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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Cited by 14 Publications

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 NYX4fY1jTnWwY4Tpc44hSXO|YYm= NFzJT|MyODEkgJpCuW0> NEfNT5ozPCCq NWHLWlU3dWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ MU[yOlE5PDl7OR?=
BCBL1 MVvGeY5kfGmxbjDBd5NigQ>? M{\CT|ExOOLCidM1US=> NF\YTpAzPCCq NFjxbIFu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> MYmyOlE5PDl7OR?=
BC3 MljHSpVv[3Srb36gRZN{[Xl? MYKxNFDjiIoEtV2= MlfQNlQhcA>? NEC2NG5u\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0ZzIILl[JVkfGmxbh?= NYPZOGxFOjZzOES5PVk>
BCBL1 M3PDfWZ2dmO2aX;uJGF{e2G7 MXuxNFDjiIoEtV2= MV2yOEBp NEe3V4Ju\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= NILISnUzPjF6NEm5PS=>
BC3 NU[4c4U3TnWwY4Tpc44hSXO|YYm= MWmxNFDjiIoEtV2= NV7GTYtUOjRiaB?= NHHWcppqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> MXiyOlE5PDl7OR?=
BCBL1 MXjGeY5kfGmxbjDBd5NigQ>? M3PkeFExOOLCidM1US=> NHTUV5ozPCCq MXzpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= NX7TWnM4OjZzOES5PVk>
SK-MEL-28 NVLZPFhjTnWwY4Tpc44hSXO|YYm= NWD4OJZPPTBxMUCw5qCKyrWP M2\OcFQ5KGh? MUPEUXNQ MlO3doVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= MkjwNlUzOTZ3MkK=
MeWo M4LGVmZ2dmO2aX;uJGF{e2G7 M2DuZ|UxNzFyMPMAjeK2VQ>? M1v4cVQ5KGh? MnjvSG1UVw>? MkD4doVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NHPnTXQzPTJzNkWyNi=>
SK-MEL-5 NGjOWIlHfW6ldHnvckBCe3OjeR?= MmT6OVAwOTBy4pEJxtVO M1mzVFQ5KGh? MVfEUXNQ NUjXdFZbemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NIm1VYozPTJzNkWyNi=>
SK-MEL-2 MX\GeY5kfGmxbjDBd5NigQ>? NHjMTpo2OC9zMEFihKnDvU1? MoPBOFghcA>? MVHEUXNQ NVzRN3k2emWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NYHXT5JlOjV{MU[1NlI>
B16-F0 NEG1cFRHfW6ldHnvckBCe3OjeR?= Mn7XOVAwOTBy4pEJxtVO NYWzXGdCPDhiaB?= M1TyU2ROW09? NU\LN4JkemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NXHsT4hCOjV{MU[1NlI>
TRPM2/HEK  MlnUSpVv[3Srb36gRZN{[Xl? MnOwNE4y6oDVMkZCpOK2VQ>? NWXScWM{OTYEoH3pci=> M4jpdWROW09? MWTy[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDFwN9MgxtVO NGntNXEzPTF5OUW3OC=>
U937  M1jhR2Z2dmO2aX;uJGF{e2G7 NWjpb3pHOC5z4pETNlXDqML3TR?= M{jOb|E2yqCvaX6= NX7HZ4dGTE2VTx?= M3z5TpJm\HWlZYOgTFJQOi2rbnT1Z4VlKEOjMjvpcoNz\WG|ZTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjygZY5lKHSqZTDJR|UxyqC4YXz1[UB4[XNiMD60xsDDvU1? NWftR45NOjVzN{m1O|Q>
TRPM2/HEK  NUjEPGl7TnWwY4Tpc44hSXO|YYm= MnnXNVDDqML3TR?= M175elQxyqCvaX6= MYHEUXNQ NWXWOYM6emWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y MVyyOVE4QTV5NB?=
GL37  Mmj6R4VtdCCYaXHibYxqfHliQYPzZZk> MljMNE0yOMLiwsXN M1nsflQ5KGh? NHfzOJh{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= M1jYOVI1QTl7NkW3
NRK-52E MV7GeY5kfGmxbjDBd5NigQ>? NYjX[FBoOcLiwsXN M2DLXFExKG2rbh?= NUjwVHFJ[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> M3TpZlI1PzFyNEKz
NRK-52E Mkm3SpVv[3Srb36gRZN{[Xl? M1T3fFHDqML3TR?= NX3rVphTOTBibXnu NWjK[HUx[myxY3vzJGFv\yCLSTDpcoR2[2WmIFPENlQh\XiycnXzd4lwdg>? M2q5OVI1PzFyNEKz
HSC  M1ezbWZ2dmO2aX;uJGF{e2G7 NYqzUYJ2OjBizszN NGjN[FIyKGh? MUfhZpJw\2G2ZYOgeIhmKGSrZn\ldoVvfGmjbDDl[oZm[3S|IH;mJIxmeHSrbjDvdkBCT0W| MonBNlQ3OTRzOUm=
EJ MkjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fIdFUxNzhyIN88US=> NWTOS21TOjRxNEivO|IhcA>? NUXrb3M6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= Mlj6NlQ2QDdyNEm=
EJ MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD2OVAwQDBizszN M2TRUFQ5KGh? NWG3fGhF[2G3c3XzJHMueGijc3WgZZJz\XO2 NXHlPWM1OjR3OEewOFk>
EJ NV;wdFFMTnWwY4Tpc44hSXO|YYm= M3HWS|UxNzhyIN88US=> NI\WO4g1QCCq NETsSW5ld3ewcnXneYxifGW|IHOtUZlkNCCleXPsbY5FOSxic4Xyeol3cW5iYX7kJHZGT0ZiZYjwdoV{e2mxboO= M13ablI1PTh5MES5
HepG2 M37ZS2Z2dmO2aX;uJGF{e2G7 MVS1NE02ODBizszN NHfOT4w3OMLibXnu MX3pcohq[mm2czD0bIUhUUxvNj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSBqVInyO|A2MSCjbnSgV3RCXDNiKGT5dlcxPSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mlv4NlQzPDJyNE[=
SGC7901 NG\LUoxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{jjclAuOTByIN88US=> M13sV|I1NzR6L{eyJIg> MXnjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= NEPuV2ozPDF3MUK1OS=>
AGS  NV65WG5qS2WubDDWbYFjcWyrdImgRZN{[Xl? NVPZfVJnOC1zMECg{txO M2fB[FI1NzR6L{eyJIg> NF\TeY1k[XW|ZYOgZUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliZH;z[U1l\XCnbnTlcpRtgSCkdYSgco91KHSrbXWt[IVx\W6mZX70cJk> NF;PWmEzPDF3MUK1OS=>
SGC7901 M1HqXGZ2dmO2aX;uJGF{e2G7 NXPRRYdkPTBizszN NYTxZ2h2OjRxNEivO|IhcA>? M{\RbZRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg M4\Ye|I1OTVzMkW1
AGS  NHjtVZZHfW6ldHnvckBCe3OjeR?= MYS1NEDPxE1? MYSyOE81QC95MjDo NXrjeHMzfGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> M3ToVVI1OTVzMkW1
SGC7901 NGr2XoRHfW6ldHnvckBCe3OjeR?= MkLrOVAh|ryP NYn5XmdROjRxNEivO|IhcA>? NXLZfVlLfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? NWexb3hROjRzNUGyOVU>
AGS  MkD4SpVv[3Srb36gRZN{[Xl? MmrlOVAh|ryP MXqyOE81QC95MjDo Mn6xeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> NGS0[28zPDF3MUK1OS=>
MC3T3-E1  NIDNNGZHfW6ldHnvckBCe3OjeR?= M4Px[lUxKM7:TR?= NFO2dI81KGh? M2m0eYlvcGmkaYTzJGhUTS2rbnT1Z4VlKEKPUEegZY5lKEeKUjDwdo91\WmwIHX4dJJme3Orb39CpC=> M3HBOVI{QDd5N{O0
7TD1-DXM M3fu[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuxNEDPxE1? Mny0O|IhcA>? NIHWcXhFVVOR Mn7qbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NX74N5ZLOjN6N{GxOVk>
7TD1-WD-90 NVu4Z2M4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;mNVAh|ryP MmT4O|IhcA>? MXfEUXNQ NFXjdnZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4rZUVI{QDdzMUW5
7TD1-DXM NIj0fGhCeG:ydH;zbZMhSXO|YYm= MX:1NEDPxE1? MljGOFghcA>? M1jlWWROW09? MoS5bY5lfWOnczDhdI9xfG:|aYO= MnPTNlM5PzFzNUm=
7TD1-WD-90 MVTBdI9xfG:|aYOgRZN{[Xl? MVW1NEDPxE1? MUe0PEBp NU\qOoFZTE2VTx?= MVLpcoR2[2W|IHHwc5B1d3Orcx?= NW\RNHBCOjN6N{GxOVk>
7TD1-WD-90  NXi4N|llTnWwY4Tpc44hSXO|YYm= M2XJZVUxKM7:TR?= NIS1N3Y3KGh? NUHhT4xbTE2VTx?= M2PRcZNq\26rZnnjZY51dHliaX7obYJqfHNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBLSUt{IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEO= NXL1RW43OjN6N{GxOVk>
HepG2  M{\uSmZ2dmO2aX;uJGF{e2G7 MkfHNVAxKM7:TR?= M1r3elEzNzJ2IHi= NH7wNopqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25? NFjtcW0zOzh|NkSwNC=>
RAW264.7  NFLldpNHfW6ldHnvckBCe3OjeR?= MUm1NOKh|ryPwrC= M{nnSFI1NzR6IHi= NUfCOXZ6e3WycILld5NmeyCUQV7LUE1qdmS3Y3XkJI9{fGWxY3zhd5Rw\2WwZYPpdy=> NInsfIUzOzZ4NUCxPC=>
RAW264.7 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlGzNE02OMLizszNxsA> NHrPe3k1QMLiaB?= NXy2OYo2cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[U1l\XCnbnTlcpRtgQ>? MnS5NlM3PjVyMUi=
RAW264.7 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHOyTJcxNTVywrFOwG3DqA>? M4[yc|Q5yqCq MXXjZZV{\XNiYX6gZZJz\XO2IH;mJHJCXzJ4ND63JINmdGy|IHH0JJRp\SCJMD;HNUBxcGG|ZTDv[kB1cGViY3XscEBkgWOuZR?= MUCyN|Y3PTBzOB?=
RAW264.7 M1fvUmZ2dmO2aX;uJGF{e2G7 M2HZSlUxyqEQvF2= M4PKcVI1NzR6IHi= MVPpcohq[mm2czDSRW5MVC2rbnT1Z4VlKE6IQWTjNUBmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gV4VzPzJ5U2TBWFM> MWGyN|Y3PTBzOB?=
A549  MYrGeY5kfGmxbjDBd5NigQ>? M4eyZ|IxNzRyIN88US=> NH\l[mozOCCq MWOyNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? NIG4fJQzOzZ{MEG5NS=>
A549  M3zvUGZ2dmO2aX;uJGF{e2G7 NV[0R4R3OTBxMkCvOFAh|ryP NFy3OIEzPCCq MmDFd5VxeHKnc4Pld{B1cGVicnHkbYF1cW:wLXnu[JVk\WRiZXzleoF1cW:wIH;mJHZGT0cEoB?= M2XUOFI{PjJyMUmx
HUVECs MlrxR4VtdCCYaXHibYxqfHliQYPzZZk> M2HzUFIxKML3TR?= MVq0JIg> MonjZZR1\W63YYTld{BJOk9{LXnu[JVk\WRiY3XscEB{cHKrbnvh[4Uh[W6mIHntdJJwfmWmIITo[UBifHSjY3jt[Y51KHKjdHWgc4YhfGinIHPlcIx{ Ml7jNlM1QDN7NE[=
HUVECs M3mzO2Fxd3C2b4Ppd{BCe3OjeR?= MkOzNlAhyrWP MXW0JIg> MXPzbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgZ4VtdCCjcH;weI91cWNiaX7k[Zg> NIfRdo0zOzR6M{m0Oi=>
BV-2  NX7kNlc4TnWwY4Tpc44hSXO|YYm= MmjXNlAhyrWP NHOy[VkyPiCq M{HORYlvcGmkaYTzJGxRWy2rbnT1Z4VlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKGGubX;zeEBkd22ybHX0[Yx6KGSrbXnubZNp\WRiaV7PV{BmgHC{ZYPzbY9v MV2yN|I{PjN5MB?=
NRK-52E  NGPCeY1HfW6ldHnvckBCe3OjeR?= MofvOeKh|ryP NVy5ZVNGOzEEoH3pci=> M4fSc4F1fGWwdXH0[ZMhSW6pLTix5qCUPylvaX7obYJqfGWmIGTHSk3PujFibWLORUBifCBzNtMgbOKh MoLHNlMyPzR5NUe=
SW620  MnfUSpVv[3Srb36gRZN{[Xl? MXOyNEDDvU1? MYmxM|YhcA>? NUDIV2g{cW6qaXLpeJMheC2VVFHUN{Bi[3SrdnH0bY9v MV[yN|EyODZ{NR?=
RPE  MmTSSpVv[3Srb36gRZN{[Xl? MoTWN|AhyrWPwrC= MnzLN{Bp Mor1bY5pcWKrdIOgeIhmKGmwZIXjeIlwdiCxZjDwMXNVSVR|IHX4dJJme3Orb36= NWXXPYdJOjNyOUSwOlc>
SW1116 MVLGeY5kfGmxbjDBd5NigQ>? MUmxNFAhyrWPwrC= NUjDXmt2OjRxNEivO|IhcA>? MUTk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? M3SwWFIzODVyN{mw
HT29 MY\GeY5kfGmxbjDBd5NigQ>? NUHxVZI{OTByINM1UeKh MkG1NlQwPDhxN{KgbC=> MX7k[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? MUiyNlA2ODd7MB?=
SW1116 MXLGeY5kfGmxbjDBd5NigQ>? NGW0XVcyODBiwsXNxsA> M4HQclI1NzR6L{eyJIg> NGraPY1l\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NV3I[JN1OjJyNUC3PVA>
HT29 MomySpVv[3Srb36gRZN{[Xl? NEi5d3cyODBiwsXNxsA> NX\wb5dUOjRxNEivO|IhcA>? NGDQOY1l\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? MYOyNlA2ODd7MB?=
ARPE-19 NXfVNXRoTnWwY4Tpc44hSXO|YYm= NHLSOGg2yqEQvF2= M4[zN|MxyqCvaX6= MYTpcohq[mm2czDKRWszKHCqb4PwbI9zcWyjdHnvci=> Ml\uNlE3OjB7NkO=
HSC-T6 MU\BdI9xfG:|aYOgRZN{[Xl? M{PvXFExyqEQvF2= NVn6TGh1OsLiaNMg NF\lZ3lqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> MVeyNVM6Pjl7OB?=
HSC-T6 NYTENIl3TnWwY4Tpc44hSXO|YYm= MYOxNOKh|ryP M3rHWFLDqGkEoB?= NF;SXYtqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= NV3TepZ7OjF|OU[5PVg>
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MZ-304 NVTWOIVDTnWwY4Tpc44hSXO|YYm= MlLFOVAwOTBywrFOwG0> M1i3SFQ5KGh? MkTVdoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u MVSyNFU5QTV{NR?=
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MZ-256 MkjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVq1NE8yODEEoN88US=> MoPWOFghcA>? M17VWoxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NHHj[XQzODV6OUWyOS=>
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A-172 NEj0R|VHfW6ldHnvckBCe3OjeR?= M3fxTVUxNzFyMNMg{txO NVXPd2loPDhiaB?= NIPLPGFz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MkjjNlA2QDl3MkW=
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MZ-256 MVfGeY5kfGmxbjDBd5NigQ>? NHr5PIM2OC9zMEFCpO69VQ>? MXS0PEBp NFzaNGFz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ Mn22NlA2QDl3MkW=
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SW1990 MWfJcpZie2mxbjDBd5NigQ>? NYjSfpdYOjBizszN NHO1OJMzPCCq MXHy[YR2[2W|IHnueoF{cW:wIH;mJHNYOTl7MDDj[Yxte8Li NUDyeJBlOjB2OEK4OVg>
THP1 MV3GeY5kfGmxbjDBd5NigQ>? NF;yXWYyOCC3TR?= MUKzNEBucW8EoB?= M4HZVYlvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCkeTDveoVzKDZyJR?= NFTqVlczODN7M{[5NC=>
BMMC MmnYSpVv[3Srb36gRZN{[Xl? MY[wMVExKM7:TR?= Ml34NVXDqG2rbh?= NUHufplPcW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? Mmf5NVk5OzV6NEW=
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OVCAR-3 MUXGeY5kfGmxbjDBd5NigQ>? MlTiNVAhfU1? MXexJIg> MX7pcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? MWWxPVY1PzN4Mx?=
PA-1 NXLjdVM6TnWwY4Tpc44hSXO|YYm= MlPuNVAhfU1? MYOxJIg> MYjpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? MoDhNVk3PDd|NkO=
OVCAR-3 MWTGeY5kfGmxbjDBd5NigQ>? MoLlNVAhfU1? MYWxJIg> MVPpcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? NWnWe5hqOTl4NEezOlM>
PA-1 M1f1O2Z2dmO2aX;uJGF{e2G7 Mk[1NVAhfU1? M3jaT|EhcA>? NVLwe2NPcW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= Mmn4NVk3PDd|NkO=
Jurkat  M2\Xbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljyOVAh|ryP MkiyNlQwPDhxN{KgbC=> MV3lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NH\DTlcyQTV4NEi5NS=>
SUPT1  MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoqxOVAh|ryP NHfHTGozPC92OD:3NkBp M{jFOoVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> NVHUNmVuOTl3NkS4PVE>
Jurkat  NIXLdFhCeG:ydH;zbZMhSXO|YYm= NHzRVVE2OCEQvF2= NGDGTFMzPC92ODDo MVrlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz M2K0ZVE6PTZ2OEmx
SUPT1  NVTze2t{SXCxcITvd4l{KEG|c3H5 NGHtO|g2OCEQvF2= NWjCT|dkOjRxNEigbC=> MXrlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz NH\PZWIyQTV4NEi5NS=>

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:

[1]

+ Expand

In vitro kinase autophosphorylation:

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

[2]

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

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


    (Only for Reference)
Animal Research:

[2]

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 294.30
Formula

C17H14N2O3

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

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Tech Support

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

Handling Instructions

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

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

  • * 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