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 NXe4RWhoTnWwY4Tpc44hSXO|YYm= NUDtblFIOTBy4pEJxtVO M4fnOlI1KGh? M4Li[I1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> NELWNlYzPjF6NEm5PS=>
BCBL1 MmPISpVv[3Srb36gRZN{[Xl? MVOxNFDjiIoEtV2= MY[yOEBp MVPt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= NFO4XJIzPjF6NEm5PS=>
BC3 MWDGeY5kfGmxbjDBd5NigQ>? NYXOU|J7OTBy4pEJxtVO MWqyOEBp Mn25cYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? NGe1SlAzPjF6NEm5PS=>
BCBL1 M3\DRmZ2dmO2aX;uJGF{e2G7 M2r2NFExOOLCidM1US=> NXPiN2U4OjRiaB?= NHXhZZZu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= NXrKVZlVOjZzOES5PVk>
BC3 M1e5dmZ2dmO2aX;uJGF{e2G7 Mk\hNVAx6oDLwsXN NGf6dVUzPCCq NXvjbHV5cW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh MmHWNlYyQDR7OUm=
BCBL1 NHzEXIRHfW6ldHnvckBCe3OjeR?= NX3TfHY3OTBy4pEJxtVO M1HQZVI1KGh? MXzpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= MYGyOlE5PDl7OR?=
SK-MEL-28 MWnGeY5kfGmxbjDBd5NigQ>? NFnNZo82OC9zMEFihKnDvU1? Mn\OOFghcA>? MWLEUXNQ NXnsSVRYemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NY\BU3dTOjV{MU[1NlI>
MeWo MnfMSpVv[3Srb36gRZN{[Xl? MWC1NE8yODEkgJpCuW0> MoHIOFghcA>? NHzy[mxFVVOR NFjBNYpz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NVjFNYx{OjV{MU[1NlI>
SK-MEL-5 NYr1R3o4TnWwY4Tpc44hSXO|YYm= MYO1NE8yODEkgJpCuW0> NVOxV5V5PDhiaB?= MYrEUXNQ M1;1fpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl MWqyOVIyPjV{Mh?=
SK-MEL-2 NUDCSlMzTnWwY4Tpc44hSXO|YYm= MXO1NE8yODEkgJpCuW0> NInle|M1QCCq NFzMXYVFVVOR M3vJRpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M1:zZ|I2OjF4NUKy
B16-F0 NXuxcGpTTnWwY4Tpc44hSXO|YYm= NV\HVoNFPTBxMUCw5qCKyrWP NWPqNo4yPDhiaB?= M4fONmROW09? MWPy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= NEL1b5AzPTJzNkWyNi=>
TRPM2/HEK  NYm3UHhmTnWwY4Tpc44hSXO|YYm= M2TrblAvOeLCk{K1xsDDvU1? NIHpWoIyPcLibXnu MljPSG1UVw>? NH\PcnVz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IEGuO:KhyrWP M3[4XFI2OTd7NUe0
U937  MXPGeY5kfGmxbjDBd5NigQ>? NUXuNGY2OC5z4pETNlXDqML3TR?= MV:xOeKhdWmw NVnqNZp{TE2VTx?= M2T1eZJm\HWlZYOgTFJQOi2rbnT1Z4VlKEOjMjvpcoNz\WG|ZTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjygZY5lKHSqZTDJR|UxyqC4YXz1[UB4[XNiMD60xsDDvU1? M1[2ZVI2OTd7NUe0
TRPM2/HEK  Mo\1SpVv[3Srb36gRZN{[Xl? NUjoVldZOTEEoNM1US=> NV:3cXBxPDEEoH3pci=> MnLTSG1UVw>? M37FPJJm\HWlZYOgWHJRVTJiYXP0bZZifGmxbjDleoVvKGG2IHjp[4gh[2:wY3XueJJifGmxboOgc4YhUDKRMh?= M4XsUVI2OTd7NUe0
GL37  M4LncmNmdGxiVnnhZoltcXS7IFHzd4F6 Mn;INE0yOMLiwsXN M2jPdlQ5KGh? MkfQd5VxeHKnc4Pld{BN[SCneIDy[ZN{cW:w MVmyOFk6QTZ3Nx?=
NRK-52E NXjZOXRzTnWwY4Tpc44hSXO|YYm= NWD5NnhzOcLiwsXN MUixNEBucW5? MnfkZoxw[2u|IITo[UB{fGmvdXzheI9zgSCnZn\lZ5Qhd2ZiQX7nJGlKKG:wIGDhfE0zKGW6cILld5Nqd28EoB?= NIj0cmQzPDdzMESyNy=>
NRK-52E MnXISpVv[3Srb36gRZN{[Xl? NH25dYEyyqEEtV2= M{\6UFExKG2rbh?= M362TYJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> MkK0NlQ4OTB2MkO=
HSC  NYfJenhWTnWwY4Tpc44hSXO|YYm= NVfSXFJKOjBizszN MYixJIg> MWPhZpJw\2G2ZYOgeIhmKGSrZn\ldoVvfGmjbDDl[oZm[3S|IH;mJIxmeHSrbjDvdkBCT0W| NWniU2tQOjR4MUSxPVk>
EJ MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e3ZlUxNzhyIN88US=> M3zGfFI1NzR6L{eyJIg> MmnPbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NYfwbnFyOjR3OEewOFk>
EJ Ml7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVq1NE85OCEQvF2= M4PLcFQ5KGh? MXLjZZV{\XNiUz3wbIF{\SCjcoLld5Q> NEPs[XgzPDV6N{C0PS=>
EJ NHjad5JHfW6ldHnvckBCe3OjeR?= NGPvfWk2OC96MDFOwG0> MYK0PEBp NF\vdZJld3ewcnXneYxifGW|IHOtUZlkNCCleXPsbY5FOSxic4Xyeol3cW5iYX7kJHZGT0ZiZYjwdoV{e2mxboO= M1jJO|I1PTh5MES5
HepG2 M1zj[WZ2dmO2aX;uJGF{e2G7 M{HwN|UxNTVyMDFOwG0> MnXpOlDDqG2rbh?= NEfCVmJqdmirYnn0d{B1cGViSVytOk1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTCoWJlzPzB3KTDhcoQhW1SDVEOgLHR6ejdyNTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NX3Gfm9vOjR{NEKwOFY>
SGC7901 NHPIU5VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWX3XmxmOC1zMECg{txO NGTsRZczPC92OD:3NkBp MoPmZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NI\NVoszPDF3MUK1OS=>
AGS  MmXPR4VtdCCYaXHibYxqfHliQYPzZZk> NIHEcIsxNTFyMDFOwG0> NXnvZmFEOjRxNEivO|IhcA>? NXPLS4xw[2G3c3XzJIEhe2mpbnnmbYNidnRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHTvd4Uu\GWyZX7k[Y51dHliYoX0JI5wfCC2aX3lMYRmeGWwZHXueIx6 NWWyVpBuOjRzNUGyOVU>
SGC7901 NWHhPIxpTnWwY4Tpc44hSXO|YYm= MVO1NEDPxE1? NEXy[HAzPC92OD:3NkBp NXLke4g{fGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> NGnYVoczPDF3MUK1OS=>
AGS  MmPPSpVv[3Srb36gRZN{[Xl? Ml\wOVAh|ryP MUeyOE81QC95MjDo Mn:4eIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= NILmdlYzPDF3MUK1OS=>
SGC7901 M1vON2Z2dmO2aX;uJGF{e2G7 MoDYOVAh|ryP NIrwR3gzPC92OD:3NkBp NVjmRYFWfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? NXHZNXZROjRzNUGyOVU>
AGS  NUPKNpp6TnWwY4Tpc44hSXO|YYm= MWG1NEDPxE1? MnHqNlQwPDhxN{KgbC=> MmLkeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> MoXpNlQyPTF{NUW=
MC3T3-E1  NYTtUnhQTnWwY4Tpc44hSXO|YYm= Ml;POVAh|ryP MknhOEBp MnLqbY5pcWKrdIOgTHNGNWmwZIXj[YQhSk2SNzDhcoQhT0iUIIDyc5RmcW5iZYjwdoV{e2mxbtMg NE\Wd5gzOzh5N{ezOC=>
7TD1-DXM MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlywNVAh|ryP MYS3NkBp MVPEUXNQ MnTKbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmLINlM5PzFzNUm=
7TD1-WD-90 M2\Ec2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNEDPxE1? M4nDRlczKGh? M4P5TmROW09? M3f6V4lvcGmkaYTzJINmdGxiZ4Lve5Rp NYPwcVcyOjN6N{GxOVk>
7TD1-DXM NYDzRWRjSXCxcITvd4l{KEG|c3H5 NIPObWE2OCEQvF2= M2DIelQ5KGh? NEjSdFJFVVOR M4rWSIlv\HWlZYOgZZBweHSxc3nz M1y2b|I{QDdzMUW5
7TD1-WD-90 MkfRRZBweHSxc3nzJGF{e2G7 NYjZ[VJYPTBizszN M3HOSFQ5KGh? NFLqUmlFVVOR NUTze2ZpcW6mdXPld{BieG:ydH;zbZM> M2DRfVI{QDdzMUW5
7TD1-WD-90  NH\vN4RHfW6ldHnvckBCe3OjeR?= NHmzTFQ2OCEQvF2= M4jsdVYhcA>? NX:wSVhYTE2VTx?= Mlu0d4lodmmoaXPhcpRtgSCrbnjpZol1eyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGpCUzJiYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMx?= NUT5VYNbOjN6N{GxOVk>
HepG2  NUfuXoF6TnWwY4Tpc44hSXO|YYm= MnrQNVAxKM7:TR?= NV21SYhLOTJxMkSgbC=> MojubY5pcWKrdIOgV3RCXDNidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9v NV3PdmJ{OjN6M{[0NFA>
RAW264.7  NIjiV4tHfW6ldHnvckBCe3OjeR?= NYfXRlF6PTEEoN88UeKh M{L3d|I1NzR6IHi= MWfzeZBxemW|c3XzJHJCVkuOLXnu[JVk\WRib4P0[Y9kdGG|dH;n[Y5me2m| NXnIOW84OjN4NkWwNVg>
RAW264.7 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWmwMVUxyqEQvF5CpC=> MUC0POKhcA>? NVfDOHFGcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[U1l\XCnbnTlcpRtgQ>? NF\EdHUzOzZ4NUCxPC=>
RAW264.7 MlfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfaUVUxNTVywrFOwG3DqA>? NYjmOlFqPDkEoHi= MnvDZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= MWOyN|Y3PTBzOB?=
RAW264.7 MYrGeY5kfGmxbjDBd5NigQ>? NHf1d2E2OMLizszN NFr4ZmMzPC92ODDo Mn\IbY5pcWKrdIOgVmFPU0xvaX7keYNm\CCQRlHUZ|Eh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNmejd{N2PURXQ{ NXPDV5BlOjN4NkWwNVg>
A549  M{jpVmZ2dmO2aX;uJGF{e2G7 NYPK[I9tOjBxNECg{txO NF3weVEzOCCq MWGyNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? MmTPNlM3OjBzOUG=
A549  NEjGVmNHfW6ldHnvckBCe3OjeR?= NIfxUWIyOC9{MD:0NEDPxE1? NEf0W4EzPCCq NUXkO5R2e3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> MlX6NlM3OjBzOUG=
HUVECs NGm3VGNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHf5WowzOCEEtV2= NWKzb5RkPCCq MmL1ZZR1\W63YYTld{BJOk9{LXnu[JVk\WRiY3XscEB{cHKrbnvh[4Uh[W6mIHntdJJwfmWmIITo[UBifHSjY3jt[Y51KHKjdHWgc4YhfGinIHPlcIx{ NUP2U5FLOjN2OEO5OFY>
HUVECs Mm\HRZBweHSxc3nzJGF{e2G7 M1y0N|IxKML3TR?= MnjCOEBp NF3pZWd{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? MVyyN|Q5Ozl2Nh?=
BV-2  MmqxSpVv[3Srb36gRZN{[Xl? M2jWfVIxKML3TR?= NH7Sd2MyPiCq MWDpcohq[mm2czDMVHMucW6mdXPl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBidG2xc4SgZ49ueGyndHXsfUBlcW2rbnnzbIVlKGmQT2Og[ZhxemW|c3nvci=> NX;lcopKOjN{M{[zO|A>
NRK-52E  MWfGeY5kfGmxbjDBd5NigQ>? NFvqT3g2yqEQvF2= M1vM[|MxyqCvaX6= MoHyZZR1\W63YYTld{BCdmdvKEJihLM4MS2rbnjpZol1\WRiVFfGMe6zOSCvUl7BJIF1KDF4wrDoxsA> MXqyN|E4PDd3Nx?=
SW620  NVjLdpQ2TnWwY4Tpc44hSXO|YYm= NYjxWJhmOjBiwsXN M2rLdFEwPiCq MWrpcohq[mm2czDwMXNVSVR|IHHjeIl3[XSrb36= NWDr[lk2OjNzMUC2NlU>
RPE  MWPGeY5kfGmxbjDBd5NigQ>? MnfVN|AhyrWPwrC= NYm1ToRkOyCq M{K2bIlvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u NE\kOnYzOzB7NEC2Oy=>
SW1116 NXPwe2JyTnWwY4Tpc44hSXO|YYm= M1PRd|ExOCEEtV5CpC=> MUiyOE81QC95MjDo MkT1[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? M2\nPFIzODVyN{mw
HT29 MU\GeY5kfGmxbjDBd5NigQ>? NFnCZZQyODBiwsXNxsA> M3qzNVI1NzR6L{eyJIg> NF\UPXVl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= NHTPUFQzOjB3MEe5NC=>
SW1116 NFXCboRHfW6ldHnvckBCe3OjeR?= MofTNVAxKML3TdMg NYqyXHBSOjRxNEivO|IhcA>? NH\jVpdl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? MmThNlIxPTB5OUC=
HT29 MV\GeY5kfGmxbjDBd5NigQ>? MnfSNVAxKML3TdMg NF3PcY0zPC92OD:3NkBp MlfZ[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> NU\Qd2kxOjJyNUC3PVA>
ARPE-19 MkLXSpVv[3Srb36gRZN{[Xl? M4fuVFXDqM7:TR?= NXj4Z4h6OzEEoH3pci=> NWDDPW53cW6qaXLpeJMhUkGNMjDwbI9{eGixcnnsZZRqd25? M4DzclIyPjJyOU[z
HSC-T6 MUnBdI9xfG:|aYOgRZN{[Xl? MnHqNVDDqM7:TR?= NHn4eXUzyqCqwrC= MnXFbY5pcWKrdIOgeIhmKGGyb4D0c5NqeyCxZjDIV2MuXDZiY3XscJMhcW6mdXPl[EBjgSCFRFW= M1rHVlIyOzl4OUm4
HSC-T6 NYLwZXJnTnWwY4Tpc44hSXO|YYm= MYqxNOKh|ryP M2Kwd|LDqGkEoB?= MXHpcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? M2PS[lIyOzl4OUm4
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MZ-304 M37RW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVe1NE8yODEEoN88US=> MWW0PEBp NX7UdmI6dGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo M1r4V|IxPTh7NUK1
A-172 M3KyeGZ2dmO2aX;uJGF{e2G7 M4q1flUxNzFyMNMg{txO NFTsWow1QCCq MnPobY5pcWKrdIOgcYloemG2aX;u MWOyNFU5QTV{NR?=
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MZ-54 NIj3bI1HfW6ldHnvckBCe3OjeR?= MYm1NE8yODEEoN88US=> NY\sXFZVPDhiaB?= NICxRlVqdmirYnn0d{BucWe{YYTpc44> MkDBNlA2QDl3MkW=
MZ-256 NX25d4NKTnWwY4Tpc44hSXO|YYm= Mlm1OVAwOTBywrFOwG0> MVi0PEBp Mke1bY5pcWKrdIOgcYloemG2aX;u Mmj6NlA2QDl3MkW=
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MZ-256 MXTGeY5kfGmxbjDBd5NigQ>? NFzGUGY2OC9zMEFCpO69VQ>? MnnzOFghcA>? M4\pdZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MVyyNFU5QTV{NR?=
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SW1990 MVTJcpZie2mxbjDBd5NigQ>? MXuyNEDPxE1? NEj5WJYzPCCq M2\YOJJm\HWlZYOgbY53[XOrb36gc4YhW1dzOUmwJINmdGy|wrC= NES0SFIzODR6Mki1PC=>
THP1 NEL3WopHfW6ldHnvckBCe3OjeR?= NHPJOZcyOCC3TR?= NXXYSGllOzBibXnuxsA> NGTpc25qdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iYomgc5ZmeiB4MDW= NIrwVlczODN7M{[5NC=>
BMMC MnXjSpVv[3Srb36gRZN{[Xl? MoXFNE0yOCEQvF2= MoTRNVXDqG2rbh?= MYLpcohq[mm2czDMWGM1yqC{ZXzlZZNmKGmwIHGg[I9{\S2mZYDlcoRmdnRiZnHzbIlwdiC5aYToJI5m[XJiY3;tdIxmfGViaX7obYJqfGmxbjDheEBkd26lZX70doF1cW:wczFird4yOMLizszN NF\4SIsyQTh|NUi0OS=>
A549 MUjGeY5kfGmxbjDBd5NigQ>? M1HUN|E2KM7:bR?= MnvyNUBp MULpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSxJI9vKHS7cn;zbY5mKDdyMTD3ZZMh\GW2ZXP0[YQhOTVibXnuJIFnfGW{IGPQSUBDKHS{ZXH0cYVvfA>? MXGxPVgxOTZ4NR?=
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PA-1 NUDxTnlLTnWwY4Tpc44hSXO|YYm= NGjyb4oyOCC3TR?= MWSxJIg> NGHpWndqdmirYnn0d{AhVFCDLXnu[JVk\WRib4\hdolidiClYX7j[ZIh[2WubDDtc5RqdGm2eR?= NFnMZlgyQTZ2N{O2Ny=>
Jurkat  NEHCNXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jW[lUxKM7:TR?= NUHQNIt7OjRxNEivO|IhcA>? NULFS5NI\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v MkizNVk2PjR6OUG=
SUPT1  NIfUNZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW1NEDPxE1? NXXLUYFLOjRxNEivO|IhcA>? NF;leVRmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> MUCxPVU3PDh7MR?=
Jurkat  NF;2UYpCeG:ydH;zbZMhSXO|YYm= MmfFOVAh|ryP MXuyOE81QCCq NXT2WZBH\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NYfuPVhvOTl3NkS4PVE>
SUPT1  NEfTUJVCeG:ydH;zbZMhSXO|YYm= MkGwOVAh|ryP NGq0bnUzPC92ODDo NHTtflBmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MYixPVU3PDh7MR?=

... 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