AZD1480 化学構造
分子量: 348.77

高品質保証

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Quality Control & MSDS

製品説明

  • Compare JAK Inhibitors
    JAK製品生物活性の比較
  • 研究分野
  • AZD1480のメカニズム

製品の説明

生物活性

製品説明 AZD1480は、JAK1とJAK2の新しいATP競争的阻害剤で、IC50がそれぞれ 1.3 nM と 0.26 nMです。
ターゲット JAK2
IC50 0.26 nM [1]
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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SW620 MnzhSpVv[3Srb36gRZN{[Xl? MojUOUDPxE1? NH7meoU1QCCq M{fNSWROW09? MWricI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= NEjDOIYzPTl3NEm3OC=>
LoVo  MWjGeY5kfGmxbjDBd5NigQ>? NFnqW4E2KM7:TR?= NXe2bpg{PDhiaB?= NEH6blNFVVOR MY\icI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= MmDpNlU6PTR7N{S=
HN5 NGS3ZXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTrcI44OiCq M3;jfmVEPTB;Mz64NUDDuSBzLkm5JO69VQ>? MXiyOVgyODBzMB?=
Cal33 NEnNfIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq5bmR{PzJiaB?= NFvsNFFGSzVyPUOuN|chyrFiMD63OUDPxE1? MoXHNlU5OTByMUC=
UM-22B MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zORlczKGh? MXrFR|UxRTJwNk[gxtEhOC5{NDFOwG0> MnLoNlU5OTByMUC=
686LN M3fHWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWG3NkBp MWnFR|UxRTJwMEWgxtEhOS5|MzFOwG0> M3rMflI2QDFyMEGw
UM SCC-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVq3NkBp M2ricWVEPTB;MT62O{DDuSByLkSyJO69VQ>? M2DIRVI2QDFyMEGw
UM-22A MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi3NkBp NUK0VIxZTUN3ME2xMlMzKMLzIECuN|kh|ryP NYfkVI5yOjV6MUCwNVA>
OSC19 M3rlfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVO3NkBp NUjpZ3pwTUN3ME2xMlI3KMLzIECuNlAh|ryP NYHCSXl{OjV6MUCwNVA>
PCI-52 NVTwWI84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[4O|IhcA>? MY\FR|UxRTFwMECgxtEhOC5yOTFOwG0> NUjKPFJDOjV6MUCwNVA>
PCI-15B NUHhPGlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HlWFczKGh? NG\nVoNGSzVyPUCuPVkhyrFiMT63OEDPxE1? M2LPPVI2QDFyMEGw
UMSCC-1 M17hNGZ2dmO2aX;uJGF{e2G7 NVrDTIF1OC5yMEC1MVEvPiEQvF2= NUDYXVA1OjRiaB?= NUnRNpk6[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWrRR41GOjV6MUCwNVA>
Cal33 MVnGeY5kfGmxbjDBd5NigQ>? NH3TfXgxNjByMEWtN{45KM7:TR?= MVOyOEBp NXH6NWU5[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXvDbWN1OjV6MUCwNVA>
HH5 NVzRT4xFTnWwY4Tpc44hSXO|YYm= M3PhflAvODByNT2zMlgh|ryP M2TvUFI1KGh? M1m2dYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX[yOVgyODBzMB?=
UM-22A MlPqSpVv[3Srb36gRZN{[Xl? M1XWZ|AvODByNT2xMlYh|ryP NGfhdZYzPCCq M4nUNYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFvwdHEzPThzMECxNC=>
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OVCAR-8 NV\jWXJUTnWwY4Tpc44hSXO|YYm= MkDYNE4xPS1zMDFOwG0> NEnJcHkzPCCq M4XO[2ROW00EoB?= NH7wfHpz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> NYXuRXdyOjV4NE[wNVU>
MOVCAR-5447 NI\OU2RHfW6ldHnvckBCe3OjeR?= MX6wMlA2NTFyIN88US=> M37IU|I1KGh? MkHkSG1UV8Li MoHOdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NHS0WFUzPTZ2NkCxOS=>
MOVCAR-5009 NVfoNoJmTnWwY4Tpc44hSXO|YYm= NFvVNXMxNjB3LUGwJO69VQ>? NYPzfZBlOjRiaB?= NWHYOYpDTE2VT9Mg NWrUbVFWemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> M4HpelI2PjR4MEG1
A1847 NFfKTGdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIDORXcxNjB3LUGwJO69VQ>? MnTDO|IhcA>? NUTPNI02TE2VTx?= MX\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGG2IITo[UBkd26lZYLueJJifGmxbjDv[kA2KM7:TR?= M2Ly[VI2PjR4MEG1
OVCAR-5 M{LoVWNmdGxiVnnhZoltcXS7IFHzd4F6 NFnlRpExNjB3LUGwJO69VQ>? M4HZT|czKGh? MVfEUXNQ MlH5doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= NWCzRmNNOjV4NE[wNVU>
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AKRSL NXK4T|NJS2WubDDWbYFjcWyrdImgRZN{[Xl? MWe3NkBp M1\WO2lEPTExvK6xNEDPxE1? MUKyOVUxPDZ|NR?=
PALJDL NFnqOWtE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlHyO|IhcA>? MWPJR|UxRTJwNDFOwG0> NGS2WZkzPTVyNE[zOS=>
MO4 NI\RdnVHfW6ldHnvckBCe3OjeR?= MlfwNE42NzFxNTFOwG0> MlfOOkBp NHnZdoVqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NEjI[oozPTF2OUWzOS=>
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GLC4 NF\rZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwN{mg{txO MVWyOFE2QDdyMR?=
H526 NUTZNW1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXRRYp5UUN3ME2zMlA5KM7:TR?= MYKyOFE2QDdyMR?=
H1173 NGr1S3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37pXGlEPTB;Mj6zPUDPxE1? Mm[5NlQyPTh5MEG=
DMS114 NVLTfIZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH24WYhKSzVyPUCuO|Mh|ryP NH7OXHMzPDF3OEewNS=>
NCI-N592 MlrmSpVv[3Srb36gRZN{[Xl? MVWwMlMwOS9|IN88US=> NInuSIszPCCq M1vaSIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Mn;2NlQyPTh5MEG=
GLC4 MYPGeY5kfGmxbjDBd5NigQ>? NWe3SJFHOC5|L{GvN{DPxE1? MUCyOEBp M4nW[Ylv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MWCyOFE2QDdyMR?=
NCI-H82 NEWwPZRHfW6ldHnvckBCe3OjeR?= M4O4SFAvOy9zL{Og{txO MXKyOEBp M3PsTYlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MViyOFE2QDdyMR?=
NCI-N592 MXjBdI9xfG:|aYOgRZN{[Xl? NH3DeXgxNjNxMT:zJO69VQ>? M2[yOVQ5KGh? MVzpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MV[yOFE2QDdyMR?=
GLC4 M3S0b2Fxd3C2b4Ppd{BCe3OjeR?= NGPhZmoxNjNxMT:zJO69VQ>? MVq0PEBp M{f3c4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? NVTEO5BWOjRzNUi3NFE>
NCI-H82 MXTBdI9xfG:|aYOgRZN{[Xl? MXewMlMwOS9|IN88US=> NFXPSGM1QCCq NUTCN5ZOcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= NV\PRXkzOjRzNUi3NFE>
CWR22Rv1  MVvBdI9xfG:|aYOgRZN{[Xl? MYXJR|UxRTBwNEiyJO69VQ>? M3zHNVI{QTR{MEm1
CWR22Pc NUX4b|c2SXCxcITvd4l{KEG|c3H5 NID4VWlKSzVyPUCuOFM5KM7:TR?= MXeyN|k1OjB7NR?=
PC-3 MlPNRZBweHSxc3nzJGF{e2G7 M3zDZ2lEPTB;MT63OVUh|ryP NV7UbIpNOjN7NEKwPVU>
DU145 NY\2ZWtmSXCxcITvd4l{KEG|c3H5 MUHJR|UxRTNwNUG3JO69VQ>? NGfuc2szOzl2MkC5OS=>
RC165N M{DmbWFxd3C2b4Ppd{BCe3OjeR?= MkS0TWM2OD1{LkC4N{DPxE1? NGTqVnozOzl2MkC5OS=>
ARPE19 NH;KO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjwTo1FVVOR M4Xqd2lEPTB;MkSuN|gh|ryP M331TVI{PTNzOUKx
HEK293 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fvOmROW09? MYLJR|UxRThwNkeg{txO M2GwTVI{PTNzOUKx
KCNR MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHqVZU3TE2VTx?= M1ryPWlEPTB;MD60OkDPxE1? MXWyN|U{OTl{MR?=
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NGP NXO5UG0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXEUXNQ MWHJR|UxRTBwNU[g{txO M3OwflI{PTNzOUKx
IMR32 MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[wSG1UVw>? MkLXTWM2OD1yLk[2JO69VQ>? M4LzN|I{PTNzOUKx
LAN5 NIjLPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFqwZmFFVVOR NIPVN2FKSzVyPUGuNFQh|ryP M{\aOFI{PTNzOUKx
RH18 MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:yUo5FVVOR MmmyTWM2OD1zLkSyJO69VQ>? NUPGeGlJOjN3M{G5NlE>
RH30 MknUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILSSopFVVOR NUfTTopQUUN3ME2xMlI2KM7:TR?= NULPVml6OjN3M{G5NlE>
RH17 M1HCbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L1Z2ROW09? MVTJR|UxRTJwNUGg{txO NXX0OI5FOjN3M{G5NlE>
RH28 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C0UGROW09? M2D5PWlEPTB;ND6yPEDPxE1? NIHOTnYzOzV|MUmyNS=>
RH36 M4jKVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK3WnJFVVOR M3uwUWlEPTB;NT6zO{DPxE1? M2\udlI{PTNzOUKx
RH41 Mmf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPEUXNQ M2DuPGlEPTB;MD60PEDPxE1? Mkm1NlM2OzF7MkG=
RD NYPpUmdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnEUXNQ MVzJR|UxRTRwM{Kg{txO M2OwRVI{PTNzOUKx
TC32 M{Lidmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\a[2ROW09? MlTrTWM2OD1|Lki1JO69VQ>? MkfBNlM2OzF7MkG=
TC71 M3TNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nnO2ROW09? M2PpZmlEPTB;ND6zN{DPxE1? NWfvVIJsOjN3M{G5NlE>
KCNR MWnBdI9xfG:|aYOgRZN{[Xl? Mn;GNE42NzFwMD:yMlUh|ryP NGrXb2ozPCCq NU\kOVBUTE2VTx?= MlXMbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NX;qe3p3OjN3M{G5NlE>
SY5Y NVjUS3NbSXCxcITvd4l{KEG|c3H5 NFnKPHYxNjVxMT6wM|IvPSEQvF2= MmHqNlQhcA>? NW\HPYZoTE2VTx?= MUfpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MVqyN|U{OTl{MR?=
Rh18 NY\4dVIxSXCxcITvd4l{KEG|c3H5 MWqwMlUwOS5yL{KuOUDPxE1? M1K5d|I1KGh? M{j3bmROW09? M1L1U4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MWeyN|U{OTl{MR?=
TC32 Mmq5RZBweHSxc3nzJGF{e2G7 NWC0O3VxOC53L{GuNE8zNjVizszN MoG3NlQhcA>? NEDMb21FVVOR MYPpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 NH3XfGwzOzV|MUmyNS=>
KCNR NIfZenhHfW6ldHnvckBCe3OjeR?= NELCTXYxNjVxMT6wM|IvPS93IN88US=> NVLIWmdROjRiaB?= NVzSTlNsTE2VTx?= NF\OfYdqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NHXnTpczOzV|MUmyNS=>
SY5Y NWS2NpRvTnWwY4Tpc44hSXO|YYm= MWGwMlUwOS5yL{KuOU82KM7:TR?= MoXKNlQhcA>? M1zpeWROW09? NEnNfVZqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> NF3EPZYzOzV|MUmyNS=>
Rh18 M1zrXGZ2dmO2aX;uJGF{e2G7 NIj6cFQxNjVxMT6wM|IvPS93IN88US=> MnPpNlQhcA>? MWTEUXNQ M1XKb4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u MVGyN|U{OTl{MR?=
TC32 NF75UHFHfW6ldHnvckBCe3OjeR?= NFHYWJgxNjVxMT6wM|IvPS93IN88US=> MYKyOEBp Mnz6SG1UVw>? MYfpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MofkNlM2OzF7MkG=
TPC-1 NYHkeWxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nHSVEhyrWP NEf1XXYxNTRiZB?= Mn7ySG1UVw>? NIDoemdqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAzKGRidILlZZRu\W62 NXzP[Yc6OjNyNU[0PVk>
MZ-CRC1  MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3CN5cyKML3TR?= NGfDPXAxNTViZB?= M1q2WGROW09? NVjS[ZF[cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= M4f0ZVI{ODV4NEm5
TT  NVHjb5NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LwZlEhyrWP MlLJNE01KGR? MX7EUXNQ NIrWZVNqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 MYSyN|A2PjR7OR?=
TPC-1 MoC2SpVv[3Srb36gRZN{[Xl? MkXXNUDDvU1? NEj2TJM4OiCq MVfEUXNQ NF7ZWlRqdmS3Y3XzJGcyKGKub3PrZYdm M2L5dlI{ODV4NEm5
MZ-CRC1  NI\QfHFHfW6ldHnvckBCe3OjeR?= NUX6RY9KOSEEtV2= MXy3NkBp MlnxSG1UVw>? NVvZWGYycW6mdXPld{BIOSCkbH;jb4Fo\Q>? NIPFZmwzOzB3NkS5PS=>
TT  NITrZYNHfW6ldHnvckBCe3OjeR?= MWqxJOK2VQ>? Ml62O|IhcA>? M3z4c2ROW09? NIfKcmtqdmS3Y3XzJGcyKGKub3PrZYdm MWiyN|A2PjR7OR?=
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TT  M{XlPGFxd3C2b4Ppd{BCe3OjeR?= M4q5UFEhyrWP M2nJW|Q5KGh? Mm\3SG1UVw>? MWTpcoR2[2W|IHHwc5B1d3Orcx?= MnvpNlMxPTZ2OUm=
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HD-LM2 MnKzSpVv[3Srb36gRZN{[Xl? MUewMlEwOC53L{GvOUDPxE1? M{nJOVcz6oDLaB?= NV7CZ5R1TE2VTx?= MoLYbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NXrtR|ZyOjJ6MkmwPVQ>
L-428 M1\uSWZ2dmO2aX;uJGF{e2G7 NEPqOIoxNjFxMD61M|EwPSEQvF2= NEnMOZY4OuLCiXi= NIrNNW5FVVOR M17YVIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v M{TMV|IzQDJ7MEm0
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... 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]
臨床試験 AZD1480 is currently in Phase I clinical trials in Asian Patients With Advanced Solid Malignancies and Asian Patients With Advanced Hepatocellular Carcinoma (HCC)
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [5]

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]

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.

動物実験: [4]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download AZD1480 SDF
分子量 348.77
化学式

C14H14ClFN8

CAS No. 935666-88-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 69 mg/mL warming (197.83 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine

文献中の引用 (13)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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