AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

99 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 99 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 M2XvbmZ2dmO2aX;uJGF{e2G7 MX[xNFDjiIoEtV2= NFO2RmIzPCCq NF\BUXZu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> MY[yOlE5PDl7OR?=
BCBL1 MVfGeY5kfGmxbjDBd5NigQ>? NWLCdVc{OTBy4pEJxtVO NFGxelYzPCCq M2TwWY1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> NF3UdIQzPjF6NEm5PS=>
BC3 MYLGeY5kfGmxbjDBd5NigQ>? NIjESWEyODEkgJpCuW0> NIfKeFUzPCCq NVLVTVA6dWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMTDy[YR2[3Srb36= M3r1UVI3OTh2OUm5
BCBL1 MW\GeY5kfGmxbjDBd5NigQ>? M1rzRVExOOLCidM1US=> Mln0NlQhcA>? MUHt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? NY\wSYc4OjZzOES5PVk>
BC3 NY\x[4lQTnWwY4Tpc44hSXO|YYm= MlLINVAx6oDLwsXN NUj3bII6OjRiaB?= NV7hVnFicW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh Ml;MNlYyQDR7OUm=
BCBL1 MY\GeY5kfGmxbjDBd5NigQ>? Ml3RNVAx6oDLwsXN MU[yOEBp NYjPU3RKcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh M{HITVI3OTh2OUm5
SK-MEL-28 NVXDXXpLTnWwY4Tpc44hSXO|YYm= MXm1NE8yODEkgJpCuW0> NEnxNVA1QCCq MWXEUXNQ MVry[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= M2HPUVI2OjF4NUKy
MeWo M3PrNGZ2dmO2aX;uJGF{e2G7 MlPzOVAwOTBy4pEJxtVO NEXLdYg1QCCq NXrDUpQyTE2VTx?= NH;0TnNz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MlrJNlUzOTZ3MkK=
SK-MEL-5 MoSzSpVv[3Srb36gRZN{[Xl? Ml3rOVAwOTBy4pEJxtVO NIfoZXc1QCCq M4n4VWROW09? NHizT2Nz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> M{PHfFI2OjF4NUKy
SK-MEL-2 NUDpcmprTnWwY4Tpc44hSXO|YYm= NFzIXHo2OC9zMEFihKnDvU1? M3XtPVQ5KGh? NHPyb2pFVVOR NXTxepZqemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> M4rRdVI2OjF4NUKy
B16-F0 MV3GeY5kfGmxbjDBd5NigQ>? MXq1NE8yODEkgJpCuW0> NFftboI1QCCq NXjObHQ{TE2VTx?= MUTy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MXyyOVIyPjV{Mh?=
TRPM2/HEK  MVXGeY5kfGmxbjDBd5NigQ>? M1rsZ|AvOeLCk{K1xsDDvU1? NUTYXnd2OTYEoH3pci=> MY\EUXNQ NFPjT2Zz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IEGuO:KhyrWP NHizdJQzPTF5OUW3OC=>
U937  M3zCW2Z2dmO2aX;uJGF{e2G7 MVWwMlHjiJN{NdMgxtVO NWPncHJFOTYEoH3pci=> NWLlV5ZjTE2VTx?= NX;0OYg1emWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= NUfGSohQOjVzN{m1O|Q>
TRPM2/HEK  Mlm3SpVv[3Srb36gRZN{[Xl? MYqxNOKhyrWP NGSzfVY1OMLibXnu MXnEUXNQ Mmi4doVlfWOnczDUVnBOOiCjY4TpeoF1cW:wIHX2[Y4h[XRiaHnnbEBkd26lZX70doF1cW:wczDv[kBJOk9{ MoL5NlUyPzl3N{S=
GL37  MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlvNNE0yOMLiwsXN MmfXOFghcA>? NU\6ZlQ3e3WycILld5NmeyCOYTDlfJBz\XO|aX;u MYCyOFk6QTZ3Nx?=
NRK-52E NGfsOZFHfW6ldHnvckBCe3OjeR?= MkXONeKhyrWP M3XoeVExKG2rbh?= NGrDN3ZjdG:la4OgeIhmKHO2aX31cIF1d3K7IHXm[oVkfCCxZjDBcochUUlib36gVIF5NTJiZYjwdoV{e2mxbtMg NFvqXIgzPDdzMESyNy=>
NRK-52E NIHveY9HfW6ldHnvckBCe3OjeR?= NVnBSph[OcLiwsXN NGPhZXYyOCCvaX6= MkfOZoxw[2u|IFHu[{BKUSCrbnT1Z4VlKEOGMkSg[ZhxemW|c3nvci=> NX7GclNoOjR5MUC0NlM>
HSC  M4P4cGZ2dmO2aX;uJGF{e2G7 Mn3KNlAh|ryP MkfUNUBp M1XKOIFjem:pYYTld{B1cGViZHnm[oVz\W62aXHsJIVn\mWldIOgc4YhdGWydHnuJI9zKEGJRYO= NXnkPWx[OjR4MUSxPVk>
EJ MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYS1NE85OCEQvF2= M3fvdVI1NzR6L{eyJIg> NF7p[25qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NVXBeXM1OjR3OEewOFk>
EJ NUjQdJR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PHWFUxNzhyIN88US=> M3P2Z|Q5KGh? M3P6UYNifXOnczDTMZBp[XOnIHHydoV{fA>? MWCyOFU5PzB2OR?=
EJ MoXYSpVv[3Srb36gRZN{[Xl? NFzvdG42OC96MDFOwG0> NHTkPWs1QCCq NYPKVoUy\G:5boLl[5Vt[XSnczDjMW16[yxiY4njcIlvTDFuIIP1dpZqfmmwIHHu[EBXTUeIIHX4dJJme3Orb37z M1nZb|I1PTh5MES5
HepG2 M3rVTGZ2dmO2aX;uJGF{e2G7 M1fEeVUxNTVyMDFOwG0> MoL0OlDDqG2rbh?= MWXpcohq[mm2czD0bIUhUUxvNj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSBqVInyO|A2MSCjbnSgV3RCXDNiKGT5dlcxPSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXqyOFI1OjB2Nh?=
SGC7901 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2XIS|AuOTByIN88US=> NITiV5MzPC92OD:3NkBp MkDUZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 M{j4ZVI1OTVzMkW1
AGS  NX[1NGVrS2WubDDWbYFjcWyrdImgRZN{[Xl? MVqwMVExOCEQvF2= MlfxNlQwPDhxN{KgbC=> MmSxZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 M{nXVVI1OTVzMkW1
SGC7901 NUTORmpzTnWwY4Tpc44hSXO|YYm= NHT3fHE2OCEQvF2= M2HJ[FI1NzR6L{eyJIg> Mo\YeIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= MXSyOFE2OTJ3NR?=
AGS  NXW2S4MzTnWwY4Tpc44hSXO|YYm= NWnVd5hNPTBizszN NYjUOJppOjRxNEivO|IhcA>? NFzVc3d1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> NFjTfmYzPDF3MUK1OS=>
SGC7901 M1u3e2Z2dmO2aX;uJGF{e2G7 MXW1NEDPxE1? M2X0bFI1NzR6L{eyJIg> MlvSeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> NFjzVpIzPDF3MUK1OS=>
AGS  NV7IRWp2TnWwY4Tpc44hSXO|YYm= M{jM[FUxKM7:TR?= NFnuXXozPC92OD:3NkBp M3TqWJRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz NGfK[pYzPDF3MUK1OS=>
MC3T3-E1  M{e2RmZ2dmO2aX;uJGF{e2G7 MlnEOVAh|ryP NHHWbpc1KGh? M3XlXIlvcGmkaYTzJGhUTS2rbnT1Z4VlKEKPUEegZY5lKEeKUjDwdo91\WmwIHX4dJJme3Orb39CpC=> MXiyN|g4Pzd|NB?=
7TD1-DXM NHv2NJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i1R|ExKM7:TR?= NEn6R|Q4OiCq MU\EUXNQ NH3W[Y9qdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUKyN|g4OTF3OR?=
7TD1-WD-90 NH3J[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;MXpEyOCEQvF2= NXzKU3RUPzJiaB?= NWPtXXlTTE2VTx?= NHXMXnFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MVOyN|g4OTF3OR?=
7TD1-DXM NVTqOIF{SXCxcITvd4l{KEG|c3H5 NFLkUG02OCEQvF2= MX20PEBp NX;nWJh7TE2VTx?= M2fRNolv\HWlZYOgZZBweHSxc3nz NI\LTVczOzh5MUG1PS=>
7TD1-WD-90 Mm\ORZBweHSxc3nzJGF{e2G7 NGfGTHc2OCEQvF2= M4jUT|Q5KGh? MoX5SG1UVw>? MnWzbY5lfWOnczDhdI9xfG:|aYO= MVyyN|g4OTF3OR?=
7TD1-WD-90  NFvTSlVHfW6ldHnvckBCe3OjeR?= NUDpNpNqPTBizszN NUHvW4dzPiCq MUjEUXNQ M2XMZZNq\26rZnnjZY51dHliaX7obYJqfHNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBLSUt{IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEO= MmPxNlM5PzFzNUm=
HepG2  M{ftVGZ2dmO2aX;uJGF{e2G7 NYjifZRGOTByIN88US=> MofvNVIwOjRiaB?= MnrWbY5pcWKrdIOgV3RCXDNidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9v M{XkbVI{QDN4NECw
RAW264.7  Mnn3SpVv[3Srb36gRZN{[Xl? NFLjdHc2OMLizszNxsA> NFXQeoIzPC92ODDo NUmzb4N[e3WycILld5NmeyCUQV7LUE1qdmS3Y3XkJI9{fGWxY3zhd5Rw\2WwZYPpdy=> MkK4NlM3PjVyMUi=
RAW264.7 NX:3PIdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorzNE02OMLizszNxsA> MkHVOFjDqGh? MkPKbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> M1zuOlI{PjZ3MEG4
RAW264.7 Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWwMVUxyqEQvF5CpC=> M3LIRVQ5yqCq M3\ININifXOnczDhckBienKnc4Sgc4YhWkGZMk[0Mlch[2WubIOgZZQhfGinIFewM2cyKHCqYYPlJI9nKHSqZTDj[YxtKGO7Y3zl MmrlNlM3PjVyMUi=
RAW264.7 NWPJRXdrTnWwY4Tpc44hSXO|YYm= NH;zRpA2OMLizszN MoDFNlQwPDhiaB?= MnHnbY5pcWKrdIOgVmFPU0xvaX7keYNm\CCQRlHUZ|Eh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNmejd{N2PURXQ{ MUKyN|Y3PTBzOB?=
A549  NHXtVWJHfW6ldHnvckBCe3OjeR?= Mlm0NlAwPDBizszN MXqyNEBp M3nUc|IxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| NVXVU3REOjN4MkCxPVE>
A549  NGXsTlNHfW6ldHnvckBCe3OjeR?= MWCxNE8zOC92MDFOwG0> MknwNlQhcA>? NFvoeWd{fXCycnXzd4V{KHSqZTDyZYRq[XSrb36tbY5lfWOnZDDlcIV3[XSrb36gc4YhXkWJRtMg MVKyN|YzODF7MR?=
HUVECs MlnpR4VtdCCYaXHibYxqfHliQYPzZZk> NUP2VoF6OjBiwsXN NFTRcGE1KGh? NUHh[Zdj[XS2ZX71ZZRmeyCKMl:yMYlv\HWlZXSgZ4VtdCC|aILpcoti\2ViYX7kJIlueHKxdnXkJJRp\SCjdIThZ4hu\W62IILheIUhd2ZidHjlJINmdGy| NHGySGgzOzR6M{m0Oi=>
HUVECs MWLBdI9xfG:|aYOgRZN{[Xl? NFzJdWIzOCEEtV2= M4jPdVQhcA>? NF;C[Hh{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? MoDJNlM1QDN7NE[=
BV-2  NEPZb49HfW6ldHnvckBCe3OjeR?= M{\TdVIxKML3TR?= M{PWZVE3KGh? MmWwbY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> NYD4eGRQOjN{M{[zO|A>
NRK-52E  MnnWSpVv[3Srb36gRZN{[Xl? NVj0S|NqPcLizszN MlrLN|DDqG2rbh?= NWCwSo1G[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? M3nlOlI{OTd2N{W3
SW620  NFfqbIdHfW6ldHnvckBCe3OjeR?= M2TKUVIxKML3TR?= NFvWT3IyNzZiaB?= NFPPe3lqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> NF;KNYEzOzFzME[yOS=>
RPE  NEXldXJHfW6ldHnvckBCe3OjeR?= NUjRdWlIOzBiwsXNxsA> MnnFN{Bp NVLoSFdbcW6qaXLpeJMhfGinIHnu[JVkfGmxbjDv[kBxNVOWQWSzJIV5eHKnc4Ppc44> NVvMXlhPOjNyOUSwOlc>
SW1116 Mn7nSpVv[3Srb36gRZN{[Xl? NHHiPW0yODBiwsXNxsA> NFLDeWgzPC92OD:3NkBp NUTQPWt{\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= MUiyNlA2ODd7MB?=
HT29 NW\xRWxNTnWwY4Tpc44hSXO|YYm= M2WyWVExOCEEtV5CpC=> MnzCNlQwPDhxN{KgbC=> M33aWYRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBLSUt{IHHu[EBxUkGNMjD0bY1mNWSncHXu[IVvfGy7 MWCyNlA2ODd7MB?=
SW1116 NX[yRnR2TnWwY4Tpc44hSXO|YYm= M{TLcFExOCEEtV5CpC=> MUSyOE81QC95MjDo M{\xe4Rm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh NXu4NYlNOjJyNUC3PVA>
HT29 MVTGeY5kfGmxbjDBd5NigQ>? NUnnUWg6OTByINM1UeKh MmKwNlQwPDhxN{KgbC=> MXHk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> NFzvdHUzOjB3MEe5NC=>
ARPE-19 NYjVPY5jTnWwY4Tpc44hSXO|YYm= MUG1xsDPxE1? M3XRUlMxyqCvaX6= MknmbY5pcWKrdIOgTmFMOiCyaH;zdIhwemmuYYTpc44> NEnUZm4zOTZ{MEm2Ny=>
HSC-T6 Mn7mRZBweHSxc3nzJGF{e2G7 NIXMW3AyOMLizszN NIK3S44zyqCqwrC= NEmxRmNqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> NGq3[Y4zOTN7Nkm5PC=>
HSC-T6 NEflSXZHfW6ldHnvckBCe3OjeR?= NVnW[2I4OTEEoN88US=> MWCyxsBpyqB? NHXBVYRqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= MY[yNVM6Pjl7OB?=
Hep-2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqyOU0yODBizszN NVS1S|ZbOjRxNEivO|IhcA>? M2LXS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MmC4NlE{ODl2OEG=
Hep-2 M37RS2Fxd3C2b4Ppd{BCe3OjeR?= Mn;WOVAh|ryP MkHJNlQwPDhxN{KgbC=> M1X6fIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNidHnt[UBl\XCnbnTlcpRtgQ>? Mo\MNlE{ODl2OEG=
Hep-2 M17TVWZ2dmO2aX;uJGF{e2G7 MljTOVAh|ryP MUSyOE81QC95MjDo MVTpcohq[mm2czDHNUB1dyCVIHPlcIwh[3mlbHWgeJJidnOrdHnvckBidmRiaX7keYNmeyCJMTDj[YxtKGO7Y3zlJIFzemW|dB?= M4TTWFIyOzB7NEix
Hep-2 NGC4VXJHfW6ldHnvckBCe3OjeR?= NGTlR2o2OCEQvF2= MUKyOE81QC95MjDo M{LjToRwf26{ZXf1cIF1\XNidHjlJHNVSVR|LDDwMXNVSVR|IHHu[EB{fXK4aY\pckBxem:2ZXnuJIxmfmWucx?= MnHUNlE{ODl2OEG=
KF8 Ml\tSpVv[3Srb36gRZN{[Xl? NV\YUlZbOTEEoN88UeKh NW\qPFY3OcLiaB?= NHvC[ZBFVVORwrC= Mlz3bY5pcWKrdIOgTWwuOzNvaX7keYNm\CCQRj5OvmIh[WO2aY\heIlwdg>? MUOyNFk1ODB2NR?=
KF8 MoPqSpVv[3Srb36gRZN{[Xl? NEjYboUyOMLizszNxsA> NFrZUG4yyqCqwrC= NUe0SVVrTE2VT9Mg M2DNdYlvcGmkaYTzJGlNNTN|LXnu[JVk\WRiSd86Ru6yKGSnZ4Lh[IF1cW:wIHHu[EBPTi4QulKgZYN1cX[jdHnvci=> M1L5dVIxQTRyMES1
HEL  M2fXWGZ2dmO2aX;uJGF{e2G7 MUSxNFDDqM7:TR?= M13WblEzNTd{IHi= MVTpcohq[mm2czD0bIUhdGW4ZXygc4YheC2MQVuyMEBLSUt{ M4PVZ|IxPjJzME[x
HEL NEHrR3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojkNVAxyqEQvF2= NHPKR|YxNTViZB?= NUjhSnQzemWmdXPld{Boem:5dHigc4YhUkGNMm[2NVdHNWW6cILld5NqdmdiSFXMJINmdGy| Mnv2NlA3OjFyNkG=
A-172 MmfiSpVv[3Srb36gRZN{[Xl? M3;oSFUxNzFyMNMg{txO M4exfVQ5KGh? MY\y[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= NUPMZVBoOjB3OEm1NlU>
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MZ-54 NUOwNW5ZTnWwY4Tpc44hSXO|YYm= NHTSNWw2OC9zMEFCpO69VQ>? M1Tz[lQ5KGh? MV3y[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= MUeyNFU5QTV{NR?=
MZ-256 NHGxTYRHfW6ldHnvckBCe3OjeR?= NGH1dJY2OC9zMEFCpO69VQ>? NUHoW25tPDhiaB?= NF3PWWxz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> MnPONlA2QDl3MkW=
MZ-304 M1qxdmZ2dmO2aX;uJGF{e2G7 Ml3rOVAwOTBywrFOwG0> NI\pOFA1QCCq M2SyWZJm\HWlZYOgeIhmKGyndnXsd{Bw\iClb37zeIl1fXSrdnXsfUBi[3SrdnH0[YQhW1SDVEOgbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQh\mG|aHnvci=> MmixNlA2QDl3MkW=
A-172 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jBPFUxNzFyMNMg{txO NWOwOlB6PDhiaB?= NUjYNJZtdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MYCyNFU5QTV{NR?=
MZ-18 M2DXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWS1NE8yODEEoN88US=> M1WyS|Q5KGh? MlH2cIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq NInhdYkzODV6OUWyOS=>
MZ-54 NXfuS|NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYO1NE8yODEEoN88US=> NGfFO5c1QCCq NYrXe2dndGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo NXnxdHJ[OjB3OEm1NlU>
MZ-256 M2exOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\GOVAwOTBywrFOwG0> NYqzVYlFPDhiaB?= MWLs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MVmyNFU5QTV{NR?=
MZ-304 NEfMNJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fEV|UxNzFyMNMg{txO NEDuclU1QCCq NIXufldt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= NVrXPVVZOjB3OEm1NlU>
A-172 NIrWSGVHfW6ldHnvckBCe3OjeR?= NVj1bo06PTBxMUCwxsDPxE1? Mn;HOFghcA>? MnLlbY5pcWKrdIOgcYloemG2aX;u M{X6OVIxPTh7NUK1
MZ-18 NHGyclJHfW6ldHnvckBCe3OjeR?= NI\pbVg2OC9zMEFCpO69VQ>? MUe0PEBp M2LKR4lvcGmkaYTzJI1q\3KjdHnvci=> NG\VW4wzODV6OUWyOS=>
MZ-54 Mmf0SpVv[3Srb36gRZN{[Xl? MmHZOVAwOTBywrFOwG0> MYm0PEBp MlLzbY5pcWKrdIOgcYloemG2aX;u NVjVZplzOjB3OEm1NlU>
MZ-256 MlXQSpVv[3Srb36gRZN{[Xl? NGXtTWo2OC9zMEFCpO69VQ>? MX:0PEBp MoTpbY5pcWKrdIOgcYloemG2aX;u NV;hPXMyOjB3OEm1NlU>
MZ-304 NV7zR3JjTnWwY4Tpc44hSXO|YYm= MVO1NE8yODEEoN88US=> NV;JcZc3PDhiaB?= NEPYOIJqdmirYnn0d{BucWe{YYTpc44> MnXuNlA2QDl3MkW=
A-172 MYXGeY5kfGmxbjDBd5NigQ>? NFPXfVcyODEEoN88US=> NIrtcZE1QCCq NEm2d4JqdmirYnn0d{Bqdn[jc3nvci=> NWW1V5JrOjB3OEm1NlU>
MZ-18 MXfGeY5kfGmxbjDBd5NigQ>? MnP4NVAxyqEQvF2= M37rNVQ5KGh? MlzSbY5pcWKrdIOgbY53[XOrb36= NWTxNpRkOjB3OEm1NlU>
MZ-54 MojqSpVv[3Srb36gRZN{[Xl? NHvaR2wyODEEoN88US=> MknQOFghcA>? MWPpcohq[mm2czDpcpZie2mxbh?= MWGyNFU5QTV{NR?=
MZ-256 NX3DcIsyTnWwY4Tpc44hSXO|YYm= M3HpTFExOMLizszN MmnoOFghcA>? M{PQN4lvcGmkaYTzJIlvfmG|aX;u M4LNVFIxPTh7NUK1
MZ-304 MonrSpVv[3Srb36gRZN{[Xl? MXixNFDDqM7:TR?= M1jVT|Q5KGh? Ml\mbY5pcWKrdIOgbY53[XOrb36= M{TxVlIxPTh7NUK1
A-172 MkTSSpVv[3Srb36gRZN{[Xl? NVznbZN1PTBxMUCwxsDPxE1? NWW5bXA4PDhiaB?= MkfEdoVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> M3fT[VIxPTh7NUK1
MZ-18 M3LBOGZ2dmO2aX;uJGF{e2G7 M3nl[FUxNzFyMNMg{txO M4jCXVQ5KGh? NHHpR2dz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ Mnf3NlA2QDl3MkW=
MZ-54 M2C5fmZ2dmO2aX;uJGF{e2G7 Ml\BOVAwOTBywrFOwG0> M3;xZlQ5KGh? MVzy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NHTCVIIzODV6OUWyOS=>
MZ-256 NF7tVllHfW6ldHnvckBCe3OjeR?= NYTPO|QyPTBxMUCwxsDPxE1? NWHhSVBZPDhiaB?= Mmi1doVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> NEn0[5QzODV6OUWyOS=>
MZ-304 NVPEcIt{TnWwY4Tpc44hSXO|YYm= MVK1NE8yODEEoN88US=> MWO0PEBp M1O3bZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MmmwNlA2QDl3MkW=
SW1990 MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnuNlAh|ryP M4nvUlI1NzR6L{eyJIg> NGTnVFNqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M3rIbVIxPDh{OEW4
SW1990 MYLGeY5kfGmxbjDBd5NigQ>? NE\HbXUzOCEQvF2= M4\jWVI1KGh? NV\HTFhU\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE2PUD2yJIFv\CCYRVfGJI1TVkG| M2K1OlIxPDh{OEW4
SW1990 MoXMSpVv[3Srb36gRZN{[Xl? MUSyNEDPxE1? NGPpOGMzPCCq NYTHXWtE\GWlcnXhd4V{KHSqZTDpcpRmdnOrdImgc4YheC2VdHH0N{BmgHC{ZYPzbY9v NEXJSYkzODR6Mki1PC=>
SW1990 NFjvOGNKdn[jc3nvckBCe3OjeR?= NXftcJhvOjBizszN M3T2c|I1KGh? M2HibpJm\HWlZYOgbY53[XOrb36gc4YhW1dzOUmwJINmdGy|wrC= NEDYVHczODR6Mki1PC=>
THP1 Mo\vSpVv[3Srb36gRZN{[Xl? NHfy[5AyOCC3TR?= MkDXN|AhdWmwwrC= NGLteIFqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= M3niOVIxOzl|Nkmw
BMMC NGD2O21HfW6ldHnvckBCe3OjeR?= Mmj1NE0yOCEQvF2= Ml7GNVXDqG2rbh?= NEPldG1qdmirYnn0d{BNXEN2wrDy[Yxm[XOnIHnuJIEh\G:|ZT3k[ZBmdmSnboSg[oF{cGmxbjD3bZRpKG6nYYKgZ49ueGyndHWgbY5pcWKrdHnvckBifCClb37j[Y51emG2aX;ud{Djsb5zMNMg{txO MkGzNVk5OzV6NEW=
A549 MlW5SpVv[3Srb36gRZN{[Xl? NWLzXlR3OTVizszt M2jXUFEhcA>? MXPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSxJI9vKHS7cn;zbY5mKDdyMTD3ZZMh\GW2ZXP0[YQhOTVibXnuJIFnfGW{IGPQSUBDKHS{ZXH0cYVvfA>? NUTHd|FGOTl6MEG2OlU>
OVCAR-3 M{fQPWZ2dmO2aX;uJGF{e2G7 MmTQNVAhfU1? NGCwbmMyKGh? MonFbY5pcWKrdIOgUHBCNWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w NFrsfW4yQTZ2N{O2Ny=>
PA-1 M{DS[WZ2dmO2aX;uJGF{e2G7 M{DtdVExKHWP M4Sy[FEhcA>? NYTNWm9scW6qaXLpeJMhVFCDLXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;u NXXh[lZpOTl4NEezOlM>
OVCAR-3 MlThSpVv[3Srb36gRZN{[Xl? NHrJOmwyOCC3TR?= NU\2d25yOSCq MlntbY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? MmfoNVk3PDd|NkO=
PA-1 NWP4WZJ[TnWwY4Tpc44hSXO|YYm= MmqxNVAhfU1? NFfrUpgyKGh? NFHvV|dqdmirYnn0d{AhVFCDLXnu[JVk\WRib4\hdolidiClYX7j[ZIh[2WubDDtc5RqdGm2eR?= MVmxPVY1PzN4Mx?=
Jurkat  NHrMOHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[1NEDPxE1? Mly5NlQwPDhxN{KgbC=> NILVOFNmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NX3HfnN1OTl3NkS4PVE>
SUPT1  MnPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13Bd|UxKM7:TR?= NUXP[o5UOjRxNEivO|IhcA>? MX3lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NGPrR3AyQTV4NEi5NS=>
Jurkat  M1izUmFxd3C2b4Ppd{BCe3OjeR?= NVXVVGVLPTBizszN MmTqNlQwPDhiaB?= NFfrPHhmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ NVnYZXU1OTl3NkS4PVE>
SUPT1  MkS2RZBweHSxc3nzJGF{e2G7 M1jjOFUxKM7:TR?= MnHCNlQwPDhiaB?= NEPr[HNmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MVyxPVU3PDh7MR?=

... 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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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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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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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'.

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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