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
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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 MmnPSpVv[3Srb36gRZN{[Xl? NX7KS5E1PSEQvF2= NILLOnA1QCCq MVPEUXNQ MoqzZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n NUHIVXRFOjV7NUS5O|Q>
LoVo  NXS5eGdbTnWwY4Tpc44hSXO|YYm= NXzN[JVVPSEQvF2= MkWwOFghcA>? NGP1TYRFVVOR MmHZZoxw[2u|IFrBT|IwW1SDVEOgd4lodmGuaX7n M2HhTVI2QTV2OUe0
HN5 M2XHN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYi3NkBp MYjFR|UxRTNwOEGgxtEhOS57OTFOwG0> M1zKOlI2QDFyMEGw
Cal33 NXWwRVRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq1XFY4OiCq Ml3FSWM2OD1|LkO3JOKyKDBwN{Wg{txO NW\mS4FkOjV6MUCwNVA>
UM-22B MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrrb2g4OiCq M1rheGVEPTB;Mj62OkDDuSByLkK0JO69VQ>? M{fmWlI2QDFyMEGw
686LN MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm3NkBp MofuSWM2OD1{LkC1JOKyKDFwM{Og{txO MnHQNlU5OTByMUC=
UM SCC-1 NX3EOXdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW1bJZPPzJiaB?= MnfDSWM2OD1zLk[3JOKyKDBwNEKg{txO MlT1NlU5OTByMUC=
UM-22A NWTMUY1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi3NkBp MWnFR|UxRTFwM{KgxtEhOC5|OTFOwG0> MXmyOVgyODBzMB?=
OSC19 MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[2[pY6PzJiaB?= NWmxSo5vTUN3ME2xMlI3KMLzIECuNlAh|ryP NYq5eIdlOjV6MUCwNVA>
PCI-52 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlziO|IhcA>? MmHCSWM2OD1zLkCwJOKyKDBwMEmg{txO MoO5NlU5OTByMUC=
PCI-15B NV3jPJlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vDWFczKGh? MWPFR|UxRTBwOUmgxtEhOS55NDFOwG0> M{K2XlI2QDFyMEGw
UMSCC-1 MmfrSpVv[3Srb36gRZN{[Xl? M4PrS|AvODByNT2xMlYh|ryP NE\WRlgzPCCq M3f3SoFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1HySlI2QDFyMEGw
Cal33 NGPIToJHfW6ldHnvckBCe3OjeR?= NVO2e4F7OC5yMEC1MVMvQCEQvF2= M4X5NlI1KGh? NH\WN3Ni[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkXQNlU5OTByMUC=
HH5 Mn\OSpVv[3Srb36gRZN{[Xl? MUWwMlAxODVvMz64JO69VQ>? NY\iN2ZQOjRiaB?= MULhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M{TUfFI2QDFyMEGw
UM-22A NGLFbldHfW6ldHnvckBCe3OjeR?= M{noXVAvODByNT2xMlYh|ryP NIXsSlQzPCCq NH3ITFRi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYS4PXhxOjV6MUCwNVA>
A1847 MVnGeY5kfGmxbjDBd5NigQ>? NY\WXmR3OC5yNT2xNEDPxE1? MlGyNlQhcA>? MU\EUXNQyqB? NFrVTZVz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=> MoPBNlU3PDZyMUW=
OVCAR-5 NWXGcopoTnWwY4Tpc44hSXO|YYm= M4\wZVAvODVvMUCg{txO NI[1VJYzPCCq MoroSG1UV8Li MYjy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MnHINlU3PDZyMUW=
OVCAR-8 M13xN2Z2dmO2aX;uJGF{e2G7 MmXsNE4xPS1zMDFOwG0> NU\ueHlyOjRiaB?= NYP5bopyTE2VT9Mg MULy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= Mly2NlU3PDZyMUW=
MOVCAR-5447 Mn2xSpVv[3Srb36gRZN{[Xl? NX\2fWZoOC5yNT2xNEDPxE1? MlfUNlQhcA>? NFrtbWlFVVORwrC= MXXy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NULpfmxtOjV4NE[wNVU>
MOVCAR-5009 NVzjfYRqTnWwY4Tpc44hSXO|YYm= Mn3HNE4xPS1zMDFOwG0> M37YUFI1KGh? M1\4emROW00EoB?= MUny[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NEjRV4szPTZ2NkCxOS=>
A1847 MnG0R4VtdCCYaXHibYxqfHliQYPzZZk> NV7BVYl2OC5yNT2xNEDPxE1? NI\mR4M4OiCq MYjEUXNQ NETLNXNz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NGDjWWkzPTZ2NkCxOS=>
OVCAR-5 NIjaZlhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFraNWUxNjB3LUGwJO69VQ>? NXzaS2doPzJiaB?= MUXEUXNQ M3[yXpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN MleyNlU3PDZyMUW=
OVCAR-8  M131TGNmdGxiVnnhZoltcXS7IFHzd4F6 NV:0SplPOC5yNT2xNEDPxE1? NUHTNo9SPzJiaB?= NIXodZVFVVOR MlPvdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= M1q3dlI2PjR4MEG1
OVCAR-5  Mm\MRZBweHSxc3nzJGF{e2G7 NWPmXlRoOC53L{GvOUDPxE1? NVm4T4plPDhiaB?= M3u1WGROW09? MmD3bY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= MmP6NlU3PDZyMUW=
OVCAR-8  NGLpeFlCeG:ydH;zbZMhSXO|YYm= MoLuNE42NzFxNTFOwG0> NVvDRVBLPDhiaB?= MVzEUXNQ NUjPZWpxcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> M3LVVVI2PjR4MEG1
AKRSL MnLBR4VtdCCYaXHibYxqfHliQYPzZZk> M2e5[|czKGh? NYrvb3BKUUN3MP-8olExKM7:TR?= MYKyOVUxPDZ|NR?=
PALJDL Ml3JR4VtdCCYaXHibYxqfHliQYPzZZk> NVX5e3NVPzJiaB?= MlHkTWM2OD1{LkSg{txO NEDlR4szPTVyNE[zOS=>
MO4 MVHGeY5kfGmxbjDBd5NigQ>? MVewMlUwOS93IN88US=> M{nsNlYhcA>? MUPpcohq[mm2czDQMXNVSVR|IHX4dJJme3Orb39CpC=> MoTqNlUyPDl3M{W=
DU145  NV7XOYxsTnWwY4Tpc44hSXO|YYm= MWKwMVIxOCCwTR?= M{fW[|EhcMLi NHi2dWZ{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n NXTxPXA3OjR3N{e5OFI>
DU145  NV\hPWpMTnWwY4Tpc44hSXO|YYm= NU\GVmgxQDByIH7N NGPHSnE4OiCq NFe0W5Z{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom= MnzONlQ2Pzd7NEK=
CWR22Rv1 MXvGeY5kfGmxbjDBd5NigQ>? NGXVU|Q5ODBibl2= NGXLeHA4OiCq M2DpepN2eHC{ZYPz[ZMhUUxvNj3pcoR2[2WmIH3p[5JifG:{eR?= MmnsNlQ2Pzd7NEK=
N592 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C0VmlEPTB;MD64OEDPxE1? Mor6NlQyPTh5MEG=
H82 NX3BS2xjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXEZ4hMUUN3ME2xMlM4KM7:TR?= Mn2wNlQyPTh5MEG=
GLC4 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr3TWM2OD1zLke5JO69VQ>? M3zBW|I1OTV6N{Cx
H526 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXveJJKSzVyPUOuNFgh|ryP M4GzU|I1OTV6N{Cx
H1173 M4\Gemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJwM{mg{txO NGrYOm4zPDF3OEewNS=>
DMS114 NF\4OZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vJXGlEPTB;MD63N{DPxE1? NVfqeYsyOjRzNUi3NFE>
NCI-N592 M2m5bmZ2dmO2aX;uJGF{e2G7 M1HBSlAvOy9zL{Og{txO MW[yOEBp MkHBbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M3nQU|I1OTV6N{Cx
GLC4 Mm\zSpVv[3Srb36gRZN{[Xl? NVnBRWhDOC5|L{GvN{DPxE1? M{H2RVI1KGh? NHrNOINqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R? NYKyTG1nOjRzNUi3NFE>
NCI-H82 Mn7oSpVv[3Srb36gRZN{[Xl? NHX0dlgxNjNxMT:zJO69VQ>? MmTXNlQhcA>? NV7vb3h{cW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M4PUZlI1OTV6N{Cx
NCI-N592 NHHofolCeG:ydH;zbZMhSXO|YYm= NEDwNmYxNjNxMT:zJO69VQ>? MV60PEBp M37iWolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? MVqyOFE2QDdyMR?=
GLC4 NEjaXXRCeG:ydH;zbZMhSXO|YYm= MV2wMlMwOS9|IN88US=> Mn\hOFghcA>? NFH5SYVqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB| Mon1NlQyPTh5MEG=
NCI-H82 M4j4bWFxd3C2b4Ppd{BCe3OjeR?= NX[0T3pxOC5|L{GvN{DPxE1? NHTZc4Y1QCCq M1L3e4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN? M2rDcFI1OTV6N{Cx
CWR22Rv1  NHjZelFCeG:ydH;zbZMhSXO|YYm= NUS2dFVCUUN3ME2wMlQ5OiEQvF2= NEPRNW4zOzl2MkC5OS=>
CWR22Pc MknMRZBweHSxc3nzJGF{e2G7 M1HLSGlEPTB;MD60N|gh|ryP M2PxOlI{QTR{MEm1
PC-3 NFXzXpZCeG:ydH;zbZMhSXO|YYm= MWPJR|UxRTFwN{W1JO69VQ>? MUKyN|k1OjB7NR?=
DU145 M3jYXWFxd3C2b4Ppd{BCe3OjeR?= NXT2Zo1CUUN3ME2zMlUyPyEQvF2= MkDiNlM6PDJyOUW=
RC165N MVXBdI9xfG:|aYOgRZN{[Xl? MoDsTWM2OD1{LkC4N{DPxE1? MmXpNlM6PDJyOUW=
ARPE19 M3PwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TxS2ROW09? NUnOfWZ5UUN3ME2yOE4{QCEQvF2= NGT1WWwzOzV|MUmyNS=>
HEK293 M4\mcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfvSG1UVw>? MYjJR|UxRThwNkeg{txO M1jYb|I{PTNzOUKx
KCNR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHBTFNGTE2VTx?= MVnJR|UxRTBwNE[g{txO MkewNlM2OzF7MkG=
SY5Y MmjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\5SG1UVw>? M1H6S2lEPTB;MD6zOkDPxE1? NXTnNXBCOjN3M{G5NlE>
BE2 M1nlPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknXSG1UVw>? M1nFXWlEPTB;MD63NUDPxE1? M4DyV|I{PTNzOUKx
AS MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moq1SG1UVw>? MmKyTWM2OD1zLkWzJO69VQ>? MYSyN|U{OTl{MR?=
NGP NEXKPZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmK3SG1UVw>? NYL3XpBWUUN3ME2wMlU3KM7:TR?= M1K1flI{PTNzOUKx
IMR32 NHPNXo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LzRmROW09? NW\FSGZHUUN3ME2wMlY3KM7:TR?= M3G5d|I{PTNzOUKx
LAN5 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3foO2ROW09? M3e3U2lEPTB;MT6wOEDPxE1? NX\LW3NrOjN3M{G5NlE>
RH18 NXfqWYIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H2T2ROW09? NYrWXo5{UUN3ME2xMlQzKM7:TR?= NH[ybmszOzV|MUmyNS=>
RH30 NYfPRnVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH6R3pVTE2VTx?= MknaTWM2OD1zLkK1JO69VQ>? MYGyN|U{OTl{MR?=
RH17 NVPRc3hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTnfo9rTE2VTx?= MnfaTWM2OD1{LkWxJO69VQ>? MorLNlM2OzF7MkG=
RH28 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mom0SG1UVw>? Ml7qTWM2OD12LkK4JO69VQ>? MYGyN|U{OTl{MR?=
RH36 NG\BNXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnftSG1UVw>? M3frcWlEPTB;NT6zO{DPxE1? NFLnb2gzOzV|MUmyNS=>
RH41 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOxcYJFVVOR M1jEdmlEPTB;MD60PEDPxE1? MnuyNlM2OzF7MkG=
RD Mn7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn3T4ZFVVOR MWDJR|UxRTRwM{Kg{txO MX:yN|U{OTl{MR?=
TC32 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrpXIlFVVOR MWnJR|UxRTNwOEWg{txO M3ixOVI{PTNzOUKx
TC71 NVLkc4ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD1SG1UVw>? NXXtZ5NOUUN3ME20MlM{KM7:TR?= MnnTNlM2OzF7MkG=
KCNR NXTucmFmSXCxcITvd4l{KEG|c3H5 M3HkTlAvPS9zLkCvNk42KM7:TR?= M4n6W|I1KGh? MULEUXNQ M{jpO4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdIm= M1f2N|I{PTNzOUKx
SY5Y M2HrNWFxd3C2b4Ppd{BCe3OjeR?= MXGwMlUwOS5yL{KuOUDPxE1? Mn:5NlQhcA>? NWDa[m02TE2VTx?= MljqbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= NGj5cG8zOzV|MUmyNS=>
Rh18 M3rMcWFxd3C2b4Ppd{BCe3OjeR?= NIDUU3AxNjVxMT6wM|IvPSEQvF2= MXGyOEBp MkDESG1UVw>? MlThbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= Mn[2NlM2OzF7MkG=
TC32 NGTuTFNCeG:ydH;zbZMhSXO|YYm= NGjFVpQxNjVxMT6wM|IvPSEQvF2= M4niZVI1KGh? NHm3eHFFVVOR Mo\wbY5lfWOnczDhckBqdmO{ZXHz[UBqdiClYYPwZZNmKDNxNzDhZ5Rqfmm2eR?= M4T5NVI{PTNzOUKx
KCNR NWfrRZp4TnWwY4Tpc44hSXO|YYm= MVqwMlUwOS5yL{KuOU82KM7:TR?= M1TVbVI1KGh? MonqSG1UVw>? M1XLT4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u NYPK[pFqOjN3M{G5NlE>
SY5Y NGTTSo9HfW6ldHnvckBCe3OjeR?= Ml63NE42NzFwMD:yMlUwPSEQvF2= MnrYNlQhcA>? MlHXSG1UVw>? MWXpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?= MUeyN|U{OTl{MR?=
Rh18 NIPU[lZHfW6ldHnvckBCe3OjeR?= MlvVNE42NzFwMD:yMlUwPSEQvF2= MmLENlQhcA>? MnPMSG1UVw>? MmrTbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR|IHHjeIl3[XSrb36= Ml\3NlM2OzF7MkG=
TC32 NFfyNZlHfW6ldHnvckBCe3OjeR?= NWnHUVRsOC53L{GuNE8zNjVxNTFOwG0> M3\PPVI1KGh? NWPqZZN5TE2VTx?= NUPj[oE3cW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NE\VNowzOzV|MUmyNS=>
TPC-1 NWPQOplTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP6NUDDvU1? M1PpNlAuPCCm NGe1[WVFVVOR MkC0bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? MoHNNlMxPTZ2OUm=
MZ-CRC1  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCxJOK2VQ>? MXuwMVUh\A>? MkHnSG1UVw>? NYW4XGl2cW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?= NYiwOXlmOjNyNU[0PVk>
TT  NFHNbZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmxJOK2VQ>? MorGNE01KGR? MWrEUXNQ NETIN4NqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 NFziWpUzOzB3NkS5PS=>
TPC-1 NGXZTodHfW6ldHnvckBCe3OjeR?= NV;RR3g{OSEEtV2= MXi3NkBp NXHDTYsyTE2VTx?= Mne2bY5lfWOnczDHNUBjdG:la3Hn[S=> NUO1Z|V3OjNyNU[0PVk>
MZ-CRC1  NE\zcWRHfW6ldHnvckBCe3OjeR?= MU[xJOK2VQ>? NFzxSXA4OiCq NVfyRo1lTE2VTx?= NYj6R5JpcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MknLNlMxPTZ2OUm=
TT  NHTYN2JHfW6ldHnvckBCe3OjeR?= MkjCNUDDvU1? M4izZ|czKGh? MXHEUXNQ NVzpcoRicW6mdXPld{BIOSCkbH;jb4Fo\Q>? NHzyNmIzOzB3NkS5PS=>
MZ-CRC1  NUn1NpZSSXCxcITvd4l{KEG|c3H5 M3LTNFEhyrWP Mmf5OFghcA>? NXzoS|NlTE2VTx?= NIK1Zo1qdmS3Y3XzJIFxd3C2b4Ppdy=> NF33RmYzOzB3NkS5PS=>
TT  NVzx[Gs{SXCxcITvd4l{KEG|c3H5 MXqxJOK2VQ>? NInlRXY1QCCq NIjVXVFFVVOR M4XIO4lv\HWlZYOgZZBweHSxc3nz MlzGNlMxPTZ2OUm=
HD-LM2 MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjWO|LjiImq M2fNWmROW09? M4\RV2lEPTB;Nz64OFQh|ryP M{niUFIzQDJ7MEm0
L-428 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHoUYRTPzMkgJno MkPUSG1UVw>? Mo\CTWM2OD15Lkm0O{DPxE1? NIrHZWQzOjh{OUC5OC=>
KM-H2 NVvteVBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHxcGlJPzMkgJno NIH5ZZNFVVOR MljtTWM2OD1zLkOwPEDPxE1? MmL6NlI5OjlyOUS=
L-540 NVfMcFNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfCTlQ4OuLCiXi= M3jCemROW09? M1PXeWlEPTB;OD6yNVYh|ryP NV;YNYpQOjJ6MkmwPVQ>
HD-LM2 Mn3nSpVv[3Srb36gRZN{[Xl? MnKyNE4yNzBwNT:xM|Uh|ryP M1LSc|cz6oDLaB?= MYHEUXNQ NEHSeFNqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? M37vU|IzQDJ7MEm0
L-428 NH73dJBHfW6ldHnvckBCe3OjeR?= MVewMlEwOC53L{GvOUDPxE1? NIHodmk4OuLCiXi= NGHTemdFVVOR MmKybY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NUT5bIpwOjJ6MkmwPVQ>
KM-H2 NWjNcFJ5TnWwY4Tpc44hSXO|YYm= MV:wMlEwOC53L{GvOUDPxE1? NHnjZlQ4OuLCiXi= NYjKfItnTE2VTx?= MlW0bY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NE\IZVczOjh{OUC5OC=>
L-540 NITldG1HfW6ldHnvckBCe3OjeR?= NVqzU29lOC5zL{CuOU8yNzVizszN MX[3NwKBkWh? NU\6OZdsTE2VTx?= MkfQbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NFXPOoozOjh{OUC5OC=>
HD-LM2 M13aO2Fxd3C2b4Ppd{BCe3OjeR?= Mom1NU82KM7:TR?= M3GwW|cz6oDLaB?= NH:xVXpFVVOR MVzpcoR2[2W|IHHwc5B1d3Orcx?= NXe5eGxmOjJ6MkmwPVQ>
L-428 M3zaWmFxd3C2b4Ppd{BCe3OjeR?= NHrSU5MyNzVizszN MoL2O|LjiImq MWfEUXNQ NHHNc3NqdmS3Y3XzJIFxd3C2b4Ppdy=> MYGyNlgzQTB7NB?=
KM-H2 NHnDUVFCeG:ydH;zbZMhSXO|YYm= M3rCcFEwPSEQvF2= Mn7OO|LjiImq NETQ[3dFVVOR NFrNfWlqdmS3Y3XzJIFxd3C2b4Ppdy=> NYrOS3ZEOjJ6MkmwPVQ>
L-540 NIDN[pZCeG:ydH;zbZMhSXO|YYm= NEXxcZYyNzVizszN NYPMPGZ[PzMkgJno NVqwVIE1TE2VTx?= NUn1[Gw6cW6mdXPld{BieG:ydH;zbZM> NX3qWZV1OjJ6MkmwPVQ>
U251-MG Mnj4SpVv[3Srb36gRZN{[Xl? NHzaZ44yKML3TR?= Mn3JNE0yPiCq MWjpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> MWeyNlAzPzZ7MR?=
U87-MG NGTTSpRHfW6ldHnvckBCe3OjeR?= M364TVEhyrWP MX6wMVE3KGh? NGDEeZhqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NIXETmYzOjB{N{[5NS=>
4C8 Ml7tSpVv[3Srb36gRZN{[Xl? NUDncYc6OSEEtV2= MViwMVE3KGh? MYLpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> M{HmZlIzODJ5Nkmx
U251-MG NHLwfopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTjNWJDOS9zMDFCuW0> NIPxc|YzPC92OD:3NkBp M{nYfolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NV3uR3VEOjJyMke2PVE>
U87-MG Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\sTIkyNzFyINM1US=> MV:yOE81QC95MjDo NWLXZ|NHcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NYD1Sm5LOjJyMke2PVE>
4C8 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jhR|EwOTBiwsXN NXzmWnc1OjRxNEivO|IhcA>? MY\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> MnLTNlIxOjd4OUG=
U266 NXXqOXZwSXCxcITvd4l{KEG|c3H5 NW\URmVYOC53LUKg{txO MYS0PE84OiCq NVHkWG9VcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYjU[oFUOjFzNkS1NVc>
Kms.11 M1;JWWFxd3C2b4Ppd{BCe3OjeR?= MYiwMlUuOiEQvF2= MnXtOFgwPzJiaB?= MYfpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M3rRPVIyOTZ2NUG3
8226 NWTNeWFtSXCxcITvd4l{KEG|c3H5 NXHoXoRGOC53LUKg{txO MmC4OFgwPzJiaB?= MnnNbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MXOyNVE3PDVzNx?=

... 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]
+ Expand

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]
+ Expand
  • 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.

  • * Indicates a Required Field

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products4

Tags: buy AZD1480 | AZD1480 supplier | purchase AZD1480 | AZD1480 cost | AZD1480 manufacturer | order AZD1480 | AZD1480 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID