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
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 15 Publications

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 M3riPGZ2dmO2aX;uJGF{e2G7 NGHy[FY2KM7:TR?= MXK0PEBp NIXPXG1FVVOR NYrwNnM4[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NUDMdpRPOjV7NUS5O|Q>
LoVo  M{PQbWZ2dmO2aX;uJGF{e2G7 MnW2OUDPxE1? M2LpS|Q5KGh? M1;WeGROW09? MlH6Zoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n NXnBN4ZvOjV7NUS5O|Q>
HN5 NGTQeGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT4T4ppPzJiaB?= M{fabmVEPTB;Mz64NUDDuSBzLkm5JO69VQ>? M3rXbVI2QDFyMEGw
Cal33 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\kO|IhcA>? NYriSoFjTUN3ME2zMlM4KMLzIECuO|Uh|ryP NW\0c3BHOjV6MUCwNVA>
UM-22B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;t[JY4OiCq M3jVO2VEPTB;Mj62OkDDuSByLkK0JO69VQ>? NWrzdJRiOjV6MUCwNVA>
686LN NEjudnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkS0O|IhcA>? MVLFR|UxRTJwMEWgxtEhOS5|MzFOwG0> NH\zNokzPThzMECxNC=>
UM SCC-1 Ml6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVe3NkBp M{\reGVEPTB;MT62O{DDuSByLkSyJO69VQ>? M3\0XVI2QDFyMEGw
UM-22A NYnNcpA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n0OVczKGh? MoHhSWM2OD1zLkOyJOKyKDBwM{mg{txO MmDnNlU5OTByMUC=
OSC19 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPrSm84OiCq NWPheHlOTUN3ME2xMlI3KMLzIECuNlAh|ryP NVq5O45NOjV6MUCwNVA>
PCI-52 NGT3emhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDKZ3o4OiCq M1T0fmVEPTB;MT6wNEDDuSByLkC5JO69VQ>? MnK5NlU5OTByMUC=
PCI-15B NWPqZnVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqzO|IhcA>? MVPFR|UxRTBwOUmgxtEhOS55NDFOwG0> NYrhV2ZROjV6MUCwNVA>
UMSCC-1 NF7pXItHfW6ldHnvckBCe3OjeR?= M2\qN|AvODByNT2xMlYh|ryP NYL6PXllOjRiaB?= NVnEfYNk[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmTyNlU5OTByMUC=
Cal33 NEHnZ25HfW6ldHnvckBCe3OjeR?= Mnu2NE4xODB3LUOuPEDPxE1? MUCyOEBp NXHS[WQ{[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3\1fFI2QDFyMEGw
HH5 NFrXZ5hHfW6ldHnvckBCe3OjeR?= M3\OOlAvODByNT2zMlgh|ryP MVSyOEBp MkPHZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXqyOVgyODBzMB?=
UM-22A MXHGeY5kfGmxbjDBd5NigQ>? NVGyNphKOC5yMEC1MVEvPiEQvF2= M1K0OVI1KGh? M4[5e4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M372fVI2QDFyMEGw
A1847 NU\Yb4ZXTnWwY4Tpc44hSXO|YYm= M3HYfFAvODVvMUCg{txO NHq5T3ozPCCq NIP2NXFFVVORwrC= MlfsdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M{S4d|I2PjR4MEG1
OVCAR-5 NYjQRot5TnWwY4Tpc44hSXO|YYm= Mn;1NE4xPS1zMDFOwG0> MmnKNlQhcA>? MljSSG1UV8Li NW[yOZpbemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NEPvXnUzPTZ2NkCxOS=>
OVCAR-8 MWHGeY5kfGmxbjDBd5NigQ>? NXTRW49uOC5yNT2xNEDPxE1? Mnf5NlQhcA>? MmG2SG1UV8Li MYXy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= M3XoSVI2PjR4MEG1
MOVCAR-5447 MkfSSpVv[3Srb36gRZN{[Xl? M3fVb|AvODVvMUCg{txO MorDNlQhcA>? M3vaTWROW00EoB?= MX;y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NF21emozPTZ2NkCxOS=>
MOVCAR-5009 M2j5[2Z2dmO2aX;uJGF{e2G7 Mn7rNE4xPS1zMDFOwG0> NX3RdVNWOjRiaB?= NYDqR5U3TE2VT9Mg NFP4enFz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NX:xR3VoOjV4NE[wNVU>
A1847 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3zLZlAvODVvMUCg{txO M4XDcVczKGh? NHrTbVJFVVOR Mnz1doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MWWyOVY1PjBzNR?=
OVCAR-5 NYLqcYk4S2WubDDWbYFjcWyrdImgRZN{[Xl? NX\mUZQxOC5yNT2xNEDPxE1? MUK3NkBp MUfEUXNQ MmrFdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MofUNlU3PDZyMUW=
OVCAR-8  MV\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYOwMlA2NTFyIN88US=> NF\McVk4OiCq Mn\XSG1UVw>? MVfy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M3vXSFI2PjR4MEG1
OVCAR-5  NEjkSm5CeG:ydH;zbZMhSXO|YYm= MVewMlUwOS93IN88US=> NWDTc|B3PDhiaB?= MlTvSG1UVw>? M3zZV4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= Ml7VNlU3PDZyMUW=
OVCAR-8  NH7USoVCeG:ydH;zbZMhSXO|YYm= NXG0fGREOC53L{GvOUDPxE1? Ml\3OFghcA>? MnXpSG1UVw>? MX\pcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w NXLZVFQ{OjV4NE[wNVU>
AKRSL M2jXfmNmdGxiVnnhZoltcXS7IFHzd4F6 NEnHS2M4OiCq MkPXTWM2OO,:nkGwJO69VQ>? M3;a[VI2PTB2NkO1
PALJDL MnLSR4VtdCCYaXHibYxqfHliQYPzZZk> MlTnO|IhcA>? M{fMTWlEPTB;Mj60JO69VQ>? M3LzV|I2PTB2NkO1
MO4 MWHGeY5kfGmxbjDBd5NigQ>? NWnJ[otGOC53L{GvOUDPxE1? MVS2JIg> MUHpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> NVX0[ldYOjVzNEm1N|U>
DU145  NIL6WXNHfW6ldHnvckBCe3OjeR?= MlThNE0zODBibl2= M3nLS|EhcMLi Mni0d5VxeHKnc4Pld{BKVC14LXHjeIl3[XSnZDDTeIF1OyCjbnSgSXJMOS9{IIPp[45idGmwZx?= NU\ENXZtOjR3N{e5OFI>
DU145  NIKxRmhHfW6ldHnvckBCe3OjeR?= NYToR5U2QDByIH7N NFm0SXI4OiCq NHnXfWR{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= M4LNXlI1PTd5OUSy
CWR22Rv1 MXPGeY5kfGmxbjDBd5NigQ>? NXnDXodLQDByIH7N M33RVlczKGh? Ml3Rd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 MnrsNlQ2Pzd7NEK=
N592 NYHlU5JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfRV5FsUUN3ME2wMlg1KM7:TR?= M3S1[FI1OTV6N{Cx
H82 Mn\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwM{eg{txO MXGyOFE2QDdyMR?=
GLC4 NXrxVIFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFwN{mg{txO NXuwXJJSOjRzNUi3NFE>
H526 MnLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTDN2l{UUN3ME2zMlA5KM7:TR?= M3nheFI1OTV6N{Cx
H1173 NX3rdZBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjMRnpuUUN3ME2yMlM6KM7:TR?= M2Dkb|I1OTV6N{Cx
DMS114 Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzhbGlrUUN3ME2wMlc{KM7:TR?= NFrWXY8zPDF3OEewNS=>
NCI-N592 NX:4RpRZTnWwY4Tpc44hSXO|YYm= MUKwMlMwOS9|IN88US=> MmfCNlQhcA>? NX\FWXM{cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NUPKdowyOjRzNUi3NFE>
GLC4 NYna[ppFTnWwY4Tpc44hSXO|YYm= MV[wMlMwOS9|IN88US=> M1TTN|I1KGh? M3T6VYlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NYHkWolmOjRzNUi3NFE>
NCI-H82 MoDxSpVv[3Srb36gRZN{[Xl? NHLxencxNjNxMT:zJO69VQ>? M2XVRVI1KGh? MYLpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NIDFd2YzPDF3OEewNS=>
NCI-N592 NFHEXXZCeG:ydH;zbZMhSXO|YYm= MV[wMlMwOS9|IN88US=> NWLy[oU2PDhiaB?= MVzpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ M2X6[lI1OTV6N{Cx
GLC4 NWjVWWZtSXCxcITvd4l{KEG|c3H5 NIHSRnMxNjNxMT:zJO69VQ>? NYPEVFU5PDhiaB?= NFLGUJlqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| M4DvZVI1OTV6N{Cx
NCI-H82 NWm1OHU1SXCxcITvd4l{KEG|c3H5 Mmj3NE4{NzFxMzFOwG0> MoG1OFghcA>? NV7nN4tscW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NXX0PVdGOjRzNUi3NFE>
CWR22Rv1  MV;BdI9xfG:|aYOgRZN{[Xl? NYLzb5JQUUN3ME2wMlQ5OiEQvF2= NGPhV5UzOzl2MkC5OS=>
CWR22Pc NXS0fYhHSXCxcITvd4l{KEG|c3H5 M4LwO2lEPTB;MD60N|gh|ryP M3[0e|I{QTR{MEm1
PC-3 Mn\lRZBweHSxc3nzJGF{e2G7 NX7RfXpyUUN3ME2xMlc2PSEQvF2= MUmyN|k1OjB7NR?=
DU145 NHX3bWlCeG:ydH;zbZMhSXO|YYm= MXzJR|UxRTNwNUG3JO69VQ>? NV\DNHBFOjN7NEKwPVU>
RC165N Mn7jRZBweHSxc3nzJGF{e2G7 NHLkblBKSzVyPUKuNFg{KM7:TR?= NI\iUJEzOzl2MkC5OS=>
ARPE19 NVXnNlhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3l[mRFVVOR NGPVdmpKSzVyPUK0MlM5KM7:TR?= MWiyN|U{OTl{MR?=
HEK293 M3j1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4f5bmROW09? MWjJR|UxRThwNkeg{txO MmLBNlM2OzF7MkG=
KCNR NX3hUHZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDEUXNQ M4fhN2lEPTB;MD60OkDPxE1? NFu1OIszOzV|MUmyNS=>
SY5Y Mnn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPHSG1UVw>? NWr5eJFLUUN3ME2wMlM3KM7:TR?= NEPn[oszOzV|MUmyNS=>
BE2 M{PDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XUUWROW09? NYHUOI9LUUN3ME2wMlcyKM7:TR?= MoXDNlM2OzF7MkG=
AS M4rhOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTEUXNQ NGHNNZNKSzVyPUGuOVMh|ryP MX2yN|U{OTl{MR?=
NGP NX7XXYpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnEUXNQ NVTR[IlRUUN3ME2wMlU3KM7:TR?= NH73bFczOzV|MUmyNS=>
IMR32 NX;WSJBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULEUXNQ NVrmNot7UUN3ME2wMlY3KM7:TR?= M3;CZlI{PTNzOUKx
LAN5 NHH2PINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfEZXlkTE2VTx?= MmXETWM2OD1zLkC0JO69VQ>? NEi2b3AzOzV|MUmyNS=>
RH18 M1\Gd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HlbGROW09? NHPLS5dKSzVyPUGuOFIh|ryP M2HuXFI{PTNzOUKx
RH30 MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLEUXNQ MoS1TWM2OD1zLkK1JO69VQ>? MXGyN|U{OTl{MR?=
RH17 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLtNnpFVVOR MWjJR|UxRTJwNUGg{txO M4PLOFI{PTNzOUKx
RH28 NInoR2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHDSG1UVw>? MnHzTWM2OD12LkK4JO69VQ>? M3\5XFI{PTNzOUKx
RH36 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWqzTpk6TE2VTx?= M2O5bWlEPTB;NT6zO{DPxE1? M2n1eFI{PTNzOUKx
RH41 NVjzfZFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK5SG1UVw>? NFvxNWFKSzVyPUCuOFgh|ryP NITJdZEzOzV|MUmyNS=>
RD MoC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrncpdFVVOR Mne3TWM2OD12LkOyJO69VQ>? MYKyN|U{OTl{MR?=
TC32 NILHN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDISG1UVw>? NXq2elJSUUN3ME2zMlg2KM7:TR?= M3TjNFI{PTNzOUKx
TC71 NIHsfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorkSG1UVw>? M{jpOmlEPTB;ND6zN{DPxE1? MUeyN|U{OTl{MR?=
KCNR MoHuRZBweHSxc3nzJGF{e2G7 MoLTNE42NzFwMD:yMlUh|ryP MnjUNlQhcA>? M4LQcGROW09? M4L2PYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MW[yN|U{OTl{MR?=
SY5Y MnG4RZBweHSxc3nzJGF{e2G7 M4\GblAvPS9zLkCvNk42KM7:TR?= NX36cVQ3OjRiaB?= M12zUWROW09? MnnMbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= M1zQSlI{PTNzOUKx
Rh18 MYjBdI9xfG:|aYOgRZN{[Xl? NGTFVXYxNjVxMT6wM|IvPSEQvF2= NImxNZkzPCCq NFP0OYpFVVOR NV\WcnFycW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NWPLRZA1OjN3M{G5NlE>
TC32 NE\VT|ZCeG:ydH;zbZMhSXO|YYm= MVuwMlUwOS5yL{KuOUDPxE1? M{\u[FI1KGh? MX3EUXNQ MojNbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= M3fmSlI{PTNzOUKx
KCNR MofISpVv[3Srb36gRZN{[Xl? M2jQeFAvPS9zLkCvNk42NzVizszN MXyyOEBp NUTuemFUTE2VTx?= MonEbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NU\2WHl5OjN3M{G5NlE>
SY5Y Mk\QSpVv[3Srb36gRZN{[Xl? M4Oxb|AvPS9zLkCvNk42NzVizszN MljyNlQhcA>? MUTEUXNQ NGHEe3dqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MX[yN|U{OTl{MR?=
Rh18 NX;0RVF[TnWwY4Tpc44hSXO|YYm= MoPDNE42NzFwMD:yMlUwPSEQvF2= MlzzNlQhcA>? MlrYSG1UVw>? MUDpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NFnCdm0zOzV|MUmyNS=>
TC32 M33yNWZ2dmO2aX;uJGF{e2G7 MVKwMlUwOS5yL{KuOU82KM7:TR?= MmW0NlQhcA>? NUWzWHF1TE2VTx?= MmW5bY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MWqyN|U{OTl{MR?=
TPC-1 MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\oVJQyKML3TR?= M2q0RVAuPCCm NYi0W2pFTE2VTx?= MW\pcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 MX:yN|A2PjR7OR?=
MZ-CRC1  M4\xe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf6N28yKML3TR?= MkPGNE02KGR? Mkj1SG1UVw>? MkDHbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MXeyN|A2PjR7OR?=
TT  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxJOK2VQ>? MUiwMVQh\A>? NHfSbZZFVVOR MnHxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? M4XIV|I{ODV4NEm5
TPC-1 NFf6dnhHfW6ldHnvckBCe3OjeR?= MnPINUDDvU1? MlzrO|IhcA>? NXHq[|NKTE2VTx?= NFrqbVRqdmS3Y3XzJGcyKGKub3PrZYdm Mn7oNlMxPTZ2OUm=
MZ-CRC1  NWXpWmp6TnWwY4Tpc44hSXO|YYm= NHnqToIyKML3TR?= MV23NkBp MnKzSG1UVw>? NX3wWIZQcW6mdXPld{BIOSCkbH;jb4Fo\Q>? Ml;JNlMxPTZ2OUm=
TT  MULGeY5kfGmxbjDBd5NigQ>? MVixJOK2VQ>? NV:2e3FpPzJiaB?= NFHZZpZFVVOR M{i5S4lv\HWlZYOgS|Eh[myxY3vh[4U> M3ztUFI{ODV4NEm5
MZ-CRC1  NEfuTHBCeG:ydH;zbZMhSXO|YYm= MUexJOK2VQ>? NH\UUYo1QCCq MmX3SG1UVw>? Ml3IbY5lfWOnczDhdI9xfG:|aYO= MoDWNlMxPTZ2OUm=
TT  MlPWRZBweHSxc3nzJGF{e2G7 NUPJWZJsOSEEtV2= M{XsT|Q5KGh? M2rSUGROW09? NUTV[GV6cW6mdXPld{BieG:ydH;zbZM> MnTTNlMxPTZ2OUm=
HD-LM2 NWPUflBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXnPJpsPzMkgJno M3XV[WROW09? M1i1R2lEPTB;Nz64OFQh|ryP NGfoOVQzOjh{OUC5OC=>
L-428 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXG3NwKBkWh? M3;Bc2ROW09? M3:5c2lEPTB;Nz65OFch|ryP NX20VlBIOjJ6MkmwPVQ>
KM-H2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3ue4o4OuLCiXi= MVLEUXNQ NXLWNYlVUUN3ME2xMlMxQCEQvF2= NFLXWlkzOjh{OUC5OC=>
L-540 NYHXSWJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTPO|LjiImq M2mxdWROW09? MkDETWM2OD16LkKxOkDPxE1? M1rLN|IzQDJ7MEm0
HD-LM2 M1HRNmZ2dmO2aX;uJGF{e2G7 NG\xUGsxNjFxMD61M|EwPSEQvF2= MXy3NwKBkWh? Ml\FSG1UVw>? M1PWXYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MkX3NlI5OjlyOUS=
L-428 NXLGVJJkTnWwY4Tpc44hSXO|YYm= M1XDcVAvOS9yLkWvNU82KM7:TR?= MmrXO|LjiImq NXq4SW14TE2VTx?= M4LMOYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NVe2Sms2OjJ6MkmwPVQ>
KM-H2 NUK0R|hYTnWwY4Tpc44hSXO|YYm= NEX4SpAxNjFxMD61M|EwPSEQvF2= MlvwO|LjiImq NH[3[WZFVVOR M3X5ZYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NFm5N2YzOjh{OUC5OC=>
L-540 Mn;5SpVv[3Srb36gRZN{[Xl? NHv4[24xNjFxMD61M|EwPSEQvF2= MYK3NwKBkWh? NVy0TVYyTE2VTx?= MlnlbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NYjTSY5EOjJ6MkmwPVQ>
HD-LM2 MVLBdI9xfG:|aYOgRZN{[Xl? NHG2XXgyNzVizszN M4L4ZVcz6oDLaB?= NFm1OmNFVVOR NHPqOmJqdmS3Y3XzJIFxd3C2b4Ppdy=> MlTzNlI5OjlyOUS=
L-428 NHLjPWZCeG:ydH;zbZMhSXO|YYm= NVrTTI8xOS93IN88US=> M3nXO|cz6oDLaB?= NVqzXVhZTE2VTx?= M2Ttd4lv\HWlZYOgZZBweHSxc3nz Mlr4NlI5OjlyOUS=
KM-H2 NVG1T3VVSXCxcITvd4l{KEG|c3H5 NGny[VAyNzVizszN NYT0cFZYPzMkgJno NFn2fYRFVVOR MlzkbY5lfWOnczDhdI9xfG:|aYO= NIDBSFgzOjh{OUC5OC=>
L-540 NGezUYVCeG:ydH;zbZMhSXO|YYm= MY[xM|Uh|ryP MkSxO|LjiImq M3vYdmROW09? NHj4dmJqdmS3Y3XzJIFxd3C2b4Ppdy=> M4HXb|IzQDJ7MEm0
U251-MG NWTQXnVOTnWwY4Tpc44hSXO|YYm= NIPy[WEyKML3TR?= MUKwMVE3KGh? NWmz[plGcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NWjJU|B6OjJyMke2PVE>
U87-MG MX7GeY5kfGmxbjDBd5NigQ>? MnjqNUDDvU1? NXPUUZlYOC1zNjDo NFjxRZRqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? M4DDZlIzODJ5Nkmx
4C8 NIWzfWNHfW6ldHnvckBCe3OjeR?= MoD5NUDDvU1? NU\vO|FNOC1zNjDo Ml:wbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v M2XONlIzODJ5Nkmx
U251-MG NGjRNZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPnNU8yOCEEtV2= NGPxUmIzPC92OD:3NkBp NHXLR5ZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? M{XBTVIzODJ5Nkmx
U87-MG M13m[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPDSGwyNzFyINM1US=> MnuzNlQwPDhxN{KgbC=> M3rXSIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO Mo\1NlIxOjd4OUG=
4C8 NH;ZbW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[xM|ExKML3TR?= M13VVFI1NzR6L{eyJIg> NF;ZOmxqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NEWxUVUzOjB{N{[5NS=>
U266 NIHDeZNCeG:ydH;zbZMhSXO|YYm= MljPNE42NTJizszN NWftVpJmPDhxN{KgbC=> M4e2fIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NUPweWs6OjFzNkS1NVc>
Kms.11 NVPETVFYSXCxcITvd4l{KEG|c3H5 MoTJNE42NTJizszN MXu0PE84OiCq M3\DbIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NYqzd41TOjFzNkS1NVc>
8226 M4CwbGFxd3C2b4Ppd{BCe3OjeR?= Mnn4NE42NTJizszN NXLHV4dFPDhxN{KgbC=> MULpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NEfBZVczOTF4NEWxOy=>

... 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]
+ Expand
  • 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
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
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
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.

  • * Indicates a Required Field

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products4

Tags: buy AZD1480 | AZD1480 supplier | purchase AZD1480 | AZD1480 cost | AZD1480 manufacturer | order AZD1480 | AZD1480 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID