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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Cited by 28 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 M3zBbGZ2dmO2aX;uJGF{e2G7 M13lXFExOOLCidM1US=> NH;lUXIzPCCq Ml:0cYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz MUKyOlE5PDl7OR?=
BCBL1 NIjaRZVHfW6ldHnvckBCe3OjeR?= MVWxNFDjiIoEtV2= Moq0NlQhcA>? MVTt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= MmHxNlYyQDR7OUm=
BC3 NGntWJFHfW6ldHnvckBCe3OjeR?= MUexNFDjiIoEtV2= NUPMPVFXOjRiaB?= MlfXcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? NXSwSItIOjZzOES5PVk>
BCBL1 MkLMSpVv[3Srb36gRZN{[Xl? NEfHdJAyODEkgJpCuW0> M4Hr[FI1KGh? MVft[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? NHrMbGUzPjF6NEm5PS=>
BC3 MXvGeY5kfGmxbjDBd5NigQ>? NETCO4kyODEkgJpCuW0> NHO5XIszPCCq M2[yXolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKG[udYlCpC=> MnHPNlYyQDR7OUm=
BCBL1 NV;vZos1TnWwY4Tpc44hSXO|YYm= NV\yPZVnOTBy4pEJxtVO MVSyOEBp NFPNcVlqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> M4jsZ|I3OTh2OUm5
SK-MEL-28 MkjQSpVv[3Srb36gRZN{[Xl? NYDmTnZjPTBxMUCw5qCKyrWP NXXX[Xp7PDhiaB?= MWfEUXNQ NFTTPFVz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MnXONlUzOTZ3MkK=
MeWo MonJSpVv[3Srb36gRZN{[Xl? MUm1NE8yODEkgJpCuW0> NE\Qepo1QCCq M2HkbWROW09? M3;HXpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NWWxcG1POjV{MU[1NlI>
SK-MEL-5 M3jpZWZ2dmO2aX;uJGF{e2G7 MlTKOVAwOTBy4pEJxtVO M{CzU|Q5KGh? MVfEUXNQ MUDy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MkP0NlUzOTZ3MkK=
SK-MEL-2 Ml\aSpVv[3Srb36gRZN{[Xl? M4T1SFUxNzFyMPMAjeK2VQ>? MVu0PEBp NHLGRopFVVOR NY\s[VBEemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MYGyOVIyPjV{Mh?=
B16-F0 MmO2SpVv[3Srb36gRZN{[Xl? MoXpOVAwOTBy4pEJxtVO MV[0PEBp Mn75SG1UVw>? M2naeJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NHXLPIkzPTJzNkWyNi=>
TRPM2/HEK  MYjGeY5kfGmxbjDBd5NigQ>? NEOxd5gxNjIkgKOyOeKhyrWP NU\mWpZUOTYEoH3pci=> MnvJSG1UVw>? NYTCeo86emWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCxMlfDqML3TR?= NEW4d5YzPTF5OUW3OC=>
U937  MlvQSpVv[3Srb36gRZN{[Xl? NF;KN44xNjIkgKOyOeKhyrWP MljYNVXDqG2rbh?= M4rvRmROW09? MmKzdoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? NInyNWszPTF5OUW3OC=>
TRPM2/HEK  NGrM[ZBHfW6ldHnvckBCe3OjeR?= MY[xNOKhyrWP NFrIPVM1OMLibXnu NHPLWHBFVVOR MWDy[YR2[2W|IGTSVG0zKGGldHn2ZZRqd25iZY\lckBifCCqaXfoJINwdmOnboTyZZRqd26|IH;mJGgzVzJ? MnzsNlUyPzl3N{S=
GL37  NGP0TplE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX:4VYRuOC1zMNMgxtVO NXzxUoVXPDhiaB?= NG\qO2p{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= Mlv5NlQ6QTl4NUe=
NRK-52E M4Kyb2Z2dmO2aX;uJGF{e2G7 MnjONeKhyrWP NFPKdpEyOCCvaX6= MVzicI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi NGPvTVMzPDdzMESyNy=>
NRK-52E M{jnbmZ2dmO2aX;uJGF{e2G7 MkL0NeKhyrWP Mn;CNVAhdWmw M3PDToJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> MWiyOFcyODR{Mx?=
HSC  M2C0VGZ2dmO2aX;uJGF{e2G7 Mo[yNlAh|ryP NIrWb48yKGh? M2juVYFjem:pYYTld{B1cGViZHnm[oVz\W62aXHsJIVn\mWldIOgc4YhdGWydHnuJI9zKEGJRYO= M3u1dlI1PjF2MUm5
EJ NVrC[olGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;IXlUxNzhyIN88US=> MnjXNlQwPDhxN{KgbC=> NHn6[2VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MkexNlQ2QDdyNEm=
EJ MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT4TIk3PTBxOECg{txO MmrrOFghcA>? NIDv[3Jk[XW|ZYOgV{1xcGG|ZTDhdpJme3R? MoDtNlQ2QDdyNEm=
EJ Mmj3SpVv[3Srb36gRZN{[Xl? NYjCZVJmPTBxOECg{txO M3y4dlQ5KGh? MUXkc5dvemWpdXzheIV{KGNvTYnjMEBkgWOuaX7ENUwhe3W{dnn2bY4h[W6mIG\FS2Yh\XiycnXzd4lwdnN? NEjlZWIzPDV6N{C0PS=>
HepG2 MnHiSpVv[3Srb36gRZN{[Xl? NVzvclR2PTBvNUCwJO69VQ>? NWHHRXY3PjEEoH3pci=> NFz3XGNqdmirYnn0d{B1cGViSVytOk1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTCoWJlzPzB3KTDhcoQhW1SDVEOgLHR6ejdyNTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NFK4XZczPDJ2MkC0Oi=>
SGC7901 NWHwTVliS2WubDDWbYFjcWyrdImgRZN{[Xl? NWjpNpBrOC1zMECg{txO NFXRZ2IzPC92OD:3NkBp NU[0eGc6[2G3c3XzJIEhe2mpbnnmbYNidnRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHTvd4Uu\GWyZX7k[Y51dHliYoX0JI5wfCC2aX3lMYRmeGWwZHXueIx6 NUK4OpJHOjRzNUGyOVU>
AGS  NITBe4dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn\JNE0yODBizszN NVXqXJkzOjRxNEivO|IhcA>? NX3RSnBK[2G3c3XzJIEhe2mpbnnmbYNidnRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHTvd4Uu\GWyZX7k[Y51dHliYoX0JI5wfCC2aX3lMYRmeGWwZHXueIx6 NXv5cW1MOjRzNUGyOVU>
SGC7901 MlHVSpVv[3Srb36gRZN{[Xl? NXv4ZZJvPTBizszN MWKyOE81QC95MjDo NGjhbpV1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> MWGyOFE2OTJ3NR?=
AGS  NXLOdFVkTnWwY4Tpc44hSXO|YYm= MWO1NEDPxE1? NVjRWnhpOjRxNEivO|IhcA>? MW\0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= NWDueFkzOjRzNUGyOVU>
SGC7901 MYfGeY5kfGmxbjDBd5NigQ>? NGLacoM2OCEQvF2= NXzrSmFkOjRxNEivO|IhcA>? MUH0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> NXfOcnM{OjRzNUGyOVU>
AGS  M2\RbWZ2dmO2aX;uJGF{e2G7 M4DS[VUxKM7:TR?= NVPZVm5iOjRxNEivO|IhcA>? MkjVeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> MXyyOFE2OTJ3NR?=
MC3T3-E1  M{\6TGZ2dmO2aX;uJGF{e2G7 NHjtXVE2OCEQvF2= NHn6ZmE1KGh? MUXpcohq[mm2czDIV2UucW6mdXPl[EBDVVB5IHHu[EBIUFJicILveIVqdiCneIDy[ZN{cW:wwrC= NVe4enlOOjN6N{e3N|Q>
7TD1-DXM MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKxNEDPxE1? NIflWXQ4OiCq M4HmOGROW09? MWLpcohq[mm2czDj[YxtKGe{b4f0bC=> NVjt[3J3OjN6N{GxOVk>
7TD1-WD-90 M1rNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{S2VVExKM7:TR?= M3rGRlczKGh? NVnWbGduTE2VTx?= NX7lbHRzcW6qaXLpeJMh[2WubDDndo94fGh? MnnKNlM5PzFzNUm=
7TD1-DXM M3fqTWFxd3C2b4Ppd{BCe3OjeR?= NIe2ZY42OCEQvF2= NIr4[|c1QCCq NHfIWI9FVVOR M{WzeIlv\HWlZYOgZZBweHSxc3nz NH7ldHAzOzh5MUG1PS=>
7TD1-WD-90 NG[yT|lCeG:ydH;zbZMhSXO|YYm= MUS1NEDPxE1? NGDhUWk1QCCq M1TRW2ROW09? Mnv4bY5lfWOnczDhdI9xfG:|aYO= M1W0S|I{QDdzMUW5
7TD1-WD-90  MYPGeY5kfGmxbjDBd5NigQ>? NX7qd3Z2PTBizszN MXW2JIg> NXTVe2R6TE2VTx?= MYrzbYdvcW[rY3HueIx6KGmwaHnibZR{KHSqZTDwbI9{eGixconsZZRqd25ib3[gTmFMOiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVR| NWjDVVE4OjN6N{GxOVk>
HepG2  NFjMW5RHfW6ldHnvckBCe3OjeR?= M3rjblExOCEQvF2= NEPrVZAyOi9{NDDo NWC5W|ZUcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:w Mmj3NlM5OzZ2MEC=
RAW264.7  Mm\qSpVv[3Srb36gRZN{[Xl? NYDQd4M5PTEEoN88UeKh NXrRS|NMOjRxNEigbC=> Mnrxd5VxeHKnc4Pld{BTSU6NTD3pcoR2[2WmIH;zeIVw[2yjc4Tv[4Vv\XOrcx?= MmfmNlM3PjVyMUi=
RAW264.7 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjXPXMxNTVywrFOwG3DqA>? M{XCN|Q5yqCq MkKzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> NHnMe40zOzZ4NUCxPC=>
RAW264.7 M3jYSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzPNE02OMLizszNxsA> NX;lZVc1PDkEoHi= M3vTUYNifXOnczDhckBienKnc4Sgc4YhWkGZMk[0Mlch[2WubIOgZZQhfGinIFewM2cyKHCqYYPlJI9nKHSqZTDj[YxtKGO7Y3zl Mn:3NlM3PjVyMUi=
RAW264.7 MmPZSpVv[3Srb36gRZN{[Xl? MnPHOVDDqM7:TR?= MXGyOE81QCCq MWLpcohq[mm2czDSRW5MVC2rbnT1Z4VlKE6IQWTjNUBmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gV4VzPzJ5U2TBWFM> NGfrb3kzOzZ4NUCxPC=>
A549  NIqzTlFHfW6ldHnvckBCe3OjeR?= MWGyNE81OCEQvF2= NIfsRoQzOCCq MV6yNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? MYiyN|YzODF7MR?=
A549  MUjGeY5kfGmxbjDBd5NigQ>? MlTtNVAwOjBxNECg{txO MmrsNlQhcA>? NYfTdoIze3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> NWXWcmQzOjN4MkCxPVE>
HUVECs MkfIR4VtdCCYaXHibYxqfHliQYPzZZk> NYTuc5B4OjBiwsXN NHfWWJg1KGh? MULheJRmdnWjdHXzJGgzVzJvaX7keYNm\CClZXzsJJNpemmwa3Hn[UBidmRiaX3wdo93\WRidHjlJIF1fGGlaH3lcpQhemG2ZTDv[kB1cGViY3XscJM> MnjvNlM1QDN7NE[=
HUVECs MWDBdI9xfG:|aYOgRZN{[Xl? MlLsNlAhyrWP NUPiZ4lFPCCq NYKzeolie2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 Mk[5NlM1QDN7NE[=
BV-2  M2GzWWZ2dmO2aX;uJGF{e2G7 MVOyNEDDvU1? M2PvOFE3KGh? NFjibFRqdmirYnn0d{BNWFNvaX7keYNm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCjbH3vd5Qh[2:vcHzleIVtgSCmaX3pcol{cGWmIHnOU3Mh\XiycnXzd4lwdg>? NH;UOWozOzJ|NkO3NC=>
NRK-52E  NX3yd5Q6TnWwY4Tpc44hSXO|YYm= MXq1xsDPxE1? M{\WOVMxyqCvaX6= MYrheJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> MVeyN|E4PDd3Nx?=
SW620  MkDoSpVv[3Srb36gRZN{[Xl? M4TEelIxKML3TR?= NHLsOY8yNzZiaB?= NV6yS3NscW6qaXLpeJMheC2VVFHUN{Bi[3SrdnH0bY9v MnLuNlMyOTB4MkW=
RPE  NYXQZYtMTnWwY4Tpc44hSXO|YYm= MUGzNEDDvU4EoB?= MmDuN{Bp NFrvUIpqdmirYnn0d{B1cGViaX7keYN1cW:wIH;mJJAuW1SDVEOg[ZhxemW|c3nvci=> NHvoNZIzOzB7NEC2Oy=>
SW1116 NHW5cGZHfW6ldHnvckBCe3OjeR?= NFrFOIkyODBiwsXNxsA> MnLlNlQwPDhxN{KgbC=> NGi0eGhl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= Ml65NlIxPTB5OUC=
HT29 MUPGeY5kfGmxbjDBd5NigQ>? M3zhZVExOCEEtV5CpC=> M1;JWVI1NzR6L{eyJIg> NFzHSnJl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= MlLINlIxPTB5OUC=
SW1116 NWPzVIJITnWwY4Tpc44hSXO|YYm= MWmxNFAhyrWPwrC= MWOyOE81QC95MjDo M4HVSYRm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh MX:yNlA2ODd7MB?=
HT29 NX\IOZlKTnWwY4Tpc44hSXO|YYm= MXSxNFAhyrWPwrC= NVjJXJJpOjRxNEivO|IhcA>? NGO5PJFl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NES4U28zOjB3MEe5NC=>
ARPE-19 NHPIWXVHfW6ldHnvckBCe3OjeR?= M3LpRlXDqM7:TR?= NIXU[W0{OMLibXnu M4DUTolvcGmkaYTzJGpCUzJicHjvd5Bpd3KrbHH0bY9v M2PyOFIyPjJyOU[z
HSC-T6 MWrBdI9xfG:|aYOgRZN{[Xl? Ml3INVDDqM7:TR?= M3PzTFLDqGkEoB?= M3TwW4lvcGmkaYTzJJRp\SCjcH;weI9{cXNib3[gTHNENVR4IHPlcIx{KGmwZIXj[YQh[nliQ1TF NUi3R|NnOjF|OU[5PVg>
HSC-T6 MlK1SpVv[3Srb36gRZN{[Xl? NYKxPVZtOTEEoN88US=> MXWyxsBpyqB? NGrMRYFqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= MXuyNVM6Pjl7OB?=
Hep-2 M1ro[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOyOU0yODBizszN M37aflI1NzR6L{eyJIg> NX\lVXhlcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NVP4XlUzOjF|MEm0PFE>
Hep-2 NEXmbZJCeG:ydH;zbZMhSXO|YYm= MUG1NEDPxE1? MX6yOE81QC95MjDo M2nkVolv\HWlZYOgZ4VtdCCjcH;weI9{cXNidHnt[UBl\XCnbnTlcpRtgQ>? NICzSlYzOTNyOUS4NS=>
Hep-2 MWHGeY5kfGmxbjDBd5NigQ>? M33iblUxKM7:TR?= NEjjZ5EzPC92OD:3NkBp MmLpbY5pcWKrdIOgS|EhfG9iUzDj[YxtKGO7Y3zlJJRz[W6|aYTpc44h[W6mIHnu[JVk\XNiR{GgZ4VtdCCleXPs[UBienKnc4S= MXyyNVMxQTR6MR?=
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KF8 MmjESpVv[3Srb36gRZN{[Xl? NULDWVZLOTEEoN88UeKh MkT6NeKhcMLi NWL5[4p3TE2VT9Mg NVTkUXBGcW6qaXLpeJMhUUxvM{OtbY5lfWOnZDDJ{tpD|rFiZHXndoFl[XSrb36gZY5lKE6ILd86RkBi[3SrdnH0bY9v MYeyNFk1ODB2NR?=
HEL  M33uVGZ2dmO2aX;uJGF{e2G7 MXGxNFDDqM7:TR?= NY\zTVhNOTJvN{KgbC=> M{GwdYlvcGmkaYTzJJRp\SCuZY\lcEBw\iCyLVrBT|ItKEqDS{K= NEfOfmEzODZ{MUC2NS=>
HEL M2ewTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDXfYd1OTBywrFOwG0> MUGwMVUh\A>? NEjwT4tz\WS3Y3XzJIdzd3e2aDDv[kBLSUt{Vk[xO2Yu\XiycnXzd4lv\yCKRVygZ4VtdHN? M2Tv[lIxPjJzME[x
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MZ-54 NGnSbXVHfW6ldHnvckBCe3OjeR?= MXi1NE8yODEEoN88US=> M4HWcFQ5KGh? M4Hhb5Jm\HWlZYOgeIhmKGyndnXsd{Bw\iClb37zeIl1fXSrdnXsfUBi[3SrdnH0[YQhW1SDVEOgbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQh\mG|aHnvci=> MlXPNlA2QDl3MkW=
MZ-256 MXLGeY5kfGmxbjDBd5NigQ>? NF3rb2g2OC9zMEFCpO69VQ>? NYrxR5hCPDhiaB?= MVvy[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= MoX3NlA2QDl3MkW=
MZ-304 M2r6cGZ2dmO2aX;uJGF{e2G7 MVq1NE8yODEEoN88US=> MWK0PEBp M2fmdpJm\HWlZYOgeIhmKGyndnXsd{Bw\iClb37zeIl1fXSrdnXsfUBi[3SrdnH0[YQhW1SDVEOgbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQh\mG|aHnvci=> MUSyNFU5QTV{NR?=
A-172 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFK4Xpg2OC9zMEFCpO69VQ>? NUD4d4kyPDhiaB?= NXLTUolHdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MnHVNlA2QDl3MkW=
MZ-18 NV\NR217T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXrS2M2OC9zMEFCpO69VQ>? MVG0PEBp M2fPV4xm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= M1T3U|IxPTh7NUK1
MZ-54 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TtTFUxNzFyMNMg{txO MUO0PEBp MmHmcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq MnzyNlA2QDl3MkW=
MZ-256 MkjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;XUlUxNzFyMNMg{txO M1:wTlQ5KGh? NUnQRZFJdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo NWPnbI4zOjB3OEm1NlU>
MZ-304 Ml3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfVZoFkPTBxMUCwxsDPxE1? M{jPTlQ5KGh? MkPScIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq MUeyNFU5QTV{NR?=
A-172 NV3sOWNzTnWwY4Tpc44hSXO|YYm= NYnTPWt4PTBxMUCwxsDPxE1? MojjOFghcA>? NX7He3BEcW6qaXLpeJMhdWmpcnH0bY9v MVmyNFU5QTV{NR?=
MZ-18 M1XGOmZ2dmO2aX;uJGF{e2G7 M4jpcVUxNzFyMNMg{txO NVXvUWtbPDhiaB?= M2GwUYlvcGmkaYTzJI1q\3KjdHnvci=> NGj0eJczODV6OUWyOS=>
MZ-54 M1LTWGZ2dmO2aX;uJGF{e2G7 Ml64OVAwOTBywrFOwG0> MUO0PEBp MlfrbY5pcWKrdIOgcYloemG2aX;u NI[0WFQzODV6OUWyOS=>
MZ-256 MV;GeY5kfGmxbjDBd5NigQ>? NF74UWQ2OC9zMEFCpO69VQ>? NWPaNW42PDhiaB?= Mn\CbY5pcWKrdIOgcYloemG2aX;u NIn2emYzODV6OUWyOS=>
MZ-304 NIqyepJHfW6ldHnvckBCe3OjeR?= NVrkRlUzPTBxMUCwxsDPxE1? NIm4UVg1QCCq M4TIWYlvcGmkaYTzJI1q\3KjdHnvci=> MnXQNlA2QDl3MkW=
A-172 MXPGeY5kfGmxbjDBd5NigQ>? MX6xNFDDqM7:TR?= MYe0PEBp M3HkW4lvcGmkaYTzJIlvfmG|aX;u NIS2cHozODV6OUWyOS=>
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MZ-54 MnnqSpVv[3Srb36gRZN{[Xl? M4jXSlExOMLizszN M4HHbVQ5KGh? NE\DbFFqdmirYnn0d{Bqdn[jc3nvci=> Mmn6NlA2QDl3MkW=
MZ-256 NF\Sb3hHfW6ldHnvckBCe3OjeR?= NEizcWkyODEEoN88US=> M1\sVFQ5KGh? NHizZVBqdmirYnn0d{Bqdn[jc3nvci=> NUHnTFU2OjB3OEm1NlU>
MZ-304 M2TIUGZ2dmO2aX;uJGF{e2G7 NFXpfFEyODEEoN88US=> M4PSclQ5KGh? M4\JdolvcGmkaYTzJIlvfmG|aX;u NX7KepBXOjB3OEm1NlU>
A-172 M4H0O2Z2dmO2aX;uJGF{e2G7 NHWyeos2OC9zMEFCpO69VQ>? MV20PEBp NFnhflVz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M1vpT|IxPTh7NUK1
MZ-18 MYHGeY5kfGmxbjDBd5NigQ>? MoTHOVAwOTBywrFOwG0> M4LJfVQ5KGh? M3PTRpJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> M1T2WFIxPTh7NUK1
MZ-54 MVLGeY5kfGmxbjDBd5NigQ>? Mkn4OVAwOTBywrFOwG0> NF:2Rmg1QCCq M4DETJJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> NWnQPJpbOjB3OEm1NlU>
MZ-256 NVTTe4dITnWwY4Tpc44hSXO|YYm= MWK1NE8yODEEoN88US=> MnXIOFghcA>? NFm3XoJz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M{fHXFIxPTh7NUK1
MZ-304 MXzGeY5kfGmxbjDBd5NigQ>? NX;vU5g{PTBxMUCwxsDPxE1? NF63PG81QCCq NWjpco04emWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? NG\CVJYzODV6OUWyOS=>
SW1990 M4nVfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\BeYQzOCEQvF2= NGfLVnAzPC92OD:3NkBp MWfpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 M1vTclIxPDh{OEW4
SW1990 NXf6dJNNTnWwY4Tpc44hSXO|YYm= MVWyNEDPxE1? NEnvWZgzPCCq MXLk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gUW1RNTJiYX7kJHZGT0ZibWLORZM> MUOyNFQ5Ojh3OB?=
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SW1990 M3HVdGlvfmG|aX;uJGF{e2G7 NIC2RXUzOCEQvF2= MVeyOEBp M1q5cpJm\HWlZYOgbY53[XOrb36gc4YhW1dzOUmwJINmdGy|wrC= MV2yNFQ5Ojh3OB?=
THP1 M{jYPGZ2dmO2aX;uJGF{e2G7 MnXXNVAhfU1? M4q2c|MxKG2rbtMg M3fwUIlvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCkeTDveoVzKDZyJR?= NIO0ZYozODN7M{[5NC=>
BMMC MkfnSpVv[3Srb36gRZN{[Xl? M2jHfVAuOTBizszN MX6xOeKhdWmw MnPwbY5pcWKrdIOgUHREPMLicnXs[YF{\SCrbjDhJIRwe2VvZHXw[Y5l\W62IH\hd4hqd25id3n0bEBv\WG{IHPvcZBt\XSnIHnubIljcXSrb36gZZQh[2:wY3XueJJifGmxboOg5sm,OTEEoN88US=> MUGxPVg{PTh2NR?=
A549 M3jjPWZ2dmO2aX;uJGF{e2G7 MnvTNVUh|ryv M4fkNlEhcA>? NVvnSZZFcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSCxbjD0fZJwe2mwZTC3NFEhf2G|IHTleIVkfGWmIEG1JI1qdiCjZoTldkBUWEViQjD0doVifG2nboS= Mki1NVk5ODF4NkW=
OVCAR-3 MkDySpVv[3Srb36gRZN{[Xl? Mlz1NVAhfU1? MX:xJIg> MWLpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? NXvYTpVCOTl4NEezOlM>
PA-1 NXW3dWNJTnWwY4Tpc44hSXO|YYm= NFnsU24yOCC3TR?= MYqxJIg> M33HW4lvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= NITtd|kyQTZ2N{O2Ny=>
OVCAR-3 MUPGeY5kfGmxbjDBd5NigQ>? M1WzeVExKHWP MmLSNUBp MW\pcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? MVGxPVY1PzN4Mx?=
PA-1 Ml:xSpVv[3Srb36gRZN{[Xl? NIXxSWsyOCC3TR?= NIX0WncyKGh? M1j4WIlvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 M4XnRVE6PjR5M{[z
Jurkat  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:1NEDPxE1? M1vURVI1NzR6L{eyJIg> M3vHVIVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> MXOxPVU3PDh7MR?=
SUPT1  Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUK1NEDPxE1? M1TNSFI1NzR6L{eyJIg> MYrlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= M3LWPFE6PTZ2OEmx
Jurkat  MVrBdI9xfG:|aYOgRZN{[Xl? M3v0dlUxKM7:TR?= MVmyOE81QCCq MWflcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz MUmxPVU3PDh7MR?=
SUPT1  M3;CWmFxd3C2b4Ppd{BCe3OjeR?= MVy1NEDPxE1? MYiyOE81QCCq NF3qVWhmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MYGxPVU3PDh7MR?=

... 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(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

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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.

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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