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 NXqwc5hwTnWwY4Tpc44hSXO|YYm= MoHUNVAx6oDLwsXN M1na[|I1KGh? M4fVU41m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> MkTmNlYyQDR7OUm=
BCBL1 NF75VotHfW6ldHnvckBCe3OjeR?= M1TtdFExOOLCidM1US=> M1rGTVI1KGh? NXi3SIhJdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ MVuyOlE5PDl7OR?=
BC3 NIG4U3pHfW6ldHnvckBCe3OjeR?= MWmxNFDjiIoEtV2= MWGyOEBp MV\t[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YyKHKnZIXjeIlwdg>? Ml;4NlYyQDR7OUm=
BCBL1 NFfVXHJHfW6ldHnvckBCe3OjeR?= MofoNVAx6oDLwsXN MWWyOEBp NF3ONoFu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= M3fNd|I3OTh2OUm5
BC3 MnHCSpVv[3Srb36gRZN{[Xl? Ml7YNVAx6oDLwsXN MYGyOEBp NV3lUpoxcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh Mn3SNlYyQDR7OUm=
BCBL1 NUfRZnE6TnWwY4Tpc44hSXO|YYm= NXfYRoZ4OTBy4pEJxtVO NWm1SYZNOjRiaB?= MXzpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= NIfmXpozPjF6NEm5PS=>
SK-MEL-28 MWjGeY5kfGmxbjDBd5NigQ>? MWS1NE8yODEkgJpCuW0> Mm\ZOFghcA>? MV;EUXNQ MYLy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MWWyOVIyPjV{Mh?=
MeWo NXjafJRZTnWwY4Tpc44hSXO|YYm= NGnqT3I2OC9zMEFihKnDvU1? MXG0PEBp NHLJWndFVVOR NVKw[olHemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NHLv[4kzPTJzNkWyNi=>
SK-MEL-5 MoDVSpVv[3Srb36gRZN{[Xl? M2rVc|UxNzFyMPMAjeK2VQ>? MW[0PEBp NXPaNXZNTE2VTx?= M3iyPZJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NHjZPYwzPTJzNkWyNi=>
SK-MEL-2 NX;wUldNTnWwY4Tpc44hSXO|YYm= Mn63OVAwOTBy4pEJxtVO M4j1SVQ5KGh? NFTLZohFVVOR NEfUZVdz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NH\xbXUzPTJzNkWyNi=>
B16-F0 MnGxSpVv[3Srb36gRZN{[Xl? MW[1NE8yODEkgJpCuW0> M1vORVQ5KGh? NV;OTZJuTE2VTx?= MYPy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= Mn7NNlUzOTZ3MkK=
TRPM2/HEK  MVXGeY5kfGmxbjDBd5NigQ>? NXL4bFJCOC5z4pETNlXDqML3TR?= MV:xOeKhdWmw NETJXGVFVVOR MVPy[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDFwN9MgxtVO M3LwbFI2OTd7NUe0
U937  M4e2WGZ2dmO2aX;uJGF{e2G7 MYOwMlHjiJN{NdMgxtVO NX7LeopVOTYEoH3pci=> Ml\zSG1UVw>? NV\s[oZ{emWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= MkfTNlUyPzl3N{S=
TRPM2/HEK  MUDGeY5kfGmxbjDBd5NigQ>? NHPobmUyOMLiwsXN MVG0NOKhdWmw NHPpPHdFVVOR NYHERoNOemWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y NYi4PJNCOjVzN{m1O|Q>
GL37  NULaTGJSS2WubDDWbYFjcWyrdImgRZN{[Xl? NV;CZXoyOC1zMNMgxtVO NE\qfpo1QCCq NITSSpN{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= NGmwTZUzPDl7OU[1Oy=>
NRK-52E M4\lV2Z2dmO2aX;uJGF{e2G7 NH;lXGYyyqEEtV2= Ml7TNVAhdWmw M1TVPIJtd2OtczD0bIUhe3SrbYXsZZRwenliZX\m[YN1KG:oIFHu[{BKUSCxbjDQZZguOiCneIDy[ZN{cW:wwrC= NF\UR5AzPDdzMESyNy=>
NRK-52E M3HuOmZ2dmO2aX;uJGF{e2G7 Mnv2NeKhyrWP M17NNFExKG2rbh?= NID2b4FjdG:la4OgRY5oKEmLIHnu[JVk\WRiQ1SyOEBmgHC{ZYPzbY9v MYSyOFcyODR{Mx?=
HSC  NWnTVIdzTnWwY4Tpc44hSXO|YYm= NWPsSWZXOjBizszN NF7hSIQyKGh? MnTPZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= M4\Ud|I1PjF2MUm5
EJ MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHiZoQ2OC96MDFOwG0> NVvJbZBrOjRxNEivO|IhcA>? NV7TUHg3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NUL1dWE5OjR3OEewOFk>
EJ MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XTPVUxNzhyIN88US=> NGnZToE1QCCq NUjKPVlv[2G3c3XzJHMueGijc3WgZZJz\XO2 MlWwNlQ2QDdyNEm=
EJ MoTySpVv[3Srb36gRZN{[Xl? M4fSXVUxNzhyIN88US=> Mlf0OFghcA>? NELYTZFld3ewcnXneYxifGW|IHOtUZlkNCCleXPsbY5FOSxic4Xyeol3cW5iYX7kJHZGT0ZiZYjwdoV{e2mxboO= NEXRbo0zPDV6N{C0PS=>
HepG2 M2S1RWZ2dmO2aX;uJGF{e2G7 M3PsdFUxNTVyMDFOwG0> MkjYOlDDqG2rbh?= NHfZdWFqdmirYnn0d{B1cGViSVytOk1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTCoWJlzPzB3KTDhcoQhW1SDVEOgLHR6ejdyNTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NUnQbZRwOjR{NEKwOFY>
SGC7901 NECwdoJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHvsUmQxNTFyMDFOwG0> NXW5ZoRVOjRxNEivO|IhcA>? MlPlZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NHPBTXEzPDF3MUK1OS=>
AGS  NIrOWVFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFnqdYExNTFyMDFOwG0> NXzrO3hOOjRxNEivO|IhcA>? MYfjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= MXKyOFE2OTJ3NR?=
SGC7901 NUf2enZGTnWwY4Tpc44hSXO|YYm= NWPV[FRKPTBizszN MXyyOE81QC95MjDo Mo\SeIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= NVPmVJR{OjRzNUGyOVU>
AGS  M4f3bGZ2dmO2aX;uJGF{e2G7 MVm1NEDPxE1? MYCyOE81QC95MjDo MUf0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= NX\xc4xvOjRzNUGyOVU>
SGC7901 M1zOTWZ2dmO2aX;uJGF{e2G7 MXG1NEDPxE1? NV\oZ|BWOjRxNEivO|IhcA>? M13BWpRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz NHrBcGgzPDF3MUK1OS=>
AGS  Mn\MSpVv[3Srb36gRZN{[Xl? M1riOVUxKM7:TR?= Mn\xNlQwPDhxN{KgbC=> NHq5VlN1cGViY4n0c5Bt[XOvaXOgcI9k[WyrenH0bY9vKG:oIIDKRWszKCiMQVuyJJBpd3OyaH;yfYxifGWmIHH0JJJme2mmdXXzJHR6ejFyMEegZY5lKFS7ckGwNFgqKGSnY4LlZZNm\CCjZoTldkBCTzR7MDD0doVifG2nboSg[o9zKDJ2IHHu[EA1QCCqcjygZpV1KHO2YYL0[YQhfG9icnXic5Vv\CCjdDC3NkBpeg>? NUP6RmxYOjRzNUGyOVU>
MC3T3-E1  MmDYSpVv[3Srb36gRZN{[Xl? NXjVdnh2PTBizszN NHjqUmo1KGh? MmG4bY5pcWKrdIOgTHNGNWmwZIXj[YQhSk2SNzDhcoQhT0iUIIDyc5RmcW5iZYjwdoV{e2mxbtMg Ml3FNlM5Pzd5M{S=
7TD1-DXM MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PnNVExKM7:TR?= M3;XUlczKGh? M2W0TmROW09? MVXpcohq[mm2czDj[YxtKGe{b4f0bC=> NXn5Z4ZJOjN6N{GxOVk>
7TD1-WD-90 Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqxNEDPxE1? M{LKbFczKGh? NXSwcIk1TE2VTx?= M1\TdYlvcGmkaYTzJINmdGxiZ4Lve5Rp NGHZSWgzOzh5MUG1PS=>
7TD1-DXM NVfMR4JqSXCxcITvd4l{KEG|c3H5 NGLjb482OCEQvF2= Mmm5OFghcA>? MUTEUXNQ MnjLbY5lfWOnczDhdI9xfG:|aYO= M4fnRVI{QDdzMUW5
7TD1-WD-90 M{DqT2Fxd3C2b4Ppd{BCe3OjeR?= NUOwXpp2PTBizszN MmCwOFghcA>? M3zLUWROW09? NGLMdG9qdmS3Y3XzJIFxd3C2b4Ppdy=> MV:yN|g4OTF3OR?=
7TD1-WD-90  MXnGeY5kfGmxbjDBd5NigQ>? Mn;MOVAh|ryP MYi2JIg> MoTiSG1UVw>? MV\zbYdvcW[rY3HueIx6KGmwaHnibZR{KHSqZTDwbI9{eGixconsZZRqd25ib3[gTmFMOiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVR| M{nKVVI{QDdzMUW5
HepG2  NX;KVohOTnWwY4Tpc44hSXO|YYm= MWSxNFAh|ryP NELDNnAyOi9{NDDo M2P0SolvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdg>? NGfHWnYzOzh|NkSwNC=>
RAW264.7  MmG5SpVv[3Srb36gRZN{[Xl? MmKxOVDDqM7:TdMg NXXjVGpjOjRxNEigbC=> Mlnyd5VxeHKnc4Pld{BTSU6NTD3pcoR2[2WmIH;zeIVw[2yjc4Tv[4Vv\XOrcx?= MViyN|Y3PTBzOB?=
RAW264.7 M4LMbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2KzO|AuPTEEoN88UeKh NYLifW9PPDkEoHi= MkjYbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> MXmyN|Y3PTBzOB?=
RAW264.7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jD[|AuPTEEoN88UeKh M3W3RlQ5yqCq MnvwZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= NX7IdoVjOjN4NkWwNVg>
RAW264.7 M{DlV2Z2dmO2aX;uJGF{e2G7 NXPKc3VCPTEEoN88US=> M2i3dVI1NzR6IHi= NYmwdHJPcW6qaXLpeJMhWkGQS1ytbY5lfWOnZDDOSmFV[zFiZYjwdoV{e2mxbjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOnckeyO3NVSVR| NWfQSlREOjN4NkWwNVg>
A549  MnriSpVv[3Srb36gRZN{[Xl? NFfsSpIzOC92MDFOwG0> NEfyWIIzOCCq M{fkcVIxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| MlnyNlM3OjBzOUG=
A549  MULGeY5kfGmxbjDBd5NigQ>? MoHHNVAwOjBxNECg{txO MWCyOEBp Mkmxd5VxeHKnc4Pld{B1cGVicnHkbYF1cW:wLXnu[JVk\WRiZXzleoF1cW:wIH;mJHZGT0cEoB?= M3vPWFI{PjJyMUmx
HUVECs NF20RpRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVWyNEDDvU1? Mkn1OEBp NHnoZYFifHSnboXheIV{KEh{T{KtbY5lfWOnZDDj[YxtKHOqcnnub4Fo\SCjbnSgbY1xem:4ZXSgeIhmKGG2dHHjbI1mdnRicnH0[UBw\iC2aHWgZ4VtdHN? M2PFd|I{PDh|OUS2
HUVECs M1jxUmFxd3C2b4Ppd{BCe3OjeR?= Mm\DNlAhyrWP MUO0JIg> NIP1WVR{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? NE\0PGwzOzR6M{m0Oi=>
BV-2  NEHyc4RHfW6ldHnvckBCe3OjeR?= M2DSUVIxKML3TR?= M3W1c|E3KGh? M3\QfIlvcGmkaYTzJGxRWy2rbnT1Z4VlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKGGubX;zeEBkd22ybHX0[Yx6KGSrbXnubZNp\WRiaV7PV{BmgHC{ZYPzbY9v NWXNfYhFOjN{M{[zO|A>
NRK-52E  NUfDUmJxTnWwY4Tpc44hSXO|YYm= NVzLOlg4PcLizszN NXv5c3Z[OzEEoH3pci=> MVrheJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> MYiyN|E4PDd3Nx?=
SW620  NIfwfodHfW6ldHnvckBCe3OjeR?= Mn;BNlAhyrWP NGD1cpUyNzZiaB?= NIG0fXVqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> MWmyN|EyODZ{NR?=
RPE  M3LHZ2Z2dmO2aX;uJGF{e2G7 MlflN|AhyrWPwrC= M3;yR|MhcA>? NEXy[FZqdmirYnn0d{B1cGViaX7keYN1cW:wIH;mJJAuW1SDVEOg[ZhxemW|c3nvci=> M4fINlI{ODl2ME[3
SW1116 Ml\DSpVv[3Srb36gRZN{[Xl? MXSxNFAhyrWPwrC= MWOyOE81QC95MjDo MYPk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? NIfIZ4szOjB3MEe5NC=>
HT29 NYq4TGVQTnWwY4Tpc44hSXO|YYm= MVKxNFAhyrWPwrC= M2\FRVI1NzR6L{eyJIg> Mlfw[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? MmKxNlIxPTB5OUC=
SW1116 NIW2ZY1HfW6ldHnvckBCe3OjeR?= MYSxNFAhyrWPwrC= NHjU[lAzPC92OD:3NkBp MmfF[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> MlPNNlIxPTB5OUC=
HT29 NWjZfJRjTnWwY4Tpc44hSXO|YYm= M1jLZ|ExOCEEtV5CpC=> NUjQN4dMOjRxNEivO|IhcA>? MWfk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> NYHsfGVKOjJyNUC3PVA>
ARPE-19 M3XyOWZ2dmO2aX;uJGF{e2G7 MWG1xsDPxE1? MXezNOKhdWmw MmHmbY5pcWKrdIOgTmFMOiCyaH;zdIhwemmuYYTpc44> NWTxOIdZOjF4MkC5OlM>
HSC-T6 M37GWGFxd3C2b4Ppd{BCe3OjeR?= M4e3U|ExyqEQvF2= NVnZTVU6OsLiaNMg NEDUTWRqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> MWWyNVM6Pjl7OB?=
HSC-T6 MmDaSpVv[3Srb36gRZN{[Xl? MUKxNOKh|ryP MVqyxsBpyqB? NILBUJhqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= NFfZOpIzOTN7Nkm5PC=>
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A-172 MnHUSpVv[3Srb36gRZN{[Xl? M37S[|ExOMLizszN MXG0PEBp MnzMbY5pcWKrdIOgbY53[XOrb36= NInONpQzODV6OUWyOS=>
MZ-18 M{jVeGZ2dmO2aX;uJGF{e2G7 MmLPNVAxyqEQvF2= MknROFghcA>? MkHrbY5pcWKrdIOgbY53[XOrb36= Mm\UNlA2QDl3MkW=
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A-172 NEjYdXpHfW6ldHnvckBCe3OjeR?= NVXPcXhXPTBxMUCwxsDPxE1? M1HpSFQ5KGh? M2D4VZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MoG1NlA2QDl3MkW=
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SW1990 NX:zTWdSTnWwY4Tpc44hSXO|YYm= MWWyNEDPxE1? Mn7uNlQhcA>? NWLTcmp[\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE2PUD2yJIFv\CCYRVfGJI1TVkG| NYrieIljOjB2OEK4OVg>
SW1990 MnXTSpVv[3Srb36gRZN{[Xl? NUK5SZpnOjBizszN NYjGPGJSOjRiaB?= MXLk[YNz\WG|ZYOgeIhmKGmwdHXud4l1gSCxZjDwMXN1[XR|IHX4dJJme3Orb36= MVmyNFQ5Ojh3OB?=
SW1990 MlXyTY53[XOrb36gRZN{[Xl? MmX6NlAh|ryP M1TxW|I1KGh? NIHobZRz\WS3Y3XzJIlvfmG|aX;uJI9nKFOZMUm5NEBk\Wyuc9Mg MkS4NlA1QDJ6NUi=
THP1 M{PYN2Z2dmO2aX;uJGF{e2G7 MmqzNVAhfU1? NH;LZmE{OCCvaX9CpC=> MlLlbY5pcWKrdIOgV3RCXDNidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGK7IH;2[ZIhPjBn MVyyNFM6OzZ7MB?=
BMMC NEDG[oJHfW6ldHnvckBCe3OjeR?= MVqwMVExKM7:TR?= MoHwNVXDqG2rbh?= MYjpcohq[mm2czDMWGM1yqC{ZXzlZZNmKGmwIHGg[I9{\S2mZYDlcoRmdnRiZnHzbIlwdiC5aYToJI5m[XJiY3;tdIxmfGViaX7obYJqfGmxbjDheEBkd26lZX70doF1cW:wczFird4yOMLizszN MojyNVk5OzV6NEW=
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PA-1 M2DmeWZ2dmO2aX;uJGF{e2G7 M1jYXFExKHWP NUfCflhHOSCq MXnpcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? NGjNenoyQTZ2N{O2Ny=>
Jurkat  NWnNN5l5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjYc5I2PTBizszN M{L6SFI1NzR6L{eyJIg> MXjlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= NUnBTpIyOTl3NkS4PVE>
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Jurkat  M1rHOWFxd3C2b4Ppd{BCe3OjeR?= NVj6UHQ4PTBizszN NWTYXpdbOjRxNEigbC=> NEjSW5NmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MXuxPVU3PDh7MR?=
SUPT1  Moe2RZBweHSxc3nzJGF{e2G7 M{HiT|UxKM7:TR?= NEH5NZUzPC92ODDo NEXwTXRmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MYGxPVU3PDh7MR?=

... 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