AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

108 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.

Selleck's AG-490 (Tyrphostin B42) has been cited by 108 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 MYfGeY5kfGmxbjDBd5NigQ>? MYmxNFDjiIoEtV2= M{fuVVI1KGh? MXzt[YRq[XSnczDQSWwh[2WubDDhdI9xfG:|aYO= MXmyOlE5PDl7OR?=
BCBL1 NH[3NnVHfW6ldHnvckBCe3OjeR?= NG\mZnQyODEkgJpCuW0> M1jTV|I1KGh? NFv0VlBu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NFfnb3QzPjF6NEm5PS=>
BC3 M2[yNWZ2dmO2aX;uJGF{e2G7 Mk\RNVAx6oDLwsXN M4nCRlI1KGh? NYTNNI5QdWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMTDy[YR2[3Srb36= MV[yOlE5PDl7OR?=
BCBL1 M324SWZ2dmO2aX;uJGF{e2G7 NVfJOHVMOTBy4pEJxtVO NHzaVYkzPCCq M3PlZo1m\GmjdHXzJIRmNXCqb4PwbI9zgWyjdHnvckBw\iCVVFHUN{Bkd3K{ZXzheIVlKHerdHigTHNRPzBiYX7kJGhUTjJicnXkeYN1cW:w NYHJWVBROjZzOES5PVk>
BC3 MnnRSpVv[3Srb36gRZN{[Xl? NIDjdmYyODEkgJpCuW0> NYPK[VRSOjRiaB?= NYnGNHhUcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh NHrwXngzPjF6NEm5PS=>
BCBL1 NUe4SYhZTnWwY4Tpc44hSXO|YYm= M4XMVlExOOLCidM1US=> MnraNlQhcA>? NULGXnRXcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh MlywNlYyQDR7OUm=
SK-MEL-28 NV7sd5ExTnWwY4Tpc44hSXO|YYm= MX[1NE8yODEkgJpCuW0> MlvmOFghcA>? NYfxfWNWTE2VTx?= M{m0fZJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl NUXNb3c3OjV{MU[1NlI>
MeWo MXTGeY5kfGmxbjDBd5NigQ>? NXnwe4x3PTBxMUCw5qCKyrWP M1PTb|Q5KGh? M17ENWROW09? NHHh[Ytz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NIGwWoYzPTJzNkWyNi=>
SK-MEL-5 MXXGeY5kfGmxbjDBd5NigQ>? MXW1NE8yODEkgJpCuW0> MWG0PEBp M3Oyb2ROW09? NHPmXoRz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> M2W1OlI2OjF4NUKy
SK-MEL-2 NGfmOHNHfW6ldHnvckBCe3OjeR?= MWi1NE8yODEkgJpCuW0> M3y3TlQ5KGh? NFu1N2NFVVOR MV\y[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MnzuNlUzOTZ3MkK=
B16-F0 NFnSfYtHfW6ldHnvckBCe3OjeR?= M3nEZVUxNzFyMPMAjeK2VQ>? NFzkSI81QCCq M1f5WGROW09? M{nzTpJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M4r4blI2OjF4NUKy
TRPM2/HEK  NGTqNoNHfW6ldHnvckBCe3OjeR?= MlflNE4y6oDVMkZCpOK2VQ>? NVjkNY9lOTYEoH3pci=> MWXEUXNQ NHmw[Xlz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IEGuO:KhyrWP M1XaVFI2OTd7NUe0
U937  NIK5TJpHfW6ldHnvckBCe3OjeR?= NUHmW5M3OC5z4pETNlXDqML3TR?= MUexOeKhdWmw M3TESWROW09? NVT4e2g6emWmdXPld{BJOk9{LXnu[JVk\WRiQ3GyL4lv[3KnYYPlJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXyMEBidmRidHjlJGlEPTEEoI\hcJVmKHejczCwMlTDqML3TR?= M{DieVI2OTd7NUe0
TRPM2/HEK  M2rQVGZ2dmO2aX;uJGF{e2G7 MYqxNOKhyrWP MoHZOFDDqG2rbh?= M{LrbGROW09? NH7ROHhz\WS3Y3XzJHRTWE1{IHHjeIl3[XSrb36g[ZZmdiCjdDDobYdpKGOxbnPlcpRz[XSrb37zJI9nKEh{T{K= MoPoNlUyPzl3N{S=
GL37  MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmGzNE0yOMLiwsXN MnGxOFghcA>? M360T5N2eHC{ZYPz[ZMhVGFiZYjwdoV{e2mxbh?= NVL0d5Q3OjR7OUm2OVc>
NRK-52E M2T6bWZ2dmO2aX;uJGF{e2G7 NVXrfGM{OcLiwsXN NUnKfYRUOTBibXnu NETTNpBjdG:la4OgeIhmKHO2aX31cIF1d3K7IHXm[oVkfCCxZjDBcochUUlib36gVIF5NTJiZYjwdoV{e2mxbtMg M{TTZVI1PzFyNEKz
NRK-52E M1P3fmZ2dmO2aX;uJGF{e2G7 MmrhNeKhyrWP NFTZSWQyOCCvaX6= MkLEZoxw[2u|IFHu[{BKUSCrbnT1Z4VlKEOGMkSg[ZhxemW|c3nvci=> NEf4WZozPDdzMESyNy=>
HSC  NVLHWYhnTnWwY4Tpc44hSXO|YYm= MXmyNEDPxE1? MlrPNUBp M4rlPIFjem:pYYTld{B1cGViZHnm[oVz\W62aXHsJIVn\mWldIOgc4YhdGWydHnuJI9zKEGJRYO= MoTKNlQ3OTRzOUm=
EJ Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXu1NE85OCEQvF2= MYeyOE81QC95MjDo MmXSbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVSyOFU5PzB2OR?=
EJ M1;ZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\uV25TPTBxOECg{txO NXz6TYQ3PDhiaB?= MnfuZ4F2e2W|IGOtdIhie2ViYYLy[ZN1 M{TC[|I1PTh5MES5
EJ NVvEWnF{TnWwY4Tpc44hSXO|YYm= Ml\TOVAwQDBizszN Ml3POFghcA>? MWDkc5dvemWpdXzheIV{KGNvTYnjMEBkgWOuaX7ENUwhe3W{dnn2bY4h[W6mIG\FS2Yh\XiycnXzd4lwdnN? MXuyOFU5PzB2OR?=
HepG2 Ml7FSpVv[3Srb36gRZN{[Xl? M2PoXlUxNTVyMDFOwG0> NF[5PHY3OMLibXnu M3zKSolvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M{X4UVI1OjR{MES2
SGC7901 MoTvR4VtdCCYaXHibYxqfHliQYPzZZk> MXiwMVExOCEQvF2= NHT3NpQzPC92OD:3NkBp MkjuZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NX:ybHRCOjRzNUGyOVU>
AGS  M4LhdWNmdGxiVnnhZoltcXS7IFHzd4F6 MVmwMVExOCEQvF2= NU\mOJFUOjRxNEivO|IhcA>? MUDjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= NHHtTpUzPDF3MUK1OS=>
SGC7901 NVzLW29nTnWwY4Tpc44hSXO|YYm= NFXtdGw2OCEQvF2= Mk\INlQwPDhxN{KgbC=> MYP0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= NWHtVmxuOjRzNUGyOVU>
AGS  NWrJeI9UTnWwY4Tpc44hSXO|YYm= Mn\UOVAh|ryP M{LudlI1NzR6L{eyJIg> NXHnTVRMfGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> MVuyOFE2OTJ3NR?=
SGC7901 NXvYZXNUTnWwY4Tpc44hSXO|YYm= MUW1NEDPxE1? M3XafFI1NzR6L{eyJIg> NHvBR5F1cGViY4n0c5Bt[XOvaXOgcI9k[WyrenH0bY9vKG:oIIDKRWszKCiMQVuyJJBpd3OyaH;yfYxifGWmIHH0JJJme2mmdXXzJHR6ejFyMEegZY5lKFS7ckGwNFgqKGSnY4LlZZNm\CCjZoTldkBCTzR7MDD0doVifG2nboSg[o9zKDJ2IHHu[EA1QCCqcjygZpV1KHO2YYL0[YQhfG9icnXic5Vv\CCjdDC3NkBpeg>? NEC4UpgzPDF3MUK1OS=>
AGS  MUjGeY5kfGmxbjDBd5NigQ>? MXy1NEDPxE1? MmDrNlQwPDhxN{KgbC=> NV3MNHI5fGinIHP5eI9xdGG|bXnjJIxw[2GuaYrheIlwdiCxZjDwTmFMOiBqSlHLNkBxcG:|cHjvdplt[XSnZDDheEBz\XOrZIXld{BVgXJzMEC3JIFv\CCWeYKxNFA5MSCmZXPy[YF{\WRiYX\0[ZIhSUd2OUCgeJJm[XSvZX70JIZweiB{NDDhcoQhPDhiaIKsJIJ2fCC|dHHyeIVlKHSxIILlZo92dmRiYYSgO|IhcHJ? MorGNlQyPTF{NUW=
MC3T3-E1  NXvPXFdmTnWwY4Tpc44hSXO|YYm= NVPOO|NEPTBizszN MXG0JIg> NYnRRmZWcW6qaXLpeJMhUFOHLXnu[JVk\WRiQl3QO{BidmRiR1jSJJBzd3SnaX6g[ZhxemW|c3nvcuKh MXyyN|g4Pzd|NB?=
7TD1-DXM NULDNZl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS0NVAh|ryP MmPEO|IhcA>? NUTGeXpjTE2VTx?= NG\yXJNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUWyN|g4OTF3OR?=
7TD1-WD-90 NULKOVlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXFNVAh|ryP MYG3NkBp Moj5SG1UVw>? MYnpcohq[mm2czDj[YxtKGe{b4f0bC=> NHPnTVIzOzh5MUG1PS=>
7TD1-DXM NV3rfZY6SXCxcITvd4l{KEG|c3H5 NFvFO5c2OCEQvF2= MU[0PEBp NWTTVJl[TE2VTx?= NHqxfphqdmS3Y3XzJIFxd3C2b4Ppdy=> MWGyN|g4OTF3OR?=
7TD1-WD-90 MXvBdI9xfG:|aYOgRZN{[Xl? NF:4XVk2OCEQvF2= MmDJOFghcA>? M16xbmROW09? MV\pcoR2[2W|IHHwc5B1d3Orcx?= NVrKPJVoOjN6N{GxOVk>
7TD1-WD-90  NX3Fc2JFTnWwY4Tpc44hSXO|YYm= MWW1NEDPxE1? NV;QVmd6PiCq M1;PPGROW09? NG\Ud4F{cWewaX\pZ4FvfGy7IHnubIljcXS|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhUkGNMjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSz MmDHNlM5PzFzNUm=
HepG2  NXjvbGRXTnWwY4Tpc44hSXO|YYm= MUGxNFAh|ryP MkHjNVIwOjRiaB?= M1rVNYlvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdg>? Mn3zNlM5OzZ2MEC=
RAW264.7  NHXG[2xHfW6ldHnvckBCe3OjeR?= MmDvOVDDqM7:TdMg MV:yOE81QCCq Mo\ud5VxeHKnc4Pld{BTSU6NTD3pcoR2[2WmIH;zeIVw[2yjc4Tv[4Vv\XOrcx?= NGTDd2EzOzZ4NUCxPC=>
RAW264.7 M4nrZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYGzU4ZCOC13MNMg{txOyqB? M4\6NlQ5yqCq MmSybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> M33VbFI{PjZ3MEG4
RAW264.7 MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fnd|AuPTEEoN88UeKh M2LvXVQ5yqCq M3L3dYNifXOnczDhckBienKnc4Sgc4YhWkGZMk[0Mlch[2WubIOgZZQhfGinIFewM2cyKHCqYYPlJI9nKHSqZTDj[YxtKGO7Y3zl MWSyN|Y3PTBzOB?=
RAW264.7 M4ixVGZ2dmO2aX;uJGF{e2G7 M4fxeFUxyqEQvF2= NFLGcG0zPC92ODDo NXuyb5J{cW6qaXLpeJMhWkGQS1ytbY5lfWOnZDDOSmFV[zFiZYjwdoV{e2mxbjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKFOnckeyO3NVSVR| MkOwNlM3PjVyMUi=
A549  MmDGSpVv[3Srb36gRZN{[Xl? MmPGNlAwPDBizszN NUO4c29HOjBiaB?= MknTNlAh|ryPIFHHOFkxKHO3cIDy[ZN{\XNidHjlJJJi\GmjdHnvck1qdmS3Y3XkJIlvfmG|aX;uJI9nKEF3NEmgZ4VtdHN? MUmyN|YzODF7MR?=
A549  NGLR[2RHfW6ldHnvckBCe3OjeR?= Mm[yNVAwOjBxNECg{txO MVGyOEBp M2rEc5N2eHC{ZYPz[ZMhfGinIILh[IlifGmxbj3pcoR2[2WmIHXs[ZZifGmxbjDv[kBXTUeIwrC= NV\yT2lVOjN4MkCxPVE>
HUVECs MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkTCNlAhyrWP NFXKRpg1KGh? NIP4T5NifHSnboXheIV{KEh{T{KtbY5lfWOnZDDj[YxtKHOqcnnub4Fo\SCjbnSgbY1xem:4ZXSgeIhmKGG2dHHjbI1mdnRicnH0[UBw\iC2aHWgZ4VtdHN? M1\NelI{PDh|OUS2
HUVECs M1uwSWFxd3C2b4Ppd{BCe3OjeR?= NGS0e|AzOCEEtV2= NWDGRmVZPCCq NVLafoJ2e2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 M4LjUFI{PDh|OUS2
BV-2  MlPGSpVv[3Srb36gRZN{[Xl? NYT0Nmh1OjBiwsXN NIDzPJgyPiCq M37URolvcGmkaYTzJGxRWy2rbnT1Z4VlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKGGubX;zeEBkd22ybHX0[Yx6KGSrbXnubZNp\WRiaV7PV{BmgHC{ZYPzbY9v MYGyN|I{PjN5MB?=
NRK-52E  M3rLN2Z2dmO2aX;uJGF{e2G7 MUS1xsDPxE1? MWezNOKhdWmw NGKwW4hifHSnboXheIV{KEGwZz2oNgKBmzdrLXnubIljcXSnZDDUS2Yu|rJzIH3SUmEh[XRiMUdCpIjDqA>? NH3JNXQzOzF5NEe1Oy=>
SW620  NXXicpY2TnWwY4Tpc44hSXO|YYm= NFjyfIMzOCEEtV2= NHrWVo4yNzZiaB?= NEj2fJdqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> MXSyN|EyODZ{NR?=
RPE  M17VeWZ2dmO2aX;uJGF{e2G7 MoG3N|AhyrWPwrC= Mlz4N{Bp NIflcWdqdmirYnn0d{B1cGViaX7keYN1cW:wIH;mJJAuW1SDVEOg[ZhxemW|c3nvci=> MVqyN|A6PDB4Nx?=
SW1116 MXTGeY5kfGmxbjDBd5NigQ>? M3f6O|ExOCEEtV5CpC=> MWeyOE81QC95MjDo NGfMNIdl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhUkGNMjDhcoQheEqDS{KgeIlu\S2mZYDlcoRmdnSueR?= NWTn[2p1OjJyNUC3PVA>
HT29 MVjGeY5kfGmxbjDBd5NigQ>? MV2xNFAhyrWPwrC= M4P2Z|I1NzR6L{eyJIg> MUHk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? NX60VXRJOjJyNUC3PVA>
SW1116 NFfOR2xHfW6ldHnvckBCe3OjeR?= MkP3NVAxKML3TdMg NX\mbYVOOjRxNEivO|IhcA>? MVjk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> NEPZTnUzOjB3MEe5NC=>
HT29 M33WXmZ2dmO2aX;uJGF{e2G7 NIe0NGQyODBiwsXNxsA> Mo\5NlQwPDhxN{KgbC=> MnLx[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> M3\LOVIzODVyN{mw
ARPE-19 NVKwd|htTnWwY4Tpc44hSXO|YYm= NEm2[ZY2yqEQvF2= NW\wcWhPOzEEoH3pci=> M2\kXIlvcGmkaYTzJGpCUzJicHjvd5Bpd3KrbHH0bY9v MWGyNVYzODl4Mx?=
HSC-T6 M{HIcmFxd3C2b4Ppd{BCe3OjeR?= M3rZeVExyqEQvF2= MX6yxsBpyqB? NFLFNFlqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> MYGyNVM6Pjl7OB?=
HSC-T6 NX3IOmk2TnWwY4Tpc44hSXO|YYm= NXrDOYtyOTEEoN88US=> NFj0fJQzyqCqwrC= MUXpcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? M3XyNVIyOzl4OUm4
Hep-2 NV71XXoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXGO5gzPS1zMECg{txO NI\wPVYzPC92OD:3NkBp M2HjZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M17ZTVIyOzB7NEix
Hep-2 Mo\MRZBweHSxc3nzJGF{e2G7 MUW1NEDPxE1? NX;yO|NzOjRxNEivO|IhcA>? MX3pcoR2[2W|IHPlcIwh[XCxcITvd4l{KHSrbXWg[IVx\W6mZX70cJk> NVz2PFNsOjF|MEm0PFE>
Hep-2 MUfGeY5kfGmxbjDBd5NigQ>? MoTkOVAh|ryP NGLqbnQzPC92OD:3NkBp NGXYOIJqdmirYnn0d{BIOSC2bzDTJINmdGxiY4njcIUhfHKjboPpeIlwdiCjbnSgbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> MUOyNVMxQTR6MR?=
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KF8 NFnzcHVHfW6ldHnvckBCe3OjeR?= NWPTZpVnOTEEoN88UeKh NGrH[pIyyqCqwrC= Mn:0SG1UV8Li M1PvfIlvcGmkaYTzJGlNNTN|LXnu[JVk\WRiSd86Ru6yKGSnZ4Lh[IF1cW:wIHHu[EBPTi4QulKgZYN1cX[jdHnvci=> MW[yNFk1ODB2NR?=
HEL  NWS3N5BQTnWwY4Tpc44hSXO|YYm= MVexNFDDqM7:TR?= NGrVR3kyOi15MjDo NUftdGZicW6qaXLpeJMhfGinIHzleoVtKG:oIICtTmFMOixiSlHLNi=> MXKyNFYzOTB4MR?=
HEL Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljaNVAxyqEQvF2= NYXUbIdVOC13IHS= NHqwOHZz\WS3Y3XzJIdzd3e2aDDv[kBLSUt{Vk[xO2Yu\XiycnXzd4lv\yCKRVygZ4VtdHN? M2jMdVIxPjJzME[x
A-172 NY\NZ5NuTnWwY4Tpc44hSXO|YYm= NVzSO3RYPTBxMUCwxsDPxE1? NHLZTo81QCCq NUHpW2VOemWmdXPld{B1cGVibHX2[Yx{KG:oIHPvcpN1cXS3dHn2[Yx6KGGldHn2ZZRm\CCVVFHUN{BqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCoYYPobY9v MYSyNFU5QTV{NR?=
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MZ-304 NVfrdoxnTnWwY4Tpc44hSXO|YYm= MXW1NE8yODEEoN88US=> MYO0PEBp MofodoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u NGLIO3MzODV6OUWyOS=>
A-172 NHS5OoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYW1NE8yODEEoN88US=> MYK0PEBp M3;oe4xm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= M2O4N|IxPTh7NUK1
MZ-18 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ftbVUxNzFyMNMg{txO M4HkOFQ5KGh? MXzs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? NGLlNYwzODV6OUWyOS=>
MZ-54 NIqyd5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInCTGw2OC9zMEFCpO69VQ>? NVTjdXhOPDhiaB?= MVjs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? M4DpfFIxPTh7NUK1
MZ-256 NGHBfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;nW3RRPTBxMUCwxsDPxE1? MkHOOFghcA>? M4HHWIxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= MUGyNFU5QTV{NR?=
MZ-304 NFO3bm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HXfVUxNzFyMNMg{txO MX[0PEBp NYrGdmVTdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo NXO5O2pFOjB3OEm1NlU>
A-172 M33C[2Z2dmO2aX;uJGF{e2G7 M{ntTlUxNzFyMNMg{txO MoHQOFghcA>? NWPzdHIycW6qaXLpeJMhdWmpcnH0bY9v NYLFdYVUOjB3OEm1NlU>
MZ-18 M1LSUGZ2dmO2aX;uJGF{e2G7 NFrB[2M2OC9zMEFCpO69VQ>? M{fzR|Q5KGh? MkD4bY5pcWKrdIOgcYloemG2aX;u NVX1R4ZDOjB3OEm1NlU>
MZ-54 NUXibGQ6TnWwY4Tpc44hSXO|YYm= NGfRVpg2OC9zMEFCpO69VQ>? MVi0PEBp MWXpcohq[mm2czDtbYdz[XSrb36= M37jV|IxPTh7NUK1
MZ-256 M2XHT2Z2dmO2aX;uJGF{e2G7 MlrzOVAwOTBywrFOwG0> NGL2SHE1QCCq NXLVfGdkcW6qaXLpeJMhdWmpcnH0bY9v NHzzNmMzODV6OUWyOS=>
MZ-304 NEXiPYRHfW6ldHnvckBCe3OjeR?= M{eyfFUxNzFyMNMg{txO M1nVSlQ5KGh? M3;q[olvcGmkaYTzJI1q\3KjdHnvci=> MoLONlA2QDl3MkW=
A-172 NEPLT25HfW6ldHnvckBCe3OjeR?= MXOxNFDDqM7:TR?= MVO0PEBp MknXbY5pcWKrdIOgbY53[XOrb36= MmLvNlA2QDl3MkW=
MZ-18 Ml35SpVv[3Srb36gRZN{[Xl? MmCwNVAxyqEQvF2= Ml;OOFghcA>? MnPsbY5pcWKrdIOgbY53[XOrb36= MlTqNlA2QDl3MkW=
MZ-54 M1Hnb2Z2dmO2aX;uJGF{e2G7 M3XRPVExOMLizszN NH\UcG41QCCq NEe1XW5qdmirYnn0d{Bqdn[jc3nvci=> MWeyNFU5QTV{NR?=
MZ-256 NHXDSohHfW6ldHnvckBCe3OjeR?= MVGxNFDDqM7:TR?= MYS0PEBp MojCbY5pcWKrdIOgbY53[XOrb36= NG\IcmgzODV6OUWyOS=>
MZ-304 NVuwRVd{TnWwY4Tpc44hSXO|YYm= M2T4e|ExOMLizszN M365WFQ5KGh? NHzHWGFqdmirYnn0d{Bqdn[jc3nvci=> MVqyNFU5QTV{NR?=
A-172 NXrqXWd[TnWwY4Tpc44hSXO|YYm= MmnLOVAwOTBywrFOwG0> M3\a[FQ5KGh? NHLPdWFz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M{\ZUlIxPTh7NUK1
MZ-18 MWDGeY5kfGmxbjDBd5NigQ>? MkW2OVAwOTBywrFOwG0> NVX3fG13PDhiaB?= NEGyfnZz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ MXiyNFU5QTV{NR?=
MZ-54 NF;UZ2FHfW6ldHnvckBCe3OjeR?= M4LSflUxNzFyMNMg{txO NYLrS|JLPDhiaB?= MWLy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NVPlUmFFOjB3OEm1NlU>
MZ-256 NGraW|BHfW6ldHnvckBCe3OjeR?= M3O5[lUxNzFyMNMg{txO NVjUeYN1PDhiaB?= MYXy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz MXGyNFU5QTV{NR?=
MZ-304 MWDGeY5kfGmxbjDBd5NigQ>? MlviOVAwOTBywrFOwG0> M{XQd|Q5KGh? MXvy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz M{PhRVIxPTh7NUK1
SW1990 NH\6XGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVi2O2MyOjBizszN NXfSV|M2OjRxNEivO|IhcA>? MoW1bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MoKxNlA1QDJ6NUi=
SW1990 MUnGeY5kfGmxbjDBd5NigQ>? NIrjSo8zOCEQvF2= NULrUVJ4OjRiaB?= Mnnh[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJG1OWC1{IHHu[EBXTUeIIH3SUmF{ Mn7hNlA1QDJ6NUi=
SW1990 M2rQTWZ2dmO2aX;uJGF{e2G7 NIPubJEzOCEQvF2= M4X5cFI1KGh? Mnu2[IVkemWjc3XzJJRp\SCrboTlcpNqfHlib3[gdE1UfGG2MzDlfJBz\XO|aX;u MknQNlA1QDJ6NUi=
SW1990 NEXqTJRKdn[jc3nvckBCe3OjeR?= NVexSXUzOjBizszN NWHyS5V{OjRiaB?= M4Dmc5Jm\HWlZYOgbY53[XOrb36gc4YhW1dzOUmwJINmdGy|wrC= NHnve4czODR6Mki1PC=>
THP1 NF:3R|dHfW6ldHnvckBCe3OjeR?= MXixNEB2VQ>? MkfkN|AhdWmwwrC= MXrpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44h[nlib4\ldkA3OCV? NF:4dIczODN7M{[5NC=>
BMMC MkKySpVv[3Srb36gRZN{[Xl? Ml\INE0yOCEQvF2= MXyxOeKhdWmw NWnMTlJ3cW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? MYKxPVg{PTh2NR?=
A549 NWq1bHM{TnWwY4Tpc44hSXO|YYm= MmL3NVUh|ryv NWjNWoJoOSCq M4jSbYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiU2TBWFEhd25idInyc5NqdmViN{CxJJdieyCmZYTlZ5Rm\CBzNTDtbY4h[W[2ZYKgV3BGKEJidILlZZRu\W62 NXrSRnE1OTl6MEG2OlU>
OVCAR-3 M{jlXmZ2dmO2aX;uJGF{e2G7 MkPhNVAhfU1? NGPwVXgyKGh? NIK4NYVqdmirYnn0d{BNWEFvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= MWGxPVY1PzN4Mx?=
PA-1 NYD4O4lKTnWwY4Tpc44hSXO|YYm= NGDlO|kyOCC3TR?= NVq2S4dyOSCq NGjCVVJqdmirYnn0d{BNWEFvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= MmDqNVk3PDd|NkO=
OVCAR-3 MWPGeY5kfGmxbjDBd5NigQ>? MX[xNEB2VQ>? M1X4cVEhcA>? MWTpcohq[mm2czCgUHBCNWmwZIXj[YQhd3[jcnnhckBk[W6lZYKgZ4VtdCCvb4TpcIl1gQ>? M3;Hb|E6PjR5M{[z
PA-1 Mm[wSpVv[3Srb36gRZN{[Xl? MoHsNVAhfU1? MUOxJIg> NWntSJBrcW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= Mn3mNVk3PDd|NkO=
Jurkat  M3PNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHQOVAh|ryP MYKyOE81QC95MjDo NYLE[mVF\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v MlriNVk2PjR6OUG=
SUPT1  NFTwXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW1NEDPxE1? M1f0O|I1NzR6L{eyJIg> NWK4TIFt\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v MmThNVk2PjR6OUG=
Jurkat  NH7Je2JCeG:ydH;zbZMhSXO|YYm= NF3XZ4k2OCEQvF2= NXf3V4lbOjRxNEigbC=> NEHtdZVmdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ NIPGfXkyQTV4NEi5NS=>
SUPT1  NH;YTW9CeG:ydH;zbZMhSXO|YYm= M{T6e|UxKM7:TR?= Mon5NlQwPDhiaB?= Ml\C[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> MmX4NVk2PjR6OUG=

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

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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 SDS / COA (available on product pages).

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

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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

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

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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