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 NFriRnhHfW6ldHnvckBCe3OjeR?= MknXOUDPxE1? NHWxSnU1QCCq NVnhdXRkTE2VTx?= M1n3UIJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MV6yOVk2PDl5NB?=
LoVo  M1TOV2Z2dmO2aX;uJGF{e2G7 M17RNlUh|ryP M1XXbVQ5KGh? MkDsSG1UVw>? Moq3Zoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n NYP0PXp7OjV7NUS5O|Q>
HN5 M3\keWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33oPFczKGh? MlL1SWM2OD1|LkixJOKyKDFwOUmg{txO MlrsNlU5OTByMUC=
Cal33 NHzKeGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjscnQyPzJiaB?= M{jaWWVEPTB;Mz6zO{DDuSByLke1JO69VQ>? NInJWmIzPThzMECxNC=>
UM-22B MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUO3NkBp MXPFR|UxRTJwNk[gxtEhOC5{NDFOwG0> NFvHdJMzPThzMECxNC=>
686LN MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWi3NkBp MYDFR|UxRTJwMEWgxtEhOS5|MzFOwG0> M3n3WFI2QDFyMEGw
UM SCC-1 M{DZUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX63NkBp NETQfpNGSzVyPUGuOlchyrFiMD60NkDPxE1? NEG5VVUzPThzMECxNC=>
UM-22A NWHGR2h5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnkO|IhcA>? NYXP[IlZTUN3ME2xMlMzKMLzIECuN|kh|ryP MXmyOVgyODBzMB?=
OSC19 NFXvV21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHHfWxwPzJiaB?= NUC0dnF{TUN3ME2xMlI3KMLzIECuNlAh|ryP MlmyNlU5OTByMUC=
PCI-52 M4e3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fsRlczKGh? MYTFR|UxRTFwMECgxtEhOC5yOTFOwG0> M3rGOVI2QDFyMEGw
PCI-15B NEfWXpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vadFczKGh? MXfFR|UxRTBwOUmgxtEhOS55NDFOwG0> MmT2NlU5OTByMUC=
UMSCC-1 NV6yc4hDTnWwY4Tpc44hSXO|YYm= MYWwMlAxODVvMT62JO69VQ>? Mm\xNlQhcA>? M3LkNoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWXPSYlEOjV6MUCwNVA>
Cal33 Mk\MSpVv[3Srb36gRZN{[Xl? NFzUOWoxNjByMEWtN{45KM7:TR?= M{HscFI1KGh? Mmj4ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGPaN2wzPThzMECxNC=>
HH5 MmHhSpVv[3Srb36gRZN{[Xl? NGjYdnoxNjByMEWtN{45KM7:TR?= MVOyOEBp MYLhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4XrZVI2QDFyMEGw
UM-22A MnHqSpVv[3Srb36gRZN{[Xl? M1fqZlAvODByNT2xMlYh|ryP Mmr5NlQhcA>? NGLZO4pi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmjsNlU5OTByMUC=
A1847 M3TifWZ2dmO2aX;uJGF{e2G7 M3TVUFAvODVvMUCg{txO NWLCSZlWOjRiaB?= NVOwVIFnTE2VT9Mg MX7y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MkLlNlU3PDZyMUW=
OVCAR-5 Ml;HSpVv[3Srb36gRZN{[Xl? M3vsPFAvODVvMUCg{txO MWGyOEBp NFXYR4xFVVORwrC= M2W1fJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz M3fZNVI2PjR4MEG1
OVCAR-8 MnjzSpVv[3Srb36gRZN{[Xl? M{ToOFAvODVvMUCg{txO NYTEe5Z2OjRiaB?= NEP2NVZFVVORwrC= NYTrZ4FZemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NEDBXZIzPTZ2NkCxOS=>
MOVCAR-5447 MkPpSpVv[3Srb36gRZN{[Xl? NVX5XI95OC5yNT2xNEDPxE1? NWfsVHFHOjRiaB?= NY\HdWFuTE2VT9Mg NFLnW2xz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NIXZSWozPTZ2NkCxOS=>
MOVCAR-5009 NHHhc|FHfW6ldHnvckBCe3OjeR?= MX6wMlA2NTFyIN88US=> M3H6OVI1KGh? M4DBR2ROW00EoB?= NF;K[JFz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MnXzNlU3PDZyMUW=
A1847 NHvhNlJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWf1R4txOC5yNT2xNEDPxE1? NY\TOVJiPzJiaB?= MXPEUXNQ M2PsT5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN Mk\hNlU3PDZyMUW=
OVCAR-5 MkDjR4VtdCCYaXHibYxqfHliQYPzZZk> MXqwMlA2NTFyIN88US=> NHTwW3I4OiCq M1vLSmROW09? NV\LbW14emWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NGiwZmszPTZ2NkCxOS=>
OVCAR-8  MmXhR4VtdCCYaXHibYxqfHliQYPzZZk> MV[wMlA2NTFyIN88US=> MUK3NkBp M{faT2ROW09? NXnD[nFyemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MUGyOVY1PjBzNR?=
OVCAR-5  M3rCRmFxd3C2b4Ppd{BCe3OjeR?= NH;3[IExNjVxMT:1JO69VQ>? NVTNW5JVPDhiaB?= Mn[xSG1UVw>? M{Tj[olv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= NYnOXIdQOjV4NE[wNVU>
OVCAR-8  M2rMTWFxd3C2b4Ppd{BCe3OjeR?= Ml7HNE42NzFxNTFOwG0> MnrPOFghcA>? NV:xRnBITE2VTx?= NVfvbnRIcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M3\ZflI2PjR4MEG1
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PALJDL Mk\IR4VtdCCYaXHibYxqfHliQYPzZZk> NY\KeXVCPzJiaB?= NGPrfmtKSzVyPUKuOEDPxE1? MkK4NlU2ODR4M{W=
MO4 NFLC[2tHfW6ldHnvckBCe3OjeR?= M334clAvPS9zL{Wg{txO M3fZU|YhcA>? NELvSotqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NF7SVmszPTF2OUWzOS=>
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DU145  NF;iUXdHfW6ldHnvckBCe3OjeR?= MXe4NFAhdk1? NIDQc5c4OiCq M4rTbJN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NFf2OZEzPDV5N{m0Ni=>
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GLC4 NVXUdpZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfqTWM2OD1zLke5JO69VQ>? MWCyOFE2QDdyMR?=
H526 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnFcJZKSzVyPUOuNFgh|ryP NH\pR5ozPDF3OEewNS=>
H1173 M1fiOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzUd2J6UUN3ME2yMlM6KM7:TR?= MWWyOFE2QDdyMR?=
DMS114 M4PSNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwN{Og{txO MUiyOFE2QDdyMR?=
NCI-N592 NFrpXnlHfW6ldHnvckBCe3OjeR?= M1uybVAvOy9zL{Og{txO NG\HdXkzPCCq M3nTbYlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MWKyOFE2QDdyMR?=
GLC4 NG\6SpJHfW6ldHnvckBCe3OjeR?= NHLPVVMxNjNxMT:zJO69VQ>? Mn7pNlQhcA>? MW\pcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NIXxfJEzPDF3OEewNS=>
NCI-H82 NECzeG1HfW6ldHnvckBCe3OjeR?= NHPnVHgxNjNxMT:zJO69VQ>? NFrSW3ozPCCq Ml75bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M1HTdVI1OTV6N{Cx
NCI-N592 NULvc4tESXCxcITvd4l{KEG|c3H5 MXywMlMwOS9|IN88US=> NXfYeXFiPDhiaB?= M4Wyb4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NFTnZWozPDF3OEewNS=>
GLC4 NHXYZVVCeG:ydH;zbZMhSXO|YYm= NHLXRmIxNjNxMT:zJO69VQ>? MmPsOFghcA>? MmnXbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NHHKVHEzPDF3OEewNS=>
NCI-H82 M3vjR2Fxd3C2b4Ppd{BCe3OjeR?= MW[wMlMwOS9|IN88US=> M4HF[|Q5KGh? NYHPVYRScW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MXSyOFE2QDdyMR?=
CWR22Rv1  NXi2bGxVSXCxcITvd4l{KEG|c3H5 NYHJSWp3UUN3ME2wMlQ5OiEQvF2= MX2yN|k1OjB7NR?=
CWR22Pc M2G0[GFxd3C2b4Ppd{BCe3OjeR?= MnLiTWM2OD1yLkSzPEDPxE1? M1ftc|I{QTR{MEm1
PC-3 MUjBdI9xfG:|aYOgRZN{[Xl? NXjaW2Q{UUN3ME2xMlc2PSEQvF2= M4fQNlI{QTR{MEm1
DU145 NULI[II1SXCxcITvd4l{KEG|c3H5 NHnmU4NKSzVyPUOuOVE4KM7:TR?= NHPpTpQzOzl2MkC5OS=>
RC165N M1zqV2Fxd3C2b4Ppd{BCe3OjeR?= MmTSTWM2OD1{LkC4N{DPxE1? NX36cYRKOjN7NEKwPVU>
ARPE19 NGLUV4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHrNpZDTE2VTx?= NETER4VKSzVyPUK0MlM5KM7:TR?= NVXCblFkOjN3M{G5NlE>
HEK293 MkPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjre29oTE2VTx?= M3O1bGlEPTB;OD62O{DPxE1? MVOyN|U{OTl{MR?=
KCNR M2[3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXEUXNQ M3HE[mlEPTB;MD60OkDPxE1? NHLnNYQzOzV|MUmyNS=>
SY5Y MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzPNW5yTE2VTx?= NITTXHBKSzVyPUCuN|Yh|ryP NUj3SWRVOjN3M{G5NlE>
BE2 M2DaVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[5NHdRTE2VTx?= M4jVO2lEPTB;MD63NUDPxE1? M4S1UVI{PTNzOUKx
AS M1LMOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;6[lNFVVOR MlfNTWM2OD1zLkWzJO69VQ>? NYO4VY9ZOjN3M{G5NlE>
NGP NGPrNXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z3NmROW09? NInpVo1KSzVyPUCuOVYh|ryP MXuyN|U{OTl{MR?=
IMR32 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrEUXNQ MnvCTWM2OD1yLk[2JO69VQ>? NV;aTXppOjN3M{G5NlE>
LAN5 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LPUmROW09? NFnHUXpKSzVyPUGuNFQh|ryP MomwNlM2OzF7MkG=
RH18 M2LleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PQ[GROW09? M4DHZWlEPTB;MT60NkDPxE1? NVv1dpB3OjN3M{G5NlE>
RH30 NX\3SGl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3XcoJFVVOR MUXJR|UxRTFwMkWg{txO NFHv[FEzOzV|MUmyNS=>
RH17 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j0UmROW09? MVrJR|UxRTJwNUGg{txO MViyN|U{OTl{MR?=
RH28 Ml\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjEUXNQ NULVd4NDUUN3ME20MlI5KM7:TR?= NInnU3czOzV|MUmyNS=>
RH36 NXe0W2UxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGweXJYTE2VTx?= NUPjO4ZFUUN3ME21MlM4KM7:TR?= NIO3[YozOzV|MUmyNS=>
RH41 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f0WWROW09? NVXwPVJ4UUN3ME2wMlQ5KM7:TR?= NEK3[2MzOzV|MUmyNS=>
RD NH3BVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnEUXNQ NV\6bIxMUUN3ME20MlMzKM7:TR?= MVeyN|U{OTl{MR?=
TC32 NX3rWpZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITYVZdFVVOR NYnKV2t7UUN3ME2zMlg2KM7:TR?= NUD3[lJtOjN3M{G5NlE>
TC71 M1ywUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fFfmROW09? NYWzSHc5UUN3ME20MlM{KM7:TR?= M4L1flI{PTNzOUKx
KCNR Mn7uRZBweHSxc3nzJGF{e2G7 M3LqeFAvPS9zLkCvNk42KM7:TR?= M1u1dVI1KGh? NIXrb4dFVVOR NUDZeIlmcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MnjsNlM2OzF7MkG=
SY5Y MkTCRZBweHSxc3nzJGF{e2G7 MoiyNE42NzFwMD:yMlUh|ryP MY[yOEBp NGX3Vo5FVVOR MVjpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MXmyN|U{OTl{MR?=
Rh18 NUfYTJN4SXCxcITvd4l{KEG|c3H5 NHXBeocxNjVxMT6wM|IvPSEQvF2= MYGyOEBp NXjWbnlFTE2VTx?= M2rjbIlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NIOzd5ozOzV|MUmyNS=>
TC32 MXjBdI9xfG:|aYOgRZN{[Xl? NXPjbVdSOC53L{GuNE8zNjVizszN MlfINlQhcA>? M2\MN2ROW09? NW\qOJJ7cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MkjoNlM2OzF7MkG=
KCNR NU\1bW5jTnWwY4Tpc44hSXO|YYm= NHrOR2gxNjVxMT6wM|IvPS93IN88US=> MoLQNlQhcA>? MYrEUXNQ M1PtcYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u Mk\LNlM2OzF7MkG=
SY5Y M{Wy[GZ2dmO2aX;uJGF{e2G7 MoLiNE42NzFwMD:yMlUwPSEQvF2= M4TXelI1KGh? MVLEUXNQ MnzNbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= Mnz5NlM2OzF7MkG=
Rh18 NUPyW|FGTnWwY4Tpc44hSXO|YYm= NIfP[YsxNjVxMT6wM|IvPS93IN88US=> MlrxNlQhcA>? NY\w[GFtTE2VTx?= Mn\zbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MYKyN|U{OTl{MR?=
TC32 NFrNbVJHfW6ldHnvckBCe3OjeR?= NInhS2kxNjVxMT6wM|IvPS93IN88US=> NVj0eolvOjRiaB?= Mki5SG1UVw>? NYHz[pprcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NGjoPG4zOzV|MUmyNS=>
TPC-1 MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTDNUDDvU1? NFvyZYoxNTRiZB?= MW\EUXNQ NH7hfHBqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAzKGRidILlZZRu\W62 M1\XXlI{ODV4NEm5
MZ-CRC1  MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxJOK2VQ>? MXKwMVUh\A>? NWDkcI9HTE2VTx?= NEDhWJRqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MWmyN|A2PjR7OR?=
TT  M1PER2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqxJOK2VQ>? NHTYVnExNTRiZB?= M3PVdWROW09? Mmq5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MXWyN|A2PjR7OR?=
TPC-1 NV\NU3NpTnWwY4Tpc44hSXO|YYm= MknnNUDDvU1? NYLtRVFYPzJiaB?= NXvCUm1rTE2VTx?= NWHqSnBzcW6mdXPld{BIOSCkbH;jb4Fo\Q>? Mni2NlMxPTZ2OUm=
MZ-CRC1  MX3GeY5kfGmxbjDBd5NigQ>? NHm5VGMyKML3TR?= NHznfpU4OiCq MnWzSG1UVw>? MmDIbY5lfWOnczDHNUBjdG:la3Hn[S=> MX:yN|A2PjR7OR?=
TT  NF3RN2dHfW6ldHnvckBCe3OjeR?= MkS1NUDDvU1? MYS3NkBp NHXpPVBFVVOR NYe0d5FJcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MmfVNlMxPTZ2OUm=
MZ-CRC1  NF3uXVlCeG:ydH;zbZMhSXO|YYm= MkXRNUDDvU1? Mn[wOFghcA>? MnnjSG1UVw>? MlmybY5lfWOnczDhdI9xfG:|aYO= NXnyVGtxOjNyNU[0PVk>
TT  M1\5[2Fxd3C2b4Ppd{BCe3OjeR?= NYjrcIlOOSEEtV2= NVTiS29zPDhiaB?= MVXEUXNQ NF3xRZpqdmS3Y3XzJIFxd3C2b4Ppdy=> MVyyN|A2PjR7OR?=
HD-LM2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILnXHY4OuLCiXi= NWHPNFRjTE2VTx?= NGfjZ4ZKSzVyPUeuPFQ1KM7:TR?= NFHrZnEzOjh{OUC5OC=>
L-428 M1njZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz6O|LjiImq NIfVbHJFVVOR MkjJTWM2OD15Lkm0O{DPxE1? M2HvdVIzQDJ7MEm0
KM-H2 NV7nRXJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYq3NwKBkWh? NXTmc4lvTE2VTx?= MYfJR|UxRTFwM{C4JO69VQ>? NI\WToUzOjh{OUC5OC=>
L-540 NFTkVnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWS3NwKBkWh? M1TqRmROW09? NETBVnhKSzVyPUiuNlE3KM7:TR?= NVXpN49lOjJ6MkmwPVQ>
HD-LM2 NVfGUHJvTnWwY4Tpc44hSXO|YYm= M1[wSVAvOS9yLkWvNU82KM7:TR?= MVS3NwKBkWh? MlztSG1UVw>? MVvpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NELiXYEzOjh{OUC5OC=>
L-428 NXflPG05TnWwY4Tpc44hSXO|YYm= NWnZWIw2OC5zL{CuOU8yNzVizszN NFvNNXQ4OuLCiXi= MmrZSG1UVw>? M{D3dIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NWfrboJZOjJ6MkmwPVQ>
KM-H2 MUHGeY5kfGmxbjDBd5NigQ>? MWGwMlEwOC53L{GvOUDPxE1? M4jROVcz6oDLaB?= NFHOV2FFVVOR MoLNbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> M{H1OVIzQDJ7MEm0
L-540 M1rTcGZ2dmO2aX;uJGF{e2G7 MVSwMlEwOC53L{GvOUDPxE1? MnjhO|LjiImq Mn;PSG1UVw>? NYTUOnJRcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NF7MSWYzOjh{OUC5OC=>
HD-LM2 M1mxSWFxd3C2b4Ppd{BCe3OjeR?= MYOxM|Uh|ryP MYK3NwKBkWh? Mnn1SG1UVw>? NYHTUmR2cW6mdXPld{BieG:ydH;zbZM> MlLoNlI5OjlyOUS=
L-428 NYHneZQzSXCxcITvd4l{KEG|c3H5 NWTjcIpVOS93IN88US=> MY[3NwKBkWh? M1vo[WROW09? MlXzbY5lfWOnczDhdI9xfG:|aYO= M{m3bVIzQDJ7MEm0
KM-H2 NGLreXZCeG:ydH;zbZMhSXO|YYm= M4XITlEwPSEQvF2= NF3kUWE4OuLCiXi= MnriSG1UVw>? NVr4S5BicW6mdXPld{BieG:ydH;zbZM> MW[yNlgzQTB7NB?=
L-540 M1O5SGFxd3C2b4Ppd{BCe3OjeR?= MVGxM|Uh|ryP M17lSlcz6oDLaB?= NIHt[2tFVVOR NUj2eWwzcW6mdXPld{BieG:ydH;zbZM> NH\wfHYzOjh{OUC5OC=>
U251-MG MlX0SpVv[3Srb36gRZN{[Xl? NF;nSnEyKML3TR?= MYiwMVE3KGh? MVTpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> NGS2[FIzOjB{N{[5NS=>
U87-MG MnTqSpVv[3Srb36gRZN{[Xl? MoHENUDDvU1? MX[wMVE3KGh? M1PNXIlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NYH4doZ{OjJyMke2PVE>
4C8 MkPJSpVv[3Srb36gRZN{[Xl? MVGxJOK2VQ>? MVuwMVE3KGh? MULpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MXyyNlAzPzZ7MR?=
U251-MG NGX2OGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfnSIx7OS9zMDFCuW0> MViyOE81QC95MjDo NH7oWnJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NH[yPFIzOjB{N{[5NS=>
U87-MG M3T5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD1NU8yOCEEtV2= NGSwPIEzPC92OD:3NkBp NUfUWJVqcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NIn0dYEzOjB{N{[5NS=>
4C8 M4nZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2q4SFEwOTBiwsXN MlnBNlQwPDhxN{KgbC=> NFXuZ4xqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MWqyNlAzPzZ7MR?=
U266 Mnv3RZBweHSxc3nzJGF{e2G7 NWG1c29LOC53LUKg{txO NVq5NnBSPDhxN{KgbC=> Mnq2bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NYXR[3E6OjFzNkS1NVc>
Kms.11 NFfjOJdCeG:ydH;zbZMhSXO|YYm= M2PsdFAvPS1{IN88US=> NX:4NpFiPDhxN{KgbC=> NGPue2xqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NF[3UmwzOTF4NEWxOy=>
8226 M{DGfmFxd3C2b4Ppd{BCe3OjeR?= NVHxdGtoOC53LUKg{txO NHvhN2E1QC95MjDo NILmfohqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Mn:wNlEyPjR3MUe=

... 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 warmed (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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