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AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

99 publications

AG-490 (Tyrphostin B42) Chemical Structure

CAS No. 133550-30-8

AG-490 (Tyrphostin B42, Zinc02557947) 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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Selleck's AG-490 (Tyrphostin B42) has been cited by 99 publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description AG-490 (Tyrphostin B42, Zinc02557947) 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
JAK2 (V617F) [8]
()
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 MVHGeY5kfGmxbjDBd5NigQ>? MYexNFDjiIoEtV2= NFvJOpczPCCq NHPvSnpu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NF3jR|EzPjF6NEm5PS=>
BCBL1 MlrISpVv[3Srb36gRZN{[Xl? M3HHblExOOLCidM1US=> NXjZeXI6OjRiaB?= NYP5WJpSdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ MkXUNlYyQDR7OUm=
BC3 MUXGeY5kfGmxbjDBd5NigQ>? NGP1WIMyODEkgJpCuW0> NX34bFZxOjRiaB?= MknmcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? NHfHW2MzPjF6NEm5PS=>
BCBL1 M{TG[WZ2dmO2aX;uJGF{e2G7 M3WzV|ExOOLCidM1US=> Mly5NlQhcA>? NEGzdJNu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= NWXoOmp5OjZzOES5PVk>
BC3 MVPGeY5kfGmxbjDBd5NigQ>? Mn7SNVAx6oDLwsXN NX\MWZE4OjRiaB?= MWLpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= MoDTNlYyQDR7OUm=
BCBL1 M1nsXmZ2dmO2aX;uJGF{e2G7 MoLLNVAx6oDLwsXN NI[4d|IzPCCq NFzIfVRqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> NGPGVnczPjF6NEm5PS=>
SK-MEL-28 Mm\CSpVv[3Srb36gRZN{[Xl? MnnFOVAwOTBy4pEJxtVO NWTzXW5TPDhiaB?= NHi0O3lFVVOR M4nNRpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NYm4Opg{OjV{MU[1NlI>
MeWo M4jnT2Z2dmO2aX;uJGF{e2G7 M2qySFUxNzFyMPMAjeK2VQ>? MUC0PEBp NV;SPXhTTE2VTx?= NVTEUld1emWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NGPiVlUzPTJzNkWyNi=>
SK-MEL-5 MUHGeY5kfGmxbjDBd5NigQ>? MorHOVAwOTBy4pEJxtVO NYHGdIJnPDhiaB?= M3zXVGROW09? MWny[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MoPjNlUzOTZ3MkK=
SK-MEL-2 NHrpeWZHfW6ldHnvckBCe3OjeR?= MVW1NE8yODEkgJpCuW0> M{jGU|Q5KGh? NHr5eFZFVVOR NFXxe5hz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> MljmNlUzOTZ3MkK=
B16-F0 M2r3[GZ2dmO2aX;uJGF{e2G7 NYTWTnhRPTBxMUCw5qCKyrWP NYS3V4FiPDhiaB?= NX3ZeXBITE2VTx?= NFLWcZdz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> M4TuXVI2OjF4NUKy
TRPM2/HEK  MlrPSpVv[3Srb36gRZN{[Xl? Mni2NE4y6oDVMkZCpOK2VQ>? M4\OflE2yqCvaX6= MVzEUXNQ NHTUXplz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IEGuO:KhyrWP NGLMZ|MzPTF5OUW3OC=>
U937  NXT3[YdzTnWwY4Tpc44hSXO|YYm= Ml\QNE4y6oDVMkZCpOK2VQ>? NGG3RWoyPcLibXnu NYeycHdxTE2VTx?= Mlr4doVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? M2Xo[VI2OTd7NUe0
TRPM2/HEK  MUTGeY5kfGmxbjDBd5NigQ>? NYC2WldTOTEEoNM1US=> MljYOFDDqG2rbh?= M3jQV2ROW09? M2e0fpJm\HWlZYOgWHJRVTJiYXP0bZZifGmxbjDleoVvKGG2IHjp[4gh[2:wY3XueJJifGmxboOgc4YhUDKRMh?= M1LRXlI2OTd7NUe0
GL37  NUC4bZdNS2WubDDWbYFjcWyrdImgRZN{[Xl? NHjF[20xNTFywrFCuW0> NU\kU3VmPDhiaB?= M{PxcZN2eHC{ZYPz[ZMhVGFiZYjwdoV{e2mxbh?= M4HGUFI1QTl7NkW3
NRK-52E MVfGeY5kfGmxbjDBd5NigQ>? MW[xxsDDvU1? MYKxNEBucW5? M33uWYJtd2OtczD0bIUhe3SrbYXsZZRwenliZX\m[YN1KG:oIFHu[{BKUSCxbjDQZZguOiCneIDy[ZN{cW:wwrC= M{TEcFI1PzFyNEKz
NRK-52E NIXQe4pHfW6ldHnvckBCe3OjeR?= NIDx[3MyyqEEtV2= MorxNVAhdWmw M1nzWoJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> Mn;sNlQ4OTB2MkO=
HSC  Mnn4SpVv[3Srb36gRZN{[Xl? Mo[zNlAh|ryP MVSxJIg> NEC4UIJi[nKxZ3H0[ZMhfGinIHTp[oZmemWwdHnhcEBm\m[nY4TzJI9nKGyncITpckBweiCDR1Xz MX6yOFYyPDF7OR?=
EJ M{TJPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;hSVUxNzhyIN88US=> MVmyOE81QC95MjDo MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHW1SZUzPDV6N{C0PS=>
EJ NULiZ4F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jFPVUxNzhyIN88US=> NF;6dGg1QCCq MnnzZ4F2e2W|IGOtdIhie2ViYYLy[ZN1 NX;pR5lnOjR3OEewOFk>
EJ MkPiSpVv[3Srb36gRZN{[Xl? MknkOVAwQDBizszN NXv0cFhTPDhiaB?= NEDueXVld3ewcnXneYxifGW|IHOtUZlkNCCleXPsbY5FOSxic4Xyeol3cW5iYX7kJHZGT0ZiZYjwdoV{e2mxboO= NXS3cnVjOjR3OEewOFk>
HepG2 NUXDTZN6TnWwY4Tpc44hSXO|YYm= NFXLOWM2OC13MECg{txO MX62NOKhdWmw M3nMOIlvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NXjLVGxPOjR{NEKwOFY>
SGC7901 MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4rQUVAuOTByIN88US=> MUKyOE81QC95MjDo MoDxZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 MljkNlQyPTF{NUW=
AGS  NGL0dllE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkfuNE0yODBizszN NUH4TmtmOjRxNEivO|IhcA>? Mo\RZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NH;Zd|kzPDF3MUK1OS=>
SGC7901 M17DSWZ2dmO2aX;uJGF{e2G7 M3v1SVUxKM7:TR?= NHXvcoMzPC92OD:3NkBp NX;iUG5PfGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> MlfuNlQyPTF{NUW=
AGS  NGnsVnBHfW6ldHnvckBCe3OjeR?= NE\TbYY2OCEQvF2= M2\LTlI1NzR6L{eyJIg> M3nIXpRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg Ml;WNlQyPTF{NUW=
SGC7901 NW\VN2dkTnWwY4Tpc44hSXO|YYm= MUi1NEDPxE1? NHrZc5czPC92OD:3NkBp MmGzeIhmKGO7dH;wcIF{dWmlIHzvZ4FtcXqjdHnvckBw\iCySlHLNkApUkGNMjDwbI9{eGixconsZZRm\CCjdDDy[ZNq\HWnczDUfZIyODB5IHHu[EBVgXJzMEC4LUBl\WO{ZXHz[YQh[W[2ZYKgRWc1QTBidILlZZRu\W62IH\vdkAzPCCjbnSgOFghcHJuIHL1eEB{fGG{dHXkJJRwKHKnYn;1coQh[XRiN{KgbJI> MWiyOFE2OTJ3NR?=
AGS  NF;pU2lHfW6ldHnvckBCe3OjeR?= MXm1NEDPxE1? NHOyRmkzPC92OD:3NkBp NX3VfI5nfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? MUCyOFE2OTJ3NR?=
MC3T3-E1  M2PvU2Z2dmO2aX;uJGF{e2G7 NUO0VohsPTBizszN M2jub|QhcA>? MlK5bY5pcWKrdIOgTHNGNWmwZIXj[YQhSk2SNzDhcoQhT0iUIIDyc5RmcW5iZYjwdoV{e2mxbtMg NEDTbnczOzh5N{ezOC=>
7TD1-DXM NIH3TWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6xNEDPxE1? Mon2O|IhcA>? NVHZXXZrTE2VTx?= NIfpTnJqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4XVZlI{QDdzMUW5
7TD1-WD-90 MoHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmxNEDPxE1? MYK3NkBp MlfuSG1UVw>? NUXCcldlcW6qaXLpeJMh[2WubDDndo94fGh? NY\JdGZMOjN6N{GxOVk>
7TD1-DXM NFnX[3VCeG:ydH;zbZMhSXO|YYm= NX\COI5uPTBizszN Mk\lOFghcA>? MYnEUXNQ NVHKNJgxcW6mdXPld{BieG:ydH;zbZM> NHP4V5AzOzh5MUG1PS=>
7TD1-WD-90 NEfsR4xCeG:ydH;zbZMhSXO|YYm= NHzoXHM2OCEQvF2= MXW0PEBp M1XaV2ROW09? MmL1bY5lfWOnczDhdI9xfG:|aYO= NEmxe3YzOzh5MUG1PS=>
7TD1-WD-90  MkHrSpVv[3Srb36gRZN{[Xl? MmixOVAh|ryP M{PKR|YhcA>? M4HCOmROW09? NEDuPG9{cWewaX\pZ4FvfGy7IHnubIljcXS|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhUkGNMjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSz M3\uc|I{QDdzMUW5
HepG2  M2LhR2Z2dmO2aX;uJGF{e2G7 MlHZNVAxKM7:TR?= NXmzOINoOTJxMkSgbC=> NGTFVlRqdmirYnn0d{BUXEGWMzD0fZJwe2mwZTDwbI9{eGixconsZZRqd25? MYmyN|g{PjRyMB?=
RAW264.7  NEXjOoNHfW6ldHnvckBCe3OjeR?= MoTLOVDDqM7:TdMg MXGyOE81QCCq NXHVdJZbe3WycILld5NmeyCUQV7LUE1qdmS3Y3XkJI9{fGWxY3zhd5Rw\2WwZYPpdy=> NUXiPYUyOjN4NkWwNVg>
RAW264.7 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWiwMVUxyqEQvF5CpC=> NUnvRW9pPDkEoHi= M1TEfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wt[IVx\W6mZX70cJk> MVOyN|Y3PTBzOB?=
RAW264.7 M3PpZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KxPVAuPTEEoN88UeKh M3\zbFQ5yqCq MoXEZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= M1LMO|I{PjZ3MEG4
RAW264.7 NELNWXBHfW6ldHnvckBCe3OjeR?= MV61NOKh|ryP MnXNNlQwPDhiaB?= M2G2eIlvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? MlvENlM3PjVyMUi=
A549  NH;W[YdHfW6ldHnvckBCe3OjeR?= NWHVV2E4OjBxNECg{txO MViyNEBp NIq5bJEzOCEQvF2gRWc1QTBic4XwdJJme3OnczD0bIUhemGmaXH0bY9vNWmwZIXj[YQhcW64YYPpc44hd2ZiQUW0PUBk\Wyucx?= M2nSblI{PjJyMUmx
A549  NUj3fFJ5TnWwY4Tpc44hSXO|YYm= MXmxNE8zOC92MDFOwG0> MXKyOEBp NHTLcoJ{fXCycnXzd4V{KHSqZTDyZYRq[XSrb36tbY5lfWOnZDDlcIV3[XSrb36gc4YhXkWJRtMg NUXRN21sOjN4MkCxPVE>
HUVECs MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn7NNlAhyrWP MV[0JIg> NFTEbVhifHSnboXheIV{KEh{T{KtbY5lfWOnZDDj[YxtKHOqcnnub4Fo\SCjbnSgbY1xem:4ZXSgeIhmKGG2dHHjbI1mdnRicnH0[UBw\iC2aHWgZ4VtdHN? NV3OTW1xOjN2OEO5OFY>
HUVECs M{GySmFxd3C2b4Ppd{BCe3OjeR?= NFT2XmgzOCEEtV2= NXPScWd6PCCq NWi2dmQ3e2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 NY\YVFFoOjN2OEO5OFY>
BV-2  NFf3bppHfW6ldHnvckBCe3OjeR?= NWPIfnF1OjBiwsXN MoewNVYhcA>? NEfpNI9qdmirYnn0d{BNWFNvaX7keYNm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCjbH3vd5Qh[2:vcHzleIVtgSCmaX3pcol{cGWmIHnOU3Mh\XiycnXzd4lwdg>? MoHCNlMzOzZ|N{C=
NRK-52E  NHy2[nBHfW6ldHnvckBCe3OjeR?= NWT1XVE4PcLizszN M3:0dFMxyqCvaX6= MV\heJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> NWm3dnN6OjNzN{S3OVc>
SW620  MYHGeY5kfGmxbjDBd5NigQ>? M4LENlIxKML3TR?= M{TpV|EwPiCq NYnHU3dzcW6qaXLpeJMheC2VVFHUN{Bi[3SrdnH0bY9v M1fOeFI{OTFyNkK1
RPE  M3Tzc2Z2dmO2aX;uJGF{e2G7 M3T0VlMxKML3TdMg MVKzJIg> MWfpcohq[mm2czD0bIUhcW6mdXP0bY9vKG:oIICtV3RCXDNiZYjwdoV{e2mxbh?= Mn;XNlMxQTRyNke=
SW1116 NUn1VJRITnWwY4Tpc44hSXO|YYm= NX[1TmZSOTByINM1UeKh M2Hq[VI1NzR6L{eyJIg> NXnySVdG\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= M{DoXFIzODVyN{mw
HT29 MUPGeY5kfGmxbjDBd5NigQ>? M1TJNVExOCEEtV5CpC=> M4HYTFI1NzR6L{eyJIg> Mkjs[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? M2nZdFIzODVyN{mw
SW1116 M4nTNmZ2dmO2aX;uJGF{e2G7 NE[z[FYyODBiwsXNxsA> NIK1epIzPC92OD:3NkBp NY\SboNl\GWlcnXhd4V{KHSqZTDwV3RCXDNibHX2[Yx{KGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? MV6yNlA2ODd7MB?=
HT29 Mk\LSpVv[3Srb36gRZN{[Xl? NFTYfVcyODBiwsXNxsA> Mmi5NlQwPDhxN{KgbC=> MnPL[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> NWrTOph{OjJyNUC3PVA>
ARPE-19 NYjpSVZJTnWwY4Tpc44hSXO|YYm= M3nZV|XDqM7:TR?= MkO4N|DDqG2rbh?= NYHWTopwcW6qaXLpeJMhUkGNMjDwbI9{eGixcnnsZZRqd25? MojWNlE3OjB7NkO=
HSC-T6 Ml;iRZBweHSxc3nzJGF{e2G7 MVKxNOKh|ryP MX2yxsBpyqB? NHvqXGJqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> NFzTWVIzOTN7Nkm5PC=>
HSC-T6 MVrGeY5kfGmxbjDBd5NigQ>? MkXPNVDDqM7:TR?= MmXoNuKhcMLi NWmyZ5h7cW6qaXLpeJMhfGinIHX4dJJme3Orb37zJI9nKHC\LWPURXQyKGGwZDDCZYQhcW6mdXPl[EBjgSCFRFW= MX6yNVM6Pjl7OB?=
Hep-2 NWTwUXFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP4RnU1OjVvMUCwJO69VQ>? NYLDWVhuOjRxNEivO|IhcA>? M17ZeolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NYm0dJJtOjF|MEm0PFE>
Hep-2 NYLVSZE1SXCxcITvd4l{KEG|c3H5 MmrUOVAh|ryP NEHhRW8zPC92OD:3NkBp M175b4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNidHnt[UBl\XCnbnTlcpRtgQ>? NEP6UFczOTNyOUS4NS=>
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KF8 Mn3CSpVv[3Srb36gRZN{[Xl? MmTKNVDDqM7:TdMg NUK3bllOOcLiaNMg M4TxRmROW00EoB?= NI\4XlRqdmirYnn0d{BKVC1|Mz3pcoR2[2WmIFpOvmLPuSCmZXfyZYRifGmxbjDhcoQhVkZvzsrCJIFkfGm4YYTpc44> Mkf6NlA6PDByNEW=
HEL  M37PRmZ2dmO2aX;uJGF{e2G7 NVPsemhbOTBywrFOwG0> MVuxNk04OiCq M4TaeolvcGmkaYTzJJRp\SCuZY\lcEBw\iCyLVrBT|ItKEqDS{K= NXjpW3BiOjB4MkGwOlE>
HEL NYL6c5JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDzV5U{OTBywrFOwG0> MkfWNE02KGR? MVLy[YR2[2W|IHfyc5d1cCCxZjDKRWszXjZzN1[t[ZhxemW|c3nu[{BJTUxiY3XscJM> NH;PV|UzODZ{MUC2NS=>
A-172 M4KxSmZ2dmO2aX;uJGF{e2G7 M{\BeFUxNzFyMNMg{txO NEHrWJM1QCCq MUny[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= M2fFUVIxPTh7NUK1
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MZ-18 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m2WFUxNzFyMNMg{txO MmPuOFghcA>? NX3nPG95dGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MXOyNFU5QTV{NR?=
MZ-54 NF:0bXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXW1NE8yODEEoN88US=> MYG0PEBp NF;3epRt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= M4rqVlIxPTh7NUK1
MZ-256 NH24TWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;uc|UxNzFyMNMg{txO M2HINlQ5KGh? NF;Ib5pt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= MXSyNFU5QTV{NR?=
MZ-304 NGjlbJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDoc5U2OC9zMEFCpO69VQ>? M33LO|Q5KGh? NITheZBt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= NWn1[ZR1OjB3OEm1NlU>
A-172 MYnGeY5kfGmxbjDBd5NigQ>? NWKzeWRoPTBxMUCwxsDPxE1? M4f6dVQ5KGh? M1vacIlvcGmkaYTzJI1q\3KjdHnvci=> M4my[|IxPTh7NUK1
MZ-18 Moe2SpVv[3Srb36gRZN{[Xl? NVT5WYJWPTBxMUCwxsDPxE1? Ml7TOFghcA>? NFLXSnFqdmirYnn0d{BucWe{YYTpc44> M4fZPVIxPTh7NUK1
MZ-54 NEnoO21HfW6ldHnvckBCe3OjeR?= NV;PWHRuPTBxMUCwxsDPxE1? M2q0fVQ5KGh? M4TDNIlvcGmkaYTzJI1q\3KjdHnvci=> NH21R20zODV6OUWyOS=>
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MZ-304 NYTXcIZuTnWwY4Tpc44hSXO|YYm= MWG1NE8yODEEoN88US=> MVi0PEBp MUjpcohq[mm2czDtbYdz[XSrb36= NVjkdVlROjB3OEm1NlU>
A-172 NX\yOm1OTnWwY4Tpc44hSXO|YYm= M3XpeFExOMLizszN MXK0PEBp M4HOUYlvcGmkaYTzJIlvfmG|aX;u Mk\vNlA2QDl3MkW=
MZ-18 M1nrdmZ2dmO2aX;uJGF{e2G7 M2f4WFExOMLizszN MW[0PEBp MXrpcohq[mm2czDpcpZie2mxbh?= NGm4bY4zODV6OUWyOS=>
MZ-54 MkH6SpVv[3Srb36gRZN{[Xl? M2XYclExOMLizszN MlznOFghcA>? NUfab3Y4cW6qaXLpeJMhcW64YYPpc44> M1;oe|IxPTh7NUK1
MZ-256 MUHGeY5kfGmxbjDBd5NigQ>? MlrTNVAxyqEQvF2= MXm0PEBp NXvMV|V4cW6qaXLpeJMhcW64YYPpc44> NX7OdnhnOjB3OEm1NlU>
MZ-304 M{Dh[2Z2dmO2aX;uJGF{e2G7 NXfTc2RMOTBywrFOwG0> NX\wbo0{PDhiaB?= M1\uXYlvcGmkaYTzJIlvfmG|aX;u MofyNlA2QDl3MkW=
A-172 MnzZSpVv[3Srb36gRZN{[Xl? NEK1XpI2OC9zMEFCpO69VQ>? NWC4OphvPDhiaB?= MWHy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz M{LmSVIxPTh7NUK1
MZ-18 M4WxbmZ2dmO2aX;uJGF{e2G7 NEHBO3M2OC9zMEFCpO69VQ>? NGOxd5U1QCCq MmnldoVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> M{TFWVIxPTh7NUK1
MZ-54 NUjpZVQ4TnWwY4Tpc44hSXO|YYm= NInEd3E2OC9zMEFCpO69VQ>? MVy0PEBp MlvjdoVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> M2jTWVIxPTh7NUK1
MZ-256 NInsV5ZHfW6ldHnvckBCe3OjeR?= M4TmTFUxNzFyMNMg{txO Mlj2OFghcA>? NInydIRz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ NH3Qe5czODV6OUWyOS=>
MZ-304 NGj2TmhHfW6ldHnvckBCe3OjeR?= NEXDUXo2OC9zMEFCpO69VQ>? M1u3fFQ5KGh? NFjST4Vz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MlviNlA2QDl3MkW=
SW1990 NVfiPVVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vP[FIxKM7:TR?= NUPzRlJwOjRxNEivO|IhcA>? MnXEbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NIDt[m4zODR6Mki1PC=>
SW1990 NE\JbVhHfW6ldHnvckBCe3OjeR?= NYPDeFRqOjBizszN NGjU[G4zPCCq Mnvl[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJG1OWC1{IHHu[EBXTUeIIH3SUmF{ Mo\nNlA1QDJ6NUi=
SW1990 M1XrWGZ2dmO2aX;uJGF{e2G7 M4m3SlIxKM7:TR?= MYKyOEBp MUjk[YNz\WG|ZYOgeIhmKGmwdHXud4l1gSCxZjDwMXN1[XR|IHX4dJJme3Orb36= M3vkVlIxPDh{OEW4
SW1990 Ml;CTY53[XOrb36gRZN{[Xl? M4nlXlIxKM7:TR?= M{fRUVI1KGh? NIfMeJlz\WS3Y3XzJIlvfmG|aX;uJI9nKFOZMUm5NEBk\Wyuc9Mg M1;vZ|IxPDh{OEW4
THP1 NV2xW441TnWwY4Tpc44hSXO|YYm= M3LPbVExKHWP NF;uWWU{OCCvaX9CpC=> MWfpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44h[nlib4\ldkA3OCV? MUWyNFM6OzZ7MB?=
BMMC NULtbm1ZTnWwY4Tpc44hSXO|YYm= MlPTNE0yOCEQvF2= NI\XNpkyPcLibXnu NWXJeHBIcW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? M4nlO|E6QDN3OES1
A549 M4PBUGZ2dmO2aX;uJGF{e2G7 M33lRlE2KM7:bR?= NFrw[|cyKGh? Mo[4bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNUBwdiC2eYLvd4lv\SB5MEGge4F{KGSndHXjeIVlKDF3IH3pckBi\nSncjDTVGUhSiC2cnXheI1mdnR? M{jDVVE6QDBzNk[1
OVCAR-3 NGDCO45HfW6ldHnvckBCe3OjeR?= NWXIfFJEOTBidV2= NH6wbIwyKGh? NUHPTGc3cW6qaXLpeJMhVFCDLXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;u NFnDeZMyQTZ2N{O2Ny=>
PA-1 NX\nT|l1TnWwY4Tpc44hSXO|YYm= Mn7hNVAhfU1? NGT2WY4yKGh? NIewR5NqdmirYnn0d{BNWEFvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= NInzSnUyQTZ2N{O2Ny=>
OVCAR-3 NUX1W5JZTnWwY4Tpc44hSXO|YYm= M{T0UVExKHWP NETSfoEyKGh? M1nYRolvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 Mn;LNVk3PDd|NkO=
PA-1 MnTuSpVv[3Srb36gRZN{[Xl? NYHtN2c4OTBidV2= MlTNNUBp M3S3[4lvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 NUHqOm1YOTl4NEezOlM>
Jurkat  MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHtOVAh|ryP NVXHSYlkOjRxNEivO|IhcA>? NInOZ2hmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NXjnU3k2OTl3NkS4PVE>
SUPT1  M2rvfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzWPJR2PTBizszN MoLCNlQwPDhxN{KgbC=> NVPqb5lj\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v Mn\oNVk2PjR6OUG=
Jurkat  M3WwXmFxd3C2b4Ppd{BCe3OjeR?= MVW1NEDPxE1? NWnhZlhbOjRxNEigbC=> MkLi[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> MoLPNVk2PjR6OUG=
SUPT1  NYSxN|h5SXCxcITvd4l{KEG|c3H5 MkTOOVAh|ryP M1;2PVI1NzR6IHi= MX\lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz MYexPVU3PDh7MR?=

... 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]

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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]

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  • 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]

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  • Animal Models: SCID mice intravenously injected with ALL cells
  • 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)
Water Insoluble
Ethanol '6 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG300+5% Tween80+50% ddH2O
For best results, use promptly after mixing.
6.25 mg/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
Smiles C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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