AZD1480

For research use only.

Catalog No.S2162

60 publications

AZD1480 Chemical Structure

Molecular Weight(MW): 348.77

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

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Selleck's AZD1480 has been cited by 60 publications

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 MnraSpVv[3Srb36gRZN{[Xl? MkDGOUDPxE1? NVe0cmJ2PDhiaB?= M2jSZmROW09? NX3Ffmtu[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o Mmj2NlU6PTR7N{S=
LoVo  NFfXdZpHfW6ldHnvckBCe3OjeR?= MkLOOUDPxE1? NU\qbZdXPDhiaB?= NIHTZmJFVVOR NXHGNIFn[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o M{nIfFI2QTV2OUe0
HN5 M4nnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfTfXY4OiCq MYfFR|UxRTNwOEGgxtEhOS57OTFOwG0> MnLINlU5OTByMUC=
Cal33 NY\LWVBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTGO|IhcA>? NHrCdYJGSzVyPUOuN|chyrFiMD63OUDPxE1? NUn4To9xOjV6MUCwNVA>
UM-22B NFzqNJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXiWYY4OiCq NXOyW3YxTUN3ME2yMlY3KMLzIECuNlQh|ryP NWTrdohPOjV6MUCwNVA>
686LN MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17US|czKGh? Mn6ySWM2OD1{LkC1JOKyKDFwM{Og{txO MkT6NlU5OTByMUC=
UM SCC-1 NYnpd4loT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlmxO|IhcA>? MnrCSWM2OD1zLk[3JOKyKDBwNEKg{txO MVGyOVgyODBzMB?=
UM-22A NXn0NIsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUO3NkBp NXf4dWZ7TUN3ME2xMlMzKMLzIECuN|kh|ryP NV3tWYZ{OjV6MUCwNVA>
OSC19 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrwO|IhcA>? NIezeoFGSzVyPUGuNlYhyrFiMD6yNEDPxE1? MoTKNlU5OTByMUC=
PCI-52 MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPvdok4OiCq MoDKSWM2OD1zLkCwJOKyKDBwMEmg{txO M4PWT|I2QDFyMEGw
PCI-15B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;0UVY4OiCq MoHvSWM2OD1yLkm5JOKyKDFwN{Sg{txO MWSyOVgyODBzMB?=
UMSCC-1 NWPO[YxtTnWwY4Tpc44hSXO|YYm= M1X0bFAvODByNT2xMlYh|ryP NU\IfIE4OjRiaB?= M{fSXIFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHLFU20zPThzMECxNC=>
Cal33 Mn\CSpVv[3Srb36gRZN{[Xl? NUn2WFV[OC5yMEC1MVMvQCEQvF2= NGDUVGkzPCCq M3vE[YFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mnz2NlU5OTByMUC=
HH5 M1TqfWZ2dmO2aX;uJGF{e2G7 MnLrNE4xODB3LUOuPEDPxE1? MnHxNlQhcA>? NXTUbFRO[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnjkNlU5OTByMUC=
UM-22A NIj4U2ZHfW6ldHnvckBCe3OjeR?= M3PabVAvODByNT2xMlYh|ryP MoPSNlQhcA>? NFH0c2Ri[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2PKTlI2QDFyMEGw
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OVCAR-5 MlfkSpVv[3Srb36gRZN{[Xl? NVrlfXRKOC5yNT2xNEDPxE1? MX[yOEBp NF;FcndFVVORwrC= M1q0R5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MmXkNlU3PDZyMUW=
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MOVCAR-5009 M3WzeGZ2dmO2aX;uJGF{e2G7 NXXX[ldsOC5yNT2xNEDPxE1? Mn31NlQhcA>? NH3MbpZFVVORwrC= Mn7WdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NUD2dGRoOjV4NE[wNVU>
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OVCAR-5 NV;JOnJiS2WubDDWbYFjcWyrdImgRZN{[Xl? NWHVcm5VOC5yNT2xNEDPxE1? MnfZO|IhcA>? MYHEUXNQ M3fxU5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN M1T0OVI2PjR4MEG1
OVCAR-8  M1i5OGNmdGxiVnnhZoltcXS7IFHzd4F6 M2nXb|AvODVvMUCg{txO NYjzOW1uPzJiaB?= NYPNeItGTE2VTx?= Mm\ZdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= M{nMNFI2PjR4MEG1
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OVCAR-8  M{XL[2Fxd3C2b4Ppd{BCe3OjeR?= M4rKTlAvPS9zL{Wg{txO MWK0PEBp MkGwSG1UVw>? M4HNb4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= NFu4OYczPTZ2NkCxOS=>
AKRSL MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVLjOXpMPzJiaB?= NUniRXYzUUN3MP-8olExKM7:TR?= NWfGVpJVOjV3MES2N|U>
PALJDL NIGyZnJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUK3NkBp NUHRUngyUUN3ME2yMlQh|ryP MWmyOVUxPDZ|NR?=
MO4 MYLGeY5kfGmxbjDBd5NigQ>? NULlfoEzOC53L{GvOUDPxE1? NGXPW|E3KGh? M2n0NIlvcGmkaYTzJHAuW1SDVEOg[ZhxemW|c3nvcuKh MY[yOVE1QTV|NR?=
DU145  MYfGeY5kfGmxbjDBd5NigQ>? MmDvNE0zODBibl2= NFvqfHgyKGkEoB?= MXPzeZBxemW|c3XzJGlNNTZvYXP0bZZifGWmIGP0ZZQ{KGGwZDDFVmsyNzJic3nncoFtcW6p NF3DcYkzPDV5N{m0Ni=>
DU145  NV62VFhKTnWwY4Tpc44hSXO|YYm= NXnQNlE3QDByIH7N Ml2zO|IhcA>? MX3zeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? NGjMNm8zPDV5N{m0Ni=>
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GLC4 NWewWYJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLXRXFMUUN3ME2xMlc6KM7:TR?= MljINlQyPTh5MEG=
H526 M17iZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j0fmlEPTB;Mz6wPEDPxE1? MkHuNlQyPTh5MEG=
H1173 M2ryNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrCTWM2OD1{LkO5JO69VQ>? NEjxOHMzPDF3OEewNS=>
DMS114 NVXMXIRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37OVWlEPTB;MD63N{DPxE1? NVHHcItvOjRzNUi3NFE>
NCI-N592 M{DUSGZ2dmO2aX;uJGF{e2G7 M{PHV|AvOy9zL{Og{txO NHrnOXEzPCCq M123eIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MYeyOFE2QDdyMR?=
GLC4 Ml3nSpVv[3Srb36gRZN{[Xl? NVXDNZBwOC5|L{GvN{DPxE1? MV2yOEBp NHHsN5VqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MWGyOFE2QDdyMR?=
NCI-H82 NVzr[ldqTnWwY4Tpc44hSXO|YYm= M{X1b|AvOy9zL{Og{txO MVGyOEBp NVLvdmZLcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NHT1T4szPDF3OEewNS=>
NCI-N592 MUnBdI9xfG:|aYOgRZN{[Xl? NHnQXlQxNjNxMT:zJO69VQ>? NX7DfoNRPDhiaB?= MnT3bY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NFnVWmozPDF3OEewNS=>
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NCI-H82 NWnSd3Z1SXCxcITvd4l{KEG|c3H5 NIq5Z2gxNjNxMT:zJO69VQ>? NVHXZ|l6PDhiaB?= NIPXVJdqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NX:xbpdIOjRzNUi3NFE>
CWR22Rv1  MWTBdI9xfG:|aYOgRZN{[Xl? MWHJR|UxRTBwNEiyJO69VQ>? M4nZTFI{QTR{MEm1
CWR22Pc M324fGFxd3C2b4Ppd{BCe3OjeR?= M1zCT2lEPTB;MD60N|gh|ryP NIXabWwzOzl2MkC5OS=>
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DU145 MoPyRZBweHSxc3nzJGF{e2G7 NEn3c4lKSzVyPUOuOVE4KM7:TR?= M3jlT|I{QTR{MEm1
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ARPE19 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPXSXdFVVOR NIH3[YlKSzVyPUK0MlM5KM7:TR?= MmTnNlM2OzF7MkG=
HEK293 MnfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3EUXNQ NX3k[4FQUUN3ME24MlY4KM7:TR?= MoHDNlM2OzF7MkG=
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AS NH60fndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj3UXZJTE2VTx?= Mn6yTWM2OD1zLkWzJO69VQ>? MoD3NlM2OzF7MkG=
NGP MoHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrEUXNQ NVP4[XBSUUN3ME2wMlU3KM7:TR?= NV7xV4tnOjN3M{G5NlE>
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RH18 NIC1PZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDVRXFFVVOR MkTNTWM2OD1zLkSyJO69VQ>? NGnlOG4zOzV|MUmyNS=>
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RH17 NXjtXWFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XTXGROW09? NYfLPIltUUN3ME2yMlUyKM7:TR?= MoHvNlM2OzF7MkG=
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RH36 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm4RpNzTE2VTx?= NGLrOW9KSzVyPUWuN|ch|ryP MnvXNlM2OzF7MkG=
RH41 M2fadWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[5[HlFVVOR MXTJR|UxRTBwNEig{txO MYKyN|U{OTl{MR?=
RD MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[5WnZFVVOR NIH5OIZKSzVyPUSuN|Ih|ryP M3HjTFI{PTNzOUKx
TC32 M2jUc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO4O5VFVVOR MVzJR|UxRTNwOEWg{txO MWGyN|U{OTl{MR?=
TC71 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYn4e5lSTE2VTx?= MkXuTWM2OD12LkOzJO69VQ>? Mlr3NlM2OzF7MkG=
KCNR M2fLN2Fxd3C2b4Ppd{BCe3OjeR?= NGXae5YxNjVxMT6wM|IvPSEQvF2= NGmxSVAzPCCq M1XUZmROW09? M3;rZolv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MXGyN|U{OTl{MR?=
SY5Y MoDtRZBweHSxc3nzJGF{e2G7 M1uzTVAvPS9zLkCvNk42KM7:TR?= M3:wOVI1KGh? NGntSYFFVVOR NXPyfVF{cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> M33kPFI{PTNzOUKx
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TC32 NWHJcHpmTnWwY4Tpc44hSXO|YYm= MWSwMlUwOS5yL{KuOU82KM7:TR?= MV:yOEBp Mnr5SG1UVw>? NVn1[4U1cW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MUOyN|U{OTl{MR?=
TPC-1 MofTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX6xJOK2VQ>? MUOwMVQh\A>? MlTqSG1UVw>? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 NFjadmozOzB3NkS5PS=>
MZ-CRC1  M2nsZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\2NUDDvU1? MnvMNE02KGR? MkXYSG1UVw>? MYrpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 MXWyN|A2PjR7OR?=
TT  MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;0clEhyrWP M2XVNVAuPCCm NVjlSVZPTE2VTx?= NWT4fIlicW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NWexRlNmOjNyNU[0PVk>
TPC-1 NIfGU25HfW6ldHnvckBCe3OjeR?= NFLDOoMyKML3TR?= NF2zdYg4OiCq M1TaS2ROW09? NE[5OINqdmS3Y3XzJGcyKGKub3PrZYdm MYGyN|A2PjR7OR?=
MZ-CRC1  MW\GeY5kfGmxbjDBd5NigQ>? NVm3dI15OSEEtV2= MWK3NkBp NEmzOndFVVOR Ml;pbY5lfWOnczDHNUBjdG:la3Hn[S=> NHvJOIUzOzB3NkS5PS=>
TT  MX;GeY5kfGmxbjDBd5NigQ>? M{X5ZlEhyrWP M1PmO|czKGh? NFvwUXNFVVOR NHzzU3RqdmS3Y3XzJGcyKGKub3PrZYdm MVWyN|A2PjR7OR?=
MZ-CRC1  NIPEemlCeG:ydH;zbZMhSXO|YYm= MnKzNUDDvU1? MUG0PEBp MnrxSG1UVw>? MYfpcoR2[2W|IHHwc5B1d3Orcx?= MnHZNlMxPTZ2OUm=
TT  M1zyUmFxd3C2b4Ppd{BCe3OjeR?= Mn;CNUDDvU1? NWnGVGU4PDhiaB?= Mle0SG1UVw>? M4rrOolv\HWlZYOgZZBweHSxc3nz MUKyN|A2PjR7OR?=
HD-LM2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPh[mY4OuLCiXi= M37IfGROW09? MkDCTWM2OD15Lki0OEDPxE1? NYfJSopHOjJ6MkmwPVQ>
L-428 NUXhUlBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYm3NwKBkWh? MnvNSG1UVw>? NWLNUWoyUUN3ME23Mlk1PyEQvF2= NEfxRmIzOjh{OUC5OC=>
KM-H2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG5O|LjiImq M3u5S2ROW09? NYmzUot7UUN3ME2xMlMxQCEQvF2= NILITGgzOjh{OUC5OC=>
L-540 MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1WyV|cz6oDLaB?= NIny[ldFVVOR NVvOOm1IUUN3ME24MlIyPiEQvF2= MkK0NlI5OjlyOUS=
HD-LM2 MVHGeY5kfGmxbjDBd5NigQ>? MmXwNE4yNzBwNT:xM|Uh|ryP NGPWbno4OuLCiXi= NULQeZp5TE2VTx?= M2O0TolvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v M{D3O|IzQDJ7MEm0
L-428 NXW0RoV2TnWwY4Tpc44hSXO|YYm= MYmwMlEwOC53L{GvOUDPxE1? MUm3NwKBkWh? NXfkV4k{TE2VTx?= NVnOU5l4cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MmCyNlI5OjlyOUS=
KM-H2 NYjqbIh4TnWwY4Tpc44hSXO|YYm= MX:wMlEwOC53L{GvOUDPxE1? M2PoTlcz6oDLaB?= MXPEUXNQ MorZbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MnPzNlI5OjlyOUS=
L-540 MUPGeY5kfGmxbjDBd5NigQ>? M3LSdlAvOS9yLkWvNU82KM7:TR?= MWW3NwKBkWh? NXz1[G42TE2VTx?= M{[zVYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MmizNlI5OjlyOUS=
HD-LM2 NYnJb4FDSXCxcITvd4l{KEG|c3H5 NG\OO|IyNzVizszN MY[3NwKBkWh? MWPEUXNQ M4j4cIlv\HWlZYOgZZBweHSxc3nz M4j6W|IzQDJ7MEm0
L-428 NX\p[JlNSXCxcITvd4l{KEG|c3H5 NXLQRod5OS93IN88US=> Ml:0O|LjiImq MkizSG1UVw>? M2XWXolv\HWlZYOgZZBweHSxc3nz NUDlW3hHOjJ6MkmwPVQ>
KM-H2 MoPTRZBweHSxc3nzJGF{e2G7 MoD2NU82KM7:TR?= MkLQO|LjiImq NXvtbIhUTE2VTx?= NVL6PYkycW6mdXPld{BieG:ydH;zbZM> M{DuSlIzQDJ7MEm0
L-540 NVnSOodSSXCxcITvd4l{KEG|c3H5 MoLRNU82KM7:TR?= NY\tbZRYPzMkgJno M2O2cGROW09? NWW1e|RycW6mdXPld{BieG:ydH;zbZM> MXGyNlgzQTB7NB?=
U251-MG MmjBSpVv[3Srb36gRZN{[Xl? MX[xJOK2VQ>? NY[2NIxsOC1zNjDo MkPNbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NV31SWMzOjJyMke2PVE>
U87-MG MWHGeY5kfGmxbjDBd5NigQ>? NX3HR5h5OSEEtV2= M1[5eVAuOTZiaB?= NIKxbIxqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MU[yNlAzPzZ7MR?=
4C8 NFPINHRHfW6ldHnvckBCe3OjeR?= MUCxJOK2VQ>? MYmwMVE3KGh? NX72NWdEcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NXHNPIpmOjJyMke2PVE>
U251-MG NGPCS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\XVm8yNzFyINM1US=> NID2dWwzPC92OD:3NkBp NEWwRZZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MUCyNlAzPzZ7MR?=
U87-MG MkXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXmXo0yNzFyINM1US=> NFzBbFgzPC92OD:3NkBp MWLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NVjESVZ2OjJyMke2PVE>
4C8 MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3VZ2V7OS9zMDFCuW0> MUmyOE81QC95MjDo MXTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> M3fOR|IzODJ5Nkmx
U266 M3jzWGFxd3C2b4Ppd{BCe3OjeR?= NXe4UnNZOC53LUKg{txO M3\HV|Q5Nzd{IHi= NGjHNoVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MmTXNlEyPjR3MUe=
Kms.11 NXLUZpBISXCxcITvd4l{KEG|c3H5 NXP4em5yOC53LUKg{txO NH;qdYs1QC95MjDo NYq0ZosxcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MWOyNVE3PDVzNx?=
8226 NF:4NGRCeG:ydH;zbZMhSXO|YYm= M{THc|AvPS1{IN88US=> NFXaRVM1QC95MjDo NYn0WZREcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MmPYNlEyPjR3MUe=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-JAK2 / JAK2 ; 

PubMed: 22027691     


Cells were treated with AZD1480 for the indicated times, lysed and immunoblotted with the indicated antibodies. 

p-STAT1 / STAT1 / p-STAT5 / STAT5 / p-STAT6 / STAT6 ; 

PubMed: 22829094     


Western blot assay of the four HL cell lines treated with increasing doses of AZD1480 (0.1–5 μM) for 72 h. 

p-ERK / ERK / p-p38 / p38 / SOCS3 / p-SHP2 / SHP2 ; 

PubMed: 22829094     


Representative western blot assay showing increased levels of ERK, p38 and SHP-2 phosphorylation in HD-LM2 and L-428, after treatment for 72 h with increasing doses of AZD1480 (0.1-5 μM). In contrast, L-540 showed a dose-dependent inhibition of ERK and p38 activation without increased SHP-2 phosphorylation. SOCS-3 levels decreased in all the cell lines.

22027691 22829094
Immunofluorescence
pSTAT5; 

PubMed: 30140255     


HepG2 cells were incubated in the presence of Pro-Gly (0.5 mM) and/or AZD1480 (1 μM) for 6 h and phospho-STAT5 translocation to nuclei was detected by ICC. Scale bar, 10 μm. The IP and ICC experiments were conducted independently for 3 times, with 3 replicates each time.

30140255
Growth inhibition assay
Cell proliferation ; 

PubMed: 22027691     


Cells were treated with AZD1480 for the indicated times, and the WST-1 cell proliferation assay performed. The 48 and 72 h time points were statistically significant. Data represent mean ± SD, replicates of three (**, p<0.001; ANOVA). 

Cell viability; 

PubMed: 25855603     


IL-3-independent Ba/F3 cells were treated with increasing concentrations of the JAK inhibitor AZD1480 showing submicromolar inhibition of proliferation.

22027691 25855603
In vivo AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. [1] In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. [3]AZD1480 blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis and metastasis in a human xenograft tumor model. [4] The Jak2 inhibitor, AZD1480, suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity. [5]

Protocol

Kinase Assay:[5]
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kinase assays:

Inhibition studies of AZD1480 are performed using recombinant Jak1, Jak2, or Jak3 under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/ml BSA, and 10 mM MgCl2. Jak3 enzyme is expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes are assayed in the presence of AZD1480 (10 point dose response, in triplicate, from 8.3 μM to 0.3 nM in half-log dilution steps) using 1.5 μM peptide substrate (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 and Jak3: FAM-SRCtide) and screened under their respective ATP Km (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) and approximated physiological ATP concentration of 5 mM. Phosphorylated and unphosphorylated peptides are separated and quantified by a Caliper LC3000 system for calculating percent inhibition.
Cell Research:[4]
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  • Cell lines: Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs
  • Concentrations: ~1 μM
  • Incubation Time: 48 or 24 hours
  • Method: Renca or 786-O cells are suspended in DMEM medium with 5% FBS , and seeded in 96-well plates (5×103 per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 hours. Cell viability is determined by MTS assay. Absorbance at 490 nm is measured with Mikrotek Laborsysteme. Mouse endothelial cells and splenic CD11b+/c- myeloid cells are enriched from tumor-bearing mice,and cultured in 5% FBS RPMI-1640 medium. HUVECs are cultured on collagen 1–coated plates in complete medium. All cells are treated with DMSO and AZD1480 at various doses for 24 hours. Cell viability is determined by counting cell number manually. All the experiments are repeated 3 times.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Female BALB/c and athymic nude (NCR - nu/nu) mice (7–8 weeks old)
  • 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
Smiles CC(NC1=NC=C(Cl)C(=N1)NC2=N[NH]C(=C2)C)C3=NC=C(F)C=N3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
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*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

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