AG-490 (Tyrphostin B42)

For research use only.

Catalog No.S1143 Synonyms: Zinc02557947

72 publications

AG-490 (Tyrphostin B42) Chemical Structure

Molecular Weight(MW): 294.30

AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

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Selleck's AG-490 (Tyrphostin B42) has been cited by 72 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
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 Mkf5SpVv[3Srb36gRZN{[Xl? NVeyNnVtOTBy4pEJxtVO NF;pTpYzPCCq M2jITY1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> MYGyOlE5PDl7OR?=
BCBL1 Ml\GSpVv[3Srb36gRZN{[Xl? NFnLN3YyODEkgJpCuW0> MXGyOEBp M4XBV41m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> M3TEdFI3OTh2OUm5
BC3 M3v4NGZ2dmO2aX;uJGF{e2G7 NX;2bXRIOTBy4pEJxtVO MofXNlQhcA>? M1HvdY1m\GmjdHXzJIRmNXCqb4PwbI9zgWyjdHnvckBw\iCVVFHUN{Bkd3K{ZXzheIVlKHerdHigTHNRPzBiYX7kJGhUTjFicnXkeYN1cW:w MVGyOlE5PDl7OR?=
BCBL1 NIrTPY9HfW6ldHnvckBCe3OjeR?= MkTUNVAx6oDLwsXN M1\uZVI1KGh? NVHRe5NTdWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMjDy[YR2[3Srb36= Ml3vNlYyQDR7OUm=
BC3 NYO0THJ6TnWwY4Tpc44hSXO|YYm= MoTPNVAx6oDLwsXN MoLtNlQhcA>? NHi1b2FqdmS3Y3XzJIEh[2:vcHzleIUh[XW2b4DoZYdq[yCobIX4xsA> Mki4NlYyQDR7OUm=
BCBL1 M2DRWWZ2dmO2aX;uJGF{e2G7 NFu2[lYyODEkgJpCuW0> NULSOW5tOjRiaB?= NVfrUnZKcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh NYjvS3FLOjZzOES5PVk>
SK-MEL-28 NWHh[2p3TnWwY4Tpc44hSXO|YYm= MkfyOVAwOTBy4pEJxtVO NF\yVYo1QCCq M4nwO2ROW09? MXjy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= M3[2SlI2OjF4NUKy
MeWo MojhSpVv[3Srb36gRZN{[Xl? M{\UNFUxNzFyMPMAjeK2VQ>? NUjTdod7PDhiaB?= NH[1dmtFVVOR M{f6VJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M3vLd|I2OjF4NUKy
SK-MEL-5 MYjGeY5kfGmxbjDBd5NigQ>? NIDK[2k2OC9zMEFihKnDvU1? M{HHSFQ5KGh? M2jNOmROW09? Mn3IdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= MUOyOVIyPjV{Mh?=
SK-MEL-2 MWDGeY5kfGmxbjDBd5NigQ>? NU[2XZo4PTBxMUCw5qCKyrWP NYTWbmhVPDhiaB?= NYTmUIhbTE2VTx?= MoLPdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= M2fCNlI2OjF4NUKy
B16-F0 Ml3GSpVv[3Srb36gRZN{[Xl? M2e5N|UxNzFyMPMAjeK2VQ>? NX3tV2s3PDhiaB?= MVfEUXNQ MmHudoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NVrTN5doOjV{MU[1NlI>
TRPM2/HEK  MUPGeY5kfGmxbjDBd5NigQ>? MnfONE4y6oDVMkZCpOK2VQ>? NXzFfJB2OTYEoH3pci=> NVn3ZZU3TE2VTx?= M1[4e5Jm\HWlZYOgTFJQOi2rbnT1Z4VlKEOjMjvpcoNz\WG|ZTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjygZY5lKHSqZTDJR|UxyqC4YXz1[UB4[XNiMT63xsDDvU1? MViyOVE4QTV5NB?=
U937  NFnINGJHfW6ldHnvckBCe3OjeR?= MVSwMlHjiJN{NdMgxtVO NID2TIEyPcLibXnu MmjRSG1UVw>? NHjUTVZz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IECuOOKhyrWP NW\OZY9JOjVzN{m1O|Q>
TRPM2/HEK  M2\1WmZ2dmO2aX;uJGF{e2G7 NUjmO3JVOTEEoNM1US=> NF24OnE1OMLibXnu Mn;ESG1UVw>? NV\QXlY1emWmdXPld{BVWlCPMjDhZ5RqfmG2aX;uJIV3\W5iYYSgbIlocCClb37j[Y51emG2aX;ud{Bw\iCKMl:y M4fKUVI2OTd7NUe0
GL37  M3H3b2NmdGxiVnnhZoltcXS7IFHzd4F6 NEi4S4ExNTFywrFCuW0> MlviOFghcA>? MkD3d5VxeHKnc4Pld{BN[SCneIDy[ZN{cW:w MlLQNlQ6QTl4NUe=
NRK-52E MlP0SpVv[3Srb36gRZN{[Xl? M1\xR|HDqML3TR?= NHTicHEyOCCvaX6= NXnRbY1G[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> NWW1dlF6OjR5MUC0NlM>
NRK-52E M3H5O2Z2dmO2aX;uJGF{e2G7 MnfPNeKhyrWP NHHUNpUyOCCvaX6= MVricI9kc3NiQX7nJGlKKGmwZIXj[YQhS0R{NDDlfJBz\XO|aX;u NWDSdpZqOjR5MUC0NlM>
HSC  M1\BT2Z2dmO2aX;uJGF{e2G7 NEj1cpkzOCEQvF2= Mlz2NUBp M33CVYFjem:pYYTld{B1cGViZHnm[oVz\W62aXHsJIVn\mWldIOgc4YhdGWydHnuJI9zKEGJRYO= MUiyOFYyPDF7OR?=
EJ NHXOT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W5R|UxNzhyIN88US=> MmXhNlQwPDhxN{KgbC=> M13yXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{PLTlI1PTh5MES5
EJ NXvFbHBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vJ[|UxNzhyIN88US=> MmT2OFghcA>? NXfNdGF7[2G3c3XzJHMueGijc3WgZZJz\XO2 NXWwfFhTOjR3OEewOFk>
EJ NVz0NpJtTnWwY4Tpc44hSXO|YYm= NIHie2s2OC96MDFOwG0> M2XtPFQ5KGh? M1La[4Rwf26{ZXf1cIF1\XNiYz3NfYMtKGO7Y3zpcmQyNCC|dYL2bZZqdiCjbnSgWmVITiCneIDy[ZN{cW:wcx?= MlzQNlQ2QDdyNEm=
HepG2 M13pdGZ2dmO2aX;uJGF{e2G7 M2L6cVUxNTVyMDFOwG0> M1i2U|YxyqCvaX6= MWnpcohq[mm2czD0bIUhUUxvNj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSBqVInyO|A2MSCjbnSgV3RCXDNiKGT5dlcxPSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{W5PVI1OjR{MES2
SGC7901 MnfaR4VtdCCYaXHibYxqfHliQYPzZZk> NXWweldWOC1zMECg{txO M1\QU|I1NzR6L{eyJIg> M4G1WINifXOnczDhJJNq\26rZnnjZY51KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCmb4PlMYRmeGWwZHXueIx6KGK3dDDuc5QhfGmvZT3k[ZBmdmSnboTsfS=> NIrVUpUzPDF3MUK1OS=>
AGS  NXuxUVhFS2WubDDWbYFjcWyrdImgRZN{[Xl? NXn3Z3k2OC1zMECg{txO NHLlNG8zPC92OD:3NkBp MnW4Z4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NH7nOGQzPDF3MUK1OS=>
SGC7901 Mm\pSpVv[3Srb36gRZN{[Xl? MV61NEDPxE1? MUGyOE81QC95MjDo MkTteIhmKGyndnXsd{Bw\iCySlHLNkBj\WejbjD0c{Bl\WOuaX7lJIF1KDJ2IHjyMEBidmRicnXic5Vv\GWmIHH0JFczKGi{wrC= NGGxe4czPDF3MUK1OS=>
AGS  NHzHWpJHfW6ldHnvckBCe3OjeR?= MV61NEDPxE1? MUGyOE81QC95MjDo NXjFOZFNfGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> NHLOT|gzPDF3MUK1OS=>
SGC7901 NILCVXlHfW6ldHnvckBCe3OjeR?= NV\FPXFWPTBizszN NYDCOXpZOjRxNEivO|IhcA>? MUH0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> Mn6xNlQyPTF{NUW=
AGS  NH7q[nFHfW6ldHnvckBCe3OjeR?= M{\CcVUxKM7:TR?= NXT1b5N[OjRxNEivO|IhcA>? MWH0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> NX;WTGY1OjRzNUGyOVU>
MC3T3-E1  NFzQUJJHfW6ldHnvckBCe3OjeR?= M2Kyb|UxKM7:TR?= NWLwT5NzPCCq MmLVbY5pcWKrdIOgTHNGNWmwZIXj[YQhSk2SNzDhcoQhT0iUIIDyc5RmcW5iZYjwdoV{e2mxbtMg NGTEVlYzOzh5N{ezOC=>
7TD1-DXM MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuxNEDPxE1? MUe3NkBp M4rJW2ROW09? MljHbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NX\Xcos3OjN6N{GxOVk>
7TD1-WD-90 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjm[ZBPOTBizszN NEjldmM4OiCq M{XkNWROW09? MkLXbY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mo\UNlM5PzFzNUm=
7TD1-DXM M{n4eWFxd3C2b4Ppd{BCe3OjeR?= MnPwOVAh|ryP M1PqZVQ5KGh? MVrEUXNQ NFHlcmlqdmS3Y3XzJIFxd3C2b4Ppdy=> NGrkR2EzOzh5MUG1PS=>
7TD1-WD-90 Mm\NRZBweHSxc3nzJGF{e2G7 MoDROVAh|ryP NEH4S5Q1QCCq NYDUOGNnTE2VTx?= M{TMUIlv\HWlZYOgZZBweHSxc3nz NHTOPJMzOzh5MUG1PS=>
7TD1-WD-90  NXPnZo5wTnWwY4Tpc44hSXO|YYm= NHHvZYk2OCEQvF2= MUK2JIg> MXXEUXNQ NUn4U4Fye2mpbnnmbYNidnSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEqDS{KgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCVVFHUNy=> MkHrNlM5PzFzNUm=
HepG2  NVHIRXkzTnWwY4Tpc44hSXO|YYm= MYGxNFAh|ryP NHuwWJkyOi9{NDDo NYPLZ4VocW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:w NFf0U5IzOzh|NkSwNC=>
RAW264.7  MkT5SpVv[3Srb36gRZN{[Xl? NYPjcnFoPTEEoN88UeKh M37YfVI1NzR6IHi= NWD3elZoe3WycILld5NmeyCUQV7LUE1qdmS3Y3XkJI9{fGWxY3zhd5Rw\2WwZYPpdy=> NWfBb2E5OjN4NkWwNVg>
RAW264.7 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfQR4QxNTVywrFOwG3DqA>? NF7NO|E1QMLiaB?= NFf0RWlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlMYRmeGWwZHXueIx6 MnjKNlM3PjVyMUi=
RAW264.7 MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TYeFAuPTEEoN88UeKh MWW0POKhcA>? MojqZ4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= NYGwZoxmOjN4NkWwNVg>
RAW264.7 M{jXZWZ2dmO2aX;uJGF{e2G7 M3rkV|UxyqEQvF2= NHniZpUzPC92ODDo MXjpcohq[mm2czDSRW5MVC2rbnT1Z4VlKE6IQWTjNUBmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gV4VzPzJ5U2TBWFM> M1mzSlI{PjZ3MEG4
A549  MWHGeY5kfGmxbjDBd5NigQ>? NH3mcm4zOC92MDFOwG0> NYjNT|dtOjBiaB?= MVSyNEDPxE1iQVe0PVAhe3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSgbY53[XOrb36gc4YhSTV2OTDj[Yxtew>? MljoNlM3OjBzOUG=
A549  M3zFbGZ2dmO2aX;uJGF{e2G7 MljGNVAwOjBxNECg{txO MUOyOEBp NXLPT5pre3WycILld5NmeyC2aHWgdoFlcWG2aX;uMYlv\HWlZXSg[YxmfmG2aX;uJI9nKF[HR1dCpC=> M1PIdlI{PjJyMUmx
HUVECs NEnrOIRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1HIWFIxKML3TR?= NVW3fG1CPCCq M17NWoF1fGWwdXH0[ZMhUDKRMj3pcoR2[2WmIHPlcIwhe2i{aX7rZYdmKGGwZDDpcZBzd3[nZDD0bIUh[XS2YXPocYVvfCC{YYTlJI9nKHSqZTDj[Yxtew>? NUDu[VBKOjN2OEO5OFY>
HUVECs MlP1RZBweHSxc3nzJGF{e2G7 M1fzZ|IxKML3TR?= M4LnflQhcA>? NHXZfFV{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUh[2WubDDhdI9xfG:2aXOgbY5l\Xh? NG\XRWUzOzR6M{m0Oi=>
BV-2  MmHtSpVv[3Srb36gRZN{[Xl? NGXN[I8zOCEEtV2= MonvNVYhcA>? NWPwXY9TcW6qaXLpeJMhVFCVLXnu[JVk\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiYXztc5N1KGOxbYDs[ZRmdHliZHntbY5qe2inZDDpUm9UKGW6cILld5Nqd25? NW[5SpBZOjN{M{[zO|A>
NRK-52E  NHzuNJFHfW6ldHnvckBCe3OjeR?= MWe1xsDPxE1? NX3DTodjOzEEoH3pci=> M1zwWIF1fGWwdXH0[ZMhSW6pLTix5qCUPylvaX7obYJqfGWmIGTHSk3PujFibWLORUBifCBzNtMgbOKh NVK0cVJzOjNzN{S3OVc>
SW620  MUTGeY5kfGmxbjDBd5NigQ>? MUCyNEDDvU1? NGLSSIoyNzZiaB?= M3fBe4lvcGmkaYTzJJAuW1SDVEOgZYN1cX[jdHnvci=> NWnsdXhEOjNzMUC2NlU>
RPE  NWTyRlBsTnWwY4Tpc44hSXO|YYm= NWHqSZo3OzBiwsXNxsA> Mke0N{Bp M33zZolvcGmkaYTzJJRp\SCrbnT1Z5Rqd25ib3[gdE1UXEGWMzDlfJBz\XO|aX;u NGDjNFczOzB7NEC2Oy=>
SW1116 NFnHS5FHfW6ldHnvckBCe3OjeR?= M2nLZVExOCEEtV5CpC=> NV3pVm9tOjRxNEivO|IhcA>? NULFRYF6\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= NYexSFlpOjJyNUC3PVA>
HT29 M1nofGZ2dmO2aX;uJGF{e2G7 MlWzNVAxKML3TdMg M3nOWFI1NzR6L{eyJIg> MkDT[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? M1f1W|IzODVyN{mw
SW1116 NYPGfJd2TnWwY4Tpc44hSXO|YYm= M4XYPVExOCEEtV5CpC=> NFf4Z5EzPC92OD:3NkBp MYrk[YNz\WG|ZYOgeIhmKHCVVFHUN{Bt\X[nbIOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYNCpC=> NUfZXHo6OjJyNUC3PVA>
HT29 MWPGeY5kfGmxbjDBd5NigQ>? MUexNFAhyrWPwrC= NVzV[|ZtOjRxNEivO|IhcA>? M3e1TIRm[3KnYYPld{B1cGVicGPURXQ{KGyndnXsd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7lduKh M{nDVlIzODVyN{mw
ARPE-19 MUDGeY5kfGmxbjDBd5NigQ>? M4XTRlXDqM7:TR?= MXWzNOKhdWmw M{LUZYlvcGmkaYTzJGpCUzJicHjvd5Bpd3KrbHH0bY9v MlHuNlE3OjB7NkO=
HSC-T6 NGnhRWNCeG:ydH;zbZMhSXO|YYm= NEPnbJcyOMLizszN NYrxPWQ1OsLiaNMg NH;xNIpqdmirYnn0d{B1cGViYYDvdJRwe2m|IH;mJGhUSy2WNjDj[YxteyCrbnT1Z4VlKGK7IFPESS=> NUnJPG9qOjF|OU[5PVg>
HSC-T6 Mm[ySpVv[3Srb36gRZN{[Xl? NFPXOlEyOMLizszN NIjEPJczyqCqwrC= MV7pcohq[mm2czD0bIUh\XiycnXzd4lwdnNib3[gdHkuW1SDVEGgZY5lKEKjZDDpcoR2[2WmIHL5JGNFTQ>? MWKyNVM6Pjl7OB?=
Hep-2 M2\IPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHviRmUzPS1zMECg{txO MYWyOE81QC95MjDo M{XQeolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NVLnN2dkOjF|MEm0PFE>
Hep-2 NIjITFlCeG:ydH;zbZMhSXO|YYm= NUHiUWxYPTBizszN Mnu5NlQwPDhxN{KgbC=> Mor6bY5lfWOnczDj[YxtKGGyb4D0c5NqeyC2aX3lJIRmeGWwZHXueIx6 NFHIcWMzOTNyOUS4NS=>
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KF8 MnzHSpVv[3Srb36gRZN{[Xl? M1jPXFExyqEQvF5CpC=> MWCxxsBp MWTEUXNQyqB? Ml3hbY5pcWKrdIOgTWwuOzNvaX7keYNm\CCQRj5OvmIh[WO2aY\heIlwdg>? MWOyNFk1ODB2NR?=
KF8 MX;GeY5kfGmxbjDBd5NigQ>? NU\HTXRsOTEEoN88UeKh NEfxWHEyyqCqwrC= M3OwbmROW00EoB?= NWjUdJFGcW6qaXLpeJMhUUxvM{OtbY5lfWOnZDDJ{tpD|rFiZHXndoFl[XSrb36gZY5lKE6ILd86RkBi[3SrdnH0bY9v NHrncpczODl2MEC0OS=>
HEL  MYrGeY5kfGmxbjDBd5NigQ>? MlyyNVAxyqEQvF2= M37yd|EzNTd{IHi= NUfUbVJNcW6qaXLpeJMhfGinIHzleoVtKG:oIICtTmFMOixiSlHLNi=> MkHUNlA3OjFyNkG=
HEL M1HyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jaeVExOMLizszN NYeyW2kyOC13IHS= MYXy[YR2[2W|IHfyc5d1cCCxZjDKRWszXjZzN1[t[ZhxemW|c3nu[{BJTUxiY3XscJM> NYTTNJVbOjB4MkGwOlE>
A-172 NX25dXRPTnWwY4Tpc44hSXO|YYm= M1GyeFUxNzFyMNMg{txO NH7VO5c1QCCq Mn6zdoVlfWOnczD0bIUhdGW4ZXzzJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4YYTl[EBUXEGWMzDpckBiKHSrbXWt[IVx\W6mZX70JIFv\CCmb4PlMYRmeGWwZHXueEBn[XOqaX;u MXyyNFU5QTV{NR?=
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MZ-304 MVnGeY5kfGmxbjDBd5NigQ>? MX[1NE8yODEEoN88US=> NYPBU2JHPDhiaB?= NH;pc4tz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NHHKPZkzODV6OUWyOS=>
A-172 NFW3Tm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPj[Yg2OC9zMEFCpO69VQ>? MWm0PEBp MXjs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? NID1[4ozODV6OUWyOS=>
MZ-18 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2H4TVUxNzFyMNMg{txO MVK0PEBp M33CSIxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NUPab4ZxOjB3OEm1NlU>
MZ-54 M4nydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq4[2c2OC9zMEFCpO69VQ>? MVW0PEBp MY\s[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MUmyNFU5QTV{NR?=
MZ-256 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTSbZU2OC9zMEFCpO69VQ>? NUjnVG9tPDhiaB?= MVns[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? NV7UWox3OjB3OEm1NlU>
MZ-304 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXMS3g2OC9zMEFCpO69VQ>? NEO3U5g1QCCq M4\hN4xm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= Mo\FNlA2QDl3MkW=
A-172 NIi1bVNHfW6ldHnvckBCe3OjeR?= NIXsWXg2OC9zMEFCpO69VQ>? MkLBOFghcA>? M1TkN4lvcGmkaYTzJI1q\3KjdHnvci=> NF7DWIgzODV6OUWyOS=>
MZ-18 MXvGeY5kfGmxbjDBd5NigQ>? NFXtXow2OC9zMEFCpO69VQ>? M4\yWVQ5KGh? MVTpcohq[mm2czDtbYdz[XSrb36= MlfFNlA2QDl3MkW=
MZ-54 NX3Z[HZ7TnWwY4Tpc44hSXO|YYm= MoDzOVAwOTBywrFOwG0> NF\2Oo81QCCq NVOzT45RcW6qaXLpeJMhdWmpcnH0bY9v NGLs[IkzODV6OUWyOS=>
MZ-256 NHPSUndHfW6ldHnvckBCe3OjeR?= NFLaeGM2OC9zMEFCpO69VQ>? NWjQNYQxPDhiaB?= NFj6WGtqdmirYnn0d{BucWe{YYTpc44> MXeyNFU5QTV{NR?=
MZ-304 MVnGeY5kfGmxbjDBd5NigQ>? NG\iWm02OC9zMEFCpO69VQ>? Mnj4OFghcA>? NHrnPGRqdmirYnn0d{BucWe{YYTpc44> MkPZNlA2QDl3MkW=
A-172 NYjYZZJGTnWwY4Tpc44hSXO|YYm= M{L1SlExOMLizszN NXHQWWFbPDhiaB?= NFHQOoFqdmirYnn0d{Bqdn[jc3nvci=> NF;rNm0zODV6OUWyOS=>
MZ-18 NWfMbIZKTnWwY4Tpc44hSXO|YYm= NUDucXc5OTBywrFOwG0> NWTRRVFpPDhiaB?= M1TWR4lvcGmkaYTzJIlvfmG|aX;u NUHpOph6OjB3OEm1NlU>
MZ-54 MmPWSpVv[3Srb36gRZN{[Xl? NIfyT2MyODEEoN88US=> NH3ZUVA1QCCq MnTTbY5pcWKrdIOgbY53[XOrb36= NFv0Z2czODV6OUWyOS=>
MZ-256 MkDtSpVv[3Srb36gRZN{[Xl? NWXhUGllOTBywrFOwG0> M1\JPFQ5KGh? MnLzbY5pcWKrdIOgbY53[XOrb36= Mn7zNlA2QDl3MkW=
MZ-304 NVfXOJQ3TnWwY4Tpc44hSXO|YYm= NFXBNIYyODEEoN88US=> MXy0PEBp MWrpcohq[mm2czDpcpZie2mxbh?= MkXyNlA2QDl3MkW=
A-172 NGSwSJlHfW6ldHnvckBCe3OjeR?= M1vwXlUxNzFyMNMg{txO MmPFOFghcA>? MYPy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz MnvzNlA2QDl3MkW=
MZ-18 MXfGeY5kfGmxbjDBd5NigQ>? MkHYOVAwOTBywrFOwG0> NYjkclA{PDhiaB?= NIfqXYxz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ NXPSSmpwOjB3OEm1NlU>
MZ-54 NXPQW|dPTnWwY4Tpc44hSXO|YYm= MWe1NE8yODEEoN88US=> MV60PEBp M4PUNZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> NFrOZXEzODV6OUWyOS=>
MZ-256 M1W0fWZ2dmO2aX;uJGF{e2G7 MmTnOVAwOTBywrFOwG0> NWXSNXg3PDhiaB?= MVPy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz MmLJNlA2QDl3MkW=
MZ-304 M{DHbGZ2dmO2aX;uJGF{e2G7 M3nHO|UxNzFyMNMg{txO MkW2OFghcA>? M3\0bZJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> MUGyNFU5QTV{NR?=
SW1990 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr2WHgzOCEQvF2= MoPmNlQwPDhxN{KgbC=> NGTLV29qdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MYCyNFQ5Ojh3OB?=
SW1990 M2HH[mZ2dmO2aX;uJGF{e2G7 NUeyXY5TOjBizszN NF;vd4UzPCCq MV;k[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gUW1RNTJiYX7kJHZGT0ZibWLORZM> MX[yNFQ5Ojh3OB?=
SW1990 NVnvXYw1TnWwY4Tpc44hSXO|YYm= MkjkNlAh|ryP NXPYZWlVOjRiaB?= Ml25[IVkemWjc3XzJJRp\SCrboTlcpNqfHlib3[gdE1UfGG2MzDlfJBz\XO|aX;u M2TIO|IxPDh{OEW4
SW1990 MXfJcpZie2mxbjDBd5NigQ>? NHHlRoMzOCEQvF2= MnPQNlQhcA>? MoDIdoVlfWOnczDpcpZie2mxbjDv[kBUXzF7OUCgZ4VtdHQEoB?= MVGyNFQ5Ojh3OB?=
THP1 NUPEUVh4TnWwY4Tpc44hSXO|YYm= MXmxNEB2VQ>? NWPQOZJROzBibXnuxsA> Mnf5bY5pcWKrdIOgV3RCXDNidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGK7IH;2[ZIhPjBn M4n3RlIxOzl|Nkmw
BMMC MXnGeY5kfGmxbjDBd5NigQ>? NXrteVFPOC1zMDFOwG0> M3zFXlE2yqCvaX6= NGmwUFhqdmirYnn0d{BNXEN2wrDy[Yxm[XOnIHnuJIEh\G:|ZT3k[ZBmdmSnboSg[oF{cGmxbjD3bZRpKG6nYYKgZ49ueGyndHWgbY5pcWKrdHnvckBifCClb37j[Y51emG2aX;ud{Djsb5zMNMg{txO NYjoepBGOTl6M{W4OFU>
A549 M4\V[mZ2dmO2aX;uJGF{e2G7 NVfPVGFuOTVizszt NULCOYtXOSCq MVLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKFOWQWSxJI9vKHS7cn;zbY5mKDdyMTD3ZZMh\GW2ZXP0[YQhOTVibXnuJIFnfGW{IGPQSUBDKHS{ZXH0cYVvfA>? M37ITVE6QDBzNk[1
OVCAR-3 M3HM[WZ2dmO2aX;uJGF{e2G7 NYr4XIxFOTBidV2= NV;ESnFROSCq M{\CcYlvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= MlziNVk3PDd|NkO=
PA-1 NESwcWdHfW6ldHnvckBCe3OjeR?= NV3TVFRROTBidV2= M{HtT|EhcA>? MYXpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? Ml\5NVk3PDd|NkO=
OVCAR-3 Mk\sSpVv[3Srb36gRZN{[Xl? MYexNEB2VQ>? MnPBNUBp NXHPcVZucW6qaXLpeJMhKEySQT3pcoR2[2WmIH;2ZZJq[W5iY3HuZ4VzKGOnbHygcY91cWyrdIm= NXy4fGtzOTl4NEezOlM>
PA-1 MofCSpVv[3Srb36gRZN{[Xl? MXuxNEB2VQ>? Mmj2NUBp M4TkcIlvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 M1:0blE6PjR5M{[z
Jurkat  NGj1V2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFGyXpY2OCEQvF2= M17rbVI1NzR6L{eyJIg> NWrBNHVX\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9v NVntOpE3OTl3NkS4PVE>
SUPT1  NVXMSYNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXG1NEDPxE1? M1HSUVI1NzR6L{eyJIg> M1K0OoVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBoem:5dHigbY5pcWKrdHnvci=> MlzGNVk2PjR6OUG=
Jurkat  Ml7iRZBweHSxc3nzJGF{e2G7 NH7wR3E2OCEQvF2= NVP2UlFxOjRxNEigbC=> M1e4dYVvcGGwY3XzJHRTSUmOLXnu[JVk\XNiY3XscEBieG:ydH;zbZM> NFr4WY0yQTV4NEi5NS=>
SUPT1  M3jKdWFxd3C2b4Ppd{BCe3OjeR?= M1u1eFUxKM7:TR?= MnPsNlQwPDhiaB?= NE\Sco5mdmijbnPld{BVWkGLTD3pcoR2[2W|IHPlcIwh[XCxcITvd4l{ NWXiNotQOTl3NkS4PVE>

... 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+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
Smiles C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N

In vivo Formulation Calculator (Clear solution)

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

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

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

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

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

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

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