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 NEPTR4dHfW6ldHnvckBCe3OjeR?= NVrNSIZEPSEQvF2= NHHxcJE1QCCq MVHEUXNQ M4jkZoJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MmHxNlU6PTR7N{S=
LoVo  MkXtSpVv[3Srb36gRZN{[Xl? NIPIWIw2KM7:TR?= MkDjOFghcA>? MlftSG1UVw>? NXOwTnNE[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NYjubJo1OjV7NUS5O|Q>
HN5 M4jLS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXW3NkBp MXrFR|UxRTNwOEGgxtEhOS57OTFOwG0> NW\tR2h[OjV6MUCwNVA>
Cal33 M2HEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHodng4OiCq NIO4eoFGSzVyPUOuN|chyrFiMD63OUDPxE1? MlPLNlU5OTByMUC=
UM-22B M1zPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy3NkBp NGS2NolGSzVyPUKuOlYhyrFiMD6yOEDPxE1? NHrNNYwzPThzMECxNC=>
686LN MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjZO|IhcA>? NH3ZbItGSzVyPUKuNFUhyrFiMT6zN{DPxE1? NFnkV2gzPThzMECxNC=>
UM SCC-1 MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVWybJJNPzJiaB?= NX:3VWExTUN3ME2xMlY4KMLzIECuOFIh|ryP MmDsNlU5OTByMUC=
UM-22A Ml3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP1N3Y4OiCq NWr6b4h7TUN3ME2xMlMzKMLzIECuN|kh|ryP MVWyOVgyODBzMB?=
OSC19 NGnZ[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr0NHNNPzJiaB?= MkLNSWM2OD1zLkK2JOKyKDBwMkCg{txO MkmyNlU5OTByMUC=
PCI-52 NYHhSGVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUO3NkBp MoW4SWM2OD1zLkCwJOKyKDBwMEmg{txO NXHRXYVxOjV6MUCwNVA>
PCI-15B NIXQOnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP5[IM4OiCq MUjFR|UxRTBwOUmgxtEhOS55NDFOwG0> MU[yOVgyODBzMB?=
UMSCC-1 NYfa[|l7TnWwY4Tpc44hSXO|YYm= NH3XZpcxNjByMEWtNU43KM7:TR?= NGDURoMzPCCq M2n2UYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3jpe|I2QDFyMEGw
Cal33 MWrGeY5kfGmxbjDBd5NigQ>? MV2wMlAxODVvMz64JO69VQ>? MVuyOEBp M1TaZoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYTOTGoxOjV6MUCwNVA>
HH5 M3PTbGZ2dmO2aX;uJGF{e2G7 NVTEUoI6OC5yMEC1MVMvQCEQvF2= NW\yR3gzOjRiaB?= MnX2ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{fuSlI2QDFyMEGw
UM-22A NUfmXYkzTnWwY4Tpc44hSXO|YYm= MUKwMlAxODVvMT62JO69VQ>? NWjxT5dmOjRiaB?= NUL3PIk1[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1KyUVI2QDFyMEGw
A1847 MmXlSpVv[3Srb36gRZN{[Xl? MmrkNE4xPS1zMDFOwG0> NUjSdZZtOjRiaB?= M3rDfmROW00EoB?= MmjFdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MWKyOVY1PjBzNR?=
OVCAR-5 NGfMcWdHfW6ldHnvckBCe3OjeR?= NUnUWWlrOC5yNT2xNEDPxE1? MVOyOEBp M2nj[GROW00EoB?= NWH2XotNemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MmDsNlU3PDZyMUW=
OVCAR-8 MoXQSpVv[3Srb36gRZN{[Xl? MnT3NE4xPS1zMDFOwG0> NGjueIIzPCCq MoCySG1UV8Li MoCxdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M4DxdlI2PjR4MEG1
MOVCAR-5447 M2DDWmZ2dmO2aX;uJGF{e2G7 M13GVFAvODVvMUCg{txO MXKyOEBp NILuRVlFVVORwrC= NXn2[2VZemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NILlRoIzPTZ2NkCxOS=>
MOVCAR-5009 M2PKVmZ2dmO2aX;uJGF{e2G7 Mk[yNE4xPS1zMDFOwG0> NIHHfYwzPCCq MmX3SG1UV8Li MVvy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NFv0Z3YzPTZ2NkCxOS=>
A1847 NHTWdZRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{nsTVAvODVvMUCg{txO NV;KW4RiPzJiaB?= NFL1S5hFVVOR NHLmVldz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> M2f1OVI2PjR4MEG1
OVCAR-5 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYOwMlA2NTFyIN88US=> NHj0bGE4OiCq M2fIbGROW09? NIrxSlRz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MmLyNlU3PDZyMUW=
OVCAR-8  NGfSdZBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFzqcHIxNjB3LUGwJO69VQ>? MnrJO|IhcA>? MXvEUXNQ MlPldoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MXmyOVY1PjBzNR?=
OVCAR-5  NYXlXldoSXCxcITvd4l{KEG|c3H5 NGDTS5AxNjVxMT:1JO69VQ>? NFLHRVI1QCCq MoTVSG1UVw>? NInC[5BqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u NVf2NIRnOjV4NE[wNVU>
OVCAR-8  MmrrRZBweHSxc3nzJGF{e2G7 M2rxelAvPS9zL{Wg{txO M3rxRlQ5KGh? NUjrVZF1TE2VTx?= NHjzfYlqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u NFTVfXgzPTZ2NkCxOS=>
AKRSL NInMfYVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHXYVGc4OiCq MUjJR|Ux97zgMUCg{txO NF7mcpEzPTVyNE[zOS=>
PALJDL M4L3dGNmdGxiVnnhZoltcXS7IFHzd4F6 Mk\ZO|IhcA>? M{DmRmlEPTB;Mj60JO69VQ>? M3TrU|I2PTB2NkO1
MO4 NYLUOWJCTnWwY4Tpc44hSXO|YYm= NEXOe5QxNjVxMT:1JO69VQ>? MV62JIg> MoT3bY5pcWKrdIOgVE1UXEGWMzDlfJBz\XO|aX;uxsA> NUL2RppQOjVzNEm1N|U>
DU145  NGWy[pFHfW6ldHnvckBCe3OjeR?= NFHJS24xNTJyMDDuUS=> MUSxJIjDqA>? M33x[pN2eHC{ZYPz[ZMhUUxvNj3hZ5RqfmG2ZXSgV5RifDNiYX7kJGVTUzFxMjDzbYdv[Wyrbne= MX[yOFU4Pzl2Mh?=
DU145  Mlj1SpVv[3Srb36gRZN{[Xl? NHzYOI05ODBibl2= M3TNRVczKGh? M1m2SpN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= MVyyOFU4Pzl2Mh?=
CWR22Rv1 MXfGeY5kfGmxbjDBd5NigQ>? MWO4NFAhdk1? NHfROJU4OiCq M2\iRpN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NHXnSGMzPDV5N{m0Ni=>
N592 MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO3bXpKSzVyPUCuPFQh|ryP MkjlNlQyPTh5MEG=
H82 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HTWGlEPTB;MT6zO{DPxE1? MX2yOFE2QDdyMR?=
GLC4 M{HKbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD4TWM2OD1zLke5JO69VQ>? NWjBNFVFOjRzNUi3NFE>
H526 M3PKVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHyeYNKSzVyPUOuNFgh|ryP MlPyNlQyPTh5MEG=
H1173 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XhPGlEPTB;Mj6zPUDPxE1? MmfJNlQyPTh5MEG=
DMS114 Mm\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwN{Og{txO MVuyOFE2QDdyMR?=
NCI-N592 MlXnSpVv[3Srb36gRZN{[Xl? MXmwMlMwOS9|IN88US=> NWi1d|BnOjRiaB?= MWfpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NH\5WlQzPDF3OEewNS=>
GLC4 M{TK[2Z2dmO2aX;uJGF{e2G7 NVz0NpRCOC5|L{GvN{DPxE1? MoHGNlQhcA>? M2K4Oolv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MknkNlQyPTh5MEG=
NCI-H82 MUHGeY5kfGmxbjDBd5NigQ>? NEnDPVcxNjNxMT:zJO69VQ>? M3jSO|I1KGh? MX7pcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> MXKyOFE2QDdyMR?=
NCI-N592 NF3JN2tCeG:ydH;zbZMhSXO|YYm= NV7RXGY4OC5|L{GvN{DPxE1? MkGxOFghcA>? MlHtbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MVuyOFE2QDdyMR?=
GLC4 MnHhRZBweHSxc3nzJGF{e2G7 NHS4VIQxNjNxMT:zJO69VQ>? NX;JeoVFPDhiaB?= NGPkW3VqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NGHtXZczPDF3OEewNS=>
NCI-H82 MX7BdI9xfG:|aYOgRZN{[Xl? M2Oy[FAvOy9zL{Og{txO NVjUdZpZPDhiaB?= NXfMRXo1cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NEXsZ|QzPDF3OEewNS=>
CWR22Rv1  MnPGRZBweHSxc3nzJGF{e2G7 NX[4PVJVUUN3ME2wMlQ5OiEQvF2= MVqyN|k1OjB7NR?=
CWR22Pc Ml;xRZBweHSxc3nzJGF{e2G7 MoXrTWM2OD1yLkSzPEDPxE1? MWSyN|k1OjB7NR?=
PC-3 NWPXblFGSXCxcITvd4l{KEG|c3H5 MWDJR|UxRTFwN{W1JO69VQ>? NXOxTlRiOjN7NEKwPVU>
DU145 MVPBdI9xfG:|aYOgRZN{[Xl? MlvITWM2OD1|LkWxO{DPxE1? NY[xOlRxOjN7NEKwPVU>
RC165N Mo\lRZBweHSxc3nzJGF{e2G7 NV\sNXNzUUN3ME2yMlA5OyEQvF2= MnjhNlM6PDJyOUW=
ARPE19 NGiwXHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzTXpBFVVOR M1X5cmlEPTB;MkSuN|gh|ryP Mln3NlM2OzF7MkG=
HEK293 M{m0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrEUXNQ MW\JR|UxRThwNkeg{txO NVHRR3hHOjN3M{G5NlE>
KCNR MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\2dZhHTE2VTx?= NFe2bXhKSzVyPUCuOFYh|ryP M4fRe|I{PTNzOUKx
SY5Y NGrPW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\1PHVFVVOR M1[1R2lEPTB;MD6zOkDPxE1? Mnz2NlM2OzF7MkG=
BE2 NYDGSGlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLqSG1UVw>? Ml\YTWM2OD1yLkexJO69VQ>? MVGyN|U{OTl{MR?=
AS NYr1OXhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXL6b3N1TE2VTx?= NHKyVWJKSzVyPUGuOVMh|ryP MmHMNlM2OzF7MkG=
NGP MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3UZZpFVVOR M4TlfWlEPTB;MD61OkDPxE1? MUSyN|U{OTl{MR?=
IMR32 NF;BcHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHQZXNFVVOR MkLWTWM2OD1yLk[2JO69VQ>? MUGyN|U{OTl{MR?=
LAN5 NXXKOGdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\sXGROW09? MXTJR|UxRTFwMESg{txO MUeyN|U{OTl{MR?=
RH18 NYTm[5ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHEUXNQ MW\JR|UxRTFwNEKg{txO MlzINlM2OzF7MkG=
RH30 Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjEUXNQ NI[0[2VKSzVyPUGuNlUh|ryP NFr4d28zOzV|MUmyNS=>
RH17 NELCdo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOySG1UVw>? M1;IdWlEPTB;Mj61NUDPxE1? M3iybFI{PTNzOUKx
RH28 NFrWZ|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULhUpBHTE2VTx?= NYDId2I5UUN3ME20MlI5KM7:TR?= M3j6N|I{PTNzOUKx
RH36 NViybFllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLEUXNQ NH[1XnNKSzVyPUWuN|ch|ryP MnLUNlM2OzF7MkG=
RH41 NVPRfpZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1[xTGROW09? M3G0ZmlEPTB;MD60PEDPxE1? NHTHUJozOzV|MUmyNS=>
RD MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmyfm02TE2VTx?= M{faNmlEPTB;ND6zNkDPxE1? M1zhO|I{PTNzOUKx
TC32 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjEUXNQ MVjJR|UxRTNwOEWg{txO NETwfHUzOzV|MUmyNS=>
TC71 NYXpNHlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLzOFBjTE2VTx?= MWPJR|UxRTRwM{Og{txO MXuyN|U{OTl{MR?=
KCNR NYLaNW9CSXCxcITvd4l{KEG|c3H5 M{\MUlAvPS9zLkCvNk42KM7:TR?= MlXwNlQhcA>? MoPuSG1UVw>? NXzsSYNjcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MmTXNlM2OzF7MkG=
SY5Y NELlPZRCeG:ydH;zbZMhSXO|YYm= MlPFNE42NzFwMD:yMlUh|ryP NIG5SFkzPCCq MUXEUXNQ NEfpbINqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 M{C2PFI{PTNzOUKx
Rh18 MV;BdI9xfG:|aYOgRZN{[Xl? NGOwNmcxNjVxMT6wM|IvPSEQvF2= NXfofo5sOjRiaB?= MVvEUXNQ NUHHO3RJcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MmHKNlM2OzF7MkG=
TC32 NYq5UZQ5SXCxcITvd4l{KEG|c3H5 M3;ibVAvPS9zLkCvNk42KM7:TR?= MmW4NlQhcA>? MnrhSG1UVw>? MlW5bY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NIK4dYUzOzV|MUmyNS=>
KCNR NF\BbpRHfW6ldHnvckBCe3OjeR?= NIDBUmExNjVxMT6wM|IvPS93IN88US=> MVuyOEBp MULEUXNQ MXfpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MnzvNlM2OzF7MkG=
SY5Y NXraOY1[TnWwY4Tpc44hSXO|YYm= NXy1V2hxOC53L{GuNE8zNjVxNTFOwG0> MkTBNlQhcA>? MlLlSG1UVw>? M1PIV4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u M2q1elI{PTNzOUKx
Rh18 NXPv[5VjTnWwY4Tpc44hSXO|YYm= Mlm2NE42NzFwMD:yMlUwPSEQvF2= NYnSOlRIOjRiaB?= NW\tOodQTE2VTx?= NHfPPFlqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NFzzW40zOzV|MUmyNS=>
TC32 MWLGeY5kfGmxbjDBd5NigQ>? NGXsbWkxNjVxMT6wM|IvPS93IN88US=> M1fhUFI1KGh? NH7wUm5FVVOR MnOxbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NF3peGkzOzV|MUmyNS=>
TPC-1 NEjjUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxJOK2VQ>? MmTTNE01KGR? MUfEUXNQ MlL2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? M{ezRVI{ODV4NEm5
MZ-CRC1  NGDS[G9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;mSlEhyrWP M4H2NFAuPSCm M3\BXGROW09? MljYbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MoezNlMxPTZ2OUm=
TT  M2juN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKxJOK2VQ>? M3O4XVAuPCCm M2DWW2ROW09? M2fZRolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NHLrbFkzOzB3NkS5PS=>
TPC-1 Mn;OSpVv[3Srb36gRZN{[Xl? M1zNcVEhyrWP NGDaV4Q4OiCq M4fxZmROW09? MUPpcoR2[2W|IFexJIJtd2OtYXfl MXWyN|A2PjR7OR?=
MZ-CRC1  NWDMNoRJTnWwY4Tpc44hSXO|YYm= NF\hNHcyKML3TR?= MWq3NkBp MY\EUXNQ MnTQbY5lfWOnczDHNUBjdG:la3Hn[S=> MXuyN|A2PjR7OR?=
TT  MVfGeY5kfGmxbjDBd5NigQ>? MnrHNUDDvU1? NX3hSJcxPzJiaB?= NX\sUJdSTE2VTx?= MlLvbY5lfWOnczDHNUBjdG:la3Hn[S=> NVjOTY96OjNyNU[0PVk>
MZ-CRC1  MkLCRZBweHSxc3nzJGF{e2G7 M1rlfFEhyrWP NHPZNWM1QCCq M{\mNGROW09? NUS1O|Z1cW6mdXPld{BieG:ydH;zbZM> M2TkZlI{ODV4NEm5
TT  NVvOfZRJSXCxcITvd4l{KEG|c3H5 MXyxJOK2VQ>? MmLnOFghcA>? MUPEUXNQ MWfpcoR2[2W|IHHwc5B1d3Orcx?= MkfGNlMxPTZ2OUm=
HD-LM2 MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVO3WGNSPzMkgJno Mn;GSG1UVw>? NWrzRnJPUUN3ME23Mlg1PCEQvF2= Ml7NNlI5OjlyOUS=
L-428 NHvDZ3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rUUVcz6oDLaB?= M3fV[mROW09? NGjPOFdKSzVyPUeuPVQ4KM7:TR?= M1rYT|IzQDJ7MEm0
KM-H2 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYm3NwKBkWh? M{D0NmROW09? MVfJR|UxRTFwM{C4JO69VQ>? NUXDSFlzOjJ6MkmwPVQ>
L-540 M3PLPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M134W|cz6oDLaB?= Ml7CSG1UVw>? NHfHZpFKSzVyPUiuNlE3KM7:TR?= NWX1RWNYOjJ6MkmwPVQ>
HD-LM2 NWfFNXJITnWwY4Tpc44hSXO|YYm= MVGwMlEwOC53L{GvOUDPxE1? NW[2UphlPzMkgJno NWDzTXZ1TE2VTx?= NH3mVmRqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NF;QSJkzOjh{OUC5OC=>
L-428 NFnIUnBHfW6ldHnvckBCe3OjeR?= M1yyO|AvOS9yLkWvNU82KM7:TR?= MXO3NwKBkWh? NHXWd2lFVVOR M33vdYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v Mlq1NlI5OjlyOUS=
KM-H2 MXfGeY5kfGmxbjDBd5NigQ>? MUOwMlEwOC53L{GvOUDPxE1? M2HGeFcz6oDLaB?= MW\EUXNQ NYjD[ZJlcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MXGyNlgzQTB7NB?=
L-540 MmeySpVv[3Srb36gRZN{[Xl? MY[wMlEwOC53L{GvOUDPxE1? M4\R[|cz6oDLaB?= MnjKSG1UVw>? MWrpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> M1HMVVIzQDJ7MEm0
HD-LM2 MY\BdI9xfG:|aYOgRZN{[Xl? MV[xM|Uh|ryP MnW2O|LjiImq M13j[mROW09? MnyybY5lfWOnczDhdI9xfG:|aYO= M1TyS|IzQDJ7MEm0
L-428 NVTpWG85SXCxcITvd4l{KEG|c3H5 MmjCNU82KM7:TR?= M{LITVcz6oDLaB?= NVLGbpV{TE2VTx?= MnfubY5lfWOnczDhdI9xfG:|aYO= NUnnR5k5OjJ6MkmwPVQ>
KM-H2 MmXFRZBweHSxc3nzJGF{e2G7 M3TPdVEwPSEQvF2= M3q0TVcz6oDLaB?= NV6y[2JNTE2VTx?= M{XPWIlv\HWlZYOgZZBweHSxc3nz MUSyNlgzQTB7NB?=
L-540 NVzNbJlLSXCxcITvd4l{KEG|c3H5 MoXzNU82KM7:TR?= M1[1S|cz6oDLaB?= NUPaemFpTE2VTx?= NUjWN3pFcW6mdXPld{BieG:ydH;zbZM> NVvGfZNLOjJ6MkmwPVQ>
U251-MG M{TmZWZ2dmO2aX;uJGF{e2G7 MU[xJOK2VQ>? NYHWTldjOC1zNjDo NGfQeXdqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? Mni5NlIxOjd4OUG=
U87-MG M3;I[WZ2dmO2aX;uJGF{e2G7 NF;ESIMyKML3TR?= NIDTVWQxNTF4IHi= NFPMO3lqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MYWyNlAzPzZ7MR?=
4C8 NGHQOIVHfW6ldHnvckBCe3OjeR?= M1fWdlEhyrWP MlfLNE0yPiCq MmLvbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NWP1foRxOjJyMke2PVE>
U251-MG NHiyRmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjLdFYyNzFyINM1US=> MmPGNlQwPDhxN{KgbC=> NYnpeFlIcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NUToem1nOjJyMke2PVE>
U87-MG M4rYbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nxR|EwOTBiwsXN NYK1ZVlYOjRxNEivO|IhcA>? NX[2cHZocW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NHfNbngzOjB{N{[5NS=>
4C8 NIHkeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfxOJozOS9zMDFCuW0> MnTPNlQwPDhxN{KgbC=> NV3pRmkycW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NF\icZkzOjB{N{[5NS=>
U266 M1\LbWFxd3C2b4Ppd{BCe3OjeR?= MUewMlUuOiEQvF2= M37NTFQ5Nzd{IHi= MYDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MVqyNVE3PDVzNx?=
Kms.11 M3GwPWFxd3C2b4Ppd{BCe3OjeR?= Mkf5NE42NTJizszN NV\2emlnPDhxN{KgbC=> M3LNW4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M2nMVlIyOTZ2NUG3
8226 M4TyW2Fxd3C2b4Ppd{BCe3OjeR?= NVi3dGs3OC53LUKg{txO M{XuVlQ5Nzd{IHi= MlrjbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= Ml3VNlEyPjR3MUe=

... Click to View More Cell Line Experimental Data

In vivo AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. [1] In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. [3]AZD1480 blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis and metastasis in a human xenograft tumor model. [4] The Jak2 inhibitor, AZD1480, suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity. [5]

Protocol

Kinase Assay:[5]
+ Expand

kinase assays:

Inhibition studies of AZD1480 are performed using recombinant Jak1, Jak2, or Jak3 under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/ml BSA, and 10 mM MgCl2. Jak3 enzyme is expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes are assayed in the presence of AZD1480 (10 point dose response, in triplicate, from 8.3 μM to 0.3 nM in half-log dilution steps) using 1.5 μM peptide substrate (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 and Jak3: FAM-SRCtide) and screened under their respective ATP Km (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) and approximated physiological ATP concentration of 5 mM. Phosphorylated and unphosphorylated peptides are separated and quantified by a Caliper LC3000 system for calculating percent inhibition.
Cell Research:[4]
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  • Cell lines: Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs
  • Concentrations: ~1 μM
  • Incubation Time: 48 or 24 hours
  • Method: Renca or 786-O cells are suspended in DMEM medium with 5% FBS , and seeded in 96-well plates (5×103 per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 hours. Cell viability is determined by MTS assay. Absorbance at 490 nm is measured with Mikrotek Laborsysteme. Mouse endothelial cells and splenic CD11b+/c- myeloid cells are enriched from tumor-bearing mice,and cultured in 5% FBS RPMI-1640 medium. HUVECs are cultured on collagen 1–coated plates in complete medium. All cells are treated with DMSO and AZD1480 at various doses for 24 hours. Cell viability is determined by counting cell number manually. All the experiments are repeated 3 times.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Female BALB/c and athymic nude (NCR - nu/nu) mice (7–8 weeks old)
  • Formulation: AZD1480 is suspended in water supplemented with 0.5% hypromellose and 0.1% Tween 80.
  • Dosages: Once a day at the dose of 50 mg/kg or twice daily at 30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL warmed (197.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 348.77
Formula

C14H14ClFN8

CAS No. 935666-88-9
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01219543 Terminated Solid Tumour|Advanced Solid Malignancies|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma|EGFR and/or ROS Mutant NSCLC|Lung Metastasis Carcinoma|Gastric Cancer AstraZeneca November 2010 Phase 1
NCT01112397 Terminated Solid Malignancies AstraZeneca April 2010 Phase 1
NCT00910728 Completed Primary Myelofibrosis (PMF)|Post-Polycythaemia Vera|Essential Thrombocythaemia Myelofibrosis AstraZeneca|University of Texas|New York City Hoffman Center|Gustave Roussy, Cancer Campus, Grand Paris May 2009 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID