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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Cited by 33 Publications

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 MWrGeY5kfGmxbjDBd5NigQ>? MVqxNFDjiIoEtV2= NVjEbpR[OjRiaB?= NXv2cYdkdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ M1zMeVI3OTh2OUm5
BCBL1 M{PvUmZ2dmO2aX;uJGF{e2G7 M2KxSVExOOLCidM1US=> NWPMXYdNOjRiaB?= NHzqRYJu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NEPmeXIzPjF6NEm5PS=>
BC3 NGXsO|lHfW6ldHnvckBCe3OjeR?= MXOxNFDjiIoEtV2= MmjINlQhcA>? NGPZW5Ru\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0ZzIILl[JVkfGmxbh?= NHjHNW0zPjF6NEm5PS=>
BCBL1 MnnsSpVv[3Srb36gRZN{[Xl? Mnr2NVAx6oDLwsXN NGXiV3QzPCCq MV\t[YRq[XSnczDk[U1xcG:|cHjvdplt[XSrb36gc4YhW1SDVEOgZ49zemWuYYTl[EB4cXSqIFjTVFcxKGGwZDDIV2YzKHKnZIXjeIlwdg>? M4\RTlI3OTh2OUm5
BC3 NWPVXGNkTnWwY4Tpc44hSXO|YYm= NXHWVXdLOTBy4pEJxtVO NWfV[5dkOjRiaB?= MoPibY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NXz4bnBnOjZzOES5PVk>
BCBL1 NET0cVdHfW6ldHnvckBCe3OjeR?= MkLHNVAx6oDLwsXN Mo\pNlQhcA>? M2HzPYlv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKG[udYlCpC=> NWXiTodvOjZzOES5PVk>
SK-MEL-28 M{TUdmZ2dmO2aX;uJGF{e2G7 NXv3SVN1PTBxMUCw5qCKyrWP MXG0PEBp NWrNfWpjTE2VTx?= NH76Tmhz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NVXNeFdsOjV{MU[1NlI>
MeWo NXLyOlJZTnWwY4Tpc44hSXO|YYm= MoPpOVAwOTBy4pEJxtVO NH7lXIk1QCCq MVXEUXNQ M3yx[ZJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NFjYT|gzPTJzNkWyNi=>
SK-MEL-5 NFjXfFFHfW6ldHnvckBCe3OjeR?= Mo[3OVAwOTBy4pEJxtVO MWG0PEBp MoHISG1UVw>? NIDzZWVz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NEfkU4UzPTJzNkWyNi=>
SK-MEL-2 MXnGeY5kfGmxbjDBd5NigQ>? M2D2clUxNzFyMPMAjeK2VQ>? NHrIR|E1QCCq MUDEUXNQ NFPJZZFz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NGDie2wzPTJzNkWyNi=>
B16-F0 MULGeY5kfGmxbjDBd5NigQ>? M2DVOlUxNzFyMPMAjeK2VQ>? NWLUeJplPDhiaB?= NXnuWm84TE2VTx?= NX7EdI1EemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NWrIVo91OjV{MU[1NlI>
TRPM2/HEK  Mlf5SpVv[3Srb36gRZN{[Xl? NGnob20xNjIkgKOyOeKhyrWP MYOxOeKhdWmw MXzEUXNQ MV;y[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDFwN9MgxtVO NGf2NlUzPTF5OUW3OC=>
U937  MV7GeY5kfGmxbjDBd5NigQ>? NGPKWG0xNjIkgKOyOeKhyrWP MoW3NVXDqG2rbh?= NGjZfVZFVVOR MkPVdoVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyByLkVCpOK2VQ>? MlfjNlUyPzl3N{S=
TRPM2/HEK  NGTwTXpHfW6ldHnvckBCe3OjeR?= M4PldVExyqEEtV2= M2OyWVQxyqCvaX6= MljzSG1UVw>? NWj2TlJmemWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y M1rWdVI2OTd7NUe0
GL37  NV71R2l6S2WubDDWbYFjcWyrdImgRZN{[Xl? MVKwMVExyqEEtV2= NGCx[YM1QCCq NGj4WWt{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= NGjJcpgzPDl7OU[1Oy=>
NRK-52E Mmn3SpVv[3Srb36gRZN{[Xl? M33yVlHDqML3TR?= M1PJUlExKG2rbh?= MoC0Zoxw[2u|IITo[UB{fGmvdXzheI9zgSCnZn\lZ5Qhd2ZiQX7nJGlKKG:wIGDhfE0zKGW6cILld5Nqd28EoB?= MnvJNlQ4OTB2MkO=
NRK-52E MUjGeY5kfGmxbjDBd5NigQ>? MWqxxsDDvU1? M{HLW|ExKG2rbh?= NWnW[5VJ[myxY3vzJGFv\yCLSTDpcoR2[2WmIFPENlQh\XiycnXzd4lwdg>? Mn[0NlQ4OTB2MkO=
HSC  NFPqNHlHfW6ldHnvckBCe3OjeR?= NHrCeZozOCEQvF2= MVexJIg> M172UYFjem:pYYTld{B1cGViZHnm[oVz\W62aXHsJIVn\mWldIOgc4YhdGWydHnuJI9zKEGJRYO= MnLuNlQ3OTRzOUm=
EJ M{LxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrqOVAwQDBizszN M322TVI1NzR6L{eyJIg> NGPGeppqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NGqxS2szPDV6N{C0PS=>
EJ MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonTOVAwQDBizszN MmDlOFghcA>? NVvad3E1[2G3c3XzJHMueGijc3WgZZJz\XO2 NFnEN3UzPDV6N{C0PS=>
EJ MXrGeY5kfGmxbjDBd5NigQ>? MV:1NE85OCEQvF2= NXnZXXRMPDhiaB?= MUnkc5dvemWpdXzheIV{KGNvTYnjMEBkgWOuaX7ENUwhe3W{dnn2bY4h[W6mIG\FS2Yh\XiycnXzd4lwdnN? NGPCNmUzPDV6N{C0PS=>
HepG2 M3TkcWZ2dmO2aX;uJGF{e2G7 NULsVY5[PTBvNUCwJO69VQ>? NX7XSlVxPjEEoH3pci=> MYXpcohq[mm2czD0bIUhUUxvNj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSBqVInyO|A2MSCjbnSgV3RCXDNiKGT5dlcxPSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1L3V|I1OjR{MES2
SGC7901 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1O0dVAuOTByIN88US=> MnrINlQwPDhxN{KgbC=> MlTTZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NEDiVXAzPDF3MUK1OS=>
AGS  NXL4foxPS2WubDDWbYFjcWyrdImgRZN{[Xl? NXfYOVRHOC1zMECg{txO MXiyOE81QC95MjDo MVvjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= M1m1NlI1OTVzMkW1
SGC7901 NYixSJFJTnWwY4Tpc44hSXO|YYm= M4ftU|UxKM7:TR?= Mn7VNlQwPDhxN{KgbC=> M1vVOZRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg M33kelI1OTVzMkW1
AGS  NYjielBPTnWwY4Tpc44hSXO|YYm= NXLiTWRLPTBizszN MlvoNlQwPDhxN{KgbC=> M1PNe5Rp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg Ml;TNlQyPTF{NUW=
SGC7901 NFW3SpVHfW6ldHnvckBCe3OjeR?= NVHIbXA3PTBizszN NXvJS49DOjRxNEivO|IhcA>? NEnsR3l1cGViY4n0c5Bt[XOvaXOgcI9k[WyrenH0bY9vKG:oIIDKRWszKCiMQVuyJJBpd3OyaH;yfYxifGWmIHH0JJJme2mmdXXzJHR6ejFyMEegZY5lKFS7ckGwNFgqKGSnY4LlZZNm\CCjZoTldkBCTzR7MDD0doVifG2nboSg[o9zKDJ2IHHu[EA1QCCqcjygZpV1KHO2YYL0[YQhfG9icnXic5Vv\CCjdDC3NkBpeg>? NVTLZnB2OjRzNUGyOVU>
AGS  MUXGeY5kfGmxbjDBd5NigQ>? MWO1NEDPxE1? Moj3NlQwPDhxN{KgbC=> M4LJ[pRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz M4fPSVI1OTVzMkW1
MC3T3-E1  NW[0UmNwTnWwY4Tpc44hSXO|YYm= NIDZd5Q2OCEQvF2= M2LKblQhcA>? M1fSOolvcGmkaYTzJGhUTS2rbnT1Z4VlKEKPUEegZY5lKEeKUjDwdo91\WmwIHX4dJJme3Orb39CpC=> M4LpNVI{QDd5N{O0
7TD1-DXM MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmxNEDPxE1? MmDFO|IhcA>? MWXEUXNQ MX7pcohq[mm2czDj[YxtKGe{b4f0bC=> M4r2ZVI{QDdzMUW5
7TD1-WD-90 NXyzUGxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXFXoMyOCEQvF2= NXL0VWJ7PzJiaB?= NEfpSYpFVVOR MnrabY5pcWKrdIOgZ4VtdCCpcn;3eIg> NVqyS2p6OjN6N{GxOVk>
7TD1-DXM NXz3S3RISXCxcITvd4l{KEG|c3H5 NVTZUFVuPTBizszN MWO0PEBp MoX4SG1UVw>? M2K2Zolv\HWlZYOgZZBweHSxc3nz NYrhW3Y{OjN6N{GxOVk>
7TD1-WD-90 MlrqRZBweHSxc3nzJGF{e2G7 NGS2NG82OCEQvF2= NXnOfms6PDhiaB?= MUPEUXNQ NF7tboVqdmS3Y3XzJIFxd3C2b4Ppdy=> MkDDNlM5PzFzNUm=
7TD1-WD-90  M3TROWZ2dmO2aX;uJGF{e2G7 M{jkWlUxKM7:TR?= MkLEOkBp MlnwSG1UVw>? MV7zbYdvcW[rY3HueIx6KGmwaHnibZR{KHSqZTDwbI9{eGixconsZZRqd25ib3[gTmFMOiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVR| MYWyN|g4OTF3OR?=
HepG2  MXLGeY5kfGmxbjDBd5NigQ>? NEXLdZYyODBizszN MYexNk8zPCCq M32zPIlvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdg>? MVmyN|g{PjRyMB?=
RAW264.7  M{PZS2Z2dmO2aX;uJGF{e2G7 NIHiTHE2OMLizszNxsA> MUGyOE81QCCq M2PtSZN2eHC{ZYPz[ZMhWkGQS1ytbY5lfWOnZDDvd5Rmd2OuYYP0c4dmdmW|aYO= NHLLfZgzOzZ4NUCxPC=>
RAW264.7 NY\4emhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHrPIFtOC13MNMg{txOyqB? MUi0POKhcA>? MVTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnLXTldIVv\GWwdHz5 MVqyN|Y3PTBzOB?=
RAW264.7 NGf6cWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXod2oxNTVywrFOwG3DqA>? Mm\GOFjDqGh? NV7aVXI2[2G3c3XzJIFvKGG{cnXzeEBw\iCUQWeyOlQvPyClZXzsd{BifCC2aHWgS|AwTzFicHjhd4Uhd2ZidHjlJINmdGxiY4njcIU> NYjkfVRMOjN4NkWwNVg>
RAW264.7 NWTaSnBVTnWwY4Tpc44hSXO|YYm= MoGyOVDDqM7:TR?= MlnUNlQwPDhiaB?= NESxWGpqdmirYnn0d{BTSU6NTD3pcoR2[2WmIF7GRXRkOSCneIDy[ZN{cW:wIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW2W{N{K3V3RCXDN? M2XLTlI{PjZ3MEG4
A549  NFXtNWpHfW6ldHnvckBCe3OjeR?= M16zdlIxNzRyIN88US=> NF;4XGkzOCCq MUiyNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? MVOyN|YzODF7MR?=
A549  M2nsZ2Z2dmO2aX;uJGF{e2G7 MnHxNVAwOjBxNECg{txO Mm\zNlQhcA>? NVjhTpFMe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> NWq4ZnhpOjN4MkCxPVE>
HUVECs MnzMR4VtdCCYaXHibYxqfHliQYPzZZk> NIrKSXUzOCEEtV2= M1fKR|QhcA>? M3L3eYF1fGWwdXH0[ZMhUDKRMj3pcoR2[2WmIHPlcIwhe2i{aX7rZYdmKGGwZDDpcZBzd3[nZDD0bIUh[XS2YXPocYVvfCC{YYTlJI9nKHSqZTDj[Yxtew>? Mk\PNlM1QDN7NE[=
HUVECs NYnaOGJsSXCxcITvd4l{KEG|c3H5 NGP2boQzOCEEtV2= MnjMOEBp MVvzbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgZ4VtdCCjcH;weI91cWNiaX7k[Zg> NXf3Vm9GOjN2OEO5OFY>
BV-2  NXr3TWRMTnWwY4Tpc44hSXO|YYm= M4fOfFIxKML3TR?= NIHXb|gyPiCq NYDvV|JwcW6qaXLpeJMhVFCVLXnu[JVk\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiYXztc5N1KGOxbYDs[ZRmdHliZHntbY5qe2inZDDpUm9UKGW6cILld5Nqd25? NE\DR4YzOzJ|NkO3NC=>
NRK-52E  M1v1VWZ2dmO2aX;uJGF{e2G7 NHKx[ZE2yqEQvF2= MmfiN|DDqG2rbh?= NGrjTXRifHSnboXheIV{KEGwZz2oNgKBmzdrLXnubIljcXSnZDDUS2Yu|rJzIH3SUmEh[XRiMUdCpIjDqA>? M1;W[|I{OTd2N{W3
SW620  MliySpVv[3Srb36gRZN{[Xl? M3zPXlIxKML3TR?= NVfwXIFYOS94IHi= NVPWVYU{cW6qaXLpeJMheC2VVFHUN{Bi[3SrdnH0bY9v MUWyN|EyODZ{NR?=
RPE  NGPnbIZHfW6ldHnvckBCe3OjeR?= MnvIN|AhyrWPwrC= NIO0eZk{KGh? MnLYbY5pcWKrdIOgeIhmKGmwZIXjeIlwdiCxZjDwMXNVSVR|IHX4dJJme3Orb36= NIn5RmYzOzB7NEC2Oy=>
SW1116 MlP1SpVv[3Srb36gRZN{[Xl? M4rESVExOCEEtV5CpC=> M{nqXFI1NzR6L{eyJIg> NVTUOndq\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= M{TsS|IzODVyN{mw
HT29 MVzGeY5kfGmxbjDBd5NigQ>? M2DUNFExOCEEtV5CpC=> MneyNlQwPDhxN{KgbC=> NXHxcoc4\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= NIW2NI4zOjB3MEe5NC=>
SW1116 MoruSpVv[3Srb36gRZN{[Xl? NIjlOpYyODBiwsXNxsA> MkTTNlQwPDhxN{KgbC=> NU\QUoJD\GWlcnXhd4V{KHSqZTDwV3RCXDNibHX2[Yx{KGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? MkPmNlIxPTB5OUC=
HT29 M1fD[GZ2dmO2aX;uJGF{e2G7 MmDVNVAxKML3TdMg M3\xblI1NzR6L{eyJIg> MYDk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> MXOyNlA2ODd7MB?=
ARPE-19 MkPSSpVv[3Srb36gRZN{[Xl? MY[1xsDPxE1? NYTCWmpWOzEEoH3pci=> MVPpcohq[mm2czDKRWszKHCqb4PwbI9zcWyjdHnvci=> NUXnPGF4OjF4MkC5OlM>
HSC-T6 NIHTfm5CeG:ydH;zbZMhSXO|YYm= Mn3XNVDDqM7:TR?= MU[yxsBpyqB? M{[yUolvcGmkaYTzJJRp\SCjcH;weI9{cXNib3[gTHNENVR4IHPlcIx{KGmwZIXj[YQh[nliQ1TF NGflN5QzOTN7Nkm5PC=>
HSC-T6 NVnydoFXTnWwY4Tpc44hSXO|YYm= M3\qSVExyqEQvF2= NV:xbHQxOsLiaNMg NGDEd3RqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= NYHHT2VxOjF|OU[5PVg>
Hep-2 M1[xSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrQOFgzPS1zMECg{txO M4TqTVI1NzR6L{eyJIg> NV3QfGRLcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MX2yNVMxQTR6MR?=
Hep-2 MnTSRZBweHSxc3nzJGF{e2G7 MXy1NEDPxE1? NFz3cFgzPC92OD:3NkBp M1\ZcYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNidHnt[UBl\XCnbnTlcpRtgQ>? NHzTNW8zOTNyOUS4NS=>
Hep-2 MmHrSpVv[3Srb36gRZN{[Xl? MVm1NEDPxE1? NIDPTmYzPC92OD:3NkBp MV3pcohq[mm2czDHNUB1dyCVIHPlcIwh[3mlbHWgeJJidnOrdHnvckBidmRiaX7keYNmeyCJMTDj[YxtKGO7Y3zlJIFzemW|dB?= NW\SOlE4OjF|MEm0PFE>
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KF8 NFm3dZRHfW6ldHnvckBCe3OjeR?= M4njWFExyqEQvF5CpC=> MmLoNeKhcA>? MXXEUXNQyqB? NV7JNXJzcW6qaXLpeJMhUUxvM{OtbY5lfWOnZDDOSk3PwkJiYXP0bZZifGmxbh?= M2fzSlIxQTRyMES1
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MZ-54 MnH0SpVv[3Srb36gRZN{[Xl? M{Owd|UxNzFyMNMg{txO MmLHOFghcA>? NVv3b3loemWmdXPld{B1cGVibHX2[Yx{KG:oIHPvcpN1cXS3dHn2[Yx6KGGldHn2ZZRm\CCVVFHUN{BqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCoYYPobY9v M1jQR|IxPTh7NUK1
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MZ-304 NY\kd2pZTnWwY4Tpc44hSXO|YYm= MXu1NE8yODEEoN88US=> NFzCXHE1QCCq NF76eo5z\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> MYGyNFU5QTV{NR?=
A-172 NX7pS|g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlK0OVAwOTBywrFOwG0> MWe0PEBp NEK4[pVt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= NYL5NGFzOjB3OEm1NlU>
MZ-18 NHnGfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnwfG5jPTBxMUCwxsDPxE1? MoTDOFghcA>? MUDs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? Ml62NlA2QDl3MkW=
MZ-54 NUCxN5ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{CyTFUxNzFyMNMg{txO NEPyeYg1QCCq MX\s[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? M3zGb|IxPTh7NUK1
MZ-256 MlnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWm1NE8yODEEoN88US=> NE\QUFk1QCCq Mn\GcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq MYOyNFU5QTV{NR?=
MZ-304 MkPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHjOVAwOTBywrFOwG0> Mm\nOFghcA>? MmnscIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq NIeweHQzODV6OUWyOS=>
A-172 NYTQW5hKTnWwY4Tpc44hSXO|YYm= NUDVS5h7PTBxMUCwxsDPxE1? NGXNemM1QCCq NFPuPXJqdmirYnn0d{BucWe{YYTpc44> M{jzclIxPTh7NUK1
MZ-18 NHnUfndHfW6ldHnvckBCe3OjeR?= M2OxVVUxNzFyMNMg{txO NITVVlI1QCCq MWHpcohq[mm2czDtbYdz[XSrb36= NH\3XZEzODV6OUWyOS=>
MZ-54 MUjGeY5kfGmxbjDBd5NigQ>? MmXGOVAwOTBywrFOwG0> MV[0PEBp NWe2cGxzcW6qaXLpeJMhdWmpcnH0bY9v M3nONFIxPTh7NUK1
MZ-256 NXLqZ5V{TnWwY4Tpc44hSXO|YYm= MV[1NE8yODEEoN88US=> NFvIZoM1QCCq NVP2XldncW6qaXLpeJMhdWmpcnH0bY9v M2njclIxPTh7NUK1
MZ-304 M2HBPWZ2dmO2aX;uJGF{e2G7 NYnhXFhIPTBxMUCwxsDPxE1? M2\WfFQ5KGh? MnHLbY5pcWKrdIOgcYloemG2aX;u NVHMR3htOjB3OEm1NlU>
A-172 M4PUbmZ2dmO2aX;uJGF{e2G7 M3m0TVExOMLizszN MoX4OFghcA>? MYDpcohq[mm2czDpcpZie2mxbh?= NE\4[GczODV6OUWyOS=>
MZ-18 NHnqfJpHfW6ldHnvckBCe3OjeR?= Mln2NVAxyqEQvF2= NYXFd|VFPDhiaB?= Ml\qbY5pcWKrdIOgbY53[XOrb36= M3rsZlIxPTh7NUK1
MZ-54 NHjJb29HfW6ldHnvckBCe3OjeR?= NEDzbFEyODEEoN88US=> NEfvOok1QCCq MmTQbY5pcWKrdIOgbY53[XOrb36= MnftNlA2QDl3MkW=
MZ-256 NX75SHE4TnWwY4Tpc44hSXO|YYm= MkLpNVAxyqEQvF2= MWW0PEBp Moq1bY5pcWKrdIOgbY53[XOrb36= M3PBbVIxPTh7NUK1
MZ-304 MofESpVv[3Srb36gRZN{[Xl? NInxRpUyODEEoN88US=> NWjFRWp3PDhiaB?= NHT3WFNqdmirYnn0d{Bqdn[jc3nvci=> MVeyNFU5QTV{NR?=
A-172 MmT6SpVv[3Srb36gRZN{[Xl? NHXtTo42OC9zMEFCpO69VQ>? M4\lSFQ5KGh? NV7GfWZxemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? MmP1NlA2QDl3MkW=
MZ-18 M4jYU2Z2dmO2aX;uJGF{e2G7 NGnaZYE2OC9zMEFCpO69VQ>? NXjyc2R7PDhiaB?= NEfvc|Nz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M{fLWVIxPTh7NUK1
MZ-54 NYLBNnFFTnWwY4Tpc44hSXO|YYm= NFL5dnE2OC9zMEFCpO69VQ>? MoK0OFghcA>? NIXi[mJz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M{PNXVIxPTh7NUK1
MZ-256 NHO3NHRHfW6ldHnvckBCe3OjeR?= MoXkOVAwOTBywrFOwG0> NHzORVg1QCCq MV\y[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NGrqeWgzODV6OUWyOS=>
MZ-304 M1naOGZ2dmO2aX;uJGF{e2G7 Ml3wOVAwOTBywrFOwG0> M1u0flQ5KGh? NEPHeHpz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ NHy1XZkzODV6OUWyOS=>
SW1990 NXu1Uod[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFmzbYwzOCEQvF2= MXSyOE81QC95MjDo NInkXoFqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NIDa[ZEzODR6Mki1PC=>
SW1990 M4nMbGZ2dmO2aX;uJGF{e2G7 M1nlUlIxKM7:TR?= NUTzcphHOjRiaB?= NGLTbHNl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhVU2SLUKgZY5lKF[HR1[gcXJPSXN? M2XQUVIxPDh{OEW4
SW1990 MYPGeY5kfGmxbjDBd5NigQ>? NYi1[5o4OjBizszN NFvxZnMzPCCq NF;6N41l\WO{ZXHz[ZMhfGinIHnueIVve2m2eTDv[kBxNVO2YYSzJIV5eHKnc4Ppc44> M{G0[FIxPDh{OEW4
SW1990 NXS1XWt5UW64YYPpc44hSXO|YYm= M2XjbVIxKM7:TR?= M3zC[lI1KGh? M3u5d5Jm\HWlZYOgbY53[XOrb36gc4YhW1dzOUmwJINmdGy|wrC= MoPGNlA1QDJ6NUi=
THP1 MYDGeY5kfGmxbjDBd5NigQ>? NGPaSZAyOCC3TR?= NYfYTIJpOzBibXnuxsA> NWj4[YFtcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wIHL5JI93\XJiNkCl NFTaWIMzODN7M{[5NC=>
BMMC NF7Lb2FHfW6ldHnvckBCe3OjeR?= M2T1ZVAuOTBizszN MYWxOeKhdWmw MWXpcohq[mm2czDMWGM1yqC{ZXzlZZNmKGmwIHGg[I9{\S2mZYDlcoRmdnRiZnHzbIlwdiC5aYToJI5m[XJiY3;tdIxmfGViaX7obYJqfGmxbjDheEBkd26lZX70doF1cW:wczFird4yOMLizszN MnW3NVk5OzV6NEW=
A549 MoTWSpVv[3Srb36gRZN{[Xl? M1TrWFE2KM7:bR?= M1TjT|EhcA>? M2PBUIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiU2TBWFEhd25idInyc5NqdmViN{CxJJdieyCmZYTlZ5Rm\CBzNTDtbY4h[W[2ZYKgV3BGKEJidILlZZRu\W62 MnvUNVk5ODF4NkW=
OVCAR-3 M1LGN2Z2dmO2aX;uJGF{e2G7 NX\zOoJuOTBidV2= NET0b3MyKGh? MWTpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? MVyxPVY1PzN4Mx?=
PA-1 MXPGeY5kfGmxbjDBd5NigQ>? NW[xclBtOTBidV2= NELjOFYyKGh? M13IUolvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= NX:0R2g3OTl4NEezOlM>
OVCAR-3 NFX5Z|dHfW6ldHnvckBCe3OjeR?= MUGxNEB2VQ>? MWixJIg> NGDDfFhqdmirYnn0d{AhVFCDLXnu[JVk\WRib4\hdolidiClYX7j[ZIh[2WubDDtc5RqdGm2eR?= M1P3eFE6PjR5M{[z
PA-1 NE\WPWRHfW6ldHnvckBCe3OjeR?= MXWxNEB2VQ>? NGXVbXcyKGh? NHroclhqdmirYnn0d{AhVFCDLXnu[JVk\WRib4\hdolidiClYX7j[ZIh[2WubDDtc5RqdGm2eR?= MlnxNVk3PDd|NkO=
Jurkat  NUnTOY16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfpOVAh|ryP NYXMSFhoOjRxNEivO|IhcA>? NFexS5FmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NGDzT5gyQTV4NEi5NS=>
SUPT1  MkXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjHWYo2OCEQvF2= NYi1XW13OjRxNEivO|IhcA>? NFnycGtmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> MmjZNVk2PjR6OUG=
Jurkat  MnPPRZBweHSxc3nzJGF{e2G7 M{fZ[VUxKM7:TR?= MXqyOE81QCCq M1j4T4VvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBieG:ydH;zbZM> M2jOXVE6PTZ2OEmx
SUPT1  M33MXGFxd3C2b4Ppd{BCe3OjeR?= MnvIOVAh|ryP NUjDfmV1OjRxNEigbC=> MYnlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz M4jCVlE6PTZ2OEmx

... 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