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.

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In DMSO USD 130 In stock
USD 100 In stock
USD 170 In stock
USD 570 In stock
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Cited by 15 Publications

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 M1vEPWZ2dmO2aX;uJGF{e2G7 MX:1JO69VQ>? MUe0PEBp M1zr[GROW09? NVrDXlFt[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o MlL1NlU6PTR7N{S=
LoVo  NGHi[5ZHfW6ldHnvckBCe3OjeR?= MWm1JO69VQ>? NWLzWGZmPDhiaB?= MnfhSG1UVw>? MYDicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= NUHN[pVJOjV7NUS5O|Q>
HN5 M{HlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vDPVczKGh? NInV[VJGSzVyPUOuPFEhyrFiMT65PUDPxE1? Ml\SNlU5OTByMUC=
Cal33 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHOVHNtPzJiaB?= MkHKSWM2OD1|LkO3JOKyKDBwN{Wg{txO M{TJZVI2QDFyMEGw
UM-22B NUfsNFVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPvV|Q3PzJiaB?= MUHFR|UxRTJwNk[gxtEhOC5{NDFOwG0> NHfMbHYzPThzMECxNC=>
686LN M1nZcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK3NkBp MX;FR|UxRTJwMEWgxtEhOS5|MzFOwG0> MnHmNlU5OTByMUC=
UM SCC-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;mWnFMPzJiaB?= M4HIWmVEPTB;MT62O{DDuSByLkSyJO69VQ>? NWnGc5Y2OjV6MUCwNVA>
UM-22A M{nYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\2O|IhcA>? MVHFR|UxRTFwM{KgxtEhOC5|OTFOwG0> NHPkSZQzPThzMECxNC=>
OSC19 MoXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjldnJ1PzJiaB?= MomzSWM2OD1zLkK2JOKyKDBwMkCg{txO MVSyOVgyODBzMB?=
PCI-52 NWHNcHpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13XUVczKGh? NUfqdoFZTUN3ME2xMlAxKMLzIECuNFkh|ryP NWjxZndmOjV6MUCwNVA>
PCI-15B M4jFZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfwPW04OiCq MmfFSWM2OD1yLkm5JOKyKDFwN{Sg{txO MXKyOVgyODBzMB?=
UMSCC-1 NI\zNVRHfW6ldHnvckBCe3OjeR?= M17mfFAvODByNT2xMlYh|ryP NEjwb2gzPCCq M1nGXYFjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1SxUVI2QDFyMEGw
Cal33 M1u1SmZ2dmO2aX;uJGF{e2G7 NH7MW4wxNjByMEWtN{45KM7:TR?= NWHhdmJ[OjRiaB?= NF;NXmpi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHH5UGkzPThzMECxNC=>
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OVCAR-5 M{m3NWZ2dmO2aX;uJGF{e2G7 MlvqNE4xPS1zMDFOwG0> NUj1V4hiOjRiaB?= MYfEUXNQyqB? MWHy[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= MlPPNlU3PDZyMUW=
OVCAR-8 M3PzemZ2dmO2aX;uJGF{e2G7 NF\FfFExNjB3LUGwJO69VQ>? MUSyOEBp NH7vSmhFVVORwrC= MW\y[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= M2XrZVI2PjR4MEG1
MOVCAR-5447 NVPmZ4VTTnWwY4Tpc44hSXO|YYm= NGjqcnMxNjB3LUGwJO69VQ>? NVrBfI9VOjRiaB?= NUTzSnV{TE2VT9Mg NVvHUo0xemWmdXPld{BxcG:|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM> MWWyOVY1PjBzNR?=
MOVCAR-5009 Mnr1SpVv[3Srb36gRZN{[Xl? M2HOfVAvODVvMUCg{txO M4XES|I1KGh? NUfET5Y6TE2VT9Mg MVny[YR2[2W|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?= NX\2Zop{OjV4NE[wNVU>
A1847 M{GwZ2NmdGxiVnnhZoltcXS7IFHzd4F6 MkXQNE4xPS1zMDFOwG0> NVzyWpFOPzJiaB?= NXvTSodjTE2VTx?= NY\veZljemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0> NGnYO|AzPTZ2NkCxOS=>
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OVCAR-8  NGSzWmFCeG:ydH;zbZMhSXO|YYm= Mk\HNE42NzFxNTFOwG0> NF3qfpY1QCCq MYHEUXNQ M3jhTIlv\HWlZYOgd4lodmmoaXPhcpQh[XCxcITvd4l{KGG2IHjp[4gh[2:wY3XycpRz[XSrb36= MkLvNlU3PDZyMUW=
AKRSL NH\OfVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUfRWXd6PzJiaB?= NFjmNVlKSzVy78{eNVAh|ryP M2HzeFI2PTB2NkO1
PALJDL MoXIR4VtdCCYaXHibYxqfHliQYPzZZk> NXSzNpB[PzJiaB?= M2HZS2lEPTB;Mj60JO69VQ>? NXTV[mFzOjV3MES2N|U>
MO4 NIXDXlRHfW6ldHnvckBCe3OjeR?= M33TdlAvPS9zL{Wg{txO NF[2dnk3KGh? NW\odYZJcW6qaXLpeJMhWC2VVFHUN{BmgHC{ZYPzbY9vyqB? NGfhZ5ozPTF2OUWzOS=>
DU145  MkjQSpVv[3Srb36gRZN{[Xl? NVLKOIx4OC1{MECgcm0> NFW0UYMyKGkEoB?= NV;nR3Zwe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=> M4K0UlI1PTd5OUSy
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H82 MkL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPqTWM2OD1zLkO3JO69VQ>? M{TCR|I1OTV6N{Cx
GLC4 NFTwXIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jrTGlEPTB;MT63PUDPxE1? NUn3ZpBEOjRzNUi3NFE>
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H1173 NEjDd3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrXb|BKSzVyPUKuN|kh|ryP NFrkbIIzPDF3OEewNS=>
DMS114 MojnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[3emZKSzVyPUCuO|Mh|ryP M1nMZ|I1OTV6N{Cx
NCI-N592 MlLjSpVv[3Srb36gRZN{[Xl? NITEdVMxNjNxMT:zJO69VQ>? MoHQNlQhcA>? M3nvZ4lv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NICyeFUzPDF3OEewNS=>
GLC4 NHXUUYZHfW6ldHnvckBCe3OjeR?= NVfFXYkxOC5|L{GvN{DPxE1? M37ufFI1KGh? MlnpbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M4rpSVI1OTV6N{Cx
NCI-H82 MVzGeY5kfGmxbjDBd5NigQ>? MUiwMlMwOS9|IN88US=> NX3LXphkOjRiaB?= Mom2bY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NVTQ[406OjRzNUi3NFE>
NCI-N592 MX7BdI9xfG:|aYOgRZN{[Xl? MlnYNE4{NzFxMzFOwG0> MWq0PEBp MkPsbY5kemWjc3XzJJRp\SCuZY\lcEBw\iClbHXheoVlNUOjc4Dhd4UhOw>? MX:yOFE2QDdyMR?=
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NCI-H82 NFvOOplCeG:ydH;zbZMhSXO|YYm= NYjzd5dlOC5|L{GvN{DPxE1? NFKweoM1QCCq MYrpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ M1f6ZVI1OTV6N{Cx
CWR22Rv1  MVTBdI9xfG:|aYOgRZN{[Xl? M{PuSmlEPTB;MD60PFIh|ryP MVeyN|k1OjB7NR?=
CWR22Pc Mkm4RZBweHSxc3nzJGF{e2G7 MkLnTWM2OD1yLkSzPEDPxE1? MnL5NlM6PDJyOUW=
PC-3 M3G4eWFxd3C2b4Ppd{BCe3OjeR?= M2nJRWlEPTB;MT63OVUh|ryP M3fCb|I{QTR{MEm1
DU145 MkTTRZBweHSxc3nzJGF{e2G7 M{HzWmlEPTB;Mz61NVch|ryP NF\NTZMzOzl2MkC5OS=>
RC165N Ml62RZBweHSxc3nzJGF{e2G7 MXfJR|UxRTJwMEizJO69VQ>? MnHCNlM6PDJyOUW=
ARPE19 M2rJeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\V[2ROW09? M{nTS2lEPTB;MkSuN|gh|ryP NYOze21POjN3M{G5NlE>
HEK293 MojpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:3V49FVVOR MXjJR|UxRThwNkeg{txO M1jaN|I{PTNzOUKx
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NGP MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTNSG1UVw>? NEnhWo5KSzVyPUCuOVYh|ryP M3r6T|I{PTNzOUKx
IMR32 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHad4tJTE2VTx?= MYLJR|UxRTBwNk[g{txO MV[yN|U{OTl{MR?=
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RH18 M2fESGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HiUGROW09? MlrvTWM2OD1zLkSyJO69VQ>? M4WzUlI{PTNzOUKx
RH30 M12yZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXUfYNFVVOR NUDaV4dKUUN3ME2xMlI2KM7:TR?= MnPTNlM2OzF7MkG=
RH17 NF3ndG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF20dlhFVVOR MVzJR|UxRTJwNUGg{txO MYmyN|U{OTl{MR?=
RH28 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{S0PWROW09? NEnnNIFKSzVyPUSuNlgh|ryP NWLlc2l3OjN3M{G5NlE>
RH36 M4LQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\6[pVFVVOR M{nTT2lEPTB;NT6zO{DPxE1? NVO4eJdTOjN3M{G5NlE>
RH41 NIrrW5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrEUXNQ NEXhSZpKSzVyPUCuOFgh|ryP MYOyN|U{OTl{MR?=
RD NHO4XmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{D5VWROW09? MUnJR|UxRTRwM{Kg{txO M3fYOVI{PTNzOUKx
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TC71 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvEUXNQ M2PFV2lEPTB;ND6zN{DPxE1? NWfs[HExOjN3M{G5NlE>
KCNR MoPDRZBweHSxc3nzJGF{e2G7 MViwMlUwOS5yL{KuOUDPxE1? NXnhSItnOjRiaB?= NEjKfHZFVVOR NUL6S3JocW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=> NUe1SZRTOjN3M{G5NlE>
SY5Y MnLMRZBweHSxc3nzJGF{e2G7 Mo\tNE42NzFwMD:yMlUh|ryP NI\m[lczPCCq M4CxdWROW09? NF\sfIlqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5 M3y5clI{PTNzOUKx
Rh18 M3O1fWFxd3C2b4Ppd{BCe3OjeR?= NEjpZlExNjVxMT6wM|IvPSEQvF2= MYGyOEBp M1PzdWROW09? MXPpcoR2[2W|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7 MkC1NlM2OzF7MkG=
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KCNR MUTGeY5kfGmxbjDBd5NigQ>? MYiwMlUwOS5yL{KuOU82KM7:TR?= MnLTNlQhcA>? M2iwNmROW09? NYXTSFBwcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> MlPrNlM2OzF7MkG=
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TC32 MV\GeY5kfGmxbjDBd5NigQ>? NHnR[VQxNjVxMT6wM|IvPS93IN88US=> Mn;2NlQhcA>? NULRXW9ZTE2VTx?= NV7se3ZbcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44> NHfOeIYzOzV|MUmyNS=>
TPC-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxJOK2VQ>? MX2wMVQh\A>? MV\EUXNQ M3HjXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR? NEPo[4EzOzB3NkS5PS=>
MZ-CRC1  M1PVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36wVFEhyrWP NYPmOVRVOC13IHS= NXKydFZtTE2VTx?= NFy4NplqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62 NILvTlgzOzB3NkS5PS=>
TT  MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzYNUDDvU1? Ml;PNE01KGR? NH;4SVRFVVOR MlTYbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? MUCyN|A2PjR7OR?=
TPC-1 MnX4SpVv[3Srb36gRZN{[Xl? MoPpNUDDvU1? NWmyOYhRPzJiaB?= MlXFSG1UVw>? NUG4U2JbcW6mdXPld{BIOSCkbH;jb4Fo\Q>? NXrlTW1JOjNyNU[0PVk>
MZ-CRC1  NHzB[mpHfW6ldHnvckBCe3OjeR?= MWWxJOK2VQ>? MWm3NkBp M{TmTWROW09? NWrxOoVScW6mdXPld{BIOSCkbH;jb4Fo\Q>? M3PS[VI{ODV4NEm5
TT  MWXGeY5kfGmxbjDBd5NigQ>? NXS3OWtnOSEEtV2= M13wbFczKGh? NHv4b4lFVVOR NHr0Z4JqdmS3Y3XzJGcyKGKub3PrZYdm MXqyN|A2PjR7OR?=
MZ-CRC1  MmW0RZBweHSxc3nzJGF{e2G7 MWOxJOK2VQ>? NHrlXYU1QCCq NWXPSIdZTE2VTx?= M1ztZYlv\HWlZYOgZZBweHSxc3nz MVOyN|A2PjR7OR?=
TT  MYnBdI9xfG:|aYOgRZN{[Xl? NX[3XXhnOSEEtV2= M4TlNVQ5KGh? M3XNdmROW09? NFnhUpVqdmS3Y3XzJIFxd3C2b4Ppdy=> MUiyN|A2PjR7OR?=
HD-LM2 NUjTSGZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzOO|LjiImq MlrmSG1UVw>? NX3tWVNtUUN3ME23Mlg1PCEQvF2= NGPB[XkzOjh{OUC5OC=>
L-428 Mk\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTXZmd6PzMkgJno Ml\3SG1UVw>? NYnTVpVwUUN3ME23Mlk1PyEQvF2= MkG4NlI5OjlyOUS=
KM-H2 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TFU|cz6oDLaB?= MlTRSG1UVw>? NGfLTIlKSzVyPUGuN|A5KM7:TR?= MVuyNlgzQTB7NB?=
L-540 NIP4eFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nScVcz6oDLaB?= NEXic5RFVVOR M{jMUWlEPTB;OD6yNVYh|ryP MXeyNlgzQTB7NB?=
HD-LM2 MUfGeY5kfGmxbjDBd5NigQ>? NYHtbGltOC5zL{CuOU8yNzVizszN MY[3NwKBkWh? MXvEUXNQ NFfUflRqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? MUGyNlgzQTB7NB?=
L-428 MX;GeY5kfGmxbjDBd5NigQ>? MlvQNE4yNzBwNT:xM|Uh|ryP NWfiXYVKPzMkgJno M2nUemROW09? MkDHbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> NUTlbFlPOjJ6MkmwPVQ>
KM-H2 M1XlV2Z2dmO2aX;uJGF{e2G7 M{XoNVAvOS9yLkWvNU82KM7:TR?= MVq3NwKBkWh? NHHEPHRFVVOR NV62dnllcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NFn3V|YzOjh{OUC5OC=>
L-540 MoXnSpVv[3Srb36gRZN{[Xl? MYqwMlEwOC53L{GvOUDPxE1? MWW3NwKBkWh? MWjEUXNQ MnvjbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MmK1NlI5OjlyOUS=
HD-LM2 MnPjRZBweHSxc3nzJGF{e2G7 M1vUOlEwPSEQvF2= NYi4c2M4PzMkgJno MnTTSG1UVw>? MnjvbY5lfWOnczDhdI9xfG:|aYO= M2HUbVIzQDJ7MEm0
L-428 M2HjemFxd3C2b4Ppd{BCe3OjeR?= M2\Ld|EwPSEQvF2= NI\1SJk4OuLCiXi= NUXRXpRrTE2VTx?= NVPPXXFScW6mdXPld{BieG:ydH;zbZM> MWWyNlgzQTB7NB?=
KM-H2 NIXPR5dCeG:ydH;zbZMhSXO|YYm= MYixM|Uh|ryP MnTEO|LjiImq NYK1V5BLTE2VTx?= M2W2[Ilv\HWlZYOgZZBweHSxc3nz NGXhXFEzOjh{OUC5OC=>
L-540 MX\BdI9xfG:|aYOgRZN{[Xl? NV\aPVdHOS93IN88US=> MnXNO|LjiImq NEPZcpRFVVOR MUjpcoR2[2W|IHHwc5B1d3Orcx?= NITHbZEzOjh{OUC5OC=>
U251-MG M3\JfWZ2dmO2aX;uJGF{e2G7 M4XacVEhyrWP MVywMVE3KGh? NXq5SWlwcW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NWL1cZNZOjJyMke2PVE>
U87-MG NYX4VpN[TnWwY4Tpc44hSXO|YYm= M{exclEhyrWP NGTHbXUxNTF4IHi= NIX2OVVqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? NX;YZmt5OjJyMke2PVE>
4C8 MWjGeY5kfGmxbjDBd5NigQ>? M1jSZVEhyrWP NEPVVIExNTF4IHi= NYPVNGo{cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w NXTIfGE1OjJyMke2PVE>
U251-MG NHjGfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFuyU2UyNzFyINM1US=> NWfyN2p{OjRxNEivO|IhcA>? MVvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NYWwPXdGOjJyMke2PVE>
U87-MG NYjIUYpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjhcmJ1OS9zMDFCuW0> NIm5eIozPC92OD:3NkBp NHnSRmZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>? MmPGNlIxOjd4OUG=
4C8 NI\wUJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHj[Yt2OS9zMDFCuW0> MVmyOE81QC95MjDo NYfBd5d1cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? MXuyNlAzPzZ7MR?=
U266 M1va[mFxd3C2b4Ppd{BCe3OjeR?= NYfkcIszOC53LUKg{txO NWP6RoVCPDhxN{KgbC=> MojBbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NX;3b|FqOjFzNkS1NVc>
Kms.11 NX7O[WdYSXCxcITvd4l{KEG|c3H5 MmXBNE42NTJizszN M{X4O|Q5Nzd{IHi= NWK1VGVmcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> Mn;WNlEyPjR3MUe=
8226 MWXBdI9xfG:|aYOgRZN{[Xl? M{LHclAvPS1{IN88US=> Mo\oOFgwPzJiaB?= MkHYbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NUnIbHl3OjFzNkS1NVc>

... 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]
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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
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*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
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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID