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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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 NYX3RllGTnWwY4Tpc44hSXO|YYm= MorTNVAx6oDLwsXN M1H4S|I1KGh? M{jpSY1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> NV\oSo97OjZzOES5PVk>
BCBL1 NWnub3ZsTnWwY4Tpc44hSXO|YYm= M1y3dlExOOLCidM1US=> NInTN3MzPCCq MWft[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= M371flI3OTh2OUm5
BC3 NHLmW4lHfW6ldHnvckBCe3OjeR?= MVKxNFDjiIoEtV2= NHTm[IczPCCq NX;tSlJzdWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMTDy[YR2[3Srb36= M2rZUVI3OTh2OUm5
BCBL1 M2XvXmZ2dmO2aX;uJGF{e2G7 Moj1NVAx6oDLwsXN NYTKXWplOjRiaB?= MoOzcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOiC{ZXT1Z5Rqd25? NVTwTJF6OjZzOES5PVk>
BC3 MorhSpVv[3Srb36gRZN{[Xl? M2jpflExOOLCidM1US=> M1vF[|I1KGh? M{Tjdolv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKG[udYlCpC=> MVSyOlE5PDl7OR?=
BCBL1 NEPUeHZHfW6ldHnvckBCe3OjeR?= NXTOdG8{OTBy4pEJxtVO NFHWTJQzPCCq Mkf2bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NGfudVQzPjF6NEm5PS=>
SK-MEL-28 NEHOUWlHfW6ldHnvckBCe3OjeR?= MlnPOVAwOTBy4pEJxtVO M{G3U|Q5KGh? NW\KbnZITE2VTx?= NVPpTHp2emWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NGXwSnMzPTJzNkWyNi=>
MeWo NX72VHRsTnWwY4Tpc44hSXO|YYm= M4XxXlUxNzFyMPMAjeK2VQ>? M1LuN|Q5KGh? NX3HOpJ6TE2VTx?= MXny[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= NIe2OZczPTJzNkWyNi=>
SK-MEL-5 MmTlSpVv[3Srb36gRZN{[Xl? NXXafGxGPTBxMUCw5qCKyrWP MX:0PEBp M4nK[WROW09? NXrBWZZXemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NH\IVFUzPTJzNkWyNi=>
SK-MEL-2 NH\hPZRHfW6ldHnvckBCe3OjeR?= NWLh[YdtPTBxMUCw5qCKyrWP MXq0PEBp MoTrSG1UVw>? NIXDbHRz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> Mo\5NlUzOTZ3MkK=
B16-F0 NXyxbHU1TnWwY4Tpc44hSXO|YYm= MkO1OVAwOTBy4pEJxtVO Mn;BOFghcA>? M1jPVWROW09? NX22SXUzemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MUeyOVIyPjV{Mh?=
TRPM2/HEK  NWDobnZwTnWwY4Tpc44hSXO|YYm= M3jZW|AvOeLCk{K1xsDDvU1? NGLzZ3YyPcLibXnu NXLYd4RKTE2VTx?= MkTadoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyBzLkhCpOK2VQ>? NVfWbnF1OjVzN{m1O|Q>
U937  NWHBd|BRTnWwY4Tpc44hSXO|YYm= NXmyd|NEOC5z4pETNlXDqML3TR?= NX7DflVjOTYEoH3pci=> NVfwelZNTE2VTx?= NIrHUGlz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IECuOOKhyrWP M17pUVI2OTd7NUe0
TRPM2/HEK  M3H0dGZ2dmO2aX;uJGF{e2G7 MUWxNOKhyrWP NH3OOGQ1OMLibXnu NX7KfnFYTE2VTx?= M3[z[pJm\HWlZYOgWHJRVTJiYXP0bZZifGmxbjDleoVvKGG2IHjp[4gh[2:wY3XueJJifGmxboOgc4YhUDKRMh?= MonLNlUyPzl3N{S=
GL37  MonSR4VtdCCYaXHibYxqfHliQYPzZZk> NXu0bnJxOC1zMNMgxtVO NVLLbFc4PDhiaB?= MkPRd5VxeHKnc4Pld{BN[SCneIDy[ZN{cW:w M36xTlI1QTl7NkW3
NRK-52E M2P5N2Z2dmO2aX;uJGF{e2G7 MYSxxsDDvU1? M{nIUlExKG2rbh?= M3vmc4Jtd2OtczD0bIUhe3SrbYXsZZRwenliZX\m[YN1KG:oIFHu[{BKUSCxbjDQZZguOiCneIDy[ZN{cW:wwrC= NWnRbpM5OjR5MUC0NlM>
NRK-52E M{SxWWZ2dmO2aX;uJGF{e2G7 MoDrNeKhyrWP NUPldZVMOTBibXnu M4PQRoJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> MmLlNlQ4OTB2MkO=
HSC  MVvGeY5kfGmxbjDBd5NigQ>? MnruNlAh|ryP NUOyRnBoOSCq Mo\HZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= M2rTUlI1PjF2MUm5
EJ M1zXVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLPOJc2OC96MDFOwG0> NHTLXm8zPC92OD:3NkBp NIfyRXNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Mor3NlQ2QDdyNEm=
EJ NEj2OlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fNS|UxNzhyIN88US=> M{[0OlQ5KGh? M4OwWYNifXOnczDTMZBp[XOnIHHydoV{fA>? M3n6NFI1PTh5MES5
EJ M4PtO2Z2dmO2aX;uJGF{e2G7 MmnaOVAwQDBizszN NITWXnA1QCCq NI\LbY1ld3ewcnXneYxifGW|IHOtUZlkNCCleXPsbY5FOSxic4Xyeol3cW5iYX7kJHZGT0ZiZYjwdoV{e2mxboO= MkiwNlQ2QDdyNEm=
HepG2 NHvqV5RHfW6ldHnvckBCe3OjeR?= NWn1TJJ4PTBvNUCwJO69VQ>? NH;CR|k3OMLibXnu NFTWdZlqdmirYnn0d{B1cGViSVytOk1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTCoWJlzPzB3KTDhcoQhW1SDVEOgLHR6ejdyNTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NX3ufm5XOjR{NEKwOFY>
SGC7901 Mny0R4VtdCCYaXHibYxqfHliQYPzZZk> NH;6SWYxNTFyMDFOwG0> MWOyOE81QC95MjDo MXfjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= MXeyOFE2OTJ3NR?=
AGS  NWWzOXozS2WubDDWbYFjcWyrdImgRZN{[Xl? MlKzNE0yODBizszN M4TaXVI1NzR6L{eyJIg> MkXLZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 MlTiNlQyPTF{NUW=
SGC7901 NF61WlFHfW6ldHnvckBCe3OjeR?= NULtco9{PTBizszN M1rub|I1NzR6L{eyJIg> M2XmNZRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg MljtNlQyPTF{NUW=
AGS  NHPycWJHfW6ldHnvckBCe3OjeR?= MoT3OVAh|ryP M1TTV|I1NzR6L{eyJIg> NHPaUVB1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> M4DlWVI1OTVzMkW1
SGC7901 M1jqWWZ2dmO2aX;uJGF{e2G7 MnG4OVAh|ryP NFi4bWwzPC92OD:3NkBp M4nrRpRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz MkDYNlQyPTF{NUW=
AGS  MYLGeY5kfGmxbjDBd5NigQ>? MnjuOVAh|ryP NXXRe45sOjRxNEivO|IhcA>? NFPnTZN1cGViY4n0c5Bt[XOvaXOgcI9k[WyrenH0bY9vKG:oIIDKRWszKCiMQVuyJJBpd3OyaH;yfYxifGWmIHH0JJJme2mmdXXzJHR6ejFyMEegZY5lKFS7ckGwNFgqKGSnY4LlZZNm\CCjZoTldkBCTzR7MDD0doVifG2nboSg[o9zKDJ2IHHu[EA1QCCqcjygZpV1KHO2YYL0[YQhfG9icnXic5Vv\CCjdDC3NkBpeg>? MVqyOFE2OTJ3NR?=
MC3T3-E1  MW\GeY5kfGmxbjDBd5NigQ>? NEK5WWY2OCEQvF2= MlXWOEBp NELmdXRqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> NHr4OlczOzh5N{ezOC=>
7TD1-DXM MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7CNVAh|ryP MkLYO|IhcA>? M3TwbWROW09? MXvpcohq[mm2czDj[YxtKGe{b4f0bC=> MWWyN|g4OTF3OR?=
7TD1-WD-90 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DsblExKM7:TR?= MmLNO|IhcA>? MWPEUXNQ NXHzfIducW6qaXLpeJMh[2WubDDndo94fGh? NVjVO5J[OjN6N{GxOVk>
7TD1-DXM NV23clRjSXCxcITvd4l{KEG|c3H5 M{n6b|UxKM7:TR?= MV20PEBp MVjEUXNQ MXzpcoR2[2W|IHHwc5B1d3Orcx?= MYeyN|g4OTF3OR?=
7TD1-WD-90 NVLOWlE{SXCxcITvd4l{KEG|c3H5 NUDYPZRoPTBizszN MXu0PEBp NHO2XnpFVVOR NH\3PGdqdmS3Y3XzJIFxd3C2b4Ppdy=> M{LjbFI{QDdzMUW5
7TD1-WD-90  M2jPXGZ2dmO2aX;uJGF{e2G7 NEXHcVg2OCEQvF2= NHXo[JU3KGh? NUfhNI9UTE2VTx?= NUTQd|N5e2mpbnnmbYNidnSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEqDS{KgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNy=> MXGyN|g4OTF3OR?=
HepG2  MWLGeY5kfGmxbjDBd5NigQ>? MoTONVAxKM7:TR?= M4fORVEzNzJ2IHi= NVjlV4ltcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:w MUWyN|g{PjRyMB?=
RAW264.7  NIXhU4lHfW6ldHnvckBCe3OjeR?= MX61NOKh|ryPwrC= M4D0WlI1NzR6IHi= NWL5T|JMe3WycILld5NmeyCUQV7LUE1qdmS3Y3XkJI9{fGWxY3zhd5Rw\2WwZYPpdy=> M{XjTlI{PjZ3MEG4
RAW264.7 NUDDRnJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMVUxyqEQvF5CpC=> NECyN5Q1QMLiaB?= M1zzU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wt[IVx\W6mZX70cJk> NVfRUVB2OjN4NkWwNVg>
RAW264.7 M{PYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIO1XnExNTVywrFOwG3DqA>? M3Wzc|Q5yqCq MkXjZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= NGTSV4MzOzZ4NUCxPC=>
RAW264.7 NFTvTpBHfW6ldHnvckBCe3OjeR?= NFzweIU2OMLizszN MkXnNlQwPDhiaB?= M4rySIlvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? NWqz[ohPOjN4NkWwNVg>
A549  MoTKSpVv[3Srb36gRZN{[Xl? NV7BRXY2OjBxNECg{txO M3\zdFIxKGh? NWPK[|JWOjBizszNJGFIPDlyIIP1dJBz\XO|ZYOgeIhmKHKjZHnheIlwdi2rbnT1Z4VlKGmwdnHzbY9vKG:oIFG1OFkh[2WubIO= NF7kbWQzOzZ{MEG5NS=>
A549  NHHjbZBHfW6ldHnvckBCe3OjeR?= M3z6fVExNzJyL{SwJO69VQ>? NV;0VW9bOjRiaB?= M{LGZpN2eHC{ZYPz[ZMhfGinIILh[IlifGmxbj3pcoR2[2WmIHXs[ZZifGmxbjDv[kBXTUeIwrC= NVOxfW9GOjN4MkCxPVE>
HUVECs MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXGyNEDDvU1? NXfQTlBoPCCq NXXjVVNU[XS2ZX71ZZRmeyCKMl:yMYlv\HWlZXSgZ4VtdCC|aILpcoti\2ViYX7kJIlueHKxdnXkJJRp\SCjdIThZ4hu\W62IILheIUhd2ZidHjlJINmdGy| NVr2Z5lROjN2OEO5OFY>
HUVECs M2ftRWFxd3C2b4Ppd{BCe3OjeR?= NVTKcFVNOjBiwsXN M1i1e|QhcA>? NYTFUXBOe2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 NIj3XoUzOzR6M{m0Oi=>
BV-2  Mn\OSpVv[3Srb36gRZN{[Xl? MXyyNEDDvU1? M{XvXVE3KGh? MUjpcohq[mm2czDMVHMucW6mdXPl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBidG2xc4SgZ49ueGyndHXsfUBlcW2rbnnzbIVlKGmQT2Og[ZhxemW|c3nvci=> M2ThdlI{OjN4M{ew
NRK-52E  MWXGeY5kfGmxbjDBd5NigQ>? MX:1xsDPxE1? NIfLR4s{OMLibXnu M1zlN4F1fGWwdXH0[ZMhSW6pLTix5qCUPylvaX7obYJqfGWmIGTHSk3PujFibWLORUBifCBzNtMgbOKh M3i1S|I{OTd2N{W3
SW620  Moq0SpVv[3Srb36gRZN{[Xl? Ml\HNlAhyrWP MlvpNU83KGh? NG\4b4dqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> MnfZNlMyOTB4MkW=
RPE  M1T6XmZ2dmO2aX;uJGF{e2G7 MlLVN|AhyrWPwrC= MX[zJIg> M{LNcIlvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u NXHLZY1QOjNyOUSwOlc>
SW1116 NUDVcYVTTnWwY4Tpc44hSXO|YYm= NIXXXoQyODBiwsXNxsA> MYGyOE81QC95MjDo M1\DboRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBLSUt{IHHu[EBxUkGNMjD0bY1mNWSncHXu[IVvfGy7 NIr4fXYzOjB3MEe5NC=>
HT29 NVm3eog{TnWwY4Tpc44hSXO|YYm= NFy3NpoyODBiwsXNxsA> MlPGNlQwPDhxN{KgbC=> M4LPXoRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBLSUt{IHHu[EBxUkGNMjD0bY1mNWSncHXu[IVvfGy7 NVzucFNLOjJyNUC3PVA>
SW1116 MoDzSpVv[3Srb36gRZN{[Xl? NYDpNpNQOTByINM1UeKh NInkSZQzPC92OD:3NkBp MXrk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> M4TZeFIzODVyN{mw
HT29 MUDGeY5kfGmxbjDBd5NigQ>? NY\kSmlXOTByINM1UeKh MX2yOE81QC95MjDo NX\oPFV{\GWlcnXhd4V{KHSqZTDwV3RCXDNibHX2[Yx{KGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? MlPjNlIxPTB5OUC=
ARPE-19 NFvOfIRHfW6ldHnvckBCe3OjeR?= MVS1xsDPxE1? NX60fpR6OzEEoH3pci=> MmW3bY5pcWKrdIOgTmFMOiCyaH;zdIhwemmuYYTpc44> Mn7yNlE3OjB7NkO=
HSC-T6 M2fnWWFxd3C2b4Ppd{BCe3OjeR?= NWOxcoFvOTEEoN88US=> NUPrTlRMOsLiaNMg NFzJRYZqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> MnPsNlE{QTZ7OUi=
HSC-T6 NHHPR2dHfW6ldHnvckBCe3OjeR?= M3LQUFExyqEQvF2= NUnlbmJDOsLiaNMg M13WS4lvcGmkaYTzJJRp\SCneIDy[ZN{cW:wczDv[kBxYS2VVFHUNUBidmRiQnHkJIlv\HWlZXSgZpkhS0SH M2e4T|IyOzl4OUm4
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MZ-304 NXLudmFpTnWwY4Tpc44hSXO|YYm= M2nSclUxNzFyMNMg{txO MmHXOFghcA>? MUnpcohq[mm2czDtbYdz[XSrb36= M161fVIxPTh7NUK1
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A-172 MX\GeY5kfGmxbjDBd5NigQ>? M3rKOVUxNzFyMNMg{txO NVXVOJplPDhiaB?= NWfJ[pdwemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? MkPCNlA2QDl3MkW=
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THP1 NIPNXG1HfW6ldHnvckBCe3OjeR?= Mn;2NVAhfU1? MmXPN|AhdWmwwrC= MoDYbY5pcWKrdIOgV3RCXDNidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGK7IH;2[ZIhPjBn MmfWNlA{QTN4OUC=
BMMC NGizT5ZHfW6ldHnvckBCe3OjeR?= M3PyXlAuOTBizszN M3Oz[|E2yqCvaX6= NUToeFU{cW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? NGrscmQyQTh|NUi0OS=>
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OVCAR-3 MXzGeY5kfGmxbjDBd5NigQ>? Mmf6NVAhfU1? MVmxJIg> M33lU4lvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 MU[xPVY1PzN4Mx?=
PA-1 NVnCVXd{TnWwY4Tpc44hSXO|YYm= NHL6eo8yOCC3TR?= MWmxJIg> MkH1bY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? M1[3eVE6PjR5M{[z
Jurkat  NHftbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHO[2M2OCEQvF2= M2DUUFI1NzR6L{eyJIg> M1r2U4VvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> NUW4boJKOTl3NkS4PVE>
SUPT1  MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofCOVAh|ryP MkDMNlQwPDhxN{KgbC=> MYHlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NF\xZ4wyQTV4NEi5NS=>
Jurkat  MXvBdI9xfG:|aYOgRZN{[Xl? NF\EWm42OCEQvF2= NIj3bIIzPC92ODDo M1HtZ4VvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBieG:ydH;zbZM> MXuxPVU3PDh7MR?=
SUPT1  MUPBdI9xfG:|aYOgRZN{[Xl? MlP0OVAh|ryP NIHHdG8zPC92ODDo NGHX[otmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ NHSyeY0yQTV4NEi5NS=>

... 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