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

  • 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.

  • 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.

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 NYT3PVV3TnWwY4Tpc44hSXO|YYm= M4S0[FExOOLCidM1US=> M1vQN|I1KGh? Ml\IcYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz MoLLNlYyQDR7OUm=
BCBL1 MYHGeY5kfGmxbjDBd5NigQ>? NVrjO4xKOTBy4pEJxtVO M3;GU|I1KGh? MUft[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= Mmi3NlYyQDR7OUm=
BC3 NFnmXJRHfW6ldHnvckBCe3OjeR?= MXixNFDjiIoEtV2= NEP5VYQzPCCq M2nXc41m\GmjdHXzJIRmNXCqb4PwbI9zgWyjdHnvckBw\iCVVFHUN{Bkd3K{ZXzheIVlKHerdHigTHNRPzBiYX7kJGhUTjFicnXkeYN1cW:w NI[5UWkzPjF6NEm5PS=>
BCBL1 MUXGeY5kfGmxbjDBd5NigQ>? NXLET5BTOTBy4pEJxtVO NWLkZoxTOjRiaB?= MnXycYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOiC{ZXT1Z5Rqd25? NYrrZ4FjOjZzOES5PVk>
BC3 Mor2SpVv[3Srb36gRZN{[Xl? M1faZlExOOLCidM1US=> MofGNlQhcA>? MWHpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= NIfVN|QzPjF6NEm5PS=>
BCBL1 NGfqZppHfW6ldHnvckBCe3OjeR?= NYHYRo5IOTBy4pEJxtVO NH;XW2IzPCCq MkG5bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg M3;KWFI3OTh2OUm5
SK-MEL-28 MVTGeY5kfGmxbjDBd5NigQ>? M4jt[|UxNzFyMPMAjeK2VQ>? NYLueWl6PDhiaB?= MVnEUXNQ Mnq1doVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NHPQW2ozPTJzNkWyNi=>
MeWo MXLGeY5kfGmxbjDBd5NigQ>? M4\sfVUxNzFyMPMAjeK2VQ>? NXK0doR4PDhiaB?= NWK2fmUxTE2VTx?= NXfQVXBZemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MmPLNlUzOTZ3MkK=
SK-MEL-5 NYf2Om5nTnWwY4Tpc44hSXO|YYm= MVm1NE8yODEkgJpCuW0> M1fWfVQ5KGh? NX6ySWJTTE2VTx?= M3XDRpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl MYmyOVIyPjV{Mh?=
SK-MEL-2 Ml\XSpVv[3Srb36gRZN{[Xl? Mn\BOVAwOTBy4pEJxtVO MlTXOFghcA>? M3\t[2ROW09? MoTwdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= M2XWflI2OjF4NUKy
B16-F0 M3jwOmZ2dmO2aX;uJGF{e2G7 NWDU[5dxPTBxMUCw5qCKyrWP MkDiOFghcA>? M2HsXGROW09? M1m4OpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M2ewSVI2OjF4NUKy
TRPM2/HEK  MUfGeY5kfGmxbjDBd5NigQ>? M3HPOFAvOeLCk{K1xsDDvU1? MkT2NVXDqG2rbh?= MkPaSG1UVw>? NUHJWIwyemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCxMlfDqML3TR?= NIO0TFIzPTF5OUW3OC=>
U937  NF\xcYdHfW6ldHnvckBCe3OjeR?= MlLDNE4y6oDVMkZCpOK2VQ>? MWmxOeKhdWmw M1TKOWROW09? Mn;1doVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? NGrhRVQzPTF5OUW3OC=>
TRPM2/HEK  NXfFXllYTnWwY4Tpc44hSXO|YYm= NU[4WndTOTEEoNM1US=> NFTucXc1OMLibXnu M17MeWROW09? MkLSdoVlfWOnczDUVnBOOiCjY4TpeoF1cW:wIHX2[Y4h[XRiaHnnbEBkd26lZX70doF1cW:wczDv[kBJOk9{ MmS5NlUyPzl3N{S=
GL37  NF36Nm5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{nROFAuOTEEoNM1US=> NIHMdYY1QCCq MXrzeZBxemW|c3XzJGxiKGW6cILld5Nqd25? MorsNlQ6QTl4NUe=
NRK-52E M{DxfWZ2dmO2aX;uJGF{e2G7 NGXQW|IyyqEEtV2= M1K4c|ExKG2rbh?= MWricI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi M2nxUVI1PzFyNEKz
NRK-52E M3zDXGZ2dmO2aX;uJGF{e2G7 MUmxxsDDvU1? M3fh[|ExKG2rbh?= Mm\GZoxw[2u|IFHu[{BKUSCrbnT1Z4VlKEOGMkSg[ZhxemW|c3nvci=> MUOyOFcyODR{Mx?=
HSC  M4npcGZ2dmO2aX;uJGF{e2G7 M1HKZVIxKM7:TR?= MUSxJIg> NYnpVJVD[WK{b3fheIV{KHSqZTDkbYZn\XKnboTpZYwh\W[oZXP0d{Bw\iCuZYD0bY4hd3JiQVfFdy=> MYiyOFYyPDF7OR?=
EJ MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlW0OVAwQDBizszN NHvUZY8zPC92OD:3NkBp NYrTdYNmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MX6yOFU5PzB2OR?=
EJ MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnDZlA2OC96MDFOwG0> NXvLdoVyPDhiaB?= MoXOZ4F2e2W|IGOtdIhie2ViYYLy[ZN1 NIDrUGczPDV6N{C0PS=>
EJ MVrGeY5kfGmxbjDBd5NigQ>? Ml;YOVAwQDBizszN NVqx[VVPPDhiaB?= MV7kc5dvemWpdXzheIV{KGNvTYnjMEBkgWOuaX7ENUwhe3W{dnn2bY4h[W6mIG\FS2Yh\XiycnXzd4lwdnN? NXnmVHZyOjR3OEewOFk>
HepG2 MVHGeY5kfGmxbjDBd5NigQ>? MmLoOVAuPTByIN88US=> MYS2NOKhdWmw M4i3ZYlvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MYGyOFI1OjB2Nh?=
SGC7901 NFj2VXJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHvGeW4xNTFyMDFOwG0> NXzNS5lGOjRxNEivO|IhcA>? M3ntU4NifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> M{XBWVI1OTVzMkW1
AGS  NELEUIhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2\PS|AuOTByIN88US=> M2LYbVI1NzR6L{eyJIg> M2jGT4NifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> NIW0SWszPDF3MUK1OS=>
SGC7901 MVHGeY5kfGmxbjDBd5NigQ>? NHX2R2c2OCEQvF2= NX\5UlJlOjRxNEivO|IhcA>? MVf0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= NEL1OYMzPDF3MUK1OS=>
AGS  M3vscmZ2dmO2aX;uJGF{e2G7 NYXXOXRjPTBizszN MVSyOE81QC95MjDo MlXDeIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= NVHybHdCOjRzNUGyOVU>
SGC7901 M2rCPGZ2dmO2aX;uJGF{e2G7 NYTvRmREPTBizszN MoPRNlQwPDhxN{KgbC=> NVLMS4hCfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? M1fEOVI1OTVzMkW1
AGS  NV;PW3RrTnWwY4Tpc44hSXO|YYm= NEXGcmQ2OCEQvF2= MWWyOE81QC95MjDo M{DJdpRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz NXqyc5hmOjRzNUGyOVU>
MC3T3-E1  MnOxSpVv[3Srb36gRZN{[Xl? MXy1NEDPxE1? NUjJW2h1PCCq MWTpcohq[mm2czDIV2UucW6mdXPl[EBDVVB5IHHu[EBIUFJicILveIVqdiCneIDy[ZN{cW:wwrC= MX6yN|g4Pzd|NB?=
7TD1-DXM M{HKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYixNEDPxE1? M{HrUlczKGh? MWTEUXNQ NHHBPFJqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWKyN|g4OTF3OR?=
7TD1-WD-90 M1qxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfPS4JyOTBizszN NXfEV4NLPzJiaB?= NUnmWo9UTE2VTx?= M1vwNolvcGmkaYTzJINmdGxiZ4Lve5Rp MkLXNlM5PzFzNUm=
7TD1-DXM MWHBdI9xfG:|aYOgRZN{[Xl? NFrncno2OCEQvF2= NVjURWNoPDhiaB?= NVv6bmJRTE2VTx?= M1vxSYlv\HWlZYOgZZBweHSxc3nz NWnzWlRPOjN6N{GxOVk>
7TD1-WD-90 NXnaWlU1SXCxcITvd4l{KEG|c3H5 NHLLSXc2OCEQvF2= NYjRfWZ[PDhiaB?= NV7WS3VKTE2VTx?= NVPkN3ZEcW6mdXPld{BieG:ydH;zbZM> MnzZNlM5PzFzNUm=
7TD1-WD-90  M{PMOGZ2dmO2aX;uJGF{e2G7 NFn4XWw2OCEQvF2= Mk\mOkBp MlXXSG1UVw>? NX7McY5Ue2mpbnnmbYNidnSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEqDS{KgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNy=> NF;ibWUzOzh5MUG1PS=>
HepG2  NXjCd|NDTnWwY4Tpc44hSXO|YYm= NFG5ZmgyODBizszN MXyxNk8zPCCq NYKye3pNcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:w M3:3NVI{QDN4NECw
RAW264.7  NVnzTHZ5TnWwY4Tpc44hSXO|YYm= NGPub2s2OMLizszNxsA> MXyyOE81QCCq MUXzeZBxemW|c3XzJHJCVkuOLXnu[JVk\WRib4P0[Y9kdGG|dH;n[Y5me2m| NYPMb|JLOjN4NkWwNVg>
RAW264.7 NWTUZWVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\xSm9nOC13MNMg{txOyqB? NEnqdI81QMLiaB?= MYTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnLXTldIVv\GWwdHz5 MV2yN|Y3PTBzOB?=
RAW264.7 NF[y[|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzwNE02OMLizszNxsA> MkfWOFjDqGh? MmHzZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= NY[2Vm8{OjN4NkWwNVg>
RAW264.7 NWPOT4VqTnWwY4Tpc44hSXO|YYm= MYS1NOKh|ryP NVPOSWZVOjRxNEigbC=> M2C4UolvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? M2K3dVI{PjZ3MEG4
A549  NH;MW29HfW6ldHnvckBCe3OjeR?= NVThUGVpOjBxNECg{txO NYKwflJWOjBiaB?= M2DwWlIxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| MmPFNlM3OjBzOUG=
A549  MYjGeY5kfGmxbjDBd5NigQ>? NHv2SG0yOC9{MD:0NEDPxE1? NVvtbmtIOjRiaB?= Mke3d5VxeHKnc4Pld{B1cGVicnHkbYF1cW:wLXnu[JVk\WRiZXzleoF1cW:wIH;mJHZGT0cEoB?= NGPBO4MzOzZ{MEG5NS=>
HUVECs NGDsNJJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2XITlIxKML3TR?= MWG0JIg> M13MUYF1fGWwdXH0[ZMhUDKRMj3pcoR2[2WmIHPlcIwhe2i{aX7rZYdmKGGwZDDpcZBzd3[nZDD0bIUh[XS2YXPocYVvfCC{YYTlJI9nKHSqZTDj[Yxtew>? MVeyN|Q5Ozl2Nh?=
HUVECs NFXKbphCeG:ydH;zbZMhSXO|YYm= NXPjUllKOjBiwsXN NXLIS|kyPCCq Ml7Ld4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJINmdGxiYYDvdJRwfGmlIHnu[IV5 Mo\wNlM1QDN7NE[=
BV-2  MnrZSpVv[3Srb36gRZN{[Xl? NFXaN3czOCEEtV2= NEDOOlEyPiCq MlTjbY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> MmnVNlMzOzZ|N{C=
NRK-52E  M33NbWZ2dmO2aX;uJGF{e2G7 M2HoelXDqM7:TR?= NHHqcms{OMLibXnu MWnheJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> NInrTZYzOzF5NEe1Oy=>
SW620  MnzNSpVv[3Srb36gRZN{[Xl? MlyxNlAhyrWP MnmyNU83KGh? M1nNfYlvcGmkaYTzJJAuW1SDVEOgZYN1cX[jdHnvci=> NWjhUZNKOjNzMUC2NlU>
RPE  NUHYb3JqTnWwY4Tpc44hSXO|YYm= M4[0Z|MxKML3TdMg MmPEN{Bp Mm\CbY5pcWKrdIOgeIhmKGmwZIXjeIlwdiCxZjDwMXNVSVR|IHX4dJJme3Orb36= MmPtNlMxQTRyNke=
SW1116 NITGSlRHfW6ldHnvckBCe3OjeR?= MmO2NVAxKML3TdMg NWS2SXF6OjRxNEivO|IhcA>? NWTLWnEx\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= M{\jcFIzODVyN{mw
HT29 M2LVXGZ2dmO2aX;uJGF{e2G7 NVGwV5N7OTByINM1UeKh MoH4NlQwPDhxN{KgbC=> NET6WFVl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= NEjjO3ozOjB3MEe5NC=>
SW1116 M1SyfWZ2dmO2aX;uJGF{e2G7 M3rP[|ExOCEEtV5CpC=> NXOyZ2c4OjRxNEivO|IhcA>? M4TaV4Rm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh MXGyNlA2ODd7MB?=
HT29 M2jYOWZ2dmO2aX;uJGF{e2G7 M2TPSFExOCEEtV5CpC=> NWnPe|dPOjRxNEivO|IhcA>? MV3k[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> MoTwNlIxPTB5OUC=
ARPE-19 NET2NIJHfW6ldHnvckBCe3OjeR?= NUDRWYI6PcLizszN MWqzNOKhdWmw Mo[xbY5pcWKrdIOgTmFMOiCyaH;zdIhwemmuYYTpc44> NVj2bW81OjF4MkC5OlM>
HSC-T6 MWnBdI9xfG:|aYOgRZN{[Xl? M{fCZVExyqEQvF2= NGjhO4szyqCqwrC= M4DX[olvcGmkaYTzJJRp\SCjcH;weI9{cXNib3[gTHNENVR4IHPlcIx{KGmwZIXj[YQh[nliQ1TF MWqyNVM6Pjl7OB?=
HSC-T6 NX;SUoZoTnWwY4Tpc44hSXO|YYm= NF7IPW8yOMLizszN NVn2WHBFOsLiaNMg NGfUcpFqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= M2LKeFIyOzl4OUm4
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A-172 M{e3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{niVFUxNzFyMNMg{txO MYS0PEBp NWewNFA4dGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo NHjmdFUzODV6OUWyOS=>
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MZ-256 MmrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV35VoY{PTBxMUCwxsDPxE1? M4n4T|Q5KGh? NXruWVdtdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo Mk[1NlA2QDl3MkW=
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A-172 M1\lU2Z2dmO2aX;uJGF{e2G7 MnTSOVAwOTBywrFOwG0> MXm0PEBp NEG5ZY1qdmirYnn0d{BucWe{YYTpc44> MVKyNFU5QTV{NR?=
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MZ-54 NWrvOGpjTnWwY4Tpc44hSXO|YYm= M2DGd|UxNzFyMNMg{txO M2jO[FQ5KGh? MnfKbY5pcWKrdIOgcYloemG2aX;u MVKyNFU5QTV{NR?=
MZ-256 MlW5SpVv[3Srb36gRZN{[Xl? NXPkW25FPTBxMUCwxsDPxE1? NU\DfnAzPDhiaB?= M13W[olvcGmkaYTzJI1q\3KjdHnvci=> MlvyNlA2QDl3MkW=
MZ-304 NV\NO5pYTnWwY4Tpc44hSXO|YYm= M{PGelUxNzFyMNMg{txO NFvLcGw1QCCq NUHKTWZzcW6qaXLpeJMhdWmpcnH0bY9v NEToTIEzODV6OUWyOS=>
A-172 MULGeY5kfGmxbjDBd5NigQ>? M17EeVExOMLizszN MUC0PEBp NEjyVnJqdmirYnn0d{Bqdn[jc3nvci=> NFjTNWgzODV6OUWyOS=>
MZ-18 MVLGeY5kfGmxbjDBd5NigQ>? MmrmNVAxyqEQvF2= M2rFN|Q5KGh? NEPlb2lqdmirYnn0d{Bqdn[jc3nvci=> MnnENlA2QDl3MkW=
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A-172 M4LkbWZ2dmO2aX;uJGF{e2G7 NUD3N5IyPTBxMUCwxsDPxE1? M4fqeFQ5KGh? MWfy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz MVqyNFU5QTV{NR?=
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SW1990 MV\GeY5kfGmxbjDBd5NigQ>? M2Twd|IxKM7:TR?= NVvDRnc3OjRiaB?= MW\k[YNz\WG|ZYOgeIhmKGmwdHXud4l1gSCxZjDwMXN1[XR|IHX4dJJme3Orb36= M{\jTVIxPDh{OEW4
SW1990 NYK3U3dLUW64YYPpc44hSXO|YYm= NVGxUosxOjBizszN MontNlQhcA>? MojEdoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= NV3yeFRbOjB2OEK4OVg>
THP1 M{T6PWZ2dmO2aX;uJGF{e2G7 NHHo[YEyOCC3TR?= M4\Zc|MxKG2rbtMg NILFWZBqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= MVKyNFM6OzZ7MB?=
BMMC NEPOd49HfW6ldHnvckBCe3OjeR?= M2W5flAuOTBizszN NFTL[VEyPcLibXnu MmHDbY5pcWKrdIOgUHREPMLicnXs[YF{\SCrbjDhJIRwe2VvZHXw[Y5l\W62IH\hd4hqd25id3n0bEBv\WG{IHPvcZBt\XSnIHnubIljcXSrb36gZZQh[2:wY3XueJJifGmxboOg5sm,OTEEoN88US=> NH;zSIEyQTh|NUi0OS=>
A549 MWHGeY5kfGmxbjDBd5NigQ>? MofuNVUh|ryv MoLoNUBp NEm4S3hqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQyKG:wIIT5do9{cW6nIEewNUB4[XNiZHX0[YN1\WRiMUWgcYlvKGGodHXyJHNRTSCEIITy[YF1dWWwdB?= MoizNVk5ODF4NkW=
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OVCAR-3 NW\BU21STnWwY4Tpc44hSXO|YYm= M4jhc|ExKHWP MU[xJIg> MnXxbY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? M3XRXlE6PjR5M{[z
PA-1 MofQSpVv[3Srb36gRZN{[Xl? M{P6ZlExKHWP NI\aTHUyKGh? MlvkbY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? NYr6NWsyOTl4NEezOlM>
Jurkat  NI\pPZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;DV3I2OCEQvF2= Ml;nNlQwPDhxN{KgbC=> NHGzV4lmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NGe3dlQyQTV4NEi5NS=>
SUPT1  NYjDfJpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHlTVNWPTBizszN MYGyOE81QC95MjDo MVXlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NFzqU4YyQTV4NEi5NS=>
Jurkat  NVjSOItMSXCxcITvd4l{KEG|c3H5 NIG5XVY2OCEQvF2= MoLqNlQwPDhiaB?= NGrsVoxmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MkfkNVk2PjR6OUG=
SUPT1  M2foSGFxd3C2b4Ppd{BCe3OjeR?= MkjaOVAh|ryP MmXJNlQwPDhiaB?= MXHlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz NGXmeG0yQTV4NEi5NS=>

... 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.

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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