcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPMVocxPzJiaB?= NI\yZlBGSzVyPUOuN|chyrFiMD63OUDPxE1? NX;TTok6OjV6MUCwNVA>
UM-22B NVjiUWRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLLO|IhcA>? NXnEcm9XTUN3ME2yMlY3KMLzIECuNlQh|ryP NYPwdlAyOjV6MUCwNVA>
686LN M4LxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy3NkBp NVjQVpE5TUN3ME2yMlA2KMLzIEGuN|Mh|ryP MmPBNlU5OTByMUC=
UM SCC-1 NX2zdpVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLaO|IhcA>? M4TMfWVEPTB;MT62O{DDuSByLkSyJO69VQ>? MmXzNlU5OTByMUC=
UM-22A MnKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[3NkBp M1HxfmVEPTB;MT6zNkDDuSByLkO5JO69VQ>? MYCyOVgyODBzMB?=
OSC19 M1ewemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWexbIxDPzJiaB?= MYXFR|UxRTFwMk[gxtEhOC5{MDFOwG0> MkLFNlU5OTByMUC=
PCI-52 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjMO|IhcA>? Mo\5SWM2OD1zLkCwJOKyKDBwMEmg{txO M3TyfVI2QDFyMEGw
PCI-15B MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ftU|czKGh? MW\FR|UxRTBwOUmgxtEhOS55NDFOwG0> M2jqS|I2QDFyMEGw
UMSCC-1 MYPGeY5kfGmxbjDBd5NigQ>? NV\POlRXOC5yMEC1MVEvPiEQvF2= MYmyOEBp Mk\sZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX2yOVgyODBzMB?=
Cal33 M{DnV2Z2dmO2aX;uJGF{e2G7 NYLHNZlsOC5yMEC1MVMvQCEQvF2= NVfqSFI{OjRiaB?= NF72dJZi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXKyOVgyODBzMB?=
HH5 Ml7hSpVv[3Srb36gRZN{[Xl? NH3KUlQxNjByMEWtN{45KM7:TR?= M3W2bVI1KGh? M{jYTIFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVSyOVgyODBzMB?=
UM-22A NIjPcWxHfW6ldHnvckBCe3OjeR?= NVnhUmVnOC5yMEC1MVEvPiEQvF2= M1H1PFI1KGh? NVyzb2E1[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUmyOVgyODBzMB?=
A1847 MWrGeY5kfGmxbjDBd5NigQ>? NF3kWVgxNjB3LUGwJO69VQ>? NH3OUnEzPCCq NEDY[FdFVVORwrC= NH\6Smtz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M1jxWFI2PjR4MEG1
OVCAR-5 MW\GeY5kfGmxbjDBd5NigQ>? MkDCNE4xPS1zMDFOwG0> MkPaNlQhcA>? MVPEUXNQyqB? NXLhfZE5emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NULnNGxOOjV4NE[wNVU>
OVCAR-8 M3y3SmZ2dmO2aX;uJGF{e2G7 M2PMclAvODVvMUCg{txO MknZNlQhcA>? M2TMNGROW00EoB?= MYry[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MXGyOVY1PjBzNR?=
MOVCAR-5447 MWrGeY5kfGmxbjDBd5NigQ>? NG\POFYxNjB3LUGwJO69VQ>? MnzNNlQhcA>? NEHz[nVFVVORwrC= NYT0S3lGemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M2XkdVI2PjR4MEG1
MOVCAR-5009 MlTISpVv[3Srb36gRZN{[Xl? NF\wXIExNjB3LUGwJO69VQ>? NHr0Zm8zPCCq NEe2[odFVVORwrC= MoLYdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M1jId|I2PjR4MEG1
A1847 M1zpdmNmdGxiVnnhZoltcXS7IFHzd4F6 MkW0NE4xPS1zMDFOwG0> MojDO|IhcA>? NVK2UlRqTE2VTx?= NIXLNZZz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NFe4cZQzPTZ2NkCxOS=>
OVCAR-5 NF[5e5BE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYKwMlA2NTFyIN88US=> NILmWYQ4OiCq MWXEUXNQ MomxdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MVOyOVY1PjBzNR?=
OVCAR-8  MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWq4bohlOC5yNT2xNEDPxE1? NY\lOoJ3PzJiaB?= NXPqW2xjTE2VTx?= M{fiUpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN Mn;FNlU3PDZyMUW=
OVCAR-5  MnLMRZBweHSxc3nzJGF{e2G7 M3nBe|AvPS9zL{Wg{txO M36z[VQ5KGh? M2XKfmROW09? MVrpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w MUWyOVY1PjBzNR?=
OVCAR-8  NXL3T5M2SXCxcITvd4l{KEG|c3H5 MorCNE42NzFxNTFOwG0> Mn7COFghcA>? MkXTSG1UVw>? NIW5O2NqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u Mn\SNlU3PDZyMUW=
AKRSL NUXzZXpIS2WubDDWbYFjcWyrdImgRZN{[Xl? NVW3OoZmPzJiaB?= NHfDUWJKSzVy78{eNVAh|ryP MUmyOVUxPDZ|NR?=
PALJDL NELQ[IFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVLpeVF1PzJiaB?= M4Xk[mlEPTB;Mj60JO69VQ>? M3jpblI2PTB2NkO1
MO4 M4rMNmZ2dmO2aX;uJGF{e2G7 NWnEV4NbOC53L{GvOUDPxE1? MV:2JIg> MkfSbY5pcWKrdIOgVE1UXEGWMzDlfJBz\XO|aX;uxsA> NW[y[VE5OjVzNEm1N|U>
DU145  NXHRfJBuTnWwY4Tpc44hSXO|YYm= MVWwMVIxOCCwTR?= MmHHNUBpyqB? M2rLbJN2eHC{ZYPz[ZMhUUxvNj3hZ5RqfmG2ZXSgV5RifDNiYX7kJGVTUzFxMjDzbYdv[Wyrbne= NHfFUpUzPDV5N{m0Ni=>
DU145  M4LmV2Z2dmO2aX;uJGF{e2G7 NF;sOFk5ODBibl2= MX[3NkBp MnL4d5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 NVrMeGF3OjR3N{e5OFI>
CWR22Rv1 M1f2TmZ2dmO2aX;uJGF{e2G7 MWi4NFAhdk1? M2XRXlczKGh? M{DaepN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= M2XlO|I1PTd5OUSy
N592 NF;qSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDIdolbUUN3ME2wMlg1KM7:TR?= MoLRNlQyPTh5MEG=
H82 M3njOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fzTWlEPTB;MT6zO{DPxE1? NIi5N2szPDF3OEewNS=>
GLC4 NXPZc45PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\WR4hKSzVyPUGuO|kh|ryP MYSyOFE2QDdyMR?=
H526 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfETWM2OD1|LkC4JO69VQ>? NF;NUHYzPDF3OEewNS=>
H1173 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\vPIdOUUN3ME2yMlM6KM7:TR?= MYmyOFE2QDdyMR?=
DMS114 NHXI[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofqTWM2OD1yLkezJO69VQ>? MUiyOFE2QDdyMR?=
NCI-N592 NH;qfpFHfW6ldHnvckBCe3OjeR?= MYKwMlMwOS9|IN88US=> M3rrXVI1KGh? MnzubY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MViyOFE2QDdyMR?=
GLC4 MmjJSpVv[3Srb36gRZN{[Xl? MWOwMlMwOS9|IN88US=> NXnFUGpqOjRiaB?= NWHpTZNOcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MXKyOFE2QDdyMR?=
NCI-H82 MkO3SpVv[3Srb36gRZN{[Xl? MY[wMlMwOS9|IN88US=> MnG2NlQhcA>? MoG5bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NGT0dJIzPDF3OEewNS=>
NCI-N592 NIDUfY9CeG:ydH;zbZMhSXO|YYm= Ml\NNE4{NzFxMzFOwG0> NIXlbmw1QCCq MYrpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MVeyOFE2QDdyMR?=
GLC4 NYXHN|RCSXCxcITvd4l{KEG|c3H5 M4W2OVAvOy9zL{Og{txO NEDJN5Y1QCCq MnHnbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NULFRZpHOjRzNUi3NFE>
NCI-H82 M4nvPWFxd3C2b4Ppd{BCe3OjeR?= M2[zfVAvOy9zL{Og{txO M2nUZVQ5KGh? M3[xZ4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M2rrSlI1OTV6N{Cx
CWR22Rv1  M4nrN2Fxd3C2b4Ppd{BCe3OjeR?= MkTVTWM2OD1yLkS4NkDPxE1? NFzsUGYzOzl2MkC5OS=>
CWR22Pc MVHBdI9xfG:|aYOgRZN{[Xl? NILaO|lKSzVyPUCuOFM5KM7:TR?= NF;UNmEzOzl2MkC5OS=>
PC-3 NUjPT5h6SXCxcITvd4l{KEG|c3H5 Ml7HTWM2OD1zLke1OUDPxE1? MkfGNlM6PDJyOUW=
DU145 MYfBdI9xfG:|aYOgRZN{[Xl? MmLMTWM2OD1|LkWxO{DPxE1? NV3ZcZhLOjN7NEKwPVU>
RC165N MkXzRZBweHSxc3nzJGF{e2G7 NUKxOXBzUUN3ME2yMlA5OyEQvF2= NHzhTYwzOzl2MkC5OS=>
ARPE19 NFmwVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;vO|dFVVOR MlPPTWM2OD1{ND6zPEDPxE1? NIfIfGwzOzV|MUmyNS=>
HEK293 NYPhVm9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLLVpBFVVOR MYDJR|UxRThwNkeg{txO MUeyN|U{OTl{MR?=
KCNR NYnPV3c5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NESwWJNFVVOR Mn33TWM2OD1yLkS2JO69VQ>? NXzieI46OjN3M{G5NlE>
SY5Y M1PhT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHlSG1UVw>? M1KwZmlEPTB;MD6zOkDPxE1? M2TrfVI{PTNzOUKx
BE2 M3zrbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTEUXNQ NYXnV4FGUUN3ME2wMlcyKM7:TR?= MWqyN|U{OTl{MR?=
AS NInoR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L2TWROW09? MV3JR|UxRTFwNUOg{txO MojUNlM2OzF7MkG=
NGP NX3zN5E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFi5RWxFVVOR M33XNmlEPTB;MD61OkDPxE1? NX\ldZV1OjN3M{G5NlE>
IMR32 NHrVelRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P2[WROW09? NXOzXoREUUN3ME2wMlY3KM7:TR?= NFHnXnMzOzV|MUmyNS=>
LAN5 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfpepdFVVOR NXzU[2VkUUN3ME2xMlA1KM7:TR?= M1nwRVI{PTNzOUKx
RH18 M{[yTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z2V2ROW09? MXrJR|UxRTFwNEKg{txO MlrPNlM2OzF7MkG=
RH30 NGrUdY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\qSG1UVw>? MlXUTWM2OD1zLkK1JO69VQ>? MknpNlM2OzF7MkG=
RH17 NFvCWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHEUXNQ M4D4UGlEPTB;Mj61NUDPxE1? MVOyN|U{OTl{MR?=
RH28 MlHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjKSG1UVw>? M3jWNWlEPTB;ND6yPEDPxE1? M{XiUVI{PTNzOUKx
RH36 MkTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO4SG1UVw>? NEnaOm5KSzVyPUWuN|ch|ryP NYW1fmdTOjN3M{G5NlE>
RH41 NX;VXW5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTEUXNQ MXnJR|UxRTBwNEig{txO NXT0U4R4OjN3M{G5NlE>
RD MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjud4pFVVOR M4XsbWlEPTB;ND6zNkDPxE1? MlmyNlM2OzF7MkG=
TC32 MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm1TZRFVVOR NVvvRVlYUUN3ME2zMlg2KM7:TR?= NX7Ec|lxOjN3M{G5NlE>
TC71 NGj6RlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfXVmNtTE2VTx?= NECwWnFKSzVyPUSuN|Mh|ryP NYDBTFN5OjN3M{G5NlE>
KCNR NYPNZ|hSSXCxcITvd4l{KEG|c3H5 NHTHOogxNjVxMT6wM|IvPSEQvF2= MUiyOEBp MXrEUXNQ NXXVVVZ1cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MnrNNlM2OzF7MkG=
SY5Y NHTSfYtCeG:ydH;zbZMhSXO|YYm= NH7Id5AxNjVxMT6wM|IvPSEQvF2= MY[yOEBp MVnEUXNQ MYLpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MXqyN|U{OTl{MR?=
Rh18 MkTSRZBweHSxc3nzJGF{e2G7 NF:yWoUxNjVxMT6wM|IvPSEQvF2= NInW[ZIzPCCq MlSySG1UVw>? NFrNOnlqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 M4nHelI{PTNzOUKx
TC32 MkPORZBweHSxc3nzJGF{e2G7 NF\lSJAxNjVxMT6wM|IvPSEQvF2= MVGyOEBp MWXEUXNQ MV\pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MWqyN|U{OTl{MR?=
KCNR NEeydIZHfW6ldHnvckBCe3OjeR?= M3f1dlAvPS9zLkCvNk42NzVizszN NXGwS5RtOjRiaB?= MU\EUXNQ M4fp[YlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NGrKXo8zOzV|MUmyNS=>
SY5Y MVTGeY5kfGmxbjDBd5NigQ>? MWKwMlUwOS5yL{KuOU82KM7:TR?= NFvidYIzPCCq Mni5SG1UVw>? MUTpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NYO2XHhFOjN3M{G5NlE>
Rh18 MnWwSpVv[3Srb36gRZN{[Xl? NXHme3NYOC53L{GuNE8zNjVxNTFOwG0> M4PMWlI1KGh? M2rGU2ROW09? MV;pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MUWyN|U{OTl{MR?=
TC32 MVvGeY5kfGmxbjDBd5NigQ>? MUewMlUwOS5yL{KuOU82KM7:TR?= NGT1OJozPCCq MYTEUXNQ M2DKW4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u M4\RUlI{PTNzOUKx
TPC-1 M2\EN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTGbmMyKML3TR?= MlXzNE01KGR? MW\EUXNQ MV;pcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 MXyyN|A2PjR7OR?=
MZ-CRC1  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjWNUDDvU1? NFjCfVAxNTViZB?= NYHTNYVZTE2VTx?= M3LuRolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MYiyN|A2PjR7OR?=
TT  Mnr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjKXWs2OSEEtV2= NG\wd2MxNTRiZB?= M3jYdmROW09? NH;SZ3FqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 M4rKdVI{ODV4NEm5
TPC-1 Mlq3SpVv[3Srb36gRZN{[Xl? NXHGUol6OSEEtV2= NIHlc|k4OiCq MYTEUXNQ MUDpcoR2[2W|IFexJIJtd2OtYXfl Mk\vNlMxPTZ2OUm=
MZ-CRC1  NYDHOoFyTnWwY4Tpc44hSXO|YYm= NY[3U2FVOSEEtV2= NXL6folCPzJiaB?= NIXUPVVFVVOR NFHieI9qdmS3Y3XzJGcyKGKub3PrZYdm NIj0TWQzOzB3NkS5PS=>
TT  NVPMfW42TnWwY4Tpc44hSXO|YYm= NX3Wd4N3OSEEtV2= M1raRVczKGh? M1PJT2ROW09? MWnpcoR2[2W|IFexJIJtd2OtYXfl MnO5NlMxPTZ2OUm=
MZ-CRC1  MWLBdI9xfG:|aYOgRZN{[Xl? M4DZ[lEhyrWP NYPkWodZPDhiaB?= NHTvWIJFVVOR MmeybY5lfWOnczDhdI9xfG:|aYO= M3LrXFI{ODV4NEm5
TT  NVG0[oNmSXCxcITvd4l{KEG|c3H5 MVKxJOK2VQ>? NFTmOow1QCCq M2fOb2ROW09? NHXUO41qdmS3Y3XzJIFxd3C2b4Ppdy=> NV[weIQ3OjNyNU[0PVk>
HD-LM2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj3[FQ4OuLCiXi= NG\5XpFFVVOR NV7wT5I2UUN3ME23Mlg1PCEQvF2= NGK5dXYzOjh{OUC5OC=>
L-428 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkC1O|LjiImq NEHuRohFVVOR NF\VcVdKSzVyPUeuPVQ4KM7:TR?= NIfLO|kzOjh{OUC5OC=>
KM-H2 NVXhUVJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\wdFZOPzMkgJno M1LMSGROW09? NIXQe|FKSzVyPUGuN|A5KM7:TR?= M3jpUVIzQDJ7MEm0
L-540 NWDHS2t7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYe3NwKBkWh? M2X0SmROW09? M{XScGlEPTB;OD6yNVYh|ryP MmLyNlI5OjlyOUS=
HD-LM2 MWjGeY5kfGmxbjDBd5NigQ>? NVrmemROOC5zL{CuOU8yNzVizszN MV:3NwKBkWh? MnLKSG1UVw>? MWfpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> M{PQN|IzQDJ7MEm0
L-428 MnLpSpVv[3Srb36gRZN{[Xl? M{D3flAvOS9yLkWvNU82KM7:TR?= MUG3NwKBkWh? M3ywdGROW09? M1y1PIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v Ml7ONlI5OjlyOUS=
KM-H2 Moq1SpVv[3Srb36gRZN{[Xl? Mk\hNE4yNzBwNT:xM|Uh|ryP MlTJO|LjiImq M2TVcmROW09? NVTjSJRJcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? M4[zSlIzQDJ7MEm0
L-540 NIn1c4ZHfW6ldHnvckBCe3OjeR?= M1vROVAvOS9yLkWvNU82KM7:TR?= NWDteYt1PzMkgJno M1:3SGROW09? M2LiOYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NXPFOmtVOjJ6MkmwPVQ>
HD-LM2 NYCyZm1CSXCxcITvd4l{KEG|c3H5 Mn76NU82KM7:TR?= MoHSO|LjiImq NH\jVJlFVVOR MV7pcoR2[2W|IHHwc5B1d3Orcx?= NGj5TIQzOjh{OUC5OC=>
L-428 MXfBdI9xfG:|aYOgRZN{[Xl? NYTZTHQ1OS93IN88US=> MlLjO|LjiImq MXvEUXNQ NIi1[VdqdmS3Y3XzJIFxd3C2b4Ppdy=> NF;Je4wzOjh{OUC5OC=>
KM-H2 MUDBdI9xfG:|aYOgRZN{[Xl? M3v2U|EwPSEQvF2= NYqxUXVnPzMkgJno MnzkSG1UVw>? MlzWbY5lfWOnczDhdI9xfG:|aYO= NWXacIg4OjJ6MkmwPVQ>
L-540 NWDDc4JVSXCxcITvd4l{KEG|c3H5 NXPSV2hjOS93IN88US=> NW\0TpQ5PzMkgJno NYDEcWhWTE2VTx?= NGDjR3lqdmS3Y3XzJIFxd3C2b4Ppdy=> MnHRNlI5OjlyOUS=
U251-MG MV3GeY5kfGmxbjDBd5NigQ>? M3O0VFEhyrWP NY\zc|VXOC1zNjDo MYXpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> M3PK[VIzODJ5Nkmx
U87-MG NGCwZYZHfW6ldHnvckBCe3OjeR?= MmLTNUDDvU1? MkXkNE0yPiCq NEnjS3dqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MlnqNlIxOjd4OUG=
4C8 NXG5VGxQTnWwY4Tpc44hSXO|YYm= MXixJOK2VQ>? M3;BRlAuOTZiaB?= MmLkbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v M3T4WlIzODJ5Nkmx
U251-MG NXPic211T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILQe2EyNzFyINM1US=> MkGwNlQwPDhxN{KgbC=> NITwcIdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NX\lfXMxOjJyMke2PVE>
U87-MG MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxM|ExKML3TR?= NUDncphJOjRxNEivO|IhcA>? M{\M[4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO MWWyNlAzPzZ7MR?=
4C8 NWLKZlZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj6NU8yOCEEtV2= M2r1[|I1NzR6L{eyJIg> NEjSZVhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MWGyNlAzPzZ7MR?=
U266 MnuzRZBweHSxc3nzJGF{e2G7 NV7qT3Z2OC53LUKg{txO MlHZOFgwPzJiaB?= NGHxNFRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NHfhS3YzOTF4NEWxOy=>
Kms.11 MUHBdI9xfG:|aYOgRZN{[Xl? NVy3UYpwOC53LUKg{txO NETrRm41QC95MjDo MmGzbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MXyyNVE3PDVzNx?=
8226 NHnjdFdCeG:ydH;zbZMhSXO|YYm= MY[wMlUuOiEQvF2= M{D0b|Q5Nzd{IHi= M36wRolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M3vwfFIyOTZ2NUG3

... 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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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID