AZD1480

製品コードS2162

AZD1480化学構造

分子量(MW):348.77

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。

サイズ 価格 在庫  
JPY 18718.43 あり
JPY 14398.80 あり
JPY 24477.96 あり
JPY 82073.16 あり

カスタマーフィードバック(3)

  • 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.

    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 [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 MVfGeY5kfGmxbjDBd5NigQ>? MXG1JO69VQ>? MUG0PEBp NHi3fo1FVVOR NGLBcldjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MV[yOVk2PDl5NB?=
LoVo  MUPGeY5kfGmxbjDBd5NigQ>? M1XtXFUh|ryP Mmn3OFghcA>? NXTrWpRsTE2VTx?= M2nhb4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> NWnkS4dZOjV7NUS5O|Q>
HN5 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTzWYRqPzJiaB?= MmLtSWM2OD1|LkixJOKyKDFwOUmg{txO M2Pq[|I2QDFyMEGw
Cal33 NXzPO3k1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\pO|IhcA>? M3yyeWVEPTB;Mz6zO{DDuSByLke1JO69VQ>? Mke1NlU5OTByMUC=
UM-22B NEjLPIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\LO|IhcA>? MXzFR|UxRTJwNk[gxtEhOC5{NDFOwG0> MnPnNlU5OTByMUC=
686LN M1HhdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVm3NkBp NGPQXXlGSzVyPUKuNFUhyrFiMT6zN{DPxE1? NV;MblRqOjV6MUCwNVA>
UM SCC-1 NXTJN25xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jjc|czKGh? NITD[4VGSzVyPUGuOlchyrFiMD60NkDPxE1? MYiyOVgyODBzMB?=
UM-22A M{XofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC3V411PzJiaB?= NIqxTnpGSzVyPUGuN|IhyrFiMD6zPUDPxE1? MnHpNlU5OTByMUC=
OSC19 NUfqOJRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm1VXV1PzJiaB?= MYHFR|UxRTFwMk[gxtEhOC5{MDFOwG0> MXeyOVgyODBzMB?=
PCI-52 NUf3b2l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlSzO|IhcA>? M2X4[mVEPTB;MT6wNEDDuSByLkC5JO69VQ>? NV;sbVAxOjV6MUCwNVA>
PCI-15B NX3h[4k1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O2XlczKGh? M3fIOmVEPTB;MD65PUDDuSBzLke0JO69VQ>? MWGyOVgyODBzMB?=
UMSCC-1 Ml7pSpVv[3Srb36gRZN{[Xl? NHu1XFUxNjByMEWtNU43KM7:TR?= NWfHSWhLOjRiaB?= M2PNUIFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmL1NlU5OTByMUC=
Cal33 NVnoNJQ6TnWwY4Tpc44hSXO|YYm= MkL1NE4xODB3LUOuPEDPxE1? NVe5S2NDOjRiaB?= MnvWZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmLZNlU5OTByMUC=
HH5 M17nOWZ2dmO2aX;uJGF{e2G7 Mmf1NE4xODB3LUOuPEDPxE1? M{TpeVI1KGh? MnywZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmHqNlU5OTByMUC=
UM-22A MmD2SpVv[3Srb36gRZN{[Xl? M3nselAvODByNT2xMlYh|ryP NG\1XpUzPCCq MXLhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4fGVVI2QDFyMEGw
A1847 NUfjTIZPTnWwY4Tpc44hSXO|YYm= M2rPVVAvODVvMUCg{txO MYSyOEBp NUHTVVlpTE2VT9Mg NWfWUI96emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MmHmNlU3PDZyMUW=
OVCAR-5 M{OxSmZ2dmO2aX;uJGF{e2G7 M4PoRlAvODVvMUCg{txO MUKyOEBp NY\qc45CTE2VT9Mg NVLabVY1emWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NEDDT3AzPTZ2NkCxOS=>
OVCAR-8 MW\GeY5kfGmxbjDBd5NigQ>? NI\U[oQxNjB3LUGwJO69VQ>? MVeyOEBp M3PLV2ROW00EoB?= MV\y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MXOyOVY1PjBzNR?=
MOVCAR-5447 M{C3N2Z2dmO2aX;uJGF{e2G7 NX;MU5l{OC5yNT2xNEDPxE1? M4Owd|I1KGh? MXPEUXNQyqB? M2[2TpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NGHIO4UzPTZ2NkCxOS=>
MOVCAR-5009 NUnMcYlyTnWwY4Tpc44hSXO|YYm= NHPifIkxNjB3LUGwJO69VQ>? NWTsZ2pSOjRiaB?= MoHtSG1UV8Li NUHQWZRYemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NGjpRW4zPTZ2NkCxOS=>
A1847 MnLoR4VtdCCYaXHibYxqfHliQYPzZZk> NXjqeXJvOC5yNT2xNEDPxE1? M1m5VVczKGh? NVjsO3pyTE2VTx?= MUDy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MXuyOVY1PjBzNR?=
OVCAR-5 NUXa[4hES2WubDDWbYFjcWyrdImgRZN{[Xl? Ml2wNE4xPS1zMDFOwG0> NVvLOpNSPzJiaB?= MmXGSG1UVw>? MYry[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= NWXMXo95OjV4NE[wNVU>
OVCAR-8  M{PhOWNmdGxiVnnhZoltcXS7IFHzd4F6 NXPDT4ljOC5yNT2xNEDPxE1? M2TrNVczKGh? Mn;zSG1UVw>? MVvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= Mn[3NlU3PDZyMUW=
OVCAR-5  NWG4V2xVSXCxcITvd4l{KEG|c3H5 M3XnfFAvPS9zL{Wg{txO MXi0PEBp MoHQSG1UVw>? NVP4VWY1cW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> NXLmNlduOjV4NE[wNVU>
OVCAR-8  MVHBdI9xfG:|aYOgRZN{[Xl? M1[0VFAvPS9zL{Wg{txO MYK0PEBp MWnEUXNQ MV;pcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w MkHJNlU3PDZyMUW=
AKRSL MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3TLRlczKGh? MXrJR|Ux97zgMUCg{txO NYHl[Jp6OjV3MES2N|U>
PALJDL NYf1[pZES2WubDDWbYFjcWyrdImgRZN{[Xl? NWP2b21FPzJiaB?= MVLJR|UxRTJwNDFOwG0> NV\uWlB2OjV3MES2N|U>
MO4 NF3qPY9HfW6ldHnvckBCe3OjeR?= NXXVNW9iOC53L{GvOUDPxE1? MWK2JIg> NHLES2lqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? MWCyOVE1QTV|NR?=
DU145  NULab|NoTnWwY4Tpc44hSXO|YYm= NGnsXnYxNTJyMDDuUS=> MX[xJIjDqA>? NX73Xm0ze3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> M3O3NVI1PTd5OUSy
DU145  M4\zcGZ2dmO2aX;uJGF{e2G7 NITGR4g5ODBibl2= M2fCOFczKGh? NE[1Omx{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NFz6dXIzPDV5N{m0Ni=>
CWR22Rv1 M1LhSGZ2dmO2aX;uJGF{e2G7 NUPuSWE3QDByIH7N MnXlO|IhcA>? NF3vcHl{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NXnhSohvOjR3N{e5OFI>
N592 NVuzVnVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkG2TWM2OD1yLki0JO69VQ>? NVS0VnBYOjRzNUi3NFE>
H82 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3qdZJKSzVyPUGuN|ch|ryP M1vub|I1OTV6N{Cx
GLC4 Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHKO|BKSzVyPUGuO|kh|ryP M4rZcVI1OTV6N{Cx
H526 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPpTYpwUUN3ME2zMlA5KM7:TR?= NY\4PXBWOjRzNUi3NFE>
H1173 MkXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXznS3RkUUN3ME2yMlM6KM7:TR?= NHPleWEzPDF3OEewNS=>
DMS114 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zQT2lEPTB;MD63N{DPxE1? NIHRVIEzPDF3OEewNS=>
NCI-N592 MorvSpVv[3Srb36gRZN{[Xl? NHXNRpYxNjNxMT:zJO69VQ>? MUWyOEBp NV;tOo9ycW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NXrIZmhuOjRzNUi3NFE>
GLC4 NUPnbJhWTnWwY4Tpc44hSXO|YYm= NFPkU20xNjNxMT:zJO69VQ>? NEX6eoMzPCCq NIOxVmdqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NEP2PVYzPDF3OEewNS=>
NCI-H82 Mly1SpVv[3Srb36gRZN{[Xl? M{nJfVAvOy9zL{Og{txO M4n0SlI1KGh? NGnWZW9qdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? MnvLNlQyPTh5MEG=
NCI-N592 MnnaRZBweHSxc3nzJGF{e2G7 MmjLNE4{NzFxMzFOwG0> M1PIWlQ5KGh? M2jBeIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NXe3To5wOjRzNUi3NFE>
GLC4 M3zoRmFxd3C2b4Ppd{BCe3OjeR?= NU\2WHBGOC5|L{GvN{DPxE1? M1\tOFQ5KGh? NIXRWpJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| NWrQTYNKOjRzNUi3NFE>
NCI-H82 NH7DfY9CeG:ydH;zbZMhSXO|YYm= M3vmfFAvOy9zL{Og{txO MUG0PEBp MXXpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MUWyOFE2QDdyMR?=
CWR22Rv1  M2nsc2Fxd3C2b4Ppd{BCe3OjeR?= M2fGZWlEPTB;MD60PFIh|ryP NWS5RWp7OjN7NEKwPVU>
CWR22Pc NFrpN2dCeG:ydH;zbZMhSXO|YYm= Mnf0TWM2OD1yLkSzPEDPxE1? MYGyN|k1OjB7NR?=
PC-3 MnvSRZBweHSxc3nzJGF{e2G7 MWTJR|UxRTFwN{W1JO69VQ>? M2nQTlI{QTR{MEm1
DU145 Mk[2RZBweHSxc3nzJGF{e2G7 NF;TSYFKSzVyPUOuOVE4KM7:TR?= MljyNlM6PDJyOUW=
RC165N Mn\yRZBweHSxc3nzJGF{e2G7 NITDU4hKSzVyPUKuNFg{KM7:TR?= NX7z[Y55OjN7NEKwPVU>
ARPE19 M2L6SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml23SG1UVw>? M3HPRmlEPTB;MkSuN|gh|ryP MlOyNlM2OzF7MkG=
HEK293 M2nJUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnTSG1UVw>? MVnJR|UxRThwNkeg{txO Mom0NlM2OzF7MkG=
KCNR MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG1SG1UVw>? NHSxfYRKSzVyPUCuOFYh|ryP NFH4b3AzOzV|MUmyNS=>
SY5Y NVrET3NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHIcYVFVVOR NYLlbZpVUUN3ME2wMlM3KM7:TR?= NUD0WYJJOjN3M{G5NlE>
BE2 MlP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TtPGROW09? NIf1[YNKSzVyPUCuO|Eh|ryP NHX1e2MzOzV|MUmyNS=>
AS MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljnSG1UVw>? M3L3RWlEPTB;MT61N{DPxE1? MUiyN|U{OTl{MR?=
NGP MmHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLlSG1UVw>? NG\ucJZKSzVyPUCuOVYh|ryP NFPGUZgzOzV|MUmyNS=>
IMR32 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17IOmROW09? NGf5NHJKSzVyPUCuOlYh|ryP NGL3WowzOzV|MUmyNS=>
LAN5 NFq3cXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorlSG1UVw>? MlmxTWM2OD1zLkC0JO69VQ>? MUeyN|U{OTl{MR?=
RH18 MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3YTGxFVVOR M3HSXmlEPTB;MT60NkDPxE1? MnmzNlM2OzF7MkG=
RH30 NFv5OJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\GZ5pYTE2VTx?= NYO5TJllUUN3ME2xMlI2KM7:TR?= NX;O[WkyOjN3M{G5NlE>
RH17 M3\rWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX0SG1UVw>? MX3JR|UxRTJwNUGg{txO NGe1b3gzOzV|MUmyNS=>
RH28 NWDQOYY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX3OJc5TE2VTx?= M3mwTWlEPTB;ND6yPEDPxE1? MUmyN|U{OTl{MR?=
RH36 MmK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf6WIVFVVOR MnrtTWM2OD13LkO3JO69VQ>? M4HoflI{PTNzOUKx
RH41 NV3scnNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLvUmxFVVOR NF;pU2FKSzVyPUCuOFgh|ryP MVKyN|U{OTl{MR?=
RD M{[2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jKZmROW09? M{jKZmlEPTB;ND6zNkDPxE1? MlHqNlM2OzF7MkG=
TC32 NXn5ZWd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfnV5BuTE2VTx?= NX73dlV[UUN3ME2zMlg2KM7:TR?= M2XXR|I{PTNzOUKx
TC71 NEXxdIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjCSG1UVw>? M3LIfmlEPTB;ND6zN{DPxE1? MoPkNlM2OzF7MkG=
KCNR Moi2RZBweHSxc3nzJGF{e2G7 M4DLe|AvPS9zLkCvNk42KM7:TR?= MnfNNlQhcA>? NYLrfJN{TE2VTx?= M1vIN4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NXyzSZJJOjN3M{G5NlE>
SY5Y NI\TNndCeG:ydH;zbZMhSXO|YYm= NFHrPZIxNjVxMT6wM|IvPSEQvF2= M1HOUlI1KGh? NUW5NI46TE2VTx?= NVrUdo1DcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NIe3UHUzOzV|MUmyNS=>
Rh18 NVvVUGtrSXCxcITvd4l{KEG|c3H5 NYq3TJd{OC53L{GuNE8zNjVizszN M3nSZlI1KGh? M4\UPWROW09? MoGybY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NYHjTVBzOjN3M{G5NlE>
TC32 MkLXRZBweHSxc3nzJGF{e2G7 NEDT[YcxNjVxMT6wM|IvPSEQvF2= M1:2WlI1KGh? NYjYVXpXTE2VTx?= Mo\BbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MoLqNlM2OzF7MkG=
KCNR NIDWZo9HfW6ldHnvckBCe3OjeR?= NYDPVFlmOC53L{GuNE8zNjVxNTFOwG0> MX6yOEBp NV7wUZhFTE2VTx?= MVnpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MmT4NlM2OzF7MkG=
SY5Y MWjGeY5kfGmxbjDBd5NigQ>? MYKwMlUwOS5yL{KuOU82KM7:TR?= NVPBbnZ3OjRiaB?= MoTUSG1UVw>? NHHRemlqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MWqyN|U{OTl{MR?=
Rh18 M2jLbWZ2dmO2aX;uJGF{e2G7 MX[wMlUwOS5yL{KuOU82KM7:TR?= NETybYYzPCCq MWPEUXNQ MmDGbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MUKyN|U{OTl{MR?=
TC32 M3;yPGZ2dmO2aX;uJGF{e2G7 NGK3UJUxNjVxMT6wM|IvPS93IN88US=> NF34eY8zPCCq NHXZ[VZFVVOR MVTpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MoDjNlM2OzF7MkG=
TPC-1 NXLXOnNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHOVIQyKML3TR?= MkH2NE01KGR? M1rIdGROW09? M{PuS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? MXmyN|A2PjR7OR?=
MZ-CRC1  NV\DdJhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr4NUDDvU1? NEf6TWUxNTViZB?= NU[zenJGTE2VTx?= NVfoWllMcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NGLXcWgzOzB3NkS5PS=>
TT  M16xe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSxJOK2VQ>? NVjOW3gzOC12IHS= NGjmeGxFVVOR NVzub2d3cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= Mm\lNlMxPTZ2OUm=
TPC-1 MYfGeY5kfGmxbjDBd5NigQ>? Mln6NUDDvU1? MkH0O|IhcA>? M{H6dGROW09? NFX2[oNqdmS3Y3XzJGcyKGKub3PrZYdm NIDP[IIzOzB3NkS5PS=>
MZ-CRC1  MWPGeY5kfGmxbjDBd5NigQ>? MmGxNUDDvU1? NHnYR|k4OiCq NIrLUYhFVVOR NES3e4VqdmS3Y3XzJGcyKGKub3PrZYdm NHXnPYkzOzB3NkS5PS=>
TT  NYHBZnJ5TnWwY4Tpc44hSXO|YYm= NH\WOW4yKML3TR?= MYO3NkBp MnPGSG1UVw>? MUHpcoR2[2W|IFexJIJtd2OtYXfl MYiyN|A2PjR7OR?=
MZ-CRC1  NYiwSVVMSXCxcITvd4l{KEG|c3H5 M2XkbVEhyrWP NUTXbWI3PDhiaB?= M13HcWROW09? MX\pcoR2[2W|IHHwc5B1d3Orcx?= M2PzNVI{ODV4NEm5
TT  MVHBdI9xfG:|aYOgRZN{[Xl? M3[3b|EhyrWP NVfNWWdxPDhiaB?= NXHhPZBDTE2VTx?= MWLpcoR2[2W|IHHwc5B1d3Orcx?= NFG3O40zOzB3NkS5PS=>
HD-LM2 MkXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDSO|LjiImq NHyyNphFVVOR Mo\BTWM2OD15Lki0OEDPxE1? MUGyNlgzQTB7NB?=
L-428 M{\RUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnS1O|LjiImq Mo[ySG1UVw>? NXzFS4o{UUN3ME23Mlk1PyEQvF2= NUm1TFczOjJ6MkmwPVQ>
KM-H2 MnrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P0NVcz6oDLaB?= Mk\sSG1UVw>? NEfTW5lKSzVyPUGuN|A5KM7:TR?= M3rOXFIzQDJ7MEm0
L-540 MlS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ryTFcz6oDLaB?= MYHEUXNQ NXLiVIp1UUN3ME24MlIyPiEQvF2= NIryR4QzOjh{OUC5OC=>
HD-LM2 NGfkVHdHfW6ldHnvckBCe3OjeR?= MVKwMlEwOC53L{GvOUDPxE1? NUX4S|RwPzMkgJno M3e4NGROW09? MY\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MlzxNlI5OjlyOUS=
L-428 MlzISpVv[3Srb36gRZN{[Xl? MlXrNE4yNzBwNT:xM|Uh|ryP M2XUOFcz6oDLaB?= NGLJ[WNFVVOR NH;5XnJqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NFTCZnUzOjh{OUC5OC=>
KM-H2 NHvORZNHfW6ldHnvckBCe3OjeR?= NVrK[5RvOC5zL{CuOU8yNzVizszN NYrsUJd5PzMkgJno NFvmSVFFVVOR NEPKU2JqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NV7QO4ViOjJ6MkmwPVQ>
L-540 Mo\ISpVv[3Srb36gRZN{[Xl? M17xTVAvOS9yLkWvNU82KM7:TR?= Ml;2O|LjiImq NGrIOGJFVVOR NFjmXHNqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? Ml30NlI5OjlyOUS=
HD-LM2 MoHRRZBweHSxc3nzJGF{e2G7 NH3EbHQyNzVizszN MXu3NwKBkWh? Mk\ZSG1UVw>? NGf1[GxqdmS3Y3XzJIFxd3C2b4Ppdy=> NEjNSlQzOjh{OUC5OC=>
L-428 M{fHWGFxd3C2b4Ppd{BCe3OjeR?= Mn33NU82KM7:TR?= M{Gyelcz6oDLaB?= NG\5Uo1FVVOR MWnpcoR2[2W|IHHwc5B1d3Orcx?= M2XveVIzQDJ7MEm0
KM-H2 NW\6N3NsSXCxcITvd4l{KEG|c3H5 MkP3NU82KM7:TR?= NGHmNmM4OuLCiXi= NF\FZZZFVVOR MXHpcoR2[2W|IHHwc5B1d3Orcx?= Ml3iNlI5OjlyOUS=
L-540 NHv3XGpCeG:ydH;zbZMhSXO|YYm= MmrINU82KM7:TR?= NFfpfWs4OuLCiXi= NVzu[YRFTE2VTx?= MnvIbY5lfWOnczDhdI9xfG:|aYO= M{XXeFIzQDJ7MEm0
U251-MG MUfGeY5kfGmxbjDBd5NigQ>? NVy0ZodnOSEEtV2= M1XBW|AuOTZiaB?= M3;iSIlvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NIDMbm4zOjB{N{[5NS=>
U87-MG Mli1SpVv[3Srb36gRZN{[Xl? NEHTbo0yKML3TR?= M2XWWlAuOTZiaB?= NFiyUm5qdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NX\6TGZ6OjJyMke2PVE>
4C8 MnTISpVv[3Srb36gRZN{[Xl? MnjONUDDvU1? NHToZmQxNTF4IHi= MofsbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MVGyNlAzPzZ7MR?=
U251-MG NHPiWIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\IZ3gyNzFyINM1US=> NHr2SZIzPC92OD:3NkBp MUfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MW[yNlAzPzZ7MR?=
U87-MG NWn0XHJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5dWRFOS9zMDFCuW0> NGG2eoozPC92OD:3NkBp M4DzNolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NISwcowzOjB{N{[5NS=>
4C8 MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXMepgyNzFyINM1US=> M17vTVI1NzR6L{eyJIg> NEjjXnNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NWX1fnh1OjJyMke2PVE>
U266 MX7BdI9xfG:|aYOgRZN{[Xl? MVywMlUuOiEQvF2= NUnnOpV2PDhxN{KgbC=> M{LQW4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MVSyNVE3PDVzNx?=
Kms.11 MkLZRZBweHSxc3nzJGF{e2G7 Mn;SNE42NTJizszN M3mxdVQ5Nzd{IHi= NFPxXHdqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NIi2VYwzOTF4NEWxOy=>
8226 M4\1PWFxd3C2b4Ppd{BCe3OjeR?= MYCwMlUuOiEQvF2= MXe0PE84OiCq NWHOfndPcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MUGyNVE3PDVzNx?=

多くの細胞株試験データを見る場合、クリックしてください

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 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 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、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

JAK信号経路図

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
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