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 MXTGeY5kfGmxbjDBd5NigQ>? NHjjOXI2KM7:TR?= NGHsXXQ1QCCq NFzOVZlFVVOR NFLJb5VjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> M1G4N|I2QTV2OUe0
LoVo  MlPQSpVv[3Srb36gRZN{[Xl? M4\v[lUh|ryP M{WyPVQ5KGh? NYDGOGZSTE2VTx?= NEXRd2ZjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NEDsUZUzPTl3NEm3OC=>
HN5 NUnoO21ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[zeIM3PzJiaB?= NHO3VoJGSzVyPUOuPFEhyrFiMT65PUDPxE1? NVXuTpR5OjV6MUCwNVA>
Cal33 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWGw[YhrPzJiaB?= MXXFR|UxRTNwM{egxtEhOC55NTFOwG0> M4rNUFI2QDFyMEGw
UM-22B M2nifGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfSRpY4OiCq MUXFR|UxRTJwNk[gxtEhOC5{NDFOwG0> NHHzU4QzPThzMECxNC=>
686LN MkHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\IXlczKGh? MYjFR|UxRTJwMEWgxtEhOS5|MzFOwG0> NH\uVXMzPThzMECxNC=>
UM SCC-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHpflY4OiCq MkXPSWM2OD1zLk[3JOKyKDBwNEKg{txO NU\qN2ttOjV6MUCwNVA>
UM-22A NETRcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm3NkBp MUTFR|UxRTFwM{KgxtEhOC5|OTFOwG0> NEHQ[nAzPThzMECxNC=>
OSC19 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\VVGo4OiCq MkWwSWM2OD1zLkK2JOKyKDBwMkCg{txO NHzpU2IzPThzMECxNC=>
PCI-52 NUjOd|B[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPDSYNsPzJiaB?= NWfVcIZOTUN3ME2xMlAxKMLzIECuNFkh|ryP NH3ONpgzPThzMECxNC=>
PCI-15B MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUS3NkBp M2DNT2VEPTB;MD65PUDDuSBzLke0JO69VQ>? NW\hRVZqOjV6MUCwNVA>
UMSCC-1 MUDGeY5kfGmxbjDBd5NigQ>? MUWwMlAxODVvMT62JO69VQ>? MmXDNlQhcA>? NI[0VIJi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHLqdY4zPThzMECxNC=>
Cal33 MlTDSpVv[3Srb36gRZN{[Xl? NF\CN3cxNjByMEWtN{45KM7:TR?= NIC4bIYzPCCq NW[5RYQy[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MorhNlU5OTByMUC=
HH5 NYjkcoJqTnWwY4Tpc44hSXO|YYm= M1r5R|AvODByNT2zMlgh|ryP NGHGV|UzPCCq MUXhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHTNd2kzPThzMECxNC=>
UM-22A MoH3SpVv[3Srb36gRZN{[Xl? NH7PWGIxNjByMEWtNU43KM7:TR?= M2[4dFI1KGh? MkW4ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Ml62NlU5OTByMUC=
A1847 MULGeY5kfGmxbjDBd5NigQ>? MorLNE4xPS1zMDFOwG0> Mn;QNlQhcA>? NHTzbIZFVVORwrC= NIfTW|Jz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NGGyemQzPTZ2NkCxOS=>
OVCAR-5 NXvHfnBRTnWwY4Tpc44hSXO|YYm= NXLPSGg4OC5yNT2xNEDPxE1? MVSyOEBp MnrpSG1UV8Li M{Ls[ZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MYmyOVY1PjBzNR?=
OVCAR-8 M2TJSWZ2dmO2aX;uJGF{e2G7 M4HaRVAvODVvMUCg{txO M{TsSlI1KGh? MnT5SG1UV8Li M4mxZZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NGTlN5QzPTZ2NkCxOS=>
MOVCAR-5447 MkHzSpVv[3Srb36gRZN{[Xl? NILEZmwxNjB3LUGwJO69VQ>? NVvVfJh6OjRiaB?= NV64RnI4TE2VT9Mg NEXzZoVz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NXTwWmRvOjV4NE[wNVU>
MOVCAR-5009 NH3xWI1HfW6ldHnvckBCe3OjeR?= M{PkZlAvODVvMUCg{txO NIS3SG4zPCCq Ml7FSG1UV8Li NF3QTWVz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NVnhd4hCOjV4NE[wNVU>
A1847 M4W4cmNmdGxiVnnhZoltcXS7IFHzd4F6 NYDnPFc4OC5yNT2xNEDPxE1? M2\yTFczKGh? NGPNNmhFVVOR NFThe2lz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> M{D6XVI2PjR4MEG1
OVCAR-5 NGXMb|JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2\afFAvODVvMUCg{txO MYS3NkBp NXzMRZJ6TE2VTx?= NX3JdFdEemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MonVNlU3PDZyMUW=
OVCAR-8  MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4P1blAvODVvMUCg{txO NVnPdWtOPzJiaB?= MkSxSG1UVw>? NUHzTGhEemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MWSyOVY1PjBzNR?=
OVCAR-5  NHXHNplCeG:ydH;zbZMhSXO|YYm= NVXVe|ZpOC53L{GvOUDPxE1? NI\yPHg1QCCq NVzPRZN1TE2VTx?= NYnW[HNmcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> MUGyOVY1PjBzNR?=
OVCAR-8  NXfFdlNoSXCxcITvd4l{KEG|c3H5 NVXJTmU6OC53L{GvOUDPxE1? MV[0PEBp NYO4OW9MTE2VTx?= Mn7FbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= NIi2cIwzPTZ2NkCxOS=>
AKRSL NW\QVJJkS2WubDDWbYFjcWyrdImgRZN{[Xl? NFzRcoc4OiCq MkLnTWM2OO,:nkGwJO69VQ>? MnrSNlU2ODR4M{W=
PALJDL NX\kZ5dQS2WubDDWbYFjcWyrdImgRZN{[Xl? MVG3NkBp NXTMVIxyUUN3ME2yMlQh|ryP MYKyOVUxPDZ|NR?=
MO4 MYrGeY5kfGmxbjDBd5NigQ>? NGLTZlQxNjVxMT:1JO69VQ>? M3P3TFYhcA>? NWHHUZZucW6qaXLpeJMhWC2VVFHUN{BmgHC{ZYPzbY9vyqB? MoPaNlUyPDl3M{W=
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DU145  M1zXcmZ2dmO2aX;uJGF{e2G7 MkDxPFAxKG6P MVq3NkBp MXTzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? M2HFelI1PTd5OUSy
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H82 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVziVWFSUUN3ME2xMlM4KM7:TR?= M2jkTlI1OTV6N{Cx
GLC4 M2n3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTFwN{mg{txO M{HwTlI1OTV6N{Cx
H526 NWfR[mdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3EblV4UUN3ME2zMlA5KM7:TR?= M2f5UVI1OTV6N{Cx
H1173 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnTOJhKSzVyPUKuN|kh|ryP M1nSeFI1OTV6N{Cx
DMS114 NWLCeVdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjETWM2OD1yLkezJO69VQ>? NYHKO3Q{OjRzNUi3NFE>
NCI-N592 MUXGeY5kfGmxbjDBd5NigQ>? NYTJemRsOC5|L{GvN{DPxE1? MVSyOEBp MV3pcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> MX6yOFE2QDdyMR?=
GLC4 M3H0SmZ2dmO2aX;uJGF{e2G7 NVrWZlJJOC5|L{GvN{DPxE1? M3jLPVI1KGh? NIXo[pVqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MkXsNlQyPTh5MEG=
NCI-H82 NEeyemZHfW6ldHnvckBCe3OjeR?= M3zGd|AvOy9zL{Og{txO NFWxXVYzPCCq NWLNXpg5cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MUmyOFE2QDdyMR?=
NCI-N592 NX3JRodnSXCxcITvd4l{KEG|c3H5 Mn3kNE4{NzFxMzFOwG0> Mkn5OFghcA>? M1H6c4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M13BcVI1OTV6N{Cx
GLC4 Mnf4RZBweHSxc3nzJGF{e2G7 NHH1TGUxNjNxMT:zJO69VQ>? NH[wN441QCCq NHTsNGpqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| M{T4TVI1OTV6N{Cx
NCI-H82 NWfIW3RTSXCxcITvd4l{KEG|c3H5 NFq2d3ExNjNxMT:zJO69VQ>? M123ZlQ5KGh? MmPFbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NVnvNXNlOjRzNUi3NFE>
CWR22Rv1  M2LFWWFxd3C2b4Ppd{BCe3OjeR?= NYLzNINjUUN3ME2wMlQ5OiEQvF2= NIDFbnAzOzl2MkC5OS=>
CWR22Pc NF3G[5dCeG:ydH;zbZMhSXO|YYm= Ml7lTWM2OD1yLkSzPEDPxE1? NF3TWWUzOzl2MkC5OS=>
PC-3 NVXUR|k3SXCxcITvd4l{KEG|c3H5 M13ue2lEPTB;MT63OVUh|ryP NETsTXEzOzl2MkC5OS=>
DU145 NUD3UZp3SXCxcITvd4l{KEG|c3H5 MoTGTWM2OD1|LkWxO{DPxE1? Mm\SNlM6PDJyOUW=
RC165N M3TBOGFxd3C2b4Ppd{BCe3OjeR?= NGrmOVBKSzVyPUKuNFg{KM7:TR?= M4OzV|I{QTR{MEm1
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HEK293 M1;zcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHZSG1UVw>? MXXJR|UxRThwNkeg{txO NWL2PGxNOjN3M{G5NlE>
KCNR NEDmSGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnOOnVFVVOR NUL5cGNNUUN3ME2wMlQ3KM7:TR?= NGe5PYQzOzV|MUmyNS=>
SY5Y MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4SzcGROW09? MVLJR|UxRTBwM{[g{txO M4HEZ|I{PTNzOUKx
BE2 MkHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2WzR2ROW09? M1HkWGlEPTB;MD63NUDPxE1? M3zLOlI{PTNzOUKx
AS M3PIfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\JdHMzTE2VTx?= NX\yT4J4UUN3ME2xMlU{KM7:TR?= NIrhV|MzOzV|MUmyNS=>
NGP Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LydmROW09? NWHmNlJKUUN3ME2wMlU3KM7:TR?= M3qwN|I{PTNzOUKx
IMR32 NFf6OYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXG3d|U6TE2VTx?= NEfRfYdKSzVyPUCuOlYh|ryP MWSyN|U{OTl{MR?=
LAN5 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLJU2NZTE2VTx?= NGPPN2pKSzVyPUGuNFQh|ryP NE\CNYEzOzV|MUmyNS=>
RH18 NYHiNXM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK4XlRFVVOR NED0PHZKSzVyPUGuOFIh|ryP NITLb2QzOzV|MUmyNS=>
RH30 MoS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzafJJlTE2VTx?= NYmyVVRrUUN3ME2xMlI2KM7:TR?= M12zOFI{PTNzOUKx
RH17 NWTIZo5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHTeXdFVVOR NFvIe|BKSzVyPUKuOVEh|ryP MnqxNlM2OzF7MkG=
RH28 NGPoN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXNUHNNTE2VTx?= NYT1cndbUUN3ME20MlI5KM7:TR?= NWf0UZZwOjN3M{G5NlE>
RH36 MkTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfEUXNQ NXfSdHRlUUN3ME21MlM4KM7:TR?= NGrVbmYzOzV|MUmyNS=>
RH41 NFPEUI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLEUXNQ M3Xmd2lEPTB;MD60PEDPxE1? NEfNbWgzOzV|MUmyNS=>
RD NWTiVWRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPEUXNQ MoGwTWM2OD12LkOyJO69VQ>? MXyyN|U{OTl{MR?=
TC32 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nsTmROW09? NGnOPWhKSzVyPUOuPFUh|ryP MViyN|U{OTl{MR?=
TC71 MorES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvEUXNQ NITFW3RKSzVyPUSuN|Mh|ryP MYSyN|U{OTl{MR?=
KCNR Ml3jRZBweHSxc3nzJGF{e2G7 M4i3blAvPS9zLkCvNk42KM7:TR?= Ml61NlQhcA>? NWfub3FZTE2VTx?= MWDpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NHnoTFYzOzV|MUmyNS=>
SY5Y MmrNRZBweHSxc3nzJGF{e2G7 NYniU|k1OC53L{GuNE8zNjVizszN NHPBTWMzPCCq M4HaW2ROW09? MmHHbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= Mo\SNlM2OzF7MkG=
Rh18 NHHaWHFCeG:ydH;zbZMhSXO|YYm= NWPxfWl6OC53L{GuNE8zNjVizszN MUiyOEBp MXHEUXNQ MofGbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= M3z6NlI{PTNzOUKx
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KCNR M1XN[mZ2dmO2aX;uJGF{e2G7 NF\mZWExNjVxMT6wM|IvPS93IN88US=> NXvwfIRLOjRiaB?= NV7CN21FTE2VTx?= NE\iXWxqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NHX2TYYzOzV|MUmyNS=>
SY5Y MXjGeY5kfGmxbjDBd5NigQ>? NYDycIE5OC53L{GuNE8zNjVxNTFOwG0> MVGyOEBp Mm\LSG1UVw>? MVnpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MmfINlM2OzF7MkG=
Rh18 MWnGeY5kfGmxbjDBd5NigQ>? NITodJExNjVxMT6wM|IvPS93IN88US=> NYjTOoF[OjRiaB?= Mn;oSG1UVw>? MV\pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MVyyN|U{OTl{MR?=
TC32 M2nLbWZ2dmO2aX;uJGF{e2G7 M2PLRlAvPS9zLkCvNk42NzVizszN NEPL[mgzPCCq M1XXZWROW09? NHjwVJlqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NHzzdYkzOzV|MUmyNS=>
TPC-1 M1uyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17XOlEhyrWP NVroVZFZOC12IHS= MmP4SG1UVw>? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 Ml7INlMxPTZ2OUm=
MZ-CRC1  NH22R5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[2c|EhyrWP MkjPNE02KGR? NWTEPGlZTE2VTx?= Mn\NbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MWCyN|A2PjR7OR?=
TT  MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TRWlEhyrWP M32wWFAuPCCm NYXJOXRtTE2VTx?= NXL0XmNbcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= MUKyN|A2PjR7OR?=
TPC-1 NGG4VItHfW6ldHnvckBCe3OjeR?= NEjqOIwyKML3TR?= NV[2Z4JiPzJiaB?= MUHEUXNQ MXnpcoR2[2W|IFexJIJtd2OtYXfl NWO4OIVkOjNyNU[0PVk>
MZ-CRC1  NUP3dW1wTnWwY4Tpc44hSXO|YYm= NEO3bFEyKML3TR?= M3iycFczKGh? MlvKSG1UVw>? M{TNfYlv\HWlZYOgS|Eh[myxY3vh[4U> NVXPdHR5OjNyNU[0PVk>
TT  MWfGeY5kfGmxbjDBd5NigQ>? NYjxbZBsOSEEtV2= NGPkbGw4OiCq NGCwOG9FVVOR NUn2dJdFcW6mdXPld{BIOSCkbH;jb4Fo\Q>? NVfZNVJxOjNyNU[0PVk>
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TT  NW\YNHNPSXCxcITvd4l{KEG|c3H5 NGrvRocyKML3TR?= M{fMTVQ5KGh? Mk[5SG1UVw>? MkLYbY5lfWOnczDhdI9xfG:|aYO= MYCyN|A2PjR7OR?=
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KM-H2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17uVVcz6oDLaB?= MUjEUXNQ M1jLN2lEPTB;MT6zNFgh|ryP NUPlZWdIOjJ6MkmwPVQ>
L-540 NVrJVVM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\6SJA4OuLCiXi= MoPKSG1UVw>? NV;nZ3ZMUUN3ME24MlIyPiEQvF2= MWSyNlgzQTB7NB?=
HD-LM2 M3LQVGZ2dmO2aX;uJGF{e2G7 NGfnOncxNjFxMD61M|EwPSEQvF2= Mmj5O|LjiImq MW\EUXNQ NGjvO5hqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? MY[yNlgzQTB7NB?=
L-428 MXvGeY5kfGmxbjDBd5NigQ>? NWT4b4tSOC5zL{CuOU8yNzVizszN NHO4NGo4OuLCiXi= MUjEUXNQ MnLUbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NXjoZmdMOjJ6MkmwPVQ>
KM-H2 NHz1bGhHfW6ldHnvckBCe3OjeR?= Mnr0NE4yNzBwNT:xM|Uh|ryP MYq3NwKBkWh? NXLpb2FHTE2VTx?= NXXyXIc4cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NHvJb4czOjh{OUC5OC=>
L-540 NXPDNWhzTnWwY4Tpc44hSXO|YYm= NYfSVVV4OC5zL{CuOU8yNzVizszN MnTEO|LjiImq NYTxeVhoTE2VTx?= NIrwO5lqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? MVKyNlgzQTB7NB?=
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L-428 M1npXmFxd3C2b4Ppd{BCe3OjeR?= MWOxM|Uh|ryP NEDQRmo4OuLCiXi= NVjzeYtwTE2VTx?= M2rHR4lv\HWlZYOgZZBweHSxc3nz M4jLelIzQDJ7MEm0
KM-H2 NV;ud4RoSXCxcITvd4l{KEG|c3H5 NWHEPI1qOS93IN88US=> NVrOd5p2PzMkgJno MlLySG1UVw>? MYPpcoR2[2W|IHHwc5B1d3Orcx?= MnfZNlI5OjlyOUS=
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U251-MG NGTySGJHfW6ldHnvckBCe3OjeR?= M4nh[VEhyrWP MnPZNE0yPiCq NF3QfW1qdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MVKyNlAzPzZ7MR?=
U87-MG MlPoSpVv[3Srb36gRZN{[Xl? NFXybnYyKML3TR?= M3XYeVAuOTZiaB?= NYPGZlIxcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MYCyNlAzPzZ7MR?=
4C8 M2\HU2Z2dmO2aX;uJGF{e2G7 NG\XWnAyKML3TR?= M{PYblAuOTZiaB?= M13J[YlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? MnvUNlIxOjd4OUG=
U251-MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjScYRJOS9zMDFCuW0> NVT0SnRiOjRxNEivO|IhcA>? MkjZbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> Ml3mNlIxOjd4OUG=
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... 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

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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