AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

65 publications

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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Selleck's AG-490 (Tyrphostin B42) has been cited by 65 publications

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 NHfjNnpHfW6ldHnvckBCe3OjeR?= NHPXXYwyODEkgJpCuW0> NXrK[GtGOjRiaB?= NYniWGdldWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ NXrNUWdrOjZzOES5PVk>
BCBL1 Ml7ESpVv[3Srb36gRZN{[Xl? MlSwNVAx6oDLwsXN NH61S20zPCCq NGrs[Jdu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NEDoU24zPjF6NEm5PS=>
BC3 MUPGeY5kfGmxbjDBd5NigQ>? NEPvN5cyODEkgJpCuW0> M2PKbVI1KGh? MWHt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YyKHKnZIXjeIlwdg>? NIXqXmszPjF6NEm5PS=>
BCBL1 MmTxSpVv[3Srb36gRZN{[Xl? MVSxNFDjiIoEtV2= MkfsNlQhcA>? MlzXcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOiC{ZXT1Z5Rqd25? Ml\GNlYyQDR7OUm=
BC3 MXnGeY5kfGmxbjDBd5NigQ>? MWCxNFDjiIoEtV2= MY[yOEBp MUDpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= MYmyOlE5PDl7OR?=
BCBL1 MX7GeY5kfGmxbjDBd5NigQ>? MlzuNVAx6oDLwsXN NG\Gbo0zPCCq Mnv2bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg M371dVI3OTh2OUm5
SK-MEL-28 Ml\4SpVv[3Srb36gRZN{[Xl? M2nZb|UxNzFyMPMAjeK2VQ>? Ml7SOFghcA>? Mn7ySG1UVw>? M3nOUZJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NVjzXlhtOjV{MU[1NlI>
MeWo MV3GeY5kfGmxbjDBd5NigQ>? MmPqOVAwOTBy4pEJxtVO NYXZdop5PDhiaB?= MlftSG1UVw>? M2jOVJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NUGy[|FTOjV{MU[1NlI>
SK-MEL-5 NWTZb2xXTnWwY4Tpc44hSXO|YYm= MX61NE8yODEkgJpCuW0> NHjKfGQ1QCCq NEfEflVFVVOR NFO0eZJz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NFvvXIQzPTJzNkWyNi=>
SK-MEL-2 Ml:2SpVv[3Srb36gRZN{[Xl? M4Dk[VUxNzFyMPMAjeK2VQ>? MkSyOFghcA>? NFr3TGhFVVOR NInxfZVz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NFzQO|UzPTJzNkWyNi=>
B16-F0 MnK3SpVv[3Srb36gRZN{[Xl? MontOVAwOTBy4pEJxtVO NULo[3FpPDhiaB?= NU[yT5NVTE2VTx?= MULy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MViyOVIyPjV{Mh?=
TRPM2/HEK  MnrlSpVv[3Srb36gRZN{[Xl? NWqzUYtYOC5z4pETNlXDqML3TR?= NIK0U2wyPcLibXnu MVrEUXNQ NYfhbFZQemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCxMlfDqML3TR?= M{jTNFI2OTd7NUe0
U937  NXv0epJvTnWwY4Tpc44hSXO|YYm= NHjYW5IxNjIkgKOyOeKhyrWP MUSxOeKhdWmw NUPoXI9tTE2VTx?= MlnxdoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? NXfMcnhbOjVzN{m1O|Q>
TRPM2/HEK  M{LuWWZ2dmO2aX;uJGF{e2G7 MkHhNVDDqML3TR?= NEDlRmo1OMLibXnu MU\EUXNQ MYDy[YR2[2W|IGTSVG0zKGGldHn2ZZRqd25iZY\lckBifCCqaXfoJINwdmOnboTyZZRqd26|IH;mJGgzVzJ? Mn7vNlUyPzl3N{S=
GL37  MoL2R4VtdCCYaXHibYxqfHliQYPzZZk> Ml7ENE0yOMLiwsXN MkXKOFghcA>? M4nXZpN2eHC{ZYPz[ZMhVGFiZYjwdoV{e2mxbh?= NFv3V2MzPDl7OU[1Oy=>
NRK-52E MVHGeY5kfGmxbjDBd5NigQ>? M1nJTFHDqML3TR?= NYG1T|RQOTBibXnu NUTu[pV6[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> NWj3XIVkOjR5MUC0NlM>
NRK-52E NWW0dI1PTnWwY4Tpc44hSXO|YYm= M2i4c|HDqML3TR?= MWSxNEBucW5? NVT0XWZ[[myxY3vzJGFv\yCLSTDpcoR2[2WmIFPENlQh\XiycnXzd4lwdg>? M4K4SVI1PzFyNEKz
HSC  NYj1cY9STnWwY4Tpc44hSXO|YYm= NGXTRYYzOCEQvF2= NWLqUm8{OSCq MoC2ZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= NF[0NmUzPDZzNEG5PS=>
EJ NVPZO4dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTHOVAwQDBizszN M{j6O|I1NzR6L{eyJIg> NGf2[IFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NFzl[HAzPDV6N{C0PS=>
EJ NVeyPXQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfvRno2OC96MDFOwG0> NWTqbWlbPDhiaB?= M{DQWoNifXOnczDTMZBp[XOnIHHydoV{fA>? MUeyOFU5PzB2OR?=
EJ MXXGeY5kfGmxbjDBd5NigQ>? MVK1NE85OCEQvF2= MlXSOFghcA>? MY\kc5dvemWpdXzheIV{KGNvTYnjMEBkgWOuaX7ENUwhe3W{dnn2bY4h[W6mIG\FS2Yh\XiycnXzd4lwdnN? NXXoZmNrOjR3OEewOFk>
HepG2 M1X0bmZ2dmO2aX;uJGF{e2G7 M3X6S|UxNTVyMDFOwG0> NUW2XldQPjEEoH3pci=> NGX0d5BqdmirYnn0d{B1cGViSVytOk1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTCoWJlzPzB3KTDhcoQhW1SDVEOgLHR6ejdyNTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MnPrNlQzPDJyNE[=
SGC7901 MkSyR4VtdCCYaXHibYxqfHliQYPzZZk> M3rDblAuOTByIN88US=> M2DU[VI1NzR6L{eyJIg> NGC4bpNk[XW|ZYOgZUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliZH;z[U1l\XCnbnTlcpRtgSCkdYSgco91KHSrbXWt[IVx\W6mZX70cJk> NI\3dWQzPDF3MUK1OS=>
AGS  M3jxZmNmdGxiVnnhZoltcXS7IFHzd4F6 NV\zZZEyOC1zMECg{txO NXr6clN7OjRxNEivO|IhcA>? MlK4Z4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 M1:wWlI1OTVzMkW1
SGC7901 M{HZOWZ2dmO2aX;uJGF{e2G7 NHLDblk2OCEQvF2= MWqyOE81QC95MjDo MVr0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= MUmyOFE2OTJ3NR?=
AGS  MV\GeY5kfGmxbjDBd5NigQ>? NHXkVnM2OCEQvF2= MkXINlQwPDhxN{KgbC=> Mk\zeIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= NXzKc49WOjRzNUGyOVU>
SGC7901 NXLhOYhTTnWwY4Tpc44hSXO|YYm= MWK1NEDPxE1? NWDtS|B7OjRxNEivO|IhcA>? Ml\XeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> M4foeFI1OTVzMkW1
AGS  M{naeGZ2dmO2aX;uJGF{e2G7 NGrRe5M2OCEQvF2= MWWyOE81QC95MjDo MlvmeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> NI\ydpUzPDF3MUK1OS=>
MC3T3-E1  MonDSpVv[3Srb36gRZN{[Xl? NIjPRZA2OCEQvF2= MoX0OEBp NXrKNFZOcW6qaXLpeJMhUFOHLXnu[JVk\WRiQl3QO{BidmRiR1jSJJBzd3SnaX6g[ZhxemW|c3nvcuKh NFzsNGMzOzh5N{ezOC=>
7TD1-DXM MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13kXVExKM7:TR?= MYG3NkBp NGrrUnNFVVOR NYDKRYI{cW6qaXLpeJMh[2WubDDndo94fGh? NFroRYMzOzh5MUG1PS=>
7TD1-WD-90 NY\0fmN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmiwNVAh|ryP Ml20O|IhcA>? MlrhSG1UVw>? NFvRUFNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MX6yN|g4OTF3OR?=
7TD1-DXM MVrBdI9xfG:|aYOgRZN{[Xl? MWW1NEDPxE1? NEjYbJY1QCCq MVrEUXNQ M{fSd4lv\HWlZYOgZZBweHSxc3nz Ml;NNlM5PzFzNUm=
7TD1-WD-90 MYLBdI9xfG:|aYOgRZN{[Xl? NFrnUZY2OCEQvF2= NVewNI9pPDhiaB?= NHj6XGlFVVOR M1fTUolv\HWlZYOgZZBweHSxc3nz NXm3NXhQOjN6N{GxOVk>
7TD1-WD-90  NUX1VGp4TnWwY4Tpc44hSXO|YYm= NFe4TIU2OCEQvF2= MortOkBp MmPySG1UVw>? M1\zTZNq\26rZnnjZY51dHliaX7obYJqfHNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBLSUt{IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEO= NWXpfY1xOjN6N{GxOVk>
HepG2  NX:4OlRKTnWwY4Tpc44hSXO|YYm= NFzHbYEyODBizszN NUH6[2RJOTJxMkSgbC=> MY\pcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NGXVfoszOzh|NkSwNC=>
RAW264.7  NIL1VJJHfW6ldHnvckBCe3OjeR?= NGPBbmY2OMLizszNxsA> NW\WPFRDOjRxNEigbC=> MYLzeZBxemW|c3XzJHJCVkuOLXnu[JVk\WRib4P0[Y9kdGG|dH;n[Y5me2m| MmPGNlM3PjVyMUi=
RAW264.7 NVeyVYV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHCemtWOC13MNMg{txOyqB? NIr4WGs1QMLiaB?= NVq4VW5IcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[U1l\XCnbnTlcpRtgQ>? NI\m[3gzOzZ4NUCxPC=>
RAW264.7 M{T3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfp[|AxNTVywrFOwG3DqA>? Mm\UOFjDqGh? MVrjZZV{\XNiYX6gZZJz\XO2IH;mJHJCXzJ4ND63JINmdGy|IHH0JJRp\SCJMD;HNUBxcGG|ZTDv[kB1cGViY3XscEBkgWOuZR?= M{HvWFI{PjZ3MEG4
RAW264.7 NX\4cGFrTnWwY4Tpc44hSXO|YYm= M3jsclUxyqEQvF2= MX:yOE81QCCq MlTWbY5pcWKrdIOgVmFPU0xvaX7keYNm\CCQRlHUZ|Eh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNmejd{N2PURXQ{ NFrtTngzOzZ4NUCxPC=>
A549  NVnJdnN3TnWwY4Tpc44hSXO|YYm= NIXRcI0zOC92MDFOwG0> M4D5eVIxKGh? MnrHNlAh|ryPIFHHOFkxKHO3cIDy[ZN{\XNidHjlJJJi\GmjdHnvck1qdmS3Y3XkJIlvfmG|aX;uJI9nKEF3NEmgZ4VtdHN? NFe3UoMzOzZ{MEG5NS=>
A549  MYjGeY5kfGmxbjDBd5NigQ>? M3vwfVExNzJyL{SwJO69VQ>? NVPId25oOjRiaB?= NGH2OVl{fXCycnXzd4V{KHSqZTDyZYRq[XSrb36tbY5lfWOnZDDlcIV3[XSrb36gc4YhXkWJRtMg MV6yN|YzODF7MR?=
HUVECs MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUPJN2toOjBiwsXN NH34eJU1KGh? MV;heJRmdnWjdHXzJGgzVzJvaX7keYNm\CClZXzsJJNpemmwa3Hn[UBidmRiaX3wdo93\WRidHjlJIF1fGGlaH3lcpQhemG2ZTDv[kB1cGViY3XscJM> MoDvNlM1QDN7NE[=
HUVECs NV:wUphpSXCxcITvd4l{KEG|c3H5 MnHuNlAhyrWP NGrLdGs1KGh? M3nzNpNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBk\WyuIHHwc5B1d3SrYzDpcoRmgA>? NF60RYozOzR6M{m0Oi=>
BV-2  M3nWe2Z2dmO2aX;uJGF{e2G7 MVSyNEDDvU1? NWTyOJp5OTZiaB?= MWHpcohq[mm2czDMVHMucW6mdXPl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBidG2xc4SgZ49ueGyndHXsfUBlcW2rbnnzbIVlKGmQT2Og[ZhxemW|c3nvci=> M1\6bFI{OjN4M{ew
NRK-52E  M4KyR2Z2dmO2aX;uJGF{e2G7 MomxOeKh|ryP NXLucpNHOzEEoH3pci=> MUDheJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> NWnXSG9ROjNzN{S3OVc>
SW620  MYLGeY5kfGmxbjDBd5NigQ>? MVGyNEDDvU1? MX2xM|YhcA>? M1O0PIlvcGmkaYTzJJAuW1SDVEOgZYN1cX[jdHnvci=> MmfXNlMyOTB4MkW=
RPE  MYjGeY5kfGmxbjDBd5NigQ>? MX2zNEDDvU4EoB?= MU[zJIg> MmPLbY5pcWKrdIOgeIhmKGmwZIXjeIlwdiCxZjDwMXNVSVR|IHX4dJJme3Orb36= MYeyN|A6PDB4Nx?=
SW1116 M{W3U2Z2dmO2aX;uJGF{e2G7 MVWxNFAhyrWPwrC= NVTubotVOjRxNEivO|IhcA>? NWTrfHNS\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= NFzVPJMzOjB3MEe5NC=>
HT29 M4f0V2Z2dmO2aX;uJGF{e2G7 M2TSOFExOCEEtV5CpC=> NUHlbmxnOjRxNEivO|IhcA>? NGLp[Ytl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= MnfXNlIxPTB5OUC=
SW1116 NV7Nc21TTnWwY4Tpc44hSXO|YYm= MWWxNFAhyrWPwrC= NF6zbXYzPC92OD:3NkBp MknH[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> MkXUNlIxPTB5OUC=
HT29 M13xTWZ2dmO2aX;uJGF{e2G7 M2TkWVExOCEEtV5CpC=> NIPDRWkzPC92OD:3NkBp NH2xc5Vl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NWfEW3BjOjJyNUC3PVA>
ARPE-19 M3G1bGZ2dmO2aX;uJGF{e2G7 NUPaZYRuPcLizszN MWOzNOKhdWmw MoGxbY5pcWKrdIOgTmFMOiCyaH;zdIhwemmuYYTpc44> NFnCV2QzOTZ{MEm2Ny=>
HSC-T6 MkHKRZBweHSxc3nzJGF{e2G7 MVqxNOKh|ryP MUCyxsBpyqB? NXXnXIdJcW6qaXLpeJMhfGinIHHwc5B1d3OrczDv[kBJW0NvVE[gZ4VtdHNiaX7keYNm\CCkeTDDSGU> MXSyNVM6Pjl7OB?=
HSC-T6 M2L2NmZ2dmO2aX;uJGF{e2G7 M2rkTVExyqEQvF2= M13SWVLDqGkEoB?= NFr2XYRqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= NV3abpA6OjF|OU[5PVg>
Hep-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DZWVI2NTFyMDFOwG0> M3rpbFI1NzR6L{eyJIg> M1rxeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{fPRlIyOzB7NEix
Hep-2 NHXN[FFCeG:ydH;zbZMhSXO|YYm= NX31RWRXPTBizszN NWHJVYpDOjRxNEivO|IhcA>? NIi4[pFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IITpcYUh\GWyZX7k[Y51dHl? NVnhTG5POjF|MEm0PFE>
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A-172 M{LzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVi1NE8yODEEoN88US=> M4DuOVQ5KGh? NV\xOotGdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MlTvNlA2QDl3MkW=
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A-172 NF[xcnlHfW6ldHnvckBCe3OjeR?= NIXSd28yODEEoN88US=> MoTTOFghcA>? MXLpcohq[mm2czDpcpZie2mxbh?= MnnQNlA2QDl3MkW=
MZ-18 NFfOfIlHfW6ldHnvckBCe3OjeR?= MlXZNVAxyqEQvF2= NHK3Wno1QCCq NGnLSWlqdmirYnn0d{Bqdn[jc3nvci=> NVLRZpZGOjB3OEm1NlU>
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SW1990 M4fQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHvSVczOjBizszN M3PO[lI1NzR6L{eyJIg> MVLpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NIDvbpEzODR6Mki1PC=>
SW1990 M1fmN2Z2dmO2aX;uJGF{e2G7 M3HZVlIxKM7:TR?= MYCyOEBp M1rwR4Rm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBOVVBvMjDhcoQhXkWJRjDtVm5Cew>? M{nQVFIxPDh{OEW4
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THP1 MYDGeY5kfGmxbjDBd5NigQ>? NGCxSZUyOCC3TR?= MYSzNEBucW8EoB?= NF;ZTZBqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= MX[yNFM6OzZ7MB?=
BMMC MVvGeY5kfGmxbjDBd5NigQ>? M3jrflAuOTBizszN MV2xOeKhdWmw NHfKe4JqdmirYnn0d{BNXEN2wrDy[Yxm[XOnIHnuJIEh\G:|ZT3k[ZBmdmSnboSg[oF{cGmxbjD3bZRpKG6nYYKgZ49ueGyndHWgbY5pcWKrdHnvckBifCClb37j[Y51emG2aX;ud{Djsb5zMNMg{txO MUOxPVg{PTh2NR?=
A549 M2PXcGZ2dmO2aX;uJGF{e2G7 M2PWUVE2KM7:bR?= M37ydlEhcA>? MXzpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSxJI9vKHS7cn;zbY5mKDdyMTD3ZZMh\GW2ZXP0[YQhOTVibXnuJIFnfGW{IGPQSUBDKHS{ZXH0cYVvfA>? M4GyOFE6QDBzNk[1
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Jurkat  NEf6c4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrIOVAh|ryP MUmyOE81QC95MjDo NEW1TmpmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NWfKZ5U4OTl3NkS4PVE>
SUPT1  M2TqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X6NlUxKM7:TR?= NXLaepFrOjRxNEivO|IhcA>? Ml:w[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u NVPiflMxOTl3NkS4PVE>
Jurkat  NX;qUJZ5SXCxcITvd4l{KEG|c3H5 MnW4OVAh|ryP MmXFNlQwPDhiaB?= MnLv[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> MorONVk2PjR6OUG=
SUPT1  M{LncGFxd3C2b4Ppd{BCe3OjeR?= M1nQZ|UxKM7:TR?= M1HWXlI1NzR6IHi= Moqy[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> NEnFc4oyQTV4NEi5NS=>

... 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]

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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]

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  • 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]

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  • Animal Models: SCID mice intravenously injected with ALL cells
  • 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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms Zinc02557947
Smiles OC1=C(O)C=C(C=C1)\C=C(C#N)\C(=O)NCC2=CC=CC=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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).

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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)

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

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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)
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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