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
USD 163 あり
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USD 718 あり
電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

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 MUTGeY5kfGmxbjDBd5NigQ>? M4TwflUh|ryP NX61UGJ6PDhiaB?= M37mVGROW09? MW\icI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= MW[yOVk2PDl5NB?=
LoVo  MlnKSpVv[3Srb36gRZN{[Xl? NYLqXYZTPSEQvF2= NILIOYc1QCCq NYL4XFZtTE2VTx?= MX7icI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= MXuyOVk2PDl5NB?=
HN5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j2SFczKGh? MnjXSWM2OD1|LkixJOKyKDFwOUmg{txO NYjXfI1yOjV6MUCwNVA>
Cal33 NWL3TmtrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXe3NkBp NXLTZY1UTUN3ME2zMlM4KMLzIECuO|Uh|ryP MlHSNlU5OTByMUC=
UM-22B NIDuWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTHXVJYPzJiaB?= Mmj0SWM2OD1{Lk[2JOKyKDBwMkSg{txO MmjENlU5OTByMUC=
686LN NYrFOGlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLkVVQ4OiCq NFPsbZJGSzVyPUKuNFUhyrFiMT6zN{DPxE1? MVSyOVgyODBzMB?=
UM SCC-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u3OVczKGh? NVLO[HNnTUN3ME2xMlY4KMLzIECuOFIh|ryP MXKyOVgyODBzMB?=
UM-22A NF7NPXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDkO|IhcA>? NYjDXWZKTUN3ME2xMlMzKMLzIECuN|kh|ryP M{DkcVI2QDFyMEGw
OSC19 MlfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1WwW|czKGh? M1vCeWVEPTB;MT6yOkDDuSByLkKwJO69VQ>? NH\IVlYzPThzMECxNC=>
PCI-52 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\XcWc4OiCq Mk[0SWM2OD1zLkCwJOKyKDBwMEmg{txO M370OlI2QDFyMEGw
PCI-15B NV3KbI1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvkbYtjPzJiaB?= M4DscmVEPTB;MD65PUDDuSBzLke0JO69VQ>? NUnKd4ZqOjV6MUCwNVA>
UMSCC-1 MVnGeY5kfGmxbjDBd5NigQ>? MUSwMlAxODVvMT62JO69VQ>? NXjTeIh[OjRiaB?= MWDhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX:yOVgyODBzMB?=
Cal33 M{naeGZ2dmO2aX;uJGF{e2G7 NIDYOHQxNjByMEWtN{45KM7:TR?= NYHDU|VNOjRiaB?= NEPvfopi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUDBb3I6OjV6MUCwNVA>
HH5 M3e5SWZ2dmO2aX;uJGF{e2G7 NUjWeZRVOC5yMEC1MVMvQCEQvF2= MVOyOEBp MVnhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYGyOVgyODBzMB?=
UM-22A MlzGSpVv[3Srb36gRZN{[Xl? NXzyT|B5OC5yMEC1MVEvPiEQvF2= MmjvNlQhcA>? NV;INFE{[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MU[yOVgyODBzMB?=
A1847 M1y4eWZ2dmO2aX;uJGF{e2G7 Ml76NE4xPS1zMDFOwG0> M2rVRVI1KGh? MX\EUXNQyqB? NU\zNJI3emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MlLpNlU3PDZyMUW=
OVCAR-5 MVTGeY5kfGmxbjDBd5NigQ>? M3LQdlAvODVvMUCg{txO M3\uTVI1KGh? M2XUXGROW00EoB?= NFfSRnFz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NXfUWVRYOjV4NE[wNVU>
OVCAR-8 MYDGeY5kfGmxbjDBd5NigQ>? NUjPWXVmOC5yNT2xNEDPxE1? Mkj6NlQhcA>? MmPySG1UV8Li M3Tub5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz M1vmO|I2PjR4MEG1
MOVCAR-5447 M2DlfGZ2dmO2aX;uJGF{e2G7 NV3ZdFlWOC5yNT2xNEDPxE1? Mlz2NlQhcA>? MnW2SG1UV8Li MmLRdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NFnNOHIzPTZ2NkCxOS=>
MOVCAR-5009 MYrGeY5kfGmxbjDBd5NigQ>? NIja[ZUxNjB3LUGwJO69VQ>? MmjLNlQhcA>? NWXBdJNjTE2VT9Mg NFfpd5dz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NHPEXFIzPTZ2NkCxOS=>
A1847 M4rERWNmdGxiVnnhZoltcXS7IFHzd4F6 MnvKNE4xPS1zMDFOwG0> NIfqNYg4OiCq NW\2N2FqTE2VTx?= NFu0[Zlz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MlLSNlU3PDZyMUW=
OVCAR-5 M2jHRWNmdGxiVnnhZoltcXS7IFHzd4F6 MknJNE4xPS1zMDFOwG0> NG\tTWE4OiCq MV\EUXNQ MUDy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MY[yOVY1PjBzNR?=
OVCAR-8  MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mk\INE4xPS1zMDFOwG0> NG[0U5I4OiCq M3y0e2ROW09? NF3EVFZz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MW[yOVY1PjBzNR?=
OVCAR-5  Mn3hRZBweHSxc3nzJGF{e2G7 MX[wMlUwOS93IN88US=> NEPFdpg1QCCq NUn2eWN7TE2VTx?= Mk[4bY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= MYSyOVY1PjBzNR?=
OVCAR-8  NVf4bnBDSXCxcITvd4l{KEG|c3H5 M3f1VlAvPS9zL{Wg{txO NXfwN5VIPDhiaB?= NWn1RnRHTE2VTx?= NFHIOoRqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u NEK0fY0zPTZ2NkCxOS=>
AKRSL MnL5R4VtdCCYaXHibYxqfHliQYPzZZk> NICybnE4OiCq MYrJR|Ux97zgMUCg{txO NHrEOpkzPTVyNE[zOS=>
PALJDL MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXjqNnVUPzJiaB?= MnfWTWM2OD1{LkSg{txO MWSyOVUxPDZ|NR?=
MO4 MUTGeY5kfGmxbjDBd5NigQ>? NXznVnNoOC53L{GvOUDPxE1? MXi2JIg> MXzpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> NETOSGozPTF2OUWzOS=>
DU145  NGnqd5RHfW6ldHnvckBCe3OjeR?= NX\s[lJ{OC1{MECgcm0> MlLnNUBpyqB? NFLQenV{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NIPT[2MzPDV5N{m0Ni=>
DU145  NUn4b2htTnWwY4Tpc44hSXO|YYm= MVK4NFAhdk1? NVTuZZhjPzJiaB?= MXjzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? MWCyOFU4Pzl2Mh?=
CWR22Rv1 NFfpNotHfW6ldHnvckBCe3OjeR?= MYm4NFAhdk1? M2jrWFczKGh? NX7Ye4k5e3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 M{PZVFI1PTd5OUSy
N592 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TSW2lEPTB;MD64OEDPxE1? MYWyOFE2QDdyMR?=
H82 NXzlUGhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH1TnRKSzVyPUGuN|ch|ryP MWGyOFE2QDdyMR?=
GLC4 NGLHfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ryUmlEPTB;MT63PUDPxE1? NF7uc24zPDF3OEewNS=>
H526 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnQbG05UUN3ME2zMlA5KM7:TR?= NH3yXoMzPDF3OEewNS=>
H1173 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\POlNKSzVyPUKuN|kh|ryP NX3CR452OjRzNUi3NFE>
DMS114 M4fkVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnKwTWM2OD1yLkezJO69VQ>? M33YXVI1OTV6N{Cx
NCI-N592 NG\JW5BHfW6ldHnvckBCe3OjeR?= MXywMlMwOS9|IN88US=> Mli3NlQhcA>? NIXt[5pqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NXvOWnhMOjRzNUi3NFE>
GLC4 M4L4fWZ2dmO2aX;uJGF{e2G7 MXuwMlMwOS9|IN88US=> M{Lw[|I1KGh? MXHpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NYjJdVlDOjRzNUi3NFE>
NCI-H82 MWTGeY5kfGmxbjDBd5NigQ>? NX;ZRYFYOC5|L{GvN{DPxE1? NEL3SnozPCCq M{\kUIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NGLReVAzPDF3OEewNS=>
NCI-N592 M33ac2Fxd3C2b4Ppd{BCe3OjeR?= MkHoNE4{NzFxMzFOwG0> NUC3dZVyPDhiaB?= NG\ZOIRqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NFjmUW4zPDF3OEewNS=>
GLC4 M{XYXWFxd3C2b4Ppd{BCe3OjeR?= MmDMNE4{NzFxMzFOwG0> M1LF[lQ5KGh? MVnpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ Mn;qNlQyPTh5MEG=
NCI-H82 MkjjRZBweHSxc3nzJGF{e2G7 NH75R2ExNjNxMT:zJO69VQ>? NWf6[IQ3PDhiaB?= M4j6Zolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M4XNUlI1OTV6N{Cx
CWR22Rv1  NWOyOHZrSXCxcITvd4l{KEG|c3H5 NHvoc5BKSzVyPUCuOFgzKM7:TR?= M1TMZ|I{QTR{MEm1
CWR22Pc NXXYVIVKSXCxcITvd4l{KEG|c3H5 NVjMemVGUUN3ME2wMlQ{QCEQvF2= Mkj3NlM6PDJyOUW=
PC-3 MnW4RZBweHSxc3nzJGF{e2G7 MorSTWM2OD1zLke1OUDPxE1? M1n3PFI{QTR{MEm1
DU145 MlvWRZBweHSxc3nzJGF{e2G7 NUXTPJNTUUN3ME2zMlUyPyEQvF2= MWWyN|k1OjB7NR?=
RC165N MojORZBweHSxc3nzJGF{e2G7 MVrJR|UxRTJwMEizJO69VQ>? NIXDWoUzOzl2MkC5OS=>
ARPE19 M4HRSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\6OWROW09? NFjpT4hKSzVyPUK0MlM5KM7:TR?= MmXUNlM2OzF7MkG=
HEK293 NWrIUJg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e5cmROW09? MU\JR|UxRThwNkeg{txO NWTLWoI5OjN3M{G5NlE>
KCNR MmDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;iSG1UVw>? NEO4WVVKSzVyPUCuOFYh|ryP M4H3VlI{PTNzOUKx
SY5Y MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrLRpNFVVOR NGDSdHdKSzVyPUCuN|Yh|ryP NXu1OHlWOjN3M{G5NlE>
BE2 Ml3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL4ZodFVVOR MWfJR|UxRTBwN{Gg{txO M13Se|I{PTNzOUKx
AS M1[zRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS5dmhFVVOR NIDFOYJKSzVyPUGuOVMh|ryP MXWyN|U{OTl{MR?=
NGP MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF71Z5dFVVOR M4PZemlEPTB;MD61OkDPxE1? NF;xT20zOzV|MUmyNS=>
IMR32 M3;me2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnKzSG1UVw>? M4jzUWlEPTB;MD62OkDPxE1? MYqyN|U{OTl{MR?=
LAN5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrEUXNQ M1j4fmlEPTB;MT6wOEDPxE1? MYiyN|U{OTl{MR?=
RH18 NVToUpJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP4SG1UVw>? NFvyU4hKSzVyPUGuOFIh|ryP MWiyN|U{OTl{MR?=
RH30 MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr6TWNFVVOR Mn;JTWM2OD1zLkK1JO69VQ>? MV:yN|U{OTl{MR?=
RH17 NIHIco1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvXTJZFVVOR M1zkTmlEPTB;Mj61NUDPxE1? NXzQRlFYOjN3M{G5NlE>
RH28 NGW0VZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjFR|NRTE2VTx?= NVfIUJZCUUN3ME20MlI5KM7:TR?= NFTUflgzOzV|MUmyNS=>
RH36 NVfU[2hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHUd5hFVVOR NGrqPIpKSzVyPUWuN|ch|ryP NEnJcmgzOzV|MUmyNS=>
RH41 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:4UmptTE2VTx?= NX;yOG5UUUN3ME2wMlQ5KM7:TR?= NEfxXmQzOzV|MUmyNS=>
RD M4rNbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LpfmROW09? MWLJR|UxRTRwM{Kg{txO NIPQbJIzOzV|MUmyNS=>
TC32 MlvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDtVlVzTE2VTx?= NFXKTo1KSzVyPUOuPFUh|ryP MlzxNlM2OzF7MkG=
TC71 NHTiU5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonGSG1UVw>? NFnSc2tKSzVyPUSuN|Mh|ryP MmnTNlM2OzF7MkG=
KCNR NYHYNmFvSXCxcITvd4l{KEG|c3H5 NYf2R2RTOC53L{GuNE8zNjVizszN MXuyOEBp MXPEUXNQ MXrpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NHTyR3gzOzV|MUmyNS=>
SY5Y MYPBdI9xfG:|aYOgRZN{[Xl? MlLlNE42NzFwMD:yMlUh|ryP NG\QNFIzPCCq MkfuSG1UVw>? MVTpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MYCyN|U{OTl{MR?=
Rh18 NXvYRYNLSXCxcITvd4l{KEG|c3H5 M1exUFAvPS9zLkCvNk42KM7:TR?= MUiyOEBp MYDEUXNQ M3jxcIlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NGjsSZUzOzV|MUmyNS=>
TC32 NI\BPJRCeG:ydH;zbZMhSXO|YYm= M{\Wc|AvPS9zLkCvNk42KM7:TR?= Ml22NlQhcA>? M{Tp[GROW09? M4jkS4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NFK1T4QzOzV|MUmyNS=>
KCNR M4K2Z2Z2dmO2aX;uJGF{e2G7 NVTlN2NpOC53L{GuNE8zNjVxNTFOwG0> MV:yOEBp MWnEUXNQ MUPpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MV:yN|U{OTl{MR?=
SY5Y NV\ZWll[TnWwY4Tpc44hSXO|YYm= NUDadWdmOC53L{GuNE8zNjVxNTFOwG0> MYiyOEBp NFzpOGJFVVOR MmPnbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MYqyN|U{OTl{MR?=
Rh18 MV;GeY5kfGmxbjDBd5NigQ>? MmHSNE42NzFwMD:yMlUwPSEQvF2= M4\1S|I1KGh? Mly4SG1UVw>? M3roPYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NETjdZQzOzV|MUmyNS=>
TC32 MWrGeY5kfGmxbjDBd5NigQ>? MlyxNE42NzFwMD:yMlUwPSEQvF2= NIPDUZIzPCCq M3T6eGROW09? NH\ZdW9qdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MVeyN|U{OTl{MR?=
TPC-1 M37TU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmxJOK2VQ>? NE[0cmQxNTRiZB?= MV\EUXNQ MkO1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? NEfiUIozOzB3NkS5PS=>
MZ-CRC1  MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIW5NmIyKML3TR?= NFzL[G8xNTViZB?= MVXEUXNQ M1PM[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? NGnpXZMzOzB3NkS5PS=>
TT  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmX6NUDDvU1? MoTJNE01KGR? NXX2To9vTE2VTx?= NWfTcY8xcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NWX4fXB1OjNyNU[0PVk>
TPC-1 NHLNTpBHfW6ldHnvckBCe3OjeR?= NF\yb4syKML3TR?= MVm3NkBp NWq2O|hqTE2VTx?= MXvpcoR2[2W|IFexJIJtd2OtYXfl MoT0NlMxPTZ2OUm=
MZ-CRC1  NFz3N29HfW6ldHnvckBCe3OjeR?= M1KzcVEhyrWP Ml;sO|IhcA>? MmOwSG1UVw>? NVKwSmpKcW6mdXPld{BIOSCkbH;jb4Fo\Q>? M2TtTVI{ODV4NEm5
TT  Mn3QSpVv[3Srb36gRZN{[Xl? NHLWfYMyKML3TR?= NYL1W2liPzJiaB?= NUDXXmd6TE2VTx?= NV2wV2h1cW6mdXPld{BIOSCkbH;jb4Fo\Q>? Ml7wNlMxPTZ2OUm=
MZ-CRC1  NEPicFRCeG:ydH;zbZMhSXO|YYm= NFSycXAyKML3TR?= MX:0PEBp NULqcohYTE2VTx?= M4P5PYlv\HWlZYOgZZBweHSxc3nz NVTlOYtrOjNyNU[0PVk>
TT  MYDBdI9xfG:|aYOgRZN{[Xl? NWG3eIpsOSEEtV2= M1rHWVQ5KGh? M3PHTGROW09? NWXze283cW6mdXPld{BieG:ydH;zbZM> MX:yN|A2PjR7OR?=
HD-LM2 NH;WXolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYK3NwKBkWh? M{TFZmROW09? NEPnPZRKSzVyPUeuPFQ1KM7:TR?= MYOyNlgzQTB7NB?=
L-428 M3vJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlO0O|LjiImq M3GwVmROW09? NU\Lc3FQUUN3ME23Mlk1PyEQvF2= Mnn4NlI5OjlyOUS=
KM-H2 M3vx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXre3o4PzMkgJno NF;NRo9FVVOR MYTJR|UxRTFwM{C4JO69VQ>? MUGyNlgzQTB7NB?=
L-540 NWfxd2JxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWW3NwKBkWh? M2nCOmROW09? M3nBXWlEPTB;OD6yNVYh|ryP NUGxfnJVOjJ6MkmwPVQ>
HD-LM2 NIjzfmZHfW6ldHnvckBCe3OjeR?= NY\OXFVHOC5zL{CuOU8yNzVizszN NGTrZ2g4OuLCiXi= NISzUHZFVVOR NVPNSm0{cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NW[0TGtCOjJ6MkmwPVQ>
L-428 MmrRSpVv[3Srb36gRZN{[Xl? NV;nZ2NKOC5zL{CuOU8yNzVizszN NIPJOWQ4OuLCiXi= MlXzSG1UVw>? NUX0TIU1cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MoHWNlI5OjlyOUS=
KM-H2 NV:zNYN6TnWwY4Tpc44hSXO|YYm= NXXEWGE2OC5zL{CuOU8yNzVizszN MlzpO|LjiImq NHPreYtFVVOR Mlr2bY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MY[yNlgzQTB7NB?=
L-540 MnnkSpVv[3Srb36gRZN{[Xl? NESybWkxNjFxMD61M|EwPSEQvF2= NVvS[Jk6PzMkgJno NVq5XnJGTE2VTx?= M4HoeIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NFHGTG8zOjh{OUC5OC=>
HD-LM2 NIfid2pCeG:ydH;zbZMhSXO|YYm= NHq2NoMyNzVizszN M3LQOVcz6oDLaB?= MXjEUXNQ NVPVUZVXcW6mdXPld{BieG:ydH;zbZM> MojRNlI5OjlyOUS=
L-428 NFmzRlhCeG:ydH;zbZMhSXO|YYm= NV;BPJRrOS93IN88US=> MWe3NwKBkWh? NVrGTG1jTE2VTx?= Mo\EbY5lfWOnczDhdI9xfG:|aYO= NUDDS|V{OjJ6MkmwPVQ>
KM-H2 M4qzfWFxd3C2b4Ppd{BCe3OjeR?= M4\uSVEwPSEQvF2= M16wdFcz6oDLaB?= NVLVdoFjTE2VTx?= MX7pcoR2[2W|IHHwc5B1d3Orcx?= M3vUXlIzQDJ7MEm0
L-540 MlXJRZBweHSxc3nzJGF{e2G7 NVTSb2dDOS93IN88US=> NX31VYtkPzMkgJno NVXITWplTE2VTx?= Mn\MbY5lfWOnczDhdI9xfG:|aYO= MXWyNlgzQTB7NB?=
U251-MG NGfOd4JHfW6ldHnvckBCe3OjeR?= MkPlNUDDvU1? M1vkUVAuOTZiaB?= NHrQOHRqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NU\vNGZ7OjJyMke2PVE>
U87-MG MUnGeY5kfGmxbjDBd5NigQ>? NWjHdmd6OSEEtV2= MoXxNE0yPiCq M2HkVYlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NFzDSlUzOjB{N{[5NS=>
4C8 NGG4V4dHfW6ldHnvckBCe3OjeR?= NGjoRXMyKML3TR?= MVuwMVE3KGh? NFfKfXlqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NWLsfZdwOjJyMke2PVE>
U251-MG M2r4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDDSm9EOS9zMDFCuW0> MoW2NlQwPDhxN{KgbC=> MWTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MkPUNlIxOjd4OUG=
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... 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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