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。

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カスタマーフィードバック(2)

  • 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.

    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。
靶点
JAK2 [1]
(Cell-free assay)
0.26 nM
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW620 MlzpSpVv[3Srb36gRZN{[Xl? M13U[VUh|ryP M{ezblQ5KGh? NIHiOJlFVVOR NV\zTYM3[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o M3nmPVI2QTV2OUe0
LoVo  MmL6SpVv[3Srb36gRZN{[Xl? NW\yNVc5PSEQvF2= NXfKN|lxPDhiaB?= NGLEW3pFVVOR MUPicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= MUKyOVk2PDl5NB?=
HN5 NGf2blJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrUcIc4OiCq MmKzSWM2OD1|LkixJOKyKDFwOUmg{txO Ml\3NlU5OTByMUC=
Cal33 NHH3UVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7vNW5JPzJiaB?= Mne2SWM2OD1|LkO3JOKyKDBwN{Wg{txO MWeyOVgyODBzMB?=
UM-22B M{HuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{mwelczKGh? MWTFR|UxRTJwNk[gxtEhOC5{NDFOwG0> MlXuNlU5OTByMUC=
686LN NFG0OJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVqzbVA{PzJiaB?= NGn3dlVGSzVyPUKuNFUhyrFiMT6zN{DPxE1? NVrQdW1OOjV6MUCwNVA>
UM SCC-1 NHjadFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fhPFczKGh? NWS0SnZVTUN3ME2xMlY4KMLzIECuOFIh|ryP MWGyOVgyODBzMB?=
UM-22A Mly1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rvUVczKGh? M{D4TGVEPTB;MT6zNkDDuSByLkO5JO69VQ>? MUKyOVgyODBzMB?=
OSC19 MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rDZ|czKGh? MWnFR|UxRTFwMk[gxtEhOC5{MDFOwG0> MmjMNlU5OTByMUC=
PCI-52 NGTpU|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnL6O|IhcA>? NVjQfm52TUN3ME2xMlAxKMLzIECuNFkh|ryP NI\We4szPThzMECxNC=>
PCI-15B MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PQU|czKGh? M{m4VmVEPTB;MD65PUDDuSBzLke0JO69VQ>? M4LDSVI2QDFyMEGw
UMSCC-1 MWfGeY5kfGmxbjDBd5NigQ>? MmHyNE4xODB3LUGuOkDPxE1? M{XIUlI1KGh? MmjuZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4nDS|I2QDFyMEGw
Cal33 MmPOSpVv[3Srb36gRZN{[Xl? M3PIcFAvODByNT2zMlgh|ryP MW[yOEBp NUSwSow2[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2rNUFI2QDFyMEGw
HH5 NVK4WJhZTnWwY4Tpc44hSXO|YYm= MlfnNE4xODB3LUOuPEDPxE1? MVqyOEBp NXLCeJVi[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NI\E[3EzPThzMECxNC=>
UM-22A Ml;4SpVv[3Srb36gRZN{[Xl? MlPoNE4xODB3LUGuOkDPxE1? NFzFcnIzPCCq M2T2VYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYiyOVgyODBzMB?=
A1847 MVfGeY5kfGmxbjDBd5NigQ>? NEOyOGYxNjB3LUGwJO69VQ>? M1XYNFI1KGh? M2L3TmROW00EoB?= NX62ZZVnemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> NGrRTYczPTZ2NkCxOS=>
OVCAR-5 Mn64SpVv[3Srb36gRZN{[Xl? NIq1TY8xNjB3LUGwJO69VQ>? M3XvWlI1KGh? M4HjZWROW00EoB?= MmHudoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MYeyOVY1PjBzNR?=
OVCAR-8 MVTGeY5kfGmxbjDBd5NigQ>? Mo\KNE4xPS1zMDFOwG0> MYeyOEBp NGjUXVFFVVORwrC= M{DCUJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NVHiU2hZOjV4NE[wNVU>
MOVCAR-5447 M3THZWZ2dmO2aX;uJGF{e2G7 Ml;jNE4xPS1zMDFOwG0> NUnYbnV[OjRiaB?= M1zCZmROW00EoB?= MVHy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= M2H6TlI2PjR4MEG1
MOVCAR-5009 Mlj1SpVv[3Srb36gRZN{[Xl? MnW5NE4xPS1zMDFOwG0> M1uzS|I1KGh? NEfRWnpFVVORwrC= Mn\EdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MXWyOVY1PjBzNR?=
A1847 MnrvR4VtdCCYaXHibYxqfHliQYPzZZk> Mk\JNE4xPS1zMDFOwG0> Mke0O|IhcA>? MmTPSG1UVw>? NYr6UZQyemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> M2TXO|I2PjR4MEG1
OVCAR-5 M2Lvb2NmdGxiVnnhZoltcXS7IFHzd4F6 NVHGe3pIOC5yNT2xNEDPxE1? NFHoZ4o4OiCq M37ySGROW09? NVTQeId7emWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NF2xemEzPTZ2NkCxOS=>
OVCAR-8  MkTjR4VtdCCYaXHibYxqfHliQYPzZZk> M4frUVAvODVvMUCg{txO NIfO[3A4OiCq MVzEUXNQ MVjy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= MViyOVY1PjBzNR?=
OVCAR-5  NIXNdpRCeG:ydH;zbZMhSXO|YYm= MmjiNE42NzFxNTFOwG0> NYPlcFk3PDhiaB?= NUPKXW9NTE2VTx?= MWPpcoR2[2W|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w NULBeXpDOjV4NE[wNVU>
OVCAR-8  MkG4RZBweHSxc3nzJGF{e2G7 MUKwMlUwOS93IN88US=> MV[0PEBp NHfZd4JFVVOR M{LJV4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MVuyOVY1PjBzNR?=
AKRSL MlrwR4VtdCCYaXHibYxqfHliQYPzZZk> MUm3NkBp MVvJR|Ux97zgMUCg{txO NX\YcXFFOjV3MES2N|U>
PALJDL M4jRbGNmdGxiVnnhZoltcXS7IFHzd4F6 M1rCSlczKGh? MXTJR|UxRTJwNDFOwG0> MoTvNlU2ODR4M{W=
MO4 NVTQU5VxTnWwY4Tpc44hSXO|YYm= NE\rN|UxNjVxMT:1JO69VQ>? NWHF[Zg5PiCq MUTpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> NGDlfHkzPTF2OUWzOS=>
DU145  MnvISpVv[3Srb36gRZN{[Xl? MojtNE0zODBibl2= MUKxJIjDqA>? MWrzeZBxemW|c3XzJGlNNTZvYXP0bZZifGWmIGP0ZZQ{KGGwZDDFVmsyNzJic3nncoFtcW6p NGOxUpYzPDV5N{m0Ni=>
DU145  MVvGeY5kfGmxbjDBd5NigQ>? M{fYS|gxOCCwTR?= M2HISlczKGh? NHLoZ|d{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= NIfBbXUzPDV5N{m0Ni=>
CWR22Rv1 NEDiZlRHfW6ldHnvckBCe3OjeR?= MYC4NFAhdk1? M2nXR|czKGh? MUnzeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? NV3oVHpWOjR3N{e5OFI>
N592 NIL5SZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwOESg{txO M3XuVFI1OTV6N{Cx
H82 NHz3VlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPo[IdKSzVyPUGuN|ch|ryP M4fR[|I1OTV6N{Cx
GLC4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3lTWM2OD1zLke5JO69VQ>? M4PEZ|I1OTV6N{Cx
H526 M4f5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTNwMEig{txO MU[yOFE2QDdyMR?=
H1173 MknzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTJwM{mg{txO NInJOJMzPDF3OEewNS=>
DMS114 NXzIcHV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH61[JBKSzVyPUCuO|Mh|ryP NESyU5QzPDF3OEewNS=>
NCI-N592 NEjB[YhHfW6ldHnvckBCe3OjeR?= NHvWPGExNjNxMT:zJO69VQ>? NF;sN4EzPCCq NGfOUZpqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NE\XSWUzPDF3OEewNS=>
GLC4 MXvGeY5kfGmxbjDBd5NigQ>? NEf5fJUxNjNxMT:zJO69VQ>? MYmyOEBp NYiydZZwcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MWqyOFE2QDdyMR?=
NCI-H82 M4rZbmZ2dmO2aX;uJGF{e2G7 MUSwMlMwOS9|IN88US=> M13ESVI1KGh? MoPmbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NUPMUFJiOjRzNUi3NFE>
NCI-N592 NHvOV2xCeG:ydH;zbZMhSXO|YYm= M4TvVlAvOy9zL{Og{txO NFnDbIE1QCCq MX7pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NYLTXmF[OjRzNUi3NFE>
GLC4 MXzBdI9xfG:|aYOgRZN{[Xl? NH2xb4gxNjNxMT:zJO69VQ>? NHH1OI41QCCq MlXjbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MXiyOFE2QDdyMR?=
NCI-H82 NIDEOHVCeG:ydH;zbZMhSXO|YYm= MX6wMlMwOS9|IN88US=> MkfZOFghcA>? MV3pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NHPy[ZkzPDF3OEewNS=>
CWR22Rv1  NEHaWJpCeG:ydH;zbZMhSXO|YYm= NUHxeZlmUUN3ME2wMlQ5OiEQvF2= NV\pU|RGOjN7NEKwPVU>
CWR22Pc Ml\SRZBweHSxc3nzJGF{e2G7 NGjlbFFKSzVyPUCuOFM5KM7:TR?= M3Lx[lI{QTR{MEm1
PC-3 NUHDV2dzSXCxcITvd4l{KEG|c3H5 M2LpSGlEPTB;MT63OVUh|ryP NXnOfJI3OjN7NEKwPVU>
DU145 M{fCeWFxd3C2b4Ppd{BCe3OjeR?= MmfQTWM2OD1|LkWxO{DPxE1? MnflNlM6PDJyOUW=
RC165N NI\ZeYFCeG:ydH;zbZMhSXO|YYm= MXLJR|UxRTJwMEizJO69VQ>? MlLZNlM6PDJyOUW=
ARPE19 NFzobINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yyZmROW09? NYHTVXp[UUN3ME2yOE4{QCEQvF2= NUL1fVhCOjN3M{G5NlE>
HEK293 MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITCdHRFVVOR MVXJR|UxRThwNkeg{txO MlXtNlM2OzF7MkG=
KCNR NX;WOnd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jJeWROW09? NF[zdG9KSzVyPUCuOFYh|ryP MYCyN|U{OTl{MR?=
SY5Y NUHmdYl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLEUXNQ M4LZXmlEPTB;MD6zOkDPxE1? M1nxR|I{PTNzOUKx
BE2 M37IbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\3SG1UVw>? M4XSUmlEPTB;MD63NUDPxE1? NWP0SHZKOjN3M{G5NlE>
AS M2XTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7OSG1UVw>? MUTJR|UxRTFwNUOg{txO NF;wbFgzOzV|MUmyNS=>
NGP MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M373NmROW09? NGL5bnlKSzVyPUCuOVYh|ryP MYKyN|U{OTl{MR?=
IMR32 NXPHcGprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPuSG1UVw>? MmTITWM2OD1yLk[2JO69VQ>? NVH2eWszOjN3M{G5NlE>
LAN5 Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\JSG1UVw>? NHHRTI5KSzVyPUGuNFQh|ryP MXeyN|U{OTl{MR?=
RH18 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXaSG1UVw>? NE\0WpBKSzVyPUGuOFIh|ryP MorpNlM2OzF7MkG=
RH30 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;SPWlWTE2VTx?= NFzoPIVKSzVyPUGuNlUh|ryP M2PLdFI{PTNzOUKx
RH17 M2TtOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjKNGdFVVOR M364bWlEPTB;Mj61NUDPxE1? MlfBNlM2OzF7MkG=
RH28 M{PKb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjEUXNQ NFu5cJdKSzVyPUSuNlgh|ryP M3P4e|I{PTNzOUKx
RH36 M2ryVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3SN5hFVVOR NIXDSpBKSzVyPUWuN|ch|ryP MWKyN|U{OTl{MR?=
RH41 MmfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7EUXNQ M4K0VGlEPTB;MD60PEDPxE1? MWGyN|U{OTl{MR?=
RD M4DSNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvUZXlFVVOR MmXsTWM2OD12LkOyJO69VQ>? MmTjNlM2OzF7MkG=
TC32 M1HWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XofWROW09? MVzJR|UxRTNwOEWg{txO Mlr1NlM2OzF7MkG=
TC71 MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PURWROW09? M3X3W2lEPTB;ND6zN{DPxE1? NWrYeJBjOjN3M{G5NlE>
KCNR NIi1c2FCeG:ydH;zbZMhSXO|YYm= M3[zU|AvPS9zLkCvNk42KM7:TR?= NH7yVIczPCCq M4XRc2ROW09? MX;pcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MVWyN|U{OTl{MR?=
SY5Y MoXlRZBweHSxc3nzJGF{e2G7 NI\PeFYxNjVxMT6wM|IvPSEQvF2= NULxSYFFOjRiaB?= M1\ySWROW09? M3X0dIlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= NEL0UZMzOzV|MUmyNS=>
Rh18 MkX0RZBweHSxc3nzJGF{e2G7 MY[wMlUwOS5yL{KuOUDPxE1? NH\PdmIzPCCq Mki4SG1UVw>? NXfs[4RicW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NFPFc4czOzV|MUmyNS=>
TC32 M{m3NWFxd3C2b4Ppd{BCe3OjeR?= MkDENE42NzFwMD:yMlUh|ryP NXTkS5psOjRiaB?= M3PZTGROW09? NUXwcollcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MXyyN|U{OTl{MR?=
KCNR M{fzW2Z2dmO2aX;uJGF{e2G7 NFnN[ZgxNjVxMT6wM|IvPS93IN88US=> NV73R3BqOjRiaB?= NXjDU2czTE2VTx?= MUTpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NF7wepkzOzV|MUmyNS=>
SY5Y MXXGeY5kfGmxbjDBd5NigQ>? MlzaNE42NzFwMD:yMlUwPSEQvF2= MmD6NlQhcA>? MmD1SG1UVw>? M4nFcYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u MYmyN|U{OTl{MR?=
Rh18 NYHvUnllTnWwY4Tpc44hSXO|YYm= NXPIeo9UOC53L{GuNE8zNjVxNTFOwG0> NFHwWI0zPCCq NY\yfnU5TE2VTx?= NFTJem5qdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NGGxPJAzOzV|MUmyNS=>
TC32 M4XrfWZ2dmO2aX;uJGF{e2G7 NWnNTY15OC53L{GuNE8zNjVxNTFOwG0> M1S0[lI1KGh? MYnEUXNQ NHXxfFNqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> Mo\YNlM2OzF7MkG=
TPC-1 NWSxZnpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHyXFhzOSEEtV2= MVGwMVQh\A>? NYjmVJFjTE2VTx?= MUDpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCyJIQhfHKnYYTt[Y51 NFPEOoszOzB3NkS5PS=>
MZ-CRC1  M4f2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13R[|EhyrWP NGi5XnoxNTViZB?= MXTEUXNQ NVLtNZNjcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NHPlVo0zOzB3NkS5PS=>
TT  NH\nU4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnlNUDDvU1? MXqwMVQh\A>? MYLEUXNQ MXTpcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 M3S2W|I{ODV4NEm5
TPC-1 M3HUcmZ2dmO2aX;uJGF{e2G7 NXnG[mlsOSEEtV2= MmL5O|IhcA>? M{XRRmROW09? MlP1bY5lfWOnczDHNUBjdG:la3Hn[S=> MX6yN|A2PjR7OR?=
MZ-CRC1  NHv0eFFHfW6ldHnvckBCe3OjeR?= MonENUDDvU1? NVvzOIdJPzJiaB?= NGHKSIxFVVOR Mmq4bY5lfWOnczDHNUBjdG:la3Hn[S=> M4W1cFI{ODV4NEm5
TT  MonpSpVv[3Srb36gRZN{[Xl? MoTQNUDDvU1? MmrwO|IhcA>? NWnN[INiTE2VTx?= M13sV4lv\HWlZYOgS|Eh[myxY3vh[4U> MWGyN|A2PjR7OR?=
MZ-CRC1  NWqxfY93SXCxcITvd4l{KEG|c3H5 Mn6xNUDDvU1? NGPuTVY1QCCq MmHySG1UVw>? M3z4S4lv\HWlZYOgZZBweHSxc3nz M17Q[VI{ODV4NEm5
TT  M{XnTWFxd3C2b4Ppd{BCe3OjeR?= MV6xJOK2VQ>? M3;kSlQ5KGh? M{H5NWROW09? NIjLeppqdmS3Y3XzJIFxd3C2b4Ppdy=> NHnFZVMzOzB3NkS5PS=>
HD-LM2 MnG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWq5eZdwPzMkgJno MnLXSG1UVw>? M1nRTmlEPTB;Nz64OFQh|ryP MXiyNlgzQTB7NB?=
L-428 MkXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS3NwKBkWh? Mlv6SG1UVw>? NIflWXNKSzVyPUeuPVQ4KM7:TR?= MW[yNlgzQTB7NB?=
KM-H2 NV;FNG1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzq[XZpPzMkgJno NFPneopFVVOR MUTJR|UxRTFwM{C4JO69VQ>? NIPKRVAzOjh{OUC5OC=>
L-540 NH\PcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[5XVcz6oDLaB?= M1PNNmROW09? MYTJR|UxRThwMkG2JO69VQ>? MYSyNlgzQTB7NB?=
HD-LM2 NUiwTZdqTnWwY4Tpc44hSXO|YYm= NEi1TmYxNjFxMD61M|EwPSEQvF2= Mn;hO|LjiImq M1rpNWROW09? MoG3bY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NWTnXnZHOjJ6MkmwPVQ>
L-428 NE\4[XVHfW6ldHnvckBCe3OjeR?= M3[3RVAvOS9yLkWvNU82KM7:TR?= NFjYdXg4OuLCiXi= NGrx[mRFVVOR NHjzN4FqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? MoPQNlI5OjlyOUS=
KM-H2 M{LhdWZ2dmO2aX;uJGF{e2G7 NI\MUXgxNjFxMD61M|EwPSEQvF2= MlfQO|LjiImq NH\TNllFVVOR MXvpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NH\VU|UzOjh{OUC5OC=>
L-540 MWTGeY5kfGmxbjDBd5NigQ>? NGLleYwxNjFxMD61M|EwPSEQvF2= MVq3NwKBkWh? MYLEUXNQ M1KzN4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NFrZelUzOjh{OUC5OC=>
HD-LM2 NULDOIJkSXCxcITvd4l{KEG|c3H5 MmSxNU82KM7:TR?= Mo\SO|LjiImq NH3MOlFFVVOR MlnnbY5lfWOnczDhdI9xfG:|aYO= MU[yNlgzQTB7NB?=
L-428 MkfPRZBweHSxc3nzJGF{e2G7 NHjBWFcyNzVizszN MmXPO|LjiImq M4DhRWROW09? MmXMbY5lfWOnczDhdI9xfG:|aYO= MmD4NlI5OjlyOUS=
KM-H2 NHnwd5NCeG:ydH;zbZMhSXO|YYm= Ml:2NU82KM7:TR?= NITxbmk4OuLCiXi= M1fRZmROW09? MUHpcoR2[2W|IHHwc5B1d3Orcx?= MojlNlI5OjlyOUS=
L-540 NInxNXNCeG:ydH;zbZMhSXO|YYm= MlH3NU82KM7:TR?= MXy3NwKBkWh? NFfSdo9FVVOR MVjpcoR2[2W|IHHwc5B1d3Orcx?= NHnGTHAzOjh{OUC5OC=>
U251-MG MYXGeY5kfGmxbjDBd5NigQ>? NYrmeYtjOSEEtV2= NEfKNGcxNTF4IHi= NUjjZ|J7cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MoixNlIxOjd4OUG=
U87-MG MnzFSpVv[3Srb36gRZN{[Xl? M{jlVFEhyrWP NIPqOIQxNTF4IHi= MUHpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MlvLNlIxOjd4OUG=
4C8 NHriOYdHfW6ldHnvckBCe3OjeR?= MUmxJOK2VQ>? M{\mPVAuOTZiaB?= NYnzdlZZcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MmHrNlIxOjd4OUG=
U251-MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojONU8yOCEEtV2= NFryWmMzPC92OD:3NkBp NVz3d2JHcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MlvHNlIxOjd4OUG=
U87-MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL2VIFjOS9zMDFCuW0> M1\COlI1NzR6L{eyJIg> MlnkbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> MnHzNlIxOjd4OUG=
4C8 NH;kUJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnWToNROS9zMDFCuW0> MlzNNlQwPDhxN{KgbC=> M{O1bYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO M1[xPFIzODJ5Nkmx
U266 Ml34RZBweHSxc3nzJGF{e2G7 M3jSXlAvPS1{IN88US=> MX60PE84OiCq MWjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M{LXdVIyOTZ2NUG3
Kms.11 NXTqPG14SXCxcITvd4l{KEG|c3H5 MUSwMlUuOiEQvF2= M1j4OVQ5Nzd{IHi= NXPYe3dlcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NW[yPHh1OjFzNkS1NVc>
8226 MoP4RZBweHSxc3nzJGF{e2G7 NX3tRpFIOC53LUKg{txO M{DCV|Q5Nzd{IHi= MXvpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NYfsfHdTOjFzNkS1NVc>

... 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[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.
細胞アッセイ: [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)
動物実験:[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 <1 mg/mL
Ethanol <1 mg/mL
体内 30% PEG400+0.5% Tween80+5% propylene glycol 5 mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID