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(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(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 NV74bZpHTnWwY4Tpc44hSXO|YYm= NHXRV3Y2KM7:TR?= MoS4OFghcA>? M4GyWmROW09? MV7icI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= MUKyOVk2PDl5NB?=
LoVo  Mof3SpVv[3Srb36gRZN{[Xl? NIDCT5k2KM7:TR?= NUDlWplGPDhiaB?= MUjEUXNQ MmDOZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n MlL5NlU6PTR7N{S=
HN5 NH3VSItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWq3NkBp NYKyT2E2TUN3ME2zMlgyKMLzIEGuPVkh|ryP NWHt[GZQOjV6MUCwNVA>
Cal33 NYjy[4Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP1d4Y4OiCq MV3FR|UxRTNwM{egxtEhOC55NTFOwG0> NY[1OZhJOjV6MUCwNVA>
UM-22B NWDPXnZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVi3NkBp M4q0WmVEPTB;Mj62OkDDuSByLkK0JO69VQ>? NFvmOXkzPThzMECxNC=>
686LN NHHOSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln2O|IhcA>? MoGwSWM2OD1{LkC1JOKyKDFwM{Og{txO Ml\rNlU5OTByMUC=
UM SCC-1 M3zLS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX34SYhVPzJiaB?= NWm0eXJwTUN3ME2xMlY4KMLzIECuOFIh|ryP MViyOVgyODBzMB?=
UM-22A MoLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWe3NkBp M{nZd2VEPTB;MT6zNkDDuSByLkO5JO69VQ>? NX2yWYFyOjV6MUCwNVA>
OSC19 M4XhNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3jeXZmPzJiaB?= NHzXPJVGSzVyPUGuNlYhyrFiMD6yNEDPxE1? MX:yOVgyODBzMB?=
PCI-52 NV32TZJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLVO|IhcA>? NGTjR4JGSzVyPUGuNFAhyrFiMD6wPUDPxE1? NWPY[XNwOjV6MUCwNVA>
PCI-15B NXXq[3RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj5e2F7PzJiaB?= NFTFcllGSzVyPUCuPVkhyrFiMT63OEDPxE1? M3\U[|I2QDFyMEGw
UMSCC-1 NV7H[I94TnWwY4Tpc44hSXO|YYm= Mn20NE4xODB3LUGuOkDPxE1? MX2yOEBp MmfNZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mm\YNlU5OTByMUC=
Cal33 M1zZdGZ2dmO2aX;uJGF{e2G7 MmjrNE4xODB3LUOuPEDPxE1? NHLhUXczPCCq NGmybFVi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHi1T4kzPThzMECxNC=>
HH5 NXXDd|dvTnWwY4Tpc44hSXO|YYm= MofYNE4xODB3LUOuPEDPxE1? M13xSlI1KGh? MnL5ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1XCVVI2QDFyMEGw
UM-22A MXnGeY5kfGmxbjDBd5NigQ>? MYqwMlAxODVvMT62JO69VQ>? Ml7yNlQhcA>? NUT4RZM1[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFnyOoEzPThzMECxNC=>
A1847 NXjC[HlKTnWwY4Tpc44hSXO|YYm= MXmwMlA2NTFyIN88US=> NXTLPZo3OjRiaB?= MoXUSG1UV8Li M2npRZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NELqXHAzPTZ2NkCxOS=>
OVCAR-5 Mlj1SpVv[3Srb36gRZN{[Xl? MX6wMlA2NTFyIN88US=> NYXveIliOjRiaB?= MXzEUXNQyqB? M{nQdZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz MW[yOVY1PjBzNR?=
OVCAR-8 MXjGeY5kfGmxbjDBd5NigQ>? Mn\QNE4xPS1zMDFOwG0> M1rRcFI1KGh? MXPEUXNQyqB? M{XH[ZJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz M3ezXVI2PjR4MEG1
MOVCAR-5447 M4LwW2Z2dmO2aX;uJGF{e2G7 MU[wMlA2NTFyIN88US=> NXnEc3k5OjRiaB?= MnTESG1UV8Li NH:wOZZz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MlPkNlU3PDZyMUW=
MOVCAR-5009 MlL4SpVv[3Srb36gRZN{[Xl? MXewMlA2NTFyIN88US=> NIfPdmYzPCCq Mne4SG1UV8Li MmS0doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= M1LDU|I2PjR4MEG1
A1847 NUPuUHdtS2WubDDWbYFjcWyrdImgRZN{[Xl? M1\NVlAvODVvMUCg{txO M4T0NVczKGh? MUnEUXNQ NIDWfGJz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MnvVNlU3PDZyMUW=
OVCAR-5 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoLGNE4xPS1zMDFOwG0> M2n3dFczKGh? MnXaSG1UVw>? NIj4U5Zz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NXXv[|Z3OjV4NE[wNVU>
OVCAR-8  M{jBeGNmdGxiVnnhZoltcXS7IFHzd4F6 M1OxWlAvODVvMUCg{txO MWW3NkBp MkPRSG1UVw>? NWnqWIVGemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NUCzd5lkOjV4NE[wNVU>
OVCAR-5  MnK3RZBweHSxc3nzJGF{e2G7 NYjKbVNTOC53L{GvOUDPxE1? MVy0PEBp NYf1fFd{TE2VTx?= NUj4VYNGcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> NF7pOYkzPTZ2NkCxOS=>
OVCAR-8  NV7nTY5XSXCxcITvd4l{KEG|c3H5 M3zIXFAvPS9zL{Wg{txO MoD6OFghcA>? MUnEUXNQ M1\ZT4lv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= M3zrUFI2PjR4MEG1
AKRSL M4jXTGNmdGxiVnnhZoltcXS7IFHzd4F6 MYm3NkBp M{LvUmlEPTExvK6xNEDPxE1? M{OxeFI2PTB2NkO1
PALJDL MWjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYXkN49nPzJiaB?= NUfEdVg6UUN3ME2yMlQh|ryP MlLsNlU2ODR4M{W=
MO4 M4\UTWZ2dmO2aX;uJGF{e2G7 NIL5W2IxNjVxMT:1JO69VQ>? MUW2JIg> MXzpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> MUGyOVE1QTV|NR?=
DU145  MUPGeY5kfGmxbjDBd5NigQ>? M4DUUFAuOjByIH7N NFrFXYUyKGkEoB?= NHGzSFJ{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NYLrWFVHOjR3N{e5OFI>
DU145  MYjGeY5kfGmxbjDBd5NigQ>? MWe4NFAhdk1? M4\FPVczKGh? NFHWfG5{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= M3PQV|I1PTd5OUSy
CWR22Rv1 MluySpVv[3Srb36gRZN{[Xl? NFyxWHE5ODBibl2= NFHwPXg4OiCq NYfrNJJve3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 MVmyOFU4Pzl2Mh?=
N592 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTzcZVKSzVyPUCuPFQh|ryP NVfPdWs2OjRzNUi3NFE>
H82 M3z4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvjTWM2OD1zLkO3JO69VQ>? MknhNlQyPTh5MEG=
GLC4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvSTWM2OD1zLke5JO69VQ>? MVGyOFE2QDdyMR?=
H526 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2foTGlEPTB;Mz6wPEDPxE1? Mn2xNlQyPTh5MEG=
H1173 M2fncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTUTW1oUUN3ME2yMlM6KM7:TR?= NGHEeY4zPDF3OEewNS=>
DMS114 MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfncXdKSzVyPUCuO|Mh|ryP M3LT[|I1OTV6N{Cx
NCI-N592 M1PWNmZ2dmO2aX;uJGF{e2G7 MUSwMlMwOS9|IN88US=> MWOyOEBp NXH4VZRLcW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MVWyOFE2QDdyMR?=
GLC4 MnvjSpVv[3Srb36gRZN{[Xl? MXewMlMwOS9|IN88US=> MnrRNlQhcA>? MnjwbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M{juVlI1OTV6N{Cx
NCI-H82 NIiz[2VHfW6ldHnvckBCe3OjeR?= MYGwMlMwOS9|IN88US=> NVPUWoY3OjRiaB?= M131NIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NYDpOVlqOjRzNUi3NFE>
NCI-N592 M3H2e2Fxd3C2b4Ppd{BCe3OjeR?= M13xO|AvOy9zL{Og{txO MlPrOFghcA>? MojkbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NGHZ[IIzPDF3OEewNS=>
GLC4 MojkRZBweHSxc3nzJGF{e2G7 MojXNE4{NzFxMzFOwG0> MY[0PEBp M{PIWIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MonMNlQyPTh5MEG=
NCI-H82 MVzBdI9xfG:|aYOgRZN{[Xl? NEPOc5ExNjNxMT:zJO69VQ>? MX:0PEBp MWnpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ NXT3e4J2OjRzNUi3NFE>
CWR22Rv1  NEjBVHNCeG:ydH;zbZMhSXO|YYm= MkKwTWM2OD1yLkS4NkDPxE1? MXOyN|k1OjB7NR?=
CWR22Pc MnnxRZBweHSxc3nzJGF{e2G7 NFjKUWlKSzVyPUCuOFM5KM7:TR?= MYeyN|k1OjB7NR?=
PC-3 MWXBdI9xfG:|aYOgRZN{[Xl? NUnPNZhVUUN3ME2xMlc2PSEQvF2= NVr4UYdWOjN7NEKwPVU>
DU145 NHi0[XNCeG:ydH;zbZMhSXO|YYm= NWPRWZhvUUN3ME2zMlUyPyEQvF2= MXqyN|k1OjB7NR?=
RC165N M3u0ZWFxd3C2b4Ppd{BCe3OjeR?= NXThVHBWUUN3ME2yMlA5OyEQvF2= MVOyN|k1OjB7NR?=
ARPE19 Mlz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzEUXNQ M{my[2lEPTB;MkSuN|gh|ryP NHjocpMzOzV|MUmyNS=>
HEK293 NIrkNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfNVIhFVVOR NFzocHFKSzVyPUiuOlch|ryP MmfrNlM2OzF7MkG=
KCNR M{D5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnGU4pFVVOR NEPCOlhKSzVyPUCuOFYh|ryP Mk[4NlM2OzF7MkG=
SY5Y M1y3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXEUXNQ MWPJR|UxRTBwM{[g{txO NX22WGVqOjN3M{G5NlE>
BE2 M4\Edmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfwW2l6TE2VTx?= M4nqNmlEPTB;MD63NUDPxE1? NFSyb|UzOzV|MUmyNS=>
AS Ml\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfoO3VpTE2VTx?= MkXnTWM2OD1zLkWzJO69VQ>? MYmyN|U{OTl{MR?=
NGP MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnEUXNQ NETBXIRKSzVyPUCuOVYh|ryP M2P2bFI{PTNzOUKx
IMR32 MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni2SG1UVw>? MoHMTWM2OD1yLk[2JO69VQ>? MkHsNlM2OzF7MkG=
LAN5 NYTEcVd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\RSmROW09? NGTOeYZKSzVyPUGuNFQh|ryP NIK4cIozOzV|MUmyNS=>
RH18 NHjMfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLtUnN{TE2VTx?= NITXc|dKSzVyPUGuOFIh|ryP NVzpUItDOjN3M{G5NlE>
RH30 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfEUXNQ NWC4dXhWUUN3ME2xMlI2KM7:TR?= M1K3WFI{PTNzOUKx
RH17 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe4PIo{TE2VTx?= MUPJR|UxRTJwNUGg{txO NV;x[XlROjN3M{G5NlE>
RH28 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVT6TIg1TE2VTx?= NIHBfVJKSzVyPUSuNlgh|ryP MoDnNlM2OzF7MkG=
RH36 M160bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITZN5JFVVOR NIPGbGFKSzVyPUWuN|ch|ryP NUX0bWxHOjN3M{G5NlE>
RH41 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\0SG1UVw>? MUXJR|UxRTBwNEig{txO M3XvXlI{PTNzOUKx
RD MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnmNIh[TE2VTx?= NIfPdG5KSzVyPUSuN|Ih|ryP NIX4NGozOzV|MUmyNS=>
TC32 M3X2XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjEUXNQ NYPl[2RFUUN3ME2zMlg2KM7:TR?= MWqyN|U{OTl{MR?=
TC71 NFj6THpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTDRY8zTE2VTx?= NHrXXGNKSzVyPUSuN|Mh|ryP NFrleJIzOzV|MUmyNS=>
KCNR NFrqUFVCeG:ydH;zbZMhSXO|YYm= MUewMlUwOS5yL{KuOUDPxE1? M1GySFI1KGh? NFLV[GtFVVOR NIThfGZqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 MlPTNlM2OzF7MkG=
SY5Y Ml3DRZBweHSxc3nzJGF{e2G7 NWLLVVdTOC53L{GuNE8zNjVizszN MkXDNlQhcA>? Mn7SSG1UVw>? NInWb2tqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 NGrISVgzOzV|MUmyNS=>
Rh18 M4HMXmFxd3C2b4Ppd{BCe3OjeR?= MWiwMlUwOS5yL{KuOUDPxE1? MlXPNlQhcA>? M17GeWROW09? MWXpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NFLUeZAzOzV|MUmyNS=>
TC32 NWXSZoV5SXCxcITvd4l{KEG|c3H5 M{jVNlAvPS9zLkCvNk42KM7:TR?= MorENlQhcA>? NV;lWnk{TE2VTx?= MoP5bY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= MX2yN|U{OTl{MR?=
KCNR M2DZfWZ2dmO2aX;uJGF{e2G7 Mn[zNE42NzFwMD:yMlUwPSEQvF2= NHfGfYMzPCCq MnLqSG1UVw>? MmrybY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= NFnzd4ozOzV|MUmyNS=>
SY5Y MnTUSpVv[3Srb36gRZN{[Xl? NVnMU5doOC53L{GuNE8zNjVxNTFOwG0> M2\TPVI1KGh? MXnEUXNQ M1;GUYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u M4HiblI{PTNzOUKx
Rh18 MUDGeY5kfGmxbjDBd5NigQ>? NUXnPHFGOC53L{GuNE8zNjVxNTFOwG0> MkXJNlQhcA>? MV;EUXNQ NFjNWI9qdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MUiyN|U{OTl{MR?=
TC32 M1LT[2Z2dmO2aX;uJGF{e2G7 M17STlAvPS9zLkCvNk42NzVizszN MmGyNlQhcA>? M{HLd2ROW09? M{TEZYlvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NUS5TY91OjN3M{G5NlE>
TPC-1 Mo[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqxJOK2VQ>? MUSwMVQh\A>? NIrnRnJFVVOR M{DURYlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? MoTKNlMxPTZ2OUm=
MZ-CRC1  NUf2XJI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXIbY5KOSEEtV2= M4\E[FAuPSCm MX3EUXNQ NGHaRXZqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MUCyN|A2PjR7OR?=
TT  Mk[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuxJOK2VQ>? MknVNE01KGR? NE\4Um1FVVOR NGr3NGFqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 M2\BcVI{ODV4NEm5
TPC-1 NWLBS49zTnWwY4Tpc44hSXO|YYm= MX2xJOK2VQ>? M4rpZVczKGh? MWfEUXNQ MXLpcoR2[2W|IFexJIJtd2OtYXfl NFv1b4UzOzB3NkS5PS=>
MZ-CRC1  NVTOb3hpTnWwY4Tpc44hSXO|YYm= M4ntR|EhyrWP MlXpO|IhcA>? MofiSG1UVw>? NULRTY4xcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MYSyN|A2PjR7OR?=
TT  NVPXdIF5TnWwY4Tpc44hSXO|YYm= MkDINUDDvU1? Mo\RO|IhcA>? M1LGbmROW09? NVPuUZJjcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MorDNlMxPTZ2OUm=
MZ-CRC1  NX3LeINySXCxcITvd4l{KEG|c3H5 M4S0fVEhyrWP NEfO[Xo1QCCq NUC0S45zTE2VTx?= M1LwRolv\HWlZYOgZZBweHSxc3nz NE[4[4ozOzB3NkS5PS=>
TT  MY\BdI9xfG:|aYOgRZN{[Xl? NF7zWIIyKML3TR?= NWrs[GVnPDhiaB?= MVnEUXNQ Ml7TbY5lfWOnczDhdI9xfG:|aYO= MnvvNlMxPTZ2OUm=
HD-LM2 NILGXXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OwPFcz6oDLaB?= NXPJWmJQTE2VTx?= NX[5dHp5UUN3ME23Mlg1PCEQvF2= NVXQTXR4OjJ6MkmwPVQ>
L-428 NX\pWW1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TTUlcz6oDLaB?= M2D0dWROW09? M3u3eWlEPTB;Nz65OFch|ryP MYiyNlgzQTB7NB?=
KM-H2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TQSVcz6oDLaB?= Mn;sSG1UVw>? NHrvfIRKSzVyPUGuN|A5KM7:TR?= MlSwNlI5OjlyOUS=
L-540 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXi3NwKBkWh? NUPUd4ppTE2VTx?= NE\2cY9KSzVyPUiuNlE3KM7:TR?= MYiyNlgzQTB7NB?=
HD-LM2 NIHQXnlHfW6ldHnvckBCe3OjeR?= NIHLbHAxNjFxMD61M|EwPSEQvF2= MV63NwKBkWh? NXK1b2N2TE2VTx?= NV3TVZZrcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NUe4d4pqOjJ6MkmwPVQ>
L-428 MX;GeY5kfGmxbjDBd5NigQ>? NX3s[5ZbOC5zL{CuOU8yNzVizszN MVu3NwKBkWh? MUHEUXNQ MYPpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NHrUSWwzOjh{OUC5OC=>
KM-H2 Ml\qSpVv[3Srb36gRZN{[Xl? NFT4N24xNjFxMD61M|EwPSEQvF2= MVK3NwKBkWh? MnLXSG1UVw>? NHT1coNqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NYHlbnJ7OjJ6MkmwPVQ>
L-540 MXrGeY5kfGmxbjDBd5NigQ>? NUHveIJ1OC5zL{CuOU8yNzVizszN NFzYbnY4OuLCiXi= M2TROmROW09? MUHpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> MUiyNlgzQTB7NB?=
HD-LM2 NXfxWo0xSXCxcITvd4l{KEG|c3H5 NXLROI5oOS93IN88US=> NYLQUHFqPzMkgJno NGLSWWFFVVOR NIrkT3JqdmS3Y3XzJIFxd3C2b4Ppdy=> M2P3U|IzQDJ7MEm0
L-428 NGXG[2dCeG:ydH;zbZMhSXO|YYm= NHzCTZYyNzVizszN M{\0S|cz6oDLaB?= NVXqTYQ3TE2VTx?= M3jRUolv\HWlZYOgZZBweHSxc3nz MYKyNlgzQTB7NB?=
KM-H2 NELDWYRCeG:ydH;zbZMhSXO|YYm= MlraNU82KM7:TR?= NUnIcGY2PzMkgJno NVrWWHN7TE2VTx?= MUDpcoR2[2W|IHHwc5B1d3Orcx?= NILpSWEzOjh{OUC5OC=>
L-540 MV7BdI9xfG:|aYOgRZN{[Xl? NGnxc5YyNzVizszN M3SxNFcz6oDLaB?= NULWOnFJTE2VTx?= MkHybY5lfWOnczDhdI9xfG:|aYO= MlLFNlI5OjlyOUS=
U251-MG NFT5eYRHfW6ldHnvckBCe3OjeR?= MVexJOK2VQ>? NGPyWo4xNTF4IHi= MVnpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> Mn;pNlIxOjd4OUG=
U87-MG NFT2XYpHfW6ldHnvckBCe3OjeR?= NYj6TZU3OSEEtV2= NXvqdFROOC1zNjDo MUfpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MXqyNlAzPzZ7MR?=
4C8 MX\GeY5kfGmxbjDBd5NigQ>? M1zoRlEhyrWP NEnSenUxNTF4IHi= Mn7xbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v NVnONmxZOjJyMke2PVE>
U251-MG NVizN2JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPYNU8yOCEEtV2= NXfUXphoOjRxNEivO|IhcA>? MVvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NVPmcG5lOjJyMke2PVE>
U87-MG NVfjb2JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXOwN|ZyOS9zMDFCuW0> NGTGWJQzPC92OD:3NkBp NH;uOItqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? NUi5RXZPOjJyMke2PVE>
4C8 NYG2R4xjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT3codlOS9zMDFCuW0> MXmyOE81QC95MjDo NFT2dG5qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MYSyNlAzPzZ7MR?=
U266 M3rMRmFxd3C2b4Ppd{BCe3OjeR?= Mm\ENE42NTJizszN NXT6NG9SPDhxN{KgbC=> M3\RVolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MUCyNVE3PDVzNx?=
Kms.11 NHjZdIdCeG:ydH;zbZMhSXO|YYm= MWCwMlUuOiEQvF2= Mmn5OFgwPzJiaB?= NYHpd3dTcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MUSyNVE3PDVzNx?=
8226 NGXSSXpCeG:ydH;zbZMhSXO|YYm= NYrqRWJ{OC53LUKg{txO NUTqdHE6PDhxN{KgbC=> NVTIfY9{cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M2j3elIyOTZ2NUG3

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
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

Related Antibodies

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
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID