AZD1480

AZD1480は一種の新たなATP競争性JAK2阻害剤で、無細胞試験でIC50値が 0.26 nMになって、JAK3とTyk2に選択性的に作用して、JAK1に作用することが弱いです。臨床1期。

価格 在庫  
USD 126 あり
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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は一種の新たなATP競争性JAK2阻害剤で、無細胞試験でIC50値が 0.26 nMになって、JAK3とTyk2に選択性的に作用して、JAK1に作用することが弱いです。臨床1期。
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 M2H1dGZ2dmO2aX;uJGF{e2G7 M2\FSVUh|ryP M1TUW|Q5KGh? NEXzZ3hFVVOR NF\XZ4JjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NGfMSYIzPTl3NEm3OC=>
LoVo  MXPGeY5kfGmxbjDBd5NigQ>? NHXKfIw2KM7:TR?= M3i4bVQ5KGh? M3jLWGROW09? M2DBUIJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> NEDocpkzPTl3NEm3OC=>
HN5 NUjj[JF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDaO|IhcA>? NYjlUGpqTUN3ME2zMlgyKMLzIEGuPVkh|ryP MYqyOVgyODBzMB?=
Cal33 MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu2UoRpPzJiaB?= NUTlOYtHTUN3ME2zMlM4KMLzIECuO|Uh|ryP M4LLO|I2QDFyMEGw
UM-22B M3nmcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnGyO|IhcA>? NFLjTGxGSzVyPUKuOlYhyrFiMD6yOEDPxE1? MonFNlU5OTByMUC=
686LN MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H2NVczKGh? Mk\WSWM2OD1{LkC1JOKyKDFwM{Og{txO NFPIXpQzPThzMECxNC=>
UM SCC-1 M3vXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTSbGc4OiCq MlP6SWM2OD1zLk[3JOKyKDBwNEKg{txO NWX4O5M5OjV6MUCwNVA>
UM-22A Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7mO|IhcA>? NFjhS41GSzVyPUGuN|IhyrFiMD6zPUDPxE1? M{X4XVI2QDFyMEGw
OSC19 MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO3NkBp M{XXeWVEPTB;MT6yOkDDuSByLkKwJO69VQ>? M3\xTlI2QDFyMEGw
PCI-52 MlHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq3NkBp NG\KXnZGSzVyPUGuNFAhyrFiMD6wPUDPxE1? NGT5cFUzPThzMECxNC=>
PCI-15B MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH0O|IhcA>? M4r3VGVEPTB;MD65PUDDuSBzLke0JO69VQ>? MXqyOVgyODBzMB?=
UMSCC-1 M1viS2Z2dmO2aX;uJGF{e2G7 NFy1OGoxNjByMEWtNU43KM7:TR?= NFKxRYMzPCCq M{TGeoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3vN[VI2QDFyMEGw
Cal33 NFLyO5dHfW6ldHnvckBCe3OjeR?= MoHGNE4xODB3LUOuPEDPxE1? MYOyOEBp NEDON2Zi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXqyOVgyODBzMB?=
HH5 MlvISpVv[3Srb36gRZN{[Xl? MWewMlAxODVvMz64JO69VQ>? MnfSNlQhcA>? MlrKZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXWyOVgyODBzMB?=
UM-22A NX:3bphMTnWwY4Tpc44hSXO|YYm= MXqwMlAxODVvMT62JO69VQ>? NGLaT|YzPCCq M3q4VoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MorwNlU5OTByMUC=
A1847 M2\GWWZ2dmO2aX;uJGF{e2G7 MX2wMlA2NTFyIN88US=> NGPDepUzPCCq MWrEUXNQyqB? M3zxN5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NUnYeWx4OjV4NE[wNVU>
OVCAR-5 NWHufZA2TnWwY4Tpc44hSXO|YYm= NH7PNooxNjB3LUGwJO69VQ>? MU[yOEBp Mmm5SG1UV8Li Mlr1doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NXzae3ZGOjV4NE[wNVU>
OVCAR-8 NFzHWWxHfW6ldHnvckBCe3OjeR?= M3\MeFAvODVvMUCg{txO NV3Dcow3OjRiaB?= M{W5S2ROW00EoB?= MWny[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MUGyOVY1PjBzNR?=
MOVCAR-5447 MmHaSpVv[3Srb36gRZN{[Xl? NWLOdZQyOC5yNT2xNEDPxE1? MomzNlQhcA>? MnO3SG1UV8Li NFfNUWFz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MWiyOVY1PjBzNR?=
MOVCAR-5009 NFuwN|RHfW6ldHnvckBCe3OjeR?= NH7OZZIxNjB3LUGwJO69VQ>? NXfiXIt6OjRiaB?= M1jEXWROW00EoB?= MonNdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NGrPc3gzPTZ2NkCxOS=>
A1847 NESyPHFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYrPZWk{OC5yNT2xNEDPxE1? M4nhWFczKGh? NHfXZZFFVVOR Mn7zdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MUCyOVY1PjBzNR?=
OVCAR-5 MkXuR4VtdCCYaXHibYxqfHliQYPzZZk> NYrNfZN4OC5yNT2xNEDPxE1? NWi3[Gw6PzJiaB?= NWLGNJY1TE2VTx?= NEnj[XJz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> M4jZ[|I2PjR4MEG1
OVCAR-8  NFPkdlZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVWwMlA2NTFyIN88US=> MVm3NkBp NHO2em9FVVOR M{LpUZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN Mn[xNlU3PDZyMUW=
OVCAR-5  NGDhNY1CeG:ydH;zbZMhSXO|YYm= NXXXS|k5OC53L{GvOUDPxE1? NXfuS5I6PDhiaB?= M{fCZmROW09? MX7pcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w M{SxT|I2PjR4MEG1
OVCAR-8  M4m2d2Fxd3C2b4Ppd{BCe3OjeR?= NVTx[W1VOC53L{GvOUDPxE1? M3TVPVQ5KGh? NIrVe4JFVVOR NWPpZVBwcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M{DyU|I2PjR4MEG1
AKRSL M13KPGNmdGxiVnnhZoltcXS7IFHzd4F6 NV3OWnoyPzJiaB?= MVXJR|Ux97zgMUCg{txO Ml:4NlU2ODR4M{W=
PALJDL MkXiR4VtdCCYaXHibYxqfHliQYPzZZk> NGnMTYk4OiCq NUH0dm5TUUN3ME2yMlQh|ryP MWqyOVUxPDZ|NR?=
MO4 NEXncnFHfW6ldHnvckBCe3OjeR?= M37zTVAvPS9zL{Wg{txO NHTSeIc3KGh? NHP6T2RqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NYP5SpNxOjVzNEm1N|U>
DU145  NWPNNFB3TnWwY4Tpc44hSXO|YYm= Mo\yNE0zODBibl2= MU[xJIjDqA>? Mnqwd5VxeHKnc4Pld{BKVC14LXHjeIl3[XSnZDDTeIF1OyCjbnSgSXJMOS9{IIPp[45idGmwZx?= MnPmNlQ2Pzd7NEK=
DU145  NEH6VpdHfW6ldHnvckBCe3OjeR?= M2q3blgxOCCwTR?= NFzSTpA4OiCq NYTRXVRLe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 NV7uN4o5OjR3N{e5OFI>
CWR22Rv1 NWjLTllFTnWwY4Tpc44hSXO|YYm= MVq4NFAhdk1? NIDPbms4OiCq NFrETod{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= MX:yOFU4Pzl2Mh?=
N592 NUW3fZFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjuNm1KSzVyPUCuPFQh|ryP NIe0d|YzPDF3OEewNS=>
H82 M3z5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH21eZlKSzVyPUGuN|ch|ryP NV3t[JJrOjRzNUi3NFE>
GLC4 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXJTWM2OD1zLke5JO69VQ>? MUOyOFE2QDdyMR?=
H526 M1nKcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluyTWM2OD1|LkC4JO69VQ>? NV6z[m12OjRzNUi3NFE>
H1173 NF3nPYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moe5TWM2OD1{LkO5JO69VQ>? NUK5VZVwOjRzNUi3NFE>
DMS114 NYj3N4twT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwN{Og{txO NV60U2dZOjRzNUi3NFE>
NCI-N592 MWnGeY5kfGmxbjDBd5NigQ>? NFy5UWsxNjNxMT:zJO69VQ>? NWThNplyOjRiaB?= NWH6bXQ2cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NGL3Rm0zPDF3OEewNS=>
GLC4 MULGeY5kfGmxbjDBd5NigQ>? NFvhfFQxNjNxMT:zJO69VQ>? NVjPOI57OjRiaB?= NYHPepc5cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M4e5c|I1OTV6N{Cx
NCI-H82 M{e5cGZ2dmO2aX;uJGF{e2G7 MnnLNE4{NzFxMzFOwG0> NY\pWW1HOjRiaB?= M{fic4lv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MVmyOFE2QDdyMR?=
NCI-N592 NIS3XZRCeG:ydH;zbZMhSXO|YYm= NHLB[3QxNjNxMT:zJO69VQ>? MWq0PEBp M33KRYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NUfFWpZ7OjRzNUi3NFE>
GLC4 MlLsRZBweHSxc3nzJGF{e2G7 NF3iO3UxNjNxMT:zJO69VQ>? MnnwOFghcA>? MnTBbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NGHsPXMzPDF3OEewNS=>
NCI-H82 MXfBdI9xfG:|aYOgRZN{[Xl? MkXQNE4{NzFxMzFOwG0> MlTOOFghcA>? MVHpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NXHMdVlWOjRzNUi3NFE>
CWR22Rv1  MUXBdI9xfG:|aYOgRZN{[Xl? M3zPZWlEPTB;MD60PFIh|ryP MX:yN|k1OjB7NR?=
CWR22Pc Ml;SRZBweHSxc3nzJGF{e2G7 NHi1foNKSzVyPUCuOFM5KM7:TR?= MlPMNlM6PDJyOUW=
PC-3 NVLBepl[SXCxcITvd4l{KEG|c3H5 NVHkNY5NUUN3ME2xMlc2PSEQvF2= MoWzNlM6PDJyOUW=
DU145 MXfBdI9xfG:|aYOgRZN{[Xl? M1PyWmlEPTB;Mz61NVch|ryP MlzlNlM6PDJyOUW=
RC165N MVzBdI9xfG:|aYOgRZN{[Xl? Mn;hTWM2OD1{LkC4N{DPxE1? NELTRo0zOzl2MkC5OS=>
ARPE19 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHvSG1UVw>? Ml6yTWM2OD1{ND6zPEDPxE1? M{LaeFI{PTNzOUKx
HEK293 NGD4UHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\kSG1UVw>? M3jGbWlEPTB;OD62O{DPxE1? MnPPNlM2OzF7MkG=
KCNR Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHiSG1UVw>? MlXzTWM2OD1yLkS2JO69VQ>? MlfSNlM2OzF7MkG=
SY5Y NWnN[Gw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrFSG1UVw>? MYDJR|UxRTBwM{[g{txO MXqyN|U{OTl{MR?=
BE2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\WOo1FVVOR MkfzTWM2OD1yLkexJO69VQ>? NF7NPYEzOzV|MUmyNS=>
AS MmmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnnSG1UVw>? M3WyVGlEPTB;MT61N{DPxE1? NG\XcogzOzV|MUmyNS=>
NGP M4HNPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTjSG1UVw>? MkDuTWM2OD1yLkW2JO69VQ>? MYqyN|U{OTl{MR?=
IMR32 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDEUXNQ MkPaTWM2OD1yLk[2JO69VQ>? NXHhSGFpOjN3M{G5NlE>
LAN5 NIK1OWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm5R3NFVVOR MlzZTWM2OD1zLkC0JO69VQ>? MWmyN|U{OTl{MR?=
RH18 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT2UWdFVVOR NH7Yfo5KSzVyPUGuOFIh|ryP NV3EU5h6OjN3M{G5NlE>
RH30 Mni1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi4SG1UVw>? M3\0TWlEPTB;MT6yOUDPxE1? MXyyN|U{OTl{MR?=
RH17 M2TVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT0NnRFVVOR NGPCRXdKSzVyPUKuOVEh|ryP NH3rS3czOzV|MUmyNS=>
RH28 NYPsSWh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHwW3FFVVOR MYPJR|UxRTRwMkig{txO MnLzNlM2OzF7MkG=
RH36 M{jGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTEUXNQ MXfJR|UxRTVwM{eg{txO NGLEUG4zOzV|MUmyNS=>
RH41 MnWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T2ZmROW09? NFTNXYFKSzVyPUCuOFgh|ryP MlXVNlM2OzF7MkG=
RD MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknaSG1UVw>? MYHJR|UxRTRwM{Kg{txO M37TTFI{PTNzOUKx
TC32 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\NT|lFVVOR MnXLTWM2OD1|Lki1JO69VQ>? M{G4fVI{PTNzOUKx
TC71 Ml:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL1fXRHTE2VTx?= M3f2d2lEPTB;ND6zN{DPxE1? MUCyN|U{OTl{MR?=
KCNR Mn3SRZBweHSxc3nzJGF{e2G7 MlTFNE42NzFwMD:yMlUh|ryP M13KTlI1KGh? M3HXeWROW09? M{DFXolv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MVqyN|U{OTl{MR?=
SY5Y MmH2RZBweHSxc3nzJGF{e2G7 NV3BR3VzOC53L{GuNE8zNjVizszN MWWyOEBp MXzEUXNQ M{\CNYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MmfINlM2OzF7MkG=
Rh18 Ml3lRZBweHSxc3nzJGF{e2G7 NEXsU4gxNjVxMT6wM|IvPSEQvF2= NW\EUZY6OjRiaB?= MWrEUXNQ NFnsTIVqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NHrtSYgzOzV|MUmyNS=>
TC32 MnvXRZBweHSxc3nzJGF{e2G7 M4n0flAvPS9zLkCvNk42KM7:TR?= NYHjSXJIOjRiaB?= MV;EUXNQ NE\PS2hqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MU[yN|U{OTl{MR?=
KCNR MV3GeY5kfGmxbjDBd5NigQ>? MmLWNE42NzFwMD:yMlUwPSEQvF2= NXH3[2MxOjRiaB?= NVjrfJc5TE2VTx?= M2DkR4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NXm5SoZ7OjN3M{G5NlE>
SY5Y MoDiSpVv[3Srb36gRZN{[Xl? NU\KR2FxOC53L{GuNE8zNjVxNTFOwG0> NGfW[IczPCCq MljuSG1UVw>? MYfpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= Ml3MNlM2OzF7MkG=
Rh18 NHXFPI1HfW6ldHnvckBCe3OjeR?= Mn;2NE42NzFwMD:yMlUwPSEQvF2= M4T2S|I1KGh? MoflSG1UVw>? M1XD[olvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u M3LRfFI{PTNzOUKx
TC32 M3;rTGZ2dmO2aX;uJGF{e2G7 NYLyS2ZkOC53L{GuNE8zNjVxNTFOwG0> MmX0NlQhcA>? M2XtRmROW09? M1nzWYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u MnTpNlM2OzF7MkG=
TPC-1 NXH0TVBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17hUFEhyrWP NEjBT5kxNTRiZB?= M1L5[WROW09? Ml3lbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? NWHEbmN1OjNyNU[0PVk>
MZ-CRC1  NYPmOmRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnGyNUDDvU1? M3jNOFAuPSCm NU\sSYdLTE2VTx?= NFO0V3BqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 NIH6elUzOzB3NkS5PS=>
TT  MnfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVexJOK2VQ>? M2jXO|AuPCCm NUjL[lZlTE2VTx?= MVzpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 MYWyN|A2PjR7OR?=
TPC-1 MVXGeY5kfGmxbjDBd5NigQ>? MWOxJOK2VQ>? MmH3O|IhcA>? NGLxUGNFVVOR NGT2ZmFqdmS3Y3XzJGcyKGKub3PrZYdm M{TLc|I{ODV4NEm5
MZ-CRC1  NWm2SG16TnWwY4Tpc44hSXO|YYm= NH[2d|UyKML3TR?= M{nhc|czKGh? NGXxPZJFVVOR Moq5bY5lfWOnczDHNUBjdG:la3Hn[S=> M2izdFI{ODV4NEm5
TT  NH21U3BHfW6ldHnvckBCe3OjeR?= NIHpUYgyKML3TR?= NEDWb2s4OiCq MUfEUXNQ Mn3EbY5lfWOnczDHNUBjdG:la3Hn[S=> MV2yN|A2PjR7OR?=
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L-428 M3zKR2Z2dmO2aX;uJGF{e2G7 MUewMlEwOC53L{GvOUDPxE1? MUi3NwKBkWh? NIW1ZVJFVVOR NGqzUIhqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? MX6yNlgzQTB7NB?=
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8226 M1vFb2Fxd3C2b4Ppd{BCe3OjeR?= MX:wMlUuOiEQvF2= NUnHN|NDPDhxN{KgbC=> M{nRbYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MkTPNlEyPjR3MUe=

... 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)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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