AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

91 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 91 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 NHPhSXlHfW6ldHnvckBCe3OjeR?= MUOxNFDjiIoEtV2= Ml7ZNlQhcA>? MXnt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= MWqyOlE5PDl7OR?=
BCBL1 NXG5U3EzTnWwY4Tpc44hSXO|YYm= M3PEflExOOLCidM1US=> NXzZcIJHOjRiaB?= NU\RZW94dWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ MojqNlYyQDR7OUm=
BC3 NWnR[GNmTnWwY4Tpc44hSXO|YYm= M3;lb|ExOOLCidM1US=> NHfB[oQzPCCq MkTZcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? M3rQZ|I3OTh2OUm5
BCBL1 MXzGeY5kfGmxbjDBd5NigQ>? MV2xNFDjiIoEtV2= NX7HbmRlOjRiaB?= MWnt[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? M4HlU|I3OTh2OUm5
BC3 MUDGeY5kfGmxbjDBd5NigQ>? NYHDOVZqOTBy4pEJxtVO MUGyOEBp M3zESolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKG[udYlCpC=> M{LabVI3OTh2OUm5
BCBL1 M1Pi[2Z2dmO2aX;uJGF{e2G7 NX35TWZ1OTBy4pEJxtVO NXTnWGEzOjRiaB?= NEHRSm9qdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> MnzXNlYyQDR7OUm=
SK-MEL-28 NH3DZlVHfW6ldHnvckBCe3OjeR?= M{nhXlUxNzFyMPMAjeK2VQ>? M33xclQ5KGh? MUHEUXNQ NEnucI5z\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MXKyOVIyPjV{Mh?=
MeWo MVPGeY5kfGmxbjDBd5NigQ>? MVq1NE8yODEkgJpCuW0> M{D3V|Q5KGh? NYrLbYFiTE2VTx?= M2DzZZJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl MoDoNlUzOTZ3MkK=
SK-MEL-5 NUj5clRlTnWwY4Tpc44hSXO|YYm= NX3Zb5pNPTBxMUCw5qCKyrWP NWPUNo42PDhiaB?= M{C3OWROW09? NUfu[G9PemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> M371UFI2OjF4NUKy
SK-MEL-2 M1TqWmZ2dmO2aX;uJGF{e2G7 NV\YW3ZSPTBxMUCw5qCKyrWP MmPEOFghcA>? NELzUlZFVVOR M2rZe5Jm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NHSyW3YzPTJzNkWyNi=>
B16-F0 MXzGeY5kfGmxbjDBd5NigQ>? MlvpOVAwOTBy4pEJxtVO NEnFemU1QCCq NHTHbY9FVVOR NGfLeoRz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NHTmfJIzPTJzNkWyNi=>
TRPM2/HEK  NFzXWVZHfW6ldHnvckBCe3OjeR?= NFX3dYkxNjIkgKOyOeKhyrWP MWSxOeKhdWmw MV;EUXNQ MXfy[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDFwN9MgxtVO NV7tZnFzOjVzN{m1O|Q>
U937  NFv4NZNHfW6ldHnvckBCe3OjeR?= NInZT5cxNjIkgKOyOeKhyrWP M3LSXlE2yqCvaX6= NUnOUWZsTE2VTx?= NYq2OHBKemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= MlHJNlUyPzl3N{S=
TRPM2/HEK  M{nKNmZ2dmO2aX;uJGF{e2G7 NH6zXncyOMLiwsXN NWHKeFN2PDEEoH3pci=> Mn2xSG1UVw>? MoH0doVlfWOnczDUVnBOOiCjY4TpeoF1cW:wIHX2[Y4h[XRiaHnnbEBkd26lZX70doF1cW:wczDv[kBJOk9{ MXSyOVE4QTV5NB?=
GL37  MlT1R4VtdCCYaXHibYxqfHliQYPzZZk> MmXLNE0yOMLiwsXN NWrJRWw1PDhiaB?= NEm1bJJ{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= M3rpdFI1QTl7NkW3
NRK-52E MmnLSpVv[3Srb36gRZN{[Xl? MVyxxsDDvU1? NYjLdW1VOTBibXnu NFi5[HpjdG:la4OgeIhmKHO2aX31cIF1d3K7IHXm[oVkfCCxZjDBcochUUlib36gVIF5NTJiZYjwdoV{e2mxbtMg NFHOflIzPDdzMESyNy=>
NRK-52E M{HMT2Z2dmO2aX;uJGF{e2G7 MoK4NeKhyrWP MVqxNEBucW5? M2ewWYJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> Mnu4NlQ4OTB2MkO=
HSC  M4[ycmZ2dmO2aX;uJGF{e2G7 MlPqNlAh|ryP MlXoNUBp MnK1ZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= NVi1TmxrOjR4MUSxPVk>
EJ MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjYOVAwQDBizszN NUfVXINpOjRxNEivO|IhcA>? M{H6PYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NUfMN5diOjR3OEewOFk>
EJ Ml7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{POZVUxNzhyIN88US=> NWLnSpdZPDhiaB?= MkDPZ4F2e2W|IGOtdIhie2ViYYLy[ZN1 M2H0WVI1PTh5MES5
EJ NI\FWlRHfW6ldHnvckBCe3OjeR?= NGH5Wmk2OC96MDFOwG0> MXy0PEBp M{LZU4Rwf26{ZXf1cIF1\XNiYz3NfYMtKGO7Y3zpcmQyNCC|dYL2bZZqdiCjbnSgWmVITiCneIDy[ZN{cW:wcx?= MWiyOFU5PzB2OR?=
HepG2 MWDGeY5kfGmxbjDBd5NigQ>? NV3HO|d7PTBvNUCwJO69VQ>? M37SSFYxyqCvaX6= MVHpcohq[mm2czD0bIUhUUxvNj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSBqVInyO|A2MSCjbnSgV3RCXDNiKGT5dlcxPSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXfYN3R2OjR{NEKwOFY>
SGC7901 NWrF[2xkS2WubDDWbYFjcWyrdImgRZN{[Xl? NXPPR5dQOC1zMECg{txO NVzQNotFOjRxNEivO|IhcA>? Ml63Z4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NX7ORVQzOjRzNUGyOVU>
AGS  MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoXFNE0yODBizszN Mn7YNlQwPDhxN{KgbC=> MVXjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= M1[3clI1OTVzMkW1
SGC7901 NYjwSFk4TnWwY4Tpc44hSXO|YYm= M2P0S|UxKM7:TR?= MYmyOE81QC95MjDo M1rCXJRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg MWSyOFE2OTJ3NR?=
AGS  Mo\1SpVv[3Srb36gRZN{[Xl? MUC1NEDPxE1? M1rZUlI1NzR6L{eyJIg> NETTVo51cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> M{TZRVI1OTVzMkW1
SGC7901 MnPTSpVv[3Srb36gRZN{[Xl? NGnYRWM2OCEQvF2= MXeyOE81QC95MjDo MlKweIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> NXXWNpp2OjRzNUGyOVU>
AGS  NX7zSpNQTnWwY4Tpc44hSXO|YYm= NGPTSos2OCEQvF2= NWfHd3ZXOjRxNEivO|IhcA>? NUnVdFNYfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? MX:yOFE2OTJ3NR?=
MC3T3-E1  Mn;HSpVv[3Srb36gRZN{[Xl? MX21NEDPxE1? NYjlcJFJPCCq MW\pcohq[mm2czDIV2UucW6mdXPl[EBDVVB5IHHu[EBIUFJicILveIVqdiCneIDy[ZN{cW:wwrC= NF7aenozOzh5N{ezOC=>
7TD1-DXM NInhWmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnXZ|YyOCEQvF2= MnLJO|IhcA>? MmrOSG1UVw>? MYLpcohq[mm2czDj[YxtKGe{b4f0bC=> MYqyN|g4OTF3OR?=
7TD1-WD-90 NYfkeYxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUm1bm1oOTBizszN NYPQdJFoPzJiaB?= Mlu3SG1UVw>? NFXWTodqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmfRNlM5PzFzNUm=
7TD1-DXM MlnlRZBweHSxc3nzJGF{e2G7 NIDkRmw2OCEQvF2= MnHqOFghcA>? MkXRSG1UVw>? MYPpcoR2[2W|IHHwc5B1d3Orcx?= MXiyN|g4OTF3OR?=
7TD1-WD-90 NGLmV2dCeG:ydH;zbZMhSXO|YYm= NEPKfmM2OCEQvF2= NXnKXXhsPDhiaB?= MYPEUXNQ M4DRV4lv\HWlZYOgZZBweHSxc3nz NITLUYczOzh5MUG1PS=>
7TD1-WD-90  M4rzemZ2dmO2aX;uJGF{e2G7 NVK2XFk2PTBizszN M4rKcFYhcA>? MVLEUXNQ NUP5NHV7e2mpbnnmbYNidnSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEqDS{KgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNy=> NITF[pEzOzh5MUG1PS=>
HepG2  MnfRSpVv[3Srb36gRZN{[Xl? MVmxNFAh|ryP NFjsVVcyOi9{NDDo NYC1cIVjcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:w M3PxfVI{QDN4NECw
RAW264.7  NIPPPVBHfW6ldHnvckBCe3OjeR?= M3Xm[FUxyqEQvF5CpC=> MlnNNlQwPDhiaB?= MnLpd5VxeHKnc4Pld{BTSU6NTD3pcoR2[2WmIH;zeIVw[2yjc4Tv[4Vv\XOrcx?= MWWyN|Y3PTBzOB?=
RAW264.7 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHFXGcxNTVywrFOwG3DqA>? NV76V|N{PDkEoHi= M4DEOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wt[IVx\W6mZX70cJk> NIXMNYczOzZ4NUCxPC=>
RAW264.7 NWXLOFlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TFfFAuPTEEoN88UeKh M4HJdFQ5yqCq M4TET4NifXOnczDhckBienKnc4Sgc4YhWkGZMk[0Mlch[2WubIOgZZQhfGinIFewM2cyKHCqYYPlJI9nKHSqZTDj[YxtKGO7Y3zl NYfBRZBjOjN4NkWwNVg>
RAW264.7 NELGZoZHfW6ldHnvckBCe3OjeR?= NV\teGpQPTEEoN88US=> NUfncZFvOjRxNEigbC=> MWPpcohq[mm2czDSRW5MVC2rbnT1Z4VlKE6IQWTjNUBmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gV4VzPzJ5U2TBWFM> NUnEZZFbOjN4NkWwNVg>
A549  NI\IOJZHfW6ldHnvckBCe3OjeR?= MVuyNE81OCEQvF2= MkTlNlAhcA>? MYOyNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? MYKyN|YzODF7MR?=
A549  M3fic2Z2dmO2aX;uJGF{e2G7 M2LnUlExNzJyL{SwJO69VQ>? NUTy[ZlqOjRiaB?= NX7jT2k6e3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> NWrBfYtIOjN4MkCxPVE>
HUVECs NF7UOpVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnnWNlAhyrWP NIT6SXo1KGh? MV7heJRmdnWjdHXzJGgzVzJvaX7keYNm\CClZXzsJJNpemmwa3Hn[UBidmRiaX3wdo93\WRidHjlJIF1fGGlaH3lcpQhemG2ZTDv[kB1cGViY3XscJM> MWGyN|Q5Ozl2Nh?=
HUVECs MlP4RZBweHSxc3nzJGF{e2G7 Ml30NlAhyrWP NXHRdVdWPCCq NX:1R3BFe2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 MYqyN|Q5Ozl2Nh?=
BV-2  MnLwSpVv[3Srb36gRZN{[Xl? MoLQNlAhyrWP NUCzbGlKOTZiaB?= NUf0c4h[cW6qaXLpeJMhVFCVLXnu[JVk\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiYXztc5N1KGOxbYDs[ZRmdHliZHntbY5qe2inZDDpUm9UKGW6cILld5Nqd25? NF\PSpYzOzJ|NkO3NC=>
NRK-52E  NXnyOXNZTnWwY4Tpc44hSXO|YYm= MXy1xsDPxE1? NV3uWY5JOzEEoH3pci=> NXzHc5l[[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? MVKyN|E4PDd3Nx?=
SW620  MnntSpVv[3Srb36gRZN{[Xl? NVvtNWk{OjBiwsXN MnjBNU83KGh? NE\LOGRqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> M4i2UlI{OTFyNkK1
RPE  NIL2fG9HfW6ldHnvckBCe3OjeR?= NF;Kb40{OCEEtV5CpC=> M1Hue|MhcA>? MYXpcohq[mm2czD0bIUhcW6mdXP0bY9vKG:oIICtV3RCXDNiZYjwdoV{e2mxbh?= MX2yN|A6PDB4Nx?=
SW1116 NIPuSlZHfW6ldHnvckBCe3OjeR?= NGP0RoYyODBiwsXNxsA> NHOzWpUzPC92OD:3NkBp MmjX[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? NHP2T|UzOjB3MEe5NC=>
HT29 NXr3eYVlTnWwY4Tpc44hSXO|YYm= NIm3do8yODBiwsXNxsA> MlvnNlQwPDhxN{KgbC=> M1H0O4Rm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBLSUt{IHHu[EBxUkGNMjD0bY1mNWSncHXu[IVvfGy7 MXeyNlA2ODd7MB?=
SW1116 MVTGeY5kfGmxbjDBd5NigQ>? Mlv0NVAxKML3TdMg NWLG[o1xOjRxNEivO|IhcA>? MV;k[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> MX6yNlA2ODd7MB?=
HT29 MVPGeY5kfGmxbjDBd5NigQ>? Mn7mNVAxKML3TdMg NG\HdJYzPC92OD:3NkBp MVfk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> M2P3PVIzODVyN{mw
ARPE-19 Mn3TSpVv[3Srb36gRZN{[Xl? MU[1xsDPxE1? MkLtN|DDqG2rbh?= NIrHUYtqdmirYnn0d{BLSUt{IIDoc5NxcG:{aXzheIlwdg>? MU[yNVYzODl4Mx?=
HSC-T6 NIXkXndCeG:ydH;zbZMhSXO|YYm= MWOxNOKh|ryP MX[yxsBpyqB? NUPESIVzcW6qaXLpeJMhfGinIHHwc5B1d3OrczDv[kBJW0NvVE[gZ4VtdHNiaX7keYNm\CCkeTDDSGU> NWDMPYlsOjF|OU[5PVg>
HSC-T6 MXzGeY5kfGmxbjDBd5NigQ>? MXmxNOKh|ryP NYHOZpVbOsLiaNMg NYfrN3U5cW6qaXLpeJMhfGinIHX4dJJme3Orb37zJI9nKHC\LWPURXQyKGGwZDDCZYQhcW6mdXPl[EBjgSCFRFW= MY[yNVM6Pjl7OB?=
Hep-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHu[mkzPS1zMECg{txO NILBdWwzPC92OD:3NkBp MkTNbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXWyNVMxQTR6MR?=
Hep-2 MXnBdI9xfG:|aYOgRZN{[Xl? M4jGeFUxKM7:TR?= NY\qV4lsOjRxNEivO|IhcA>? NVzIc4lXcW6mdXPld{Bk\WyuIHHwc5B1d3OrczD0bY1mKGSncHXu[IVvfGy7 NWHkfog5OjF|MEm0PFE>
Hep-2 NECxcpdHfW6ldHnvckBCe3OjeR?= MonuOVAh|ryP NHrzTZYzPC92OD:3NkBp MXfpcohq[mm2czDHNUB1dyCVIHPlcIwh[3mlbHWgeJJidnOrdHnvckBidmRiaX7keYNmeyCJMTDj[YxtKGO7Y3zlJIFzemW|dB?= MYqyNVMxQTR6MR?=
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KF8 MmLvSpVv[3Srb36gRZN{[Xl? MYOxNOKh|ryPwrC= MojjNeKhcMLi NWHjeml2TE2VT9Mg M12yS4lvcGmkaYTzJGlNNTN|LXnu[JVk\WRiSd86Ru6yKGSnZ4Lh[IF1cW:wIHHu[EBPTi4QulKgZYN1cX[jdHnvci=> MWGyNFk1ODB2NR?=
HEL  MXHGeY5kfGmxbjDBd5NigQ>? NFvsWnEyODEEoN88US=> MkHCNVIuPzJiaB?= MlvWbY5pcWKrdIOgeIhmKGyndnXsJI9nKHBvSlHLNkwhUkGNMh?= MorsNlA3OjFyNkG=
HEL MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjlNVAxyqEQvF2= Mlz2NE02KGR? M{nBOpJm\HWlZYOg[5Jwf3SqIH;mJGpCUzKYNkG3Sk1mgHC{ZYPzbY5oKEiHTDDj[Yxtew>? NInLXoszODZ{MUC2NS=>
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MZ-304 NEO5bo5HfW6ldHnvckBCe3OjeR?= NUD0b21XPTBxMUCwxsDPxE1? MknTOFghcA>? MoCydoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u NWHrdXBYOjB3OEm1NlU>
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MZ-18 NXPP[|dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLLOnBOPTBxMUCwxsDPxE1? M3q1WlQ5KGh? NXizW4UxdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo NFq0eVIzODV6OUWyOS=>
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MZ-256 M2\wfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LPNFUxNzFyMNMg{txO MWS0PEBp M4fxRoxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= M3XDfVIxPTh7NUK1
MZ-304 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzTOVAwOTBywrFOwG0> NH\GUVE1QCCq MWXs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MnLmNlA2QDl3MkW=
A-172 M{nTbGZ2dmO2aX;uJGF{e2G7 NGX0[G82OC9zMEFCpO69VQ>? M4[zblQ5KGh? NV;IcW9KcW6qaXLpeJMhdWmpcnH0bY9v MXGyNFU5QTV{NR?=
MZ-18 NIG4ZolHfW6ldHnvckBCe3OjeR?= MUS1NE8yODEEoN88US=> MnrIOFghcA>? M1uxU4lvcGmkaYTzJI1q\3KjdHnvci=> MX6yNFU5QTV{NR?=
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MZ-256 MYPGeY5kfGmxbjDBd5NigQ>? MXW1NE8yODEEoN88US=> M13xdlQ5KGh? MlrnbY5pcWKrdIOgcYloemG2aX;u NXnD[5hROjB3OEm1NlU>
MZ-304 MWXGeY5kfGmxbjDBd5NigQ>? NF7wXnI2OC9zMEFCpO69VQ>? NYW3XotvPDhiaB?= NYnZfnV2cW6qaXLpeJMhdWmpcnH0bY9v MUCyNFU5QTV{NR?=
A-172 NH35NXZHfW6ldHnvckBCe3OjeR?= NEe2XIQyODEEoN88US=> NHO5XGw1QCCq NVPwdXZ{cW6qaXLpeJMhcW64YYPpc44> NXHld49uOjB3OEm1NlU>
MZ-18 MmC1SpVv[3Srb36gRZN{[Xl? MYCxNFDDqM7:TR?= NIDVPXk1QCCq MkTGbY5pcWKrdIOgbY53[XOrb36= MXmyNFU5QTV{NR?=
MZ-54 M{XOWGZ2dmO2aX;uJGF{e2G7 MUWxNFDDqM7:TR?= M3yz[VQ5KGh? NGfnWVVqdmirYnn0d{Bqdn[jc3nvci=> MYWyNFU5QTV{NR?=
MZ-256 MV\GeY5kfGmxbjDBd5NigQ>? MVOxNFDDqM7:TR?= MY[0PEBp MlL0bY5pcWKrdIOgbY53[XOrb36= M2TveVIxPTh7NUK1
MZ-304 NX;4bVJlTnWwY4Tpc44hSXO|YYm= NInlVZQyODEEoN88US=> Ml\xOFghcA>? M{\pdolvcGmkaYTzJIlvfmG|aX;u NVXwfGFDOjB3OEm1NlU>
A-172 NG\SO5RHfW6ldHnvckBCe3OjeR?= MWG1NE8yODEEoN88US=> M32yXVQ5KGh? M1X1NZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> M2\O[FIxPTh7NUK1
MZ-18 M4m0O2Z2dmO2aX;uJGF{e2G7 MUO1NE8yODEEoN88US=> M3\nTlQ5KGh? MV3y[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz M4LRc|IxPTh7NUK1
MZ-54 MXTGeY5kfGmxbjDBd5NigQ>? M13FUlUxNzFyMNMg{txO NEjKTXA1QCCq MVny[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz M{L6VVIxPTh7NUK1
MZ-256 Mn;5SpVv[3Srb36gRZN{[Xl? NVr1TopTPTBxMUCwxsDPxE1? NV;IPYY4PDhiaB?= NGn3flJz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MVWyNFU5QTV{NR?=
MZ-304 NVLqOZVXTnWwY4Tpc44hSXO|YYm= M1vhUFUxNzFyMNMg{txO MYC0PEBp NXnFT2tUemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? MnTyNlA2QDl3MkW=
SW1990 NFP0[3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrLVIYzOCEQvF2= NFX1eYEzPC92OD:3NkBp Ml;FbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NHex[YozODR6Mki1PC=>
SW1990 M3[4UmZ2dmO2aX;uJGF{e2G7 MkPKNlAh|ryP M3TYUFI1KGh? Ml\Z[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJG1OWC1{IHHu[EBXTUeIIH3SUmF{ MlHQNlA1QDJ6NUi=
SW1990 M33udmZ2dmO2aX;uJGF{e2G7 MUGyNEDPxE1? M3LLTlI1KGh? MoDR[IVkemWjc3XzJJRp\SCrboTlcpNqfHlib3[gdE1UfGG2MzDlfJBz\XO|aX;u M{nvcFIxPDh{OEW4
SW1990 NUTEOJF{UW64YYPpc44hSXO|YYm= MkTMNlAh|ryP NFvvWIszPCCq MYHy[YR2[2W|IHnueoF{cW:wIH;mJHNYOTl7MDDj[Yxte8Li NWjQSWhJOjB2OEK4OVg>
THP1 NGnGNWhHfW6ldHnvckBCe3OjeR?= NFrXWJUyOCC3TR?= MlnFN|AhdWmwwrC= NWjKdm91cW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wIHL5JI93\XJiNkCl NYPNOmNZOjB|OUO2PVA>
BMMC NF;qOpdHfW6ldHnvckBCe3OjeR?= MYGwMVExKM7:TR?= MmLPNVXDqG2rbh?= NXH4bXZKcW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? NVjMO|BmOTl6M{W4OFU>
A549 NVztRoR[TnWwY4Tpc44hSXO|YYm= NI[5Zo8yPSEQvH2= NUe1SYRPOSCq MUHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSxJI9vKHS7cn;zbY5mKDdyMTD3ZZMh\GW2ZXP0[YQhOTVibXnuJIFnfGW{IGPQSUBDKHS{ZXH0cYVvfA>? M2i0OlE6QDBzNk[1
OVCAR-3 NFr4PJNHfW6ldHnvckBCe3OjeR?= M4rSVFExKHWP M1nxRVEhcA>? M4\XcYlvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= NF[wenIyQTZ2N{O2Ny=>
PA-1 MVvGeY5kfGmxbjDBd5NigQ>? NHnNcYQyOCC3TR?= NV\2NYY3OSCq MYDpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? M{XzUlE6PjR5M{[z
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PA-1 NGTVVm5HfW6ldHnvckBCe3OjeR?= M2WyU|ExKHWP MVuxJIg> NVO3WJF6cW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= NWHaPXRvOTl4NEezOlM>
Jurkat  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmewOVAh|ryP NGftO5ozPC92OD:3NkBp NEPadZRmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> MUOxPVU3PDh7MR?=
SUPT1  MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS1NEDPxE1? M2HRfVI1NzR6L{eyJIg> NGfkbHNmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NXe3TIhYOTl3NkS4PVE>
Jurkat  M2\wT2Fxd3C2b4Ppd{BCe3OjeR?= MWG1NEDPxE1? NFO0O|EzPC92ODDo M3vhcoVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBieG:ydH;zbZM> MYexPVU3PDh7MR?=
SUPT1  M4i0SmFxd3C2b4Ppd{BCe3OjeR?= MWS1NEDPxE1? NVLV[ItROjRxNEigbC=> Mluy[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> MUexPVU3PDh7MR?=

... 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+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 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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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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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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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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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