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 43 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 NWGxRXJsTnWwY4Tpc44hSXO|YYm= M3LZdVExOOLCidM1US=> M2m5XVI1KGh? NIHlPGRu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NX7IdVhJOjZzOES5PVk>
BCBL1 NH32e3pHfW6ldHnvckBCe3OjeR?= MlLONVAx6oDLwsXN M2TR[VI1KGh? NXW3Ro5zdWWmaXH0[ZMhWEWOIHPlcIwh[XCxcITvd4l{ M132fVI3OTh2OUm5
BC3 MkjZSpVv[3Srb36gRZN{[Xl? MV2xNFDjiIoEtV2= NVXLZnc1OjRiaB?= M1;lZ41m\GmjdHXzJIRmNXCqb4PwbI9zgWyjdHnvckBw\iCVVFHUN{Bkd3K{ZXzheIVlKHerdHigTHNRPzBiYX7kJGhUTjFicnXkeYN1cW:w M1f3SlI3OTh2OUm5
BCBL1 MX3GeY5kfGmxbjDBd5NigQ>? MX:xNFDjiIoEtV2= M1npc|I1KGh? NEHiV|Vu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0Z{IILl[JVkfGmxbh?= M4\vPVI3OTh2OUm5
BC3 NEfWPJJHfW6ldHnvckBCe3OjeR?= MoDqNVAx6oDLwsXN MonoNlQhcA>? MkDqbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg M4PIPFI3OTh2OUm5
BCBL1 NXn3ZXp[TnWwY4Tpc44hSXO|YYm= MUexNFDjiIoEtV2= M3:0[lI1KGh? MmfFbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMh\my3eNMg NFL1UXAzPjF6NEm5PS=>
SK-MEL-28 MXHGeY5kfGmxbjDBd5NigQ>? MXW1NE8yODEkgJpCuW0> MoDzOFghcA>? M4TBZmROW09? NYe0PHFSemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> MVuyOVIyPjV{Mh?=
MeWo NHm0VI1HfW6ldHnvckBCe3OjeR?= Mk\SOVAwOTBy4pEJxtVO MWe0PEBp NHHSWWpFVVOR M1XYV5Jm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NGXtRYczPTJzNkWyNi=>
SK-MEL-5 M2\MXWZ2dmO2aX;uJGF{e2G7 NEnkblE2OC9zMEFihKnDvU1? M1LROFQ5KGh? M4L0RWROW09? NHuzUGhz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NVLmVHhXOjV{MU[1NlI>
SK-MEL-2 MoH2SpVv[3Srb36gRZN{[Xl? MmHHOVAwOTBy4pEJxtVO M4\ZeFQ5KGh? NXyyNZFTTE2VTx?= M3vpdpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M1Lpe|I2OjF4NUKy
B16-F0 NH;KVYVHfW6ldHnvckBCe3OjeR?= NV36[FJLPTBxMUCw5qCKyrWP MkPBOFghcA>? MV;EUXNQ NGfORVJz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NHLiXGczPTJzNkWyNi=>
TRPM2/HEK  NFu1OoRHfW6ldHnvckBCe3OjeR?= M4qzUlAvOeLCk{K1xsDDvU1? NILsNYwyPcLibXnu Mn\KSG1UVw>? MUHy[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDFwN9MgxtVO MYeyOVE4QTV5NB?=
U937  MoW1SpVv[3Srb36gRZN{[Xl? MXKwMlHjiJN{NdMgxtVO M4HtfVE2yqCvaX6= NFLjSVdFVVOR NEH2fFNz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IECuOOKhyrWP MVKyOVE4QTV5NB?=
TRPM2/HEK  NULCU|E5TnWwY4Tpc44hSXO|YYm= MnfCNVDDqML3TR?= NX65emtKPDEEoH3pci=> NYK1XHlKTE2VTx?= NX3yXnJWemWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y MknPNlUyPzl3N{S=
GL37  NFv3SmFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXHjVY1jOC1zMNMgxtVO Mn;tOFghcA>? NEfyV5V{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= M{no[|I1QTl7NkW3
NRK-52E NWTCb49oTnWwY4Tpc44hSXO|YYm= NYrMV3VOOcLiwsXN NFnmPXAyOCCvaX6= NUDXbIxK[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> NX7peVBkOjR5MUC0NlM>
NRK-52E NHjNTmdHfW6ldHnvckBCe3OjeR?= MU[xxsDDvU1? M4T4SFExKG2rbh?= MXPicI9kc3NiQX7nJGlKKGmwZIXj[YQhS0R{NDDlfJBz\XO|aX;u NULI[phoOjR5MUC0NlM>
HSC  MorhSpVv[3Srb36gRZN{[Xl? NI\sPFczOCEQvF2= M1fydVEhcA>? Mn35ZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= MmK2NlQ3OTRzOUm=
EJ M{fDcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnKOVAwQDBizszN NGTtbFAzPC92OD:3NkBp NHrJWmRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MViyOFU5PzB2OR?=
EJ MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfEWG1iPTBxOECg{txO M1HFWFQ5KGh? MWDjZZV{\XNiUz3wbIF{\SCjcoLld5Q> MlOyNlQ2QDdyNEm=
EJ M{G1[WZ2dmO2aX;uJGF{e2G7 MXG1NE85OCEQvF2= MX:0PEBp NVfBcXJK\G:5boLl[5Vt[XSnczDjMW16[yxiY4njcIlvTDFuIIP1dpZqfmmwIHHu[EBXTUeIIHX4dJJme3Orb37z NXT5cG1wOjR3OEewOFk>
HepG2 NU\aV3E4TnWwY4Tpc44hSXO|YYm= M1PJV|UxNTVyMDFOwG0> Mk\POlDDqG2rbh?= MojhbY5pcWKrdIOgeIhmKEmOLU[tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gV3RCXDFiKGT5dlcxPSliYX7kJHNVSVR|IDjUfZI4ODVrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mn7jNlQzPDJyNE[=
SGC7901 MlfiR4VtdCCYaXHibYxqfHliQYPzZZk> MV6wMVExOCEQvF2= NXvNU4JKOjRxNEivO|IhcA>? NFnXcYNk[XW|ZYOgZUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliZH;z[U1l\XCnbnTlcpRtgSCkdYSgco91KHSrbXWt[IVx\W6mZX70cJk> M1PseFI1OTVzMkW1
AGS  MlXvR4VtdCCYaXHibYxqfHliQYPzZZk> M3T2SlAuOTByIN88US=> NWD0fGhtOjRxNEivO|IhcA>? MnH4Z4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 M2L0UVI1OTVzMkW1
SGC7901 M{HBUmZ2dmO2aX;uJGF{e2G7 NVXUfGFjPTBizszN MW[yOE81QC95MjDo M3fLeJRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg Mn\ZNlQyPTF{NUW=
AGS  MlHnSpVv[3Srb36gRZN{[Xl? MnLYOVAh|ryP NX3Wc|BQOjRxNEivO|IhcA>? NGfuXpF1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> M4Hp[|I1OTVzMkW1
SGC7901 NXTjTI1WTnWwY4Tpc44hSXO|YYm= NEHlUZA2OCEQvF2= M4XxTFI1NzR6L{eyJIg> NVjOcXVlfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? MmDNNlQyPTF{NUW=
AGS  MkS0SpVv[3Srb36gRZN{[Xl? NVvRcG5EPTBizszN NHHxS2MzPC92OD:3NkBp NWPwe2dsfGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? M17SbFI1OTVzMkW1
MC3T3-E1  M1vBSWZ2dmO2aX;uJGF{e2G7 MV:1NEDPxE1? M1zPNFQhcA>? MYPpcohq[mm2czDIV2UucW6mdXPl[EBDVVB5IHHu[EBIUFJicILveIVqdiCneIDy[ZN{cW:wwrC= MlPzNlM5Pzd5M{S=
7TD1-DXM M1LmOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HUSVExKM7:TR?= NULxdWZWPzJiaB?= MnHPSG1UVw>? NInxc2JqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NVzjUYI5OjN6N{GxOVk>
7TD1-WD-90 NWOwO5FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H2NlExKM7:TR?= MVS3NkBp NGHNWWxFVVOR MVfpcohq[mm2czDj[YxtKGe{b4f0bC=> MmTQNlM5PzFzNUm=
7TD1-DXM NUn6TVU1SXCxcITvd4l{KEG|c3H5 MXO1NEDPxE1? NInLdXM1QCCq NWr0ZYhwTE2VTx?= NU[ye5hEcW6mdXPld{BieG:ydH;zbZM> MlLRNlM5PzFzNUm=
7TD1-WD-90 NFnaNFdCeG:ydH;zbZMhSXO|YYm= NEPVOWg2OCEQvF2= MlfDOFghcA>? NH7ZSoJFVVOR M4\kT4lv\HWlZYOgZZBweHSxc3nz NWnKNmduOjN6N{GxOVk>
7TD1-WD-90  NHrITIpHfW6ldHnvckBCe3OjeR?= M2j4VFUxKM7:TR?= MWC2JIg> MV7EUXNQ M4r1cpNq\26rZnnjZY51dHliaX7obYJqfHNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBLSUt{IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhW1SDVEO= MUSyN|g4OTF3OR?=
HepG2  MWPGeY5kfGmxbjDBd5NigQ>? MX6xNFAh|ryP MlrsNVIwOjRiaB?= MXfpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> Mlq5NlM5OzZ2MEC=
RAW264.7  NEnhPJVHfW6ldHnvckBCe3OjeR?= MVm1NOKh|ryPwrC= NYjzd49mOjRxNEigbC=> NFLjPI5{fXCycnXzd4V{KFKDTlvMMYlv\HWlZXSgc5N1\W:lbHHzeI9o\W6nc3nz MlH1NlM3PjVyMUi=
RAW264.7 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PBW|AuPTEEoN88UeKh MVm0POKhcA>? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnLXTldIVv\GWwdHz5 MoKxNlM3PjVyMUi=
RAW264.7 NEDyeGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOwMVUxyqEQvF5CpC=> NULwZ5duPDkEoHi= M2TFV4NifXOnczDhckBienKnc4Sgc4YhWkGZMk[0Mlch[2WubIOgZZQhfGinIFewM2cyKHCqYYPlJI9nKHSqZTDj[YxtKGO7Y3zl NEXUWIwzOzZ4NUCxPC=>
RAW264.7 NGHiNJFHfW6ldHnvckBCe3OjeR?= NH3Vcmk2OMLizszN M1vKPVI1NzR6IHi= M3jiNolvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? MoLYNlM3PjVyMUi=
A549  NEK1OphHfW6ldHnvckBCe3OjeR?= NGi0bmkzOC92MDFOwG0> NWrLWIV1OjBiaB?= M2Gx[lIxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| Ml60NlM3OjBzOUG=
A549  NHLTW2NHfW6ldHnvckBCe3OjeR?= M3vaflExNzJyL{SwJO69VQ>? MYqyOEBp NVTjVGlKe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> MXqyN|YzODF7MR?=
HUVECs MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmPrNlAhyrWP NYXoWHZpPCCq Ml20ZZR1\W63YYTld{BJOk9{LXnu[JVk\WRiY3XscEB{cHKrbnvh[4Uh[W6mIHntdJJwfmWmIITo[UBifHSjY3jt[Y51KHKjdHWgc4YhfGinIHPlcIx{ NHP3W4szOzR6M{m0Oi=>
HUVECs NWjhU4w2SXCxcITvd4l{KEG|c3H5 MmD6NlAhyrWP NWfnN4ZpPCCq M3PLXZNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBk\WyuIHHwc5B1d3SrYzDpcoRmgA>? NIHNNJozOzR6M{m0Oi=>
BV-2  MnPESpVv[3Srb36gRZN{[Xl? NIfSe3IzOCEEtV2= M{T4SlE3KGh? MoO3bY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> MWKyN|I{PjN5MB?=
NRK-52E  MVjGeY5kfGmxbjDBd5NigQ>? NH3pelk2yqEQvF2= NXXpT4liOzEEoH3pci=> NV;KNpE{[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? NGDnVXQzOzF5NEe1Oy=>
SW620  M4L5[mZ2dmO2aX;uJGF{e2G7 M3P2NFIxKML3TR?= MorONU83KGh? MWTpcohq[mm2czDwMXNVSVR|IHHjeIl3[XSrb36= Mk[3NlMyOTB4MkW=
RPE  NFPHcWFHfW6ldHnvckBCe3OjeR?= M1Hi[lMxKML3TdMg NVftb25qOyCq MV\pcohq[mm2czD0bIUhcW6mdXP0bY9vKG:oIICtV3RCXDNiZYjwdoV{e2mxbh?= MYWyN|A6PDB4Nx?=
SW1116 NXvIfW9UTnWwY4Tpc44hSXO|YYm= MVyxNFAhyrWPwrC= MoW5NlQwPDhxN{KgbC=> M2TFT4Rm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBLSUt{IHHu[EBxUkGNMjD0bY1mNWSncHXu[IVvfGy7 NIftSHAzOjB3MEe5NC=>
HT29 NFLvfGFHfW6ldHnvckBCe3OjeR?= MlPiNVAxKML3TdMg NX3reYhmOjRxNEivO|IhcA>? MoW1[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? Mn;ONlIxPTB5OUC=
SW1116 M17SW2Z2dmO2aX;uJGF{e2G7 MlPjNVAxKML3TdMg NHHrR2UzPC92OD:3NkBp MmnC[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> MVWyNlA2ODd7MB?=
HT29 NVvnbplnTnWwY4Tpc44hSXO|YYm= Mlz2NVAxKML3TdMg Mmf3NlQwPDhxN{KgbC=> NH;KUpJl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? NY\h[WR7OjJyNUC3PVA>
ARPE-19 NXu1S2lFTnWwY4Tpc44hSXO|YYm= M3\PR|XDqM7:TR?= MXqzNOKhdWmw NInOSJhqdmirYnn0d{BLSUt{IIDoc5NxcG:{aXzheIlwdg>? NH\4PVgzOTZ{MEm2Ny=>
HSC-T6 NGTGboRCeG:ydH;zbZMhSXO|YYm= MX2xNOKh|ryP MmDQNuKhcMLi MXTpcohq[mm2czD0bIUh[XCxcITvd4l{KG:oIFjTR{1VPiClZXzsd{BqdmS3Y3XkJIJ6KEOGRR?= MWKyNVM6Pjl7OB?=
HSC-T6 NGrjSWRHfW6ldHnvckBCe3OjeR?= MXuxNOKh|ryP Mn;mNuKhcMLi M2DtOIlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wczDv[kBxYS2VVFHUNUBidmRiQnHkJIlv\HWlZXSgZpkhS0SH MkLvNlE{QTZ7OUi=
Hep-2 NWXFeopDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nUNFI2NTFyMDFOwG0> NFixTXIzPC92OD:3NkBp MnO0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NI\tWXUzOTNyOUS4NS=>
Hep-2 M2XGemFxd3C2b4Ppd{BCe3OjeR?= MmX6OVAh|ryP MlKwNlQwPDhxN{KgbC=> MnfVbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC2aX3lJIRmeGWwZHXueIx6 MVuyNVMxQTR6MR?=
Hep-2 NX\BeIdwTnWwY4Tpc44hSXO|YYm= NVzYVIt5PTBizszN MWWyOE81QC95MjDo Mme4bY5pcWKrdIOgS|EhfG9iUzDj[YxtKGO7Y3zlJJRz[W6|aYTpc44h[W6mIHnu[JVk\XNiR{GgZ4VtdCCleXPs[UBienKnc4S= NICwflQzOTNyOUS4NS=>
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KF8 MWTGeY5kfGmxbjDBd5NigQ>? NV:1col7OTEEoN88UeKh MVyxxsBp MojUSG1UV8Li NHPk[5hqdmirYnn0d{BKVC1|Mz3pcoR2[2WmIF7GMe67SiCjY4TpeoF1cW:w M4e2e|IxQTRyMES1
KF8 Ml\oSpVv[3Srb36gRZN{[Xl? NVvjfIFNOTEEoN88UeKh M1XrUVHDqGkEoB?= MmPESG1UV8Li M2X6XolvcGmkaYTzJGlNNTN|LXnu[JVk\WRiSd86Ru6yKGSnZ4Lh[IF1cW:wIHHu[EBPTi4QulKgZYN1cX[jdHnvci=> NIXIbW0zODl2MEC0OS=>
HEL  NYHObYpKTnWwY4Tpc44hSXO|YYm= NGr2bVQyODEEoN88US=> MmfTNVIuPzJiaB?= NHHwV25qdmirYnn0d{B1cGVibHX2[Ywhd2ZicD3KRWszNCCMQVuy NUH0[|MzOjB4MkGwOlE>
HEL MlG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\Ce|ExOMLizszN MofBNE02KGR? M4HlNpJm\HWlZYOg[5Jwf3SqIH;mJGpCUzKYNkG3Sk1mgHC{ZYPzbY5oKEiHTDDj[Yxtew>? NUDuZo5mOjB4MkGwOlE>
A-172 MUDGeY5kfGmxbjDBd5NigQ>? NWjMeVJlPTBxMUCwxsDPxE1? MmjNOFghcA>? MmnRdoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u M{f6UVIxPTh7NUK1
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MZ-54 M1Tse2Z2dmO2aX;uJGF{e2G7 NXW1So9QPTBxMUCwxsDPxE1? M2LnXlQ5KGh? MoTFdoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u M3L3[FIxPTh7NUK1
MZ-256 M{jLSmZ2dmO2aX;uJGF{e2G7 Ml7mOVAwOTBywrFOwG0> NX;xbGROPDhiaB?= NFrPeJdz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NHTXZ4MzODV6OUWyOS=>
MZ-304 MXHGeY5kfGmxbjDBd5NigQ>? MUO1NE8yODEEoN88US=> NWjLNVJYPDhiaB?= MnzldoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u MnzuNlA2QDl3MkW=
A-172 MljhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX21NE8yODEEoN88US=> NUfkPHJtPDhiaB?= MUns[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? NHftbpozODV6OUWyOS=>
MZ-18 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HkSlUxNzFyMNMg{txO NVLMN|cyPDhiaB?= M{KxfIxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= MU[yNFU5QTV{NR?=
MZ-54 NFTKZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYK1NE8yODEEoN88US=> NUPNWIZKPDhiaB?= M{PTcYxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= M4LjdlIxPTh7NUK1
MZ-256 M2HjfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD1OVAwOTBywrFOwG0> MnrrOFghcA>? NES1RpJt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= NFfQb4QzODV6OUWyOS=>
MZ-304 MlTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jneFUxNzFyMNMg{txO NIKxUXk1QCCq MojtcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq MYiyNFU5QTV{NR?=
A-172 MmLBSpVv[3Srb36gRZN{[Xl? MnTnOVAwOTBywrFOwG0> M{fRd|Q5KGh? MV3pcohq[mm2czDtbYdz[XSrb36= NVfkO|JWOjB3OEm1NlU>
MZ-18 MnT6SpVv[3Srb36gRZN{[Xl? NF7YfIY2OC9zMEFCpO69VQ>? NYPT[2pQPDhiaB?= MWLpcohq[mm2czDtbYdz[XSrb36= M{myRlIxPTh7NUK1
MZ-54 M4DmRWZ2dmO2aX;uJGF{e2G7 MYO1NE8yODEEoN88US=> MkHWOFghcA>? NUjTfXdIcW6qaXLpeJMhdWmpcnH0bY9v M3\2WlIxPTh7NUK1
MZ-256 MVPGeY5kfGmxbjDBd5NigQ>? M3XMTlUxNzFyMNMg{txO Mmj2OFghcA>? M17DWolvcGmkaYTzJI1q\3KjdHnvci=> NHXYRYozODV6OUWyOS=>
MZ-304 MXfGeY5kfGmxbjDBd5NigQ>? M2XM[VUxNzFyMNMg{txO MlvNOFghcA>? MmrvbY5pcWKrdIOgcYloemG2aX;u M1nJNlIxPTh7NUK1
A-172 M1TyTmZ2dmO2aX;uJGF{e2G7 NFrNdJMyODEEoN88US=> NWjQT4Z7PDhiaB?= M2riTolvcGmkaYTzJIlvfmG|aX;u MlrlNlA2QDl3MkW=
MZ-18 MYHGeY5kfGmxbjDBd5NigQ>? M3jPe|ExOMLizszN NWHxVWg4PDhiaB?= MmHybY5pcWKrdIOgbY53[XOrb36= NHO5b4UzODV6OUWyOS=>
MZ-54 MXPGeY5kfGmxbjDBd5NigQ>? NXLKO2xLOTBywrFOwG0> M{L3RlQ5KGh? M1v6c4lvcGmkaYTzJIlvfmG|aX;u MmXWNlA2QDl3MkW=
MZ-256 NFTq[W5HfW6ldHnvckBCe3OjeR?= M3nXV|ExOMLizszN NUmyWXB4PDhiaB?= MVTpcohq[mm2czDpcpZie2mxbh?= MYGyNFU5QTV{NR?=
MZ-304 Ml7KSpVv[3Srb36gRZN{[Xl? MoPqNVAxyqEQvF2= NVvhd3RZPDhiaB?= MnTSbY5pcWKrdIOgbY53[XOrb36= NF3LRWwzODV6OUWyOS=>
A-172 MoDjSpVv[3Srb36gRZN{[Xl? MWO1NE8yODEEoN88US=> NWrTb2UzPDhiaB?= M3LtWZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MWqyNFU5QTV{NR?=
MZ-18 NGHWXphHfW6ldHnvckBCe3OjeR?= M3LHd|UxNzFyMNMg{txO M2DmdVQ5KGh? NF65R29z\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MXqyNFU5QTV{NR?=
MZ-54 NVrV[VE3TnWwY4Tpc44hSXO|YYm= NX7PeGpMPTBxMUCwxsDPxE1? MYW0PEBp NITtcnZz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MX2yNFU5QTV{NR?=
MZ-256 NIL1SHlHfW6ldHnvckBCe3OjeR?= M4jUUFUxNzFyMNMg{txO MUi0PEBp MnLGdoVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> NVeyV2JpOjB3OEm1NlU>
MZ-304 NX32e40yTnWwY4Tpc44hSXO|YYm= NXXzOIRtPTBxMUCwxsDPxE1? NILFSGE1QCCq MVPy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz M3zO[lIxPTh7NUK1
SW1990 NXnCRpczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDNdmpXOjBizszN MnP3NlQwPDhxN{KgbC=> NEnVbpBqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NFHwVGYzODR6Mki1PC=>
SW1990 Mni1SpVv[3Srb36gRZN{[Xl? NH;QeG0zOCEQvF2= NEnCOYMzPCCq NWXHXYR{\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE2PUD2yJIFv\CCYRVfGJI1TVkG| Mn;DNlA1QDJ6NUi=
SW1990 MknRSpVv[3Srb36gRZN{[Xl? MUGyNEDPxE1? NXzsUWxCOjRiaB?= M4XWUIRm[3KnYYPld{B1cGViaX70[Y5{cXS7IH;mJJAuW3SjdEOg[ZhxemW|c3nvci=> NHzNOXgzODR6Mki1PC=>
SW1990 M13F[GlvfmG|aX;uJGF{e2G7 M4DPOVIxKM7:TR?= NV30fXlROjRiaB?= MnjadoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= NXTqZVJmOjB2OEK4OVg>
THP1 NETWU2RHfW6ldHnvckBCe3OjeR?= M1ftZVExKHWP NIm4e3g{OCCvaX9CpC=> MYLpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44h[nlib4\ldkA3OCV? NILNXWYzODN7M{[5NC=>
BMMC M3zPSWZ2dmO2aX;uJGF{e2G7 M1rJbVAuOTBizszN MXWxOeKhdWmw NHvqZ|JqdmirYnn0d{BNXEN2wrDy[Yxm[XOnIHnuJIEh\G:|ZT3k[ZBmdmSnboSg[oF{cGmxbjD3bZRpKG6nYYKgZ49ueGyndHWgbY5pcWKrdHnvckBifCClb37j[Y51emG2aX;ud{Djsb5zMNMg{txO MoL6NVk5OzV6NEW=
A549 NGXyOJZHfW6ldHnvckBCe3OjeR?= NWjJeHVqOTVizszt M1HwTVEhcA>? NHT3UVBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQyKG:wIIT5do9{cW6nIEewNUB4[XNiZHX0[YN1\WRiMUWgcYlvKGGodHXyJHNRTSCEIITy[YF1dWWwdB?= MnvUNVk5ODF4NkW=
OVCAR-3 M{nKe2Z2dmO2aX;uJGF{e2G7 MUKxNEB2VQ>? MlnTNUBp NV\rU4R5cW6qaXLpeJMhVFCDLXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;u M2X2R|E6PjR5M{[z
PA-1 MVjGeY5kfGmxbjDBd5NigQ>? M2L0WFExKHWP NETCc4YyKGh? MXHpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? MoTXNVk3PDd|NkO=
OVCAR-3 NIXMTndHfW6ldHnvckBCe3OjeR?= Mn2yNVAhfU1? NIHTbFMyKGh? NILZWHFqdmirYnn0d{AhVFCDLXnu[JVk\WRib4\hdolidiClYX7j[ZIh[2WubDDtc5RqdGm2eR?= NHzhZnAyQTZ2N{O2Ny=>
PA-1 MmC0SpVv[3Srb36gRZN{[Xl? NYDJVmtwOTBidV2= M3nxTFEhcA>? MXPpcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? Ml\iNVk3PDd|NkO=
Jurkat  NXXEVJJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[1NEDPxE1? MlvtNlQwPDhxN{KgbC=> NEG1S25mdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44> NIra[2syQTV4NEi5NS=>
SUPT1  MnXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF65N4E2OCEQvF2= M170UlI1NzR6L{eyJIg> M3faT4VvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> MYexPVU3PDh7MR?=
Jurkat  MVnBdI9xfG:|aYOgRZN{[Xl? NFrF[GU2OCEQvF2= NULZS45MOjRxNEigbC=> Mo\B[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> NF3qOmYyQTV4NEi5NS=>
SUPT1  MWXBdI9xfG:|aYOgRZN{[Xl? NUjoNFJXPTBizszN M3;rTVI1NzR6IHi= Mmfr[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> NVH1S4ZMOTl3NkS4PVE>

... 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
  • 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