AZD1480 化学構造
分子量: 348.77

高品質保証

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Quality Control & MSDS

製品説明

  • Compare JAK Inhibitors
    JAK製品生物活性の比較
  • 研究分野
  • AZD1480のメカニズム

製品の説明

生物活性

製品説明 AZD1480は、JAK1とJAK2の新しいATP競争的阻害剤で、IC50がそれぞれ 1.3 nM と 0.26 nMです。
ターゲット JAK2
IC50 0.26 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SW620 NEfafXBHfW6ldHnvckBCe3OjeR?= NXf3e4E1PSEQvF2= NVTuW4VrPDhiaB?= NVf3fm9uTE2VTx?= Mn3nZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n M1fT[|I2QTV2OUe0
LoVo  M1;pNWZ2dmO2aX;uJGF{e2G7 MkHOOUDPxE1? NFrseXo1QCCq MmewSG1UVw>? NEDlV3FjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NF;NN|QzPTl3NEm3OC=>
HN5 NEP6XZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;Pc|czKGh? M2LlXGVEPTB;Mz64NUDDuSBzLkm5JO69VQ>? NIrPOmQzPThzMECxNC=>
Cal33 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT3SHI4OiCq M1nWVWVEPTB;Mz6zO{DDuSByLke1JO69VQ>? NGnie|UzPThzMECxNC=>
UM-22B NV\0[mJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvrO|IhcA>? MWTFR|UxRTJwNk[gxtEhOC5{NDFOwG0> NEi4PYozPThzMECxNC=>
686LN MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXe3NkBp NEPiXpZGSzVyPUKuNFUhyrFiMT6zN{DPxE1? NXH0[Gl2OjV6MUCwNVA>
UM SCC-1 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzON5pwPzJiaB?= MoHVSWM2OD1zLk[3JOKyKDBwNEKg{txO NEnxTo8zPThzMECxNC=>
UM-22A MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[3NkBp NG\YTVhGSzVyPUGuN|IhyrFiMD6zPUDPxE1? NFHx[2szPThzMECxNC=>
OSC19 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\UZos4OiCq NGmxUmRGSzVyPUGuNlYhyrFiMD6yNEDPxE1? MVeyOVgyODBzMB?=
PCI-52 M4T0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7yO|IhcA>? NWXVeZVETUN3ME2xMlAxKMLzIECuNFkh|ryP NWK3WVJJOjV6MUCwNVA>
PCI-15B MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUW3NkBp MkDOSWM2OD1yLkm5JOKyKDFwN{Sg{txO MlvTNlU5OTByMUC=
UMSCC-1 MoPFSpVv[3Srb36gRZN{[Xl? MXmwMlAxODVvMT62JO69VQ>? NGTUNmwzPCCq M{HjRYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFXGTm0zPThzMECxNC=>
Cal33 MoDpSpVv[3Srb36gRZN{[Xl? NV;TfodyOC5yMEC1MVMvQCEQvF2= M{DXTFI1KGh? MUThZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFi1TIkzPThzMECxNC=>
HH5 Mny5SpVv[3Srb36gRZN{[Xl? NI[1d3oxNjByMEWtN{45KM7:TR?= MXqyOEBp NXLLdo9s[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVH1ZWN1OjV6MUCwNVA>
UM-22A NVzUdVQ6TnWwY4Tpc44hSXO|YYm= MVWwMlAxODVvMT62JO69VQ>? NFj6NoszPCCq MUfhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mmm1NlU5OTByMUC=
A1847 NIrIVWhHfW6ldHnvckBCe3OjeR?= NVvacmxOOC5yNT2xNEDPxE1? NI\hWIUzPCCq MVPEUXNQyqB? MkDDdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NXrsZnJ5OjV4NE[wNVU>
OVCAR-5 NVe5dVN[TnWwY4Tpc44hSXO|YYm= MkXENE4xPS1zMDFOwG0> MkH3NlQhcA>? MXvEUXNQyqB? M{PGW5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MnPjNlU3PDZyMUW=
OVCAR-8 NEG4eGlHfW6ldHnvckBCe3OjeR?= MmnjNE4xPS1zMDFOwG0> M{L5bVI1KGh? Mon1SG1UV8Li MoLvdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M2jlNVI2PjR4MEG1
MOVCAR-5447 M2i1WmZ2dmO2aX;uJGF{e2G7 MoHUNE4xPS1zMDFOwG0> MX2yOEBp MWLEUXNQyqB? MlThdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= Ml3UNlU3PDZyMUW=
MOVCAR-5009 NVPQSo4zTnWwY4Tpc44hSXO|YYm= NXv0NpJjOC5yNT2xNEDPxE1? MYeyOEBp NHHZPI9FVVORwrC= M2TrNJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz M3fWTVI2PjR4MEG1
A1847 MnzYR4VtdCCYaXHibYxqfHliQYPzZZk> NELUXlIxNjB3LUGwJO69VQ>? MUi3NkBp MYLEUXNQ M4\G[ZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MWiyOVY1PjBzNR?=
OVCAR-5 M1jEWWNmdGxiVnnhZoltcXS7IFHzd4F6 MWKwMlA2NTFyIN88US=> M{C5[VczKGh? NYP4[|Z{TE2VTx?= NY\GeWpKemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> M2\3clI2PjR4MEG1
OVCAR-8  MnLpR4VtdCCYaXHibYxqfHliQYPzZZk> M3jrSFAvODVvMUCg{txO NGXBVIQ4OiCq NID0N|hFVVOR MlHWdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MViyOVY1PjBzNR?=
OVCAR-5  NXfVdFdESXCxcITvd4l{KEG|c3H5 NGPpPFgxNjVxMT:1JO69VQ>? MnLuOFghcA>? NV7EXppqTE2VTx?= M1;mbIlv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= M2HjdVI2PjR4MEG1
OVCAR-8  NVLUR|dxSXCxcITvd4l{KEG|c3H5 NVXiVld7OC53L{GvOUDPxE1? NGTTOJM1QCCq MkfxSG1UVw>? NXXCUlFqcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M{TMXVI2PjR4MEG1
AKRSL M{jxc2NmdGxiVnnhZoltcXS7IFHzd4F6 NXz2Z3kxPzJiaB?= NHXpN|ZKSzVy78{eNVAh|ryP MoTKNlU2ODR4M{W=
PALJDL MlTNR4VtdCCYaXHibYxqfHliQYPzZZk> NX3rRpBxPzJiaB?= NHrTd45KSzVyPUKuOEDPxE1? NYfPXWVWOjV3MES2N|U>
MO4 NH7BWGlHfW6ldHnvckBCe3OjeR?= MWOwMlUwOS93IN88US=> NFLWd3g3KGh? MWHpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> NWXpOXNmOjVzNEm1N|U>
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DU145  MX\GeY5kfGmxbjDBd5NigQ>? M3\lWFgxOCCwTR?= NGPsbmY4OiCq M3TESJN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NH;pSmkzPDV5N{m0Ni=>
CWR22Rv1 NUfpS3l1TnWwY4Tpc44hSXO|YYm= M2HYTVgxOCCwTR?= MVm3NkBp MUfzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? NX7k[2FNOjR3N{e5OFI>
N592 M2f3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4CxSWlEPTB;MD64OEDPxE1? NGPLb2UzPDF3OEewNS=>
H82 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXjWFRKSzVyPUGuN|ch|ryP MVSyOFE2QDdyMR?=
GLC4 M4[wVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjEPVhCUUN3ME2xMlc6KM7:TR?= M3TLT|I1OTV6N{Cx
H526 NXXJc4xVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\ScJlKSzVyPUOuNFgh|ryP MlWwNlQyPTh5MEG=
H1173 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJwM{mg{txO MVWyOFE2QDdyMR?=
DMS114 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHKRnl4UUN3ME2wMlc{KM7:TR?= NY\kd2xtOjRzNUi3NFE>
NCI-N592 MYjGeY5kfGmxbjDBd5NigQ>? MnWzNE4{NzFxMzFOwG0> NYHifVMxOjRiaB?= NGPqOFhqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NGrUZ2czPDF3OEewNS=>
GLC4 MorVSpVv[3Srb36gRZN{[Xl? NUTMPYNkOC5|L{GvN{DPxE1? NYfDN5Q4OjRiaB?= NHHJOW9qdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? M{jTelI1OTV6N{Cx
NCI-H82 NUPEPYJKTnWwY4Tpc44hSXO|YYm= NUXoVVM4OC5|L{GvN{DPxE1? NInJR|IzPCCq M36wcolv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NFHqVm0zPDF3OEewNS=>
NCI-N592 MlzxRZBweHSxc3nzJGF{e2G7 NF\Cfm4xNjNxMT:zJO69VQ>? Mmq0OFghcA>? Mnq0bY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? M{DwcFI1OTV6N{Cx
GLC4 NHHQU5NCeG:ydH;zbZMhSXO|YYm= NE[1[|AxNjNxMT:zJO69VQ>? NWT3UYR1PDhiaB?= M3fmV4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NHfscWEzPDF3OEewNS=>
NCI-H82 MmnWRZBweHSxc3nzJGF{e2G7 NWC0fHN6OC5|L{GvN{DPxE1? M1LPR|Q5KGh? NHuyWVFqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MX:yOFE2QDdyMR?=
CWR22Rv1  NF6z[FRCeG:ydH;zbZMhSXO|YYm= MnjITWM2OD1yLkS4NkDPxE1? M1;SR|I{QTR{MEm1
CWR22Pc NWT1PJFMSXCxcITvd4l{KEG|c3H5 NGTFUpdKSzVyPUCuOFM5KM7:TR?= NX[2N5NmOjN7NEKwPVU>
PC-3 M{[5cmFxd3C2b4Ppd{BCe3OjeR?= MWrJR|UxRTFwN{W1JO69VQ>? M3v3XVI{QTR{MEm1
DU145 MmjIRZBweHSxc3nzJGF{e2G7 NHLrVW1KSzVyPUOuOVE4KM7:TR?= M3TsTFI{QTR{MEm1
RC165N MmO1RZBweHSxc3nzJGF{e2G7 MkLnTWM2OD1{LkC4N{DPxE1? MkewNlM6PDJyOUW=
ARPE19 Ml\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu3emlFVVOR MlGxTWM2OD1{ND6zPEDPxE1? MoG0NlM2OzF7MkG=
HEK293 Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Hy[WROW09? NWTlWoZzUUN3ME24MlY4KM7:TR?= NYH4e4ZvOjN3M{G5NlE>
KCNR NWO2PIJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3TSG1UVw>? MVXJR|UxRTBwNE[g{txO MknFNlM2OzF7MkG=
SY5Y MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDKSG1UVw>? MVTJR|UxRTBwM{[g{txO MkW5NlM2OzF7MkG=
BE2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT2SG1UVw>? NGG3d|lKSzVyPUCuO|Eh|ryP NWrOXXpuOjN3M{G5NlE>
AS NYr0ZpZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;EUXNQ NFfjcIpKSzVyPUGuOVMh|ryP MWmyN|U{OTl{MR?=
NGP M2XJbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlSzSG1UVw>? M2T1U2lEPTB;MD61OkDPxE1? NHvEeXEzOzV|MUmyNS=>
IMR32 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLiSG1UVw>? MXLJR|UxRTBwNk[g{txO MYOyN|U{OTl{MR?=
LAN5 MonxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrIdoFFVVOR M2TkfmlEPTB;MT6wOEDPxE1? Mn;iNlM2OzF7MkG=
RH18 NHzI[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofQSG1UVw>? NFjTTHBKSzVyPUGuOFIh|ryP MVSyN|U{OTl{MR?=
RH30 NFHuNGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXtNpBFVVOR NV60boo5UUN3ME2xMlI2KM7:TR?= M{iyNlI{PTNzOUKx
RH17 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2P3XmROW09? NFfQbWNKSzVyPUKuOVEh|ryP NVK5UmR1OjN3M{G5NlE>
RH28 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GyR2ROW09? MYrJR|UxRTRwMkig{txO NX\NOYFQOjN3M{G5NlE>
RH36 NGjXfWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvtSG1UVw>? M2\oUWlEPTB;NT6zO{DPxE1? MoDxNlM2OzF7MkG=
RH41 M3fmXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\TU|RFVVOR NUPzeFh7UUN3ME2wMlQ5KM7:TR?= MkjuNlM2OzF7MkG=
RD Mmf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHEUXNQ NIXYcIpKSzVyPUSuN|Ih|ryP MXmyN|U{OTl{MR?=
TC32 M1HaUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DsNGROW09? NF\FZ4RKSzVyPUOuPFUh|ryP NV;CWnV1OjN3M{G5NlE>
TC71 NUDjfWpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fEPWROW09? NF;NTGhKSzVyPUSuN|Mh|ryP NEC3cYIzOzV|MUmyNS=>
KCNR Ml\BRZBweHSxc3nzJGF{e2G7 NXfQVIdNOC53L{GuNE8zNjVizszN Mny2NlQhcA>? M4DTVGROW09? Mnj2bY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NGXwfGYzOzV|MUmyNS=>
SY5Y NU\6c|R3SXCxcITvd4l{KEG|c3H5 M2DRbVAvPS9zLkCvNk42KM7:TR?= NUfBUIN7OjRiaB?= MmnhSG1UVw>? NV3MOW83cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MXWyN|U{OTl{MR?=
Rh18 NV\rc5lHSXCxcITvd4l{KEG|c3H5 NIjCRYMxNjVxMT6wM|IvPSEQvF2= Mn3zNlQhcA>? NV:xR3FlTE2VTx?= M3jVXYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= Mnj5NlM2OzF7MkG=
TC32 M1vPfmFxd3C2b4Ppd{BCe3OjeR?= NIfhZYsxNjVxMT6wM|IvPSEQvF2= NWXveWpkOjRiaB?= Mn:ySG1UVw>? MlezbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NHLWfHEzOzV|MUmyNS=>
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SY5Y MXrGeY5kfGmxbjDBd5NigQ>? NUS5U2J[OC53L{GuNE8zNjVxNTFOwG0> M2i1TVI1KGh? NWHpcmtQTE2VTx?= MnThbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MYCyN|U{OTl{MR?=
Rh18 NWT4PYZzTnWwY4Tpc44hSXO|YYm= MXOwMlUwOS5yL{KuOU82KM7:TR?= MWGyOEBp M{nmR2ROW09? MmDpbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NUjFXJp6OjN3M{G5NlE>
TC32 MUXGeY5kfGmxbjDBd5NigQ>? NYrJT4tSOC53L{GuNE8zNjVxNTFOwG0> NWP3RmZXOjRiaB?= M{HEWmROW09? NWq2WVRmcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MoG3NlM2OzF7MkG=
TPC-1 NUTt[lY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHGOFQyKML3TR?= MXOwMVQh\A>? Ml6zSG1UVw>? NEjwdJFqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAzKGRidILlZZRu\W62 M4TXfFI{ODV4NEm5
MZ-CRC1  MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33MUVEhyrWP M3PUVlAuPSCm MnHRSG1UVw>? NIjOTpBqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MkTPNlMxPTZ2OUm=
TT  M2TrUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnzOoFYOSEEtV2= MXiwMVQh\A>? MVfEUXNQ M{jYO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MW[yN|A2PjR7OR?=
TPC-1 MljMSpVv[3Srb36gRZN{[Xl? MknFNUDDvU1? MVi3NkBp NELt[GZFVVOR NGWx[Y1qdmS3Y3XzJGcyKGKub3PrZYdm MnXqNlMxPTZ2OUm=
MZ-CRC1  NGCzOYtHfW6ldHnvckBCe3OjeR?= MUKxJOK2VQ>? M{DFUlczKGh? M17ofGROW09? NHPhfFRqdmS3Y3XzJGcyKGKub3PrZYdm M1[0flI{ODV4NEm5
TT  MoXtSpVv[3Srb36gRZN{[Xl? MkPWNUDDvU1? MXG3NkBp NX65PGpQTE2VTx?= NH\NOVRqdmS3Y3XzJGcyKGKub3PrZYdm M4e4XVI{ODV4NEm5
MZ-CRC1  NH;FXlhCeG:ydH;zbZMhSXO|YYm= NF\iVXoyKML3TR?= M4my[|Q5KGh? M1i3dmROW09? NYnBSYZrcW6mdXPld{BieG:ydH;zbZM> MVqyN|A2PjR7OR?=
TT  MVHBdI9xfG:|aYOgRZN{[Xl? NFLuNVAyKML3TR?= NXnOO4ZiPDhiaB?= M17VVmROW09? NV\qcHhpcW6mdXPld{BieG:ydH;zbZM> MorGNlMxPTZ2OUm=
HD-LM2 NXm0S2xHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jqWFcz6oDLaB?= NUXGXWNWTE2VTx?= NG\uOFhKSzVyPUeuPFQ1KM7:TR?= NIW5dYgzOjh{OUC5OC=>
L-428 Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnEZYFlPzMkgJno NWL1PWo1TE2VTx?= MXzJR|UxRTdwOUS3JO69VQ>? MWWyNlgzQTB7NB?=
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HD-LM2 MXvGeY5kfGmxbjDBd5NigQ>? NHvJSYoxNjFxMD61M|EwPSEQvF2= NUDr[oVCPzMkgJno NYX0SJdZTE2VTx?= Ml3ObY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NFTXVZkzOjh{OUC5OC=>
L-428 M2qxS2Z2dmO2aX;uJGF{e2G7 M4XlNVAvOS9yLkWvNU82KM7:TR?= NHHEbYc4OuLCiXi= M2[yNWROW09? MUTpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MmPCNlI5OjlyOUS=
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L-540 NWPKT2pxTnWwY4Tpc44hSXO|YYm= NWezbVlmOC5zL{CuOU8yNzVizszN M3nuWFcz6oDLaB?= MmnmSG1UVw>? Mm\mbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NUf4bpBOOjJ6MkmwPVQ>
HD-LM2 NHz2NZVCeG:ydH;zbZMhSXO|YYm= MVSxM|Uh|ryP NFPvfIk4OuLCiXi= M3zScGROW09? MV\pcoR2[2W|IHHwc5B1d3Orcx?= M370e|IzQDJ7MEm0
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4C8 NXLEbHdmTnWwY4Tpc44hSXO|YYm= M{nm[lEhyrWP M4\EWlAuOTZiaB?= NV\rOYxqcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w M2m1UVIzODJ5Nkmx
U251-MG M3rCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYGy[ot6OS9zMDFCuW0> NVzmV5pSOjRxNEivO|IhcA>? NVPrbnh5cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NH3nXJYzOjB{N{[5NS=>
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4C8 NWHDcpk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jlWlEwOTBiwsXN MUSyOE81QC95MjDo NUHNZWNTcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NUOwV5NwOjJyMke2PVE>
U266 NUDsdWg6SXCxcITvd4l{KEG|c3H5 M37XcVAvPS1{IN88US=> MWW0PE84OiCq NHvNTVJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MlW1NlEyPjR3MUe=
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8226 NH;6S3lCeG:ydH;zbZMhSXO|YYm= NX\NclRuOC53LUKg{txO NFHGb4c1QC95MjDo MY\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NETsWHYzOTF4NEWxOy=>

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 AZD1480 is currently in Phase I clinical trials in Asian Patients With Advanced Solid Malignancies and Asian Patients With Advanced Hepatocellular Carcinoma (HCC)
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [5]

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.

細胞アッセイ: [4]

細胞株 Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs
濃度 ~1 μM
反応時間 48 or 24 hours
実験の流れ 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.

動物実験: [4]

動物モデル Female BALB/c and athymic nude (NCR - nu/nu) mice (7–8 weeks old)
製剤 AZD1480 is suspended in water supplemented with 0.5% hypromellose and 0.1% Tween 80.
投薬量 Once a day at the dose of 50 mg/kg or twice daily at 30 mg/kg
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download AZD1480 SDF
分子量 348.77
化学式

C14H14ClFN8

CAS No. 935666-88-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 69 mg/mL warming (197.83 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 (S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine

カスタマーフィードバック (2)


Click to enlarge
Rating
Source , , Nat Cell Biol, 2015, 17(1): 57-67. AZD1480 purchased from Selleck
Method bDNA Analysis
Cell Lines PSC-WA
Concentrations 0.1-5 μM
Incubation Time
Results Three other JAK1/2 inhibitors, AZD1480, CYT387 and Baricitinib, also showed up-regulation of UCP1 expression.

Click to enlarge
Rating
Source M.Sc. Karoline Gaebler and Dr. Claude Haan of Université du Luxembour. AZD1480 purchased from Selleck
Method Western blot
Cell Lines HEL cells
Concentrations 0-10 μM
Incubation Time 3 h
Results AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar concentrations in intact cells.

文献中の引用 (12)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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