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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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 MoGxSpVv[3Srb36gRZN{[Xl? M2fmR|ExOOLCidM1US=> NGD5UlczPCCq MXrt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= MlzzNlYyQDR7OUm=
BCBL1 M{XKZWZ2dmO2aX;uJGF{e2G7 MlzYNVAx6oDLwsXN MnfWNlQhcA>? NEDG[3Fu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NYiwTmZWOjZzOES5PVk>
BC3 M1rON2Z2dmO2aX;uJGF{e2G7 NXy5U3U1OTBy4pEJxtVO NGXRU28zPCCq NF61cGFu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0ZzIILl[JVkfGmxbh?= Ml\sNlYyQDR7OUm=
BCBL1 MWDGeY5kfGmxbjDBd5NigQ>? NYHwflZNOTBy4pEJxtVO MlXoNlQhcA>? MX;t[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? M3LEOFI3OTh2OUm5
BC3 MXHGeY5kfGmxbjDBd5NigQ>? NFPrSVcyODEkgJpCuW0> MnzWNlQhcA>? MlW5bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NVrLVZJIOjZzOES5PVk>
BCBL1 MVjGeY5kfGmxbjDBd5NigQ>? NYT0S49XOTBy4pEJxtVO NYr3bFBjOjRiaB?= MX7pcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= NX6zOoQ4OjZzOES5PVk>
SK-MEL-28 NWT4fWJUTnWwY4Tpc44hSXO|YYm= NImyVHQ2OC9zMEFihKnDvU1? MWi0PEBp M3vl[2ROW09? MmjvdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= MoSzNlUzOTZ3MkK=
MeWo M2rKRmZ2dmO2aX;uJGF{e2G7 M1r2UVUxNzFyMPMAjeK2VQ>? NF\zd4Q1QCCq M{TjTmROW09? M4LobpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl MU[yOVIyPjV{Mh?=
SK-MEL-5 MUXGeY5kfGmxbjDBd5NigQ>? M1jzNVUxNzFyMPMAjeK2VQ>? MUC0PEBp M3;ocmROW09? NHPoW|Fz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> M3HSUVI2OjF4NUKy
SK-MEL-2 NE\peoVHfW6ldHnvckBCe3OjeR?= Mof3OVAwOTBy4pEJxtVO NVLs[2gyPDhiaB?= M2\HdmROW09? NInhdmpz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> Ml\RNlUzOTZ3MkK=
B16-F0 NUjFWYN4TnWwY4Tpc44hSXO|YYm= M3Tk[FUxNzFyMPMAjeK2VQ>? MmPpOFghcA>? M{\NPGROW09? Mn3ydoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NULES3hkOjV{MU[1NlI>
TRPM2/HEK  MmDDSpVv[3Srb36gRZN{[Xl? MkC0NE4y6oDVMkZCpOK2VQ>? MV[xOeKhdWmw NVvEU3d{TE2VTx?= NXTUNm92emWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCxMlfDqML3TR?= M1juRVI2OTd7NUe0
U937  MkTxSpVv[3Srb36gRZN{[Xl? NI[xXZMxNjIkgKOyOeKhyrWP MU[xOeKhdWmw M{DNNWROW09? M3rPOpJm\HWlZYOgTFJQOi2rbnT1Z4VlKEOjMjvpcoNz\WG|ZTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjygZY5lKHSqZTDJR|UxyqC4YXz1[UB4[XNiMD60xsDDvU1? MlHSNlUyPzl3N{S=
TRPM2/HEK  M3XheGZ2dmO2aX;uJGF{e2G7 M2jlclExyqEEtV2= NY[0VZI4PDEEoH3pci=> NF;zbnhFVVOR NXHTdY5CemWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y MVWyOVE4QTV5NB?=
GL37  MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXH5c482OC1zMNMgxtVO M2PUSlQ5KGh? NWP4RXVGe3WycILld5NmeyCOYTDlfJBz\XO|aX;u NEXLW48zPDl7OU[1Oy=>
NRK-52E M3[3XWZ2dmO2aX;uJGF{e2G7 MnjqNeKhyrWP MYqxNEBucW5? MVHicI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi M1;YblI1PzFyNEKz
NRK-52E NEXxPGlHfW6ldHnvckBCe3OjeR?= MWmxxsDDvU1? MUWxNEBucW5? NXfwO4Fb[myxY3vzJGFv\yCLSTDpcoR2[2WmIFPENlQh\XiycnXzd4lwdg>? NUPYbXRbOjR5MUC0NlM>
HSC  MV\GeY5kfGmxbjDBd5NigQ>? NGnId2czOCEQvF2= NH\6dIEyKGh? MVrhZpJw\2G2ZYOgeIhmKGSrZn\ldoVvfGmjbDDl[oZm[3S|IH;mJIxmeHSrbjDvdkBCT0W| MWmyOFYyPDF7OR?=
EJ Ml7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXq1NE85OCEQvF2= M2H6flI1NzR6L{eyJIg> M4PwXYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NGDsOFYzPDV6N{C0PS=>
EJ MlnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvJOVAwQDBizszN M4TFclQ5KGh? Mm\jZ4F2e2W|IGOtdIhie2ViYYLy[ZN1 NV[xOHVOOjR3OEewOFk>
EJ NXHnfmdDTnWwY4Tpc44hSXO|YYm= MoPvOVAwQDBizszN NIjre2w1QCCq NXzCfZl1\G:5boLl[5Vt[XSnczDjMW16[yxiY4njcIlvTDFuIIP1dpZqfmmwIHHu[EBXTUeIIHX4dJJme3Orb37z NH;3ZnMzPDV6N{C0PS=>
HepG2 M175NWZ2dmO2aX;uJGF{e2G7 NWfmeYJ3PTBvNUCwJO69VQ>? NGrPTYo3OMLibXnu NXvkfItmcW6qaXLpeJMhfGinIFnMMVYucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEGgLHR6ejdyNTmgZY5lKFOWQWSzJEhVgXJ5MEWpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mn;RNlQzPDJyNE[=
SGC7901 MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVOwMVExOCEQvF2= NEHqZXYzPC92OD:3NkBp MoXGZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NGnERmgzPDF3MUK1OS=>
AGS  MoOzR4VtdCCYaXHibYxqfHliQYPzZZk> NU\TVHNXOC1zMECg{txO MlXYNlQwPDhxN{KgbC=> MYjjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= NVvPS45xOjRzNUGyOVU>
SGC7901 M3HZNmZ2dmO2aX;uJGF{e2G7 M3XHXVUxKM7:TR?= MUGyOE81QC95MjDo NG\s[XV1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> MVyyOFE2OTJ3NR?=
AGS  NV34cJNUTnWwY4Tpc44hSXO|YYm= MoW5OVAh|ryP MonHNlQwPDhxN{KgbC=> MoW0eIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= M3fsS|I1OTVzMkW1
SGC7901 NHX6V2NHfW6ldHnvckBCe3OjeR?= NF\yRlQ2OCEQvF2= M1LOcFI1NzR6L{eyJIg> MXH0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> NFi5OG8zPDF3MUK1OS=>
AGS  Mlz1SpVv[3Srb36gRZN{[Xl? NUTX[5JsPTBizszN MorQNlQwPDhxN{KgbC=> NV7mXIV5fGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? NHvsOHkzPDF3MUK1OS=>
MC3T3-E1  NH;YWGlHfW6ldHnvckBCe3OjeR?= MV:1NEDPxE1? Mof0OEBp NF\EPFJqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> NXSyXIVkOjN6N{e3N|Q>
7TD1-DXM MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ixVlExKM7:TR?= NEDKOHk4OiCq NELxemVFVVOR M3nGS4lvcGmkaYTzJINmdGxiZ4Lve5Rp NU\J[HRUOjN6N{GxOVk>
7TD1-WD-90 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNEDPxE1? NWnJT2E{PzJiaB?= NFrnR4pFVVOR Mo\SbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4TvU|I{QDdzMUW5
7TD1-DXM NHnybWZCeG:ydH;zbZMhSXO|YYm= Ml\MOVAh|ryP MUS0PEBp NULnWoJ7TE2VTx?= Mnn5bY5lfWOnczDhdI9xfG:|aYO= MV:yN|g4OTF3OR?=
7TD1-WD-90 NH;pT5pCeG:ydH;zbZMhSXO|YYm= NUX2c3dKPTBizszN M3LsdVQ5KGh? NY\acYlsTE2VTx?= M2DUV4lv\HWlZYOgZZBweHSxc3nz MoruNlM5PzFzNUm=
7TD1-WD-90  MoLBSpVv[3Srb36gRZN{[Xl? M4Oxd|UxKM7:TR?= M4\zW|YhcA>? MYLEUXNQ MmDKd4lodmmoaXPhcpRtgSCrbnjpZol1eyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGpCUzJiYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMx?= NGLieIozOzh5MUG1PS=>
HepG2  M{DpfmZ2dmO2aX;uJGF{e2G7 M1W5PFExOCEQvF2= NWPHZ2tYOTJxMkSgbC=> MUnpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MUWyN|g{PjRyMB?=
RAW264.7  NX3xd3c2TnWwY4Tpc44hSXO|YYm= Ml3IOVDDqM7:TdMg M2XIcVI1NzR6IHi= NITndm1{fXCycnXzd4V{KFKDTlvMMYlv\HWlZXSgc5N1\W:lbHHzeI9o\W6nc3nz NIHzU3kzOzZ4NUCxPC=>
RAW264.7 NFHhUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T4SFAuPTEEoN88UeKh MoW5OFjDqGh? NGDCb3hqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlMYRmeGWwZHXueIx6 NWLES3I3OjN4NkWwNVg>
RAW264.7 NHW5dYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;EVoExNTVywrFOwG3DqA>? NF2xRZk1QMLiaB?= NVLhR2oz[2G3c3XzJIFvKGG{cnXzeEBw\iCUQWeyOlQvPyClZXzsd{BifCC2aHWgS|AwTzFicHjhd4Uhd2ZidHjlJINmdGxiY4njcIU> NV7zOYhzOjN4NkWwNVg>
RAW264.7 NW\FRYhjTnWwY4Tpc44hSXO|YYm= NIP0bFE2OMLizszN M4HteVI1NzR6IHi= MlXmbY5pcWKrdIOgVmFPU0xvaX7keYNm\CCQRlHUZ|Eh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNmejd{N2PURXQ{ M1Thd|I{PjZ3MEG4
A549  M1rDWmZ2dmO2aX;uJGF{e2G7 NVTKenR5OjBxNECg{txO MU[yNEBp NEPRfXgzOCEQvF2gRWc1QTBic4XwdJJme3OnczD0bIUhemGmaXH0bY9vNWmwZIXj[YQhcW64YYPpc44hd2ZiQUW0PUBk\Wyucx?= NX6y[|BVOjN4MkCxPVE>
A549  MlLISpVv[3Srb36gRZN{[Xl? NIHoTmgyOC9{MD:0NEDPxE1? M1\m[FI1KGh? M3roTZN2eHC{ZYPz[ZMhfGinIILh[IlifGmxbj3pcoR2[2WmIHXs[ZZifGmxbjDv[kBXTUeIwrC= MWCyN|YzODF7MR?=
HUVECs NEOwS4tE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4H3U|IxKML3TR?= M4HO[FQhcA>? NXn3bpg4[XS2ZX71ZZRmeyCKMl:yMYlv\HWlZXSgZ4VtdCC|aILpcoti\2ViYX7kJIlueHKxdnXkJJRp\SCjdIThZ4hu\W62IILheIUhd2ZidHjlJINmdGy| NUfNNHNTOjN2OEO5OFY>
HUVECs M1nVVmFxd3C2b4Ppd{BCe3OjeR?= M4DxdFIxKML3TR?= NV\5boZbPCCq MoTxd4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJINmdGxiYYDvdJRwfGmlIHnu[IV5 NYnwdJNEOjN2OEO5OFY>
BV-2  M1PUO2Z2dmO2aX;uJGF{e2G7 M4jQdlIxKML3TR?= NHfBblEyPiCq NEfoeYpqdmirYnn0d{BNWFNvaX7keYNm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCjbH3vd5Qh[2:vcHzleIVtgSCmaX3pcol{cGWmIHnOU3Mh\XiycnXzd4lwdg>? M4\KbVI{OjN4M{ew
NRK-52E  NGjNWnNHfW6ldHnvckBCe3OjeR?= M13MflXDqM7:TR?= MmDTN|DDqG2rbh?= MoTGZZR1\W63YYTld{BCdmdvKEJihLM4MS2rbnjpZol1\WRiVFfGMe6zOSCvUl7BJIF1KDF4wrDoxsA> M2XpSVI{OTd2N{W3
SW620  NX3pNoxRTnWwY4Tpc44hSXO|YYm= Mn7uNlAhyrWP NETQe5gyNzZiaB?= MVvpcohq[mm2czDwMXNVSVR|IHHjeIl3[XSrb36= NVTQTo5sOjNzMUC2NlU>
RPE  MYfGeY5kfGmxbjDBd5NigQ>? NVzOTHdkOzBiwsXNxsA> NHjDW5k{KGh? M3vxUolvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u MX6yN|A6PDB4Nx?=
SW1116 NGe0b5lHfW6ldHnvckBCe3OjeR?= MYixNFAhyrWPwrC= NXLRUoduOjRxNEivO|IhcA>? NYqwcYdM\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= NHfqO3MzOjB3MEe5NC=>
HT29 Ml3LSpVv[3Srb36gRZN{[Xl? M{j3XlExOCEEtV5CpC=> NY[4dXRsOjRxNEivO|IhcA>? NV\EemRo\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= NFjZdWszOjB3MEe5NC=>
SW1116 NWPj[Gd2TnWwY4Tpc44hSXO|YYm= NEH5NZcyODBiwsXNxsA> NVPqPVVnOjRxNEivO|IhcA>? NG\jbY1l\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NGLlemMzOjB3MEe5NC=>
HT29 MnjQSpVv[3Srb36gRZN{[Xl? Mln5NVAxKML3TdMg NFm4[nYzPC92OD:3NkBp NWe3OVVW\GWlcnXhd4V{KHSqZTDwV3RCXDNibHX2[Yx{KGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? MXOyNlA2ODd7MB?=
ARPE-19 NHriSZhHfW6ldHnvckBCe3OjeR?= M4rjTFXDqM7:TR?= NHe3fGw{OMLibXnu NYjCUXhIcW6qaXLpeJMhUkGNMjDwbI9{eGixcnnsZZRqd25? MVGyNVYzODl4Mx?=
HSC-T6 NFLSVmZCeG:ydH;zbZMhSXO|YYm= NH3MfZAyOMLizszN Mo\PNuKhcMLi MoW4bY5pcWKrdIOgeIhmKGGyb4D0c5NqeyCxZjDIV2MuXDZiY3XscJMhcW6mdXPl[EBjgSCFRFW= MW[yNVM6Pjl7OB?=
HSC-T6 MnnYSpVv[3Srb36gRZN{[Xl? NYn4PXdnOTEEoN88US=> NEToUmwzyqCqwrC= MVLpcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? MmLENlE{QTZ7OUi=
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MZ-256 NYTPcZB[TnWwY4Tpc44hSXO|YYm= MVO1NE8yODEEoN88US=> Mom0OFghcA>? NHHJTW9qdmirYnn0d{BucWe{YYTpc44> NHexPZMzODV6OUWyOS=>
MZ-304 NFfsV49HfW6ldHnvckBCe3OjeR?= MXO1NE8yODEEoN88US=> MmLDOFghcA>? NHPGPINqdmirYnn0d{BucWe{YYTpc44> NXPwNoptOjB3OEm1NlU>
A-172 NILR[WlHfW6ldHnvckBCe3OjeR?= NWq4Xo5ROTBywrFOwG0> NHy1fmM1QCCq MVzpcohq[mm2czDpcpZie2mxbh?= MkSzNlA2QDl3MkW=
MZ-18 MmnsSpVv[3Srb36gRZN{[Xl? MVWxNFDDqM7:TR?= M1\i[FQ5KGh? M3jOe4lvcGmkaYTzJIlvfmG|aX;u NGHyU|czODV6OUWyOS=>
MZ-54 MYnGeY5kfGmxbjDBd5NigQ>? MofONVAxyqEQvF2= MkS4OFghcA>? MUjpcohq[mm2czDpcpZie2mxbh?= MViyNFU5QTV{NR?=
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MZ-304 M2LYT2Z2dmO2aX;uJGF{e2G7 NFjuXoQyODEEoN88US=> NU[4U2l3PDhiaB?= MXnpcohq[mm2czDpcpZie2mxbh?= NX\tVVVSOjB3OEm1NlU>
A-172 NH33fFZHfW6ldHnvckBCe3OjeR?= Ml[zOVAwOTBywrFOwG0> NGP5OZU1QCCq NXf6TXNGemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? Moq5NlA2QDl3MkW=
MZ-18 NXjQe5hGTnWwY4Tpc44hSXO|YYm= MVm1NE8yODEEoN88US=> Ml[4OFghcA>? M4O1S5Jm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> M2XGR|IxPTh7NUK1
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MZ-256 MofRSpVv[3Srb36gRZN{[Xl? Ml3COVAwOTBywrFOwG0> NIjJ[IY1QCCq M3TqN5Jm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MXOyNFU5QTV{NR?=
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SW1990 MWjGeY5kfGmxbjDBd5NigQ>? MV6yNEDPxE1? NFq1[pUzPCCq NYK5c2Rk\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE2PUD2yJIFv\CCYRVfGJI1TVkG| NFi4Z20zODR6Mki1PC=>
SW1990 M2G2[mZ2dmO2aX;uJGF{e2G7 M2DqZVIxKM7:TR?= MoLTNlQhcA>? M3q5N4Rm[3KnYYPld{B1cGViaX70[Y5{cXS7IH;mJJAuW3SjdEOg[ZhxemW|c3nvci=> MojtNlA1QDJ6NUi=
SW1990 M{PDRmlvfmG|aX;uJGF{e2G7 NUWwXZhNOjBizszN MkHmNlQhcA>? MVry[YR2[2W|IHnueoF{cW:wIH;mJHNYOTl7MDDj[Yxte8Li NHjZWFEzODR6Mki1PC=>
THP1 MYfGeY5kfGmxbjDBd5NigQ>? MojGNVAhfU1? MWezNEBucW8EoB?= NGDhdHFqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= MonONlA{QTN4OUC=
BMMC M4jObWZ2dmO2aX;uJGF{e2G7 NFGzZ5kxNTFyIN88US=> M3rrTlE2yqCvaX6= M2LSdolvcGmkaYTzJGxVSzUEoILlcIVie2ViaX6gZUBld3OnLXTldIVv\GWwdDDmZZNpcW:wIIfpeIghdmWjcjDjc41xdGW2ZTDpcohq[mm2aX;uJIF1KGOxbnPlcpRz[XSrb37zJQKqxjFywrFOwG0> NYq2foo1OTl6M{W4OFU>
A549 MVXGeY5kfGmxbjDBd5NigQ>? Mm\sNVUh|ryv NUnhOGJPOSCq Mn\qbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNUBwdiC2eYLvd4lv\SB5MEGge4F{KGSndHXjeIVlKDF3IH3pckBi\nSncjDTVGUhSiC2cnXheI1mdnR? NWe5dHBTOTl6MEG2OlU>
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PA-1 M37BZ2Z2dmO2aX;uJGF{e2G7 MWSxNEB2VQ>? Mn;QNUBp MVPpcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? NVLrNmJVOTl4NEezOlM>
Jurkat  MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PrS|UxKM7:TR?= NH;BSoIzPC92OD:3NkBp Mn\i[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u NF3wNYUyQTV4NEi5NS=>
SUPT1  NHTPPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHpOVAh|ryP NELyenQzPC92OD:3NkBp MX7lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NEjRdG0yQTV4NEi5NS=>
Jurkat  MX7BdI9xfG:|aYOgRZN{[Xl? M4DFXVUxKM7:TR?= MlvqNlQwPDhiaB?= NWPifG5C\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NIXDRowyQTV4NEi5NS=>
SUPT1  NX\GclZlSXCxcITvd4l{KEG|c3H5 NUPKc2FiPTBizszN NELzfWIzPC92ODDo NHq2[49mdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MVGxPVU3PDh7MR?=

... 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 individually and in order:
5% DMSO+45% PEG 300+ddH2O
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