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 111 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 M4fYfWZ2dmO2aX;uJGF{e2G7 NYqzPGszOTBy4pEJxtVO MnHVNlQhcA>? NEjwR5du\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> NWPGWng5OjZzOES5PVk>
BCBL1 NXf0PHN3TnWwY4Tpc44hSXO|YYm= NGfLVHMyODEkgJpCuW0> NVK5eYQ{OjRiaB?= NHq0cWJu\WSrYYTld{BRTUxiY3XscEBieG:ydH;zbZM> MV:yOlE5PDl7OR?=
BC3 MYTGeY5kfGmxbjDBd5NigQ>? M4HjXVExOOLCidM1US=> NFzkOVgzPCCq NGrsbWFu\WSrYYTld{Bl\S2yaH;zdIhwenmuYYTpc44hd2ZiU2TBWFMh[2:{cnXsZZRm\CC5aYToJGhUWDdyIHHu[EBJW0ZzIILl[JVkfGmxbh?= NXHmSnZHOjZzOES5PVk>
BCBL1 NUP6cGZCTnWwY4Tpc44hSXO|YYm= MV6xNFDjiIoEtV2= NITmNHUzPCCq NUW3c4tldWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMjDy[YR2[3Srb36= MX[yOlE5PDl7OR?=
BC3 Mn;SSpVv[3Srb36gRZN{[Xl? NIPEU3MyODEkgJpCuW0> NE[xO4UzPCCq MUnpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= NHfZV5MzPjF6NEm5PS=>
BCBL1 M3Xie2Z2dmO2aX;uJGF{e2G7 MoOyNVAx6oDLwsXN NYr5OIRvOjRiaB?= MYHpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{BndHW6wrC= NYjjd2w3OjZzOES5PVk>
SK-MEL-28 MoDhSpVv[3Srb36gRZN{[Xl? MlSxOVAwOTBy4pEJxtVO NWLtXFlmPDhiaB?= NUXDSZdbTE2VTx?= NGjhWnBz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> M3W3XFI2OjF4NUKy
MeWo M2n1NGZ2dmO2aX;uJGF{e2G7 MWC1NE8yODEkgJpCuW0> MkX1OFghcA>? NXfwW5NrTE2VTx?= MYTy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= NYnZfVV5OjV{MU[1NlI>
SK-MEL-5 NUO5U4NwTnWwY4Tpc44hSXO|YYm= NXnlZ2h1PTBxMUCw5qCKyrWP M135cVQ5KGh? MX7EUXNQ MXTy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= MoHlNlUzOTZ3MkK=
SK-MEL-2 MXXGeY5kfGmxbjDBd5NigQ>? M1K5eVUxNzFyMPMAjeK2VQ>? MlzuOFghcA>? NFzodnhFVVOR NHSxd5hz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NIHoRpgzPTJzNkWyNi=>
B16-F0 NYKyUIIyTnWwY4Tpc44hSXO|YYm= MkHiOVAwOTBy4pEJxtVO M2DNdFQ5KGh? M4\QSGROW09? Mn7LdoVlfWOnczDhco9qc2m|IILld4l{fGGwY3W= NVzZUpE1OjV{MU[1NlI>
TRPM2/HEK  MoHySpVv[3Srb36gRZN{[Xl? M1v6clAvOeLCk{K1xsDDvU1? MVKxOeKhdWmw NYrpZYFITE2VTx?= M3rnUpJm\HWlZYOgTFJQOi2rbnT1Z4VlKEOjMjvpcoNz\WG|ZTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjygZY5lKHSqZTDJR|UxyqC4YXz1[UB4[XNiMT63xsDDvU1? NWfUS3NrOjVzN{m1O|Q>
U937  NUe0bFRQTnWwY4Tpc44hSXO|YYm= M{jDWFAvOeLCk{K1xsDDvU1? MVGxOeKhdWmw NGXoOXhFVVOR NH7oT4Jz\WS3Y3XzJGgzVzJvaX7keYNm\CCFYUKrbY5kemWjc3WgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYKsJIFv\CC2aHWgTWM2OMLidnHseYUhf2G|IECuOOKhyrWP NWDHbm9xOjVzN{m1O|Q>
TRPM2/HEK  NI\kb2NHfW6ldHnvckBCe3OjeR?= Mn;LNVDDqML3TR?= NH30UoM1OMLibXnu NHvVcllFVVOR MXjy[YR2[2W|IGTSVG0zKGGldHn2ZZRqd25iZY\lckBifCCqaXfoJINwdmOnboTyZZRqd26|IH;mJGgzVzJ? MnS0NlUyPzl3N{S=
GL37  MofaR4VtdCCYaXHibYxqfHliQYPzZZk> NVfFWXFrOC1zMNMgxtVO M{ezeFQ5KGh? NHW1c|J{fXCycnXzd4V{KEyjIHX4dJJme3Orb36= MWiyOFk6QTZ3Nx?=
NRK-52E NGLXRnVHfW6ldHnvckBCe3OjeR?= MmHKNeKhyrWP NX74dI9ZOTBibXnu MVTicI9kc3NidHjlJJN1cW23bHH0c5J6KGWoZnXjeEBw\iCDbnegTWkhd25iUHH4MVIh\XiycnXzd4lwdsLi NFPqVYozPDdzMESyNy=>
NRK-52E NH63XoRHfW6ldHnvckBCe3OjeR?= MWOxxsDDvU1? M1fucFExKG2rbh?= M{[1T4Jtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> M{S0PVI1PzFyNEKz
HSC  MkLZSpVv[3Srb36gRZN{[Xl? NVzxN4hZOjBizszN M2LiS|EhcA>? MlHPZYJzd2ejdHXzJJRp\SCmaX\m[ZJmdnSrYXyg[YZn\WO2czDv[kBt\XC2aX6gc5IhSUeHcx?= NXfYN2tROjR4MUSxPVk>
EJ MoriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXzc2I2OC96MDFOwG0> M{K1OFI1NzR6L{eyJIg> NIfKeGJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NWnjfmxnOjR3OEewOFk>
EJ M2Hi[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXu1NE85OCEQvF2= MoLhOFghcA>? NUXmUIVW[2G3c3XzJHMueGijc3WgZZJz\XO2 MnnCNlQ2QDdyNEm=
EJ M4LjPGZ2dmO2aX;uJGF{e2G7 M3zqdVUxNzhyIN88US=> MoPyOFghcA>? MlTv[I94dnKnZ4XsZZRmeyClLV35Z{wh[3mlbHnuSFEtKHO3co\peolvKGGwZDDWSWdHKGW6cILld5Nqd26| NYnXSGlVOjR3OEewOFk>
HepG2 NWXObFU{TnWwY4Tpc44hSXO|YYm= NVv6UYRIPTBvNUCwJO69VQ>? NWPQNIVkPjEEoH3pci=> M2X1XYlvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXeyOFI1OjB2Nh?=
SGC7901 MojJR4VtdCCYaXHibYxqfHliQYPzZZk> NEjhXm4xNTFyMDFOwG0> MX:yOE81QC95MjDo NIr6XXZk[XW|ZYOgZUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliZH;z[U1l\XCnbnTlcpRtgSCkdYSgco91KHSrbXWt[IVx\W6mZX70cJk> NH7rTlgzPDF3MUK1OS=>
AGS  MYTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHu4e2YxNTFyMDFOwG0> NI\TSnAzPC92OD:3NkBp MlPBZ4F2e2W|IHGgd4lodmmoaXPhcpQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGSxc3Wt[IVx\W6mZX70cJkh[nW2IH7veEB1cW2nLXTldIVv\GWwdHz5 NFrybnozPDF3MUK1OS=>
SGC7901 MoXPSpVv[3Srb36gRZN{[Xl? MoPUOVAh|ryP NWHxVlhIOjRxNEivO|IhcA>? MUT0bIUhdGW4ZXzzJI9nKHCMQVuyJIJm\2GwIITvJIRm[2yrbnWgZZQhOjRiaIKsJIFv\CC{ZXLveY5l\WRiYYSgO|IhcHMEoB?= Ml;jNlQyPTF{NUW=
AGS  Mm[wSpVv[3Srb36gRZN{[Xl? Mo\VOVAh|ryP M{GxNFI1NzR6L{eyJIg> NIjtbGJ1cGVibHX2[Yx{KG:oIIDKRWszKGKnZ3HuJJRwKGSnY3zpcoUh[XRiMkSgbJItKGGwZDDy[YJwfW6mZXSgZZQhPzJiaINCpC=> MYGyOFE2OTJ3NR?=
SGC7901 NH2xeIZHfW6ldHnvckBCe3OjeR?= NVHtPIVKPTBizszN NITKPGQzPC92OD:3NkBp MV30bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> M2nOZlI1OTVzMkW1
AGS  NF\sNnlHfW6ldHnvckBCe3OjeR?= NWHzSJJPPTBizszN Ml71NlQwPDhxN{KgbC=> M2HEUpRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz NVjNU3I2OjRzNUGyOVU>
MC3T3-E1  NX;0[W1TTnWwY4Tpc44hSXO|YYm= M4naNVUxKM7:TR?= MlnDOEBp M2\WSolvcGmkaYTzJGhUTS2rbnT1Z4VlKEKPUEegZY5lKEeKUjDwdo91\WmwIHX4dJJme3Orb39CpC=> M36wNFI{QDd5N{O0
7TD1-DXM M1T0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;R[2YyOCEQvF2= M1j5TVczKGh? M4\BU2ROW09? MXHpcohq[mm2czDj[YxtKGe{b4f0bC=> NEfwSogzOzh5MUG1PS=>
7TD1-WD-90 NH3NZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVixNEDPxE1? MnH6O|IhcA>? Mo\hSG1UVw>? NFHSTXFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M{\Ge|I{QDdzMUW5
7TD1-DXM NXfjSGpkSXCxcITvd4l{KEG|c3H5 MljNOVAh|ryP M{LNTFQ5KGh? Mlr1SG1UVw>? M2nRUIlv\HWlZYOgZZBweHSxc3nz NWjDU3FYOjN6N{GxOVk>
7TD1-WD-90 MnXtRZBweHSxc3nzJGF{e2G7 M4fRVlUxKM7:TR?= Mk[1OFghcA>? MW\EUXNQ M4rSUYlv\HWlZYOgZZBweHSxc3nz M3LESlI{QDdzMUW5
7TD1-WD-90  NFnhT5RHfW6ldHnvckBCe3OjeR?= MYK1NEDPxE1? MYW2JIg> MXPEUXNQ Mn:zd4lodmmoaXPhcpRtgSCrbnjpZol1eyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGpCUzJiYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMx?= NGLJeFYzOzh5MUG1PS=>
HepG2  MV;GeY5kfGmxbjDBd5NigQ>? M3rRWFExOCEQvF2= NHj5booyOi9{NDDo NVjDcWRRcW6qaXLpeJMhW1SDVEOgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:w MoXHNlM5OzZ2MEC=
RAW264.7  NUTzdZVvTnWwY4Tpc44hSXO|YYm= NFHEXlE2OMLizszNxsA> M2TjfFI1NzR6IHi= NEn3S5l{fXCycnXzd4V{KFKDTlvMMYlv\HWlZXSgc5N1\W:lbHHzeI9o\W6nc3nz NYTTT2g6OjN4NkWwNVg>
RAW264.7 NW\NfHZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;tOWUxNTVywrFOwG3DqA>? MXu0POKhcA>? Ml;RbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZT3k[ZBmdmSnboTsfS=> NGrLcXEzOzZ4NUCxPC=>
RAW264.7 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHEeXAxNTVywrFOwG3DqA>? NFOyd|Y1QMLiaB?= Mnv6Z4F2e2W|IHHuJIFzemW|dDDv[kBTSVd{NkSuO{Bk\WyuczDheEB1cGViR{CvS|EheGijc3Wgc4YhfGinIHPlcIwh[3mlbHW= M1W5blI{PjZ3MEG4
RAW264.7 NWTveFdiTnWwY4Tpc44hSXO|YYm= M3HrXlUxyqEQvF2= MYSyOE81QCCq M4DVVYlvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? MnXoNlM3PjVyMUi=
A549  NXTVc|hyTnWwY4Tpc44hSXO|YYm= M2jhNVIxNzRyIN88US=> M{HYPVIxKGh? M1TFVVIxKM7:TTDBS|Q6OCC|dYDwdoV{e2W|IITo[UBz[WSrYYTpc44ucW6mdXPl[EBqdn[jc3nvckBw\iCDNUS5JINmdGy| MlzKNlM3OjBzOUG=
A549  M2PxTGZ2dmO2aX;uJGF{e2G7 NEHxe2EyOC9{MD:0NEDPxE1? NUnaUplDOjRiaB?= MVPzeZBxemW|c3XzJJRp\SC{YXTpZZRqd25vaX7keYNm\CCnbHX2ZZRqd25ib3[gWmVITsLi NVvPRYdKOjN4MkCxPVE>
HUVECs NGXhSXFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIPITYYzOCEEtV2= NH6zS4s1KGh? NWfFc3BE[XS2ZX71ZZRmeyCKMl:yMYlv\HWlZXSgZ4VtdCC|aILpcoti\2ViYX7kJIlueHKxdnXkJJRp\SCjdIThZ4hu\W62IILheIUhd2ZidHjlJINmdGy| NWDoVnpTOjN2OEO5OFY>
HUVECs MVnBdI9xfG:|aYOgRZN{[Xl? MmWxNlAhyrWP MVO0JIg> NYrwPHhHe2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 MWCyN|Q5Ozl2Nh?=
BV-2  M1rTe2Z2dmO2aX;uJGF{e2G7 NXLx[GwyOjBiwsXN Mom5NVYhcA>? MnrRbY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> MnPqNlMzOzZ|N{C=
NRK-52E  NVTHXGxtTnWwY4Tpc44hSXO|YYm= M{ns[VXDqM7:TR?= M2TROVMxyqCvaX6= M2nr[4F1fGWwdXH0[ZMhSW6pLTix5qCUPylvaX7obYJqfGWmIGTHSk3PujFibWLORUBifCBzNtMgbOKh NGjFXXUzOzF5NEe1Oy=>
SW620  M{Do[GZ2dmO2aX;uJGF{e2G7 NHGxbpkzOCEEtV2= M17GO|EwPiCq NGDEbnhqdmirYnn0d{BxNVOWQWSzJIFkfGm4YYTpc44> MnzxNlMyOTB4MkW=
RPE  NFXJcnRHfW6ldHnvckBCe3OjeR?= NFHLNZI{OCEEtV5CpC=> MlTvN{Bp MnXnbY5pcWKrdIOgeIhmKGmwZIXjeIlwdiCxZjDwMXNVSVR|IHX4dJJme3Orb36= MmmzNlMxQTRyNke=
SW1116 MVrGeY5kfGmxbjDBd5NigQ>? MV[xNFAhyrWPwrC= MYWyOE81QC95MjDo MYTk[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gTmFMOiCjbnSgdGpCUzJidHnt[U1l\XCnbnTlcpRtgQ>? M{nCUFIzODVyN{mw
HT29 NX\Rem1GTnWwY4Tpc44hSXO|YYm= MkH2NVAxKML3TdMg Mn7HNlQwPDhxN{KgbC=> MmHp[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGpCUzJiYX7kJJBLSUt{IITpcYUu\GWyZX7k[Y51dHl? Ml3vNlIxPTB5OUC=
SW1116 M3P5cWZ2dmO2aX;uJGF{e2G7 NF\SZZIyODBiwsXNxsA> NYPFVI9EOjRxNEivO|IhcA>? Ml\i[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> MVKyNlA2ODd7MB?=
HT29 MmDsSpVv[3Srb36gRZN{[Xl? NEXSOGgyODBiwsXNxsA> MUOyOE81QC95MjDo NG\LdFhl\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? M2LPNlIzODVyN{mw
ARPE-19 NWDifmdpTnWwY4Tpc44hSXO|YYm= M3vwfVXDqM7:TR?= NGfRXJU{OMLibXnu NXexbZE5cW6qaXLpeJMhUkGNMjDwbI9{eGixcnnsZZRqd25? NITER3YzOTZ{MEm2Ny=>
HSC-T6 M2nZcWFxd3C2b4Ppd{BCe3OjeR?= MX2xNOKh|ryP MnfGNuKhcMLi NXzZbII4cW6qaXLpeJMhfGinIHHwc5B1d3OrczDv[kBJW0NvVE[gZ4VtdHNiaX7keYNm\CCkeTDDSGU> NYjye|hjOjF|OU[5PVg>
HSC-T6 MoHiSpVv[3Srb36gRZN{[Xl? M4DQdFExyqEQvF2= M3nidFLDqGkEoB?= NHrHT2VqdmirYnn0d{B1cGViZYjwdoV{e2mxboOgc4YheFlvU2TBWFEh[W6mIFLh[EBqdmS3Y3XkJIJ6KEOGRR?= MkjSNlE{QTZ7OUi=
Hep-2 M3i0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWxNYtqOjVvMUCwJO69VQ>? NEPyW4YzPC92OD:3NkBp MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NV3KWllCOjF|MEm0PFE>
Hep-2 M13XXWFxd3C2b4Ppd{BCe3OjeR?= NETwTGI2OCEQvF2= NXvVV|VNOjRxNEivO|IhcA>? NIHEc5BqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IITpcYUh\GWyZX7k[Y51dHl? NHXNUGQzOTNyOUS4NS=>
Hep-2 MXXGeY5kfGmxbjDBd5NigQ>? MVu1NEDPxE1? M1rwSFI1NzR6L{eyJIg> NUC0V|VDcW6qaXLpeJMhTzFidH:gV{Bk\WyuIHP5Z4xmKHS{YX7zbZRqd25iYX7kJIlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> NF7lNGwzOTNyOUS4NS=>
Hep-2 NIDIRZRHfW6ldHnvckBCe3OjeR?= MlLBOVAh|ryP MWqyOE81QC95MjDo MoDv[I94dnKnZ4XsZZRmeyC2aHWgV3RCXDNuIICtV3RCXDNiYX7kJJN2en[rdnnuJJBzd3SnaX6gcIV3\Wy| NX;kNFAzOjF|MEm0PFE>
KF8 MUjGeY5kfGmxbjDBd5NigQ>? NVXQd5BKOTEEoN88UeKh MlK1NeKhcA>? M3rhR2ROW00EoB?= NF;mVmRqdmirYnn0d{BKVC1|Mz3pcoR2[2WmIF7GMe67SiCjY4TpeoF1cW:w NIXnWZozODl2MEC0OS=>
KF8 MXjGeY5kfGmxbjDBd5NigQ>? NVvXcnJMOTEEoN88UeKh M2LWV|HDqGkEoB?= Mn65SG1UV8Li M4jWUolvcGmkaYTzJGlNNTN|LXnu[JVk\WRiSd86Ru6yKGSnZ4Lh[IF1cW:wIHHu[EBPTi4QulKgZYN1cX[jdHnvci=> M1WzVVIxQTRyMES1
HEL  MkD1SpVv[3Srb36gRZN{[Xl? M4TTUlExOMLizszN MmnLNVIuPzJiaB?= NIDpSlNqdmirYnn0d{B1cGVibHX2[Ywhd2ZicD3KRWszNCCMQVuy MmjBNlA3OjFyNkG=
HEL M1H1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGxNFDDqM7:TR?= NECwcJcxNTViZB?= MXjy[YR2[2W|IHfyc5d1cCCxZjDKRWszXjZzN1[t[ZhxemW|c3nu[{BJTUxiY3XscJM> MljaNlA3OjFyNkG=
A-172 M3jM[WZ2dmO2aX;uJGF{e2G7 MWG1NE8yODEEoN88US=> M17OeVQ5KGh? M2LvUJJm\HWlZYOgeIhmKGyndnXsd{Bw\iClb37zeIl1fXSrdnXsfUBi[3SrdnH0[YQhW1SDVEOgbY4h[SC2aX3lMYRmeGWwZHXueEBidmRiZH;z[U1l\XCnbnTlcpQh\mG|aHnvci=> MnnLNlA2QDl3MkW=
MZ-18 NU[2b3ZVTnWwY4Tpc44hSXO|YYm= MWS1NE8yODEEoN88US=> MnHEOFghcA>? NIfaTIVz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NX20[G1oOjB3OEm1NlU>
MZ-54 MkG0SpVv[3Srb36gRZN{[Xl? MlTpOVAwOTBywrFOwG0> MXi0PEBp MULy[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= MWWyNFU5QTV{NR?=
MZ-256 NIT4N|hHfW6ldHnvckBCe3OjeR?= NWWyNHhGPTBxMUCwxsDPxE1? M{TlbVQ5KGh? MYfy[YR2[2W|IITo[UBt\X[nbIOgc4Yh[2:wc4TpeJV1cX[nbImgZYN1cX[jdHXkJHNVSVR|IHnuJIEhfGmvZT3k[ZBmdmSnboSgZY5lKGSxc3Wt[IVx\W6mZX70JIZie2irb36= MoflNlA2QDl3MkW=
MZ-304 NVPBeGRuTnWwY4Tpc44hSXO|YYm= MnLMOVAwOTBywrFOwG0> Ml\xOFghcA>? NXHhcmFvemWmdXPld{B1cGVibHX2[Yx{KG:oIHPvcpN1cXS3dHn2[Yx6KGGldHn2ZZRm\CCVVFHUN{BqdiCjIITpcYUu\GWyZX7k[Y51KGGwZDDkc5NmNWSncHXu[IVvfCCoYYPobY9v NFjNPWYzODV6OUWyOS=>
A-172 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWS1NE8yODEEoN88US=> NVLNSot7PDhiaB?= M3;BXoxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NWTRcFh6OjB3OEm1NlU>
MZ-18 NYHsW3A2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy3bWs2OC9zMEFCpO69VQ>? NGfnW5Y1QCCq NHP1[5dt\WGmczD0c{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQhemWmdXP0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDveoVzKGFidHnt[UBx\XKrb3Sgc4YhPDkEoHi= MlvPNlA2QDl3MkW=
MZ-54 M2XSRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3MWHM1PTBxMUCwxsDPxE1? Ml;0OFghcA>? M1nV[Yxm[WS|IITvJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;2[ZIh[SC2aX3lJJBmemmxZDDv[kA1QMLiaB?= NVfjU|lyOjB3OEm1NlU>
MZ-256 NXrxNXBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi1NE8yODEEoN88US=> M4\6bFQ5KGh? NVLmNWM2dGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo MmjRNlA2QDl3MkW=
MZ-304 NEK4VYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1T2cVUxNzFyMNMg{txO MnnuOFghcA>? MkTVcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq MmLCNlA2QDl3MkW=
A-172 NFXGeHNHfW6ldHnvckBCe3OjeR?= M1zFRlUxNzFyMNMg{txO M4nVU|Q5KGh? Mli1bY5pcWKrdIOgcYloemG2aX;u NVj2SndlOjB3OEm1NlU>
MZ-18 NFGxflRHfW6ldHnvckBCe3OjeR?= NFTkTGU2OC9zMEFCpO69VQ>? NVnpc2tyPDhiaB?= NGTMU25qdmirYnn0d{BucWe{YYTpc44> NFr1bWMzODV6OUWyOS=>
MZ-54 NF2ydWtHfW6ldHnvckBCe3OjeR?= NHHYS2Q2OC9zMEFCpO69VQ>? MmfGOFghcA>? MnSybY5pcWKrdIOgcYloemG2aX;u NWPSc3JDOjB3OEm1NlU>
MZ-256 MnHoSpVv[3Srb36gRZN{[Xl? M3yyPVUxNzFyMNMg{txO NGXa[Gk1QCCq NXHydZFLcW6qaXLpeJMhdWmpcnH0bY9v NULJcJJLOjB3OEm1NlU>
MZ-304 MofqSpVv[3Srb36gRZN{[Xl? MY[1NE8yODEEoN88US=> M3vWUlQ5KGh? NX\1d2JFcW6qaXLpeJMhdWmpcnH0bY9v M3S2SlIxPTh7NUK1
A-172 NFPXRolHfW6ldHnvckBCe3OjeR?= NXvUNY81OTBywrFOwG0> M1rOS|Q5KGh? NXrBR29pcW6qaXLpeJMhcW64YYPpc44> NWX0e5d{OjB3OEm1NlU>
MZ-18 NHHuNolHfW6ldHnvckBCe3OjeR?= NXXE[Y5QOTBywrFOwG0> NWPRSZVCPDhiaB?= NWnaUFEycW6qaXLpeJMhcW64YYPpc44> NFzVW3ozODV6OUWyOS=>
MZ-54 MkLVSpVv[3Srb36gRZN{[Xl? MWmxNFDDqM7:TR?= M33UblQ5KGh? NHH6SWRqdmirYnn0d{Bqdn[jc3nvci=> MYKyNFU5QTV{NR?=
MZ-256 MnTOSpVv[3Srb36gRZN{[Xl? NWPOfXhCOTBywrFOwG0> NGPOSXk1QCCq NH20fYpqdmirYnn0d{Bqdn[jc3nvci=> MmjtNlA2QDl3MkW=
MZ-304 MYXGeY5kfGmxbjDBd5NigQ>? NX3scos5OTBywrFOwG0> NXnRWm1kPDhiaB?= MYjpcohq[mm2czDpcpZie2mxbh?= NHnaT2wzODV6OUWyOS=>
A-172 MlK0SpVv[3Srb36gRZN{[Xl? MkT6OVAwOTBywrFOwG0> M4nQS|Q5KGh? MVLy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NV7ZWYNqOjB3OEm1NlU>
MZ-18 MkDPSpVv[3Srb36gRZN{[Xl? MVS1NE8yODEEoN88US=> NWfaNGxyPDhiaB?= MnzUdoVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> MYSyNFU5QTV{NR?=
MZ-54 M2jqVmZ2dmO2aX;uJGF{e2G7 NVTHXGdIPTBxMUCwxsDPxE1? NXztOVVSPDhiaB?= NH7oSXBz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M1PQbVIxPTh7NUK1
MZ-256 MkTISpVv[3Srb36gRZN{[Xl? NVLkZ2pbPTBxMUCwxsDPxE1? M{nFSFQ5KGh? MXXy[YR2[2W|IITyZY5{[3KrcITpc44hd2ZiTV3QJIdmdmW|IHHu[EBz\WS3Y3XzJIVvgnmvYYTpZ{Bi[3Srdnn0fUBw\iCPTWDz NHTubnAzODV6OUWyOS=>
MZ-304 MoDSSpVv[3Srb36gRZN{[Xl? MX21NE8yODEEoN88US=> M3z4T|Q5KGh? NYTCfoRVemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? NHPuZYkzODV6OUWyOS=>
SW1990 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmyNEDPxE1? MlHuNlQwPDhxN{KgbC=> NUPpfZpHcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NGLlTHQzODR6Mki1PC=>
SW1990 M2rqUGZ2dmO2aX;uJGF{e2G7 MkPsNlAh|ryP MVuyOEBp NGewXZdl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhVU2SLUKgZY5lKF[HR1[gcXJPSXN? NFP0ZYUzODR6Mki1PC=>
SW1990 M2nLdmZ2dmO2aX;uJGF{e2G7 NH7Nd4szOCEQvF2= NFLJdo4zPCCq NFXRe3Vl\WO{ZXHz[ZMhfGinIHnueIVve2m2eTDv[kBxNVO2YYSzJIV5eHKnc4Ppc44> MlPzNlA1QDJ6NUi=
SW1990 NV;0N5l{UW64YYPpc44hSXO|YYm= NFTpdmQzOCEQvF2= NUPnPJZkOjRiaB?= NWqwSnRXemWmdXPld{Bqdn[jc3nvckBw\iCVV{G5PVAh[2WubIRCpC=> NHqyT2UzODR6Mki1PC=>
THP1 M1nybWZ2dmO2aX;uJGF{e2G7 NGrwc5QyOCC3TR?= MoXJN|AhdWmwwrC= MofsbY5pcWKrdIOgV3RCXDNidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGK7IH;2[ZIhPjBn M{S3VVIxOzl|Nkmw
BMMC MlHoSpVv[3Srb36gRZN{[Xl? MUSwMVExKM7:TR?= MXSxOeKhdWmw M2rNeIlvcGmkaYTzJGxVSzUEoILlcIVie2ViaX6gZUBld3OnLXTldIVv\GWwdDDmZZNpcW:wIIfpeIghdmWjcjDjc41xdGW2ZTDpcohq[mm2aX;uJIF1KGOxbnPlcpRz[XSrb37zJQKqxjFywrFOwG0> NFXhc28yQTh|NUi0OS=>
A549 NVjFV3dRTnWwY4Tpc44hSXO|YYm= MVyxOUDPxG1? M{[zUFEhcA>? NVjYPZJycW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSCxbjD0fZJwe2mwZTC3NFEhf2G|IHTleIVkfGWmIEG1JI1qdiCjZoTldkBUWEViQjD0doVifG2nboS= MXqxPVgxOTZ4NR?=
OVCAR-3 NHnVU5pHfW6ldHnvckBCe3OjeR?= M1fqPVExKHWP MlPpNUBp M{HxVolvcGmkaYTzJGxRSS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= M1KySFE6PjR5M{[z
PA-1 MlnySpVv[3Srb36gRZN{[Xl? NEjvNncyOCC3TR?= NUP5WnZmOSCq MWnpcohq[mm2czDMVGEucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25? MWCxPVY1PzN4Mx?=
OVCAR-3 NVixT4h[TnWwY4Tpc44hSXO|YYm= MoX3NVAhfU1? M3z1OlEhcA>? M2HsRYlvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 M1nMTVE6PjR5M{[z
PA-1 Mnr3SpVv[3Srb36gRZN{[Xl? MVWxNEB2VQ>? MmHoNUBp M4L3b4lvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 MofrNVk3PDd|NkO=
Jurkat  M13pOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\PT2w2OCEQvF2= NHjXeFYzPC92OD:3NkBp MonW[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u NH3PXGEyQTV4NEi5NS=>
SUPT1  NYfEflRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTCOVAh|ryP NYXROmpzOjRxNEivO|IhcA>? MnfS[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIdzd3e2aDDpcohq[mm2aX;u NF6wVYgyQTV4NEi5NS=>
Jurkat  NXfqXVdySXCxcITvd4l{KEG|c3H5 NVXtO4dzPTBizszN MUSyOE81QCCq MV7lcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz MUSxPVU3PDh7MR?=
SUPT1  M{j5cGFxd3C2b4Ppd{BCe3OjeR?= NWPSR|dSPTBizszN MoXkNlQwPDhiaB?= MXPlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHygZZBweHSxc3nz MoHENVk2PjR6OUG=
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.

  • (Only for Reference)
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
  • (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 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

Tel: +1-832-582-8158 Ext:3
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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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