AG-490 (Tyrphostin B42)

For research use only. Not for use in humans.

Catalog No.S1143 Synonyms: Zinc02557947

43 publications

AG-490 (Tyrphostin B42) Chemical Structure

Molecular Weight(MW): 294.30

AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

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Selleck's AG-490 (Tyrphostin B42) has been cited by 43 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 NILyRohHfW6ldHnvckBCe3OjeR?= NEj5XYUyODEkgJpCuW0> NX7LfVdFOjRiaB?= MmnWcYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz NVLLe5BvOjZzOES5PVk>
BCBL1 NGPCUVBHfW6ldHnvckBCe3OjeR?= MmPpNVAx6oDLwsXN M4nCdFI1KGh? M3iz[o1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> M2fFVlI3OTh2OUm5
BC3 M4PZdmZ2dmO2aX;uJGF{e2G7 MV[xNFDjiIoEtV2= MX[yOEBp MYLt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YyKHKnZIXjeIlwdg>? Ml;ENlYyQDR7OUm=
BCBL1 MYrGeY5kfGmxbjDBd5NigQ>? NWjxRXF7OTBy4pEJxtVO M1niSlI1KGh? MXvt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? MmnsNlYyQDR7OUm=
BC3 MULGeY5kfGmxbjDBd5NigQ>? NH7RRoQyODEkgJpCuW0> Mn;zNlQhcA>? NHfaWJZqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> NVTTXmxUOjZzOES5PVk>
BCBL1 NGm2[YtHfW6ldHnvckBCe3OjeR?= MUOxNFDjiIoEtV2= NXXV[2hwOjRiaB?= MkPEbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NIrscG8zPjF6NEm5PS=>
SK-MEL-28 NYK0T3lsTnWwY4Tpc44hSXO|YYm= M2TmclUxNzFyMPMAjeK2VQ>? M4LYUVQ5KGh? NH6ye4pFVVOR M{TIdJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl MXSyOVIyPjV{Mh?=
MeWo NUnYOog6TnWwY4Tpc44hSXO|YYm= NHnRUIc2OC9zMEFihKnDvU1? NXjsepNkPDhiaB?= MUnEUXNQ NVfM[FBvemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MVyyOVIyPjV{Mh?=
SK-MEL-5 MlPMSpVv[3Srb36gRZN{[Xl? MWi1NE8yODEkgJpCuW0> MUK0PEBp MlfISG1UVw>? MmXGdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NIPLbXczPTJzNkWyNi=>
SK-MEL-2 M2XXVmZ2dmO2aX;uJGF{e2G7 M2\LUFUxNzFyMPMAjeK2VQ>? NFXT[JA1QCCq MlPHSG1UVw>? NHvzbVlz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NVLLfZdZOjV{MU[1NlI>
B16-F0 MljhSpVv[3Srb36gRZN{[Xl? M1W1ZVUxNzFyMPMAjeK2VQ>? MW[0PEBp NXTLNpU3TE2VTx?= NF;sfWhz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NF3NSVQzPTJzNkWyNi=>
TRPM2/HEK  MmjsSpVv[3Srb36gRZN{[Xl? MXmwMlHjiJN{NdMgxtVO NFq4UmsyPcLibXnu NIDnR4tFVVOR NGPMbmVz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IEGuO:KhyrWP M3zQb|I2OTd7NUe0
U937  NE\NeWZHfW6ldHnvckBCe3OjeR?= NVixVmVVOC5z4pETNlXDqML3TR?= MWOxOeKhdWmw NVzmRnc5TE2VTx?= NV65[pptemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= MlfVNlUyPzl3N{S=
TRPM2/HEK  MkHqSpVv[3Srb36gRZN{[Xl? M2DvPFExyqEEtV2= Ml\DOFDDqG2rbh?= MmDKSG1UVw>? MnHxdoVlfWOnczDUVnBOOiCjY4TpeoF1cW:wIHX2[Y4h[XRiaHnnbEBkd26lZX70doF1cW:wczDv[kBJOk9{ NWL5b3Q3OjVzN{m1O|Q>
GL37  NEDmeHJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVnsUmFVOC1zMNMgxtVO M3vRTlQ5KGh? NWi4VJIze3WycILld5NmeyCOYTDlfJBz\XO|aX;u NWHFPIhKOjR7OUm2OVc>
NRK-52E MWrGeY5kfGmxbjDBd5NigQ>? MYOxxsDDvU1? MW[xNEBucW5? MWficI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi NIKw[mIzPDdzMESyNy=>
NRK-52E MWTGeY5kfGmxbjDBd5NigQ>? MY[xxsDDvU1? MUGxNEBucW5? M3LwO4Jtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> NFvjdmozPDdzMESyNy=>
HSC  MWjGeY5kfGmxbjDBd5NigQ>? NGjMWogzOCEQvF2= MoTiNUBp MWHhZpJw\2G2ZYOgeIhmKGSrZn\ldoVvfGmjbDDl[oZm[3S|IH;mJIxmeHSrbjDvdkBCT0W| MoPmNlQ3OTRzOUm=
EJ NXjrWYl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjCXJJVPTBxOECg{txO M3zwcFI1NzR6L{eyJIg> NF;P[WVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MlfwNlQ2QDdyNEm=
EJ MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW0OVAwQDBizszN Mor4OFghcA>? M3r4OYNifXOnczDTMZBp[XOnIHHydoV{fA>? M3nEO|I1PTh5MES5
EJ MlPBSpVv[3Srb36gRZN{[Xl? NELyclk2OC96MDFOwG0> MojOOFghcA>? M1\lWoRwf26{ZXf1cIF1\XNiYz3NfYMtKGO7Y3zpcmQyNCC|dYL2bZZqdiCjbnSgWmVITiCneIDy[ZN{cW:wcx?= NVP4eJdsOjR3OEewOFk>
HepG2 MWrGeY5kfGmxbjDBd5NigQ>? NXyxNpNjPTBvNUCwJO69VQ>? MUK2NOKhdWmw M3S2[YlvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NYjN[VM6OjR{NEKwOFY>
SGC7901 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUWwMVExOCEQvF2= Ml:4NlQwPDhxN{KgbC=> NXzMPXdr[2G3c3XzJIEhe2mpbnnmbYNidnRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHTvd4Uu\GWyZX7k[Y51dHliYoX0JI5wfCC2aX3lMYRmeGWwZHXueIx6 MWSyOFE2OTJ3NR?=
AGS  MmHwR4VtdCCYaXHibYxqfHliQYPzZZk> MmjWNE0yODBizszN NVjte29KOjRxNEivO|IhcA>? M1LsVINifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> NV7QWXd7OjRzNUGyOVU>
SGC7901 NV7S[JJITnWwY4Tpc44hSXO|YYm= M3P2VFUxKM7:TR?= NEfGbmYzPC92OD:3NkBp MWn0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= M2jlelI1OTVzMkW1
AGS  MXvGeY5kfGmxbjDBd5NigQ>? MnnyOVAh|ryP MUeyOE81QC95MjDo NH;mVmV1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> M2HZUFI1OTVzMkW1
SGC7901 MkX0SpVv[3Srb36gRZN{[Xl? NIr5TXo2OCEQvF2= MYWyOE81QC95MjDo MV70bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> M3rIT|I1OTVzMkW1
AGS  MYDGeY5kfGmxbjDBd5NigQ>? MonSOVAh|ryP Mlj3NlQwPDhxN{KgbC=> MXz0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> MlLjNlQyPTF{NUW=
MC3T3-E1  NVrQR3dTTnWwY4Tpc44hSXO|YYm= MYC1NEDPxE1? NUX3Nox2PCCq NFzmUIFqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> MmHXNlM5Pzd5M{S=
7TD1-DXM MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGxNEDPxE1? MVu3NkBp Mof2SG1UVw>? MXfpcohq[mm2czDj[YxtKGe{b4f0bC=> MUKyN|g4OTF3OR?=
7TD1-WD-90 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GyTVExKM7:TR?= MYq3NkBp M4DCWWROW09? NYP2SFFscW6qaXLpeJMh[2WubDDndo94fGh? MViyN|g4OTF3OR?=
7TD1-DXM M2PjSWFxd3C2b4Ppd{BCe3OjeR?= M2Po[FUxKM7:TR?= NIf1[WE1QCCq MWHEUXNQ MmDibY5lfWOnczDhdI9xfG:|aYO= MnrINlM5PzFzNUm=
7TD1-WD-90 NYHtW4JTSXCxcITvd4l{KEG|c3H5 NIjzdpg2OCEQvF2= NFXa[ZY1QCCq MV;EUXNQ NXfMTIdMcW6mdXPld{BieG:ydH;zbZM> NHPH[lczOzh5MUG1PS=>
7TD1-WD-90  NFm0bHVHfW6ldHnvckBCe3OjeR?= NXTZVFJ3PTBizszN MWG2JIg> MXfEUXNQ MUHzbYdvcW[rY3HueIx6KGmwaHnibZR{KHSqZTDwbI9{eGixconsZZRqd25ib3[gTmFMOiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVR| MnvlNlM5PzFzNUm=
HepG2  NH3N[YZHfW6ldHnvckBCe3OjeR?= NVXLfm5QOTByIN88US=> MkjTNVIwOjRiaB?= NIPwOZJqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25? NV7QOVIyOjN6M{[0NFA>
RAW264.7  MkDZSpVv[3Srb36gRZN{[Xl? NI\qZYs2OMLizszNxsA> MYiyOE81QCCq NX\jPG45e3WycILld5NmeyCUQV7LUE1qdmS3Y3XkJI9{fGWxY3zhd5Rw\2WwZYPpdy=> MmLQNlM3PjVyMUi=
RAW264.7 NHHlWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHUNE02OMLizszNxsA> NHe3b4k1QMLiaB?= MlTJbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> NX:x[5F{OjN4NkWwNVg>
RAW264.7 MljIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjzUI4xNTVywrFOwG3DqA>? M1fSelQ5yqCq MVfjZZV{\XNiYX6gZZJz\XO2IH;mJHJCXzJ4ND63JINmdGy|IHH0JJRp\SCJMD;HNUBxcGG|ZTDv[kB1cGViY3XscEBkgWOuZR?= NEjhNmMzOzZ4NUCxPC=>
RAW264.7 NX3RPG95TnWwY4Tpc44hSXO|YYm= Mn3BOVDDqM7:TR?= MonSNlQwPDhiaB?= NUTtTXE{cW6qaXLpeJMhWkGQS1ytbY5lfWOnZDDOSmFV[zFiZYjwdoV{e2mxbjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOnckeyO3NVSVR| MmrQNlM3PjVyMUi=
A549  NWHLSYJETnWwY4Tpc44hSXO|YYm= M{PwWFIxNzRyIN88US=> MUOyNEBp M4PPO|IxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| MYiyN|YzODF7MR?=
A549  NHvo[WFHfW6ldHnvckBCe3OjeR?= NFPPcpQyOC9{MD:0NEDPxE1? Mn;hNlQhcA>? MWTzeZBxemW|c3XzJJRp\SC{YXTpZZRqd25vaX7keYNm\CCnbHX2ZZRqd25ib3[gWmVITsLi MYKyN|YzODF7MR?=
HUVECs M{TZV2NmdGxiVnnhZoltcXS7IFHzd4F6 MYeyNEDDvU1? NHjOUHQ1KGh? NULK[WRX[XS2ZX71ZZRmeyCKMl:yMYlv\HWlZXSgZ4VtdCC|aILpcoti\2ViYX7kJIlueHKxdnXkJJRp\SCjdIThZ4hu\W62IILheIUhd2ZidHjlJINmdGy| NIfQeIwzOzR6M{m0Oi=>
HUVECs MUTBdI9xfG:|aYOgRZN{[Xl? M{P1[FIxKML3TR?= M17xUVQhcA>? NUToVoVXe2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 NGfYb28zOzR6M{m0Oi=>
BV-2  NIn3U5RHfW6ldHnvckBCe3OjeR?= MX2yNEDDvU1? NVnpXXo4OTZiaB?= M17VTIlvcGmkaYTzJGxRWy2rbnT1Z4VlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKGGubX;zeEBkd22ybHX0[Yx6KGSrbXnubZNp\WRiaV7PV{BmgHC{ZYPzbY9v M1LNc|I{OjN4M{ew
NRK-52E  NU\zN3pYTnWwY4Tpc44hSXO|YYm= NWnm[lhtPcLizszN M2jHdFMxyqCvaX6= NYTSSWxG[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? M{juOFI{OTd2N{W3
SW620  M3P4TmZ2dmO2aX;uJGF{e2G7 NHSwWJUzOCEEtV2= NH\ZcXUyNzZiaB?= NYS1WW5VcW6qaXLpeJMheC2VVFHUN{Bi[3SrdnH0bY9v NYH0OVJCOjNzMUC2NlU>
RPE  NFzRUpVHfW6ldHnvckBCe3OjeR?= MUCzNEDDvU4EoB?= MXezJIg> M3f3[IlvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u MYSyN|A6PDB4Nx?=
SW1116 NGXkXGlHfW6ldHnvckBCe3OjeR?= NIPH[oEyODBiwsXNxsA> M3TRXFI1NzR6L{eyJIg> NH3rdFNl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= NGC4UIEzOjB3MEe5NC=>
HT29 MX\GeY5kfGmxbjDBd5NigQ>? NF7WTm4yODBiwsXNxsA> MWOyOE81QC95MjDo Mn;3[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? MX[yNlA2ODd7MB?=
SW1116 NWrGTJlITnWwY4Tpc44hSXO|YYm= NILs[IcyODBiwsXNxsA> Ml3INlQwPDhxN{KgbC=> MXjk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> M{jqeVIzODVyN{mw
HT29 MXPGeY5kfGmxbjDBd5NigQ>? NIPLSIwyODBiwsXNxsA> M1;OSFI1NzR6L{eyJIg> MYTk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> MVmyNlA2ODd7MB?=
ARPE-19 M4\UeGZ2dmO2aX;uJGF{e2G7 NGfRfZA2yqEQvF2= NH7vZlI{OMLibXnu NXjoPZdxcW6qaXLpeJMhUkGNMjDwbI9{eGixcnnsZZRqd25? MVeyNVYzODl4Mx?=
HSC-T6 NVPke3ZLSXCxcITvd4l{KEG|c3H5 NVPFeI5iOTEEoN88US=> NF7r[2kzyqCqwrC= MUDpcohq[mm2czD0bIUh[XCxcITvd4l{KG:oIFjTR{1VPiClZXzsd{BqdmS3Y3XkJIJ6KEOGRR?= NE[ye4kzOTN7Nkm5PC=>
HSC-T6 NUiwPYxnTnWwY4Tpc44hSXO|YYm= MV2xNOKh|ryP NVjB[Gd2OsLiaNMg MV;pcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? Mn;ZNlE{QTZ7OUi=
Hep-2 NYDuVZdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnBdmpoOjVvMUCwJO69VQ>? MofxNlQwPDhxN{KgbC=> NILuc3lqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NWX2RpZjOjF|MEm0PFE>
Hep-2 NWfFdJc3SXCxcITvd4l{KEG|c3H5 MmPjOVAh|ryP NYTWUHBxOjRxNEivO|IhcA>? MUHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHSrbXWg[IVx\W6mZX70cJk> NY\4VWlyOjF|MEm0PFE>
Hep-2 NVzwZ|hqTnWwY4Tpc44hSXO|YYm= Mlf4OVAh|ryP MXSyOE81QC95MjDo NYD3S5F4cW6qaXLpeJMhTzFidH:gV{Bk\WyuIHP5Z4xmKHS{YX7zbZRqd25iYX7kJIlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> NYHySmlOOjF|MEm0PFE>
Hep-2 M4noWWZ2dmO2aX;uJGF{e2G7 NHrpZnI2OCEQvF2= Mly3NlQwPDhxN{KgbC=> MmGx[I94dnKnZ4XsZZRmeyC2aHWgV3RCXDNuIICtV3RCXDNiYX7kJJN2en[rdnnuJJBzd3SnaX6gcIV3\Wy| MmPMNlE{ODl2OEG=
KF8 M3PV[GZ2dmO2aX;uJGF{e2G7 NYDac5d7OTEEoN88UeKh NV\B[VJ{OcLiaB?= M1XjbWROW00EoB?= NHn0eZNqdmirYnn0d{BKVC1|Mz3pcoR2[2WmIF7GMe67SiCjY4TpeoF1cW:w NYS5eVI6OjB7NECwOFU>
KF8 MVLGeY5kfGmxbjDBd5NigQ>? M{XLN|ExyqEQvF5CpC=> MnftNeKhcMLi M{K5V2ROW00EoB?= MlTabY5pcWKrdIOgTWwuOzNvaX7keYNm\CCLzsrC{tEh\GWpcnHkZZRqd25iYX7kJG5HNc78QjDhZ5RqfmG2aX;u M4D4eVIxQTRyMES1
HEL  MoGwSpVv[3Srb36gRZN{[Xl? M4ru[FExOMLizszN MWSxNk04OiCq MlfzbY5pcWKrdIOgeIhmKGyndnXsJI9nKHBvSlHLNkwhUkGNMh?= NYmwTnVyOjB4MkGwOlE>
HEL MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGxNFDDqM7:TR?= NV34SmNuOC13IHS= Mn7WdoVlfWOnczDndo94fGhib3[gTmFMOlZ4MUfGMYV5eHKnc4PpcochUEWOIHPlcIx{ MlLlNlA3OjFyNkG=
A-172 NGDSXIJHfW6ldHnvckBCe3OjeR?= M2rM[|UxNzFyMNMg{txO NFvDOGY1QCCq NXnsfJk3emWmdXPld{B1cGVibHX2[Yx{KG:oIHPvcpN1cXS3dHn2[Yx6KGGldHn2ZZRm\CCVVFHUN{BqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCoYYPobY9v NHPLSXEzODV6OUWyOS=>
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MZ-54 MYnGeY5kfGmxbjDBd5NigQ>? MkPvOVAwOTBywrFOwG0> MojhOFghcA>? MYHy[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= NXyyXHoxOjB3OEm1NlU>
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MZ-304 MnnWSpVv[3Srb36gRZN{[Xl? MXG1NE8yODEEoN88US=> MV[0PEBp NFPGPYpz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NFO3eowzODV6OUWyOS=>
A-172 NX3RWnJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u4ZlUxNzFyMNMg{txO Mkf4OFghcA>? MV\s[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? M3LveVIxPTh7NUK1
MZ-18 M4T5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33wZlUxNzFyMNMg{txO MoP3OFghcA>? M2HWTIxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NX7Eb5dyOjB3OEm1NlU>
MZ-54 NHrUWZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;pOVAwOTBywrFOwG0> NUXMe3R5PDhiaB?= NUiyS3F2dGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MVmyNFU5QTV{NR?=
MZ-256 M3PESmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXu1NE8yODEEoN88US=> MWq0PEBp MV\s[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MViyNFU5QTV{NR?=
MZ-304 M4H5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDWOVAwOTBywrFOwG0> NVnEUVI{PDhiaB?= MnnjcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq NG\tRnIzODV6OUWyOS=>
A-172 NFPnb3BHfW6ldHnvckBCe3OjeR?= MVS1NE8yODEEoN88US=> M3SxO|Q5KGh? M1H1[YlvcGmkaYTzJI1q\3KjdHnvci=> M3nCNlIxPTh7NUK1
MZ-18 M{jBb2Z2dmO2aX;uJGF{e2G7 MYi1NE8yODEEoN88US=> MYO0PEBp NYjkcIk2cW6qaXLpeJMhdWmpcnH0bY9v M13BXFIxPTh7NUK1
MZ-54 MkX1SpVv[3Srb36gRZN{[Xl? NVzWWHU3PTBxMUCwxsDPxE1? MnT1OFghcA>? NF;LOWVqdmirYnn0d{BucWe{YYTpc44> MYqyNFU5QTV{NR?=
MZ-256 M1PkOmZ2dmO2aX;uJGF{e2G7 M4jlVFUxNzFyMNMg{txO MWi0PEBp MWfpcohq[mm2czDtbYdz[XSrb36= MknyNlA2QDl3MkW=
MZ-304 NI\ZWnJHfW6ldHnvckBCe3OjeR?= M1HDZ|UxNzFyMNMg{txO NFTYPZA1QCCq MWjpcohq[mm2czDtbYdz[XSrb36= MoD3NlA2QDl3MkW=
A-172 MVzGeY5kfGmxbjDBd5NigQ>? M36yd|ExOMLizszN MXq0PEBp NEXNcmlqdmirYnn0d{Bqdn[jc3nvci=> NX;hZWppOjB3OEm1NlU>
MZ-18 MYnGeY5kfGmxbjDBd5NigQ>? M1;CZ|ExOMLizszN MnjpOFghcA>? MV\pcohq[mm2czDpcpZie2mxbh?= NV7nTFQ1OjB3OEm1NlU>
MZ-54 NVHjeoExTnWwY4Tpc44hSXO|YYm= Mlf3NVAxyqEQvF2= MUi0PEBp NHLjb45qdmirYnn0d{Bqdn[jc3nvci=> MoLjNlA2QDl3MkW=
MZ-256 NITNSGVHfW6ldHnvckBCe3OjeR?= M1TSfFExOMLizszN NV[1XIM2PDhiaB?= M1fG[IlvcGmkaYTzJIlvfmG|aX;u Mmf1NlA2QDl3MkW=
MZ-304 NEeyenNHfW6ldHnvckBCe3OjeR?= NHGwPGoyODEEoN88US=> M3PLc|Q5KGh? M3frd4lvcGmkaYTzJIlvfmG|aX;u NUP5RpNlOjB3OEm1NlU>
A-172 M37NbmZ2dmO2aX;uJGF{e2G7 Ml\rOVAwOTBywrFOwG0> Mni3OFghcA>? NWjmSmZ{emWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? Mo\PNlA2QDl3MkW=
MZ-18 M373eWZ2dmO2aX;uJGF{e2G7 M3fCSlUxNzFyMNMg{txO M4e5fFQ5KGh? M3jQTJJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MljVNlA2QDl3MkW=
MZ-54 MWDGeY5kfGmxbjDBd5NigQ>? MoX1OVAwOTBywrFOwG0> NHyyOlg1QCCq NUDENnFTemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? NY\CNYpsOjB3OEm1NlU>
MZ-256 MWHGeY5kfGmxbjDBd5NigQ>? NYPXTY9nPTBxMUCwxsDPxE1? M2HnflQ5KGh? NUnMRZNWemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? MUKyNFU5QTV{NR?=
MZ-304 NFfMRo5HfW6ldHnvckBCe3OjeR?= NIfSZWw2OC9zMEFCpO69VQ>? MXS0PEBp NHfWZ2lz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MoewNlA2QDl3MkW=
SW1990 NIDJPWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2yNEDPxE1? Ml35NlQwPDhxN{KgbC=> NHG3cnZqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MW[yNFQ5Ojh3OB?=
SW1990 NEnr[IFHfW6ldHnvckBCe3OjeR?= MkjVNlAh|ryP Mlj6NlQhcA>? Mnz5[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJG1OWC1{IHHu[EBXTUeIIH3SUmF{ MoLLNlA1QDJ6NUi=
SW1990 MW\GeY5kfGmxbjDBd5NigQ>? NWXkb|U6OjBizszN MXqyOEBp M1j4XYRm[3KnYYPld{B1cGViaX70[Y5{cXS7IH;mJJAuW3SjdEOg[ZhxemW|c3nvci=> NXvIPYNLOjB2OEK4OVg>
SW1990 MX7JcpZie2mxbjDBd5NigQ>? MUKyNEDPxE1? MlnsNlQhcA>? NVfzSJlWemWmdXPld{Bqdn[jc3nvckBw\iCVV{G5PVAh[2WubIRCpC=> NHHVVGkzODR6Mki1PC=>
THP1 MVnGeY5kfGmxbjDBd5NigQ>? NGXrPFgyOCC3TR?= MWezNEBucW8EoB?= MWHpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44h[nlib4\ldkA3OCV? NXz0c2pFOjB|OUO2PVA>
BMMC NGKzcWNHfW6ldHnvckBCe3OjeR?= MXWwMVExKM7:TR?= NXOzdG9ROTYEoH3pci=> NUPXRW5kcW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? Mn\WNVk5OzV6NEW=
A549 NYr6T|Y{TnWwY4Tpc44hSXO|YYm= MV6xOUDPxG1? MYOxJIg> NGDqcmRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQyKG:wIIT5do9{cW6nIEewNUB4[XNiZHX0[YN1\WRiMUWgcYlvKGGodHXyJHNRTSCEIITy[YF1dWWwdB?= M3G1NlE6QDBzNk[1
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PA-1 M2nW[WZ2dmO2aX;uJGF{e2G7 M1;Ue|ExKHWP MnTiNUBp NHXL[FdqdmirYnn0d{BNWEFvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= NV\k[5ZjOTl4NEezOlM>
OVCAR-3 NGHiTGNHfW6ldHnvckBCe3OjeR?= MljiNVAhfU1? M4W3dVEhcA>? MkTobY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? NGfYS5oyQTZ2N{O2Ny=>
PA-1 M4XlUmZ2dmO2aX;uJGF{e2G7 MYWxNEB2VQ>? NGTEN3AyKGh? NYDnfXRvcW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= NHi5UnIyQTZ2N{O2Ny=>
Jurkat  NGjMbWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUe1NEDPxE1? Ml7aNlQwPDhxN{KgbC=> MXvlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= M3j6eFE6PTZ2OEmx
SUPT1  MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELvcGo2OCEQvF2= M2[zRlI1NzR6L{eyJIg> NYm0XmhK\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v M2rIZ|E6PTZ2OEmx
Jurkat  Ml:yRZBweHSxc3nzJGF{e2G7 NWe3SVhtPTBizszN M3frUFI1NzR6IHi= NGTqTYxmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MmK4NVk2PjR6OUG=
SUPT1  MWDBdI9xfG:|aYOgRZN{[Xl? NYPHZVhQPTBizszN NVPnVZJ6OjRxNEigbC=> M1TSU4VvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBieG:ydH;zbZM> NF\nU5cyQTV4NEi5NS=>

... 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
  • 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
Smiles OC1=C(O)C=C(C=C1)\C=C(C#N)\C(=O)NCC2=CC=CC=C2

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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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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