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 NXjUcXdvTnWwY4Tpc44hSXO|YYm= M3PZVVExOOLCidM1US=> NGT0THUzPCCq MmHPcYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz NFnnN|QzPjF6NEm5PS=>
BCBL1 MofrSpVv[3Srb36gRZN{[Xl? M4XXfFExOOLCidM1US=> MUKyOEBp NEGyV|Ru\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NUHET4U5OjZzOES5PVk>
BC3 NH3RNXdHfW6ldHnvckBCe3OjeR?= NIjQ[VEyODEkgJpCuW0> Ml3wNlQhcA>? MVPt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YyKHKnZIXjeIlwdg>? MnXINlYyQDR7OUm=
BCBL1 MVrGeY5kfGmxbjDBd5NigQ>? NXLmbYpxOTBy4pEJxtVO MXqyOEBp NWT0VGJIdWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMjDy[YR2[3Srb36= MX[yOlE5PDl7OR?=
BC3 NVP0e2NYTnWwY4Tpc44hSXO|YYm= NV3CZ2MxOTBy4pEJxtVO NFj0PJQzPCCq MUXpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= M{XmOVI3OTh2OUm5
BCBL1 MVfGeY5kfGmxbjDBd5NigQ>? Mm[xNVAx6oDLwsXN Ml;FNlQhcA>? MmTJbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NFjRcY8zPjF6NEm5PS=>
SK-MEL-28 MnLHSpVv[3Srb36gRZN{[Xl? MkPWOVAwOTBy4pEJxtVO M{f0cFQ5KGh? M1z1T2ROW09? M4PQcJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M3nzSVI2OjF4NUKy
MeWo MVPGeY5kfGmxbjDBd5NigQ>? MVO1NE8yODEkgJpCuW0> MkS3OFghcA>? M4C5ZWROW09? NUO5WVB6emWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NFr3cpAzPTJzNkWyNi=>
SK-MEL-5 NEjq[YVHfW6ldHnvckBCe3OjeR?= NVfJVIp[PTBxMUCw5qCKyrWP NFntV3I1QCCq MYDEUXNQ NEj0OFdz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MWmyOVIyPjV{Mh?=
SK-MEL-2 MXfGeY5kfGmxbjDBd5NigQ>? M{D2dVUxNzFyMPMAjeK2VQ>? MkXsOFghcA>? M{jMNGROW09? MlP2doVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= M162XlI2OjF4NUKy
B16-F0 Mnv2SpVv[3Srb36gRZN{[Xl? M1f3blUxNzFyMPMAjeK2VQ>? M1u5eFQ5KGh? NFnOdFFFVVOR MonRdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NV;LW|VQOjV{MU[1NlI>
TRPM2/HEK  M4rxc2Z2dmO2aX;uJGF{e2G7 MYiwMlHjiJN{NdMgxtVO MUOxOeKhdWmw NGS2[mhFVVOR NHvHOYhz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IEGuO:KhyrWP M4\MR|I2OTd7NUe0
U937  NW\teI91TnWwY4Tpc44hSXO|YYm= NUX3VYxoOC5z4pETNlXDqML3TR?= MYWxOeKhdWmw NIXsS29FVVOR Mn:2doVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? NWT4cW1JOjVzN{m1O|Q>
TRPM2/HEK  NUfjXpp{TnWwY4Tpc44hSXO|YYm= MnKxNVDDqML3TR?= MnS5OFDDqG2rbh?= MoTxSG1UVw>? M2rXSZJm\HWlZYOgWHJRVTJiYXP0bZZifGmxbjDleoVvKGG2IHjp[4gh[2:wY3XueJJifGmxboOgc4YhUDKRMh?= M37OXlI2OTd7NUe0
GL37  M4qzSmNmdGxiVnnhZoltcXS7IFHzd4F6 M4roblAuOTEEoNM1US=> MnvlOFghcA>? NFG3[VR{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= NXfWToNmOjR7OUm2OVc>
NRK-52E MXLGeY5kfGmxbjDBd5NigQ>? NV:zVGxNOcLiwsXN NIHxTncyOCCvaX6= NUmxTlV3[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> MYOyOFcyODR{Mx?=
NRK-52E MnKxSpVv[3Srb36gRZN{[Xl? NXHXR4p3OcLiwsXN NY\wR21pOTBibXnu MU\icI9kc3NiQX7nJGlKKGmwZIXj[YQhS0R{NDDlfJBz\XO|aX;u MUKyOFcyODR{Mx?=
HSC  Mn;ISpVv[3Srb36gRZN{[Xl? MkixNlAh|ryP NVTWbZI3OSCq NFnqSoZi[nKxZ3H0[ZMhfGinIHTp[oZmemWwdHnhcEBm\m[nY4TzJI9nKGyncITpckBweiCDR1Xz NGCxWIIzPDZzNEG5PS=>
EJ NXHRRYFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXm1NE85OCEQvF2= M2rLNFI1NzR6L{eyJIg> NGKydXlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M3nKeVI1PTh5MES5
EJ MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PqV|UxNzhyIN88US=> NYLJbJlxPDhiaB?= Mlj0Z4F2e2W|IGOtdIhie2ViYYLy[ZN1 M2fLO|I1PTh5MES5
EJ Ml\ySpVv[3Srb36gRZN{[Xl? M17lcVUxNzhyIN88US=> M2nEOVQ5KGh? NWjTcJJD\G:5boLl[5Vt[XSnczDjMW16[yxiY4njcIlvTDFuIIP1dpZqfmmwIHHu[EBXTUeIIHX4dJJme3Orb37z M{f2PFI1PTh5MES5
HepG2 M3K5dGZ2dmO2aX;uJGF{e2G7 M4O1fFUxNTVyMDFOwG0> NGPUTFA3OMLibXnu NYPqZmhKcW6qaXLpeJMhfGinIFnMMVYucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEGgLHR6ejdyNTmgZY5lKFOWQWSzJEhVgXJ5MEWpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NH60[I4zPDJ2MkC0Oi=>
SGC7901 NWC5XpBqS2WubDDWbYFjcWyrdImgRZN{[Xl? MYOwMVExOCEQvF2= MXeyOE81QC95MjDo M1TiboNifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> NIXpd2QzPDF3MUK1OS=>
AGS  MlrPR4VtdCCYaXHibYxqfHliQYPzZZk> MWSwMVExOCEQvF2= NUnxOplzOjRxNEivO|IhcA>? Ml;BZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 MXuyOFE2OTJ3NR?=
SGC7901 MmDCSpVv[3Srb36gRZN{[Xl? NFnQ[G02OCEQvF2= M3TQRlI1NzR6L{eyJIg> M1X2PZRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg MYWyOFE2OTJ3NR?=
AGS  MlP0SpVv[3Srb36gRZN{[Xl? NIK5OGY2OCEQvF2= MmPDNlQwPDhxN{KgbC=> MUD0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= NEPaWmEzPDF3MUK1OS=>
SGC7901 M{i4RmZ2dmO2aX;uJGF{e2G7 NH;MT|k2OCEQvF2= NFvCUFczPC92OD:3NkBp MXz0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> NVThOnhUOjRzNUGyOVU>
AGS  NE\6SZhHfW6ldHnvckBCe3OjeR?= NUnrT5RMPTBizszN NXW3b5Z3OjRxNEivO|IhcA>? MonqeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> MVmyOFE2OTJ3NR?=
MC3T3-E1  NUHSUppNTnWwY4Tpc44hSXO|YYm= M13OXFUxKM7:TR?= MVK0JIg> NEDrZotqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> M122VlI{QDd5N{O0
7TD1-DXM NUXtWIdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULqSW1KOTBizszN NVTCV25tPzJiaB?= NWjPc4RnTE2VTx?= MUjpcohq[mm2czDj[YxtKGe{b4f0bC=> NEHndWozOzh5MUG1PS=>
7TD1-WD-90 MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HDXlExKM7:TR?= MkTRO|IhcA>? NH3PXnVFVVOR M12yW4lvcGmkaYTzJINmdGxiZ4Lve5Rp MoD6NlM5PzFzNUm=
7TD1-DXM NHHTXmlCeG:ydH;zbZMhSXO|YYm= Mnj1OVAh|ryP Mn3SOFghcA>? MmO4SG1UVw>? Mkm2bY5lfWOnczDhdI9xfG:|aYO= MlzGNlM5PzFzNUm=
7TD1-WD-90 NGjkc|FCeG:ydH;zbZMhSXO|YYm= MU[1NEDPxE1? NGWxVGk1QCCq MoTTSG1UVw>? Mn\KbY5lfWOnczDhdI9xfG:|aYO= NFvsZ44zOzh5MUG1PS=>
7TD1-WD-90  M{[wZ2Z2dmO2aX;uJGF{e2G7 MkjnOVAh|ryP Ml7LOkBp MYTEUXNQ MWPzbYdvcW[rY3HueIx6KGmwaHnibZR{KHSqZTDwbI9{eGixconsZZRqd25ib3[gTmFMOiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVR| NYjFXnhDOjN6N{GxOVk>
HepG2  NFvMOGVHfW6ldHnvckBCe3OjeR?= M4POZ|ExOCEQvF2= MnHXNVIwOjRiaB?= MXPpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> M1G2clI{QDN4NECw
RAW264.7  MYjGeY5kfGmxbjDBd5NigQ>? NUHqbmlVPTEEoN88UeKh MmfQNlQwPDhiaB?= MmXPd5VxeHKnc4Pld{BTSU6NTD3pcoR2[2WmIH;zeIVw[2yjc4Tv[4Vv\XOrcx?= MnrhNlM3PjVyMUi=
RAW264.7 NGLCTm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWwMVUxyqEQvF5CpC=> NXS5Ong6PDkEoHi= NFriNotqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlMYRmeGWwZHXueIx6 NFnQWlEzOzZ4NUCxPC=>
RAW264.7 M1OwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPQT5NLOC13MNMg{txOyqB? MnnnOFjDqGh? NHfKcY9k[XW|ZYOgZY4h[XK{ZYP0JI9nKFKDV{K2OE44KGOnbHzzJIF1KHSqZTDHNE9IOSCyaHHz[UBw\iC2aHWgZ4VtdCCleXPs[S=> M2Dp[VI{PjZ3MEG4
RAW264.7 NWjJeGJSTnWwY4Tpc44hSXO|YYm= MWq1NOKh|ryP M4f2WFI1NzR6IHi= M1:0eIlvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? NYGxbWtLOjN4NkWwNVg>
A549  MlvMSpVv[3Srb36gRZN{[Xl? MX6yNE81OCEQvF2= M2q5dFIxKGh? Mn3pNlAh|ryPIFHHOFkxKHO3cIDy[ZN{\XNidHjlJJJi\GmjdHnvck1qdmS3Y3XkJIlvfmG|aX;uJI9nKEF3NEmgZ4VtdHN? NXXOdJU5OjN4MkCxPVE>
A549  M3XKVmZ2dmO2aX;uJGF{e2G7 NI\KdW8yOC9{MD:0NEDPxE1? MoHaNlQhcA>? M1rSRZN2eHC{ZYPz[ZMhfGinIILh[IlifGmxbj3pcoR2[2WmIHXs[ZZifGmxbjDv[kBXTUeIwrC= MWSyN|YzODF7MR?=
HUVECs NUTtSXE5S2WubDDWbYFjcWyrdImgRZN{[Xl? M3i3PFIxKML3TR?= NEfwW4s1KGh? NX:xU4M3[XS2ZX71ZZRmeyCKMl:yMYlv\HWlZXSgZ4VtdCC|aILpcoti\2ViYX7kJIlueHKxdnXkJJRp\SCjdIThZ4hu\W62IILheIUhd2ZidHjlJINmdGy| M{HJVFI{PDh|OUS2
HUVECs NVnN[41nSXCxcITvd4l{KEG|c3H5 NH7kSmczOCEEtV2= MonBOEBp NFeyR3p{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? M2DlWVI{PDh|OUS2
BV-2  MXPGeY5kfGmxbjDBd5NigQ>? NIHsbGwzOCEEtV2= MmLmNVYhcA>? MVfpcohq[mm2czDMVHMucW6mdXPl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBidG2xc4SgZ49ueGyndHXsfUBlcW2rbnnzbIVlKGmQT2Og[ZhxemW|c3nvci=> NELybnkzOzJ|NkO3NC=>
NRK-52E  MV3GeY5kfGmxbjDBd5NigQ>? MV:1xsDPxE1? M{jOc|MxyqCvaX6= NH3iZVFifHSnboXheIV{KEGwZz2oNgKBmzdrLXnubIljcXSnZDDUS2Yu|rJzIH3SUmEh[XRiMUdCpIjDqA>? M2riNVI{OTd2N{W3
SW620  MWPGeY5kfGmxbjDBd5NigQ>? MYOyNEDDvU1? NXPyS4JzOS94IHi= Mm\1bY5pcWKrdIOgdE1UXEGWMzDhZ5RqfmG2aX;u NF3vOVAzOzFzME[yOS=>
RPE  M{TsWmZ2dmO2aX;uJGF{e2G7 MU[zNEDDvU4EoB?= MWmzJIg> NH;qTlVqdmirYnn0d{B1cGViaX7keYN1cW:wIH;mJJAuW1SDVEOg[ZhxemW|c3nvci=> NHXJVoozOzB7NEC2Oy=>
SW1116 MX7GeY5kfGmxbjDBd5NigQ>? M2TKWlExOCEEtV5CpC=> NYLy[|VLOjRxNEivO|IhcA>? MoXo[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? M1PYWVIzODVyN{mw
HT29 MkLNSpVv[3Srb36gRZN{[Xl? MUexNFAhyrWPwrC= NYPte5FOOjRxNEivO|IhcA>? NYHrdoZD\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= NIPPUpozOjB3MEe5NC=>
SW1116 NFrMV49HfW6ldHnvckBCe3OjeR?= NYT6U5k4OTByINM1UeKh Mm\hNlQwPDhxN{KgbC=> M{H3V4Rm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh MljGNlIxPTB5OUC=
HT29 NYfPOHBkTnWwY4Tpc44hSXO|YYm= MWKxNFAhyrWPwrC= MnH0NlQwPDhxN{KgbC=> MmPs[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> MoixNlIxPTB5OUC=
ARPE-19 Ml7sSpVv[3Srb36gRZN{[Xl? NVrXTHZ7PcLizszN M4[3e|MxyqCvaX6= NVfvVpRPcW6qaXLpeJMhUkGNMjDwbI9{eGixcnnsZZRqd25? M{i4O|IyPjJyOU[z
HSC-T6 NED0NVRCeG:ydH;zbZMhSXO|YYm= M4P2dlExyqEQvF2= NIrRXmwzyqCqwrC= NXz5S2NrcW6qaXLpeJMhfGinIHHwc5B1d3OrczDv[kBJW0NvVE[gZ4VtdHNiaX7keYNm\CCkeTDDSGU> NEjqO2gzOTN7Nkm5PC=>
HSC-T6 M4rTdGZ2dmO2aX;uJGF{e2G7 MVOxNOKh|ryP NYHydI9XOsLiaNMg MWfpcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? M4W2SFIyOzl4OUm4
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MZ-304 MmizSpVv[3Srb36gRZN{[Xl? MX61NE8yODEEoN88US=> NUn3e4lQPDhiaB?= MXvy[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= MnO2NlA2QDl3MkW=
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MZ-304 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\KR|UxNzFyMNMg{txO NXTydVFtPDhiaB?= MYDs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? NITFOpkzODV6OUWyOS=>
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MZ-18 NUexcYFUTnWwY4Tpc44hSXO|YYm= MYC1NE8yODEEoN88US=> NVjXXWl[PDhiaB?= MlqwbY5pcWKrdIOgcYloemG2aX;u MlHiNlA2QDl3MkW=
MZ-54 NWrLdndqTnWwY4Tpc44hSXO|YYm= MVS1NE8yODEEoN88US=> NVq3PHZIPDhiaB?= MlfHbY5pcWKrdIOgcYloemG2aX;u MV[yNFU5QTV{NR?=
MZ-256 Mli2SpVv[3Srb36gRZN{[Xl? MXi1NE8yODEEoN88US=> NFPTeVI1QCCq NXy0OmhFcW6qaXLpeJMhdWmpcnH0bY9v MmjRNlA2QDl3MkW=
MZ-304 MVjGeY5kfGmxbjDBd5NigQ>? MUG1NE8yODEEoN88US=> MXq0PEBp MljNbY5pcWKrdIOgcYloemG2aX;u NWPEbJZ[OjB3OEm1NlU>
A-172 MkK3SpVv[3Srb36gRZN{[Xl? M1TOelExOMLizszN Mn;WOFghcA>? NIHhSHpqdmirYnn0d{Bqdn[jc3nvci=> NYfHZ2tsOjB3OEm1NlU>
MZ-18 NHXJe4VHfW6ldHnvckBCe3OjeR?= MWGxNFDDqM7:TR?= M3jZb|Q5KGh? MVfpcohq[mm2czDpcpZie2mxbh?= NXvLc5FMOjB3OEm1NlU>
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MZ-304 MXTGeY5kfGmxbjDBd5NigQ>? NGHOSVIyODEEoN88US=> MmiwOFghcA>? NEKxbHdqdmirYnn0d{Bqdn[jc3nvci=> MlzONlA2QDl3MkW=
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SW1990 M1\LVWlvfmG|aX;uJGF{e2G7 MYGyNEDPxE1? MlPJNlQhcA>? MofTdoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= M3n2TlIxPDh{OEW4
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BMMC MYTGeY5kfGmxbjDBd5NigQ>? M1fGblAuOTBizszN NYfGflN4OTYEoH3pci=> NHKzWZFqdmirYnn0d{BNXEN2wrDy[Yxm[XOnIHnuJIEh\G:|ZT3k[ZBmdmSnboSg[oF{cGmxbjD3bZRpKG6nYYKgZ49ueGyndHWgbY5pcWKrdHnvckBifCClb37j[Y51emG2aX;ud{Djsb5zMNMg{txO MUmxPVg{PTh2NR?=
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PA-1 MnLiSpVv[3Srb36gRZN{[Xl? Ml;FNVAhfU1? NWXRNnVQOSCq MYDpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? Ml6zNVk3PDd|NkO=
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Jurkat  M2ryTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3NfmNvPTBizszN M2L3bVI1NzR6L{eyJIg> NVe0c3Bo\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v NXXYRY9uOTl3NkS4PVE>
SUPT1  M1\LVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHHTJp6PTBizszN NX\XVGdIOjRxNEivO|IhcA>? M3ftR4VvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> NIT2bZoyQTV4NEi5NS=>
Jurkat  M4HhVGFxd3C2b4Ppd{BCe3OjeR?= MnztOVAh|ryP NGjnN3QzPC92ODDo NHHtWW5mdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ NYrZTINnOTl3NkS4PVE>
SUPT1  NUnQdJFjSXCxcITvd4l{KEG|c3H5 NHjrNJo2OCEQvF2= MWeyOE81QCCq NWf5Nmhx\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M37rNlE6PTZ2OEmx

... 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