AG-490 (Tyrphostin B42)

Catalog No.S1143 Synonyms: Zinc02557947

AG-490 (Tyrphostin B42) Chemical Structure

Molecular Weight(MW): 294.30

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

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In DMSO USD 70 In stock
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6 Customer Reviews

  • Increased expression of VEGF and p-STAT3 induced by CXCL1 was blocked by either AG490 or SB225022 in AGS cells.

    Cancer Letters, 2015, 359(2): 335-43 . AG-490 (Tyrphostin B42) purchased from Selleck.

    Pre-treatment with AG490 and PD98059 alone or in combination leads to significant decrease in spheroid formation and number compared with PRL treatment alone.

    Carcinogenesis, 2014, 35(4): 795-806 . AG-490 (Tyrphostin B42) purchased from Selleck.

  • IL6 normally induces WASF3 expression in MDA231 cells, but co-treatments with AG490 (a pan-JAK inhibitor) show a dose-dependent reduction of both WASF3 levels and activated STAT3 levels.

    Carcinogenesis 2013 34, 1994-9. AG-490 (Tyrphostin B42) purchased from Selleck.

    Inhibition of JAK1/2 with AG490 or STAT3 with S3I-201 leads to reduced STAT3 activation and reduced WASF3 levels. In contrast, treatment with Dasatinib (SRC inhibitor) or Gefitinib (EGFR inhibitor) does not significantly affect activated STAT3 or WASF3 levels

    Carcinogenesis 2013 34, 1994-9. AG-490 (Tyrphostin B42) purchased from Selleck.

  • Prostate 2013 73(3), 267-77. AG-490 (Tyrphostin B42) purchased from Selleck.

    Biochem Biophys Res Commun 2013 435(4), 533-9. AG-490 (Tyrphostin B42) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
Targets
EGFR [1]
(Cell-free assay)
0.1 μM
In vitro

AG-490 inhibits HER-2 driven cell proliferation with IC50 of 3.5 μM. [1] Corresponding to the specific dose-dependent inhibition of constitutively activated JAK2 in pre-B acute leukemia (ALL) cells, AG-490 (5 μM) almost completely blocks the growth of all ALL cells by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 does not inhibit the activities of Lck, Lyn, Btk, Syk, and Src. [2] AG-490 (60-100 μM) blocks the constitutive activation of Stat3sm, and inhibits spontaneous as well as interleukin 2-induced growth of mycosis fungoides (MF) tumor cells with IC50 values of 75 μM and 20 μM, respectively. [3] AG-490 potently inhibits IL-2-mediated human T cell growth with an IC50 of 25 μM by blocking the activities of JAK3 and STAT5a/b. [4] Although AG-490 alone has no effect on proliferation of FDrv210H cells at a concentration of 5 μM, AG-490 can synergize with STI571 to enhance its inhibitory effect on p210bcr-abl driven proliferation. [5] AG-490 significantly inhibits the constitutive activation of Stat3 in MOPC, MPC11, and S194 cells, leading to dramatic dose-dependent apoptosis. [6] AG-490 (100 μM) inhibits Akt phosphorylation, inhibits the activation of nuclear factor-κB, and causes the activation of GSK-3β, leading to the reduction of c-Myc. AG-490 (50 μM) can induce apoptosis of imatinib-resistant BaF3 cells expressing T315I and E255K mutants of Bcr-Abl. [7] AG-490 at 30 μM inhibits not only Epo-induced phosphorylation of wild-type JAK2 but also constitutive phosphorylation of the JAK2 V617F mutant. AG-490 also potently inhibits cytokine-independent cell growth induced by the JAK2 V617F mutant in BaF3 cells. [8]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BC3 NIC2RotHfW6ldHnvckBCe3OjeR?= MVyxNFDjiIoEtV2= M{jzWVI1KGh? Ml;LcYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz M1jTUlI3OTh2OUm5
BCBL1 NFHCWGZHfW6ldHnvckBCe3OjeR?= NXj0SXBROTBy4pEJxtVO MYSyOEBp MlnxcYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz NUDGdYdYOjZzOES5PVk>
BC3 NVnOdGZzTnWwY4Tpc44hSXO|YYm= MnHhNVAx6oDLwsXN MUKyOEBp NHvufotu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0ZzIILl[JVkfGmxbh?= NYC3ZXhkOjZzOES5PVk>
BCBL1 M4XpOGZ2dmO2aX;uJGF{e2G7 MXixNFDjiIoEtV2= NXrXcGZFOjRiaB?= NEnob49u\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= Mny5NlYyQDR7OUm=
BC3 NF7O[IpHfW6ldHnvckBCe3OjeR?= NY\mbZF1OTBy4pEJxtVO NF\wbpkzPCCq MlXtbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg M4DCZlI3OTh2OUm5
BCBL1 NViyWmtxTnWwY4Tpc44hSXO|YYm= Mn3jNVAx6oDLwsXN NHTHW2UzPCCq MWfpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= M1zZdlI3OTh2OUm5
SK-MEL-28 Ml7JSpVv[3Srb36gRZN{[Xl? M1nNXFUxNzFyMPMAjeK2VQ>? MorqOFghcA>? NYHZZpc5TE2VTx?= M4rSTJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl MUiyOVIyPjV{Mh?=
MeWo NYHrN3ZbTnWwY4Tpc44hSXO|YYm= M165blUxNzFyMPMAjeK2VQ>? MojZOFghcA>? NEfPTGpFVVOR NXnFRoo2emWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MnPjNlUzOTZ3MkK=
SK-MEL-5 M3fac2Z2dmO2aX;uJGF{e2G7 NWLyVVd3PTBxMUCw5qCKyrWP NF74V281QCCq MX;EUXNQ NVfhVGZVemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> M{fXVFI2OjF4NUKy
SK-MEL-2 NEPxV3lHfW6ldHnvckBCe3OjeR?= NELRRZU2OC9zMEFihKnDvU1? M33UclQ5KGh? NYLub5J7TE2VTx?= NFLr[25z\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> M3P1N|I2OjF4NUKy
B16-F0 NVzUXIF3TnWwY4Tpc44hSXO|YYm= NW\SSpZtPTBxMUCw5qCKyrWP MkS1OFghcA>? NYW0NJFMTE2VTx?= M4Xvc5Jm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NFTqdFEzPTJzNkWyNi=>
TRPM2/HEK  NHXiNGZHfW6ldHnvckBCe3OjeR?= M3i4NFAvOeLCk{K1xsDDvU1? MUGxOeKhdWmw MYfEUXNQ MmqydoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyBzLkhCpOK2VQ>? NH75SokzPTF5OUW3OC=>
U937  NWHYZWJsTnWwY4Tpc44hSXO|YYm= NF7XflcxNjIkgKOyOeKhyrWP M3XuZ|E2yqCvaX6= MUjEUXNQ NFvzSHlz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IECuOOKhyrWP Mn3rNlUyPzl3N{S=
TRPM2/HEK  MnzGSpVv[3Srb36gRZN{[Xl? NH3jT4UyOMLiwsXN NVHEWpY6PDEEoH3pci=> MknxSG1UVw>? M3vPfZJm\HWlZYOgWHJRVTJiYXP0bZZifGmxbjDleoVvKGG2IHjp[4gh[2:wY3XueJJifGmxboOgc4YhUDKRMh?= M4nLfVI2OTd7NUe0
GL37  M4PHOWNmdGxiVnnhZoltcXS7IFHzd4F6 MnTaNE0yOMLiwsXN MXm0PEBp NY[4UWhUe3WycILld5NmeyCOYTDlfJBz\XO|aX;u MViyOFk6QTZ3Nx?=
NRK-52E NUHZfoRRTnWwY4Tpc44hSXO|YYm= M2rablHDqML3TR?= MYixNEBucW5? MUHicI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi MlXqNlQ4OTB2MkO=
NRK-52E M1:2fGZ2dmO2aX;uJGF{e2G7 NXTqbVZkOcLiwsXN MXSxNEBucW5? M4\NWYJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> NH\r[ZIzPDdzMESyNy=>
HSC  MVnGeY5kfGmxbjDBd5NigQ>? MWOyNEDPxE1? NXrsbog{OSCq NETEfJli[nKxZ3H0[ZMhfGinIHTp[oZmemWwdHnhcEBm\m[nY4TzJI9nKGyncITpckBweiCDR1Xz NG\DXpMzPDZzNEG5PS=>
EJ NGG1XnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLMRYxMPTBxOECg{txO NHq4flEzPC92OD:3NkBp NHTjcYJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NGDSVVEzPDV6N{C0PS=>
EJ MoXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVy1NE85OCEQvF2= MWW0PEBp NVnCR4dR[2G3c3XzJHMueGijc3WgZZJz\XO2 M173NVI1PTh5MES5
EJ M2PWcWZ2dmO2aX;uJGF{e2G7 NXnUXWdnPTBxOECg{txO Mn73OFghcA>? M{DwPYRwf26{ZXf1cIF1\XNiYz3NfYMtKGO7Y3zpcmQyNCC|dYL2bZZqdiCjbnSgWmVITiCneIDy[ZN{cW:wcx?= NF3JbmgzPDV6N{C0PS=>
HepG2 MnX0SpVv[3Srb36gRZN{[Xl? MXi1NE02ODBizszN Mk\DOlDDqG2rbh?= NX;rbWpWcW6qaXLpeJMhfGinIFnMMVYucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEGgLHR6ejdyNTmgZY5lKFOWQWSzJEhVgXJ5MEWpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MUOyOFI1OjB2Nh?=
SGC7901 NXfySlg{S2WubDDWbYFjcWyrdImgRZN{[Xl? NWrrOm41OC1zMECg{txO NUniW4k6OjRxNEivO|IhcA>? M2LzeYNifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> MXSyOFE2OTJ3NR?=
AGS  MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlXPNE0yODBizszN Ml\hNlQwPDhxN{KgbC=> MmjkZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 M2jtPVI1OTVzMkW1
SGC7901 MVrGeY5kfGmxbjDBd5NigQ>? NFrXW|Q2OCEQvF2= MVqyOE81QC95MjDo MnrXeIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= NVrDSoRDOjRzNUGyOVU>
AGS  NG\IVVJHfW6ldHnvckBCe3OjeR?= M1;OXFUxKM7:TR?= NXj1NWNvOjRxNEivO|IhcA>? M4DobZRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg NGT5dIgzPDF3MUK1OS=>
SGC7901 MonvSpVv[3Srb36gRZN{[Xl? MkP2OVAh|ryP MWKyOE81QC95MjDo Ml20eIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> NFLoNWUzPDF3MUK1OS=>
AGS  M3jSNGZ2dmO2aX;uJGF{e2G7 M4XQVFUxKM7:TR?= MYGyOE81QC95MjDo MWP0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> NVfVTHU4OjRzNUGyOVU>
MC3T3-E1  M3XHTmZ2dmO2aX;uJGF{e2G7 M3nKRlUxKM7:TR?= MVu0JIg> M{jVOolvcGmkaYTzJGhUTS2rbnT1Z4VlKEKPUEegZY5lKEeKUjDwdo91\WmwIHX4dJJme3Orb39CpC=> MViyN|g4Pzd|NB?=
7TD1-DXM MlnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqxNEDPxE1? M{jaTlczKGh? MVnEUXNQ NIO4VIhqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NG\1R3UzOzh5MUG1PS=>
7TD1-WD-90 MkHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG3b483OTBizszN NUjEfZJ7PzJiaB?= NY[wWmF3TE2VTx?= M4X1colvcGmkaYTzJINmdGxiZ4Lve5Rp M3;zdFI{QDdzMUW5
7TD1-DXM MYXBdI9xfG:|aYOgRZN{[Xl? MnTUOVAh|ryP M1L5[|Q5KGh? M3zZPWROW09? MnK1bY5lfWOnczDhdI9xfG:|aYO= NIf6OmQzOzh5MUG1PS=>
7TD1-WD-90 Mn\PRZBweHSxc3nzJGF{e2G7 MoK2OVAh|ryP MoPNOFghcA>? NX\r[VM5TE2VTx?= NYrWe4FMcW6mdXPld{BieG:ydH;zbZM> MmOzNlM5PzFzNUm=
7TD1-WD-90  Mn36SpVv[3Srb36gRZN{[Xl? NFi2XZc2OCEQvF2= M130dlYhcA>? MXvEUXNQ M4rQdZNq\26rZnnjZY51dHliaX7obYJqfHNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBLSUt{IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEO= MkH1NlM5PzFzNUm=
HepG2  MX\GeY5kfGmxbjDBd5NigQ>? MWmxNFAh|ryP MlXFNVIwOjRiaB?= NHzlWJJqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25? MXiyN|g{PjRyMB?=
RAW264.7  MVzGeY5kfGmxbjDBd5NigQ>? M1Hw[FUxyqEQvF5CpC=> M2PC[lI1NzR6IHi= M4D3[ZN2eHC{ZYPz[ZMhWkGQS1ytbY5lfWOnZDDvd5Rmd2OuYYP0c4dmdmW|aYO= MWKyN|Y3PTBzOB?=
RAW264.7 MoLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKwMVUxyqEQvF5CpC=> MmG3OFjDqGh? NVP5U25UcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[U1l\XCnbnTlcpRtgQ>? NFv2ZoYzOzZ4NUCxPC=>
RAW264.7 NYjVOmlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DQclAuPTEEoN88UeKh NFTTZ2M1QMLiaB?= MlPCZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= M1S1RlI{PjZ3MEG4
RAW264.7 NUW4OWZvTnWwY4Tpc44hSXO|YYm= NVnYUogyPTEEoN88US=> MmSwNlQwPDhiaB?= MY\pcohq[mm2czDSRW5MVC2rbnT1Z4VlKE6IQWTjNUBmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gV4VzPzJ5U2TBWFM> NGTOZ3ozOzZ4NUCxPC=>
A549  M1;L[2Z2dmO2aX;uJGF{e2G7 NUnRTIR5OjBxNECg{txO M3zVOVIxKGh? MkHBNlAh|ryPIFHHOFkxKHO3cIDy[ZN{\XNidHjlJJJi\GmjdHnvck1qdmS3Y3XkJIlvfmG|aX;uJI9nKEF3NEmgZ4VtdHN? NH3u[GkzOzZ{MEG5NS=>
A549  MV7GeY5kfGmxbjDBd5NigQ>? M3rkOlExNzJyL{SwJO69VQ>? MmrPNlQhcA>? MXzzeZBxemW|c3XzJJRp\SC{YXTpZZRqd25vaX7keYNm\CCnbHX2ZZRqd25ib3[gWmVITsLi NXLJUW1kOjN4MkCxPVE>
HUVECs MnXpR4VtdCCYaXHibYxqfHliQYPzZZk> M33CSlIxKML3TR?= MnHQOEBp MYnheJRmdnWjdHXzJGgzVzJvaX7keYNm\CClZXzsJJNpemmwa3Hn[UBidmRiaX3wdo93\WRidHjlJIF1fGGlaH3lcpQhemG2ZTDv[kB1cGViY3XscJM> NX;WcXJbOjN2OEO5OFY>
HUVECs NV7JOpg3SXCxcITvd4l{KEG|c3H5 NFzud2ozOCEEtV2= NIrYe441KGh? M4nFTZNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBk\WyuIHHwc5B1d3SrYzDpcoRmgA>? MVWyN|Q5Ozl2Nh?=
BV-2  NFfYVmNHfW6ldHnvckBCe3OjeR?= Mom5NlAhyrWP NVHPUmNvOTZiaB?= MX\pcohq[mm2czDMVHMucW6mdXPl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBidG2xc4SgZ49ueGyndHXsfUBlcW2rbnnzbIVlKGmQT2Og[ZhxemW|c3nvci=> MkX3NlMzOzZ|N{C=
NRK-52E  NWLrRoxvTnWwY4Tpc44hSXO|YYm= NV3zeFZ[PcLizszN NV73R4NGOzEEoH3pci=> MYjheJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> M17ISlI{OTd2N{W3
SW620  MoGySpVv[3Srb36gRZN{[Xl? M3PVVFIxKML3TR?= M33LclEwPiCq NEXOZW1qdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> NFfrRowzOzFzME[yOS=>
RPE  MlvCSpVv[3Srb36gRZN{[Xl? NHryS3Y{OCEEtV5CpC=> MXqzJIg> NGnGSHBqdmirYnn0d{B1cGViaX7keYN1cW:wIH;mJJAuW1SDVEOg[ZhxemW|c3nvci=> NXf0d5A2OjNyOUSwOlc>
SW1116 M2rQdGZ2dmO2aX;uJGF{e2G7 M1jTV|ExOCEEtV5CpC=> MnLPNlQwPDhxN{KgbC=> NXj6T3o{\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= MonmNlIxPTB5OUC=
HT29 MmPrSpVv[3Srb36gRZN{[Xl? NUmwfJI1OTByINM1UeKh MkLQNlQwPDhxN{KgbC=> NVviPIxv\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= MXKyNlA2ODd7MB?=
SW1116 NFfQOWFHfW6ldHnvckBCe3OjeR?= M3S4RVExOCEEtV5CpC=> MX6yOE81QC95MjDo M4DoTIRm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh Mki0NlIxPTB5OUC=
HT29 NGrOPI5HfW6ldHnvckBCe3OjeR?= M4DNcVExOCEEtV5CpC=> NWfEXmdqOjRxNEivO|IhcA>? NHfEToxl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NGm3WGczOjB3MEe5NC=>
ARPE-19 NUT0[|Z6TnWwY4Tpc44hSXO|YYm= Mof4OeKh|ryP MlPMN|DDqG2rbh?= MlHvbY5pcWKrdIOgTmFMOiCyaH;zdIhwemmuYYTpc44> MkfkNlE3OjB7NkO=
HSC-T6 MY\BdI9xfG:|aYOgRZN{[Xl? NF;DPXAyOMLizszN NHjtUWkzyqCqwrC= MUfpcohq[mm2czD0bIUh[XCxcITvd4l{KG:oIFjTR{1VPiClZXzsd{BqdmS3Y3XkJIJ6KEOGRR?= Ml3HNlE{QTZ7OUi=
HSC-T6 NUTDOHlETnWwY4Tpc44hSXO|YYm= NWjMSmVyOTEEoN88US=> M1jZXlLDqGkEoB?= MlnZbY5pcWKrdIOgeIhmKGW6cILld5Nqd26|IH;mJJB[NVOWQWSxJIFv\CCEYXSgbY5lfWOnZDDifUBETEV? NV\NcINWOjF|OU[5PVg>
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THP1 Mle3SpVv[3Srb36gRZN{[Xl? MWOxNEB2VQ>? NVL1dZdMOzBibXnuxsA> NYj0S|ZNcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wIHL5JI93\XJiNkCl M2S3U|IxOzl|Nkmw
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Jurkat  Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GycVUxKM7:TR?= M{jhb|I1NzR6L{eyJIg> MlzU[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u M3nIPFE6PTZ2OEmx
SUPT1  MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MontOVAh|ryP NInrVIQzPC92OD:3NkBp MV7lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NILOZlcyQTV4NEi5NS=>
Jurkat  MnjsRZBweHSxc3nzJGF{e2G7 MlTVOVAh|ryP Mn7PNlQwPDhiaB?= NHG4fIRmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ M2TqUVE6PTZ2OEmx
SUPT1  MVLBdI9xfG:|aYOgRZN{[Xl? NVjNV|lUPTBizszN M3XjZ|I1NzR6IHi= MYPlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz NX7Hfpl{OTl3NkS4PVE>

... Click to View More Cell Line Experimental Data

In vivo Administration of AG-490 drastically reduces the numbers of CD45+ and HLA-DR+ cells from 48 % and 46% in bone marrow of untreated mice, as well as 38% and 22% in the spleen of untreated mice to undetectale levels. [2] In vivo administration of AG-490 causes murine myeloma tumor cell apoptosis but does not inhibit IL-12-mediated macrophage activation and IFN-γ production by lymphocytes. [6] Consistent with the in vitro blocking of JAK2 V617F mutant activity, AG-490 treatment at 0.5 mg/day for 10 days effectively inhibits JAK2 V617F mutant-induced tumorigenesis and tumor cell invasion in nude mice. [8] Combined therapy with AG-490 and IL-12 induces greater antitumor effects than either agent alone in a murine myeloma tumor model. [6]

Protocol

Kinase Assay:

[1]

+ Expand

In vitro kinase autophosphorylation:

AG-490 is dissolved in DMSO 10%-H2O-ethanol 45%. Crude membrane extracts (0.125 μg/mL) are preactivated with EGF (20 nM) in 50 mM HEPES buffer, pH 7.6, and 125 mM NaCl, for 15 minutes at 4 °C. Autophosphorylation activity of EGFR or ErbB2 kinase is assayed at 4 °C for 30 seconds in V-shaped 96-well plates. Membrane extracts (8 μL) are added to each well containing reaction mixture (12 μL, 50mM, HEPES, pH 7.4,125 mM NaCl, 12 mM M8Ac2, 2 mM MnCl2, 1 mM NaVO3, 1 μM ATP, and 1 μCi[γ-32P]ATP, final concentrations) and increasing concentrations of AG-490 (4 μL). After termination by addition of hot sample buffer, the samples are run on a 6% SDS-polyacrylamide gel electrophoresis minigel, the gels dried, and autoradiography performed during the linear exposure time period. The receptor bands are scanned densitrometrically, and the results analyzed by the Ez-Fit program. For the analysis of autophosphorylation of JAK2, JAK2 is immunoprecipitated by using anti-JAK2 antibody from lysates of G2 cells pretreated for 16 hours with increasing concentrations of AG-490 (0-50 μM). Immune complexes are then immunoblotted with anti-phosphotyrosine antibody. A dose-dependent inhibition of in vitro kinase activity is demonstrated by assessing JAK2 autophosphorylation.
Cell Research:

[2]

+ Expand
  • Cell lines: Pre-B ALL
  • Concentrations: Dissolved in DMSO, final concentrations ~ 50 μM
  • Incubation Time: 16 hours
  • Method:

    Cells are exposed to different concentrations of AG-490 for 16 hours. For the determination of cell proliferation, [3H]tymidine (1 μCi) is added 6 hours or more before the cultures are terminated. Cells are then collected and samples counted in a liquid scintillation counter.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: SCID mice intravenously injected with ALL cells
  • Formulation: Dissolved in DMSO
  • Dosages: 0.85 mg + 0.5 mg daily
  • Administration: Continuous pump infusion supplemented with daily intraperitoneal injections
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 58 mg/mL (197.07 mM)
Ethanol 6 mg/mL (20.38 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 294.30
Formula

C17H14N2O3

CAS No. 133550-30-8
Storage powder
Synonyms Zinc02557947

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    I would like to know whether AG490 (S1143) goes to CNS through BBB, or not?

  • Answer:

    AG-490 can go through the BBB. You can see this reference: http://bloodjournal.hematologylibrary.org/content/111/4/2062.full.html.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID