AG-490 (Tyrphostin B42)

Catalog No.S1143 Synonyms: Zinc02557947

For research use only.

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.

AG-490 (Tyrphostin B42) Chemical Structure

CAS No. 133550-30-8

Selleck's AG-490 (Tyrphostin B42) has been cited by 115 publications

Purity & Quality Control

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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 NFnOT3FHfW6ldHnvckBCe3OjeR?= NYDIZpZ1OTBy4pEJxtVO NEPuWYczPCCq M1H1OY1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> NFTrTXIzPjF6NEm5PS=>
BCBL1 NVvHdXFHTnWwY4Tpc44hSXO|YYm= MYqxNFDjiIoEtV2= MonsNlQhcA>? M4DIPY1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> M2ftNVI3OTh2OUm5
BC3 NHzIPI9HfW6ldHnvckBCe3OjeR?= MnXNNVAx6oDLwsXN NYPxUGprOjRiaB?= MmTJcYVlcWG2ZYOg[IUueGixc4Doc5J6dGG2aX;uJI9nKFOWQWSzJINwenKnbHH0[YQhf2m2aDDIV3A4OCCjbnSgTHNHOSC{ZXT1Z5Rqd25? M1L6OVI3OTh2OUm5
BCBL1 NV\OdoZnTnWwY4Tpc44hSXO|YYm= NIL1VlAyODEkgJpCuW0> NHnD[oszPCCq NHjzWIRu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= Mk\oNlYyQDR7OUm=
BC3 NULvfoQyTnWwY4Tpc44hSXO|YYm= NWXadZZNOTBy4pEJxtVO MmjXNlQhcA>? MkTtbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NXfveHc{OjZzOES5PVk>
BCBL1 MnvtSpVv[3Srb36gRZN{[Xl? MWWxNFDjiIoEtV2= NIjHU2UzPCCq NIT6eW9qdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> MlHYNlYyQDR7OUm=
SK-MEL-28 NVfHSm5lTnWwY4Tpc44hSXO|YYm= M1PmNVUxNzFyMPMAjeK2VQ>? M{j5U|Q5KGh? MoX3SG1UVw>? MWny[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= M3fES|I2OjF4NUKy
MeWo NXyx[5RvTnWwY4Tpc44hSXO|YYm= Mkm0OVAwOTBy4pEJxtVO MlzvOFghcA>? MUnEUXNQ NYX3[2ZmemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> M4XGNFI2OjF4NUKy
SK-MEL-5 MlrESpVv[3Srb36gRZN{[Xl? MX[1NE8yODEkgJpCuW0> MnnXOFghcA>? NVfPb3VlTE2VTx?= NWXyeppxemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MXyyOVIyPjV{Mh?=
SK-MEL-2 Mn\hSpVv[3Srb36gRZN{[Xl? NEL1XnE2OC9zMEFihKnDvU1? NYPZWZFsPDhiaB?= MmTOSG1UVw>? NGG5foJz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NXPjNoljOjV{MU[1NlI>
B16-F0 MV3GeY5kfGmxbjDBd5NigQ>? Mor4OVAwOTBy4pEJxtVO NULESoFUPDhiaB?= M1rVUGROW09? NVXnZYVyemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NV\HXlhNOjV{MU[1NlI>
TRPM2/HEK  NF\Bc2lHfW6ldHnvckBCe3OjeR?= M3rQT|AvOeLCk{K1xsDDvU1? MYKxOeKhdWmw MYfEUXNQ Mn\6doVlfWOnczDINm8zNWmwZIXj[YQhS2F{K3nuZ5Jm[XOnIHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{LDDhcoQhfGinIFnDOVDDqH[jbIXlJJdieyBzLkhCpOK2VQ>? NXvQbmt1OjVzN{m1O|Q>
U937  NY\0b5hnTnWwY4Tpc44hSXO|YYm= M3W3d|AvOeLCk{K1xsDDvU1? Ml3ONVXDqG2rbh?= M2rQUWROW09? NUDJWWNvemWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= NVTK[HJ5OjVzN{m1O|Q>
TRPM2/HEK  M3fuSmZ2dmO2aX;uJGF{e2G7 M37YblExyqEEtV2= MYO0NOKhdWmw M3nybmROW09? NE[1[Jhz\WS3Y3XzJHRTWE1{IHHjeIl3[XSrb36g[ZZmdiCjdDDobYdpKGOxbnPlcpRz[XSrb37zJI9nKEh{T{K= MmfrNlUyPzl3N{S=
GL37  NHPuVnZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHX3V2ExNTFywrFCuW0> M{\LcFQ5KGh? MYPzeZBxemW|c3XzJGxiKGW6cILld5Nqd25? NYPUOJlyOjR7OUm2OVc>
NRK-52E MljTSpVv[3Srb36gRZN{[Xl? M1;ZblHDqML3TR?= NF7keWEyOCCvaX6= MYDicI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi MkXnNlQ4OTB2MkO=
NRK-52E NX3n[|R4TnWwY4Tpc44hSXO|YYm= NWHHe2JLOcLiwsXN MmjyNVAhdWmw NFrRc2pjdG:la4OgRY5oKEmLIHnu[JVk\WRiQ1SyOEBmgHC{ZYPzbY9v MmHVNlQ4OTB2MkO=
HSC  MVLGeY5kfGmxbjDBd5NigQ>? M{fJWVIxKM7:TR?= Mmr6NUBp MofTZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= M2TEPVI1PjF2MUm5
EJ MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvSOVAwQDBizszN Mk\1NlQwPDhxN{KgbC=> NULJfIlPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M{nvblI1PTh5MES5
EJ MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny1OVAwQDBizszN NHf5Wmo1QCCq MXTjZZV{\XNiUz3wbIF{\SCjcoLld5Q> M1zCWFI1PTh5MES5
EJ NILH[FFHfW6ldHnvckBCe3OjeR?= MV:1NE85OCEQvF2= M{PWcVQ5KGh? NYH6OoJK\G:5boLl[5Vt[XSnczDjMW16[yxiY4njcIlvTDFuIIP1dpZqfmmwIHHu[EBXTUeIIHX4dJJme3Orb37z NFK2O3ozPDV6N{C0PS=>
HepG2 M2LsT2Z2dmO2aX;uJGF{e2G7 MWi1NE02ODBizszN NUfvfI43PjEEoH3pci=> M1PTSolvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXeyOFI1OjB2Nh?=
SGC7901 M4HvZ2NmdGxiVnnhZoltcXS7IFHzd4F6 MVewMVExOCEQvF2= MXyyOE81QC95MjDo NFXCZ3Rk[XW|ZYOgZUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliZH;z[U1l\XCnbnTlcpRtgSCkdYSgco91KHSrbXWt[IVx\W6mZX70cJk> Mkn0NlQyPTF{NUW=
AGS  NHK3eFdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkP4NE0yODBizszN M{[1cFI1NzR6L{eyJIg> MYLjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= M3vFSFI1OTVzMkW1
SGC7901 M4XLTmZ2dmO2aX;uJGF{e2G7 M{fRTVUxKM7:TR?= NUe2PXViOjRxNEivO|IhcA>? MmD1eIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= M1;GfFI1OTVzMkW1
AGS  M1jnWmZ2dmO2aX;uJGF{e2G7 M4XPdVUxKM7:TR?= MnzFNlQwPDhxN{KgbC=> MVz0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= NHjIc5UzPDF3MUK1OS=>
SGC7901 NID1S5pHfW6ldHnvckBCe3OjeR?= NXHlS|l7PTBizszN NEC4WFgzPC92OD:3NkBp MXH0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> M1TpPFI1OTVzMkW1
AGS  MkDPSpVv[3Srb36gRZN{[Xl? MmDjOVAh|ryP NVntd4t[OjRxNEivO|IhcA>? NEjCcFJ1cGViY4n0c5Bt[XOvaXOgcI9k[WyrenH0bY9vKG:oIIDKRWszKCiMQVuyJJBpd3OyaH;yfYxifGWmIHH0JJJme2mmdXXzJHR6ejFyMEegZY5lKFS7ckGwNFgqKGSnY4LlZZNm\CCjZoTldkBCTzR7MDD0doVifG2nboSg[o9zKDJ2IHHu[EA1QCCqcjygZpV1KHO2YYL0[YQhfG9icnXic5Vv\CCjdDC3NkBpeg>? MYWyOFE2OTJ3NR?=
MC3T3-E1  NEHQbHZHfW6ldHnvckBCe3OjeR?= NHrLZpg2OCEQvF2= NHrqcHo1KGh? NUnRZVJRcW6qaXLpeJMhUFOHLXnu[JVk\WRiQl3QO{BidmRiR1jSJJBzd3SnaX6g[ZhxemW|c3nvcuKh MmHGNlM5Pzd5M{S=
7TD1-DXM NUnRTo06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXLNVAh|ryP NIfYUIk4OiCq M3HZR2ROW09? Mm[4bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MXSyN|g4OTF3OR?=
7TD1-WD-90 NELFd|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rZXlExKM7:TR?= NVKz[JZWPzJiaB?= NFTaNHBFVVOR MnTnbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MkDiNlM5PzFzNUm=
7TD1-DXM MlrhRZBweHSxc3nzJGF{e2G7 MVe1NEDPxE1? MW[0PEBp M4XYemROW09? NEOyVmlqdmS3Y3XzJIFxd3C2b4Ppdy=> NF\F[VUzOzh5MUG1PS=>
7TD1-WD-90 MX7BdI9xfG:|aYOgRZN{[Xl? MmG0OVAh|ryP NFXiWIo1QCCq M1\GUGROW09? NXjubXRUcW6mdXPld{BieG:ydH;zbZM> MkjXNlM5PzFzNUm=
7TD1-WD-90  NELtNXlHfW6ldHnvckBCe3OjeR?= MkTmOVAh|ryP NXy1UYg3PiCq NXTuXnQ5TE2VTx?= MXXzbYdvcW[rY3HueIx6KGmwaHnibZR{KHSqZTDwbI9{eGixconsZZRqd25ib3[gTmFMOiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVR| NV7xO5J6OjN6N{GxOVk>
HepG2  MXrGeY5kfGmxbjDBd5NigQ>? MW[xNFAh|ryP M3fJSVEzNzJ2IHi= M4\RbIlvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdg>? NWrIPJhqOjN6M{[0NFA>
RAW264.7  M1q0XWZ2dmO2aX;uJGF{e2G7 MVO1NOKh|ryPwrC= NWHHTWFDOjRxNEigbC=> MVXzeZBxemW|c3XzJHJCVkuOLXnu[JVk\WRib4P0[Y9kdGG|dH;n[Y5me2m| MnvyNlM3PjVyMUi=
RAW264.7 NH2wSFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\HTWJLOC13MNMg{txOyqB? M1TZOlQ5yqCq MkLRbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> NIHJSYUzOzZ4NUCxPC=>
RAW264.7 NVr6c|JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLBNE02OMLizszNxsA> NXvJbIp{PDkEoHi= NIf6ZWRk[XW|ZYOgZY4h[XK{ZYP0JI9nKFKDV{K2OE44KGOnbHzzJIF1KHSqZTDHNE9IOSCyaHHz[UBw\iC2aHWgZ4VtdCCleXPs[S=> MWKyN|Y3PTBzOB?=
RAW264.7 Mn63SpVv[3Srb36gRZN{[Xl? M1\j[VUxyqEQvF2= NEe1PZMzPC92ODDo NIjDbGdqdmirYnn0d{BTSU6NTD3pcoR2[2WmIF7GRXRkOSCneIDy[ZN{cW:wIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW2W{N{K3V3RCXDN? MoTLNlM3PjVyMUi=
A549  NIPrdGhHfW6ldHnvckBCe3OjeR?= MX6yNE81OCEQvF2= MoC3NlAhcA>? MYeyNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? MnH2NlM3OjBzOUG=
A549  M{fJ[WZ2dmO2aX;uJGF{e2G7 M2LkWVExNzJyL{SwJO69VQ>? M4f2SlI1KGh? M4\0SZN2eHC{ZYPz[ZMhfGinIILh[IlifGmxbj3pcoR2[2WmIHXs[ZZifGmxbjDv[kBXTUeIwrC= MYCyN|YzODF7MR?=
HUVECs NWDlPYdVS2WubDDWbYFjcWyrdImgRZN{[Xl? NU\wc|k1OjBiwsXN MXm0JIg> M4HlbIF1fGWwdXH0[ZMhUDKRMj3pcoR2[2WmIHPlcIwhe2i{aX7rZYdmKGGwZDDpcZBzd3[nZDD0bIUh[XS2YXPocYVvfCC{YYTlJI9nKHSqZTDj[Yxtew>? MVyyN|Q5Ozl2Nh?=
HUVECs M1;tOWFxd3C2b4Ppd{BCe3OjeR?= NE\aNlQzOCEEtV2= MofiOEBp NIi4T5h{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? MnmxNlM1QDN7NE[=
BV-2  NX6wbpRFTnWwY4Tpc44hSXO|YYm= MVWyNEDDvU1? MXWxOkBp M4ficYlvcGmkaYTzJGxRWy2rbnT1Z4VlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKGGubX;zeEBkd22ybHX0[Yx6KGSrbXnubZNp\WRiaV7PV{BmgHC{ZYPzbY9v NWn5UXRxOjN{M{[zO|A>
NRK-52E  MVrGeY5kfGmxbjDBd5NigQ>? NV;j[3ZIPcLizszN NH\UWpY{OMLibXnu MUjheJRmdnWjdHXzJGFv\y1qMfMAl|cqNWmwaHnibZRm\CCWR1[t{tIyKG2UTlGgZZQhOTcEoHlCpC=> M3;sb|I{OTd2N{W3
SW620  Mnz2SpVv[3Srb36gRZN{[Xl? M1HtWVIxKML3TR?= MY[xM|YhcA>? MYXpcohq[mm2czDwMXNVSVR|IHHjeIl3[XSrb36= MUGyN|EyODZ{NR?=
RPE  MkjBSpVv[3Srb36gRZN{[Xl? NWrERXpSOzBiwsXNxsA> MWizJIg> NGXIcFJqdmirYnn0d{B1cGViaX7keYN1cW:wIH;mJJAuW1SDVEOg[ZhxemW|c3nvci=> M{D3WVI{ODl2ME[3
SW1116 Mk\vSpVv[3Srb36gRZN{[Xl? NGrjcJcyODBiwsXNxsA> NHvmRZMzPC92OD:3NkBp NFfmcmZl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= NW\nPXlsOjJyNUC3PVA>
HT29 MkPZSpVv[3Srb36gRZN{[Xl? M{LZclExOCEEtV5CpC=> NHv0NHgzPC92OD:3NkBp MXTk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? MlizNlIxPTB5OUC=
SW1116 NUXWTmhwTnWwY4Tpc44hSXO|YYm= NX3RSXBROTByINM1UeKh M13vSVI1NzR6L{eyJIg> M1PMRYRm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh NH;sU2wzOjB3MEe5NC=>
HT29 MXPGeY5kfGmxbjDBd5NigQ>? NFPUWlQyODBiwsXNxsA> MX6yOE81QC95MjDo NXPaU2l[\GWlcnXhd4V{KHSqZTDwV3RCXDNibHX2[Yx{KGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? MUOyNlA2ODd7MB?=
ARPE-19 MoW4SpVv[3Srb36gRZN{[Xl? M{niO|XDqM7:TR?= Mn\qN|DDqG2rbh?= M{TGWolvcGmkaYTzJGpCUzJicHjvd5Bpd3KrbHH0bY9v MXSyNVYzODl4Mx?=
HSC-T6 NHWyO2RCeG:ydH;zbZMhSXO|YYm= MVWxNOKh|ryP MVGyxsBpyqB? NF\QSVVqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> NYj1eHlrOjF|OU[5PVg>
HSC-T6 MlnrSpVv[3Srb36gRZN{[Xl? NV7a[pBTOTEEoN88US=> Mn65NuKhcMLi MVfpcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? MoLINlE{QTZ7OUi=
Hep-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG2NlUuOTByIN88US=> Mo\nNlQwPDhxN{KgbC=> NVnFe2w{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MmTSNlE{ODl2OEG=
Hep-2 M2LBdGFxd3C2b4Ppd{BCe3OjeR?= M{DsW|UxKM7:TR?= MoHmNlQwPDhxN{KgbC=> MXnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHSrbXWg[IVx\W6mZX70cJk> NHO5bmszOTNyOUS4NS=>
Hep-2 M1HCfWZ2dmO2aX;uJGF{e2G7 NI\ob4U2OCEQvF2= NFjKdWYzPC92OD:3NkBp NVzUNWJwcW6qaXLpeJMhTzFidH:gV{Bk\WyuIHP5Z4xmKHS{YX7zbZRqd25iYX7kJIlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MYWyNVMxQTR6MR?=
Hep-2 NULQTG5nTnWwY4Tpc44hSXO|YYm= MXK1NEDPxE1? NX75VnZMOjRxNEivO|IhcA>? NI\4T25ld3ewcnXneYxifGW|IITo[UBUXEGWMzygdE1UXEGWMzDhcoQhe3W{dnn2bY4heHKxdHXpckBt\X[nbIO= M3:0OFIyOzB7NEix
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HEL  MUDGeY5kfGmxbjDBd5NigQ>? Mnn4NVAxyqEQvF2= MU[xNk04OiCq MYrpcohq[mm2czD0bIUhdGW4ZXygc4YheC2MQVuyMEBLSUt{ NH7aNHUzODZ{MUC2NS=>
HEL M2j6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxNFDDqM7:TR?= NEHtVpgxNTViZB?= M33IXpJm\HWlZYOg[5Jwf3SqIH;mJGpCUzKYNkG3Sk1mgHC{ZYPzbY5oKEiHTDDj[Yxtew>? MnHMNlA3OjFyNkG=
A-172 MnzkSpVv[3Srb36gRZN{[Xl? Ml;OOVAwOTBywrFOwG0> NGTM[3I1QCCq NG\COG9z\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> Mlj5NlA2QDl3MkW=
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MZ-256 MonJSpVv[3Srb36gRZN{[Xl? NVHFXWpxPTBxMUCwxsDPxE1? NWjKUlRKPDhiaB?= MlHqdoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u NYfCcm0zOjB3OEm1NlU>
MZ-304 NFPIUm5HfW6ldHnvckBCe3OjeR?= MYq1NE8yODEEoN88US=> NFqwZ|E1QCCq MlfrdoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u M3rWdlIxPTh7NUK1
A-172 NXvlfGVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYe1NE8yODEEoN88US=> NXfNOFNHPDhiaB?= MnXLcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq NV3mWWN3OjB3OEm1NlU>
MZ-18 MlrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzYZYtMPTBxMUCwxsDPxE1? M4jIRVQ5KGh? NXzwdXQ2dGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MYCyNFU5QTV{NR?=
MZ-54 NH;qTHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDTW5k2OC9zMEFCpO69VQ>? MVK0PEBp M3jtToxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NYXBd3NIOjB3OEm1NlU>
MZ-256 NXPE[mlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjOU|k5PTBxMUCwxsDPxE1? NVWz[XlSPDhiaB?= NXPpVIVHdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MnfGNlA2QDl3MkW=
MZ-304 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUG1NE8yODEEoN88US=> M{L6RVQ5KGh? NVz0WlAydGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MX2yNFU5QTV{NR?=
A-172 M4H1PGZ2dmO2aX;uJGF{e2G7 NVXnfZltPTBxMUCwxsDPxE1? NHX1d|g1QCCq M2PpNIlvcGmkaYTzJI1q\3KjdHnvci=> Ml3HNlA2QDl3MkW=
MZ-18 M3PwS2Z2dmO2aX;uJGF{e2G7 M4XvO|UxNzFyMNMg{txO MlrpOFghcA>? MXPpcohq[mm2czDtbYdz[XSrb36= NIPO[5czODV6OUWyOS=>
MZ-54 NYe4PWNOTnWwY4Tpc44hSXO|YYm= NIOwNXU2OC9zMEFCpO69VQ>? NInjOXo1QCCq NFn3VGhqdmirYnn0d{BucWe{YYTpc44> MWKyNFU5QTV{NR?=
MZ-256 NGqwTIhHfW6ldHnvckBCe3OjeR?= MXe1NE8yODEEoN88US=> M1fhe|Q5KGh? MXTpcohq[mm2czDtbYdz[XSrb36= MlLjNlA2QDl3MkW=
MZ-304 M{DSUWZ2dmO2aX;uJGF{e2G7 M{jTbFUxNzFyMNMg{txO MVS0PEBp NVzNOplPcW6qaXLpeJMhdWmpcnH0bY9v NEnsSYszODV6OUWyOS=>
A-172 NWXJOnoxTnWwY4Tpc44hSXO|YYm= M2m4blExOMLizszN M3TaSVQ5KGh? NX60d5pscW6qaXLpeJMhcW64YYPpc44> NIrYfoEzODV6OUWyOS=>
MZ-18 MX7GeY5kfGmxbjDBd5NigQ>? MnPNNVAxyqEQvF2= MmK1OFghcA>? NVfJbHJucW6qaXLpeJMhcW64YYPpc44> NWrxTWt5OjB3OEm1NlU>
MZ-54 NEPs[3FHfW6ldHnvckBCe3OjeR?= M1[zdlExOMLizszN NYnVbIQ2PDhiaB?= NE\aVotqdmirYnn0d{Bqdn[jc3nvci=> NHLNWlQzODV6OUWyOS=>
MZ-256 MVLGeY5kfGmxbjDBd5NigQ>? NEe4WVQyODEEoN88US=> MVG0PEBp NVS4OY9IcW6qaXLpeJMhcW64YYPpc44> MmD0NlA2QDl3MkW=
MZ-304 Mnu2SpVv[3Srb36gRZN{[Xl? M2naVlExOMLizszN NWry[YhbPDhiaB?= MnOwbY5pcWKrdIOgbY53[XOrb36= NWHKV|l5OjB3OEm1NlU>
A-172 NWnhNnlWTnWwY4Tpc44hSXO|YYm= MYm1NE8yODEEoN88US=> M{i5flQ5KGh? NEnvbXhz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MWSyNFU5QTV{NR?=
MZ-18 NVzPXm1qTnWwY4Tpc44hSXO|YYm= M2fTd|UxNzFyMNMg{txO M3nGNlQ5KGh? MVPy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz MV:yNFU5QTV{NR?=
MZ-54 MlfXSpVv[3Srb36gRZN{[Xl? MYG1NE8yODEEoN88US=> MYS0PEBp M3HpeJJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MV6yNFU5QTV{NR?=
MZ-256 M3HRcWZ2dmO2aX;uJGF{e2G7 M3PmPVUxNzFyMNMg{txO MkPxOFghcA>? NHjXOmVz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MYiyNFU5QTV{NR?=
MZ-304 MlXESpVv[3Srb36gRZN{[Xl? NIjVflM2OC9zMEFCpO69VQ>? NXK4NGJOPDhiaB?= NHnZb4Fz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M3nITVIxPTh7NUK1
SW1990 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPqfY9MOjBizszN MnLINlQwPDhxN{KgbC=> MV\pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NH7YR|YzODR6Mki1PC=>
SW1990 NEm5XJdHfW6ldHnvckBCe3OjeR?= MXiyNEDPxE1? Mn\iNlQhcA>? MXTk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gUW1RNTJiYX7kJHZGT0ZibWLORZM> MWWyNFQ5Ojh3OB?=
SW1990 NEG2c|lHfW6ldHnvckBCe3OjeR?= M3q5NlIxKM7:TR?= NUnuc21COjRiaB?= NH7FfJBl\WO{ZXHz[ZMhfGinIHnueIVve2m2eTDv[kBxNVO2YYSzJIV5eHKnc4Ppc44> NYHke2ViOjB2OEK4OVg>
SW1990 NEHlW2dKdn[jc3nvckBCe3OjeR?= Ml;VNlAh|ryP MWOyOEBp NVnufXBIemWmdXPld{Bqdn[jc3nvckBw\iCVV{G5PVAh[2WubIRCpC=> NHnETXAzODR6Mki1PC=>
THP1 M1PWUWZ2dmO2aX;uJGF{e2G7 M36xbFExKHWP MoT5N|AhdWmwwrC= NYDrfWNpcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wIHL5JI93\XJiNkCl MnjhNlA{QTN4OUC=
BMMC MluxSpVv[3Srb36gRZN{[Xl? Ml\uNE0yOCEQvF2= MYGxOeKhdWmw Mkn0bY5pcWKrdIOgUHREPMLicnXs[YF{\SCrbjDhJIRwe2VvZHXw[Y5l\W62IH\hd4hqd25id3n0bEBv\WG{IHPvcZBt\XSnIHnubIljcXSrb36gZZQh[2:wY3XueJJifGmxboOg5sm,OTEEoN88US=> MWCxPVg{PTh2NR?=
A549 NGjpWVFHfW6ldHnvckBCe3OjeR?= MnjBNVUh|ryv NHvMSnYyKGh? MXzpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSxJI9vKHS7cn;zbY5mKDdyMTD3ZZMh\GW2ZXP0[YQhOTVibXnuJIFnfGW{IGPQSUBDKHS{ZXH0cYVvfA>? NX;pXYxUOTl6MEG2OlU>
OVCAR-3 M1\xbmZ2dmO2aX;uJGF{e2G7 MWexNEB2VQ>? MXWxJIg> M3u4RolvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= MX[xPVY1PzN4Mx?=
PA-1 NX;uRlR3TnWwY4Tpc44hSXO|YYm= MWSxNEB2VQ>? NGLsRpcyKGh? M1HBdIlvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= MYmxPVY1PzN4Mx?=
OVCAR-3 NYToelhbTnWwY4Tpc44hSXO|YYm= M2H3RVExKHWP MkDWNUBp M{n6T4lvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 MlLwNVk3PDd|NkO=
PA-1 M{SxfGZ2dmO2aX;uJGF{e2G7 NXHKNVBKOTBidV2= M13tdVEhcA>? NGG0NotqdmirYnn0d{AhVFCDLXnu[JVk\WRib4\hdolidiClYX7j[ZIh[2WubDDtc5RqdGm2eR?= NW\uVo5DOTl4NEezOlM>
Jurkat  M1LKOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHS3SYw2OCEQvF2= M3u0RVI1NzR6L{eyJIg> Mnjj[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u MnfzNVk2PjR6OUG=
SUPT1  M3PIbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXxN3c2OCEQvF2= NXrXR4JYOjRxNEivO|IhcA>? NGKyU5hmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> MkTrNVk2PjR6OUG=
Jurkat  NXHIbIpjSXCxcITvd4l{KEG|c3H5 MojJOVAh|ryP MUCyOE81QCCq NFLBUYxmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ Mli4NVk2PjR6OUG=
SUPT1  M2nDc2Fxd3C2b4Ppd{BCe3OjeR?= MV[1NEDPxE1? NXPWcopVOjRxNEigbC=> MYLlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz NXL5VHV{OTl3NkS4PVE>
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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[2]

  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 294.30
Formula

C17H14N2O3

CAS No. 133550-30-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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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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