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。

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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 NYjVS|htTnWwY4Tpc44hSXO|YYm= NH\Nd2s2KM7:TR?= MnTYOFghcA>? M1\CS2ROW09? Mlr2Zoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n MnjQNlU6PTR7N{S=
LoVo  M1PXWGZ2dmO2aX;uJGF{e2G7 MWi1JO69VQ>? M4DpVVQ5KGh? MnnmSG1UVw>? NYDjVIpr[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NWrZOWI2OjV7NUS5O|Q>
HN5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7YXWE4OiCq MnPvSWM2OD1|LkixJOKyKDFwOUmg{txO MVOyOVgyODBzMB?=
Cal33 NUTsbXFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL6WIg4OiCq MVnFR|UxRTNwM{egxtEhOC55NTFOwG0> MkfINlU5OTByMUC=
UM-22B M1X4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXSO|IhcA>? MnTnSWM2OD1{Lk[2JOKyKDBwMkSg{txO NGHIe5EzPThzMECxNC=>
686LN NW[ydHV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jHS|czKGh? MoTESWM2OD1{LkC1JOKyKDFwM{Og{txO MYqyOVgyODBzMB?=
UM SCC-1 MoLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fVN|czKGh? M4DJfGVEPTB;MT62O{DDuSByLkSyJO69VQ>? M2fScVI2QDFyMEGw
UM-22A M3vyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\VNZNlPzJiaB?= NILSPJRGSzVyPUGuN|IhyrFiMD6zPUDPxE1? MYKyOVgyODBzMB?=
OSC19 MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYK3NkBp MY\FR|UxRTFwMk[gxtEhOC5{MDFOwG0> M{X3dVI2QDFyMEGw
PCI-52 M{X0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUe3NkBp Ml72SWM2OD1zLkCwJOKyKDBwMEmg{txO MXiyOVgyODBzMB?=
PCI-15B NYrPXXZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFryenQ4OiCq MXrFR|UxRTBwOUmgxtEhOS55NDFOwG0> NIfIc5kzPThzMECxNC=>
UMSCC-1 M{XVbGZ2dmO2aX;uJGF{e2G7 NGrncHMxNjByMEWtNU43KM7:TR?= NHy1SXEzPCCq M2TYNIFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYq5UFFyOjV6MUCwNVA>
Cal33 MljhSpVv[3Srb36gRZN{[Xl? Mn:zNE4xODB3LUOuPEDPxE1? M1PPflI1KGh? M4PRZoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYGyOVgyODBzMB?=
HH5 M3;o[mZ2dmO2aX;uJGF{e2G7 MmjRNE4xODB3LUOuPEDPxE1? NGq0R3EzPCCq NXrPco1Y[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2\1TVI2QDFyMEGw
UM-22A NUDaWnF{TnWwY4Tpc44hSXO|YYm= NUDaTYxvOC5yMEC1MVEvPiEQvF2= MVmyOEBp NV7ORZlD[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkfHNlU5OTByMUC=
A1847 M1XU[WZ2dmO2aX;uJGF{e2G7 MljCNE4xPS1zMDFOwG0> M2rlbFI1KGh? M4rIfGROW00EoB?= MUTy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= M2T5UFI2PjR4MEG1
OVCAR-5 NYLoVnlwTnWwY4Tpc44hSXO|YYm= NXyzWotwOC5yNT2xNEDPxE1? NUmxW4dIOjRiaB?= NH\CZ2lFVVORwrC= NEDIcJBz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NEHHW2QzPTZ2NkCxOS=>
OVCAR-8 MYLGeY5kfGmxbjDBd5NigQ>? NGfhbnExNjB3LUGwJO69VQ>? MYKyOEBp NF3YXIpFVVORwrC= MorCdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NIPlbowzPTZ2NkCxOS=>
MOVCAR-5447 NEj0WJhHfW6ldHnvckBCe3OjeR?= NX2xRXlLOC5yNT2xNEDPxE1? NF;hWWozPCCq MkXFSG1UV8Li NVTNeXFIemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M2TGS|I2PjR4MEG1
MOVCAR-5009 MXLGeY5kfGmxbjDBd5NigQ>? MlTTNE4xPS1zMDFOwG0> NE\nTYwzPCCq M1r5W2ROW00EoB?= MYLy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MXmyOVY1PjBzNR?=
A1847 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2i1[lAvODVvMUCg{txO NYLiUpBCPzJiaB?= Mn;DSG1UVw>? MYry[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= NYrGZ3Q5OjV4NE[wNVU>
OVCAR-5 MnzlR4VtdCCYaXHibYxqfHliQYPzZZk> MW[wMlA2NTFyIN88US=> NHLy[Fc4OiCq MXrEUXNQ MVvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MWOyOVY1PjBzNR?=
OVCAR-8  MmLhR4VtdCCYaXHibYxqfHliQYPzZZk> NHPCXXMxNjB3LUGwJO69VQ>? NGPoZlU4OiCq MkXJSG1UVw>? MUny[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MUiyOVY1PjBzNR?=
OVCAR-5  NH70PYxCeG:ydH;zbZMhSXO|YYm= NXT3NpBtOC53L{GvOUDPxE1? NUHUUWs4PDhiaB?= MUfEUXNQ M{fKXIlv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MWCyOVY1PjBzNR?=
OVCAR-8  MX7BdI9xfG:|aYOgRZN{[Xl? NV25OY9wOC53L{GvOUDPxE1? NHKxVnc1QCCq M1ywUGROW09? NHfaW2VqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u MnuwNlU3PDZyMUW=
AKRSL NGXzSHFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVG3NkBp NHL3ZoJKSzVy78{eNVAh|ryP M2nJWFI2PTB2NkO1
PALJDL NHLPeG1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnnqO|IhcA>? MVzJR|UxRTJwNDFOwG0> M37BR|I2PTB2NkO1
MO4 MnP3SpVv[3Srb36gRZN{[Xl? MXOwMlUwOS93IN88US=> MXK2JIg> NVi1VY5DcW6qaXLpeJMhWC2VVFHUN{BmgHC{ZYPzbY9vyqB? MWKyOVE1QTV|NR?=
DU145  M4i2fWZ2dmO2aX;uJGF{e2G7 M3vaXFAuOjByIH7N NUHiZo5POSCqwrC= MVTzeZBxemW|c3XzJGlNNTZvYXP0bZZifGWmIGP0ZZQ{KGGwZDDFVmsyNzJic3nncoFtcW6p Mm[2NlQ2Pzd7NEK=
DU145  MXLGeY5kfGmxbjDBd5NigQ>? M3zKR|gxOCCwTR?= NHy2SJQ4OiCq MoT0d5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 M1jNd|I1PTd5OUSy
CWR22Rv1 MlfhSpVv[3Srb36gRZN{[Xl? NEfWZXQ5ODBibl2= MVe3NkBp MlXYd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 MVuyOFU4Pzl2Mh?=
N592 M{fhe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfkTWM2OD1yLki0JO69VQ>? NWC1N49NOjRzNUi3NFE>
H82 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjrTWM2OD1zLkO3JO69VQ>? NF64T|QzPDF3OEewNS=>
GLC4 NHO5T4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHQ[GxuUUN3ME2xMlc6KM7:TR?= NVWzb5V5OjRzNUi3NFE>
H526 M3rHRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf6[lFKSzVyPUOuNFgh|ryP NEPmd|YzPDF3OEewNS=>
H1173 MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XOcmlEPTB;Mj6zPUDPxE1? MVqyOFE2QDdyMR?=
DMS114 M4nHdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmK0TWM2OD1yLkezJO69VQ>? M3e3XlI1OTV6N{Cx
NCI-N592 MUHGeY5kfGmxbjDBd5NigQ>? NHHN[HUxNjNxMT:zJO69VQ>? NGO2WIszPCCq MWfpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> MmH0NlQyPTh5MEG=
GLC4 MmXlSpVv[3Srb36gRZN{[Xl? M{fIclAvOy9zL{Og{txO MlTaNlQhcA>? NYrOXHUzcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NXvUXGJxOjRzNUi3NFE>
NCI-H82 MVrGeY5kfGmxbjDBd5NigQ>? NXT1UIlvOC5|L{GvN{DPxE1? MnXiNlQhcA>? M1TqNolv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NY\uNFVmOjRzNUi3NFE>
NCI-N592 Mm\nRZBweHSxc3nzJGF{e2G7 MUmwMlMwOS9|IN88US=> MnHFOFghcA>? NVXPNHBZcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NGjldHUzPDF3OEewNS=>
GLC4 NWTESJdPSXCxcITvd4l{KEG|c3H5 M3fHeVAvOy9zL{Og{txO NYPwVWs5PDhiaB?= NWnmbJpFcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MUOyOFE2QDdyMR?=
NCI-H82 NFrSfXlCeG:ydH;zbZMhSXO|YYm= NFLvfJExNjNxMT:zJO69VQ>? NUGxOopQPDhiaB?= MknBbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? M2jn[FI1OTV6N{Cx
CWR22Rv1  NYrYZ3l[SXCxcITvd4l{KEG|c3H5 M3j1[mlEPTB;MD60PFIh|ryP M2\pWVI{QTR{MEm1
CWR22Pc NXLKbm9FSXCxcITvd4l{KEG|c3H5 MYfJR|UxRTBwNEO4JO69VQ>? NYfwOpk6OjN7NEKwPVU>
PC-3 MVrBdI9xfG:|aYOgRZN{[Xl? NI[0epBKSzVyPUGuO|U2KM7:TR?= NF\qOYozOzl2MkC5OS=>
DU145 NY\XW3dlSXCxcITvd4l{KEG|c3H5 MVvJR|UxRTNwNUG3JO69VQ>? MWGyN|k1OjB7NR?=
RC165N MXzBdI9xfG:|aYOgRZN{[Xl? MUHJR|UxRTJwMEizJO69VQ>? MnzTNlM6PDJyOUW=
ARPE19 NIHMXpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH2TYNFVVOR NV7LVFhZUUN3ME2yOE4{QCEQvF2= M4m0b|I{PTNzOUKx
HEK293 NHvPUnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zvO2ROW09? NFKxNG9KSzVyPUiuOlch|ryP Mn7QNlM2OzF7MkG=
KCNR M4Hq[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe5OWlFVVOR M4CycGlEPTB;MD60OkDPxE1? NITjZ3QzOzV|MUmyNS=>
SY5Y NF6welJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3ZSGtFVVOR NIXVbIRKSzVyPUCuN|Yh|ryP M2XXZlI{PTNzOUKx
BE2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfINJRCTE2VTx?= MU\JR|UxRTBwN{Gg{txO M{jCPFI{PTNzOUKx
AS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[ySG1UVw>? NUP6NmM4UUN3ME2xMlU{KM7:TR?= M1zWdFI{PTNzOUKx
NGP MkDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHGydXZFVVOR MnjmTWM2OD1yLkW2JO69VQ>? NEnhN4MzOzV|MUmyNS=>
IMR32 NUjHSZNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK1b4hFVVOR M{HMfWlEPTB;MD62OkDPxE1? NIXNeYIzOzV|MUmyNS=>
LAN5 NGTQdlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDYcW5FVVOR NX\DV5lHUUN3ME2xMlA1KM7:TR?= NXjsU|hoOjN3M{G5NlE>
RH18 Mnn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zTZWROW09? NWL6R2V1UUN3ME2xMlQzKM7:TR?= MYKyN|U{OTl{MR?=
RH30 M1z3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u5[WROW09? MVfJR|UxRTFwMkWg{txO NELjNVMzOzV|MUmyNS=>
RH17 NH7Yc|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnEUXNQ NXjUSWplUUN3ME2yMlUyKM7:TR?= MXqyN|U{OTl{MR?=
RH28 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m0eGROW09? MnLiTWM2OD12LkK4JO69VQ>? NXzadWFqOjN3M{G5NlE>
RH36 M33xcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTPSG1UVw>? MofiTWM2OD13LkO3JO69VQ>? M4\BR|I{PTNzOUKx
RH41 NHvlVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTEUXNQ M3PoSGlEPTB;MD60PEDPxE1? MY[yN|U{OTl{MR?=
RD Mm\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nPSGROW09? MnLVTWM2OD12LkOyJO69VQ>? Mn3sNlM2OzF7MkG=
TC32 MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFf4cZpFVVOR NEn6NWRKSzVyPUOuPFUh|ryP NVfjcGt5OjN3M{G5NlE>
TC71 NVzMXG9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1foXmROW09? NGLBemdKSzVyPUSuN|Mh|ryP NXTmWZluOjN3M{G5NlE>
KCNR NFfPTolCeG:ydH;zbZMhSXO|YYm= NH3QdGExNjVxMT6wM|IvPSEQvF2= NXT1c3BWOjRiaB?= NIq2e|hFVVOR MYnpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NW[xfG1wOjN3M{G5NlE>
SY5Y MVTBdI9xfG:|aYOgRZN{[Xl? M{CyVVAvPS9zLkCvNk42KM7:TR?= NY\lS3dDOjRiaB?= M4DkN2ROW09? NVTIVoo3cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MmKzNlM2OzF7MkG=
Rh18 MkPURZBweHSxc3nzJGF{e2G7 NH\PXpMxNjVxMT6wM|IvPSEQvF2= MUiyOEBp MnXjSG1UVw>? M4SwVolv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MkC5NlM2OzF7MkG=
TC32 NFnjRoZCeG:ydH;zbZMhSXO|YYm= MWiwMlUwOS5yL{KuOUDPxE1? NV;EXJFyOjRiaB?= NYHpbVV1TE2VTx?= NEfNeXVqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NVXW[ZEyOjN3M{G5NlE>
KCNR MWTGeY5kfGmxbjDBd5NigQ>? MX6wMlUwOS5yL{KuOU82KM7:TR?= MWGyOEBp NH7B[HJFVVOR MWLpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NYjWO4ZXOjN3M{G5NlE>
SY5Y MXTGeY5kfGmxbjDBd5NigQ>? M4[1ZlAvPS9zLkCvNk42NzVizszN NV7FXYJkOjRiaB?= MWXEUXNQ MYPpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NXrWcVVWOjN3M{G5NlE>
Rh18 MnTZSpVv[3Srb36gRZN{[Xl? MoDuNE42NzFwMD:yMlUwPSEQvF2= NIXlOVMzPCCq Ml7hSG1UVw>? MWLpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MYWyN|U{OTl{MR?=
TC32 NUjwR4p1TnWwY4Tpc44hSXO|YYm= NHj6TYExNjVxMT6wM|IvPS93IN88US=> NXfVcJVxOjRiaB?= MXLEUXNQ NF\Uc2NqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NIDpfYszOzV|MUmyNS=>
TPC-1 M3[3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\XOnliOSEEtV2= NGi3WI8xNTRiZB?= MnnaSG1UVw>? NUHMbYNlcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOiCmIITy[YF1dWWwdB?= NILYbFkzOzB3NkS5PS=>
MZ-CRC1  NXvsbog5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUCxJOK2VQ>? MYKwMVUh\A>? MXXEUXNQ Mm[zbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? NEXjWJMzOzB3NkS5PS=>
TT  MoLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXXOoo1OSEEtV2= NV[4NIdxOC12IHS= NIP5cJlFVVOR NXGzPG9YcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NEGwOGIzOzB3NkS5PS=>
TPC-1 NUjOWXF6TnWwY4Tpc44hSXO|YYm= NF;mTGsyKML3TR?= M{j0ZVczKGh? MVzEUXNQ M3;teolv\HWlZYOgS|Eh[myxY3vh[4U> M3zw[VI{ODV4NEm5
MZ-CRC1  NXPVU2oyTnWwY4Tpc44hSXO|YYm= NVrNb2ROOSEEtV2= NYSxO2F6PzJiaB?= M2HOfWROW09? NEfaNoFqdmS3Y3XzJGcyKGKub3PrZYdm NFHQVIozOzB3NkS5PS=>
TT  M1vPZ2Z2dmO2aX;uJGF{e2G7 M{O4WFEhyrWP NYf3d5Q2PzJiaB?= NIXxXXRFVVOR NIL2dHZqdmS3Y3XzJGcyKGKub3PrZYdm NHvsWXYzOzB3NkS5PS=>
MZ-CRC1  MmTURZBweHSxc3nzJGF{e2G7 MkjwNUDDvU1? NGLuOJo1QCCq MW\EUXNQ NYPHNIlEcW6mdXPld{BieG:ydH;zbZM> NGTiXJAzOzB3NkS5PS=>
TT  MmixRZBweHSxc3nzJGF{e2G7 NEnvSXIyKML3TR?= M3nncFQ5KGh? M4fiTWROW09? MVPpcoR2[2W|IHHwc5B1d3Orcx?= M3\C[lI{ODV4NEm5
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L-428 M3nQ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVntZ5plPzMkgJno MnLsSG1UVw>? MmjOTWM2OD15Lkm0O{DPxE1? NVfGT|FMOjJ6MkmwPVQ>
KM-H2 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHNU4M5PzMkgJno M17Wc2ROW09? M{j4Z2lEPTB;MT6zNFgh|ryP MnPwNlI5OjlyOUS=
L-540 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLqO|LjiImq MVHEUXNQ M1XxcmlEPTB;OD6yNVYh|ryP MVOyNlgzQTB7NB?=
HD-LM2 M1z2dmZ2dmO2aX;uJGF{e2G7 MmK4NE4yNzBwNT:xM|Uh|ryP NFjhNJU4OuLCiXi= MXnEUXNQ MoDlbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NILsWWYzOjh{OUC5OC=>
L-428 MkP4SpVv[3Srb36gRZN{[Xl? NGTwcpAxNjFxMD61M|EwPSEQvF2= NFTKOJg4OuLCiXi= NFHXOJdFVVOR M3q2b4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v Mn33NlI5OjlyOUS=
KM-H2 NES4c|BHfW6ldHnvckBCe3OjeR?= MkLoNE4yNzBwNT:xM|Uh|ryP MlPjO|LjiImq M1PObGROW09? M3\PTolvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MkfnNlI5OjlyOUS=
L-540 NIG3fZlHfW6ldHnvckBCe3OjeR?= MXGwMlEwOC53L{GvOUDPxE1? NIHKSoY4OuLCiXi= MnS2SG1UVw>? M4rNbolvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NFjPSIwzOjh{OUC5OC=>
HD-LM2 NHSyZ2dCeG:ydH;zbZMhSXO|YYm= M1fqTVEwPSEQvF2= NIXwZ5c4OuLCiXi= NFPhZmdFVVOR MlzRbY5lfWOnczDhdI9xfG:|aYO= M4jOS|IzQDJ7MEm0
L-428 MonlRZBweHSxc3nzJGF{e2G7 MYmxM|Uh|ryP M1H1flcz6oDLaB?= NVnlUlJiTE2VTx?= NFy5S|ZqdmS3Y3XzJIFxd3C2b4Ppdy=> MWGyNlgzQTB7NB?=
KM-H2 NU\4OnZJSXCxcITvd4l{KEG|c3H5 MoTvNU82KM7:TR?= M{n4OFcz6oDLaB?= Ml;CSG1UVw>? NH3Hd5hqdmS3Y3XzJIFxd3C2b4Ppdy=> MXmyNlgzQTB7NB?=
L-540 NI\HSXNCeG:ydH;zbZMhSXO|YYm= M3XuO|EwPSEQvF2= MWG3NwKBkWh? NHXjWZNFVVOR MUDpcoR2[2W|IHHwc5B1d3Orcx?= MYCyNlgzQTB7NB?=
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U87-MG NVHjdlJSTnWwY4Tpc44hSXO|YYm= M37jZ|EhyrWP M2HaO|AuOTZiaB?= NGHiV5VqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NYjHbZBoOjJyMke2PVE>
4C8 MV\GeY5kfGmxbjDBd5NigQ>? NEnQdZQyKML3TR?= M2S1NlAuOTZiaB?= MmmxbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NIHPPVkzOjB{N{[5NS=>
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8226 MlzIRZBweHSxc3nzJGF{e2G7 M4fnPVAvPS1{IN88US=> NInBSmU1QC95MjDo M1[wOIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MlnXNlEyPjR3MUe=

... 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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