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 M2\jdGZ2dmO2aX;uJGF{e2G7 M3OzVFUh|ryP NXOxZ5hqPDhiaB?= MWXEUXNQ NGDPNmFjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> M13vNVI2QTV2OUe0
LoVo  MlPhSpVv[3Srb36gRZN{[Xl? MU[1JO69VQ>? NVrqNIVGPDhiaB?= MWjEUXNQ NFjqZVdjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NXfv[2RJOjV7NUS5O|Q>
HN5 MoqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\HO|IhcA>? MkLrSWM2OD1|LkixJOKyKDFwOUmg{txO M3X1elI2QDFyMEGw
Cal33 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[3NkBp NHTN[IZGSzVyPUOuN|chyrFiMD63OUDPxE1? MmX3NlU5OTByMUC=
UM-22B MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfTXVBRPzJiaB?= M2D1SGVEPTB;Mj62OkDDuSByLkK0JO69VQ>? M3SzeFI2QDFyMEGw
686LN MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX30c5BZPzJiaB?= MUfFR|UxRTJwMEWgxtEhOS5|MzFOwG0> NIXxO3YzPThzMECxNC=>
UM SCC-1 NIjmTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDP[nJ2PzJiaB?= MnTzSWM2OD1zLk[3JOKyKDBwNEKg{txO NXTwPYg5OjV6MUCwNVA>
UM-22A M2\odWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDVOIM4OiCq M13BfWVEPTB;MT6zNkDDuSByLkO5JO69VQ>? MnfRNlU5OTByMUC=
OSC19 MlzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi5O|IhcA>? MXzFR|UxRTFwMk[gxtEhOC5{MDFOwG0> NULDUXNPOjV6MUCwNVA>
PCI-52 M1i5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XKTFczKGh? NWK4bIJNTUN3ME2xMlAxKMLzIECuNFkh|ryP MYWyOVgyODBzMB?=
PCI-15B Mlv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2n3NVczKGh? NIPHUlhGSzVyPUCuPVkhyrFiMT63OEDPxE1? MXGyOVgyODBzMB?=
UMSCC-1 Mo\FSpVv[3Srb36gRZN{[Xl? NGHBdIsxNjByMEWtNU43KM7:TR?= NWT0Rnd5OjRiaB?= M4jqVoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGrKcYgzPThzMECxNC=>
Cal33 NHLMcpVHfW6ldHnvckBCe3OjeR?= MVWwMlAxODVvMz64JO69VQ>? MUOyOEBp NVjPWYV[[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIHOTmozPThzMECxNC=>
HH5 NHq4b5JHfW6ldHnvckBCe3OjeR?= MYWwMlAxODVvMz64JO69VQ>? NEixbJYzPCCq NV32O|NR[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVr6Om9xOjV6MUCwNVA>
UM-22A Ml;oSpVv[3Srb36gRZN{[Xl? MYOwMlAxODVvMT62JO69VQ>? NYPHWFg2OjRiaB?= NYf6ZY15[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUX3[XVROjV6MUCwNVA>
A1847 M1TWN2Z2dmO2aX;uJGF{e2G7 NHjwZ5MxNjB3LUGwJO69VQ>? M3\tVlI1KGh? MnTuSG1UV8Li NF\sVYVz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NY\iV|NwOjV4NE[wNVU>
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MOVCAR-5447 NVraW|hoTnWwY4Tpc44hSXO|YYm= NVqyV4NXOC5yNT2xNEDPxE1? NHTIb5EzPCCq NVG1NIVUTE2VT9Mg MVvy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MW[yOVY1PjBzNR?=
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A1847 NUjEcGtqS2WubDDWbYFjcWyrdImgRZN{[Xl? NU\mU|VTOC5yNT2xNEDPxE1? NX;lU4hPPzJiaB?= MnX6SG1UVw>? Mk\5doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NX3oO2VLOjV4NE[wNVU>
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OVCAR-8  NIPl[nVCeG:ydH;zbZMhSXO|YYm= NWnQNJVOOC53L{GvOUDPxE1? M1LQd|Q5KGh? M4PpeGROW09? MmG0bY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= NH3FO5MzPTZ2NkCxOS=>
AKRSL MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoHNO|IhcA>? Moq2TWM2OO,:nkGwJO69VQ>? NXvhUFdLOjV3MES2N|U>
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MO4 MVTGeY5kfGmxbjDBd5NigQ>? MoDBNE42NzFxNTFOwG0> MUm2JIg> M3;ycIlvcGmkaYTzJHAuW1SDVEOg[ZhxemW|c3nvcuKh MXiyOVE1QTV|NR?=
DU145  NHnBVndHfW6ldHnvckBCe3OjeR?= NVK2VXBUOC1{MECgcm0> NV3m[XE1OSCqwrC= MU\zeZBxemW|c3XzJGlNNTZvYXP0bZZifGWmIGP0ZZQ{KGGwZDDFVmsyNzJic3nncoFtcW6p NWPwO3NoOjR3N{e5OFI>
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NCI-N592 NX\yfJVZTnWwY4Tpc44hSXO|YYm= M{TrNVAvOy9zL{Og{txO M{TkUFI1KGh? MYfpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> MXuyOFE2QDdyMR?=
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NCI-N592 NIPZRWNCeG:ydH;zbZMhSXO|YYm= Mkn4NE4{NzFxMzFOwG0> NX7OS3poPDhiaB?= NHz5RoJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| MmHxNlQyPTh5MEG=
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NGP MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[zNVBFVVOR NVHSVVJEUUN3ME2wMlU3KM7:TR?= NYfoVG9ROjN3M{G5NlE>
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LAN5 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInNfGJFVVOR MUfJR|UxRTFwMESg{txO NGHqbnAzOzV|MUmyNS=>
RH18 NVTWUINYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XZPGROW09? MXTJR|UxRTFwNEKg{txO MXyyN|U{OTl{MR?=
RH30 NFSweWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\EUXNQ M4\M[mlEPTB;MT6yOUDPxE1? MVWyN|U{OTl{MR?=
RH17 NHLuT|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXRSG1UVw>? M3yySGlEPTB;Mj61NUDPxE1? NVnoc25sOjN3M{G5NlE>
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RH36 NX;4WVN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrEUXNQ NVi3SHExUUN3ME21MlM4KM7:TR?= MlP4NlM2OzF7MkG=
RH41 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnzfWlFVVOR NVLNdVdiUUN3ME2wMlQ5KM7:TR?= M3zGRVI{PTNzOUKx
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TC32 M4jEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XabWROW09? MYTJR|UxRTNwOEWg{txO NELuflMzOzV|MUmyNS=>
TC71 NVjkemtiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDGSG1UVw>? MYnJR|UxRTRwM{Og{txO MYiyN|U{OTl{MR?=
KCNR M1PmUmFxd3C2b4Ppd{BCe3OjeR?= MoS5NE42NzFwMD:yMlUh|ryP MXmyOEBp NXPuOYlbTE2VTx?= NXfJN5RIcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> MV6yN|U{OTl{MR?=
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TC32 NHXnRmJHfW6ldHnvckBCe3OjeR?= MV2wMlUwOS5yL{KuOU82KM7:TR?= NIDScVkzPCCq MWDEUXNQ MmPMbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= MX[yN|U{OTl{MR?=
TPC-1 M1HHTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3GRnMyKML3TR?= NGe1[nYxNTRiZB?= NHuwS|BFVVOR NUn0Xo1LcW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOiCmIITy[YF1dWWwdB?= M2TFbVI{ODV4NEm5
MZ-CRC1  NEPaXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnsUnVKOSEEtV2= M2XCUlAuPSCm M3fRfWROW09? MX3pcohq[mm2czDj[YxtKGe{b4f0bEBi\nSncjCxJIQhfHKnYYTt[Y51 MVyyN|A2PjR7OR?=
TT  MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjLWoZEOSEEtV2= NGfCSVIxNTRiZB?= NFGxcYtFVVOR NY\COY44cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= M1\pWVI{ODV4NEm5
TPC-1 M2jBbWZ2dmO2aX;uJGF{e2G7 M3P6NFEhyrWP M4exVFczKGh? MlvnSG1UVw>? MmPsbY5lfWOnczDHNUBjdG:la3Hn[S=> NGjtfWozOzB3NkS5PS=>
MZ-CRC1  MVHGeY5kfGmxbjDBd5NigQ>? MoDtNUDDvU1? Mo\uO|IhcA>? M1Hne2ROW09? NF36XmdqdmS3Y3XzJGcyKGKub3PrZYdm Mn35NlMxPTZ2OUm=
TT  NID1bJNHfW6ldHnvckBCe3OjeR?= NYKxdm9NOSEEtV2= M4LCVlczKGh? MXPEUXNQ MUXpcoR2[2W|IFexJIJtd2OtYXfl M{LqbFI{ODV4NEm5
MZ-CRC1  NUTiZnlsSXCxcITvd4l{KEG|c3H5 MkLTNUDDvU1? MUW0PEBp NF3ZfnNFVVOR NXvOUm5LcW6mdXPld{BieG:ydH;zbZM> NFfH[mkzOzB3NkS5PS=>
TT  MmDuRZBweHSxc3nzJGF{e2G7 MnHUNUDDvU1? NVzxSJpiPDhiaB?= NXPhUGlYTE2VTx?= NH[wNlhqdmS3Y3XzJIFxd3C2b4Ppdy=> M3zh[|I{ODV4NEm5
HD-LM2 M3OyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fnfVcz6oDLaB?= MWHEUXNQ MlTUTWM2OD15Lki0OEDPxE1? NXrMVYFzOjJ6MkmwPVQ>
L-428 NEDRd2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fVbVcz6oDLaB?= NULEbmpKTE2VTx?= MnHjTWM2OD15Lkm0O{DPxE1? M33JcFIzQDJ7MEm0
KM-H2 NY[0WGFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PSelcz6oDLaB?= NH7tZ5lFVVOR MVnJR|UxRTFwM{C4JO69VQ>? MoTKNlI5OjlyOUS=
L-540 NXPqN21zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LmVVcz6oDLaB?= NX;GSW9ZTE2VTx?= MUfJR|UxRThwMkG2JO69VQ>? NV7Vc4NKOjJ6MkmwPVQ>
HD-LM2 NEW3RZVHfW6ldHnvckBCe3OjeR?= M{Loe|AvOS9yLkWvNU82KM7:TR?= NIPFfIU4OuLCiXi= MULEUXNQ M3\mPYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MoDWNlI5OjlyOUS=
L-428 MXfGeY5kfGmxbjDBd5NigQ>? NGjPeZQxNjFxMD61M|EwPSEQvF2= NGfOdGw4OuLCiXi= NG\MPWhFVVOR MUHpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> M4i1XlIzQDJ7MEm0
KM-H2 MmnxSpVv[3Srb36gRZN{[Xl? NXWycnF4OC5zL{CuOU8yNzVizszN NFLKdIw4OuLCiXi= NWXFTJFHTE2VTx?= NX;0UFB6cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NUfkNG1ROjJ6MkmwPVQ>
L-540 NXvTfHY5TnWwY4Tpc44hSXO|YYm= NF:0S3cxNjFxMD61M|EwPSEQvF2= NWPRTXZ5PzMkgJno M4DQV2ROW09? M{HoVYlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NYDSU41SOjJ6MkmwPVQ>
HD-LM2 NHrO[GVCeG:ydH;zbZMhSXO|YYm= M1;PfFEwPSEQvF2= M{P5bFcz6oDLaB?= Mo\zSG1UVw>? MnjSbY5lfWOnczDhdI9xfG:|aYO= MVuyNlgzQTB7NB?=
L-428 NEj1V41CeG:ydH;zbZMhSXO|YYm= MWCxM|Uh|ryP MnS2O|LjiImq M4nQbmROW09? MnHObY5lfWOnczDhdI9xfG:|aYO= M4nCV|IzQDJ7MEm0
KM-H2 M3z6UGFxd3C2b4Ppd{BCe3OjeR?= M{X5S|EwPSEQvF2= NV3qU4ZVPzMkgJno Mlv5SG1UVw>? NIjZSmVqdmS3Y3XzJIFxd3C2b4Ppdy=> MoHnNlI5OjlyOUS=
L-540 Mn;YRZBweHSxc3nzJGF{e2G7 MkHENU82KM7:TR?= MnrBO|LjiImq MYrEUXNQ MmW3bY5lfWOnczDhdI9xfG:|aYO= Mly3NlI5OjlyOUS=
U251-MG NX\YTHMyTnWwY4Tpc44hSXO|YYm= MXyxJOK2VQ>? MlHsNE0yPiCq M{DKc4lvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NUWzdXNIOjJyMke2PVE>
U87-MG MWfGeY5kfGmxbjDBd5NigQ>? MnjYNUDDvU1? MXSwMVE3KGh? NEewbJBqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MUeyNlAzPzZ7MR?=
4C8 MmHLSpVv[3Srb36gRZN{[Xl? NFvRPWYyKML3TR?= NGHQPWcxNTF4IHi= M3nHeolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT|Ih[WO2aY\heIlwdg>? NIHtfVAzOjB{N{[5NS=>
U251-MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPkc4lnOS9zMDFCuW0> NHfvNIMzPC92OD:3NkBp MUfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NX[4ZWtFOjJyMke2PVE>
U87-MG NF;Ub4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDxUJZjOS9zMDFCuW0> MkLSNlQwPDhxN{KgbC=> NUPjO3lVcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MnrkNlIxOjd4OUG=
4C8 NYPxPJlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrMPZd[OS9zMDFCuW0> Mn3hNlQwPDhxN{KgbC=> NGmwUY5qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? M3:yUFIzODJ5Nkmx
U266 NHPNXopCeG:ydH;zbZMhSXO|YYm= MWKwMlUuOiEQvF2= NIjDW|A1QC95MjDo NHntfXBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NWj2NYVMOjFzNkS1NVc>
Kms.11 M3;5UmFxd3C2b4Ppd{BCe3OjeR?= NW\UXFlDOC53LUKg{txO MnziOFgwPzJiaB?= NFvzO2pqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4\4VFIyOTZ2NUG3
8226 MXPBdI9xfG:|aYOgRZN{[Xl? MkTSNE42NTJizszN NXnOeHRiPDhxN{KgbC=> NVPqNWZPcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> Mmr2NlEyPjR3MUe=

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
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
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
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

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID