AZD1480 化学構造
分子量: 348.77

高品質保証

カスタマーフィードバック(2)

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 NV3SOZhYTnWwY4Tpc44hSXO|YYm= NHvGeG82KM7:TR?= NF21cHU1QCCq NYrEVlhCTE2VTx?= MYficI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= NYHJNWFxOjV7NUS5O|Q>
LoVo  NGnvRmlHfW6ldHnvckBCe3OjeR?= NVnjcmxEPSEQvF2= NXjPZXR{PDhiaB?= NEPV[5RFVVOR NFnrOFdjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MVWyOVk2PDl5NB?=
HN5 MlTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy3NkBp NYW4PG9OTUN3ME2zMlgyKMLzIEGuPVkh|ryP MlvkNlU5OTByMUC=
Cal33 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjCSYw4OiCq NV\jcI1PTUN3ME2zMlM4KMLzIECuO|Uh|ryP NETBc4czPThzMECxNC=>
UM-22B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHub5A4OiCq NVfxTWh2TUN3ME2yMlY3KMLzIECuNlQh|ryP MojYNlU5OTByMUC=
686LN M2PpbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj4UG9qPzJiaB?= MYnFR|UxRTJwMEWgxtEhOS5|MzFOwG0> Mn7vNlU5OTByMUC=
UM SCC-1 NFW3VHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHpO|IhcA>? MYDFR|UxRTFwNkegxtEhOC52MjFOwG0> NFvnRZczPThzMECxNC=>
UM-22A MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jFTFczKGh? NVjyRVVOTUN3ME2xMlMzKMLzIECuN|kh|ryP M3nX[VI2QDFyMEGw
OSC19 NWfvSodOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TUZ|czKGh? M1HrZ2VEPTB;MT6yOkDDuSByLkKwJO69VQ>? MYSyOVgyODBzMB?=
PCI-52 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi3NkBp MmX0SWM2OD1zLkCwJOKyKDBwMEmg{txO NWDVVIk6OjV6MUCwNVA>
PCI-15B M4LySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrNO|IhcA>? Mnv6SWM2OD1yLkm5JOKyKDFwN{Sg{txO MnG1NlU5OTByMUC=
UMSCC-1 M4\2bGZ2dmO2aX;uJGF{e2G7 NHmydFMxNjByMEWtNU43KM7:TR?= MYiyOEBp M4DHWoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVKyOVgyODBzMB?=
Cal33 NUXuUnVOTnWwY4Tpc44hSXO|YYm= MU[wMlAxODVvMz64JO69VQ>? NYTTc2d3OjRiaB?= MkX2ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlnuNlU5OTByMUC=
HH5 NWjjPZA4TnWwY4Tpc44hSXO|YYm= M2f2TVAvODByNT2zMlgh|ryP NUHtd|NOOjRiaB?= NI\SO2Ri[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGTu[3gzPThzMECxNC=>
UM-22A NHzpTWhHfW6ldHnvckBCe3OjeR?= MUOwMlAxODVvMT62JO69VQ>? NUjyW5Q6OjRiaB?= M4XTR4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYTveFNOOjV6MUCwNVA>
A1847 M3PKXWZ2dmO2aX;uJGF{e2G7 NXmxR404OC5yNT2xNEDPxE1? MU[yOEBp MX;EUXNQyqB? Moj6doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NUfhVVg3OjV4NE[wNVU>
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MOVCAR-5447 NXzMOGpNTnWwY4Tpc44hSXO|YYm= NUXSXXUzOC5yNT2xNEDPxE1? NXHxXmJJOjRiaB?= M3;2RmROW00EoB?= M2\INZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz M3OwZVI2PjR4MEG1
MOVCAR-5009 M{nWOWZ2dmO2aX;uJGF{e2G7 MlzPNE4xPS1zMDFOwG0> NIC0e5EzPCCq M4\3XGROW00EoB?= NHfrfmdz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> M4rOfFI2PjR4MEG1
A1847 MkHDR4VtdCCYaXHibYxqfHliQYPzZZk> NU\JUFhsOC5yNT2xNEDPxE1? NWrP[XdlPzJiaB?= NGW5Z4pFVVOR NV:wXFBvemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MXuyOVY1PjBzNR?=
OVCAR-5 NFvuVZFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIrGW2YxNjB3LUGwJO69VQ>? NYL0cIpwPzJiaB?= NHn6eWVFVVOR MVvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MXmyOVY1PjBzNR?=
OVCAR-8  NX[yV29JS2WubDDWbYFjcWyrdImgRZN{[Xl? M3vjOlAvODVvMUCg{txO MlfZO|IhcA>? M3TkbmROW09? MmPndoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NGfyRmEzPTZ2NkCxOS=>
OVCAR-5  MV7BdI9xfG:|aYOgRZN{[Xl? MYCwMlUwOS93IN88US=> MYq0PEBp MYPEUXNQ NVLnXHdKcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M1XjT|I2PjR4MEG1
OVCAR-8  NGPy[ZJCeG:ydH;zbZMhSXO|YYm= NWS0d5BKOC53L{GvOUDPxE1? M2PZPFQ5KGh? MYXEUXNQ NWLXfG1scW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> MXWyOVY1PjBzNR?=
AKRSL NWjtNohOS2WubDDWbYFjcWyrdImgRZN{[Xl? MnLMO|IhcA>? M3vNSWlEPTExvK6xNEDPxE1? M4TyR|I2PTB2NkO1
PALJDL M1fRdWNmdGxiVnnhZoltcXS7IFHzd4F6 M2C5dFczKGh? M{LVfGlEPTB;Mj60JO69VQ>? NEPzfWIzPTVyNE[zOS=>
MO4 M{jvWWZ2dmO2aX;uJGF{e2G7 MXuwMlUwOS93IN88US=> NGjOXVk3KGh? NHLkc4RqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? M2LkWVI2OTR7NUO1
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DU145  NIfZdJRHfW6ldHnvckBCe3OjeR?= NVr5S3ZwQDByIH7N NH\mRpQ4OiCq M1njOJN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NU[4WppwOjR3N{e5OFI>
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H82 NWj5b|hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nnSmlEPTB;MT6zO{DPxE1? NV3HSXF{OjRzNUi3NFE>
GLC4 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrsTWM2OD1zLke5JO69VQ>? NWLoTZIzOjRzNUi3NFE>
H526 NEjNV21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjrTI9KSzVyPUOuNFgh|ryP NEnEPWgzPDF3OEewNS=>
H1173 MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HWUWlEPTB;Mj6zPUDPxE1? MmDHNlQyPTh5MEG=
DMS114 NVLOdGZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q5VmlEPTB;MD63N{DPxE1? NW\pZ4FKOjRzNUi3NFE>
NCI-N592 MXXGeY5kfGmxbjDBd5NigQ>? NXz4UmtwOC5|L{GvN{DPxE1? MWCyOEBp MkL0bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M1XZeVI1OTV6N{Cx
GLC4 M4fW[2Z2dmO2aX;uJGF{e2G7 M161flAvOy9zL{Og{txO MnfPNlQhcA>? M1;5O4lv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MoD5NlQyPTh5MEG=
NCI-H82 NIHSbXBHfW6ldHnvckBCe3OjeR?= M3HDb|AvOy9zL{Og{txO NWL2VFA2OjRiaB?= MYjpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> M3PQRVI1OTV6N{Cx
NCI-N592 MV;BdI9xfG:|aYOgRZN{[Xl? NGPlTJoxNjNxMT:zJO69VQ>? NWS1fI4{PDhiaB?= NUjhNWNqcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MkiwNlQyPTh5MEG=
GLC4 NHThSHdCeG:ydH;zbZMhSXO|YYm= NUKyXJhUOC5|L{GvN{DPxE1? Mn\UOFghcA>? MXjpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ Ml;YNlQyPTh5MEG=
NCI-H82 MkTmRZBweHSxc3nzJGF{e2G7 NFjreYsxNjNxMT:zJO69VQ>? M4fMOVQ5KGh? NEjC[YhqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NG[ybGszPDF3OEewNS=>
CWR22Rv1  M2jVVWFxd3C2b4Ppd{BCe3OjeR?= MoroTWM2OD1yLkS4NkDPxE1? M1r2e|I{QTR{MEm1
CWR22Pc NHzSb2lCeG:ydH;zbZMhSXO|YYm= NUHJdpJ4UUN3ME2wMlQ{QCEQvF2= NWLBR4xZOjN7NEKwPVU>
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DU145 MV\BdI9xfG:|aYOgRZN{[Xl? Mof0TWM2OD1|LkWxO{DPxE1? MlLDNlM6PDJyOUW=
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ARPE19 Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVez[ZlnTE2VTx?= M2XsTGlEPTB;MkSuN|gh|ryP MUmyN|U{OTl{MR?=
HEK293 M{Hu[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUW0VnJETE2VTx?= NGPUelJKSzVyPUiuOlch|ryP MWeyN|U{OTl{MR?=
KCNR Mn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PzNWROW09? NYH0WJVvUUN3ME2wMlQ3KM7:TR?= M2P1b|I{PTNzOUKx
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BE2 NH:3cWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\EUXNQ NVSwdXlXUUN3ME2wMlcyKM7:TR?= M2jLe|I{PTNzOUKx
AS NV\1VZN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3ueJhFVVOR NGjTc4tKSzVyPUGuOVMh|ryP NFfQNGszOzV|MUmyNS=>
NGP M3P1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jJbmROW09? NGnIR3dKSzVyPUCuOVYh|ryP NUXE[Jd2OjN3M{G5NlE>
IMR32 M1PENmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzBNldKTE2VTx?= M2jL[2lEPTB;MD62OkDPxE1? MWmyN|U{OTl{MR?=
LAN5 M{fJVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDEUXNQ NYrZ[ZFLUUN3ME2xMlA1KM7:TR?= NIfUUowzOzV|MUmyNS=>
RH18 M3HFZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\nW2tLTE2VTx?= MYXJR|UxRTFwNEKg{txO MUeyN|U{OTl{MR?=
RH30 M2GyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TE[mROW09? NHy0Xm9KSzVyPUGuNlUh|ryP MUWyN|U{OTl{MR?=
RH17 M3rzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PJeGROW09? MmLqTWM2OD1{LkWxJO69VQ>? NUHsd4NrOjN3M{G5NlE>
RH28 M3;oe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVv1TZRSTE2VTx?= NI\JbmlKSzVyPUSuNlgh|ryP M1XwUVI{PTNzOUKx
RH36 M2\KPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPOSG1UVw>? NHzET2NKSzVyPUWuN|ch|ryP NVfobFgzOjN3M{G5NlE>
RH41 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G0OGROW09? NHjid3BKSzVyPUCuOFgh|ryP M4X0cVI{PTNzOUKx
RD MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvEUXNQ M1;mTWlEPTB;ND6zNkDPxE1? MVqyN|U{OTl{MR?=
TC32 NUnJWmdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT5RpBFVVOR M3jMeGlEPTB;Mz64OUDPxE1? M2nwcFI{PTNzOUKx
TC71 NVvBdYYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfV[IJpTE2VTx?= MknZTWM2OD12LkOzJO69VQ>? M3K5SlI{PTNzOUKx
KCNR MVXBdI9xfG:|aYOgRZN{[Xl? MkC3NE42NzFwMD:yMlUh|ryP MmPRNlQhcA>? M1XjR2ROW09? M3HSXYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NGjpdW0zOzV|MUmyNS=>
SY5Y MYXBdI9xfG:|aYOgRZN{[Xl? M3fKZ|AvPS9zLkCvNk42KM7:TR?= M1H1elI1KGh? NX7lUnBLTE2VTx?= M2L3OYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MUKyN|U{OTl{MR?=
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Rh18 NIj4ZodHfW6ldHnvckBCe3OjeR?= MYqwMlUwOS5yL{KuOU82KM7:TR?= Mn;iNlQhcA>? MY\EUXNQ M{G1S4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NX\JSIx4OjN3M{G5NlE>
TC32 NETLbHZHfW6ldHnvckBCe3OjeR?= NX71d|d4OC53L{GuNE8zNjVxNTFOwG0> MnzBNlQhcA>? NWLpcZhyTE2VTx?= MkDKbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NV72bpdlOjN3M{G5NlE>
TPC-1 M16yfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG1fXlJOSEEtV2= NU\u[lg2OC12IHS= NVznOmxVTE2VTx?= Ml;3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? Mni5NlMxPTZ2OUm=
MZ-CRC1  MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T2eFEhyrWP MUGwMVUh\A>? NUXsd5BRTE2VTx?= NWTQNXk3cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NVrpdoU{OjNyNU[0PVk>
TT  Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O1UFEhyrWP MWewMVQh\A>? NGjJU2FFVVOR MmnhbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? M3SzdVI{ODV4NEm5
TPC-1 MorZSpVv[3Srb36gRZN{[Xl? NEHJZZIyKML3TR?= MmfhO|IhcA>? Mn\XSG1UVw>? MWfpcoR2[2W|IFexJIJtd2OtYXfl NH3UNYgzOzB3NkS5PS=>
MZ-CRC1  Mn3GSpVv[3Srb36gRZN{[Xl? MXqxJOK2VQ>? M1vJb|czKGh? M{frZWROW09? NF7pcGpqdmS3Y3XzJGcyKGKub3PrZYdm NXfnWo9POjNyNU[0PVk>
TT  NWHUcoZWTnWwY4Tpc44hSXO|YYm= M3rXOlEhyrWP M2jBR|czKGh? Mn:1SG1UVw>? M2rIRYlv\HWlZYOgS|Eh[myxY3vh[4U> NWnjVVN1OjNyNU[0PVk>
MZ-CRC1  NInzOm9CeG:ydH;zbZMhSXO|YYm= Mnu0NUDDvU1? M4DsW|Q5KGh? MXjEUXNQ M4\mXIlv\HWlZYOgZZBweHSxc3nz MlTqNlMxPTZ2OUm=
TT  NVnzb21PSXCxcITvd4l{KEG|c3H5 NH70cFQyKML3TR?= Mlv6OFghcA>? M3\ZT2ROW09? NW\2[IFLcW6mdXPld{BieG:ydH;zbZM> MX6yN|A2PjR7OR?=
HD-LM2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUm3NwKBkWh? NHz6XGlFVVOR NV3ofIg2UUN3ME23Mlg1PCEQvF2= NYq4VlBGOjJ6MkmwPVQ>
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KM-H2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYO3NwKBkWh? NEHBVI9FVVOR NFm5WJZKSzVyPUGuN|A5KM7:TR?= NELrOmczOjh{OUC5OC=>
L-540 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj2O|LjiImq NWq1RldXTE2VTx?= MWfJR|UxRThwMkG2JO69VQ>? MVqyNlgzQTB7NB?=
HD-LM2 M3izbmZ2dmO2aX;uJGF{e2G7 MmrTNE4yNzBwNT:xM|Uh|ryP M3fGOFcz6oDLaB?= MXfEUXNQ M3faNIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MXKyNlgzQTB7NB?=
L-428 Ml24SpVv[3Srb36gRZN{[Xl? MWWwMlEwOC53L{GvOUDPxE1? NHfQZow4OuLCiXi= MWrEUXNQ NXjW[4ljcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MWmyNlgzQTB7NB?=
KM-H2 MonTSpVv[3Srb36gRZN{[Xl? NWrON5I6OC5zL{CuOU8yNzVizszN M2rq[Fcz6oDLaB?= MVjEUXNQ NFn5UoRqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NInrWGQzOjh{OUC5OC=>
L-540 Mn3hSpVv[3Srb36gRZN{[Xl? M1HiWVAvOS9yLkWvNU82KM7:TR?= NVq4O5dsPzMkgJno M3fFNmROW09? MY\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NWezW|NkOjJ6MkmwPVQ>
HD-LM2 NFvZS|NCeG:ydH;zbZMhSXO|YYm= MoTmNU82KM7:TR?= MnnGO|LjiImq NEjLflBFVVOR MU\pcoR2[2W|IHHwc5B1d3Orcx?= MmK2NlI5OjlyOUS=
L-428 NX33eZkzSXCxcITvd4l{KEG|c3H5 NU\vfmR3OS93IN88US=> NIn3SWo4OuLCiXi= MkXPSG1UVw>? MXrpcoR2[2W|IHHwc5B1d3Orcx?= M1\BWFIzQDJ7MEm0
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U251-MG NHvsS2lHfW6ldHnvckBCe3OjeR?= MlLoNUDDvU1? M4qxOFAuOTZiaB?= MVLpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> NF\hfJUzOjB{N{[5NS=>
U87-MG MV7GeY5kfGmxbjDBd5NigQ>? NFSzVm0yKML3TR?= M1TPcFAuOTZiaB?= NXTC[lRucW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NIfhOpgzOjB{N{[5NS=>
4C8 M{Tid2Z2dmO2aX;uJGF{e2G7 NV7OSW93OSEEtV2= MljONE0yPiCq NWfHbHVGcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NYPnWGtPOjJyMke2PVE>
U251-MG NF7YfpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfYVIRHOS9zMDFCuW0> NYC5R25kOjRxNEivO|IhcA>? M2fJ[YlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO MnHDNlIxOjd4OUG=
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8226 NFjF[41CeG:ydH;zbZMhSXO|YYm= M2fKSFAvPS1{IN88US=> M2TCW|Q5Nzd{IHi= NUDCPVVHcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M3\4XFIyOTZ2NUG3

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 69 mg/mL warming (197.83 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 (13)

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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