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 MUHGeY5kfGmxbjDBd5NigQ>? NHfTZlU2KM7:TR?= MmXqOFghcA>? NUHuOVhHTE2VTx?= NHnENYtjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NXz0OWxzOjV7NUS5O|Q>
LoVo  M3nJNWZ2dmO2aX;uJGF{e2G7 NUfaOoxFPSEQvF2= MVi0PEBp Mon5SG1UVw>? NEflUW1jdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NH3kTnUzPTl3NEm3OC=>
HN5 NF\hSoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHnO|IhcA>? MoDYSWM2OD1|LkixJOKyKDFwOUmg{txO M2S1ZlI2QDFyMEGw
Cal33 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUW3NkBp NUi3U4NuTUN3ME2zMlM4KMLzIECuO|Uh|ryP NX;R[HY6OjV6MUCwNVA>
UM-22B M{HERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fpW|czKGh? NHzuZWRGSzVyPUKuOlYhyrFiMD6yOEDPxE1? NVjz[XcxOjV6MUCwNVA>
686LN NHfvPW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XiZ|czKGh? NUjxTXVFTUN3ME2yMlA2KMLzIEGuN|Mh|ryP MV:yOVgyODBzMB?=
UM SCC-1 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL3O|IhcA>? Ml70SWM2OD1zLk[3JOKyKDBwNEKg{txO MXGyOVgyODBzMB?=
UM-22A NHXRT3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCy[GRPPzJiaB?= MXfFR|UxRTFwM{KgxtEhOC5|OTFOwG0> MoLpNlU5OTByMUC=
OSC19 NVfwZ5UxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv4cJI4OiCq M3;6cGVEPTB;MT6yOkDDuSByLkKwJO69VQ>? NE\EWlYzPThzMECxNC=>
PCI-52 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLnXJdoPzJiaB?= NUTQ[WZrTUN3ME2xMlAxKMLzIECuNFkh|ryP NXjJfZhHOjV6MUCwNVA>
PCI-15B M4fCVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP2TnY4OiCq NFnVUHRGSzVyPUCuPVkhyrFiMT63OEDPxE1? NVrvO5FwOjV6MUCwNVA>
UMSCC-1 MlLWSpVv[3Srb36gRZN{[Xl? M362RlAvODByNT2xMlYh|ryP NH\KWHkzPCCq NH;BXoJi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXqyOVgyODBzMB?=
Cal33 NIPJcoNHfW6ldHnvckBCe3OjeR?= MnG1NE4xODB3LUOuPEDPxE1? MYWyOEBp MVvhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MXyyOVgyODBzMB?=
HH5 MWrGeY5kfGmxbjDBd5NigQ>? NXfjelFwOC5yMEC1MVMvQCEQvF2= NWDnbWs1OjRiaB?= MWXhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2PvfVI2QDFyMEGw
UM-22A NF;FOVhHfW6ldHnvckBCe3OjeR?= NVHEcW1qOC5yMEC1MVEvPiEQvF2= NFG3VHIzPCCq M{\ucoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1rMXlI2QDFyMEGw
A1847 Mn[4SpVv[3Srb36gRZN{[Xl? MVywMlA2NTFyIN88US=> Mk\rNlQhcA>? M4LjUGROW00EoB?= M{G2bpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NG\sW|IzPTZ2NkCxOS=>
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MOVCAR-5447 MmHhSpVv[3Srb36gRZN{[Xl? NEDBelQxNjB3LUGwJO69VQ>? MlrUNlQhcA>? NIXiblBFVVORwrC= MnnzdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MnvYNlU3PDZyMUW=
MOVCAR-5009 NGDobphHfW6ldHnvckBCe3OjeR?= NILVfm0xNjB3LUGwJO69VQ>? NFzJN5IzPCCq MYrEUXNQyqB? NEHJTJRz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M{jBUlI2PjR4MEG1
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OVCAR-5  NH\HOGNCeG:ydH;zbZMhSXO|YYm= NVLpPZlOOC53L{GvOUDPxE1? MV:0PEBp MUnEUXNQ NV7yeJNLcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> NWjEZ5E1OjV4NE[wNVU>
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DMS114 Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojXTWM2OD1yLkezJO69VQ>? NF\nTHkzPDF3OEewNS=>
NCI-N592 MYrGeY5kfGmxbjDBd5NigQ>? M3LLRVAvOy9zL{Og{txO M4fjc|I1KGh? MVfpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NUfmdo9COjRzNUi3NFE>
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NCI-H82 MkXRSpVv[3Srb36gRZN{[Xl? M4LSUFAvOy9zL{Og{txO M{HaelI1KGh? MmXqbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MYeyOFE2QDdyMR?=
NCI-N592 NIPQ[HlCeG:ydH;zbZMhSXO|YYm= NIHB[GwxNjNxMT:zJO69VQ>? MUS0PEBp M2rjd4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MoLPNlQyPTh5MEG=
GLC4 MXzBdI9xfG:|aYOgRZN{[Xl? M2PYWFAvOy9zL{Og{txO NVfRdmdyPDhiaB?= NFH2clJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NHLLbHEzPDF3OEewNS=>
NCI-H82 MWHBdI9xfG:|aYOgRZN{[Xl? NH\DbYkxNjNxMT:zJO69VQ>? NUnn[FhVPDhiaB?= NXjrWVNOcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= M2DNXFI1OTV6N{Cx
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DU145 MlnKRZBweHSxc3nzJGF{e2G7 MlrPTWM2OD1|LkWxO{DPxE1? NILDeYQzOzl2MkC5OS=>
RC165N NEnwTWxCeG:ydH;zbZMhSXO|YYm= NU\LSlJHUUN3ME2yMlA5OyEQvF2= Mk\rNlM6PDJyOUW=
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RH18 MnrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXudJhFVVOR MofNTWM2OD1zLkSyJO69VQ>? M4HsZ|I{PTNzOUKx
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RH41 M4r1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrZS3dSTE2VTx?= NX\m[XF6UUN3ME2wMlQ5KM7:TR?= MkDUNlM2OzF7MkG=
RD MlHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TBSGROW09? NFLZVlZKSzVyPUSuN|Ih|ryP MV[yN|U{OTl{MR?=
TC32 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz6SG1UVw>? MUnJR|UxRTNwOEWg{txO MmDDNlM2OzF7MkG=
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KCNR NG\xZWdCeG:ydH;zbZMhSXO|YYm= NF7SZoQxNjVxMT6wM|IvPSEQvF2= MV[yOEBp NFjjOVJFVVOR NVizPG5LcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> M2LpPFI{PTNzOUKx
SY5Y NV[2O4N[SXCxcITvd4l{KEG|c3H5 MVywMlUwOS5yL{KuOUDPxE1? NYC5dIl4OjRiaB?= MVPEUXNQ NH3RW2FqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MVmyN|U{OTl{MR?=
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TC32 NGrpbohHfW6ldHnvckBCe3OjeR?= MkTpNE42NzFwMD:yMlUwPSEQvF2= M3\aOVI1KGh? MkjvSG1UVw>? MV;pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NVTmNJFVOjN3M{G5NlE>
TPC-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;jS4UyKML3TR?= Mn;CNE01KGR? MoXDSG1UVw>? Ml3hbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? NVTtOVlTOjNyNU[0PVk>
MZ-CRC1  MnnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nKZVEhyrWP M2PEeFAuPSCm MVrEUXNQ NYLCZXlxcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= MkXWNlMxPTZ2OUm=
TT  MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm0TZJROSEEtV2= MXOwMVQh\A>? M1XVWGROW09? NVPiVlRbcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NHLoOFUzOzB3NkS5PS=>
TPC-1 NIH5RlBHfW6ldHnvckBCe3OjeR?= NVvVfodUOSEEtV2= M2rCdFczKGh? M4rQfGROW09? NFXibVdqdmS3Y3XzJGcyKGKub3PrZYdm NGPhNpIzOzB3NkS5PS=>
MZ-CRC1  NX\JRmRoTnWwY4Tpc44hSXO|YYm= Mnu4NUDDvU1? NHrvRZQ4OiCq NH:0VnlFVVOR NVjBOld4cW6mdXPld{BIOSCkbH;jb4Fo\Q>? NI\ufpgzOzB3NkS5PS=>
TT  MWTGeY5kfGmxbjDBd5NigQ>? MWexJOK2VQ>? MUC3NkBp M2THV2ROW09? NV[4Zm9lcW6mdXPld{BIOSCkbH;jb4Fo\Q>? NGHF[ZEzOzB3NkS5PS=>
MZ-CRC1  MUTBdI9xfG:|aYOgRZN{[Xl? MVqxJOK2VQ>? NUjETVBJPDhiaB?= NXnCU21mTE2VTx?= NGrjOZBqdmS3Y3XzJIFxd3C2b4Ppdy=> Mn30NlMxPTZ2OUm=
TT  M3PNW2Fxd3C2b4Ppd{BCe3OjeR?= Ml7jNUDDvU1? NXrMSWtzPDhiaB?= M3fXWGROW09? MmDFbY5lfWOnczDhdI9xfG:|aYO= M4LiNlI{ODV4NEm5
HD-LM2 M3Xkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi1Ook4OuLCiXi= MYrEUXNQ MoPVTWM2OD15Lki0OEDPxE1? NHPXWnkzOjh{OUC5OC=>
L-428 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLhTpY4OuLCiXi= MkDHSG1UVw>? NIO4[mxKSzVyPUeuPVQ4KM7:TR?= MlLzNlI5OjlyOUS=
KM-H2 NVfO[ItJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzBPYw{PzMkgJno MnPUSG1UVw>? NF3D[IRKSzVyPUGuN|A5KM7:TR?= NVvF[JBmOjJ6MkmwPVQ>
L-540 MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[3NwKBkWh? MkLMSG1UVw>? NUP5Ool6UUN3ME24MlIyPiEQvF2= NWS4U2JnOjJ6MkmwPVQ>
HD-LM2 MlzrSpVv[3Srb36gRZN{[Xl? NYLtcnY3OC5zL{CuOU8yNzVizszN MUO3NwKBkWh? MUPEUXNQ M2flT4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MUeyNlgzQTB7NB?=
L-428 NFrxb2xHfW6ldHnvckBCe3OjeR?= Mn\ONE4yNzBwNT:xM|Uh|ryP NIqwRm84OuLCiXi= MWrEUXNQ M2TmcolvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MnfuNlI5OjlyOUS=
KM-H2 MXXGeY5kfGmxbjDBd5NigQ>? NVH6cmtPOC5zL{CuOU8yNzVizszN NVTqNXNmPzMkgJno M{TNS2ROW09? NHTSSmtqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? M4\kcFIzQDJ7MEm0
L-540 M4jlNWZ2dmO2aX;uJGF{e2G7 MWewMlEwOC53L{GvOUDPxE1? NGDmU3o4OuLCiXi= M1S1c2ROW09? NV7ad5lLcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MlLLNlI5OjlyOUS=
HD-LM2 MnLmRZBweHSxc3nzJGF{e2G7 NGPGOnYyNzVizszN MVy3NwKBkWh? M3H6R2ROW09? MV7pcoR2[2W|IHHwc5B1d3Orcx?= NWXNVGFFOjJ6MkmwPVQ>
L-428 MnWwRZBweHSxc3nzJGF{e2G7 NWjUW|lbOS93IN88US=> NIKwOmc4OuLCiXi= NHyzbXBFVVOR NXiweYJycW6mdXPld{BieG:ydH;zbZM> NFzyXHczOjh{OUC5OC=>
KM-H2 Mki5RZBweHSxc3nzJGF{e2G7 NWPyXFJGOS93IN88US=> MYC3NwKBkWh? NHTpSlNFVVOR MoXLbY5lfWOnczDhdI9xfG:|aYO= NUfMNXc{OjJ6MkmwPVQ>
L-540 NVW3WFNDSXCxcITvd4l{KEG|c3H5 MoDuNU82KM7:TR?= Mn\LO|LjiImq NH71enlFVVOR NX;iZo5GcW6mdXPld{BieG:ydH;zbZM> NUDhWYhWOjJ6MkmwPVQ>
U251-MG NVrYPYRsTnWwY4Tpc44hSXO|YYm= MXGxJOK2VQ>? NETOU20xNTF4IHi= M{\KdolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NITEbYgzOjB{N{[5NS=>
U87-MG MYTGeY5kfGmxbjDBd5NigQ>? M4DV[|EhyrWP Mo[5NE0yPiCq NYrTfpBzcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MUmyNlAzPzZ7MR?=
4C8 M1GwOGZ2dmO2aX;uJGF{e2G7 NUXUVZh3OSEEtV2= NF7LXYgxNTF4IHi= MWrpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MYqyNlAzPzZ7MR?=
U251-MG NILTfVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDhUIcyNzFyINM1US=> NIm3W|EzPC92OD:3NkBp NUnqT|RYcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MYiyNlAzPzZ7MR?=
U87-MG M2XGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED3RXUyNzFyINM1US=> MVmyOE81QC95MjDo NV;yfmtPcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NV:5eWF4OjJyMke2PVE>
4C8 NVLCVGx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxM|ExKML3TR?= NVTaRopxOjRxNEivO|IhcA>? NVzCZWs5cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? M2HkfFIzODJ5Nkmx
U266 NYTOSG54SXCxcITvd4l{KEG|c3H5 NHnUS2MxNjVvMjFOwG0> NUDt[HRjPDhxN{KgbC=> MlLLbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MUeyNVE3PDVzNx?=
Kms.11 NF\TOHZCeG:ydH;zbZMhSXO|YYm= M3nBNlAvPS1{IN88US=> Mn:2OFgwPzJiaB?= M4\5XYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MmS0NlEyPjR3MUe=
8226 NVy4SlBISXCxcITvd4l{KEG|c3H5 NWXXbZdbOC53LUKg{txO M{TFO|Q5Nzd{IHi= M1zVc4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MUKyNVE3PDVzNx?=

... 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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