AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

103 publications

AG-490 (Tyrphostin B42) Chemical Structure

CAS No. 133550-30-8

AG-490 (Tyrphostin B42, Zinc02557947) 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 103 publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description AG-490 (Tyrphostin B42, Zinc02557947) 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
JAK2 (V617F) [8]
()
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 MVHGeY5kfGmxbjDBd5NigQ>? M4rWT|ExOOLCidM1US=> MmrkNlQhcA>? NWC4bYpwdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ MUiyOlE5PDl7OR?=
BCBL1 MVLGeY5kfGmxbjDBd5NigQ>? MlnENVAx6oDLwsXN MlzFNlQhcA>? NUDoc3dRdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ NGDLUlAzPjF6NEm5PS=>
BC3 NGnaT3BHfW6ldHnvckBCe3OjeR?= NIPpfXAyODEkgJpCuW0> M3HEbVI1KGh? Mnj6cYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? MofMNlYyQDR7OUm=
BCBL1 MkTuSpVv[3Srb36gRZN{[Xl? M2DvZlExOOLCidM1US=> MXiyOEBp MVvt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? NGCyOokzPjF6NEm5PS=>
BC3 M2XQe2Z2dmO2aX;uJGF{e2G7 NF3rcpMyODEkgJpCuW0> Mli3NlQhcA>? Mn;ybY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NWe1VIE{OjZzOES5PVk>
BCBL1 MnfJSpVv[3Srb36gRZN{[Xl? MmjJNVAx6oDLwsXN NVLqVWNWOjRiaB?= NHPaWYFqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> NGnVVYgzPjF6NEm5PS=>
SK-MEL-28 M3;VUmZ2dmO2aX;uJGF{e2G7 NHG0UZQ2OC9zMEFihKnDvU1? MnnWOFghcA>? M{i5TWROW09? NXPv[JNbemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MYOyOVIyPjV{Mh?=
MeWo NHnPcIdHfW6ldHnvckBCe3OjeR?= NF\iU2Y2OC9zMEFihKnDvU1? NU\pZ5dkPDhiaB?= Mk\1SG1UVw>? NUXTR|I6emWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NF\2Z4szPTJzNkWyNi=>
SK-MEL-5 MUfGeY5kfGmxbjDBd5NigQ>? NVqx[3NFPTBxMUCw5qCKyrWP M3nEVlQ5KGh? Mlq2SG1UVw>? NV;jZm5oemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> M4f1[lI2OjF4NUKy
SK-MEL-2 NUfFNYVDTnWwY4Tpc44hSXO|YYm= MV61NE8yODEkgJpCuW0> MYi0PEBp NEjISlRFVVOR NVPjfYkzemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MVuyOVIyPjV{Mh?=
B16-F0 NUXWc5VzTnWwY4Tpc44hSXO|YYm= NEXQOWY2OC9zMEFihKnDvU1? NVjReok{PDhiaB?= NGHSZY5FVVOR M2rscJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NYLqeXdyOjV{MU[1NlI>
TRPM2/HEK  MmfiSpVv[3Srb36gRZN{[Xl? NU[zcFJ2OC5z4pETNlXDqML3TR?= NE\yUIoyPcLibXnu M2XFR2ROW09? MmXidoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyBzLkhCpOK2VQ>? NWfMclBEOjVzN{m1O|Q>
U937  MoThSpVv[3Srb36gRZN{[Xl? NHHrenQxNjIkgKOyOeKhyrWP M2CzUlE2yqCvaX6= NHXXXG9FVVOR NVzNV5VJemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= MUSyOVE4QTV5NB?=
TRPM2/HEK  NXu1dWF[TnWwY4Tpc44hSXO|YYm= MmWwNVDDqML3TR?= NI\LT3Q1OMLibXnu NXLJUo9mTE2VTx?= MVHy[YR2[2W|IGTSVG0zKGGldHn2ZZRqd25iZY\lckBifCCqaXfoJINwdmOnboTyZZRqd26|IH;mJGgzVzJ? NX7jNpZXOjVzN{m1O|Q>
GL37  NWT0PXpXS2WubDDWbYFjcWyrdImgRZN{[Xl? NELCeIwxNTFywrFCuW0> NVr3dI5vPDhiaB?= M{n2e5N2eHC{ZYPz[ZMhVGFiZYjwdoV{e2mxbh?= MYiyOFk6QTZ3Nx?=
NRK-52E M{\SUmZ2dmO2aX;uJGF{e2G7 MnLRNeKhyrWP NE\qR2YyOCCvaX6= NX;1fGJ1[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> MY[yOFcyODR{Mx?=
NRK-52E M37DXWZ2dmO2aX;uJGF{e2G7 NFm3WHcyyqEEtV2= MVyxNEBucW5? MWnicI9kc3NiQX7nJGlKKGmwZIXj[YQhS0R{NDDlfJBz\XO|aX;u NXnPS492OjR5MUC0NlM>
HSC  M374bWZ2dmO2aX;uJGF{e2G7 NEP3UWEzOCEQvF2= Ml3iNUBp NWrhPZRs[WK{b3fheIV{KHSqZTDkbYZn\XKnboTpZYwh\W[oZXP0d{Bw\iCuZYD0bY4hd3JiQVfFdy=> NFizTJczPDZzNEG5PS=>
EJ NELH[ZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DNUlUxNzhyIN88US=> NGPGfIYzPC92OD:3NkBp M2LWeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ Mn7VNlQ2QDdyNEm=
EJ MmnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXK1NE85OCEQvF2= Ml60OFghcA>? MWrjZZV{\XNiUz3wbIF{\SCjcoLld5Q> NYnHW3hZOjR3OEewOFk>
EJ M3\DUWZ2dmO2aX;uJGF{e2G7 MkTVOVAwQDBizszN M1rsUlQ5KGh? NXPo[2Vm\G:5boLl[5Vt[XSnczDjMW16[yxiY4njcIlvTDFuIIP1dpZqfmmwIHHu[EBXTUeIIHX4dJJme3Orb37z MXuyOFU5PzB2OR?=
HepG2 NGrFZm5HfW6ldHnvckBCe3OjeR?= MWm1NE02ODBizszN NVnkRW5UPjEEoH3pci=> MlnEbY5pcWKrdIOgeIhmKEmOLU[tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gV3RCXDFiKGT5dlcxPSliYX7kJHNVSVR|IDjUfZI4ODVrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXywSGhUOjR{NEKwOFY>
SGC7901 MkfLR4VtdCCYaXHibYxqfHliQYPzZZk> MmPyNE0yODBizszN MmfHNlQwPDhxN{KgbC=> MYjjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= MX2yOFE2OTJ3NR?=
AGS  MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEf6cm8xNTFyMDFOwG0> Mk\mNlQwPDhxN{KgbC=> MmrOZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 MlXnNlQyPTF{NUW=
SGC7901 NX;IOm9xTnWwY4Tpc44hSXO|YYm= MXK1NEDPxE1? NIHBTIIzPC92OD:3NkBp NFnxNGJ1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> NVvQdnY1OjRzNUGyOVU>
AGS  NIDhSZRHfW6ldHnvckBCe3OjeR?= NYT1O3pQPTBizszN NX\HOIZnOjRxNEivO|IhcA>? Mme2eIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= MU[yOFE2OTJ3NR?=
SGC7901 NETyZ2RHfW6ldHnvckBCe3OjeR?= NGHVTHY2OCEQvF2= NIHnOpYzPC92OD:3NkBp NV7EWXgzfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? MV:yOFE2OTJ3NR?=
AGS  MknVSpVv[3Srb36gRZN{[Xl? MVm1NEDPxE1? NGHlOG4zPC92OD:3NkBp NYX3R4N[fGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? NWeyd4lyOjRzNUGyOVU>
MC3T3-E1  NXj6PVYxTnWwY4Tpc44hSXO|YYm= M4D5NlUxKM7:TR?= MnHIOEBp MkPRbY5pcWKrdIOgTHNGNWmwZIXj[YQhSk2SNzDhcoQhT0iUIIDyc5RmcW5iZYjwdoV{e2mxbtMg NFnRfGYzOzh5N{ezOC=>
7TD1-DXM NEfzV|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTkbHdOOTBizszN MkfVO|IhcA>? NITxTIpFVVOR MkTjbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NXzPe2VzOjN6N{GxOVk>
7TD1-WD-90 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj5NVAh|ryP M3KyU|czKGh? MYrEUXNQ NV;TWow4cW6qaXLpeJMh[2WubDDndo94fGh? NGG1OXAzOzh5MUG1PS=>
7TD1-DXM MnT0RZBweHSxc3nzJGF{e2G7 NVvCWJhJPTBizszN NV[5[2tNPDhiaB?= NEnKOWZFVVOR MXfpcoR2[2W|IHHwc5B1d3Orcx?= MlXVNlM5PzFzNUm=
7TD1-WD-90 Mm\0RZBweHSxc3nzJGF{e2G7 NWrCSGQ6PTBizszN M17xNFQ5KGh? MUDEUXNQ M4ezeolv\HWlZYOgZZBweHSxc3nz MmO1NlM5PzFzNUm=
7TD1-WD-90  MorKSpVv[3Srb36gRZN{[Xl? NEnBWlE2OCEQvF2= MmPQOkBp NG\YXVRFVVOR NY\3WllHe2mpbnnmbYNidnSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEqDS{KgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNy=> MYGyN|g4OTF3OR?=
HepG2  MlrwSpVv[3Srb36gRZN{[Xl? Mn:yNVAxKM7:TR?= MWGxNk8zPCCq MYDpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NW\RTopOOjN6M{[0NFA>
RAW264.7  MWPGeY5kfGmxbjDBd5NigQ>? NVu4dZg5PTEEoN88UeKh M4\oVFI1NzR6IHi= MmTvd5VxeHKnc4Pld{BTSU6NTD3pcoR2[2WmIH;zeIVw[2yjc4Tv[4Vv\XOrcx?= MU[yN|Y3PTBzOB?=
RAW264.7 NHGwNFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViwMVUxyqEQvF5CpC=> MoXDOFjDqGh? MnPObY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> MUKyN|Y3PTBzOB?=
RAW264.7 M1fke2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS2VVVpOC13MNMg{txOyqB? MYO0POKhcA>? MWrjZZV{\XNiYX6gZZJz\XO2IH;mJHJCXzJ4ND63JINmdGy|IHH0JJRp\SCJMD;HNUBxcGG|ZTDv[kB1cGViY3XscEBkgWOuZR?= NWjBNG9EOjN4NkWwNVg>
RAW264.7 MYLGeY5kfGmxbjDBd5NigQ>? M4\KXVUxyqEQvF2= NGrnOI0zPC92ODDo Mn;nbY5pcWKrdIOgVmFPU0xvaX7keYNm\CCQRlHUZ|Eh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNmejd{N2PURXQ{ NWP5PJFMOjN4NkWwNVg>
A549  Ml7zSpVv[3Srb36gRZN{[Xl? MVGyNE81OCEQvF2= NIXBN5AzOCCq M2PTfVIxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| M3G2UlI{PjJyMUmx
A549  Mn36SpVv[3Srb36gRZN{[Xl? NWXCe|R{OTBxMkCvOFAh|ryP NYjwPHJLOjRiaB?= NF;YbJl{fXCycnXzd4V{KHSqZTDyZYRq[XSrb36tbY5lfWOnZDDlcIV3[XSrb36gc4YhXkWJRtMg MXmyN|YzODF7MR?=
HUVECs MmToR4VtdCCYaXHibYxqfHliQYPzZZk> MUGyNEDDvU1? M3G0OFQhcA>? M3;zZoF1fGWwdXH0[ZMhUDKRMj3pcoR2[2WmIHPlcIwhe2i{aX7rZYdmKGGwZDDpcZBzd3[nZDD0bIUh[XS2YXPocYVvfCC{YYTlJI9nKHSqZTDj[Yxtew>? M3:4SFI{PDh|OUS2
HUVECs NFHFV|JCeG:ydH;zbZMhSXO|YYm= NIK2XYQzOCEEtV2= NH7wUVc1KGh? NHjtS4x{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? NWPGRnJyOjN2OEO5OFY>
BV-2  M2H3PWZ2dmO2aX;uJGF{e2G7 NF;RfG8zOCEEtV2= MV:xOkBp NYnpNWJOcW6qaXLpeJMhVFCVLXnu[JVk\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiYXztc5N1KGOxbYDs[ZRmdHliZHntbY5qe2inZDDpUm9UKGW6cILld5Nqd25? M1X1PVI{OjN4M{ew
NRK-52E  M4rzfWZ2dmO2aX;uJGF{e2G7 NXW5XoYyPcLizszN MVGzNOKhdWmw NX\vXHlS[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? NUThUG16OjNzN{S3OVc>
SW620  NWOxd4s3TnWwY4Tpc44hSXO|YYm= MWmyNEDDvU1? Mor5NU83KGh? NETMN|hqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> MmnpNlMyOTB4MkW=
RPE  NI\3bIFHfW6ldHnvckBCe3OjeR?= NXL3dIlQOzBiwsXNxsA> NVjuflNWOyCq M1ziTolvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u NXLINIFIOjNyOUSwOlc>
SW1116 NEDocVlHfW6ldHnvckBCe3OjeR?= NW\reFhrOTByINM1UeKh NEfZeYwzPC92OD:3NkBp NVv1bYRx\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= Mk\ONlIxPTB5OUC=
HT29 MonZSpVv[3Srb36gRZN{[Xl? NYHGeYY1OTByINM1UeKh NH\5Z4szPC92OD:3NkBp MWrk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? M3fxVlIzODVyN{mw
SW1116 MX3GeY5kfGmxbjDBd5NigQ>? Mn3SNVAxKML3TdMg M{TTb|I1NzR6L{eyJIg> NE\Lcm9l\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? MYmyNlA2ODd7MB?=
HT29 M2fkdWZ2dmO2aX;uJGF{e2G7 M3GyOlExOCEEtV5CpC=> MoTRNlQwPDhxN{KgbC=> NGiyVYFl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? M4ez[lIzODVyN{mw
ARPE-19 NVXPc21TTnWwY4Tpc44hSXO|YYm= MUG1xsDPxE1? M{HEVlMxyqCvaX6= M4jxW4lvcGmkaYTzJGpCUzJicHjvd5Bpd3KrbHH0bY9v M4DDSlIyPjJyOU[z
HSC-T6 NFu2W3ZCeG:ydH;zbZMhSXO|YYm= NXW1SJdzOTEEoN88US=> Mn60NuKhcMLi MnzlbY5pcWKrdIOgeIhmKGGyb4D0c5NqeyCxZjDIV2MuXDZiY3XscJMhcW6mdXPl[EBjgSCFRFW= Mn24NlE{QTZ7OUi=
HSC-T6 NGTMUIVHfW6ldHnvckBCe3OjeR?= NEj3eVEyOMLizszN Ml7MNuKhcMLi M{CxVYlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wczDv[kBxYS2VVFHUNUBidmRiQnHkJIlv\HWlZXSgZpkhS0SH NXzsTldjOjF|OU[5PVg>
Hep-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP3NlUuOTByIN88US=> NVnjc41COjRxNEivO|IhcA>? M37HZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MkLBNlE{ODl2OEG=
Hep-2 NVPCc|l2SXCxcITvd4l{KEG|c3H5 NWTPdoJiPTBizszN NX\aOmpDOjRxNEivO|IhcA>? NIfRSFJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IITpcYUh\GWyZX7k[Y51dHl? M3WzcFIyOzB7NEix
Hep-2 MmXwSpVv[3Srb36gRZN{[Xl? M2HvVVUxKM7:TR?= MXWyOE81QC95MjDo MUjpcohq[mm2czDHNUB1dyCVIHPlcIwh[3mlbHWgeJJidnOrdHnvckBidmRiaX7keYNmeyCJMTDj[YxtKGO7Y3zlJIFzemW|dB?= M1i1flIyOzB7NEix
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HEL  NGjDc2tHfW6ldHnvckBCe3OjeR?= Mk\lNVAxyqEQvF2= MnLrNVIuPzJiaB?= NHXVUllqdmirYnn0d{B1cGVibHX2[Ywhd2ZicD3KRWszNCCMQVuy NGG2dHYzODZ{MUC2NS=>
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A-172 NEfUSWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LZV|UxNzFyMNMg{txO M3XZOlQ5KGh? MU\s[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MXiyNFU5QTV{NR?=
MZ-18 MkDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;NOVAwOTBywrFOwG0> M4XMVlQ5KGh? MYXs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? Mln6NlA2QDl3MkW=
MZ-54 MmXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLHblM2OC9zMEFCpO69VQ>? MXK0PEBp M{TuNIxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NGjxVZYzODV6OUWyOS=>
MZ-256 NGXG[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HNTVUxNzFyMNMg{txO NHfLVJc1QCCq NVXKXVNZdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo Mn3wNlA2QDl3MkW=
MZ-304 NUCwS|BsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHzWYo2OC9zMEFCpO69VQ>? MX[0PEBp NWf3NFMxdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo M3W5c|IxPTh7NUK1
A-172 NF3rNIxHfW6ldHnvckBCe3OjeR?= M4DCZ|UxNzFyMNMg{txO M3[3bFQ5KGh? NWnJSoJxcW6qaXLpeJMhdWmpcnH0bY9v MlPYNlA2QDl3MkW=
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MZ-54 MlyySpVv[3Srb36gRZN{[Xl? NWrtbIJtPTBxMUCwxsDPxE1? Mkn1OFghcA>? NGfCbIRqdmirYnn0d{BucWe{YYTpc44> M3L6VFIxPTh7NUK1
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A-172 MXXGeY5kfGmxbjDBd5NigQ>? NVTwUnBNOTBywrFOwG0> NXfke3JqPDhiaB?= NYPXcIRNcW6qaXLpeJMhcW64YYPpc44> NEDTVW0zODV6OUWyOS=>
MZ-18 NEH0cYZHfW6ldHnvckBCe3OjeR?= MYCxNFDDqM7:TR?= MXi0PEBp NGTzfm5qdmirYnn0d{Bqdn[jc3nvci=> Mn\zNlA2QDl3MkW=
MZ-54 NIP1dIFHfW6ldHnvckBCe3OjeR?= NIn0PYsyODEEoN88US=> NXHNeWtUPDhiaB?= M1nsO4lvcGmkaYTzJIlvfmG|aX;u NIPp[2czODV6OUWyOS=>
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MZ-304 NVnzTnE5TnWwY4Tpc44hSXO|YYm= NXr2W|N2OTBywrFOwG0> NYfYdZo6PDhiaB?= Mny1bY5pcWKrdIOgbY53[XOrb36= MYeyNFU5QTV{NR?=
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MZ-54 NGHsVYZHfW6ldHnvckBCe3OjeR?= MoXvOVAwOTBywrFOwG0> Mnq1OFghcA>? MV3y[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NWf1Rm5UOjB3OEm1NlU>
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MZ-304 NH61W4pHfW6ldHnvckBCe3OjeR?= MkK1OVAwOTBywrFOwG0> M4G5NFQ5KGh? NV3zW4tnemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? MXuyNFU5QTV{NR?=
SW1990 NWO1emt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDHOHVTOjBizszN MnjtNlQwPDhxN{KgbC=> NVXuRYcycW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MWqyNFQ5Ojh3OB?=
SW1990 MnLZSpVv[3Srb36gRZN{[Xl? M{XLelIxKM7:TR?= NEjvfXAzPCCq M2fJcIRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBOVVBvMjDhcoQhXkWJRjDtVm5Cew>? MUGyNFQ5Ojh3OB?=
SW1990 MVTGeY5kfGmxbjDBd5NigQ>? Ml7oNlAh|ryP NESzNHEzPCCq NUTy[pV4\GWlcnXhd4V{KHSqZTDpcpRmdnOrdImgc4YheC2VdHH0N{BmgHC{ZYPzbY9v MmPGNlA1QDJ6NUi=
SW1990 M2fEcGlvfmG|aX;uJGF{e2G7 NHzFRVYzOCEQvF2= NHPRd2szPCCq MlLudoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= NWL5dGl5OjB2OEK4OVg>
THP1 MmPySpVv[3Srb36gRZN{[Xl? M2jPPFExKHWP NX;5fVhxOzBibXnuxsA> NEWxXpZqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= MWGyNFM6OzZ7MB?=
BMMC NHz5dolHfW6ldHnvckBCe3OjeR?= NVnxTWJtOC1zMDFOwG0> MonHNVXDqG2rbh?= M{PJeolvcGmkaYTzJGxVSzUEoILlcIVie2ViaX6gZUBld3OnLXTldIVv\GWwdDDmZZNpcW:wIIfpeIghdmWjcjDjc41xdGW2ZTDpcohq[mm2aX;uJIF1KGOxbnPlcpRz[XSrb37zJQKqxjFywrFOwG0> Mln4NVk5OzV6NEW=
A549 NUTtdVlrTnWwY4Tpc44hSXO|YYm= NHfRWnAyPSEQvH2= NH3NeWUyKGh? NHy1XWhqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQyKG:wIIT5do9{cW6nIEewNUB4[XNiZHX0[YN1\WRiMUWgcYlvKGGodHXyJHNRTSCEIITy[YF1dWWwdB?= MUmxPVgxOTZ4NR?=
OVCAR-3 M{nRZ2Z2dmO2aX;uJGF{e2G7 NXv4SJlGOTBidV2= NGrNOlUyKGh? NYnTTFVkcW6qaXLpeJMhVFCDLXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;u M3fqPFE6PjR5M{[z
PA-1 NHW2UHBHfW6ldHnvckBCe3OjeR?= NVnJepd2OTBidV2= M1HBUVEhcA>? M12yfIlvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= MXOxPVY1PzN4Mx?=
OVCAR-3 NF7NTlhHfW6ldHnvckBCe3OjeR?= NXjQ[XZHOTBidV2= MkXDNUBp MlnnbY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? NXLHRm5[OTl4NEezOlM>
PA-1 MUXGeY5kfGmxbjDBd5NigQ>? M2DtblExKHWP NVe1TpVQOSCq NXe1U5BkcW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= MUKxPVY1PzN4Mx?=
Jurkat  NIfTVZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X2UVUxKM7:TR?= MkfpNlQwPDhxN{KgbC=> MWrlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= M1jQUlE6PTZ2OEmx
SUPT1  M{XlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LwWlUxKM7:TR?= M2TyflI1NzR6L{eyJIg> M{HyZYVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> NHfzVY8yQTV4NEi5NS=>
Jurkat  M33vOmFxd3C2b4Ppd{BCe3OjeR?= NVWzVotoPTBizszN MXuyOE81QCCq MnLv[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> NH;3NWUyQTV4NEi5NS=>
SUPT1  M3v1fGFxd3C2b4Ppd{BCe3OjeR?= MmniOVAh|ryP NWfSfI1JOjRxNEigbC=> NIHobFNmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MnXzNVk2PjR6OUG=

... 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)
Water Insoluble
Ethanol '6 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG300+5% Tween80+50% ddH2O
For best results, use promptly after mixing.
6.25 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 294.30
Formula

C17H14N2O3

CAS No. 133550-30-8
Storage powder
in solvent
Synonyms Zinc02557947
Smiles C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N

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
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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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