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 MVPGeY5kfGmxbjDBd5NigQ>? NEfSblU2KM7:TR?= M1\VO|Q5KGh? MoTHSG1UVw>? NXLM[Y9W[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o MmPCNlU6PTR7N{S=
LoVo  NETXW5ZHfW6ldHnvckBCe3OjeR?= MX21JO69VQ>? MWG0PEBp NWrVb4U3TE2VTx?= MV3icI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= NHLufXkzPTl3NEm3OC=>
HN5 M372V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zTTVczKGh? MmHwSWM2OD1|LkixJOKyKDFwOUmg{txO M{fRdFI2QDFyMEGw
Cal33 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfRd2k4OiCq NIrr[I9GSzVyPUOuN|chyrFiMD63OUDPxE1? MWOyOVgyODBzMB?=
UM-22B M1\vOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjVcZlTPzJiaB?= Ml\KSWM2OD1{Lk[2JOKyKDBwMkSg{txO NVvTO4tKOjV6MUCwNVA>
686LN NWKwdoVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUm3NkBp NH[0foFGSzVyPUKuNFUhyrFiMT6zN{DPxE1? M{\RNFI2QDFyMEGw
UM SCC-1 NEDuPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K3RVczKGh? NVPHPY9NTUN3ME2xMlY4KMLzIECuOFIh|ryP MXyyOVgyODBzMB?=
UM-22A MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG3NkBp MVrFR|UxRTFwM{KgxtEhOC5|OTFOwG0> MYCyOVgyODBzMB?=
OSC19 MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDKO|IhcA>? MX;FR|UxRTFwMk[gxtEhOC5{MDFOwG0> NWP6cGlbOjV6MUCwNVA>
PCI-52 Ml3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVG3NkBp NFrSSHBGSzVyPUGuNFAhyrFiMD6wPUDPxE1? NGL6RWMzPThzMECxNC=>
PCI-15B NEXkNlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLuO2s4OiCq MlvWSWM2OD1yLkm5JOKyKDFwN{Sg{txO MUmyOVgyODBzMB?=
UMSCC-1 NXrpV3lETnWwY4Tpc44hSXO|YYm= M1\TclAvODByNT2xMlYh|ryP M12ye|I1KGh? MoTqZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWTKOZl6OjV6MUCwNVA>
Cal33 NXPOc5M1TnWwY4Tpc44hSXO|YYm= M4TLfFAvODByNT2zMlgh|ryP MojXNlQhcA>? MWDhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MU[yOVgyODBzMB?=
HH5 MnvlSpVv[3Srb36gRZN{[Xl? MWOwMlAxODVvMz64JO69VQ>? NH;DdYMzPCCq MknuZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUeyOVgyODBzMB?=
UM-22A MlXLSpVv[3Srb36gRZN{[Xl? M{P2ZlAvODByNT2xMlYh|ryP NF3ETG4zPCCq NYnSU3hv[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGXNbpEzPThzMECxNC=>
A1847 MX3GeY5kfGmxbjDBd5NigQ>? NYH1TG9OOC5yNT2xNEDPxE1? NYPQR4M5OjRiaB?= MX;EUXNQyqB? M4jI[pJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MlnqNlU3PDZyMUW=
OVCAR-5 NYD0dVZXTnWwY4Tpc44hSXO|YYm= M{TaUFAvODVvMUCg{txO NY[4SodpOjRiaB?= MUnEUXNQyqB? NX\CUYszemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MYWyOVY1PjBzNR?=
OVCAR-8 NF65bpNHfW6ldHnvckBCe3OjeR?= NXTXV4M3OC5yNT2xNEDPxE1? NFvVTYszPCCq M4flOmROW00EoB?= M{PQTJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NIT1ZmozPTZ2NkCxOS=>
MOVCAR-5447 NUDlcGY6TnWwY4Tpc44hSXO|YYm= MWWwMlA2NTFyIN88US=> NUfzUW9YOjRiaB?= NITKc4VFVVORwrC= M{f5R5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MXSyOVY1PjBzNR?=
MOVCAR-5009 NWTSbWFiTnWwY4Tpc44hSXO|YYm= NEnlUnAxNjB3LUGwJO69VQ>? NF;KOYMzPCCq NUSxWYNpTE2VT9Mg NWXzV3p[emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NInDdmYzPTZ2NkCxOS=>
A1847 NYTUdmRmS2WubDDWbYFjcWyrdImgRZN{[Xl? MoTKNE4xPS1zMDFOwG0> MmD5O|IhcA>? NVzQbIM6TE2VTx?= NGHYXZRz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> M2nVd|I2PjR4MEG1
OVCAR-5 NF3Md5pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MoHLNE4xPS1zMDFOwG0> NFSzeJI4OiCq NH7FUVdFVVOR NYKwUo5bemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MmTmNlU3PDZyMUW=
OVCAR-8  NIHvO|RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4jKPFAvODVvMUCg{txO NV3QXpJCPzJiaB?= NIHqe5RFVVOR MVjy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MV:yOVY1PjBzNR?=
OVCAR-5  M4nIbmFxd3C2b4Ppd{BCe3OjeR?= MlrLNE42NzFxNTFOwG0> MVu0PEBp MWXEUXNQ MVHpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w Mom4NlU3PDZyMUW=
OVCAR-8  MoHERZBweHSxc3nzJGF{e2G7 M17qSFAvPS9zL{Wg{txO MX[0PEBp NF7GcHNFVVOR NY\PeGhjcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M{nxTVI2PjR4MEG1
AKRSL MoHLR4VtdCCYaXHibYxqfHliQYPzZZk> NGrFRlc4OiCq NELUSoRKSzVy78{eNVAh|ryP MUeyOVUxPDZ|NR?=
PALJDL MoPKR4VtdCCYaXHibYxqfHliQYPzZZk> NGXZTWc4OiCq MYHJR|UxRTJwNDFOwG0> NV;vNIV{OjV3MES2N|U>
MO4 MX;GeY5kfGmxbjDBd5NigQ>? MkK1NE42NzFxNTFOwG0> NYLxfJRNPiCq MV\pcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> M3zLWVI2OTR7NUO1
DU145  MmSxSpVv[3Srb36gRZN{[Xl? NH\NR4sxNTJyMDDuUS=> MXuxJIjDqA>? MYDzeZBxemW|c3XzJGlNNTZvYXP0bZZifGWmIGP0ZZQ{KGGwZDDFVmsyNzJic3nncoFtcW6p MVmyOFU4Pzl2Mh?=
DU145  Ml;MSpVv[3Srb36gRZN{[Xl? MmLOPFAxKG6P MofrO|IhcA>? NEL6bIZ{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NVnGd5VUOjR3N{e5OFI>
CWR22Rv1 NXH1VVJ2TnWwY4Tpc44hSXO|YYm= NH7vWGQ5ODBibl2= NWTUeGp7PzJiaB?= M1PDV5N2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= MnLRNlQ2Pzd7NEK=
N592 M4jzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInuTXVKSzVyPUCuPFQh|ryP MXOyOFE2QDdyMR?=
H82 M3r1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[5eW9KSzVyPUGuN|ch|ryP M1fSXlI1OTV6N{Cx
GLC4 NWXUWJN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnIN4FZUUN3ME2xMlc6KM7:TR?= Ml:0NlQyPTh5MEG=
H526 NG\oXVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nUemlEPTB;Mz6wPEDPxE1? NIH2OHEzPDF3OEewNS=>
H1173 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfUWXdKSzVyPUKuN|kh|ryP MkDVNlQyPTh5MEG=
DMS114 NIXVNlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LacGlEPTB;MD63N{DPxE1? NEnXUmQzPDF3OEewNS=>
NCI-N592 M2rJVGZ2dmO2aX;uJGF{e2G7 NFT6NVgxNjNxMT:zJO69VQ>? NX;IOG0{OjRiaB?= NYDqRllTcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NIPKS|EzPDF3OEewNS=>
GLC4 NGPFR4FHfW6ldHnvckBCe3OjeR?= MoPTNE4{NzFxMzFOwG0> NH3UZW4zPCCq NGmxWWZqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MWmyOFE2QDdyMR?=
NCI-H82 NUXLZldVTnWwY4Tpc44hSXO|YYm= NIXye3UxNjNxMT:zJO69VQ>? NXK5O3VYOjRiaB?= M4rEd4lv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MlzBNlQyPTh5MEG=
NCI-N592 NEPxV4hCeG:ydH;zbZMhSXO|YYm= Mkn2NE4{NzFxMzFOwG0> M3nCR|Q5KGh? MV\pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MY[yOFE2QDdyMR?=
GLC4 NXPwTpJHSXCxcITvd4l{KEG|c3H5 NFfrbmwxNjNxMT:zJO69VQ>? NELtNWs1QCCq Mn3GbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NEPi[ZkzPDF3OEewNS=>
NCI-H82 MnHQRZBweHSxc3nzJGF{e2G7 NHW4dogxNjNxMT:zJO69VQ>? MmLxOFghcA>? NYHaXGtPcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MmDiNlQyPTh5MEG=
CWR22Rv1  MmnWRZBweHSxc3nzJGF{e2G7 MYTJR|UxRTBwNEiyJO69VQ>? NFzLNXkzOzl2MkC5OS=>
CWR22Pc MV\BdI9xfG:|aYOgRZN{[Xl? M3rxfGlEPTB;MD60N|gh|ryP NV7kOGJxOjN7NEKwPVU>
PC-3 NG\u[nRCeG:ydH;zbZMhSXO|YYm= M3[3O2lEPTB;MT63OVUh|ryP MoTuNlM6PDJyOUW=
DU145 NGP5T2RCeG:ydH;zbZMhSXO|YYm= MW\JR|UxRTNwNUG3JO69VQ>? MnHtNlM6PDJyOUW=
RC165N NYfpXWp5SXCxcITvd4l{KEG|c3H5 M1PpTWlEPTB;Mj6wPFMh|ryP MYWyN|k1OjB7NR?=
ARPE19 MmLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETyTmJFVVOR Mm\BTWM2OD1{ND6zPEDPxE1? M{HCT|I{PTNzOUKx
HEK293 NWjpOm9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13BVWROW09? M3LzSWlEPTB;OD62O{DPxE1? NVnXXINoOjN3M{G5NlE>
KCNR MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHtOItFVVOR MY\JR|UxRTBwNE[g{txO Mn\JNlM2OzF7MkG=
SY5Y NITGOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInoN5BFVVOR NYHITFU3UUN3ME2wMlM3KM7:TR?= MVWyN|U{OTl{MR?=
BE2 NXiwVYhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLVVHlFVVOR MVfJR|UxRTBwN{Gg{txO Mo\pNlM2OzF7MkG=
AS MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjvfZdFVVOR NXzzd|dnUUN3ME2xMlU{KM7:TR?= NEHUXFEzOzV|MUmyNS=>
NGP NIDLfGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXTSG1UVw>? MXfJR|UxRTBwNU[g{txO NVfLOVZGOjN3M{G5NlE>
IMR32 M{fXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP6RnpuTE2VTx?= MV7JR|UxRTBwNk[g{txO M2H2fVI{PTNzOUKx
LAN5 MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDxdGNFVVOR MXvJR|UxRTFwMESg{txO M1X4SVI{PTNzOUKx
RH18 M2P6TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Gxc2ROW09? Mk\aTWM2OD1zLkSyJO69VQ>? MYqyN|U{OTl{MR?=
RH30 M1npUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnoSG1UVw>? Ml:wTWM2OD1zLkK1JO69VQ>? NX7LZ4I2OjN3M{G5NlE>
RH17 M1z6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r5b2ROW09? M4rjWmlEPTB;Mj61NUDPxE1? M2jXd|I{PTNzOUKx
RH28 M2PQbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHxTWpFVVOR NE\NRlRKSzVyPUSuNlgh|ryP M{CxPVI{PTNzOUKx
RH36 NHfjPFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvydYZ1TE2VTx?= NEC0fpNKSzVyPUWuN|ch|ryP MWWyN|U{OTl{MR?=
RH41 NXzRWpI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnEUXNQ MWTJR|UxRTBwNEig{txO M4HXb|I{PTNzOUKx
RD NFiwe2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPwfYdCTE2VTx?= NVLU[JhHUUN3ME20MlMzKM7:TR?= MYGyN|U{OTl{MR?=
TC32 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7EUXNQ NXvNcmtHUUN3ME2zMlg2KM7:TR?= M3jqOFI{PTNzOUKx
TC71 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVSxPFB4TE2VTx?= NH20b4pKSzVyPUSuN|Mh|ryP M1f4S|I{PTNzOUKx
KCNR NYjpN5Z2SXCxcITvd4l{KEG|c3H5 MonzNE42NzFwMD:yMlUh|ryP MkS5NlQhcA>? MnvGSG1UVw>? NUPGbmNKcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NWrHSFdKOjN3M{G5NlE>
SY5Y NVzKTZpVSXCxcITvd4l{KEG|c3H5 M2DaO|AvPS9zLkCvNk42KM7:TR?= Ml7VNlQhcA>? NYLPc3RWTE2VTx?= NF3vXodqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NXzWRmUyOjN3M{G5NlE>
Rh18 M1jRWGFxd3C2b4Ppd{BCe3OjeR?= MnnUNE42NzFwMD:yMlUh|ryP MWKyOEBp NH:2O|RFVVOR MnTCbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= M37vcVI{PTNzOUKx
TC32 NEnGNG1CeG:ydH;zbZMhSXO|YYm= NX3LU4VxOC53L{GuNE8zNjVizszN NXrOUHFCOjRiaB?= MWTEUXNQ MYLpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NXiyW|BYOjN3M{G5NlE>
KCNR MX;GeY5kfGmxbjDBd5NigQ>? NI\yXo8xNjVxMT6wM|IvPS93IN88US=> NVXyVXJ7OjRiaB?= MnjkSG1UVw>? M2rzOIlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u M2nB[lI{PTNzOUKx
SY5Y NYDiSmJrTnWwY4Tpc44hSXO|YYm= NF;lOVYxNjVxMT6wM|IvPS93IN88US=> M3LJbFI1KGh? MV;EUXNQ MXnpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MYmyN|U{OTl{MR?=
Rh18 MnXUSpVv[3Srb36gRZN{[Xl? M4nTPVAvPS9zLkCvNk42NzVizszN MoPwNlQhcA>? NUXkV48zTE2VTx?= MWLpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MkHHNlM2OzF7MkG=
TC32 M3PvT2Z2dmO2aX;uJGF{e2G7 MkftNE42NzFwMD:yMlUwPSEQvF2= MYmyOEBp M13sO2ROW09? MVnpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NWnjVZM2OjN3M{G5NlE>
TPC-1 NIfmSI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCxJOK2VQ>? M{XaNFAuPCCm MUDEUXNQ NVrwUplocW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOiCmIITy[YF1dWWwdB?= M2TLTVI{ODV4NEm5
MZ-CRC1  MoryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7scGpYOSEEtV2= MVWwMVUh\A>? MlTLSG1UVw>? Mn;vbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MmrUNlMxPTZ2OUm=
TT  MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETkOIoyKML3TR?= M1fhXlAuPCCm MmX1SG1UVw>? M2r3e4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NWWxXlZJOjNyNU[0PVk>
TPC-1 MWHGeY5kfGmxbjDBd5NigQ>? NGPHXFIyKML3TR?= NFjhbpM4OiCq NXfFXJNoTE2VTx?= M2mzUYlv\HWlZYOgS|Eh[myxY3vh[4U> NVSycVNYOjNyNU[0PVk>
MZ-CRC1  Mn\CSpVv[3Srb36gRZN{[Xl? NX\ifY06OSEEtV2= NYfocFZRPzJiaB?= NGfKO2dFVVOR Mm[4bY5lfWOnczDHNUBjdG:la3Hn[S=> NVTNbWJsOjNyNU[0PVk>
TT  NXPVZ45xTnWwY4Tpc44hSXO|YYm= M4O5UVEhyrWP MV63NkBp NVfKdmN3TE2VTx?= MYDpcoR2[2W|IFexJIJtd2OtYXfl MXmyN|A2PjR7OR?=
MZ-CRC1  NVLDNnR2SXCxcITvd4l{KEG|c3H5 NYnvR2loOSEEtV2= NGHHNoY1QCCq MWnEUXNQ MmHabY5lfWOnczDhdI9xfG:|aYO= MUmyN|A2PjR7OR?=
TT  MnfoRZBweHSxc3nzJGF{e2G7 NUPBVGNKOSEEtV2= MoD0OFghcA>? MnXVSG1UVw>? MmTBbY5lfWOnczDhdI9xfG:|aYO= MoXhNlMxPTZ2OUm=
HD-LM2 M3zncGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYeydmFzPzMkgJno MVjEUXNQ MnG2TWM2OD15Lki0OEDPxE1? M1PUSlIzQDJ7MEm0
L-428 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTtO|LjiImq MoO5SG1UVw>? MVXJR|UxRTdwOUS3JO69VQ>? NHLSfnczOjh{OUC5OC=>
KM-H2 MlLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfs[HhOPzMkgJno MnjySG1UVw>? MoO5TWM2OD1zLkOwPEDPxE1? MkPHNlI5OjlyOUS=
L-540 NHPCPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M324RVcz6oDLaB?= NFrrSG9FVVOR NF7XfYVKSzVyPUiuNlE3KM7:TR?= MXiyNlgzQTB7NB?=
HD-LM2 MWHGeY5kfGmxbjDBd5NigQ>? NYDPN5JSOC5zL{CuOU8yNzVizszN Ml7vO|LjiImq NFThdmJFVVOR MmLobY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MXqyNlgzQTB7NB?=
L-428 MYHGeY5kfGmxbjDBd5NigQ>? MYSwMlEwOC53L{GvOUDPxE1? Mon6O|LjiImq NVH0b4p2TE2VTx?= NF3id3pqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? M17nOVIzQDJ7MEm0
KM-H2 Mn;SSpVv[3Srb36gRZN{[Xl? NYnRZoRYOC5zL{CuOU8yNzVizszN MlrsO|LjiImq MYHEUXNQ M33JRYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NUP5[5p6OjJ6MkmwPVQ>
L-540 NYjDSIo1TnWwY4Tpc44hSXO|YYm= Mo[xNE4yNzBwNT:xM|Uh|ryP M2DTW|cz6oDLaB?= M130fmROW09? MU\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MmHqNlI5OjlyOUS=
HD-LM2 MXHBdI9xfG:|aYOgRZN{[Xl? MoDKNU82KM7:TR?= MYi3NwKBkWh? NXuwOWNwTE2VTx?= M4\RUYlv\HWlZYOgZZBweHSxc3nz NUnkW48{OjJ6MkmwPVQ>
L-428 NX3WcFA5SXCxcITvd4l{KEG|c3H5 NUnpTml{OS93IN88US=> NHLKc4E4OuLCiXi= MVXEUXNQ MnLUbY5lfWOnczDhdI9xfG:|aYO= M{fX[lIzQDJ7MEm0
KM-H2 NVjURWhpSXCxcITvd4l{KEG|c3H5 NGjEWGcyNzVizszN M4XWS|cz6oDLaB?= NYfJe45ETE2VTx?= M1rqcYlv\HWlZYOgZZBweHSxc3nz M1;BSVIzQDJ7MEm0
L-540 NEHZRVlCeG:ydH;zbZMhSXO|YYm= MVyxM|Uh|ryP NF3UTIU4OuLCiXi= M3yyeWROW09? NV3McI1LcW6mdXPld{BieG:ydH;zbZM> NYfKW4JWOjJ6MkmwPVQ>
U251-MG NFHn[4NHfW6ldHnvckBCe3OjeR?= MoLONUDDvU1? MWWwMVE3KGh? NXvFRoJtcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NGr1OVUzOjB{N{[5NS=>
U87-MG NVjYdox1TnWwY4Tpc44hSXO|YYm= M2\yNlEhyrWP M1TKeFAuOTZiaB?= MmTobY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NIn4dIczOjB{N{[5NS=>
4C8 MXvGeY5kfGmxbjDBd5NigQ>? NF\QSnAyKML3TR?= MkXrNE0yPiCq NFjpS2pqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NGXmNY0zOjB{N{[5NS=>
U251-MG M2jaVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGxM|ExKML3TR?= M3z0[VI1NzR6L{eyJIg> NEPRO4dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MnnxNlIxOjd4OUG=
U87-MG NU\xSmwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ThRlEwOTBiwsXN NHXSelQzPC92OD:3NkBp MWfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MXSyNlAzPzZ7MR?=
4C8 NIC1elhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUC1[I9COS9zMDFCuW0> M1nhOlI1NzR6L{eyJIg> NIrEN29qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NXSwR3lPOjJyMke2PVE>
U266 M4K0ZWFxd3C2b4Ppd{BCe3OjeR?= NWe1SlY6OC53LUKg{txO M3TXT|Q5Nzd{IHi= MW\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M3fneVIyOTZ2NUG3
Kms.11 NFPPZmtCeG:ydH;zbZMhSXO|YYm= Ml;nNE42NTJizszN NGXwWHI1QC95MjDo NYnaOIZCcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYrPfYJbOjFzNkS1NVc>
8226 NYO4TIFMSXCxcITvd4l{KEG|c3H5 Mn\iNE42NTJizszN NGfxfow1QC95MjDo NHfM[ldqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M{DjUFIyOTZ2NUG3

... 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