AZD1480

Catalog No.S2162

AZD1480 Chemical Structure

Molecular Weight(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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 100 In stock
USD 170 In stock
USD 570 In stock
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4 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Description 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.
Targets
JAK2 [1]
(Cell-free assay)
0.26 nM
In vitro

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 MYLGeY5kfGmxbjDBd5NigQ>? MVu1JO69VQ>? M1TzOFQ5KGh? NYr0OWNZTE2VTx?= MmXrZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n NYXCfXBbOjV7NUS5O|Q>
LoVo  MnvYSpVv[3Srb36gRZN{[Xl? NIrud5k2KM7:TR?= NF7HdZU1QCCq MUPEUXNQ MYXicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= MmHONlU6PTR7N{S=
HN5 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXMV3Q4OiCq NWj6W2ZyTUN3ME2zMlgyKMLzIEGuPVkh|ryP MoruNlU5OTByMUC=
Cal33 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\JO|IhcA>? NXr5RYxNTUN3ME2zMlM4KMLzIECuO|Uh|ryP NFv0c5QzPThzMECxNC=>
UM-22B MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\xe444OiCq M{S2fWVEPTB;Mj62OkDDuSByLkK0JO69VQ>? NX62NIJkOjV6MUCwNVA>
686LN Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm3NkBp NFjBTopGSzVyPUKuNFUhyrFiMT6zN{DPxE1? MlTjNlU5OTByMUC=
UM SCC-1 MnrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jiTFczKGh? MnLDSWM2OD1zLk[3JOKyKDBwNEKg{txO M3jpZlI2QDFyMEGw
UM-22A M2jzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGG0TFk4OiCq NV;TS|VLTUN3ME2xMlMzKMLzIECuN|kh|ryP M{DxcFI2QDFyMEGw
OSC19 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEKwXFk4OiCq MljCSWM2OD1zLkK2JOKyKDBwMkCg{txO M4\4d|I2QDFyMEGw
PCI-52 NEXoco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PsRlczKGh? NYfve2w2TUN3ME2xMlAxKMLzIECuNFkh|ryP MmLUNlU5OTByMUC=
PCI-15B NXfGdFJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PSbVczKGh? M{jUVmVEPTB;MD65PUDDuSBzLke0JO69VQ>? M{XublI2QDFyMEGw
UMSCC-1 M2TMTGZ2dmO2aX;uJGF{e2G7 MoHENE4xODB3LUGuOkDPxE1? NF\CepgzPCCq MYLhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFz0ZZIzPThzMECxNC=>
Cal33 NGK0dXVHfW6ldHnvckBCe3OjeR?= M{nROFAvODByNT2zMlgh|ryP M4T3dVI1KGh? NWDmNIY{[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR|VInyO|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVHhSFI5OjV6MUCwNVA>
HH5 MoDzSpVv[3Srb36gRZN{[Xl? NUfX[lVZOC5yMEC1MVMvQCEQvF2= NWDqOZFVOjRiaB?= MVThZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NUDyT5hLOjV6MUCwNVA>
UM-22A Ml3ZSpVv[3Srb36gRZN{[Xl? M33QUlAvODByNT2xMlYh|ryP NI\z[WMzPCCq M1PT[4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2L0WFI2QDFyMEGw
A1847 NF[xS5ZHfW6ldHnvckBCe3OjeR?= NUPOWY1POC5yNT2xNEDPxE1? NGft[lkzPCCq M4XqPGROW00EoB?= MnvOdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MnPxNlU3PDZyMUW=
OVCAR-5 MWLGeY5kfGmxbjDBd5NigQ>? MX[wMlA2NTFyIN88US=> NHTocIszPCCq MYnEUXNQyqB? Mk\KdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= NGXIXYYzPTZ2NkCxOS=>
OVCAR-8 NFuydG9HfW6ldHnvckBCe3OjeR?= MoLLNE4xPS1zMDFOwG0> MmjENlQhcA>? M3P3SWROW00EoB?= NFy1U|Nz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MV2yOVY1PjBzNR?=
MOVCAR-5447 NV:yVm9nTnWwY4Tpc44hSXO|YYm= NVPZbFBEOC5yNT2xNEDPxE1? NH3tWG4zPCCq NI\UXItFVVORwrC= MoTBdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= MYGyOVY1PjBzNR?=
MOVCAR-5009 M3e5dmZ2dmO2aX;uJGF{e2G7 MYSwMlA2NTFyIN88US=> M3PaWFI1KGh? NYLnUY1pTE2VT9Mg M{\OVJJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz NEPNcoQzPTZ2NkCxOS=>
A1847 MkSxR4VtdCCYaXHibYxqfHliQYPzZZk> M1\ENVAvODVvMUCg{txO MWq3NkBp NYHBOoltTE2VTx?= NXf1PYF2emWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> MWeyOVY1PjBzNR?=
OVCAR-5 Mo\5R4VtdCCYaXHibYxqfHliQYPzZZk> NFHQUGsxNjB3LUGwJO69VQ>? M2HVZVczKGh? NVPPdVg1TE2VTx?= NFr1SYhz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MV6yOVY1PjBzNR?=
OVCAR-8  MojJR4VtdCCYaXHibYxqfHliQYPzZZk> NHHIPW8xNjB3LUGwJO69VQ>? M4Phd|czKGh? NIPSUI9FVVOR M{Wxb5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MX[yOVY1PjBzNR?=
OVCAR-5  MnizRZBweHSxc3nzJGF{e2G7 NEK4UJYxNjVxMT:1JO69VQ>? MoLIOFghcA>? NFHxTHFFVVOR MnPybY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= NFvaVpMzPTZ2NkCxOS=>
OVCAR-8  Mlq1RZBweHSxc3nzJGF{e2G7 NGP2foExNjVxMT:1JO69VQ>? NUGzZ|h3PDhiaB?= M1PISGROW09? NXzyWYNHcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M1[zNFI2PjR4MEG1
AKRSL MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUj1RmZJPzJiaB?= MnvBTWM2OO,:nkGwJO69VQ>? NYHKUYpQOjV3MES2N|U>
PALJDL NXfsSnFkS2WubDDWbYFjcWyrdImgRZN{[Xl? NH\IPFI4OiCq MX7JR|UxRTJwNDFOwG0> NF75SJIzPTVyNE[zOS=>
MO4 MmSzSpVv[3Srb36gRZN{[Xl? MofaNE42NzFxNTFOwG0> NGnPcGg3KGh? NIH0e3lqdmirYnn0d{BRNVOWQWSzJIV5eHKnc4Ppc47DqA>? NX7KUmg5OjVzNEm1N|U>
DU145  MXnGeY5kfGmxbjDBd5NigQ>? MXGwMVIxOCCwTR?= MoH2NUBpyqB? MlTVd5VxeHKnc4Pld{BKVC14LXHjeIl3[XSnZDDTeIF1OyCjbnSgSXJMOS9{IIPp[45idGmwZx?= NFfxT|QzPDV5N{m0Ni=>
DU145  MoPMSpVv[3Srb36gRZN{[Xl? NFfEV5c5ODBibl2= MV:3NkBp NXTj[5RNe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 NH\WUJYzPDV5N{m0Ni=>
CWR22Rv1 M17zV2Z2dmO2aX;uJGF{e2G7 M3vPeVgxOCCwTR?= M4XMfVczKGh? MW\zeZBxemW|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl? Mkn0NlQ2Pzd7NEK=
N592 Mon1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfTToZKSzVyPUCuPFQh|ryP Mk\xNlQyPTh5MEG=
H82 NY\5N2k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnNXldDUUN3ME2xMlM4KM7:TR?= Mn;0NlQyPTh5MEG=
GLC4 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rZW2lEPTB;MT63PUDPxE1? M4rZVlI1OTV6N{Cx
H526 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPEWGhLUUN3ME2zMlA5KM7:TR?= NE\WWVkzPDF3OEewNS=>
H1173 M3e0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj5TWM2OD1{LkO5JO69VQ>? M{\SUFI1OTV6N{Cx
DMS114 NWHNWnZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3UTWM2OD1yLkezJO69VQ>? MmrJNlQyPTh5MEG=
NCI-N592 M1mx[2Z2dmO2aX;uJGF{e2G7 MVmwMlMwOS9|IN88US=> NVfyO|VJOjRiaB?= NWjLeoxocW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MUSyOFE2QDdyMR?=
GLC4 M2frU2Z2dmO2aX;uJGF{e2G7 MnXyNE4{NzFxMzFOwG0> MXWyOEBp Mn7ybY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NF32U2wzPDF3OEewNS=>
NCI-H82 Mlz6SpVv[3Srb36gRZN{[Xl? MmTxNE4{NzFxMzFOwG0> MlLGNlQhcA>? NF3aSVhqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? M3ridFI1OTV6N{Cx
NCI-N592 NGPhfFlCeG:ydH;zbZMhSXO|YYm= MYWwMlMwOS9|IN88US=> NVvPblhzPDhiaB?= MorJbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? M{m3UlI1OTV6N{Cx
GLC4 NYXqdmlQSXCxcITvd4l{KEG|c3H5 M1mzbVAvOy9zL{Og{txO NUDCbVh5PDhiaB?= MnrpbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? NFrGT4MzPDF3OEewNS=>
NCI-H82 MljnRZBweHSxc3nzJGF{e2G7 MXGwMlMwOS9|IN88US=> MYm0PEBp MkXtbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MkG2NlQyPTh5MEG=
CWR22Rv1  MmfrRZBweHSxc3nzJGF{e2G7 NY\uWGd6UUN3ME2wMlQ5OiEQvF2= MU[yN|k1OjB7NR?=
CWR22Pc MlK4RZBweHSxc3nzJGF{e2G7 NFPnR5hKSzVyPUCuOFM5KM7:TR?= M1HsTlI{QTR{MEm1
PC-3 MoD3RZBweHSxc3nzJGF{e2G7 NFPzbW9KSzVyPUGuO|U2KM7:TR?= M3LFbFI{QTR{MEm1
DU145 NG[4XXlCeG:ydH;zbZMhSXO|YYm= MYfJR|UxRTNwNUG3JO69VQ>? M3TCfFI{QTR{MEm1
RC165N MlfkRZBweHSxc3nzJGF{e2G7 NGTsUlVKSzVyPUKuNFg{KM7:TR?= M3P1OlI{QTR{MEm1
ARPE19 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjEUXNQ NHTnXHNKSzVyPUK0MlM5KM7:TR?= MUmyN|U{OTl{MR?=
HEK293 NUfQTJk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nF[2ROW09? NF;TS4NKSzVyPUiuOlch|ryP NX;tUlVUOjN3M{G5NlE>
KCNR MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXZW4U2TE2VTx?= NWjQ[2NUUUN3ME2wMlQ3KM7:TR?= NHLzdHEzOzV|MUmyNS=>
SY5Y M{TUUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzie|JFVVOR NXjydot2UUN3ME2wMlM3KM7:TR?= NXv3[ok6OjN3M{G5NlE>
BE2 MojPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzPN41FVVOR NYDCV2FuUUN3ME2wMlcyKM7:TR?= MXKyN|U{OTl{MR?=
AS MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\5UWROW09? M1jndGlEPTB;MT61N{DPxE1? NEjON4wzOzV|MUmyNS=>
NGP NYDHXGd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\jOnRJTE2VTx?= MmX1TWM2OD1yLkW2JO69VQ>? NXnDR|hwOjN3M{G5NlE>
IMR32 MnrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLlNId[TE2VTx?= M3n2VGlEPTB;MD62OkDPxE1? NUj4V2k6OjN3M{G5NlE>
LAN5 M2PxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXqSG1UVw>? M3;TUmlEPTB;MT6wOEDPxE1? NXO3[5YxOjN3M{G5NlE>
RH18 NVPjZZpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7mSVJFVVOR NWrOSpZwUUN3ME2xMlQzKM7:TR?= Moe1NlM2OzF7MkG=
RH30 MkHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPLe2tZTE2VTx?= M4nEPWlEPTB;MT6yOUDPxE1? MmG5NlM2OzF7MkG=
RH17 NF;TZ|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\ESG1UVw>? MWjJR|UxRTJwNUGg{txO Mnz1NlM2OzF7MkG=
RH28 M1zmRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHqzT2ZFVVOR MnrWTWM2OD12LkK4JO69VQ>? MX[yN|U{OTl{MR?=
RH36 M4XuTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33xW2ROW09? NX3CSmhjUUN3ME21MlM4KM7:TR?= M3j6clI{PTNzOUKx
RH41 NYSzNFdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S5PWROW09? NX7Kd4JkUUN3ME2wMlQ5KM7:TR?= MlHBNlM2OzF7MkG=
RD M2LvTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHeyOWJFVVOR M4\0[WlEPTB;ND6zNkDPxE1? NGnTSWszOzV|MUmyNS=>
TC32 M4Tr[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDaNY8xTE2VTx?= MWPJR|UxRTNwOEWg{txO MWSyN|U{OTl{MR?=
TC71 NF;SWoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7iVppFVVOR NV\ROopjUUN3ME20MlM{KM7:TR?= MnP6NlM2OzF7MkG=
KCNR MUTBdI9xfG:|aYOgRZN{[Xl? MWewMlUwOS5yL{KuOUDPxE1? MoHCNlQhcA>? MlPrSG1UVw>? M4fGVYlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MkLrNlM2OzF7MkG=
SY5Y NIfLOGJCeG:ydH;zbZMhSXO|YYm= MViwMlUwOS5yL{KuOUDPxE1? NUPrR4M{OjRiaB?= M2\vO2ROW09? NU[yN|F2cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NYH5[4h6OjN3M{G5NlE>
Rh18 M2nFN2Fxd3C2b4Ppd{BCe3OjeR?= M4G3cVAvPS9zLkCvNk42KM7:TR?= MWKyOEBp M4joZmROW09? M1rIb4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= MnH2NlM2OzF7MkG=
TC32 MVrBdI9xfG:|aYOgRZN{[Xl? M{XWPVAvPS9zLkCvNk42KM7:TR?= NWXiZoNoOjRiaB?= NXz3ZVlHTE2VTx?= NXz5eZE1cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> M4W5NVI{PTNzOUKx
KCNR Mnm5SpVv[3Srb36gRZN{[Xl? NX7W[WZSOC53L{GuNE8zNjVxNTFOwG0> MVmyOEBp M1\vZ2ROW09? NHvLWFZqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=> MkOyNlM2OzF7MkG=
SY5Y NILsXJFHfW6ldHnvckBCe3OjeR?= MWiwMlUwOS5yL{KuOU82KM7:TR?= NYjF[JJzOjRiaB?= MlnVSG1UVw>? NV\2WHc1cW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NXLJR2N{OjN3M{G5NlE>
Rh18 NWr2NZdoTnWwY4Tpc44hSXO|YYm= MWOwMlUwOS5yL{KuOU82KM7:TR?= MlXkNlQhcA>? MWXEUXNQ MWfpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= NFjaSpczOzV|MUmyNS=>
TC32 NET2VlFHfW6ldHnvckBCe3OjeR?= MWewMlUwOS5yL{KuOU82KM7:TR?= MUiyOEBp NULD[lI4TE2VTx?= NX\FVphJcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NVTrPG5GOjN3M{G5NlE>
TPC-1 NGLBR5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT1NUDDvU1? NGXqS4ExNTRiZB?= MmDJSG1UVw>? NIXJdZlqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAzKGRidILlZZRu\W62 Mn\wNlMxPTZ2OUm=
MZ-CRC1  NYHtUWk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH4TowyKML3TR?= MnfSNE02KGR? NHu5dXBFVVOR M1Xj[olvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR? MmS1NlMxPTZ2OUm=
TT  NVnWXoNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXxZ2UyKML3TR?= NW\HboFbOC12IHS= NXv6WpdETE2VTx?= NE\NNWJqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 M3m1e|I{ODV4NEm5
TPC-1 M2HhdWZ2dmO2aX;uJGF{e2G7 NHfQNIoyKML3TR?= MkLQO|IhcA>? M3nTXWROW09? NIHROFJqdmS3Y3XzJGcyKGKub3PrZYdm NXHhfIpPOjNyNU[0PVk>
MZ-CRC1  MXjGeY5kfGmxbjDBd5NigQ>? MkjtNUDDvU1? M1u2dFczKGh? Mly4SG1UVw>? NGjUfmNqdmS3Y3XzJGcyKGKub3PrZYdm MnT3NlMxPTZ2OUm=
TT  NH\tdnhHfW6ldHnvckBCe3OjeR?= NV\2UY9lOSEEtV2= NGPVcnc4OiCq MlfrSG1UVw>? MkPYbY5lfWOnczDHNUBjdG:la3Hn[S=> MlH3NlMxPTZ2OUm=
MZ-CRC1  MlP0RZBweHSxc3nzJGF{e2G7 NVy3WWE1OSEEtV2= M3vuXlQ5KGh? NFfiRXFFVVOR MVHpcoR2[2W|IHHwc5B1d3Orcx?= NYHxSFlLOjNyNU[0PVk>
TT  MYDBdI9xfG:|aYOgRZN{[Xl? M4ThSVEhyrWP Ml\IOFghcA>? M13JS2ROW09? NG[1clJqdmS3Y3XzJIFxd3C2b4Ppdy=> NVLuN5ExOjNyNU[0PVk>
HD-LM2 NXnOSJRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC3NwKBkWh? MkW3SG1UVw>? Ml7FTWM2OD15Lki0OEDPxE1? NWHjUm02OjJ6MkmwPVQ>
L-428 NWXXPY1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLMO|LjiImq MYXEUXNQ M4jlRmlEPTB;Nz65OFch|ryP NGXxUYMzOjh{OUC5OC=>
KM-H2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnQWGI4OuLCiXi= MU\EUXNQ NGW3c4pKSzVyPUGuN|A5KM7:TR?= NX6yOFRzOjJ6MkmwPVQ>
L-540 Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfNS|k4OuLCiXi= MXXEUXNQ M4TnPGlEPTB;OD6yNVYh|ryP NILQVIgzOjh{OUC5OC=>
HD-LM2 NVW4W5ZiTnWwY4Tpc44hSXO|YYm= MXOwMlEwOC53L{GvOUDPxE1? MmX6O|LjiImq MWPEUXNQ NGjSb5lqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? MXKyNlgzQTB7NB?=
L-428 MYjGeY5kfGmxbjDBd5NigQ>? NGPKelUxNjFxMD61M|EwPSEQvF2= M3LCe|cz6oDLaB?= NInMVYJFVVOR MkLLbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> M4ixSFIzQDJ7MEm0
KM-H2 M4PJOWZ2dmO2aX;uJGF{e2G7 MnTrNE4yNzBwNT:xM|Uh|ryP MUW3NwKBkWh? M3nLN2ROW09? M135TIlvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v MYSyNlgzQTB7NB?=
L-540 NUnoeFlOTnWwY4Tpc44hSXO|YYm= MV6wMlEwOC53L{GvOUDPxE1? NGDYcIw4OuLCiXi= M{HxS2ROW09? MmDvbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> M3Lj[|IzQDJ7MEm0
HD-LM2 NGni[GZCeG:ydH;zbZMhSXO|YYm= NFToUFMyNzVizszN MUW3NwKBkWh? NV7JNmlpTE2VTx?= M3;rfolv\HWlZYOgZZBweHSxc3nz MYSyNlgzQTB7NB?=
L-428 MXnBdI9xfG:|aYOgRZN{[Xl? NWXSfXRbOS93IN88US=> MoqxO|LjiImq MnS0SG1UVw>? MXzpcoR2[2W|IHHwc5B1d3Orcx?= M{PUUVIzQDJ7MEm0
KM-H2 MlW0RZBweHSxc3nzJGF{e2G7 Mn2zNU82KM7:TR?= NF\2emI4OuLCiXi= MVjEUXNQ MUTpcoR2[2W|IHHwc5B1d3Orcx?= NEDNd|EzOjh{OUC5OC=>
L-540 Ml7ZRZBweHSxc3nzJGF{e2G7 NWjURVZ3OS93IN88US=> MmPqO|LjiImq NFrh[HhFVVOR M2Sx[Ylv\HWlZYOgZZBweHSxc3nz MkD1NlI5OjlyOUS=
U251-MG MmHQSpVv[3Srb36gRZN{[Xl? NF;K[IgyKML3TR?= NIrtVmoxNTF4IHi= NY[5WFVmcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w M37Yb|IzODJ5Nkmx
U87-MG MmjMSpVv[3Srb36gRZN{[Xl? NX\FOWdZOSEEtV2= NVnrenNlOC1zNjDo MmHnbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v M134dVIzODJ5Nkmx
4C8 MoHoSpVv[3Srb36gRZN{[Xl? M{HRR|EhyrWP NV\s[pg2OC1zNjDo MnX5bY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v MYWyNlAzPzZ7MR?=
U251-MG NVTRXYRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxM|ExKML3TR?= Mk\nNlQwPDhxN{KgbC=> MXvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MV2yNlAzPzZ7MR?=
U87-MG M4\iZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXe5dplNOS9zMDFCuW0> M2XaXlI1NzR6L{eyJIg> MWTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> M2jIXlIzODJ5Nkmx
4C8 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\EOGl6OS9zMDFCuW0> MWmyOE81QC95MjDo NW\G[Wl[cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? M4S1[VIzODJ5Nkmx
U266 NWWyVmRZSXCxcITvd4l{KEG|c3H5 NWPzUZVrOC53LUKg{txO NV[xPIpuPDhxN{KgbC=> MnLubY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M1PvZVIyOTZ2NUG3
Kms.11 MYPBdI9xfG:|aYOgRZN{[Xl? MV6wMlUuOiEQvF2= M{D2VFQ5Nzd{IHi= NELhdXJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M3PBTVIyOTZ2NUG3
8226 M4f6cWFxd3C2b4Ppd{BCe3OjeR?= NYnRUVlYOC53LUKg{txO NGDLWVE1QC95MjDo MYLpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NWqxfXR[OjFzNkS1NVc>

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[5]
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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.
Cell Research:[4]
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  • Cell lines: Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs
  • Concentrations: ~1 μM
  • Incubation Time: 48 or 24 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Female BALB/c and athymic nude (NCR - nu/nu) mice (7–8 weeks old)
  • Formulation: AZD1480 is suspended in water supplemented with 0.5% hypromellose and 0.1% Tween 80.
  • Dosages: Once a day at the dose of 50 mg/kg or twice daily at 30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL warmed (197.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
5 mg/mL

* 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.

Chemical Information

Molecular Weight 348.77
Formula

C14H14ClFN8

CAS No. 935666-88-9
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID