AZD1480

製品コードS2162

AZD1480化学構造

分子量(MW):348.77

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

サイズ 価格(税別)  
JPY 21580.00
JPY 16600.00
JPY 28220.00
JPY 94620.00

カスタマーフィードバック(4)

  • bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.

    Nat Cell Biol, 2015, 17(1): 57-67. AZD1480 purchased from Selleck.

    Adipocytes were pre-infected with pAd-Foxc2 or si-Foxc2, and incubated with AZD1480 or not. Figures show protein levels of leptin, IL-6 and TNFα in adipocytes.

    Int J Obes, 2018, 42(2):252-259. AZD1480 purchased from Selleck.

  • A431 cells were treated with ALA-PDT alone or pretreated with 1μM AZD1480 for 1h or pretreated with 1ng/ml OSM for 10 minutes and the protein expression of Bcl-2 and Bax were analyzed by Western Blot.

    Photodiagnosis Photodyn Ther, 2016, 14:119-27. AZD1480 purchased from Selleck.

    HEL cells were treated for 3 hours with the indicated concentrations of AZD1480. AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar  concentrations in intact cells.

     

     

    M.Sc. Karoline Gaebler and Dr. Claude Haan of Université du Luxembour. AZD1480 purchased from Selleck.

製品安全説明書

JAK阻害剤の選択性比較

生物活性

製品説明 AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.
ターゲット
JAK2 [1]
(Cell-free assay)
0.26 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW620 MXjGeY5kfGmxbjDBd5NigQ>? Ml7pOUDPxE1? MVu0PEBp NWm5R3hXTE2VTx?= NXnDXXAy[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o NWj2eJA{OjV7NUS5O|Q>
LoVo  MYLGeY5kfGmxbjDBd5NigQ>? NEfjZ|k2KM7:TR?= NFy5[Hc1QCCq MV\EUXNQ Mn7yZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n Mn\oNlU6PTR7N{S=
HN5 NYfkZ|dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\RTFh[PzJiaB?= NULGfoJETUN3ME2zMlgyKMLzIEGuPVkh|ryP MlLXNlU5OTByMUC=
Cal33 M4\VcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HBTVczKGh? MlL3SWM2OD1|LkO3JOKyKDBwN{Wg{txO NEnIU4QzPThzMECxNC=>
UM-22B NX\IO49MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK3NkBp NWHWWVZ1TUN3ME2yMlY3KMLzIECuNlQh|ryP MWCyOVgyODBzMB?=
686LN NYnDXlRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nZblczKGh? MYrFR|UxRTJwMEWgxtEhOS5|MzFOwG0> M1fPWVI2QDFyMEGw
UM SCC-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVm3NkBp NYLpb|B7TUN3ME2xMlY4KMLzIECuOFIh|ryP M1[xcFI2QDFyMEGw
UM-22A NX21foN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7GUFFQPzJiaB?= MXfFR|UxRTFwM{KgxtEhOC5|OTFOwG0> MkD3NlU5OTByMUC=
OSC19 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPmS5A4OiCq MX7FR|UxRTFwMk[gxtEhOC5{MDFOwG0> NX7vc3k3OjV6MUCwNVA>
PCI-52 NUjoTXZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3juRVczKGh? MXfFR|UxRTFwMECgxtEhOC5yOTFOwG0> NYXjeIVpOjV6MUCwNVA>
PCI-15B MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LyT|czKGh? MkjFSWM2OD1yLkm5JOKyKDFwN{Sg{txO NGXrSXAzPThzMECxNC=>
UMSCC-1 MnXBSpVv[3Srb36gRZN{[Xl? MmrONE4xODB3LUGuOkDPxE1? NYThUFk5OjRiaB?= NXO3XXVo[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4fHelI2QDFyMEGw
Cal33 M3HrTGZ2dmO2aX;uJGF{e2G7 M1rESFAvODByNT2zMlgh|ryP M2fLcFI1KGh? NGrMcGxi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUDhPVl3OjV6MUCwNVA>
HH5 NFnFbXRHfW6ldHnvckBCe3OjeR?= MUWwMlAxODVvMz64JO69VQ>? M2niOVI1KGh? NGH0bYxi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIi0flUzPThzMECxNC=>
UM-22A Ml6wSpVv[3Srb36gRZN{[Xl? M4LV[lAvODByNT2xMlYh|ryP NEC3VmszPCCq NXntOXNO[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn7SNlU5OTByMUC=
A1847 NVq4cJFoTnWwY4Tpc44hSXO|YYm= MnPjNE4xPS1zMDFOwG0> NHX2dlAzPCCq MUXEUXNQyqB? MYXy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MUOyOVY1PjBzNR?=
OVCAR-5 NYHTWYpoTnWwY4Tpc44hSXO|YYm= M1PISFAvODVvMUCg{txO MnKxNlQhcA>? MWfEUXNQyqB? MX;y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MlrHNlU3PDZyMUW=
OVCAR-8 NUjLNYVNTnWwY4Tpc44hSXO|YYm= M2GxSVAvODVvMUCg{txO MUSyOEBp NXyzb3M4TE2VT9Mg M1G3W5Jm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MY[yOVY1PjBzNR?=
MOVCAR-5447 NWnWeodnTnWwY4Tpc44hSXO|YYm= Moi4NE4xPS1zMDFOwG0> MYqyOEBp MYTEUXNQyqB? MofkdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NUCzTmdXOjV4NE[wNVU>
MOVCAR-5009 MkTZSpVv[3Srb36gRZN{[Xl? NW\3fIlIOC5yNT2xNEDPxE1? MonNNlQhcA>? MofJSG1UV8Li NX35Tm9wemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NYL0RYNlOjV4NE[wNVU>
A1847 MoflR4VtdCCYaXHibYxqfHliQYPzZZk> MV6wMlA2NTFyIN88US=> M3;rc|czKGh? M3;EcGROW09? M4K5UJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN NYL1VI86OjV4NE[wNVU>
OVCAR-5 NYr4bHpVS2WubDDWbYFjcWyrdImgRZN{[Xl? MXWwMlA2NTFyIN88US=> NWHYdII6PzJiaB?= NIrZcmNFVVOR M3XGXZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN NFLyTmozPTZ2NkCxOS=>
OVCAR-8  NEDLXVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NH2yfYUxNjB3LUGwJO69VQ>? NWjV[mU4PzJiaB?= MVjEUXNQ MV\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M3ezbVI2PjR4MEG1
OVCAR-5  M120S2Fxd3C2b4Ppd{BCe3OjeR?= NUH3Uod5OC53L{GvOUDPxE1? NHvydow1QCCq MYXEUXNQ MoLsbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= M13QRVI2PjR4MEG1
OVCAR-8  Mof4RZBweHSxc3nzJGF{e2G7 NYj3[W1oOC53L{GvOUDPxE1? NXHJUGlbPDhiaB?= NWnYbVVnTE2VTx?= NGP0eXhqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u MYiyOVY1PjBzNR?=
AKRSL MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYK3NkBp NH\wNYZKSzVy78{eNVAh|ryP MYeyOVUxPDZ|NR?=
PALJDL NIjhO|NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NH\kR5g4OiCq M1zKS2lEPTB;Mj60JO69VQ>? NGjSNYwzPTVyNE[zOS=>
MO4 MUHGeY5kfGmxbjDBd5NigQ>? MWKwMlUwOS93IN88US=> NI\IfnI3KGh? NIXLRpdqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? MV:yOVE1QTV|NR?=
DU145  NILoW5lHfW6ldHnvckBCe3OjeR?= M2XiXlAuOjByIH7N MU[xJIjDqA>? Mon6d5VxeHKnc4Pld{BKVC14LXHjeIl3[XSnZDDTeIF1OyCjbnSgSXJMOS9{IIPp[45idGmwZx?= NXvmWoQ2OjR3N{e5OFI>
DU145  MXXGeY5kfGmxbjDBd5NigQ>? M1;mUlgxOCCwTR?= MknHO|IhcA>? NUTub4Y5e3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 MWmyOFU4Pzl2Mh?=
CWR22Rv1 MmfISpVv[3Srb36gRZN{[Xl? MlrUPFAxKG6P M{K0W|czKGh? M4X1dZN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= NUnCZmxmOjR3N{e5OFI>
N592 NGSxcmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vWdmlEPTB;MD64OEDPxE1? M{DhR|I1OTV6N{Cx
H82 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoH6TWM2OD1zLkO3JO69VQ>? M3vLbFI1OTV6N{Cx
GLC4 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PwOmlEPTB;MT63PUDPxE1? MUmyOFE2QDdyMR?=
H526 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNwMEig{txO NXXJS486OjRzNUi3NFE>
H1173 M{flcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfSTWM2OD1{LkO5JO69VQ>? NEizU|IzPDF3OEewNS=>
DMS114 NIDVcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoD0TWM2OD1yLkezJO69VQ>? NFr2VnIzPDF3OEewNS=>
NCI-N592 M4\te2Z2dmO2aX;uJGF{e2G7 MkKxNE4{NzFxMzFOwG0> M4i5XlI1KGh? M2jrZ4lv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NUXLVnFjOjRzNUi3NFE>
GLC4 MorjSpVv[3Srb36gRZN{[Xl? MoDBNE4{NzFxMzFOwG0> M{f6SVI1KGh? M{XJfIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M1XiVFI1OTV6N{Cx
NCI-H82 MUfGeY5kfGmxbjDBd5NigQ>? MmfINE4{NzFxMzFOwG0> MWeyOEBp MXTpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NXH1NZo2OjRzNUi3NFE>
NCI-N592 M2mzeWFxd3C2b4Ppd{BCe3OjeR?= NG[3bZYxNjNxMT:zJO69VQ>? M4fYVFQ5KGh? M1PER4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MUmyOFE2QDdyMR?=
GLC4 NHXBc4NCeG:ydH;zbZMhSXO|YYm= NUDUTWF1OC5|L{GvN{DPxE1? MXi0PEBp NV3JXWtVcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= MlLvNlQyPTh5MEG=
NCI-H82 MWLBdI9xfG:|aYOgRZN{[Xl? NIrzSYMxNjNxMT:zJO69VQ>? MWm0PEBp M{DYWIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M1PuVlI1OTV6N{Cx
CWR22Rv1  MoPBRZBweHSxc3nzJGF{e2G7 NXq1U3U{UUN3ME2wMlQ5OiEQvF2= NFq4TYozOzl2MkC5OS=>
CWR22Pc M3;yemFxd3C2b4Ppd{BCe3OjeR?= MoGzTWM2OD1yLkSzPEDPxE1? NX3Pd2tlOjN7NEKwPVU>
PC-3 M3LE[GFxd3C2b4Ppd{BCe3OjeR?= NFTGTlNKSzVyPUGuO|U2KM7:TR?= NE\EUJkzOzl2MkC5OS=>
DU145 NH;IflhCeG:ydH;zbZMhSXO|YYm= MX3JR|UxRTNwNUG3JO69VQ>? M4nNPVI{QTR{MEm1
RC165N NV3PVGt5SXCxcITvd4l{KEG|c3H5 MVjJR|UxRTJwMEizJO69VQ>? MnrvNlM6PDJyOUW=
ARPE19 NUXDXo1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTDSG1UVw>? MVnJR|UxRTJ2LkO4JO69VQ>? NVT5PZpGOjN3M{G5NlE>
HEK293 NXfl[Vh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXlbnpHTE2VTx?= M4r4OWlEPTB;OD62O{DPxE1? MUWyN|U{OTl{MR?=
KCNR MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HzcWROW09? MUjJR|UxRTBwNE[g{txO NGDG[|kzOzV|MUmyNS=>
SY5Y MkLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DsSGROW09? NYTL[GdRUUN3ME2wMlM3KM7:TR?= NUDiSVlyOjN3M{G5NlE>
BE2 NIK3eI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PGXWROW09? M1\TXmlEPTB;MD63NUDPxE1? NUTEN2lJOjN3M{G5NlE>
AS M3XsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjEUXNQ MmjJTWM2OD1zLkWzJO69VQ>? MlX5NlM2OzF7MkG=
NGP M1LkV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTwc2FDTE2VTx?= MlLXTWM2OD1yLkW2JO69VQ>? NVXkdZJROjN3M{G5NlE>
IMR32 Ml[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTEUXNQ MUHJR|UxRTBwNk[g{txO MUmyN|U{OTl{MR?=
LAN5 NHj0cZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33nSmROW09? M3vqOWlEPTB;MT6wOEDPxE1? NUnUd5VPOjN3M{G5NlE>
RH18 M1jBPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUW4dFBiTE2VTx?= MYDJR|UxRTFwNEKg{txO NIq3XpUzOzV|MUmyNS=>
RH30 MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrqSG1UVw>? MUjJR|UxRTFwMkWg{txO MXyyN|U{OTl{MR?=
RH17 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[ySpc5TE2VTx?= M3\GTGlEPTB;Mj61NUDPxE1? NFn2SZAzOzV|MUmyNS=>
RH28 Mn3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjFSG1UVw>? MVLJR|UxRTRwMkig{txO NXS4boV5OjN3M{G5NlE>
RH36 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPkXZJFVVOR M1rrSWlEPTB;NT6zO{DPxE1? M4LLfFI{PTNzOUKx
RH41 NVixXGlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3xSWtJTE2VTx?= NXLIPYFOUUN3ME2wMlQ5KM7:TR?= MmjtNlM2OzF7MkG=
RD NFrYcIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\qc2ROW09? NWjFbJBSUUN3ME20MlMzKM7:TR?= NX\ZenNEOjN3M{G5NlE>
TC32 NELNWJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjPTHViTE2VTx?= NGTEOGdKSzVyPUOuPFUh|ryP NGfZZoszOzV|MUmyNS=>
TC71 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLvdFdFVVOR MlfGTWM2OD12LkOzJO69VQ>? NX;wWldDOjN3M{G5NlE>
KCNR MmjxRZBweHSxc3nzJGF{e2G7 NWjVUnUyOC53L{GuNE8zNjVizszN MY[yOEBp MXfEUXNQ NHLh[oNqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 M1v2XFI{PTNzOUKx
SY5Y MYTBdI9xfG:|aYOgRZN{[Xl? M2\iPVAvPS9zLkCvNk42KM7:TR?= MoXUNlQhcA>? NVu3TppwTE2VTx?= M3PSVYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NXjrZ5QyOjN3M{G5NlE>
Rh18 MULBdI9xfG:|aYOgRZN{[Xl? MX[wMlUwOS5yL{KuOUDPxE1? MWmyOEBp M13QR2ROW09? MV\pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MV6yN|U{OTl{MR?=
TC32 NFjoSW1CeG:ydH;zbZMhSXO|YYm= NH;2WIMxNjVxMT6wM|IvPSEQvF2= MVGyOEBp MnLrSG1UVw>? NHPSbmNqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NHfEcFczOzV|MUmyNS=>
KCNR M3vkdWZ2dmO2aX;uJGF{e2G7 NUfM[mRLOC53L{GuNE8zNjVxNTFOwG0> MoDwNlQhcA>? NGO3bmFFVVOR NGHuSXNqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> M2jheVI{PTNzOUKx
SY5Y MUHGeY5kfGmxbjDBd5NigQ>? M1XXVVAvPS9zLkCvNk42NzVizszN MnfBNlQhcA>? M2f6VGROW09? NVTlSWdvcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MWmyN|U{OTl{MR?=
Rh18 MmfpSpVv[3Srb36gRZN{[Xl? MWiwMlUwOS5yL{KuOU82KM7:TR?= NXHmOnJEOjRiaB?= MUjEUXNQ M4\VVIlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u MYKyN|U{OTl{MR?=
TC32 MWXGeY5kfGmxbjDBd5NigQ>? M4\ZflAvPS9zLkCvNk42NzVizszN Mny4NlQhcA>? MnrMSG1UVw>? NG[zbYpqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NHTGSXgzOzV|MUmyNS=>
TPC-1 NYrFdlBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jKZ|EhyrWP NYXae49YOC12IHS= NV7lfGdlTE2VTx?= MVHpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 NUTFW5JCOjNyNU[0PVk>
MZ-CRC1  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUexJOK2VQ>? MlXwNE02KGR? M1XweWROW09? NUXMS|czcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= M4LVb|I{ODV4NEm5
TT  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITB[FAyKML3TR?= MnWwNE01KGR? M4TWWmROW09? NWe3ZpBucW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= M3PCOlI{ODV4NEm5
TPC-1 NEXqSGdHfW6ldHnvckBCe3OjeR?= NHzTWlUyKML3TR?= NX7zXFdNPzJiaB?= M3vtVWROW09? MVHpcoR2[2W|IFexJIJtd2OtYXfl M4PXOVI{ODV4NEm5
MZ-CRC1  MnPISpVv[3Srb36gRZN{[Xl? MXyxJOK2VQ>? NH;k[II4OiCq MknWSG1UVw>? MVnpcoR2[2W|IFexJIJtd2OtYXfl M1zkZ|I{ODV4NEm5
TT  MYPGeY5kfGmxbjDBd5NigQ>? NUDSNXdWOSEEtV2= Ml7oO|IhcA>? MWfEUXNQ NFrSVYpqdmS3Y3XzJGcyKGKub3PrZYdm NFPWeYszOzB3NkS5PS=>
MZ-CRC1  NI\2fGxCeG:ydH;zbZMhSXO|YYm= NGW3d3cyKML3TR?= MofYOFghcA>? MWTEUXNQ NFLEVIZqdmS3Y3XzJIFxd3C2b4Ppdy=> MUGyN|A2PjR7OR?=
TT  NHOy[2xCeG:ydH;zbZMhSXO|YYm= M2[zUlEhyrWP NFTLTlA1QCCq MoDSSG1UVw>? NXfjdXg1cW6mdXPld{BieG:ydH;zbZM> MV6yN|A2PjR7OR?=
HD-LM2 MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\rdIZyPzMkgJno MX7EUXNQ M3naPWlEPTB;Nz64OFQh|ryP M3TjUlIzQDJ7MEm0
L-428 NUDYN3YxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHRO|LjiImq Mo\rSG1UVw>? MojSTWM2OD15Lkm0O{DPxE1? MW[yNlgzQTB7NB?=
KM-H2 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\CZWo4OuLCiXi= MXrEUXNQ MV;JR|UxRTFwM{C4JO69VQ>? NYW2O|lXOjJ6MkmwPVQ>
L-540 NYHmbGF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7OSpE4OuLCiXi= NIX4bphFVVOR NYWxRm5bUUN3ME24MlIyPiEQvF2= NFfZUFQzOjh{OUC5OC=>
HD-LM2 NH7yU2ZHfW6ldHnvckBCe3OjeR?= NIK2eoUxNjFxMD61M|EwPSEQvF2= M2rGSVcz6oDLaB?= NX7jUndQTE2VTx?= NUnieJhzcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? M4\hSVIzQDJ7MEm0
L-428 MWDGeY5kfGmxbjDBd5NigQ>? MYOwMlEwOC53L{GvOUDPxE1? M1LDPFcz6oDLaB?= NWDnNmd2TE2VTx?= M1HvV4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v M1zPdlIzQDJ7MEm0
KM-H2 M{nodWZ2dmO2aX;uJGF{e2G7 MXmwMlEwOC53L{GvOUDPxE1? NYPxNI56PzMkgJno Mn3zSG1UVw>? MV\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MmXHNlI5OjlyOUS=
L-540 MVvGeY5kfGmxbjDBd5NigQ>? M2i2fFAvOS9yLkWvNU82KM7:TR?= MUW3NwKBkWh? NIK3e2dFVVOR Ml6xbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NWTEV45JOjJ6MkmwPVQ>
HD-LM2 MY\BdI9xfG:|aYOgRZN{[Xl? Ml60NU82KM7:TR?= MXi3NwKBkWh? MnHFSG1UVw>? MX;pcoR2[2W|IHHwc5B1d3Orcx?= NVnGUXpWOjJ6MkmwPVQ>
L-428 MWXBdI9xfG:|aYOgRZN{[Xl? M{HSd|EwPSEQvF2= NH\hVJQ4OuLCiXi= M{HyN2ROW09? NFzPdXFqdmS3Y3XzJIFxd3C2b4Ppdy=> M{XSTlIzQDJ7MEm0
KM-H2 NWDLW4lySXCxcITvd4l{KEG|c3H5 MlG3NU82KM7:TR?= M{fhZlcz6oDLaB?= MlzmSG1UVw>? M4TSPYlv\HWlZYOgZZBweHSxc3nz MVOyNlgzQTB7NB?=
L-540 MVTBdI9xfG:|aYOgRZN{[Xl? NETOXoUyNzVizszN NWS2enJNPzMkgJno MUfEUXNQ NWn0SnFncW6mdXPld{BieG:ydH;zbZM> MUCyNlgzQTB7NB?=
U251-MG MXPGeY5kfGmxbjDBd5NigQ>? NFj4TVEyKML3TR?= MUCwMVE3KGh? MXvpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> NEfBfGczOjB{N{[5NS=>
U87-MG NYP6fHdvTnWwY4Tpc44hSXO|YYm= MmHTNUDDvU1? NIfOXnUxNTF4IHi= M3TtZolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NXf5RnpGOjJyMke2PVE>
4C8 M{HteGZ2dmO2aX;uJGF{e2G7 NGDD[YUyKML3TR?= NYjuO3pTOC1zNjDo MmDTbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MY[yNlAzPzZ7MR?=
U251-MG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGxM|ExKML3TR?= M{C5ZVI1NzR6L{eyJIg> NIrPcIRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MUOyNlAzPzZ7MR?=
U87-MG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\ZflEwOTBiwsXN M1PmXFI1NzR6L{eyJIg> M{nGZolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO M4C2T|IzODJ5Nkmx
4C8 NU\Ze491T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j2cVEwOTBiwsXN MnnMNlQwPDhxN{KgbC=> MlHnbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> NYDaeHJUOjJyMke2PVE>
U266 M{DjcWFxd3C2b4Ppd{BCe3OjeR?= MYqwMlUuOiEQvF2= MoPIOFgwPzJiaB?= NFnF[WpqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NH7od2UzOTF4NEWxOy=>
Kms.11 MlHzRZBweHSxc3nzJGF{e2G7 M3O2OVAvPS1{IN88US=> NIj3Vmo1QC95MjDo M4ruSIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NUe1PW1COjFzNkS1NVc>
8226 NUC5S4dsSXCxcITvd4l{KEG|c3H5 MUewMlUuOiEQvF2= MX20PE84OiCq MljobY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MVeyNVE3PDVzNx?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[5]
+ 展開

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.
細胞試験: [4]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[4]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 69 mg/mL (197.83 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
混合させたのち直ちに使用することを推奨します。
5 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 348.77
化学式

C14H14ClFN8

CAS No. 935666-88-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01219543 Terminated Solid Tumour|Advanced Solid Malignancies|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma|EGFR and/or ROS Mutant NSCLC|Lung Metastasis Carcinoma|Gastric Cancer AstraZeneca November 2010 Phase 1
NCT01112397 Terminated Solid Malignancies AstraZeneca April 2010 Phase 1
NCT00910728 Completed Primary Myelofibrosis (PMF)|Post-Polycythaemia Vera|Essential Thrombocythaemia Myelofibrosis AstraZeneca|University of Texas|New York City Hoffman Center|Gustave Roussy Cancer Campus Grand Paris May 2009 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

JAKシグナル伝達経路

JAK Inhibitors with Unique Features

相関JAK製品

Tags: AZD1480を買う | AZD1480 ic50 | AZD1480供給者 | AZD1480を購入する | AZD1480費用 | AZD1480生産者 | オーダーAZD1480 | AZD1480化学構造 | AZD1480分子量 | AZD1480代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID