AG-490 (Tyrphostin B42)

Catalog No.S1143 Synonyms: Zinc02557947

AG-490 (Tyrphostin B42) Chemical Structure

Molecular Weight(MW): 294.30

AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

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6 Customer Reviews

  • Increased expression of VEGF and p-STAT3 induced by CXCL1 was blocked by either AG490 or SB225022 in AGS cells.

    Cancer Letters, 2015, 359(2): 335-43 . AG-490 (Tyrphostin B42) purchased from Selleck.

    Pre-treatment with AG490 and PD98059 alone or in combination leads to significant decrease in spheroid formation and number compared with PRL treatment alone.

    Carcinogenesis, 2014, 35(4): 795-806 . AG-490 (Tyrphostin B42) purchased from Selleck.

  • IL6 normally induces WASF3 expression in MDA231 cells, but co-treatments with AG490 (a pan-JAK inhibitor) show a dose-dependent reduction of both WASF3 levels and activated STAT3 levels.

    Carcinogenesis 2013 34, 1994-9. AG-490 (Tyrphostin B42) purchased from Selleck.

    Inhibition of JAK1/2 with AG490 or STAT3 with S3I-201 leads to reduced STAT3 activation and reduced WASF3 levels. In contrast, treatment with Dasatinib (SRC inhibitor) or Gefitinib (EGFR inhibitor) does not significantly affect activated STAT3 or WASF3 levels

    Carcinogenesis 2013 34, 1994-9. AG-490 (Tyrphostin B42) purchased from Selleck.

  • Prostate 2013 73(3), 267-77. AG-490 (Tyrphostin B42) purchased from Selleck.

    Biochem Biophys Res Commun 2013 435(4), 533-9. AG-490 (Tyrphostin B42) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
Targets
EGFR [1]
(Cell-free assay)
0.1 μM
In vitro

AG-490 inhibits HER-2 driven cell proliferation with IC50 of 3.5 μM. [1] Corresponding to the specific dose-dependent inhibition of constitutively activated JAK2 in pre-B acute leukemia (ALL) cells, AG-490 (5 μM) almost completely blocks the growth of all ALL cells by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 does not inhibit the activities of Lck, Lyn, Btk, Syk, and Src. [2] AG-490 (60-100 μM) blocks the constitutive activation of Stat3sm, and inhibits spontaneous as well as interleukin 2-induced growth of mycosis fungoides (MF) tumor cells with IC50 values of 75 μM and 20 μM, respectively. [3] AG-490 potently inhibits IL-2-mediated human T cell growth with an IC50 of 25 μM by blocking the activities of JAK3 and STAT5a/b. [4] Although AG-490 alone has no effect on proliferation of FDrv210H cells at a concentration of 5 μM, AG-490 can synergize with STI571 to enhance its inhibitory effect on p210bcr-abl driven proliferation. [5] AG-490 significantly inhibits the constitutive activation of Stat3 in MOPC, MPC11, and S194 cells, leading to dramatic dose-dependent apoptosis. [6] AG-490 (100 μM) inhibits Akt phosphorylation, inhibits the activation of nuclear factor-κB, and causes the activation of GSK-3β, leading to the reduction of c-Myc. AG-490 (50 μM) can induce apoptosis of imatinib-resistant BaF3 cells expressing T315I and E255K mutants of Bcr-Abl. [7] AG-490 at 30 μM inhibits not only Epo-induced phosphorylation of wild-type JAK2 but also constitutive phosphorylation of the JAK2 V617F mutant. AG-490 also potently inhibits cytokine-independent cell growth induced by the JAK2 V617F mutant in BaF3 cells. [8]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BC3 Ml7kSpVv[3Srb36gRZN{[Xl? Ml;SNVAx6oDLwsXN NIO3RnkzPCCq MYXt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= NGr4Um8zPjF6NEm5PS=>
BCBL1 M4j1WGZ2dmO2aX;uJGF{e2G7 M3WyelExOOLCidM1US=> MXeyOEBp NVTrNo5WdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ M1HzTVI3OTh2OUm5
BC3 Mln1SpVv[3Srb36gRZN{[Xl? NHnuWXcyODEkgJpCuW0> MWKyOEBp MW\t[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YyKHKnZIXjeIlwdg>? NYja[oJQOjZzOES5PVk>
BCBL1 MojMSpVv[3Srb36gRZN{[Xl? NGPZWVQyODEkgJpCuW0> NIHKPGczPCCq NIfNUYlu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= NEXqUYQzPjF6NEm5PS=>
BC3 NUDRSpgxTnWwY4Tpc44hSXO|YYm= M3LYS|ExOOLCidM1US=> NIrSdGszPCCq NEOxSpBqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> NWXGXnFjOjZzOES5PVk>
BCBL1 MoTkSpVv[3Srb36gRZN{[Xl? NGHsU5cyODEkgJpCuW0> MkTxNlQhcA>? MU\pcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= M2X0S|I3OTh2OUm5
SK-MEL-28 MnPySpVv[3Srb36gRZN{[Xl? NWThOZlsPTBxMUCw5qCKyrWP Ml32OFghcA>? M4\J[2ROW09? NXrnN5NEemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> M1\VdVI2OjF4NUKy
MeWo M1jSeWZ2dmO2aX;uJGF{e2G7 NHezWm02OC9zMEFihKnDvU1? M136PVQ5KGh? M4HEbWROW09? NUjSZ3pPemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> Ml7ZNlUzOTZ3MkK=
SK-MEL-5 MlG3SpVv[3Srb36gRZN{[Xl? NVKzXm52PTBxMUCw5qCKyrWP MoP5OFghcA>? M{WwZmROW09? M{n2[JJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NXnNWY5QOjV{MU[1NlI>
SK-MEL-2 MoHXSpVv[3Srb36gRZN{[Xl? MYm1NE8yODEkgJpCuW0> NGrxcoc1QCCq MX;EUXNQ NE\2VoVz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MX2yOVIyPjV{Mh?=
B16-F0 NXjBO5dMTnWwY4Tpc44hSXO|YYm= NGnkOGc2OC9zMEFihKnDvU1? NUnrbYV1PDhiaB?= MV3EUXNQ M2K1N5Jm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NU\PVINnOjV{MU[1NlI>
TRPM2/HEK  Mne2SpVv[3Srb36gRZN{[Xl? M2LNWlAvOeLCk{K1xsDDvU1? NVXyUZNuOTYEoH3pci=> MXvEUXNQ NWHjN5FKemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCxMlfDqML3TR?= NUDrRWxROjVzN{m1O|Q>
U937  MkDtSpVv[3Srb36gRZN{[Xl? NHvjeXUxNjIkgKOyOeKhyrWP M1LLelE2yqCvaX6= NWqyU4xiTE2VTx?= MlS2doVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? MlfRNlUyPzl3N{S=
TRPM2/HEK  MWTGeY5kfGmxbjDBd5NigQ>? NX7WSYdtOTEEoNM1US=> NGXIV481OMLibXnu NILOWlVFVVOR MmTKdoVlfWOnczDUVnBOOiCjY4TpeoF1cW:wIHX2[Y4h[XRiaHnnbEBkd26lZX70doF1cW:wczDv[kBJOk9{ M3WyT|I2OTd7NUe0
GL37  MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWO2V2pyOC1zMNMgxtVO M2jtWVQ5KGh? MYPzeZBxemW|c3XzJGxiKGW6cILld5Nqd25? MYGyOFk6QTZ3Nx?=
NRK-52E NWfj[481TnWwY4Tpc44hSXO|YYm= MkPYNeKhyrWP NXHDb5E6OTBibXnu MlvDZoxw[2u|IITo[UB{fGmvdXzheI9zgSCnZn\lZ5Qhd2ZiQX7nJGlKKG:wIGDhfE0zKGW6cILld5Nqd28EoB?= NU\Db2hIOjR5MUC0NlM>
NRK-52E NUH3[YVLTnWwY4Tpc44hSXO|YYm= Mk\yNeKhyrWP M2rsZlExKG2rbh?= NFz6b2RjdG:la4OgRY5oKEmLIHnu[JVk\WRiQ1SyOEBmgHC{ZYPzbY9v NHHUfZAzPDdzMESyNy=>
HSC  Ml;WSpVv[3Srb36gRZN{[Xl? NWLHbG9nOjBizszN MYqxJIg> Mkj5ZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= M1nuSFI1PjF2MUm5
EJ MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW1NE85OCEQvF2= M2f6cVI1NzR6L{eyJIg> MkmxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHP2[48zPDV6N{C0PS=>
EJ MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPlbmFlPTBxOECg{txO NVeyTXVkPDhiaB?= NVfkV5VV[2G3c3XzJHMueGijc3WgZZJz\XO2 NHjqNHYzPDV6N{C0PS=>
EJ NELYdINHfW6ldHnvckBCe3OjeR?= Mn;ZOVAwQDBizszN MYG0PEBp NFTyR3Jld3ewcnXneYxifGW|IHOtUZlkNCCleXPsbY5FOSxic4Xyeol3cW5iYX7kJHZGT0ZiZYjwdoV{e2mxboO= NGDUOGczPDV6N{C0PS=>
HepG2 M37pV2Z2dmO2aX;uJGF{e2G7 MnPFOVAuPTByIN88US=> NEHFXGg3OMLibXnu NWjDXHg3cW6qaXLpeJMhfGinIFnMMVYucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEGgLHR6ejdyNTmgZY5lKFOWQWSzJEhVgXJ5MEWpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NEDHfJMzPDJ2MkC0Oi=>
SGC7901 NXLibYJHS2WubDDWbYFjcWyrdImgRZN{[Xl? NIfTRlIxNTFyMDFOwG0> NFjwWnczPC92OD:3NkBp NH\ZOmhk[XW|ZYOgZUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliZH;z[U1l\XCnbnTlcpRtgSCkdYSgco91KHSrbXWt[IVx\W6mZX70cJk> NUjqfpZpOjRzNUGyOVU>
AGS  M1HkZWNmdGxiVnnhZoltcXS7IFHzd4F6 MVewMVExOCEQvF2= NEDOR5EzPC92OD:3NkBp M1:1SoNifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> NITobW0zPDF3MUK1OS=>
SGC7901 MkH2SpVv[3Srb36gRZN{[Xl? NFLYT4M2OCEQvF2= MmPLNlQwPDhxN{KgbC=> NYTjelU5fGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> MlGyNlQyPTF{NUW=
AGS  NYrjeWpGTnWwY4Tpc44hSXO|YYm= MUW1NEDPxE1? Mo\UNlQwPDhxN{KgbC=> NFfIO3h1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> NELwcZMzPDF3MUK1OS=>
SGC7901 MWrGeY5kfGmxbjDBd5NigQ>? MnjqOVAh|ryP M3HRclI1NzR6L{eyJIg> NV3jc5hnfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? NYPYemdMOjRzNUGyOVU>
AGS  NYPkT|N6TnWwY4Tpc44hSXO|YYm= NXe0WIpQPTBizszN Mmq0NlQwPDhxN{KgbC=> MVn0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> M4nlPFI1OTVzMkW1
MC3T3-E1  MXrGeY5kfGmxbjDBd5NigQ>? Ml3IOVAh|ryP NInQZm01KGh? NIHsTGZqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> M3Pnc|I{QDd5N{O0
7TD1-DXM M{T4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TVc|ExKM7:TR?= NF:wfVc4OiCq MnH3SG1UVw>? M13oO4lvcGmkaYTzJINmdGxiZ4Lve5Rp MYmyN|g4OTF3OR?=
7TD1-WD-90 NH7ySVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrOeJIyOCEQvF2= MkjRO|IhcA>? Mom5SG1UVw>? Mn3DbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlXDNlM5PzFzNUm=
7TD1-DXM NEDrRplCeG:ydH;zbZMhSXO|YYm= Mn\KOVAh|ryP M33xN|Q5KGh? NWPmeGR3TE2VTx?= MYnpcoR2[2W|IHHwc5B1d3Orcx?= M2TkS|I{QDdzMUW5
7TD1-WD-90 MlnFRZBweHSxc3nzJGF{e2G7 MojtOVAh|ryP M4nMRlQ5KGh? M1zrV2ROW09? Ml:1bY5lfWOnczDhdI9xfG:|aYO= MVKyN|g4OTF3OR?=
7TD1-WD-90  NUL2cYI5TnWwY4Tpc44hSXO|YYm= NWroWJVpPTBizszN MlfzOkBp M4XYOWROW09? M1vyfZNq\26rZnnjZY51dHliaX7obYJqfHNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBLSUt{IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEO= MX6yN|g4OTF3OR?=
HepG2  M3ruUmZ2dmO2aX;uJGF{e2G7 M3njNVExOCEQvF2= MYSxNk8zPCCq MVrpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MWmyN|g{PjRyMB?=
RAW264.7  M13tVWZ2dmO2aX;uJGF{e2G7 MXe1NOKh|ryPwrC= M3v1UVI1NzR6IHi= MXvzeZBxemW|c3XzJHJCVkuOLXnu[JVk\WRib4P0[Y9kdGG|dH;n[Y5me2m| MX6yN|Y3PTBzOB?=
RAW264.7 NHfaNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTRNE02OMLizszNxsA> MUO0POKhcA>? MlXjbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> MYmyN|Y3PTBzOB?=
RAW264.7 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGSzVpIxNTVywrFOwG3DqA>? M13KSlQ5yqCq MU\jZZV{\XNiYX6gZZJz\XO2IH;mJHJCXzJ4ND63JINmdGy|IHH0JJRp\SCJMD;HNUBxcGG|ZTDv[kB1cGViY3XscEBkgWOuZR?= NVLHc5NyOjN4NkWwNVg>
RAW264.7 NEnreWdHfW6ldHnvckBCe3OjeR?= M3LsdFUxyqEQvF2= M2HaVlI1NzR6IHi= NVPRbpNXcW6qaXLpeJMhWkGQS1ytbY5lfWOnZDDOSmFV[zFiZYjwdoV{e2mxbjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOnckeyO3NVSVR| MVGyN|Y3PTBzOB?=
A549  NF;tOHNHfW6ldHnvckBCe3OjeR?= NI\kOHUzOC92MDFOwG0> NGT1N4wzOCCq NIqyfXozOCEQvF2gRWc1QTBic4XwdJJme3OnczD0bIUhemGmaXH0bY9vNWmwZIXj[YQhcW64YYPpc44hd2ZiQUW0PUBk\Wyucx?= NXvLcWwxOjN4MkCxPVE>
A549  MlrxSpVv[3Srb36gRZN{[Xl? NVLXWpZQOTBxMkCvOFAh|ryP MVeyOEBp NVjRfZZxe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> NF3Sb4gzOzZ{MEG5NS=>
HUVECs MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXqyNEDDvU1? M3;pblQhcA>? NEHIXlZifHSnboXheIV{KEh{T{KtbY5lfWOnZDDj[YxtKHOqcnnub4Fo\SCjbnSgbY1xem:4ZXSgeIhmKGG2dHHjbI1mdnRicnH0[UBw\iC2aHWgZ4VtdHN? NHzzVWYzOzR6M{m0Oi=>
HUVECs M4X2XmFxd3C2b4Ppd{BCe3OjeR?= M2G2bFIxKML3TR?= NY\ORpBbPCCq NIDrWXl{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? MnL2NlM1QDN7NE[=
BV-2  NF75OpJHfW6ldHnvckBCe3OjeR?= NVW4e5p6OjBiwsXN NIDjcXcyPiCq Mm\ObY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> MnrJNlMzOzZ|N{C=
NRK-52E  NGXkNIVHfW6ldHnvckBCe3OjeR?= NYHOPWNnPcLizszN NWn2R3pzOzEEoH3pci=> NXn0O5Ex[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? MUmyN|E4PDd3Nx?=
SW620  MkmzSpVv[3Srb36gRZN{[Xl? NFHVeHQzOCEEtV2= NUf6Tm5UOS94IHi= MkXubY5pcWKrdIOgdE1UXEGWMzDhZ5RqfmG2aX;u MnroNlMyOTB4MkW=
RPE  NWX4cYluTnWwY4Tpc44hSXO|YYm= NVfYTmx3OzBiwsXNxsA> MlfVN{Bp NYPBS4M{cW6qaXLpeJMhfGinIHnu[JVkfGmxbjDv[kBxNVOWQWSzJIV5eHKnc4Ppc44> Ml:zNlMxQTRyNke=
SW1116 M2rDPGZ2dmO2aX;uJGF{e2G7 M3P2OVExOCEEtV5CpC=> MlqzNlQwPDhxN{KgbC=> MXHk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? NWPuRYlqOjJyNUC3PVA>
HT29 MlO4SpVv[3Srb36gRZN{[Xl? M4nGeFExOCEEtV5CpC=> NV;YdZpwOjRxNEivO|IhcA>? NGPHSldl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= M2DHZlIzODVyN{mw
SW1116 NVLZWXVWTnWwY4Tpc44hSXO|YYm= MmPwNVAxKML3TdMg NV25fodQOjRxNEivO|IhcA>? Mnyw[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> MWSyNlA2ODd7MB?=
HT29 M4jVW2Z2dmO2aX;uJGF{e2G7 NUnsTIlCOTByINM1UeKh NHfyd3QzPC92OD:3NkBp MoHT[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> NHPNdHUzOjB3MEe5NC=>
ARPE-19 M2XJR2Z2dmO2aX;uJGF{e2G7 MUS1xsDPxE1? MXmzNOKhdWmw NFv5VVJqdmirYnn0d{BLSUt{IIDoc5NxcG:{aXzheIlwdg>? MVeyNVYzODl4Mx?=
HSC-T6 M1rvU2Fxd3C2b4Ppd{BCe3OjeR?= NUPhfXp2OTEEoN88US=> NYHwTY96OsLiaNMg MnXDbY5pcWKrdIOgeIhmKGGyb4D0c5NqeyCxZjDIV2MuXDZiY3XscJMhcW6mdXPl[EBjgSCFRFW= M1PHOFIyOzl4OUm4
HSC-T6 MkTkSpVv[3Srb36gRZN{[Xl? MWWxNOKh|ryP NGSwcXczyqCqwrC= NEm1W2RqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= NV74S2Z6OjF|OU[5PVg>
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A-172 M4LS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLMOVAwOTBywrFOwG0> NULndlkyPDhiaB?= NF;Pe4pt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= NEG3NFYzODV6OUWyOS=>
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MZ-18 MVzGeY5kfGmxbjDBd5NigQ>? NETJO4g2OC9zMEFCpO69VQ>? NXHwdVFjPDhiaB?= NVLx[Ic4cW6qaXLpeJMhdWmpcnH0bY9v MoLVNlA2QDl3MkW=
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MZ-256 NG\0WYdHfW6ldHnvckBCe3OjeR?= MYG1NE8yODEEoN88US=> M1ntSVQ5KGh? MnP5bY5pcWKrdIOgcYloemG2aX;u NGDu[FkzODV6OUWyOS=>
MZ-304 NFHEb2FHfW6ldHnvckBCe3OjeR?= MojHOVAwOTBywrFOwG0> NXLKRZFrPDhiaB?= M4PyOIlvcGmkaYTzJI1q\3KjdHnvci=> NEPiN5YzODV6OUWyOS=>
A-172 NH;ndHdHfW6ldHnvckBCe3OjeR?= Mn;SNVAxyqEQvF2= Mn7KOFghcA>? MYTpcohq[mm2czDpcpZie2mxbh?= MYqyNFU5QTV{NR?=
MZ-18 MXvGeY5kfGmxbjDBd5NigQ>? NYHzTmlPOTBywrFOwG0> NGjFfIk1QCCq NWjtSXZQcW6qaXLpeJMhcW64YYPpc44> MmHhNlA2QDl3MkW=
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MZ-304 NGntN2xHfW6ldHnvckBCe3OjeR?= NV3ORpNIOTBywrFOwG0> M{jYdVQ5KGh? NYLYVlAxcW6qaXLpeJMhcW64YYPpc44> MViyNFU5QTV{NR?=
A-172 M2TvdmZ2dmO2aX;uJGF{e2G7 M1\xV|UxNzFyMNMg{txO M4DmNlQ5KGh? MV3y[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz Mly1NlA2QDl3MkW=
MZ-18 NEDW[pdHfW6ldHnvckBCe3OjeR?= MmTUOVAwOTBywrFOwG0> NUmzR4JiPDhiaB?= MVry[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz MWmyNFU5QTV{NR?=
MZ-54 NFfhTm5HfW6ldHnvckBCe3OjeR?= M2XEXlUxNzFyMNMg{txO MVm0PEBp MV3y[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NFOwSVYzODV6OUWyOS=>
MZ-256 M1;IZWZ2dmO2aX;uJGF{e2G7 M3fwV|UxNzFyMNMg{txO MnqzOFghcA>? NFHQWZNz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MkXTNlA2QDl3MkW=
MZ-304 NFTn[lBHfW6ldHnvckBCe3OjeR?= MWi1NE8yODEEoN88US=> MnHBOFghcA>? M3zDXJJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> NEfY[mYzODV6OUWyOS=>
SW1990 NFvZWGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSyNEDPxE1? MWqyOE81QC95MjDo MlXubY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NUXTU3NIOjB2OEK4OVg>
SW1990 M2CwXmZ2dmO2aX;uJGF{e2G7 M2\SfFIxKM7:TR?= NI[zfFQzPCCq NY\uflVT\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE2PUD2yJIFv\CCYRVfGJI1TVkG| M3f5SlIxPDh{OEW4
SW1990 MlLGSpVv[3Srb36gRZN{[Xl? NGLnXIwzOCEQvF2= MUCyOEBp M3rmTIRm[3KnYYPld{B1cGViaX70[Y5{cXS7IH;mJJAuW3SjdEOg[ZhxemW|c3nvci=> NHjZW3kzODR6Mki1PC=>
SW1990 M3L1XGlvfmG|aX;uJGF{e2G7 NEm5[VUzOCEQvF2= NVPIRnZHOjRiaB?= MlWxdoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= NHfYS4EzODR6Mki1PC=>
THP1 M2iwemZ2dmO2aX;uJGF{e2G7 NV;hTHdjOTBidV2= MUSzNEBucW8EoB?= NHH1PG9qdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= MlnZNlA{QTN4OUC=
BMMC MX7GeY5kfGmxbjDBd5NigQ>? NVrMWW01OC1zMDFOwG0> M1ftS|E2yqCvaX6= MkDMbY5pcWKrdIOgUHREPMLicnXs[YF{\SCrbjDhJIRwe2VvZHXw[Y5l\W62IH\hd4hqd25id3n0bEBv\WG{IHPvcZBt\XSnIHnubIljcXSrb36gZZQh[2:wY3XueJJifGmxboOg5sm,OTEEoN88US=> MX6xPVg{PTh2NR?=
A549 MmS1SpVv[3Srb36gRZN{[Xl? M3nwdVE2KM7:bR?= Ml71NUBp M1vBS4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiU2TBWFEhd25idInyc5NqdmViN{CxJJdieyCmZYTlZ5Rm\CBzNTDtbY4h[W[2ZYKgV3BGKEJidILlZZRu\W62 NGn0VWcyQThyMU[2OS=>
OVCAR-3 MUXGeY5kfGmxbjDBd5NigQ>? NV72V2lVOTBidV2= MluxNUBp M1z1SIlvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= M{f0S|E6PjR5M{[z
PA-1 MWPGeY5kfGmxbjDBd5NigQ>? M17RSFExKHWP NUfzbIgzOSCq Mn32bY5pcWKrdIOgUHBCNWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w Mn\qNVk3PDd|NkO=
OVCAR-3 MlTRSpVv[3Srb36gRZN{[Xl? MnrwNVAhfU1? Mn\wNUBp MWfpcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? NWrBb3RkOTl4NEezOlM>
PA-1 MnfJSpVv[3Srb36gRZN{[Xl? NWPxSGRJOTBidV2= M1\5SVEhcA>? M3\UcolvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 NVy1cnZsOTl4NEezOlM>
Jurkat  NF\IbGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XXR|UxKM7:TR?= MYSyOE81QC95MjDo NET2[JFmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NV;yPG9LOTl3NkS4PVE>
SUPT1  MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXLOVAh|ryP NXqyNnhzOjRxNEivO|IhcA>? MlHN[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u NGfMSIgyQTV4NEi5NS=>
Jurkat  MWfBdI9xfG:|aYOgRZN{[Xl? NXGybFVTPTBizszN M4nMWFI1NzR6IHi= M3HqdoVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBieG:ydH;zbZM> M4\TUFE6PTZ2OEmx
SUPT1  MlXmRZBweHSxc3nzJGF{e2G7 MWK1NEDPxE1? MWGyOE81QCCq MX7lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz M3m1UlE6PTZ2OEmx

... Click to View More Cell Line Experimental Data

In vivo Administration of AG-490 drastically reduces the numbers of CD45+ and HLA-DR+ cells from 48 % and 46% in bone marrow of untreated mice, as well as 38% and 22% in the spleen of untreated mice to undetectale levels. [2] In vivo administration of AG-490 causes murine myeloma tumor cell apoptosis but does not inhibit IL-12-mediated macrophage activation and IFN-γ production by lymphocytes. [6] Consistent with the in vitro blocking of JAK2 V617F mutant activity, AG-490 treatment at 0.5 mg/day for 10 days effectively inhibits JAK2 V617F mutant-induced tumorigenesis and tumor cell invasion in nude mice. [8] Combined therapy with AG-490 and IL-12 induces greater antitumor effects than either agent alone in a murine myeloma tumor model. [6]

Protocol

Kinase Assay:

[1]

+ Expand

In vitro kinase autophosphorylation:

AG-490 is dissolved in DMSO 10%-H2O-ethanol 45%. Crude membrane extracts (0.125 μg/mL) are preactivated with EGF (20 nM) in 50 mM HEPES buffer, pH 7.6, and 125 mM NaCl, for 15 minutes at 4 °C. Autophosphorylation activity of EGFR or ErbB2 kinase is assayed at 4 °C for 30 seconds in V-shaped 96-well plates. Membrane extracts (8 μL) are added to each well containing reaction mixture (12 μL, 50mM, HEPES, pH 7.4,125 mM NaCl, 12 mM M8Ac2, 2 mM MnCl2, 1 mM NaVO3, 1 μM ATP, and 1 μCi[γ-32P]ATP, final concentrations) and increasing concentrations of AG-490 (4 μL). After termination by addition of hot sample buffer, the samples are run on a 6% SDS-polyacrylamide gel electrophoresis minigel, the gels dried, and autoradiography performed during the linear exposure time period. The receptor bands are scanned densitrometrically, and the results analyzed by the Ez-Fit program. For the analysis of autophosphorylation of JAK2, JAK2 is immunoprecipitated by using anti-JAK2 antibody from lysates of G2 cells pretreated for 16 hours with increasing concentrations of AG-490 (0-50 μM). Immune complexes are then immunoblotted with anti-phosphotyrosine antibody. A dose-dependent inhibition of in vitro kinase activity is demonstrated by assessing JAK2 autophosphorylation.
Cell Research:

[2]

+ Expand
  • Cell lines: Pre-B ALL
  • Concentrations: Dissolved in DMSO, final concentrations ~ 50 μM
  • Incubation Time: 16 hours
  • Method:

    Cells are exposed to different concentrations of AG-490 for 16 hours. For the determination of cell proliferation, [3H]tymidine (1 μCi) is added 6 hours or more before the cultures are terminated. Cells are then collected and samples counted in a liquid scintillation counter.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: SCID mice intravenously injected with ALL cells
  • Formulation: Dissolved in DMSO
  • Dosages: 0.85 mg + 0.5 mg daily
  • Administration: Continuous pump infusion supplemented with daily intraperitoneal injections
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 58 mg/mL (197.07 mM)
Ethanol 6 mg/mL (20.38 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+45% PEG 300+ddH2O
15mg/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 294.30
Formula

C17H14N2O3

CAS No. 133550-30-8
Storage powder
Synonyms Zinc02557947

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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

Frequently Asked Questions

  • Question 1:

    I would like to know whether AG490 (S1143) goes to CNS through BBB, or not?

  • Answer:

    AG-490 can go through the BBB. You can see this reference: http://bloodjournal.hematologylibrary.org/content/111/4/2062.full.html.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID