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 M2WxRmZ2dmO2aX;uJGF{e2G7 MUO1JO69VQ>? NIPablk1QCCq NEnubodFVVOR NGXUWpFjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NHu4cYQzPTl3NEm3OC=>
LoVo  MmHWSpVv[3Srb36gRZN{[Xl? NULDcoNsPSEQvF2= MmjCOFghcA>? NXuze5BWTE2VTx?= NFPTNpdjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> M1naRVI2QTV2OUe0
HN5 M3;4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj4[llCPzJiaB?= MXzFR|UxRTNwOEGgxtEhOS57OTFOwG0> NUTnRXFnOjV6MUCwNVA>
Cal33 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL2TXlbPzJiaB?= M4L4NmVEPTB;Mz6zO{DDuSByLke1JO69VQ>? NIr6VG8zPThzMECxNC=>
UM-22B NWHuTHl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXS3NkBp MUjFR|UxRTJwNk[gxtEhOC5{NDFOwG0> MkLrNlU5OTByMUC=
686LN NXfsNmJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX63NkBp NGDyZmFGSzVyPUKuNFUhyrFiMT6zN{DPxE1? MkXRNlU5OTByMUC=
UM SCC-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPzOFd3PzJiaB?= M3PyNGVEPTB;MT62O{DDuSByLkSyJO69VQ>? MYiyOVgyODBzMB?=
UM-22A M1fuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPrO|IhcA>? M2jvcmVEPTB;MT6zNkDDuSByLkO5JO69VQ>? M3znXVI2QDFyMEGw
OSC19 NHPLbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H6NlczKGh? MnXZSWM2OD1zLkK2JOKyKDBwMkCg{txO NGPKW4kzPThzMECxNC=>
PCI-52 NUHEWpU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXDO|U4OiCq NFnBOYRGSzVyPUGuNFAhyrFiMD6wPUDPxE1? Mn\UNlU5OTByMUC=
PCI-15B NGK5cFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfXXVY4OiCq NFTsU5JGSzVyPUCuPVkhyrFiMT63OEDPxE1? M1\j[lI2QDFyMEGw
UMSCC-1 NGLDcWFHfW6ldHnvckBCe3OjeR?= NWHjT|gzOC5yMEC1MVEvPiEQvF2= NVuySoxjOjRiaB?= MWThZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2XDdFI2QDFyMEGw
Cal33 M{fzdGZ2dmO2aX;uJGF{e2G7 MmTuNE4xODB3LUOuPEDPxE1? NETTUnAzPCCq NFHINFFi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX7BXXpnOjV6MUCwNVA>
HH5 MXvGeY5kfGmxbjDBd5NigQ>? NF3QXXYxNjByMEWtN{45KM7:TR?= MYWyOEBp NHzSZ5li[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFy1b5MzPThzMECxNC=>
UM-22A NES3R3NHfW6ldHnvckBCe3OjeR?= MkXwNE4xODB3LUGuOkDPxE1? M1XTTVI1KGh? MnjDZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWm5eplDOjV6MUCwNVA>
A1847 M{DIWmZ2dmO2aX;uJGF{e2G7 NUewXHc1OC5yNT2xNEDPxE1? NGLxb|EzPCCq M{jkfGROW00EoB?= M2jDXZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MknpNlU3PDZyMUW=
OVCAR-5 M{DtS2Z2dmO2aX;uJGF{e2G7 NVrrVHA6OC5yNT2xNEDPxE1? MmLvNlQhcA>? M2rOVGROW00EoB?= Mnr1doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M3;rRVI2PjR4MEG1
OVCAR-8 MlXOSpVv[3Srb36gRZN{[Xl? MlfNNE4xPS1zMDFOwG0> NFHVUG0zPCCq NIjqdI5FVVORwrC= NITDSYtz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MlG0NlU3PDZyMUW=
MOVCAR-5447 M{fDbmZ2dmO2aX;uJGF{e2G7 MXWwMlA2NTFyIN88US=> MnK0NlQhcA>? M4LIOWROW00EoB?= NV3aV2p6emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NIfvU|kzPTZ2NkCxOS=>
MOVCAR-5009 NUjJ[2FTTnWwY4Tpc44hSXO|YYm= NVLDbpU{OC5yNT2xNEDPxE1? M4PSbFI1KGh? M2G4bWROW00EoB?= NU\IU5A1emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NWHHW4FwOjV4NE[wNVU>
A1847 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlXnNE4xPS1zMDFOwG0> NVTNVVBKPzJiaB?= MVfEUXNQ NUfCRXo5emWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> M3HjdFI2PjR4MEG1
OVCAR-5 M3HpUmNmdGxiVnnhZoltcXS7IFHzd4F6 NUTJfHAyOC5yNT2xNEDPxE1? NFPFbHg4OiCq MX;EUXNQ MY\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= NHTMb4czPTZ2NkCxOS=>
OVCAR-8  NFK0TVdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{jhR|AvODVvMUCg{txO MVm3NkBp NYrJdVRETE2VTx?= MmfPdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NFnsfHgzPTZ2NkCxOS=>
OVCAR-5  NVfSVGtCSXCxcITvd4l{KEG|c3H5 M2LDcVAvPS9zL{Wg{txO NYPMOFAxPDhiaB?= MnrsSG1UVw>? MljWbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= NWS0NIZLOjV4NE[wNVU>
OVCAR-8  M3;5O2Fxd3C2b4Ppd{BCe3OjeR?= NWC0T4NTOC53L{GvOUDPxE1? M{TOb|Q5KGh? M2fJOGROW09? MmrvbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= MkPINlU3PDZyMUW=
AKRSL MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVm3NkBp MYHJR|Ux97zgMUCg{txO NF71N2ozPTVyNE[zOS=>
PALJDL NVHEUI1HS2WubDDWbYFjcWyrdImgRZN{[Xl? M1vWW|czKGh? MkX4TWM2OD1{LkSg{txO M1:wbFI2PTB2NkO1
MO4 M1jxVWZ2dmO2aX;uJGF{e2G7 NHK0eXQxNjVxMT:1JO69VQ>? NVHZN4VqPiCq Mkm2bY5pcWKrdIOgVE1UXEGWMzDlfJBz\XO|aX;uxsA> Ml\FNlUyPDl3M{W=
DU145  M37UV2Z2dmO2aX;uJGF{e2G7 NGK0d5kxNTJyMDDuUS=> NWP2RnJTOSCqwrC= NGfJWJN{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NFOybGgzPDV5N{m0Ni=>
DU145  M3LibWZ2dmO2aX;uJGF{e2G7 NVL0Om1WQDByIH7N M4PoelczKGh? M3fJfJN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NFjq[WIzPDV5N{m0Ni=>
CWR22Rv1 Mn22SpVv[3Srb36gRZN{[Xl? M1;HUFgxOCCwTR?= NWDidVZsPzJiaB?= NWjpN5lve3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 NWrGdoNrOjR3N{e5OFI>
N592 MnzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH2TWM2OD1yLki0JO69VQ>? M3jMVlI1OTV6N{Cx
H82 NXLBZZhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrRTWM2OD1zLkO3JO69VQ>? NHzLSG8zPDF3OEewNS=>
GLC4 Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HUcWlEPTB;MT63PUDPxE1? NYfNXmhOOjRzNUi3NFE>
H526 NHvrSY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTNwMEig{txO NX;0PIlkOjRzNUi3NFE>
H1173 NF3TRVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLJXFljUUN3ME2yMlM6KM7:TR?= MVeyOFE2QDdyMR?=
DMS114 NGr1WXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ntSWlEPTB;MD63N{DPxE1? Ml7MNlQyPTh5MEG=
NCI-N592 MWLGeY5kfGmxbjDBd5NigQ>? MU[wMlMwOS9|IN88US=> NVXU[IlJOjRiaB?= MmL1bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NGHz[5ozPDF3OEewNS=>
GLC4 MmLISpVv[3Srb36gRZN{[Xl? NFzEb3gxNjNxMT:zJO69VQ>? NXvxbVVSOjRiaB?= MlvWbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NGntU4IzPDF3OEewNS=>
NCI-H82 M1mw[GZ2dmO2aX;uJGF{e2G7 MXqwMlMwOS9|IN88US=> Ml\uNlQhcA>? NVixW2I2cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NWS0Oo5GOjRzNUi3NFE>
NCI-N592 NEewdpVCeG:ydH;zbZMhSXO|YYm= M1XBNVAvOy9zL{Og{txO NETOdpo1QCCq NG\UdmFqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MnPVNlQyPTh5MEG=
GLC4 NV3ZZ|BjSXCxcITvd4l{KEG|c3H5 MonlNE4{NzFxMzFOwG0> MVS0PEBp MXHpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MkK4NlQyPTh5MEG=
NCI-H82 MUjBdI9xfG:|aYOgRZN{[Xl? MYmwMlMwOS9|IN88US=> M3TmUlQ5KGh? NHr3NGVqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NHvyVWszPDF3OEewNS=>
CWR22Rv1  NWHJVJdsSXCxcITvd4l{KEG|c3H5 MorWTWM2OD1yLkS4NkDPxE1? M3G0elI{QTR{MEm1
CWR22Pc NFfEcnRCeG:ydH;zbZMhSXO|YYm= Mn7RTWM2OD1yLkSzPEDPxE1? MUOyN|k1OjB7NR?=
PC-3 NIPO[JFCeG:ydH;zbZMhSXO|YYm= MkXDTWM2OD1zLke1OUDPxE1? NG\mWnozOzl2MkC5OS=>
DU145 NYDLXlgxSXCxcITvd4l{KEG|c3H5 NH3ZVXBKSzVyPUOuOVE4KM7:TR?= M4W5UFI{QTR{MEm1
RC165N NInEdGNCeG:ydH;zbZMhSXO|YYm= NXzSRpdSUUN3ME2yMlA5OyEQvF2= M3zSOVI{QTR{MEm1
ARPE19 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nHbmROW09? MULJR|UxRTJ2LkO4JO69VQ>? MVOyN|U{OTl{MR?=
HEK293 M{HtTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXkcWRsTE2VTx?= MnTaTWM2OD16Lk[3JO69VQ>? NHLaNHEzOzV|MUmyNS=>
KCNR MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T4NmROW09? MXrJR|UxRTBwNE[g{txO MnHWNlM2OzF7MkG=
SY5Y NVT4SGlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPzSG1UVw>? NYPYeFNQUUN3ME2wMlM3KM7:TR?= NFe1eJIzOzV|MUmyNS=>
BE2 M3nwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\NSG1UVw>? NILnbphKSzVyPUCuO|Eh|ryP M4LUZlI{PTNzOUKx
AS M2\pcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHaZnNFVVOR M4DSNmlEPTB;MT61N{DPxE1? M3e1N|I{PTNzOUKx
NGP NUHMS|ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;EUXNQ Mof1TWM2OD1yLkW2JO69VQ>? Mo\zNlM2OzF7MkG=
IMR32 NEWzXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTkTppTTE2VTx?= NYDxO3Q1UUN3ME2wMlY3KM7:TR?= M1rXSFI{PTNzOUKx
LAN5 M1[5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\RSG1UVw>? MVfJR|UxRTFwMESg{txO NWjsSFhXOjN3M{G5NlE>
RH18 NWC3eYV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7YSG1UVw>? M3qxeGlEPTB;MT60NkDPxE1? MoHTNlM2OzF7MkG=
RH30 NVi3[5l{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni0SG1UVw>? MXfJR|UxRTFwMkWg{txO NHS2ZpczOzV|MUmyNS=>
RH17 M1LOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TYUWROW09? NIHPc4pKSzVyPUKuOVEh|ryP NYnZOoY3OjN3M{G5NlE>
RH28 NEL0R5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS2TpA6TE2VTx?= M2n0OmlEPTB;ND6yPEDPxE1? M2rjb|I{PTNzOUKx
RH36 NFS0UohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLEUXNQ NFS3U|BKSzVyPUWuN|ch|ryP MlriNlM2OzF7MkG=
RH41 NWroNVNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W4NGROW09? NHznZoxKSzVyPUCuOFgh|ryP NUjOTIhTOjN3M{G5NlE>
RD M4LpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2W3NGROW09? NX;Ne|VUUUN3ME20MlMzKM7:TR?= NWKzU5VZOjN3M{G5NlE>
TC32 NEDnUm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrBNnlvTE2VTx?= NIe5OGVKSzVyPUOuPFUh|ryP MVOyN|U{OTl{MR?=
TC71 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjEUXNQ Mne4TWM2OD12LkOzJO69VQ>? NYm0WpBrOjN3M{G5NlE>
KCNR NV2xNXpRSXCxcITvd4l{KEG|c3H5 M{\oe|AvPS9zLkCvNk42KM7:TR?= NUfDdmszOjRiaB?= NEH6fVlFVVOR MX3pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MXOyN|U{OTl{MR?=
SY5Y NX[1c5FLSXCxcITvd4l{KEG|c3H5 NIfDOJYxNjVxMT6wM|IvPSEQvF2= M4XzVFI1KGh? NYfvVYc3TE2VTx?= NXnVSYxVcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> M4nEN|I{PTNzOUKx
Rh18 M2fJR2Fxd3C2b4Ppd{BCe3OjeR?= MmfvNE42NzFwMD:yMlUh|ryP MnXONlQhcA>? NWr4dWh7TE2VTx?= MmPKbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MlHDNlM2OzF7MkG=
TC32 NUC1T3I4SXCxcITvd4l{KEG|c3H5 Mn7sNE42NzFwMD:yMlUh|ryP M2S4cVI1KGh? NIDwPHZFVVOR MX3pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 M1O1WFI{PTNzOUKx
KCNR MoO4SpVv[3Srb36gRZN{[Xl? M4KzO|AvPS9zLkCvNk42NzVizszN NIXhe|YzPCCq MUnEUXNQ MXrpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= M{LnWlI{PTNzOUKx
SY5Y M4niXGZ2dmO2aX;uJGF{e2G7 NHfhV2kxNjVxMT6wM|IvPS93IN88US=> MUOyOEBp NYLYZ4U5TE2VTx?= NY\GR|RtcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MYmyN|U{OTl{MR?=
Rh18 M3;XPGZ2dmO2aX;uJGF{e2G7 MX:wMlUwOS5yL{KuOU82KM7:TR?= Mn\sNlQhcA>? MUXEUXNQ NFfOPIxqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MlLINlM2OzF7MkG=
TC32 MojJSpVv[3Srb36gRZN{[Xl? MmPKNE42NzFwMD:yMlUwPSEQvF2= MXyyOEBp MUDEUXNQ MV7pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MXKyN|U{OTl{MR?=
TPC-1 NWLlbJo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnCNUDDvU1? MlPENE01KGR? M1rpfmROW09? NVPETXB6cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOiCmIITy[YF1dWWwdB?= NHrWV4QzOzB3NkS5PS=>
MZ-CRC1  MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXXNUDDvU1? MnXINE02KGR? MojuSG1UVw>? MVHpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 M3;YPFI{ODV4NEm5
TT  MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWra[5FUOSEEtV2= MUOwMVQh\A>? NWC3RVJPTE2VTx?= MVTpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 Mn\rNlMxPTZ2OUm=
TPC-1 NW[yOmdlTnWwY4Tpc44hSXO|YYm= MkXDNUDDvU1? MnTUO|IhcA>? MUTEUXNQ NX\GUFdocW6mdXPld{BIOSCkbH;jb4Fo\Q>? MmexNlMxPTZ2OUm=
MZ-CRC1  NILoPXVHfW6ldHnvckBCe3OjeR?= NHfUeFUyKML3TR?= MXG3NkBp MlnnSG1UVw>? MlfsbY5lfWOnczDHNUBjdG:la3Hn[S=> NHHVVmszOzB3NkS5PS=>
TT  Mn31SpVv[3Srb36gRZN{[Xl? NWexellSOSEEtV2= NWWw[5hRPzJiaB?= M1jFb2ROW09? NHK5VGtqdmS3Y3XzJGcyKGKub3PrZYdm MWOyN|A2PjR7OR?=
MZ-CRC1  M3jVO2Fxd3C2b4Ppd{BCe3OjeR?= MlzsNUDDvU1? NY\rS|BMPDhiaB?= NVPuVYhsTE2VTx?= MX3pcoR2[2W|IHHwc5B1d3Orcx?= NHzDVm0zOzB3NkS5PS=>
TT  NWfZN5A1SXCxcITvd4l{KEG|c3H5 MYqxJOK2VQ>? NW\sVYVXPDhiaB?= M3fRdGROW09? NHH1dVNqdmS3Y3XzJIFxd3C2b4Ppdy=> Mlf5NlMxPTZ2OUm=
HD-LM2 NFLjcpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ntNlcz6oDLaB?= NUHxTpd2TE2VTx?= NFnMSXBKSzVyPUeuPFQ1KM7:TR?= NIXuXIszOjh{OUC5OC=>
L-428 NEKyTmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvEcWNxPzMkgJno MmX0SG1UVw>? NG\veVdKSzVyPUeuPVQ4KM7:TR?= NHHFVZIzOjh{OUC5OC=>
KM-H2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO1WGI4OuLCiXi= NXrSRnhOTE2VTx?= M3exdWlEPTB;MT6zNFgh|ryP NVLzdZhyOjJ6MkmwPVQ>
L-540 M3P0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUe3NwKBkWh? NIPyc3BFVVOR NF;nPVdKSzVyPUiuNlE3KM7:TR?= M{TNXFIzQDJ7MEm0
HD-LM2 MmD5SpVv[3Srb36gRZN{[Xl? M2rlWFAvOS9yLkWvNU82KM7:TR?= M1LxdFcz6oDLaB?= NFXvVIJFVVOR NIPrcIRqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? M4fOWVIzQDJ7MEm0
L-428 NV7FWHlqTnWwY4Tpc44hSXO|YYm= M2PZNVAvOS9yLkWvNU82KM7:TR?= MVy3NwKBkWh? MneySG1UVw>? Mk[zbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NYDBZ2hPOjJ6MkmwPVQ>
KM-H2 MWnGeY5kfGmxbjDBd5NigQ>? Ml:yNE4yNzBwNT:xM|Uh|ryP NVe2bpozPzMkgJno NXPMdHpmTE2VTx?= NIrNOFZqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NWjhelVDOjJ6MkmwPVQ>
L-540 NFnMWXhHfW6ldHnvckBCe3OjeR?= NVnPVZVkOC5zL{CuOU8yNzVizszN NITWeWQ4OuLCiXi= M1;n[2ROW09? MkfjbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MorwNlI5OjlyOUS=
HD-LM2 NYjpeIdtSXCxcITvd4l{KEG|c3H5 MX2xM|Uh|ryP M3jDblcz6oDLaB?= MXnEUXNQ Mn3TbY5lfWOnczDhdI9xfG:|aYO= NYP4cJNwOjJ6MkmwPVQ>
L-428 MmfmRZBweHSxc3nzJGF{e2G7 NWnpO|BMOS93IN88US=> NIDOOmg4OuLCiXi= NXzaUlR4TE2VTx?= MkjMbY5lfWOnczDhdI9xfG:|aYO= NI\aRpQzOjh{OUC5OC=>
KM-H2 MX3BdI9xfG:|aYOgRZN{[Xl? MoC0NU82KM7:TR?= Moq2O|LjiImq MXXEUXNQ NGXx[5BqdmS3Y3XzJIFxd3C2b4Ppdy=> MUSyNlgzQTB7NB?=
L-540 M4\Jc2Fxd3C2b4Ppd{BCe3OjeR?= MlzQNU82KM7:TR?= MlT4O|LjiImq MWjEUXNQ NGPoT2tqdmS3Y3XzJIFxd3C2b4Ppdy=> NHrHTWozOjh{OUC5OC=>
U251-MG MUPGeY5kfGmxbjDBd5NigQ>? M3\ITVEhyrWP MmfINE0yPiCq MYHpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> M4P3SlIzODJ5Nkmx
U87-MG MWnGeY5kfGmxbjDBd5NigQ>? MmjxNUDDvU1? MmnONE0yPiCq NET1TIdqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NVLxRYJnOjJyMke2PVE>
4C8 M1TRWGZ2dmO2aX;uJGF{e2G7 NVfXS3I1OSEEtV2= NYLSbmpSOC1zNjDo M3m5dolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? MljCNlIxOjd4OUG=
U251-MG M3i3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDYcnZqOS9zMDFCuW0> Ml3SNlQwPDhxN{KgbC=> MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> M2DWXVIzODJ5Nkmx
U87-MG NIC0cFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvHSGtuOS9zMDFCuW0> MWeyOE81QC95MjDo M4HlVYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NVrsd5htOjJyMke2PVE>
4C8 M17rcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxM|ExKML3TR?= M37sNlI1NzR6L{eyJIg> MnvPbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> NYHmbXFuOjJyMke2PVE>
U266 NEHx[mFCeG:ydH;zbZMhSXO|YYm= NFLNSpIxNjVvMjFOwG0> MVe0PE84OiCq Ml\PbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHfhUokzOTF4NEWxOy=>
Kms.11 MXHBdI9xfG:|aYOgRZN{[Xl? NV;vOFRDOC53LUKg{txO MlLUOFgwPzJiaB?= NVzIT5lLcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MnPDNlEyPjR3MUe=
8226 NFfndYVCeG:ydH;zbZMhSXO|YYm= M2\uU|AvPS1{IN88US=> M{exTFQ5Nzd{IHi= M2f1Wolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MknhNlEyPjR3MUe=

... 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
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