AG-490 (Tyrphostin B42)

For research use only. Not for use in humans.

目录号:S1143 别名: Zinc02557947

AG-490 (Tyrphostin B42) Chemical Structure

CAS No. 133550-30-8

AG-490 (Tyrphostin B42, Zinc02557947) 是一种EGFR抑制剂,在无细胞试验中IC50为0.1 μM,作用于EGFR比作用于ErbB2选择性高135倍,对JAK2也有抑制作用,对Lck,Lyn,Btk,Syk和Src没有抑制活性。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 564.48 现货
RMB 647.01 现货
RMB 819.84 现货
RMB 1449.63 现货
RMB 2760.17 现货
RMB 5872.23 现货
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客户使用Selleck生产的AG-490 (Tyrphostin B42)发表文献109篇:

产品安全说明书

EGFR抑制剂选择性比较

生物活性

产品描述 AG-490 (Tyrphostin B42, Zinc02557947) 是一种EGFR抑制剂,在无细胞试验中IC50为0.1 μM,作用于EGFR比作用于ErbB2选择性高135倍,对JAK2也有抑制作用,对Lck,Lyn,Btk,Syk和Src没有抑制活性。
靶点
JAK2 (V617F) [8]
()
EGFR [1]
(Cell-free assay)
0.1 μM
体外研究

AG-490抑制EGF依赖的HER 14细胞增殖,IC50为3.5 μM。[1] 与特异性作用于前B细胞急性白血病(ALL)细胞抑制组成型激活的JAK2 相一致,5 μM AG-490通过诱导程序性细胞死亡,几乎完全抑制所有ALL 细胞生长,而对正常造血功能不会造成有害影响。AG-490不会抑制Lck, Lyn, Btk, Syk, 和 Src激活。[2]AG-490 (60-100 μM) 抑制Stat3sm组成型激活,且抑制自发的或白细胞介素2诱导的蕈菌(MF)肿瘤细胞生长 ,IC50分别为75 μM和 20 μM。[3]通过抑制JAK3和 STAT5a/b.的活性,AG-490有效抑制IL-2调节的人 T 细胞生长, IC50 为 25 μM。[4] 虽然5 μM AG-490 单独给药处理对FDrv210H细胞增殖没有效果,但是AG-490可以协同 STI571而增强 STI571抑制p210bcr-abl促进增殖的效果。[5]AG-490 作用于MOPC, MPC11, 和S194细胞 ,显著抑制Stat3 组成型激活,导致显著的细胞凋亡,这种作用存在剂量依赖性。[6] AG-490 (100 μM) 抑制Akt磷酸化, 抑制核因子-κB激活, 且激活GSK-3β,导致c-Myc降低。AG-490 (50 μM)可以诱导表达Bcr-Abl 突变型T315I 和E255K 的抗Imatinib的BaF3细胞凋亡。[7] 30 μM AG-490 不仅抑制Epo诱导的野生型JAK2磷酸化,也抑制 组成型的JAK2 V617F突变型磷酸化。AG-490作用于BaF3细胞,有效抑制JAK 2 V617F 突变诱导的细胞因子非依赖的细胞生长。[8]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BC3 MVvGeY5kfGmxbjDBd5NigQ>? NILkdpUyODEkgJpCuW0> M1jIOlI1KGh? MlS1cYVlcWG2ZYOgVGVNKGOnbHygZZBweHSxc3nz NVLnOIN{OjZzOES5PVk>
BCBL1 MVzGeY5kfGmxbjDBd5NigQ>? MX6xNFDjiIoEtV2= NGnvZ5QzPCCq M2XwVo1m\GmjdHXzJHBGVCClZXzsJIFxd3C2b4Ppdy=> MV[yOlE5PDl7OR?=
BC3 Ml7XSpVv[3Srb36gRZN{[Xl? MVKxNFDjiIoEtV2= NX7rZXkyOjRiaB?= NYTvRWl3dWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMTDy[YR2[3Srb36= NY\MO2ZwOjZzOES5PVk>
BCBL1 NFTDTVFHfW6ldHnvckBCe3OjeR?= NXKzN3dGOTBy4pEJxtVO NIC0NHQzPCCq NY[xe2xzdWWmaXH0[ZMh\GVvcHjvd5Bpd3K7bHH0bY9vKG:oIGPURXQ{KGOxcoLlcIF1\WRid3n0bEBJW1B5MDDhcoQhUFOIMjDy[YR2[3Srb36= NE\tTIszPjF6NEm5PS=>
BC3 NH\3cIZHfW6ldHnvckBCe3OjeR?= NXnxNnZ{OTBy4pEJxtVO NHTQZ3MzPCCq NYS4fVBtcW6mdXPld{BiKGOxbYDs[ZRmKGG3dH;wbIFocWNiZnz1fOKh MlewNlYyQDR7OUm=
BCBL1 MnTESpVv[3Srb36gRZN{[Xl? MXWxNFDjiIoEtV2= MXWyOEBp M3TkbYlv\HWlZYOgZUBkd22ybHX0[UBifXSxcHjh[4lkKG[udYlCpC=> MlLTNlYyQDR7OUm=
SK-MEL-28 Ml63SpVv[3Srb36gRZN{[Xl? MVO1NE8yODEkgJpCuW0> NEXiSJA1QCCq M1LWUGROW09? NI\iXXpz\WS3Y3XzJIFvd2mtaYOgdoV{cXO2YX7j[S=> NIXqSIkzPTJzNkWyNi=>
MeWo MkHwSpVv[3Srb36gRZN{[Xl? M2HiNlUxNzFyMPMAjeK2VQ>? M4DPXlQ5KGh? Mk\4SG1UVw>? NWXJbG1SemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NGPGUHMzPTJzNkWyNi=>
SK-MEL-5 NGTvR3ZHfW6ldHnvckBCe3OjeR?= NYDhZnVQPTBxMUCw5qCKyrWP MnHNOFghcA>? NYTv[5A1TE2VTx?= M4jDTJJm\HWlZYOgZY5wcWurczDy[ZNqe3SjbnPl M3TwSVI2OjF4NUKy
SK-MEL-2 MnTqSpVv[3Srb36gRZN{[Xl? MY[1NE8yODEkgJpCuW0> Mn36OFghcA>? NI\lXmJFVVOR NWP5UXFYemWmdXPld{Bidm:ra3nzJJJme2m|dHHuZ4U> NGniVJUzPTJzNkWyNi=>
B16-F0 NFTS[GVHfW6ldHnvckBCe3OjeR?= NGnJVlU2OC9zMEFihKnDvU1? M3G1OFQ5KGh? NEXt[lJFVVOR MWDy[YR2[2W|IHHuc4lscXNicnXzbZN1[W6lZR?= NE\KV4ozPTJzNkWyNi=>
TRPM2/HEK  M3y1eWZ2dmO2aX;uJGF{e2G7 M3vXdFAvOeLCk{K1xsDDvU1? M1roTlE2yqCvaX6= MXPEUXNQ MWLy[YR2[2W|IFiyU|IucW6mdXPl[EBE[TJtaX7jdoVie2ViaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJuIHHu[EB1cGViSVO1NOKhfmGudXWge4F{KDFwN9MgxtVO MnnZNlUyPzl3N{S=
U937  MkTOSpVv[3Srb36gRZN{[Xl? MlzZNE4y6oDVMkZCpOK2VQ>? NH[0bWkyPcLibXnu MXzEUXNQ M1\SdJJm\HWlZYOgTFJQOi2rbnT1Z4VlKEOjMjvpcoNz\WG|ZTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6ncjygZY5lKHSqZTDJR|UxyqC4YXz1[UB4[XNiMD60xsDDvU1? M4LaWlI2OTd7NUe0
TRPM2/HEK  NHjZ[VNHfW6ldHnvckBCe3OjeR?= M{HFXVExyqEEtV2= NUHoOXY2PDEEoH3pci=> MlexSG1UVw>? NHzhN|Bz\WS3Y3XzJHRTWE1{IHHjeIl3[XSrb36g[ZZmdiCjdDDobYdpKGOxbnPlcpRz[XSrb37zJI9nKEh{T{K= MVyyOVE4QTV5NB?=
GL37  NYDFeHBpS2WubDDWbYFjcWyrdImgRZN{[Xl? NIXBVYkxNTFywrFCuW0> M3vub|Q5KGh? NX:wZYZNe3WycILld5NmeyCOYTDlfJBz\XO|aX;u NX\HdGtUOjR7OUm2OVc>
NRK-52E NYPOc4p3TnWwY4Tpc44hSXO|YYm= MmfyNeKhyrWP MVexNEBucW5? NXOxcnBP[myxY3vzJJRp\SC|dHnteYxifG:{eTDl[oZm[3Rib3[gRY5oKEmLIH;uJHBigC1{IHX4dJJme3Orb39CpC=> MUOyOFcyODR{Mx?=
NRK-52E MVjGeY5kfGmxbjDBd5NigQ>? NV7VSmhlOcLiwsXN MorNNVAhdWmw M3LoVYJtd2OtczDBcochUUliaX7keYNm\CCFREK0JIV5eHKnc4Ppc44> NVHIRWlVOjR5MUC0NlM>
HSC  NGCw[XFHfW6ldHnvckBCe3OjeR?= NGLMSVEzOCEQvF2= MmnCNUBp MV\hZpJw\2G2ZYOgeIhmKGSrZn\ldoVvfGmjbDDl[oZm[3S|IH;mJIxmeHSrbjDvdkBCT0W| NWDp[YdvOjR4MUSxPVk>
EJ NXfHNWJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DWRlUxNzhyIN88US=> Mo\WNlQwPDhxN{KgbC=> M1\a[IlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M3zEblI1PTh5MES5
EJ MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;GOVAwQDBizszN MnLlOFghcA>? M1zIbINifXOnczDTMZBp[XOnIHHydoV{fA>? Ml3GNlQ2QDdyNEm=
EJ NYn5c4JjTnWwY4Tpc44hSXO|YYm= NGja[mk2OC96MDFOwG0> MnWxOFghcA>? M1fjUIRwf26{ZXf1cIF1\XNiYz3NfYMtKGO7Y3zpcmQyNCC|dYL2bZZqdiCjbnSgWmVITiCneIDy[ZN{cW:wcx?= MWKyOFU5PzB2OR?=
HepG2 MVLGeY5kfGmxbjDBd5NigQ>? MljBOVAuPTByIN88US=> NVXmOnhHPjEEoH3pci=> M1OxUIlvcGmkaYTzJJRp\SCLTD22MYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIDjUfZI4ODVrIHHu[EBUXEGWMzCoWJlzPzB3KTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGTGRmwzPDJ2MkC0Oi=>
SGC7901 NUW0SXRQS2WubDDWbYFjcWyrdImgRZN{[Xl? MoXmNE0yODBizszN MV2yOE81QC95MjDo NVvqbo9U[2G3c3XzJIEhe2mpbnnmbYNidnRicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHTvd4Uu\GWyZX7k[Y51dHliYoX0JI5wfCC2aX3lMYRmeGWwZHXueIx6 NIHnRlEzPDF3MUK1OS=>
AGS  NFT1TnVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MV2wMVExOCEQvF2= M4f0W|I1NzR6L{eyJIg> MXXjZZV{\XNiYTDzbYdvcW[rY3HueEBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh\G:|ZT3k[ZBmdmSnboTsfUBjfXRibn;0JJRqdWVvZHXw[Y5l\W62bIm= NVix[GU2OjRzNUGyOVU>
SGC7901 Mn[xSpVv[3Srb36gRZN{[Xl? NIToelI2OCEQvF2= MVyyOE81QC95MjDo M{\mUJRp\SCuZY\lcJMhd2ZicFrBT|Ih[mWpYX6geI8h\GWlbHnu[UBifCB{NDDodkwh[W6mIILlZo92dmSnZDDheEA4OiCqctMg NW\XZYQyOjRzNUGyOVU>
AGS  M3S5ZmZ2dmO2aX;uJGF{e2G7 NHqw[5E2OCEQvF2= NGjtUmczPC92OD:3NkBp NYjK[XRHfGinIHzleoVteyCxZjDwTmFMOiCkZXfhckB1dyCmZXPsbY5mKGG2IEK0JIhzNCCjbnSgdoVjd3WwZHXkJIF1KDd{IHjyxsA> NUTYWJFwOjRzNUGyOVU>
SGC7901 MUfGeY5kfGmxbjDBd5NigQ>? MorNOVAh|ryP NXm3NVNEOjRxNEivO|IhcA>? M1jYZpRp\SCleYTvdIxie22rYzDsc4NidGm8YYTpc44hd2ZicFrBT|IhMEqDS{KgdIhwe3Cqb4L5cIF1\WRiYYSgdoV{cWS3ZYOgWJlzOTByNzDhcoQhXHm{MUCwPEkh\GWlcnXhd4VlKGGodHXyJGFIPDlyIITy[YF1dWWwdDDmc5IhOjRiYX7kJFQ5KGi{LDDieZQhe3SjcoTl[EB1dyC{ZXLveY5lKGG2IEeyJIhz NF3UbIQzPDF3MUK1OS=>
AGS  MkO3SpVv[3Srb36gRZN{[Xl? NFf4cZo2OCEQvF2= MmTnNlQwPDhxN{KgbC=> MYP0bIUh[3m2b4DsZZNucWNibH;jZYxqgmG2aX;uJI9nKHCMQVuyJEhLSUt{IIDoc5NxcG:{eXzheIVlKGG2IILld4llfWW|IGT5dlExODdiYX7kJHR6ejFyMEipJIRm[3KnYYPl[EBi\nSncjDBS|Q6OCC2cnXheI1mdnRiZn;yJFI1KGGwZDC0PEBpeixiYoX0JJN1[XK2ZXSgeI8hemWkb4Xu[EBifCB5MjDodi=> MVyyOFE2OTJ3NR?=
MC3T3-E1  M17nRWZ2dmO2aX;uJGF{e2G7 NIPrWZU2OCEQvF2= MX20JIg> NHTteolqdmirYnn0d{BJW0VvaX7keYNm\CCETWC3JIFv\CCJSGKgdJJwfGWrbjDlfJBz\XO|aX;uxsA> MUGyN|g4Pzd|NB?=
7TD1-DXM Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPvNYgzOTBizszN NUCxNWZLPzJiaB?= MkDDSG1UVw>? MV7pcohq[mm2czDj[YxtKGe{b4f0bC=> NFjXWo8zOzh5MUG1PS=>
7TD1-WD-90 NV3oPYFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfwVYEyOCEQvF2= MofyO|IhcA>? M1j3c2ROW09? MkfQbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NEXU[FMzOzh5MUG1PS=>
7TD1-DXM M{PB[2Fxd3C2b4Ppd{BCe3OjeR?= NWD4WJFtPTBizszN Ml\mOFghcA>? MkTSSG1UVw>? NGDuXnVqdmS3Y3XzJIFxd3C2b4Ppdy=> MkKxNlM5PzFzNUm=
7TD1-WD-90 M1nh[mFxd3C2b4Ppd{BCe3OjeR?= MmjXOVAh|ryP NUnLRlNVPDhiaB?= MlnsSG1UVw>? MXTpcoR2[2W|IHHwc5B1d3Orcx?= MnrrNlM5PzFzNUm=
7TD1-WD-90  NUjJdolHTnWwY4Tpc44hSXO|YYm= NU\pSHo1PTBizszN MoPHOkBp NIXJc3BFVVOR MkO0d4lodmmoaXPhcpRtgSCrbnjpZol1eyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGpCUzJiYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMx?= M{fiV|I{QDdzMUW5
HepG2  M2D3UmZ2dmO2aX;uJGF{e2G7 MYmxNFAh|ryP MknkNVIwOjRiaB?= MWXpcohq[mm2czDTWGFVOyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> M3roSVI{QDN4NECw
RAW264.7  MXfGeY5kfGmxbjDBd5NigQ>? MXK1NOKh|ryPwrC= NFLJNlQzPC92ODDo NIix[pp{fXCycnXzd4V{KFKDTlvMMYlv\HWlZXSgc5N1\W:lbHHzeI9o\W6nc3nz NGHRUXUzOzZ4NUCxPC=>
RAW264.7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGiwbIkxNTVywrFOwG3DqA>? NEjCRYQ1QMLiaB?= MXPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnLXTldIVv\GWwdHz5 NHWxNW8zOzZ4NUCxPC=>
RAW264.7 MmPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XnclAuPTEEoN88UeKh NWHIO|U1PDkEoHi= MV;jZZV{\XNiYX6gZZJz\XO2IH;mJHJCXzJ4ND63JINmdGy|IHH0JJRp\SCJMD;HNUBxcGG|ZTDv[kB1cGViY3XscEBkgWOuZR?= MlXhNlM3PjVyMUi=
RAW264.7 NFrsZ2tHfW6ldHnvckBCe3OjeR?= NWj6[HgyPTEEoN88US=> M1j2bVI1NzR6IHi= M33ie4lvcGmkaYTzJHJCVkuOLXnu[JVk\WRiTl\BWIMyKGW6cILld5Nqd25iYX7kJJBpd3OyaH;yfYxifGmxbjDv[kBU\XJ5MkfTWGFVOw>? MXiyN|Y3PTBzOB?=
A549  MUTGeY5kfGmxbjDBd5NigQ>? MmLYNlAwPDBizszN M3PZUVIxKGh? MkToNlAh|ryPIFHHOFkxKHO3cIDy[ZN{\XNidHjlJJJi\GmjdHnvck1qdmS3Y3XkJIlvfmG|aX;uJI9nKEF3NEmgZ4VtdHN? MlTuNlM3OjBzOUG=
A549  Mnu2SpVv[3Srb36gRZN{[Xl? NHG2d2gyOC9{MD:0NEDPxE1? NFzQOJAzPCCq M2H3fZN2eHC{ZYPz[ZMhfGinIILh[IlifGmxbj3pcoR2[2WmIHXs[ZZifGmxbjDv[kBXTUeIwrC= MXSyN|YzODF7MR?=
HUVECs MWjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MW[yNEDDvU1? NUfQdWNbPCCq NF7Mc21ifHSnboXheIV{KEh{T{KtbY5lfWOnZDDj[YxtKHOqcnnub4Fo\SCjbnSgbY1xem:4ZXSgeIhmKGG2dHHjbI1mdnRicnH0[UBw\iC2aHWgZ4VtdHN? M4XHRVI{PDh|OUS2
HUVECs MoDlRZBweHSxc3nzJGF{e2G7 NIHJUGQzOCEEtV2= M3vCeFQhcA>? NWm2OYV{e2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKGOnbHygZZBweHSxdHnjJIlv\GW6 NHHnT5gzOzR6M{m0Oi=>
BV-2  MVnGeY5kfGmxbjDBd5NigQ>? MWWyNEDDvU1? M4PSc|E3KGh? MnnTbY5pcWKrdIOgUHBUNWmwZIXj[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIgh[Wyvb4P0JINwdXCuZYTlcJkh\GmvaX7pd4hm\CCrTl;TJIV5eHKnc4Ppc44> M2f6R|I{OjN4M{ew
NRK-52E  M1zqcmZ2dmO2aX;uJGF{e2G7 MYO1xsDPxE1? Ml63N|DDqG2rbh?= NVvzSHdC[XS2ZX71ZZRmeyCDbnetLFHjiJN5KT3pcohq[mm2ZXSgWGdHNc7{MTDtVm5CKGG2IEG2xsBpyqB? MmjxNlMyPzR5NUe=
SW620  NXzyZVNwTnWwY4Tpc44hSXO|YYm= NGPaXVAzOCEEtV2= NGS0Sm8yNzZiaB?= M4K2S4lvcGmkaYTzJJAuW1SDVEOgZYN1cX[jdHnvci=> NFzUZ44zOzFzME[yOS=>
RPE  NXe5SoVFTnWwY4Tpc44hSXO|YYm= M1jOTlMxKML3TdMg NEHiSZo{KGh? NVvnc5dYcW6qaXLpeJMhfGinIHnu[JVkfGmxbjDv[kBxNVOWQWSzJIV5eHKnc4Ppc44> M3;DV|I{ODl2ME[3
SW1116 NVOwemZsTnWwY4Tpc44hSXO|YYm= MWGxNFAhyrWPwrC= NHPUOWIzPC92OD:3NkBp M1vV[IRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBLSUt{IHHu[EBxUkGNMjD0bY1mNWSncHXu[IVvfGy7 MYWyNlA2ODd7MB?=
HT29 MnHjSpVv[3Srb36gRZN{[Xl? MmnnNVAxKML3TdMg M1H4OlI1NzR6L{eyJIg> NVHlO|c2\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKEqDS{KgZY5lKHCMQVuyJJRqdWVvZHXw[Y5l\W62bIm= MljRNlIxPTB5OUC=
SW1116 NITGV|dHfW6ldHnvckBCe3OjeR?= M{PQeFExOCEEtV5CpC=> NXvLO|hVOjRxNEivO|IhcA>? MoLY[IVkemWjc3XzJJRp\SCyU2TBWFMhdGW4ZXzzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyxsA> M{TzblIzODVyN{mw
HT29 MWPGeY5kfGmxbjDBd5NigQ>? MYmxNFAhyrWPwrC= MonZNlQwPDhxN{KgbC=> NIO2Xm1l\WO{ZXHz[ZMhfGinIIDTWGFVOyCuZY\lcJMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZLDqA>? M1;lXFIzODVyN{mw
ARPE-19 M3HJd2Z2dmO2aX;uJGF{e2G7 NGLEfZk2yqEQvF2= NXLZO2VQOzEEoH3pci=> M4i3NIlvcGmkaYTzJGpCUzJicHjvd5Bpd3KrbHH0bY9v MnX4NlE3OjB7NkO=
HSC-T6 M4\qdGFxd3C2b4Ppd{BCe3OjeR?= MXqxNOKh|ryP M2K5eVLDqGkEoB?= M{iyNYlvcGmkaYTzJJRp\SCjcH;weI9{cXNib3[gTHNENVR4IHPlcIx{KGmwZIXj[YQh[nliQ1TF NV24cFRoOjF|OU[5PVg>
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MZ-54 NInKc5pHfW6ldHnvckBCe3OjeR?= NXHuWo1XPTBxMUCwxsDPxE1? MXO0PEBp NIf5TGRz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NEXOOYQzODV6OUWyOS=>
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MZ-304 MmnaSpVv[3Srb36gRZN{[Xl? M3exblUxNzFyMNMg{txO M3;n[FQ5KGh? NITGZ4xz\WS3Y3XzJJRp\SCuZY\lcJMhd2ZiY3;ud5RqfHW2aY\lcJkh[WO2aY\heIVlKFOWQWSzJIlvKGFidHnt[U1l\XCnbnTlcpQh[W6mIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NILwfFEzODV6OUWyOS=>
A-172 NUi2VZhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki3OVAwOTBywrFOwG0> MlHOOFghcA>? MoDOcIVi\HNidH:gZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70JJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib4\ldkBiKHSrbXWgdIVzcW:mIH;mJFQ5yqCq NHnJR2UzODV6OUWyOS=>
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MZ-54 M3rxcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXK1NE8yODEEoN88US=> MWK0PEBp MVvs[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MoPUNlA2QDl3MkW=
MZ-256 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVu1NE8yODEEoN88US=> NIjDd4w1QCCq MY\s[YFleyC2bzDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCxdnXyJIEhfGmvZTDw[ZJqd2Rib3[gOFjDqGh? MmS4NlA2QDl3MkW=
MZ-304 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLPOVAwOTBywrFOwG0> NVO4NHk3PDhiaB?= NVHINZZXdGWjZIOgeI8h[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51KHKnZIXjeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gc5ZmeiCjIITpcYUheGW{aX;kJI9nKDR6wrDo Ml:yNlA2QDl3MkW=
A-172 NWTXbXpiTnWwY4Tpc44hSXO|YYm= M{nOR|UxNzFyMNMg{txO M1TkSlQ5KGh? MVzpcohq[mm2czDtbYdz[XSrb36= Mo[5NlA2QDl3MkW=
MZ-18 NGjIVGFHfW6ldHnvckBCe3OjeR?= NUjhNJA3PTBxMUCwxsDPxE1? NHjIUoE1QCCq NWLycHpJcW6qaXLpeJMhdWmpcnH0bY9v Ml3kNlA2QDl3MkW=
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MZ-256 MV\GeY5kfGmxbjDBd5NigQ>? Mlu1OVAwOTBywrFOwG0> NFXB[Yg1QCCq MlT5bY5pcWKrdIOgcYloemG2aX;u MmXhNlA2QDl3MkW=
MZ-304 MmrSSpVv[3Srb36gRZN{[Xl? NFvRUlM2OC9zMEFCpO69VQ>? MnvQOFghcA>? MUXpcohq[mm2czDtbYdz[XSrb36= MV:yNFU5QTV{NR?=
A-172 NIThT3BHfW6ldHnvckBCe3OjeR?= M3PSS|ExOMLizszN NWT5bHN4PDhiaB?= MoPMbY5pcWKrdIOgbY53[XOrb36= M1HvZlIxPTh7NUK1
MZ-18 MlL6SpVv[3Srb36gRZN{[Xl? MmTONVAxyqEQvF2= M1rwfFQ5KGh? MYHpcohq[mm2czDpcpZie2mxbh?= MVqyNFU5QTV{NR?=
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MZ-304 M2S1RWZ2dmO2aX;uJGF{e2G7 NWL5d3J6OTBywrFOwG0> NH\a[I41QCCq NYDaR3NPcW6qaXLpeJMhcW64YYPpc44> MkLyNlA2QDl3MkW=
A-172 MXHGeY5kfGmxbjDBd5NigQ>? MYO1NE8yODEEoN88US=> MYe0PEBp Mkn3doVlfWOnczD0doFve2O{aYD0bY9vKG:oIF3NVEBo\W6nczDhcoQhemWmdXPld{Bmdnq7bXH0bYMh[WO2aY\peJkhd2ZiTV3Qdy=> NHPvcHgzODV6OUWyOS=>
MZ-18 MX7GeY5kfGmxbjDBd5NigQ>? NU\GR2pjPTBxMUCwxsDPxE1? NWnrfZBzPDhiaB?= NVLCWJFyemWmdXPld{B1emGwc3PybZB1cW:wIH;mJG1OWCCpZX7ld{BidmRicnXkeYNmeyCnbor5cYF1cWNiYXP0bZZqfHlib3[gUW1Rew>? NXH3VZd7OjB3OEm1NlU>
MZ-54 MkPuSpVv[3Srb36gRZN{[Xl? M1nBPFUxNzFyMNMg{txO M17BTVQ5KGh? NGH1V3hz\WS3Y3XzJJRz[W6|Y4LpdJRqd25ib3[gUW1RKGenbnXzJIFv\CC{ZXT1Z4V{KGWweontZZRq[yCjY4Tpeol1gSCxZjDNUXB{ M3exfVIxPTh7NUK1
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MZ-304 MojZSpVv[3Srb36gRZN{[Xl? M3OzSVUxNzFyMNMg{txO MYS0PEBp M3\YdJJm\HWlZYOgeJJidnOlcnnweIlwdiCxZjDNUXAh\2WwZYOgZY5lKHKnZIXj[ZMh\W68eX3heIlkKGGldHn2bZR6KG:oIF3NVJM> M13meFIxPTh7NUK1
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SW1990 M{exRmZ2dmO2aX;uJGF{e2G7 M4DXT|IxKM7:TR?= NGrrNW4zPCCq NHT5Voll\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhVU2SLUKgZY5lKF[HR1[gcXJPSXN? MmD5NlA1QDJ6NUi=
SW1990 NUiyTnVqTnWwY4Tpc44hSXO|YYm= MVOyNEDPxE1? Ml7ONlQhcA>? NH7hVIxl\WO{ZXHz[ZMhfGinIHnueIVve2m2eTDv[kBxNVO2YYSzJIV5eHKnc4Ppc44> NVjwW5hTOjB2OEK4OVg>
SW1990 MlfJTY53[XOrb36gRZN{[Xl? MnPINlAh|ryP M1\E[lI1KGh? M1jifZJm\HWlZYOgbY53[XOrb36gc4YhW1dzOUmwJINmdGy|wrC= MWSyNFQ5Ojh3OB?=
THP1 NF;mW|RHfW6ldHnvckBCe3OjeR?= NInVcYsyOCC3TR?= M2[zelMxKG2rbtMg M2H1VIlvcGmkaYTzJHNVSVR|IIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCkeTDveoVzKDZyJR?= NYjHNFFROjB|OUO2PVA>
BMMC NUT0WHJ[TnWwY4Tpc44hSXO|YYm= NX3pOmR[OC1zMDFOwG0> Ml\lNVXDqG2rbh?= NWSwfGd2cW6qaXLpeJMhVFSFNNMgdoVt\WG|ZTDpckBiKGSxc3Wt[IVx\W6mZX70JIZie2irb36ge4l1cCCwZXHyJINwdXCuZYTlJIlvcGmkaYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh6qn-MUFCpO69VQ>? M3nCNlE6QDN3OES1
A549 NGfleYRHfW6ldHnvckBCe3OjeR?= MXKxOUDPxG1? MkexNUBp NWC0NmlqcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSCxbjD0fZJwe2mwZTC3NFEhf2G|IHTleIVkfGWmIEG1JI1qdiCjZoTldkBUWEViQjD0doVifG2nboS= MoHvNVk5ODF4NkW=
OVCAR-3 NHPmbYNHfW6ldHnvckBCe3OjeR?= M1;1W|ExKHWP MoPENUBp MlXKbY5pcWKrdIOgUHBCNWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w NYDjR5pROTl4NEezOlM>
PA-1 NFrIWJFHfW6ldHnvckBCe3OjeR?= M4mzV|ExKHWP NYSwe3pPOSCq NWq1U|JtcW6qaXLpeJMhVFCDLXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;u MYqxPVY1PzN4Mx?=
OVCAR-3 NH7SdXBHfW6ldHnvckBCe3OjeR?= NF;ZXpAyOCC3TR?= M{P1fVEhcA>? MnTxbY5pcWKrdIOgJGxRSS2rbnT1Z4VlKG:4YYLpZY4h[2GwY3XyJINmdGxibX;0bYxqfHl? NWP6[FNSOTl4NEezOlM>
PA-1 MXXGeY5kfGmxbjDBd5NigQ>? NVTDPVFTOTBidV2= MoTZNUBp M{nOdYlvcGmkaYTzJEBNWEFvaX7keYNm\CCxdnHybYFvKGOjbnPldkBk\WyuIH3veIltcXS7 NEWwRYsyQTZ2N{O2Ny=>
Jurkat  NVfPWYZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWmzWmVIPTBizszN NGfib2wzPC92OD:3NkBp MXLlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= MUKxPVU3PDh7MR?=
SUPT1  MoLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nGcVUxKM7:TR?= NWP4O3hyOjRxNEivO|IhcA>? MVLlcohidmOnczDUVmFKVC2rbnT1Z4V{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36= M4PnW|E6PTZ2OEmx
Jurkat  M13qbmFxd3C2b4Ppd{BCe3OjeR?= M3vRVVUxKM7:TR?= NVTlPVRCOjRxNEigbC=> MmXF[Y5p[W6lZYOgWHJCUUxvaX7keYNmeyClZXzsJIFxd3C2b4Ppdy=> NFzXXlkyQTV4NEi5NS=>
SUPT1  NY\xO3dJSXCxcITvd4l{KEG|c3H5 NWr0ZpVnPTBizszN NWDSfoo2OjRxNEigbC=> NYPYZpVT\W6qYX7j[ZMhXFKDSVytbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NX;DcIpuOTl3NkS4PVE>

... Click to View More Cell Line Experimental Data

体内研究 AG-490处理,大幅降低 CD45+和HLA-DR+ 细胞数,作用于骨髓时,这两种细胞数分别从48% 和46%降低到不可检测水平,作用于未处理小鼠脾脏时,这两种细胞数分别从 38%和 22% 降低到不可检测水平。[2] 在体内,AG-490 处理,引起小鼠骨髓瘤细胞凋亡,但是不抑制IL-12诱导的巨噬细胞活化和IFN-γ产量。[6]与在体外抑制 JAK2 V617F 突变活性一致,AG-490每天按0.5 mg处理裸鼠 10天,高效抑制JAK2 V617F突变诱导的肿瘤形成和肿瘤细胞入侵。[8]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验: [1] [2]
- 合并

体外激酶自磷酸化检测:

AG-490溶于DMSO 10%-H2O-乙醇 45%。原油膜提取物 (0.125 μg/mL)与EGF (20 nM) 在50 mM HEPES buffer, pH 7.6, 和125 mM NaCl中在 4oC下预温育15分钟。在V形 96孔板上进行 EGFR 或 ErbB2激酶自磷酸化活性检测,在4oC 进行30分钟。在含反应混合物(12 μL, 50mM, HEPES, pH 7.4,125 mM NaCl, 12 mM M8Ac2, 2 mM MnCl2, 1 mM NaVO3, 1 μM ATP, 及1 μCi[γ-32P]ATP,) 及浓度不断增高的AG-490 (4 μL)的每孔中加入膜抽提物(8 μL)。加入热样本缓冲液终止反应,样本在6% SDS-聚丙烯酰胺凝胶电泳微小胶体上跑胶,然后烘干凝胶,在线性处理时间进行自显影。扫描受体带,然后通过Ez-Fit 程序分析结果。 为了分析 JAK2, JAK2的自磷酸化,使用从G2期细胞得到的裂解物抗JAK2抗体,进行免疫沉淀,与浓度不断增高的AG-490(0-50 μM)预处理16小时。免疫复合物与抗磷酸抗体进行免疫印迹。通过测量JAK2自磷酸化而测定对体外激酶活性的抑制情况。
细胞实验:[2]
- 合并
  • Cell lines: Pre-B ALL
  • Concentrations: 溶于DMSO, 终浓度为~ 50 μM
  • Incubation Time: 16小时
  • Method: 使用不同浓度AG-490 处理细胞16小时。为了测定细胞增殖,加入[3H]胸甘(1 μCi) 培养,6小时或更长时间以后终止培养。收集细胞,样本在液体闪烁计数器上计数。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 静脉注射ALL 细胞的SCID小鼠
  • Dosages: 每天0.85 mg + 0.5 mg
  • Administration: 持续输液泵输液加之以每天腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 58 mg/mL (197.07 mM)
Water Insoluble
Ethanol '6 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG300+5% Tween80+50% ddH2O
6.25 mg/ml

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 294.30
化学式

C17H14N2O3

CAS号 133550-30-8
储存条件 粉状
溶于溶剂
别名 Zinc02557947

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    I would like to know whether AG490 (S1143) goes to CNS through BBB, or not?

  • 回答:

    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