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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In DMSO USD 70 In stock
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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 NFTnfoxHfW6ldHnvckBCe3OjeR?= M1rvV|ExOOLCidM1US=> NInMcVkzPCCq MXjt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= MkXGNlYyQDR7OUm=
BCBL1 MVrGeY5kfGmxbjDBd5NigQ>? NUH2cZFWOTBy4pEJxtVO NV;oRnFKOjRiaB?= NIXXZmNu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> MkPuNlYyQDR7OUm=
BC3 Mke3SpVv[3Srb36gRZN{[Xl? MmnkNVAx6oDLwsXN M3\LSVI1KGh? MorGcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? NWWydWRyOjZzOES5PVk>
BCBL1 MUnGeY5kfGmxbjDBd5NigQ>? Mn;DNVAx6oDLwsXN M4C5[|I1KGh? M13jZo1m\GmjdHXzJIRmNXCqb4PwbI9zgWyjdHnvckBw\iCVVFHUN{Bkd3K{ZXzheIVlKHerdHigTHNRPzBiYX7kJGhUTjJicnXkeYN1cW:w MXiyOlE5PDl7OR?=
BC3 MofFSpVv[3Srb36gRZN{[Xl? NVjvWG16OTBy4pEJxtVO MknXNlQhcA>? NW\Ue3RxcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh NFfHWYozPjF6NEm5PS=>
BCBL1 NGDUXnlHfW6ldHnvckBCe3OjeR?= MlrwNVAx6oDLwsXN M{G2[lI1KGh? M{\Ecolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKG[udYlCpC=> MVGyOlE5PDl7OR?=
SK-MEL-28 NILpbHZHfW6ldHnvckBCe3OjeR?= NFvrVYY2OC9zMEFihKnDvU1? M{fNZVQ5KGh? NI\tV3JFVVOR MVTy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MmfNNlUzOTZ3MkK=
MeWo Mmi5SpVv[3Srb36gRZN{[Xl? NXH1b2t5PTBxMUCw5qCKyrWP NHfabGQ1QCCq MVLEUXNQ MnS2doVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= M3PJWVI2OjF4NUKy
SK-MEL-5 NFvDUYJHfW6ldHnvckBCe3OjeR?= M{HXeVUxNzFyMPMAjeK2VQ>? MmfEOFghcA>? MoewSG1UVw>? MVvy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= NUD5WWM6OjV{MU[1NlI>
SK-MEL-2 MXvGeY5kfGmxbjDBd5NigQ>? M37vSFUxNzFyMPMAjeK2VQ>? MVe0PEBp NHrvPYxFVVOR NIS2fJBz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MX[yOVIyPjV{Mh?=
B16-F0 MkPGSpVv[3Srb36gRZN{[Xl? M1vrclUxNzFyMPMAjeK2VQ>? NXT6bWtwPDhiaB?= MXvEUXNQ NWewdVdiemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MV6yOVIyPjV{Mh?=
TRPM2/HEK  MVHGeY5kfGmxbjDBd5NigQ>? MWKwMlHjiJN{NdMgxtVO MWSxOeKhdWmw M1zQZmROW09? MnHJdoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyBzLkhCpOK2VQ>? NWSyO3NsOjVzN{m1O|Q>
U937  MWjGeY5kfGmxbjDBd5NigQ>? NHu3fHIxNjIkgKOyOeKhyrWP M1XRfFE2yqCvaX6= NHjM[nNFVVOR MUXy[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDBwNNMgxtVO NFPjVWkzPTF5OUW3OC=>
TRPM2/HEK  MXrGeY5kfGmxbjDBd5NigQ>? Mnj3NVDDqML3TR?= MUG0NOKhdWmw MWnEUXNQ NXzibI5YemWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y MWmyOVE4QTV5NB?=
GL37  NUHtPYtlS2WubDDWbYFjcWyrdImgRZN{[Xl? NVP2OWM6OC1zMNMgxtVO M1;zT|Q5KGh? MXHzeZBxemW|c3XzJGxiKGW6cILld5Nqd25? M3rkWFI1QTl7NkW3
NRK-52E MmPlSpVv[3Srb36gRZN{[Xl? NIfRSI8yyqEEtV2= M1vYV|ExKG2rbh?= MX;icI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi M{nuSFI1PzFyNEKz
NRK-52E MVHGeY5kfGmxbjDBd5NigQ>? MVWxxsDDvU1? M3vFSlExKG2rbh?= MmmyZoxw[2u|IFHu[{BKUSCrbnT1Z4VlKEOGMkSg[ZhxemW|c3nvci=> MXeyOFcyODR{Mx?=
HSC  MWDGeY5kfGmxbjDBd5NigQ>? MWeyNEDPxE1? M1;zd|EhcA>? MnP1ZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= MWOyOFYyPDF7OR?=
EJ MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fT[|UxNzhyIN88US=> NHqycpkzPC92OD:3NkBp Mo[2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NV;QWlEyOjR3OEewOFk>
EJ MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVO1NE85OCEQvF2= MVm0PEBp MnT6Z4F2e2W|IGOtdIhie2ViYYLy[ZN1 NGO0XIEzPDV6N{C0PS=>
EJ MnT3SpVv[3Srb36gRZN{[Xl? MYS1NE85OCEQvF2= MoXnOFghcA>? M2\LNIRwf26{ZXf1cIF1\XNiYz3NfYMtKGO7Y3zpcmQyNCC|dYL2bZZqdiCjbnSgWmVITiCneIDy[ZN{cW:wcx?= M2XCXVI1PTh5MES5
HepG2 M17CPWZ2dmO2aX;uJGF{e2G7 NXrkXXlsPTBvNUCwJO69VQ>? NED5ZoU3OMLibXnu NH7SVHJqdmirYnn0d{B1cGViSVytOk1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTCoWJlzPzB3KTDhcoQhW1SDVEOgLHR6ejdyNTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NUTmVHNGOjR{NEKwOFY>
SGC7901 NVnQ[|RiS2WubDDWbYFjcWyrdImgRZN{[Xl? NYX1flZDOC1zMECg{txO MmjWNlQwPDhxN{KgbC=> MXjjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= M2n5[|I1OTVzMkW1
AGS  NVrScYFqS2WubDDWbYFjcWyrdImgRZN{[Xl? NHPQZYQxNTFyMDFOwG0> M3PVWFI1NzR6L{eyJIg> M3jmWYNifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> NUTMbGxWOjRzNUGyOVU>
SGC7901 NWHKWYFYTnWwY4Tpc44hSXO|YYm= MofQOVAh|ryP MWKyOE81QC95MjDo MWP0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= M{LkelI1OTVzMkW1
AGS  NHrFUHdHfW6ldHnvckBCe3OjeR?= NEPtUVE2OCEQvF2= NH\lNYMzPC92OD:3NkBp NVPQNYVLfGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> M1;kelI1OTVzMkW1
SGC7901 M{m0bWZ2dmO2aX;uJGF{e2G7 NGDFe5M2OCEQvF2= M1K4TlI1NzR6L{eyJIg> MYD0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> Ml[zNlQyPTF{NUW=
AGS  M3HaUGZ2dmO2aX;uJGF{e2G7 MWW1NEDPxE1? Ml20NlQwPDhxN{KgbC=> M4rTbpRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz M{XUbVI1OTVzMkW1
MC3T3-E1  M1TtfmZ2dmO2aX;uJGF{e2G7 NUXCUJNPPTBizszN M4LjdlQhcA>? NFjDeGFqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> NI\xe4MzOzh5N{ezOC=>
7TD1-DXM NH;NSoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljXNVAh|ryP MnP6O|IhcA>? MYLEUXNQ Mn\pbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NFnsOlgzOzh5MUG1PS=>
7TD1-WD-90 MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13ue|ExKM7:TR?= NFfJ[XQ4OiCq MY\EUXNQ MVzpcohq[mm2czDj[YxtKGe{b4f0bC=> MVKyN|g4OTF3OR?=
7TD1-DXM NVjRcnFuSXCxcITvd4l{KEG|c3H5 MnzHOVAh|ryP NIfGN3g1QCCq M4i4bGROW09? NFTI[2VqdmS3Y3XzJIFxd3C2b4Ppdy=> MV[yN|g4OTF3OR?=
7TD1-WD-90 Mo[xRZBweHSxc3nzJGF{e2G7 M4\PVVUxKM7:TR?= M2S2VVQ5KGh? M2PsdGROW09? M1T3O4lv\HWlZYOgZZBweHSxc3nz M1SwT|I{QDdzMUW5
7TD1-WD-90  MWTGeY5kfGmxbjDBd5NigQ>? M1ToeFUxKM7:TR?= NEXjVos3KGh? M{S1SGROW09? NGqxe5h{cWewaX\pZ4FvfGy7IHnubIljcXS|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhUkGNMjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSz NVPUXmRSOjN6N{GxOVk>
HepG2  MlrWSpVv[3Srb36gRZN{[Xl? NV7NXHJQOTByIN88US=> NWDUZllsOTJxMkSgbC=> NETCcnhqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25? MmPDNlM5OzZ2MEC=
RAW264.7  MVfGeY5kfGmxbjDBd5NigQ>? NV\kfXNRPTEEoN88UeKh MnvyNlQwPDhiaB?= MY\zeZBxemW|c3XzJHJCVkuOLXnu[JVk\WRib4P0[Y9kdGG|dH;n[Y5me2m| M{\FdlI{PjZ3MEG4
RAW264.7 M{LndGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XS[FAuPTEEoN88UeKh MUG0POKhcA>? M3;PWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wt[IVx\W6mZX70cJk> MV6yN|Y3PTBzOB?=
RAW264.7 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vJPVAuPTEEoN88UeKh NVjlZW5LPDkEoHi= NFLRbldk[XW|ZYOgZY4h[XK{ZYP0JI9nKFKDV{K2OE44KGOnbHzzJIF1KHSqZTDHNE9IOSCyaHHz[UBw\iC2aHWgZ4VtdCCleXPs[S=> M1vPOFI{PjZ3MEG4
RAW264.7 NGeyeVhHfW6ldHnvckBCe3OjeR?= NGXudHQ2OMLizszN MnG0NlQwPDhiaB?= NWO0Xo9bcW6qaXLpeJMhWkGQS1ytbY5lfWOnZDDOSmFV[zFiZYjwdoV{e2mxbjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOnckeyO3NVSVR| MXmyN|Y3PTBzOB?=
A549  MkDoSpVv[3Srb36gRZN{[Xl? NGOzcnIzOC92MDFOwG0> Mk\HNlAhcA>? Mn3PNlAh|ryPIFHHOFkxKHO3cIDy[ZN{\XNidHjlJJJi\GmjdHnvck1qdmS3Y3XkJIlvfmG|aX;uJI9nKEF3NEmgZ4VtdHN? MmK2NlM3OjBzOUG=
A549  MWLGeY5kfGmxbjDBd5NigQ>? NIHPdVgyOC9{MD:0NEDPxE1? MV[yOEBp NVi1[21Ve3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> NIe5engzOzZ{MEG5NS=>
HUVECs MmO2R4VtdCCYaXHibYxqfHliQYPzZZk> M2DPVVIxKML3TR?= NVPjVoEzPCCq MkTLZZR1\W63YYTld{BJOk9{LXnu[JVk\WRiY3XscEB{cHKrbnvh[4Uh[W6mIHntdJJwfmWmIITo[UBifHSjY3jt[Y51KHKjdHWgc4YhfGinIHPlcIx{ MV6yN|Q5Ozl2Nh?=
HUVECs M3XJbmFxd3C2b4Ppd{BCe3OjeR?= MUSyNEDDvU1? MUG0JIg> NGDoXYJ{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? NIPIV4wzOzR6M{m0Oi=>
BV-2  MYDGeY5kfGmxbjDBd5NigQ>? Ml3PNlAhyrWP MX6xOkBp MkDmbY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> NH\5NGczOzJ|NkO3NC=>
NRK-52E  NEfsU49HfW6ldHnvckBCe3OjeR?= M1LtclXDqM7:TR?= MUKzNOKhdWmw M4DaU4F1fGWwdXH0[ZMhSW6pLTix5qCUPylvaX7obYJqfGWmIGTHSk3PujFibWLORUBifCBzNtMgbOKh MmLvNlMyPzR5NUe=
SW620  Ml\rSpVv[3Srb36gRZN{[Xl? MUKyNEDDvU1? M4fOW|EwPiCq M3rXWIlvcGmkaYTzJJAuW1SDVEOgZYN1cX[jdHnvci=> NEPoc3kzOzFzME[yOS=>
RPE  NXTNV2s2TnWwY4Tpc44hSXO|YYm= M131[|MxKML3TdMg NEjEPW0{KGh? M37kZolvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u NH3FeJUzOzB7NEC2Oy=>
SW1116 NHfKUIpHfW6ldHnvckBCe3OjeR?= M4PCbVExOCEEtV5CpC=> M3[ybFI1NzR6L{eyJIg> MoDN[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? M4rMdlIzODVyN{mw
HT29 MkOzSpVv[3Srb36gRZN{[Xl? MnLaNVAxKML3TdMg NXXBdIwxOjRxNEivO|IhcA>? Mmnz[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? MUeyNlA2ODd7MB?=
SW1116 MYrGeY5kfGmxbjDBd5NigQ>? NWf4N5c1OTByINM1UeKh NYHKR2hzOjRxNEivO|IhcA>? MUTk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> M3fDcVIzODVyN{mw
HT29 M1j6eWZ2dmO2aX;uJGF{e2G7 NYDSUVFHOTByINM1UeKh NWXjVZY6OjRxNEivO|IhcA>? Mom2[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> M1PVdlIzODVyN{mw
ARPE-19 MmX1SpVv[3Srb36gRZN{[Xl? Mnr6OeKh|ryP M3PqeVMxyqCvaX6= NIruR4pqdmirYnn0d{BLSUt{IIDoc5NxcG:{aXzheIlwdg>? M17UR|IyPjJyOU[z
HSC-T6 NUC0fnU3SXCxcITvd4l{KEG|c3H5 NFHSXVgyOMLizszN NXjjN|dnOsLiaNMg NH3ZdIRqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> M2rTTlIyOzl4OUm4
HSC-T6 M1XXVGZ2dmO2aX;uJGF{e2G7 MmnUNVDDqM7:TR?= M{jXWlLDqGkEoB?= M2i4W4lvcGmkaYTzJJRp\SCneIDy[ZN{cW:wczDv[kBxYS2VVFHUNUBidmRiQnHkJIlv\HWlZXSgZpkhS0SH M4r0XVIyOzl4OUm4
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MZ-304 M17Dfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[1NE8yODEEoN88US=> MoCyOFghcA>? NHvHNllt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= NUT0b|hxOjB3OEm1NlU>
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MZ-54 NFXEXGhHfW6ldHnvckBCe3OjeR?= M3XoVFUxNzFyMNMg{txO NXHPUYFTPDhiaB?= NVHYepppcW6qaXLpeJMhdWmpcnH0bY9v M3[5NFIxPTh7NUK1
MZ-256 MljOSpVv[3Srb36gRZN{[Xl? M2XkT|UxNzFyMNMg{txO MoLOOFghcA>? MY\pcohq[mm2czDtbYdz[XSrb36= NYL3[5JIOjB3OEm1NlU>
MZ-304 NFTLU4VHfW6ldHnvckBCe3OjeR?= MmrnOVAwOTBywrFOwG0> MkjzOFghcA>? M3\3bIlvcGmkaYTzJI1q\3KjdHnvci=> NYTwZlhOOjB3OEm1NlU>
A-172 NWnJTY1KTnWwY4Tpc44hSXO|YYm= MW[xNFDDqM7:TR?= MUe0PEBp NF3rPVRqdmirYnn0d{Bqdn[jc3nvci=> MY[yNFU5QTV{NR?=
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MZ-304 NFTx[IZHfW6ldHnvckBCe3OjeR?= MYWxNFDDqM7:TR?= MXO0PEBp NXvBU4dEcW6qaXLpeJMhcW64YYPpc44> M1yzU|IxPTh7NUK1
A-172 NXfKbZFxTnWwY4Tpc44hSXO|YYm= M3G2[|UxNzFyMNMg{txO MmruOFghcA>? NH\1bmRz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ NIrCcXEzODV6OUWyOS=>
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MZ-304 NXXhXGFZTnWwY4Tpc44hSXO|YYm= NGjTNnU2OC9zMEFCpO69VQ>? MoXBOFghcA>? Mo[2doVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> NVTNVXp{OjB3OEm1NlU>
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SW1990 MkXuTY53[XOrb36gRZN{[Xl? MmnZNlAh|ryP NU\jdmNqOjRiaB?= MmTHdoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= NYrKWFlPOjB2OEK4OVg>
THP1 MULGeY5kfGmxbjDBd5NigQ>? Mn;VNVAhfU1? M3PnblMxKG2rbtMg MYTpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44h[nlib4\ldkA3OCV? M1\CZ|IxOzl|Nkmw
BMMC NF\DNVhHfW6ldHnvckBCe3OjeR?= MXKwMVExKM7:TR?= NF3tNIoyPcLibXnu NUDBUIE4cW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? Mn3FNVk5OzV6NEW=
A549 MUnGeY5kfGmxbjDBd5NigQ>? MnLLNVUh|ryv MlT2NUBp NGL2NGNqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQyKG:wIIT5do9{cW6nIEewNUB4[XNiZHX0[YN1\WRiMUWgcYlvKGGodHXyJHNRTSCEIITy[YF1dWWwdB?= Moe0NVk5ODF4NkW=
OVCAR-3 MlnlSpVv[3Srb36gRZN{[Xl? NV3WW4trOTBidV2= MWixJIg> NYPFNlVLcW6qaXLpeJMhVFCDLXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;u M2DhUVE6PjR5M{[z
PA-1 NF7aZpNHfW6ldHnvckBCe3OjeR?= NFW3VVcyOCC3TR?= M{fWTVEhcA>? MXXpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? NYTMdnhWOTl4NEezOlM>
OVCAR-3 NWj5UnpvTnWwY4Tpc44hSXO|YYm= MoPENVAhfU1? MVmxJIg> NXPSeW9[cW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= MUWxPVY1PzN4Mx?=
PA-1 NHy3OYNHfW6ldHnvckBCe3OjeR?= MlnUNVAhfU1? NWrROpZTOSCq NYPaTXBYcW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= MUSxPVY1PzN4Mx?=
Jurkat  NEjFR2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvZOVAh|ryP NGfJUY8zPC92OD:3NkBp M2jNbIVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> NFHxWmoyQTV4NEi5NS=>
SUPT1  M2C3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXNOVAh|ryP NIjndnMzPC92OD:3NkBp NHjwZpZmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> MU[xPVU3PDh7MR?=
Jurkat  MlzWRZBweHSxc3nzJGF{e2G7 MnnPOVAh|ryP MlfxNlQwPDhiaB?= MnTl[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> NGjLbZEyQTV4NEi5NS=>
SUPT1  M3v5XGFxd3C2b4Ppd{BCe3OjeR?= NX;z[XF1PTBizszN NGjNXnYzPC92ODDo MkO0[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> M4\JOFE6PTZ2OEmx

... 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 to the product individually and in order:
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
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