Tivantinib (ARQ 197) 化学構造
分子量: 369.42

高品質保証

カスタマーフィードバック(1)

Quality Control & MSDS

製品説明

  • Compare c-Met Inhibitors
    c-Met製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 Tivantinib (ARQ 197)は、小説と選択的な人間のc-Met受容体型チロシンキナーゼ阻害剤で、 IC50 が0.1 μM。
ターゲット c-Met
IC50 0.355 μM (Ki) [1]
In vitro試験 ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549, DBTRG and NCI-H441 cells with IC50 of 0.38, 0.45, 0.29 μM. Treatment with ARQ-197 results in a decrease in phosphorylation of the MAPK signaling cascade and prevention of invasion and migration. In addition, ectopic expression of c-Met in NCI-H661, a cell line having no endogenous expression of c-Met, causes it to acquire an invasive phenotype that is also suppressed by ARQ-197. Although the addition of increasing concentrations of ARQ-197 does not significantly affect the Km of ATP, exposure of c-Met to 0.5 μM ARQ-197 decreased the Vmax of c-Met by approximately 3-fold. The ability of ARQ-197 to decrease the Vmax without affecting the Km of ATP confirmed that ARQ-197 inhibits c-Met through a non–ATP-competitive mechanism and may therefore account for its high degree of kinase selectivity. ARQ-197 prevents human recombinant c-Met with a calculated inhibitory constant Ki of approximately 355 nM. Although the highest concentration of ATP used is 200 μM, the potency of ARQ-197 against c-Met is not reduced by using concentrations of ATP up to 1 mM. ARQ-197 blocks c-Met phosphorylation and downstream c-Met signaling pathways. ARQ-197 suppresses constitutive and ligand-mediated c-Met autophosphorylation and, by extension, c-Met activity, in turn leading to the inhibition of downstream c-Met effectors. ARQ-197 induction of caspase-dependent apoptosis is increased in c-Met–expressing human cancer cells including HT29, MKN-45, and MDA-MB-231 cells.[1][2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MNK-45 MnO5T4lv[XOnIHHzd4F6 NWHhelNkhjFyIN88US=> NFXzZ2RqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MXuyNFQ5PDBzOB?=
HT29 NILoWXVMcW6jc3WgZZN{[Xl? MmDNglExKM7:TR?= MWfpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NWHsOlV{OjB2OESwNVg>
MDA-MB-231 NIjrR4pMcW6jc3WgZZN{[Xl? M2\Te54yOCEQvF2= NVnVV|FvcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> M{PXUlIxPDh2MEG4
NCI-H441 MVLLbY5ie2ViYYPzZZk> NIH4cWx,OTBizszN M{XXbIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NXHKTZFrOjB2OESwNVg>
SK-MEL-28 M1y0fmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVOzN{DPxE1? MoPjTWM2OD5|MzFOwG0> NFXyOoIzODR6NECxPC=>
NCI-H661 MoDDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{LjNVM{KM7:TR?= M361eGlEPTB-M{Og{txO Mn:1NlA1QDRyMUi=
NCI-H446 NIHodoFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPvcGU{OyEQvF2= MmXyTWM2OD15IN88US=> M{npRVIxPDh2MEG4
MDA-MB-231 NXXLe2w1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVOzN{DPxE1? M{frWmlEPTB;MD61OUDPxE1? MoDrNlA1QDRyMUi=
DLD-1 NEWxZm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPGUYc{OyEQvF2= NGDoNJNKSzVyPUCuOVMh|ryP MVKyNFQ5PDBzOB?=
A549 M{fRR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWLDOYpiOzNizszN NF;wcHdKSzVyPUCuOVkh|ryP MVSyNFQ5PDBzOB?=
SK-OV-3 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{DaeFM{KM7:TR?= NVfwS493UUN3ME2wMlY3KM7:TR?= MV:yNFQ5PDBzOB?=
NCI-H460 Mn:3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NET4PWQ{OyEQvF2= MWHJR|UxRTBwNjFOwG0> MVOyNFQ5PDBzOB?=
A375 Mmq4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml30N|Mh|ryP MmOyTWM2OD1yLkSyJO69VQ>? NGL0TpczODR6NECxPC=>
NCI-H441 NWj4[WxET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlvoN|Mh|ryP NV\4UGc3UUN3ME2wMlMh|ryP Mk[5NlA1QDRyMUi=
HT29 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPhN|Mh|ryP MkXMTWM2OD1yLkS5JO69VQ>? NIrabJUzODR6NECxPC=>
MKN-45 NUHRSmZOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUD0cJlSOzNizszN MVXJR|UxRTBwNUig{txO MYiyNFQ5PDBzOB?=
HT29 NVXRU49OSXCxcITvd4l{KGG|c3H5 Ml7xglExKM7:TR?= NV;pfWtFe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu MVOyNFQ5PDBzOB?=
MKN-45 NWfHW5JpSXCxcITvd4l{KGG|c3H5 NEWxTWR,OTBizszN NF23bpp{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= M{Hoe|IxPDh2MEG4
MDA-MB-231 M1;6T2Fxd3C2b4Ppd{Bie3OjeR?= Ml;WglExKM7:TR?= NFnwZmVud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu NFyze5EzODR6NECxPC=>
MDA-MB-231/TGL NVzqW4xsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIS0ZW5,OTByIN88US=> MlrjS2k2OD1zLkKg{txO Mn35NlIxOjd4OUC=
1833/TGL MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3H4TZ4yODBizszN M4DydmdKPTB;Mz63JO69VQ>? MYWyNlAzPzZ7MB?=
EBC1 NXnFWoNlS3m2b4TvfIlkyqCjc4PhfS=> MnS2glExKM7:TR?= MW\pcohq[mm2czD0bIUh[2WubDDndo94fGhw NWn4TGdUOjN3OUiyO|Y>
SNU638 MVLDfZRwfG:6aXRCpIF{e2G7 NUj5RlV5hjFyIN88US=> NFzrT2lqdmirYnn0d{B1cGViY3XscEBoem:5dHiu MlXINlM2QTh{N{[=
A549 NED6W3NEgXSxdH;4bYPDqGG|c3H5 M4TWWJ4yOCEQvF2= NIW1Zmdvd3RiYX\m[YN1 M3;ldlI{PTl6Mke2
H460 NIW0OWpEgXSxdH;4bYPDqGG|c3H5 MlrjglExKM7:TR?= MlHUco91KGGoZnXjeC=> M{PDNFI{PTl6Mke2
HCC827 NE\sU21EgXSxdH;4bYPDqGG|c3H5 NYe3OldlhjFyIN88US=> MnKzco91KGGoZnXjeC=> NHvTPWEzOzV7OEK3Oi=>
A549 MmHzSpVv[3Srb36gZZN{[Xl? MVWxNEDPxE1? M4\yWoRqe3K3cITzJI1q[3KxdIXieYxm NVTEVpVvOjN3OUiyO|Y>
EBC1 M3TyWmZ2dmO2aX;uJIF{e2G7 MYOxNEDPxE1? NIDxbZhlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? MmXjNlM2QTh{N{[=
H460 NWHGV215TnWwY4Tpc44h[XO|YYm= MkfCNVAh|ryP NFK1XJBqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w M4HIflI2OzF|MEGw
K562/VCR NVLBZ3U2S3m2b4TvfIlkyqCjc4PhfS=> MmPrglExKM7:TR?= MUXzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NXfacoczOjV|MUOwNVA>
CEM/VBL NHnweGVEgXSxdH;4bYPDqGG|c3H5 MWD+NVAh|ryP M1jETZNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= NXLwZ3BnOjV|MUOwNVA>
U266 MUHDfZRwfG:6aXRCpIF{e2G7 MoPTglMh|ryPwrC= NUnMS2NOUUN3ME2xMlEh|ryP M4XYSFI2QDFyMEGz
OPM-2 NF6yVpREgXSxdH;4bYPDqGG|c3H5 NG\YeHN,OyEQvF5CpC=> NUHtTpprUUN3ME2xMlgh|ryP NWrkcnJyOjV6MUCwNVM>
MM.1S M4\3bGN6fG:2b4jpZ:Kh[XO|YYm= NGjBU2p,OyEQvF5CpC=> M37jWGlEPTB;MT62JO69VQ>? MmKzNlU5OTByMUO=
MM.1R MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEjxRpI{KM7:TdMg NX\NVmJ{cW6qaXLpeJMh[2WubDDndo94fGhiYomgOFkm NFL6flEzPThzMECxNy=>
RPMI-8226 M3;1WmN6fG:2b4jpZ:Kh[XO|YYm= NVnOfoFzhjNizszNxsA> NFToPIxKSzVyPUCuPUDPxE1? M1;FNVI2QDFyMEGz
ANBL-6 MVfDfZRwfG:6aXRCpIF{e2G7 MV2xJO69VcLi M{nz[4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl Mk\KNlU5OTByMUO=
ANLB-6/V10R Ml7rR5l1d3SxeHnjxsBie3OjeR?= MXKxJO69VcLi M1fQdYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NVzVXYxzOjV6MUCwNVM>
KAS-6/1 NXPXSY1GS3m2b4TvfIlkyqCjc4PhfS=> MmGzNUDPxE4EoB?= M4jxVolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NIPZR2YzPThzMECxNy=>
KAS-6/V10R Ml\nR5l1d3SxeHnjxsBie3OjeR?= Mly0NUDPxE4EoB?= NFHhOWhqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MX6yOVgyODBzMx?=
KAS-6/R10R NHPCV|FEgXSxdH;4bYPDqGG|c3H5 NFLTeokyKM7:TdMg MmfJbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NWPmeJZLOjV6MUCwNVM>
8226/S MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml\zN{DPxE4EoB?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= MXeyOVgyODBzMx?=
8226/LR-5 MmfBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoTtN{DPxE4EoB?= NXWxSXJKcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm MlvLNlU5OTByMUO=
Huh7 M3nscGN6fG:2b4jpZ:Kh[XO|YYm= MoHTglQvQCEQvF5CpC=> MYrEUXNQ MXzJR|UxRTlwOTDuUS=> MUSyOlI2QTJ3MB?=
Hep3B MYTDfZRwfG:6aXRCpIF{e2G7 MVP+OE45KM7:TdMg NFPPXmpFVVOR MYrJR|UxRTR2OD63JI5O M3PrUFI3OjV7MkWw
HepG2 MYnDfZRwfG:6aXRCpIF{e2G7 NFrHVnd,PC56IN88UeKh NFHTc2xFVVOR Mnm3TWM2OD1zM{muO|chdk1? NX62SYtUOjZ{NUmyOVA>
Chang NFS3cI5EgXSxdH;4bYPDqGG|c3H5 NGTvSGt,PC56IN88UeKh MmnrSG1UVw>? MmP3TWM2OD12NEiuO{BvVQ>? NUD3XGl[OjZ{NUmyOVA>
Huh7 NYPOWFVwTnWwY4Tpc44h[XO|YYm= MUSxMlYh|ryPwrC= M1fVTWROW09? M2rqS4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NUDQb4dsOjZ{NUmyOVA>
Hep3B NU\yOVhjTnWwY4Tpc44h[XO|YYm= NVT2cYtVOS54IN88UeKh NVO2PGNpTE2VTx?= MX;jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NX\rdGZDOjZ{NUmyOVA>
HepG2 NYXFRZlkTnWwY4Tpc44h[XO|YYm= M3\peFEvPiEQvF5CpC=> NI\2bldFVVOR M4O4foNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NIP6UYUzPjJ3OUK1NC=>
Chang MUHGeY5kfGmxbjDhd5NigQ>? MoL1NU43KM7:TdMg NYXpO3FFTE2VTx?= MWDjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NUmzVFZQOjZ{NUmyOVA>
MHCC97L MnvOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2q2U54yOCEQvF2= NGDwc3RFVVOR MUnJR|UxRTNzNTDuUS=> MX[yOlQ2QDl3Mx?=
MHCC97H NFLuO4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHTYSVR,OTBizszN M1zJPWROW09? NFW5[29KSzVyPUO2PQKBkSCwTR?= M2jsSlI3PDV6OUWz
Huh7 NEfX[XBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1vKcJ4yOCEQvF2= NGTvT5RFVVOR MmDXTWM2OD1{NkWgcm0> Mn:3NlY1PTh7NUO=
HepG2 NHXsS3JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn23glExKM7:TR?= MVnEUXNQ M1:3bmlEPTB;M{myJI5O NG\Fd28zPjR3OEm1Ny=>
MHCC97L M4jNTWZ2dmO2aX;uJIF{e2G7 MVKxJO69VcLi Mn7mSG1UVw>? NY\FelJRcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NEHudlIzPjR3OEm1Ny=>
Huh7 NF;uRlhHfW6ldHnvckBie3OjeR?= M2O2blEh|ryPwrC= MojZSG1UVw>? NHyxN3ZqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MYCyOlQ2QDl3Mx?=
MHCC97L MWfBdI9xfG:|aYOgZZN{[Xl? MWqxJO69VcLi MULEUXNQ NHXX[YZqdmS3Y3XzJIFxd3C2b4Ppdy=> NGPHdFgzPjR3OEm1Ny=>
Huh7 M3W2UWFxd3C2b4Ppd{Bie3OjeR?= NVn2UWVyOSEQvF5CpC=> NETzVHBFVVOR NWn4SmhScW6mdXPld{BieG:ydH;zbZM> NWrLZlFtOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts MY\LbY5ie2ViYYPzZZk> NULPSXF7OjVizszN MVzEUXNQ M4LNO5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MmLlNlA2OzR|NEW=
H23 NXvmUHpWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml7oNlUh|ryP NX7NT4ZtTE2VTx?= MWnzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= M3jvRVIxPTN2M{S1
WM35 M4XzRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHvUNYoyOCEQvF2= NVz5XZlqTE2VTx?= MUjzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= M1HJc|IxPTN2M{S1
NIH 3T3 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVL4UoM6OTBizszN MYXEUXNQ Mm\E[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MkXUNlA2OzR|NEW=
H838 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX3WTHY4OTBizszN MX7EUXNQ MoXJ[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 M2DMe|IxPTN2M{S1
H1395 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MorLNVAh|ryP NX3rUIpGTE2VTx?= MXjkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= M1TtV|IxPTN2M{S1
Quiescent S2 NInHfHNMcW6jc3WgZZN{[Xl? NF[2Upg{OCEQvF2= M2rZO2ROW09? MnTTZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| Ml3ONlE2OTh7MUW=
PC3 MonZRZBweHSxc3nzJIF{e2G7 MlTUNlAh|ryP MmPZSG1UVw>? MlnxbY5lfWOnczDhdI9xfG:|aYO= MWCyNVcxQTF|MB?=
Du145 MVLBdI9xfG:|aYOgZZN{[Xl? MYOyNEDPxE1? MVjEUXNQ NYr4eYE2cW6mdXPld{BieG:ydH;zbZM> NVXQfGYyOjF5MEmxN|A>
LNCaP M4XQZmFxd3C2b4Ppd{Bie3OjeR?= MWiyNEDPxE1? MU\EUXNQ Moi4bY5lfWOnczDhdI9xfG:|aYO= MYeyNVcxQTF|MB?=
LAPC-4 M2fMPWFxd3C2b4Ppd{Bie3OjeR?= NXXzbnNzOjBizszN NWP4XmxuTE2VTx?= NX\3VGFvcW6mdXPld{BieG:ydH;zbZM> M1XhfVIyPzB7MUOw
LNCaP MUfGeY5kfGmxbjDhd5NigQ>? MUWyNEDPxE1? NGfMb3pFVVOR Mlnu[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NIr4WHYzOTdyOUGzNC=>
LAPC-4 M{HLZWZ2dmO2aX;uJIF{e2G7 MYmyNEDPxE1? NGLDcHJFVVOR NG\DU5dl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NFLXfHgzOTdyOUGzNC=>
Kasumi-1 M3fIPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXX+OVAh|ryP M3vXPGROW09? MnzhbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M{HMWFI{OzlyNUO2
SKNO-1 M{GxNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXXvUXNIhjVyIN88US=> MofnSG1UVw>? NEK3RYpqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M1uxSlI{OzlyNUO2
Kasumi-1 Ml\YT4lv[XOnIHHzd4F6 M4DM[J4yOCEQvF2= MnzZSG1UVw>? MWDy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= M1naUFI{OzlyNUO2
SKNO-1 NETyepZMcW6jc3WgZZN{[Xl? NHK1VGh,OTBizszN M3\rbWROW09? MX3y[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NF;IXmczOzN7MEWzOi=>
A549 MUDGeY5kfGmxbjDhd5NigQ>? MYexNEDPxE1? MY\EUXNQ MoTn[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> MkHpNlQ4PDZ3N{S=
NRK-52E M4HrPGZ2dmO2aX;uJIF{e2G7 MWqxNEDPxE1? M3HSWmROW09? MlnXbY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiU2TBWFMhdnWlbHXhdkB1emGwc3zvZ4F1cW:wIHHu[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEBkd2yuYXflckBKXiCjbnSg[oljem:wZXP0bY4> NHjzW4wzPTB6OECwNi=>
PC12 NIDjPHpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWX+NVIvPSEQvF2= MU\EUXNQ MnG3dJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> MYeyOVEzQDN6Nh?=
HPMCs M4j0Z2Z2dmO2aX;uJIF{e2G7 MmXFdoV3\XK|ZYOg[ZBqfGinbHnhcEB1dyCvZYPlcoNpgW2jbDD0doFve2m2aX;uJI9nKGi3bXHuJJBmemm2b37lZYwhdWW|b4To[Yxq[WxiY3XscJM> MV:yOlA1PTd6MB?=
A549 M2HBZWZ2dmO2aX;uJIF{e2G7 M1qzSJ42OCEQvF2= NWjOZYVZTE2VTx?= Mn\xZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> NX\0NXU{OjZ5MUG3OFg>
RAW264.7 NIj2dZhHfW6ldHnvckBie3OjeR?= NGHXWYZ,OzBizszN NW\3U4djTE2VTx?= M1zyNpJm\HWlZYOgdJJwNWmwZnzhcY1ifG:{eTDn[Y5mKGW6cILld5Nqd25? MViyOlcyQDV6Nh?=
MEMM MnXJT4lv[XOnIHHzd4F6 MmjqNVUhyrWP NW\pW3lFTE2VTx?= NWrT[IJu\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> NVXweZR{OjZ7MkG1NFY>
MEMM NVLiV5J2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnTjglIxKML3TR?= NYXXZYJuTE2VTx?= NF7nWmtqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NULnVoJmOjZ7MkG1NFY>
MEMM Mn;TRZBweHSxc3nzJIF{e2G7 MUOxOUDDvU1? MoD1SG1UVw>? M{HwNolv\HWlZYOgeIhmKHC{ZYPlcoNmKG:oIITo[UBieG:ydH;zbZMheHKxdHXpckwh[2ynYY\l[EBE[XOyYYPlMVM> MYWyOlkzOTVyNh?=
T47D M2r6d2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWGxNEDPxE1? MXLEUXNQ NX7Ee40{UUN3ME23NkBvVQ>? MnPBNVg{QDF2NES=
ZR-75-1 Ml\1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVSxNEDPxE1? MnPYSG1UVw>? MonlTWM2OD15OTDuUS=> M2[5XVE5OzhzNES0
BT474 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlLUNVAh|ryP MWDEUXNQ MYfJR|UxRTh4IH7N M2na[VE5OzhzNES0
HCC1954 MmHUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4HST|ExKM7:TR?= M4HMeWROW09? MoO3TWM2OD1zMUmgcm0> NYHiSVljOTh|OEG0OFQ>
MDA-MB-453 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDUNY4yOCEQvF2= Ml;0SG1UVw>? M3vCW2lEPTB;OUe1JI5O MXOxPFM5OTR2NB?=
MDA-MB-468 MoHCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW[xNEDPxE1? NVL2OI9nTE2VTx?= MVfJR|UxRTN{MEigcm0> Ml\ONVg{QDF2NES=
SkBr3 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVSxNEDPxE1? MYjEUXNQ NGjjZY5KSzVyPkGwMFAxOCCwTR?= NUDPR3NsOTh|OEG0OFQ>
MDA-MB-231 NVTGeWg3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUSxNEDPxE1? NYTGW3V3TE2VTx?= NHPlcoVKSzVyPkGwMFAxOCCwTR?= NXzWXIhPOTh|OEG0OFQ>
HCT116 NYDWSFlnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFHacGEyOCEQvF2= MmnaSG1UVw>? NVzRNYU2UUN3ME21PFM3KG6P M2HublE5OzhzNES0
HT29 NVfMPYZST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWfoNng6OTBizszN NELIZopFVVOR NWXSbpE2UUN3ME6xNEwxODBibl2= M3f0[|E5OzhzNES0
HFF M4PUVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MorLNVAh|ryP NUOwPIRrTE2VTx?= NWG3TGVYUUN3ME23OlE2KG6P MYmxPFM5OTR2NB?=
HN5 Mn;NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4fxSlExKM7:TR?= NWHUTVBoTE2VTx?= MofXTWM2OD5zMDywNFAhdk1? MoXPNVg{QDF2NES=
786-0 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3rsWVExKM7:TR?= NXH1PWFwTE2VTx?= NE\QTIZKSzVyPUSwNFkhdk1? NXXoW4RkOTh|OEG0OFQ>
H157 M1\4dWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX:xNEDPxE1? NHTveXhFVVOR MlWyTWM2OD1{NkSyJI5O NVHzR4s5OTh|OEG0OFQ>
NCI-H460 MmniS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmnoNVAh|ryP NX\ndVZ3TE2VTx?= MWjJR|UxRjJuNUCwJI5O M162PVE5OzhzNES0
SKOV-3 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4SwO|ExKM7:TR?= NGjT[mlFVVOR MYTJR|UxRTJzMk[gcm0> NGXPNIsyQDN6MUS0OC=>
OVCAR-3 M17w[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFrodIcyOCEQvF2= M2LWNWROW09? MVLJR|UxRTJ7MUigcm0> M1rpNlE5OzhzNES0
BXPC3 NYm5e5RYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUGxNEDPxE1? MnzFSG1UVw>? MVPJR|UxRTNzNEGgcm0> M1HWSVE5OzhzNES0
MiaPaCa MlywS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn;MNVAh|ryP MWTEUXNQ MVjJR|UxRTV2M{Ogcm0> Mlf3NVg{QDF2NES=
PANC-1 M{\VOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoXmNVAh|ryP M1vZNWROW09? MXvJR|UxRTh4OEGgcm0> MVWxPFM5OTR2NB?=
LNCaP M2rI[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHT5cVkyOCEQvF2= NGHR[ppFVVOR MYjJR|UxRTF2NzDuUS=> MX2xPFM5OTR2NB?=
DU145 NUPvRZFLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkjTNVAh|ryP Ml;nSG1UVw>? NF\WNWdKSzVyPUO4NVIhdk1? NViwNpVROTh|OEG0OFQ>
PC3 M1Ppd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYjEVZQ{OTBizszN MkC5SG1UVw>? MknCTWM2OD5zMDywNFAhdk1? NGHaXJQyQDN6MUS0OC=>
BT474 MYXLbY5ie2ViYYPzZZk> NEDjUFIyOCEQvF2= NH3iUFBFVVOR NEL2PHVqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNkCgcm0> Mn7CNVg{QDF2NES=
786-0 M3HYcmtqdmG|ZTDhd5NigQ>? MkPFNVAh|ryP NH[0U4dFVVOR M{H3colvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> M3z3PVE5OzhzNES0
LNCaP M2f4PGtqdmG|ZTDhd5NigQ>? NVjDcWdIOTBizszN NYHuXGJyTE2VTx?= MUDpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1OyCwTR?= MWGxPFM5OTR2NB?=
PC3 MlTET4lv[XOnIHHzd4F6 MkH5NVAh|ryP MlPvSG1UVw>? NVfU[|ZZcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEmgcm0> MmD6NVg{QDF2NES=
KARPAS-231 Mlr5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlTCNVAh|ryP MVvEUXNQ NHWwbmlGSzVyPUSxJI5O NWHyTVVOOTlyNkS3N|A>
CCRFSB MkTWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVO3TG15OTBizszN MknHSG1UVw>? M3LXe2VEPTB;MUW1JI5O NFrNfY0yQTB4NEezNC=>
SUP B15 NHfuXo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXixNEDPxE1? M4D0fWROW09? NIDQUmtGSzVyPUG5O{BvVQ>? MV[xPVA3PDd|MB?=
SD-1 M4PaOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mkf5NVAh|ryP M2PhZ2ROW09? Ml;DSWM2OD1|MkCgcm0> NGCxUpUyQTB4NEezNC=>
RS4;11 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXv6coQ{OTBizszN NVT3fWxCTE2VTx?= NYHPU2c5TUN3ME22OVQhdk1? Mnr0NVkxPjR5M{C=
MN-60 M3Pte2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUPwcoFQOTBizszN NVTRW3pRTE2VTx?= NFWxT2xGSzVyPUO2NFIhdk1? MnH0NVkxPjR5M{C=
Tanoue M2rvbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVmxNEDPxE1? M1PjOWROW09? NHu0OZpGSzVyPUS1NVchdk1? NHHUOZoyQTB4NEezNC=>
RCH-ACV M{j3emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXmxNEDPxE1? MYrEUXNQ M2DpbmVEPTB;MUWyJI5O NE\sXYgyQTB4NEezNC=>
SEM MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWPRPZpyOTBizszN NGrnSVhFVVOR NIPZeoNGSzVyPUKwNkBvVQ>? MnXSNVkxPjR5M{C=
KASUMI-2 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mo\HNVAh|ryP MY\EUXNQ NVy3SGhRTUN3ME2yNlUhdk1? NXj0[ZlpOTlyNkS3N|A>
REH MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUXyUXdOOTBizszN MWTEUXNQ MXTFR|UxRTJ6ODDuUS=> MkLENVkxPjR5M{C=
697 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3fl[FExKM7:TR?= Ml;XSG1UVw>? MV3FR|UxRTN|ODDuUS=> MlPPNVkxPjR5M{C=
NALM-6 M4faT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYjYWW5vOTBizszN NVPDcFhTTE2VTx?= MWnFR|UxRTR{MTDuUS=> NXfBeGRWOTlyNkS3N|A>
MHH-CALL–3 M4TLb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHXVWlEyOCEQvF2= NUXYTFdKTE2VTx?= MYjFR|UxRThzMjDuUS=> NHPLbIcyQTB4NEezNC=>
MHH-CALL–2 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoLPNVAh|ryP NHvX[WhFVVOR MoDpSWM2OD1{MUG0JI5O MmL5NVkxPjR5M{C=
J.GAMMA-1 NGjqPFZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF;VRZEyOCEQvF2= MWnEUXNQ NIfQUWhGSzVyPU[1JI5O NUftcZhJOTlyNkS3N|A>
JR45.01 Ml\MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4j0fFExKM7:TR?= NYP0e2g4TE2VTx?= M2X2dGVEPTB;Nkigcm0> NID0[|IyQTB4NEezNC=>
A3 NEHiXJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWjifVFFOTBizszN MVPEUXNQ NYq5b|NDTUN3ME22PUBvVQ>? MUSxPVA3PDd|MB?=
I 2.1 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NETve5oyOCEQvF2= MmDBSG1UVw>? NYfST3Z7TUN3ME23N{BvVQ>? MVWxPVA3PDd|MB?=
MOLT-3 M1zXXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV2xNEDPxE1? MoTvSG1UVw>? NIfsXodGSzVyPUe0JI5O M3HsOlE6ODZ2N{Ow
P116 NEPuXlRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWOxNEDPxE1? NHXNSldFVVOR NYjyVZltTUN3ME23PEBvVQ>? NYXkbodNOTlyNkS3N|A>
J.Cam1.6 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NE\FNpkyOCEQvF2= MoPpSG1UVw>? MlzSSWM2OD15OTDuUS=> M1ewXFE6ODZ2N{Ow
I 9.2 M2fINmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWGxNEDPxE1? M2\MSmROW09? MmrZSWM2OD16MDDuUS=> NEfDU5AyQTB4NEezNC=>
LOUCY NWGxfGRkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2jhc|ExKM7:TR?= NXfxSpFpTE2VTx?= MmLmSWM2OD1zMUegcm0> MVqxPVA3PDd|MB?=
J.RT3-T3.5 NGLLR21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYTidHdOOTBizszN M3LXPWROW09? MmTZSWM2OD1zMkOgcm0> NG\lSG0yQTB4NEezNC=>
800000 M1Hq[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGqxSYUyOCEQvF2= NYLXfHY2TE2VTx?= M3n0[GVEPTB;MU[zJI5O NIXVSIYyQTB4NEezNC=>
Jurkat NEezcZFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX;WZ4JzOTBizszN MUDEUXNQ NUn3R4FyTUN3ME2yNlUhdk1? Mm\GNVkxPjR5M{C=
MOLT-4 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXexNEDPxE1? NHe5O5VFVVOR NFPwU4JGSzVyPUKzNkBvVQ>? M1S3fVE6ODZ2N{Ow
Molt-16 NIDienhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV7KfZJxOTBizszN MkXRSG1UVw>? M2PVcmVEPTB;MkSxJI5O M2nCd|E6ODZ2N{Ow
CEM/C3 NVXB[YRYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWnuVmp3OTBizszN MkDySG1UVw>? NVP4b5AxTUN3ME2yOVchdk1? MXqxPVA3PDd|MB?=
CEM/C2 M1:2Rmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M16zWFExKM7:TR?= NGHXUVJFVVOR NV;VOVU{TUN3ME2yO|Ehdk1? MnXPNVkxPjR5M{C=
CCRFCEM MnH2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1vPT|ExKM7:TR?= M2rCZmROW09? MUjFR|UxRTN{NzDuUS=> MnjnNVkxPjR5M{C=
CEM/C1 NIfmZY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXjvU2R1OTBizszN M33TcWROW09? NHnUe3dGSzVyPUO4NkBvVQ>? MWWxPVA3PDd|MB?=
SUPTI[VB] NYDyNJl6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEjYSXUyOCEQvF2= MknHSG1UVw>? MWXFR|UxRTZzOTDuUS=> M2PjZlE6ODZ2N{Ow
CCRF–HSB-2 MlPxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mk[zNVAh|ryP NG\DcXpFVVOR MmXDSWM2OD1{MUG3JI5O NUTP[2pIOTlyNkS3N|A>
I 2.1 MorVRZBweHSxc3nzJIF{e2G7 NELMdI4yOCEQvF2= MUjEUXNQ MlflbY5lfWOnczDhdI9xfG:|aYO= Mne1NVkxPjR5M{C=
I 9.2 NFH2SGxCeG:ydH;zbZMh[XO|YYm= MVqxNEDPxE1? NFfORZBFVVOR NVPRZZl[cW6mdXPld{BieG:ydH;zbZM> MlPiNVkxPjR5M{C=
A3 MWrBdI9xfG:|aYOgZZN{[Xl? M{\pPFExKM7:TR?= MVPEUXNQ NFrXUnZqdmS3Y3XzJIFxd3C2b4Ppdy=> M2LsO|E6ODZ2N{Ow
RD NXnLeWNVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXOxNEDPxE1? MVXJR|UxRjFyIN88US=> NWX3WoVNOjB5NEC2NlM>
Rh41 MkXzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYSxVJlkOTBizszN NHPub2RKSzVyPUOzMlghdk1? NETQW4gzODd2ME[yNy=>
Rh18 M3vGZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXyxNEDPxE1? M1OxRWlEPTB;M{CzJI5O NIH2NnkzODd2ME[yNy=>
Rh30 MkOwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXuxNEDPxE1? MkO3TWM2OD12LkixJO69VQ>? M4DIWlIxPzRyNkKz
BT-12 M4TmUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGm4eJoyOCEQvF2= Mor6TWM2OD5zMDFOwG0> MnLaNlA4PDB4MkO=
CHLA-266 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUf0VZdSOTBizszN M1vITmlEPTB;MT6yNkDPxE1? NXvEWJF4OjB5NEC2NlM>
TC-71 MoLzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV65dm86OTBizszN Mof3TWM2OD1{LkWyJO69VQ>? MVqyNFc1ODZ{Mx?=
CHLA-9 NWTDbnljT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmPKNVAh|ryP NF7mVpRKSzVyPUW5NUBvVQ>? NFjvboIzODd2ME[yNy=>
CHLA-10 MoTZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYOxNEDPxE1? M{i1PGlEPTB;MUCyJI5O MlHxNlA4PDB4MkO=
CHLA-258 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1vXSVExKM7:TR?= NXHEeIpWUUN3ME2xMlA2KM7:TR?= NWTQTWkxOjB5NEC2NlM>
GBM2 NHuweIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV:xNEDPxE1? NFLaN29KSzVyPUmuNVUh|ryP MlfLNlA4PDB4MkO=
NB-1643 NEDOfmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVPaVotPOTBizszN MkPSTWM2OD13LkSg{txO MnPMNlA4PDB4MkO=
NB-Ebc1 Ml;MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLEW3d5OTBizszN MYDJR|UxRjFyIN88US=> NX7XNpZmOjB5NEC2NlM>
CHLA-90 NVzHdlI2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIKxTW4yOCEQvF2= NYfoOolYUUN3ME6xNEDPxE1? M4nSe|IxPzRyNkKz
CHLA-136 NEDuTJdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXixNEDPxE1? MX\JR|UxRjFyIN88US=> NHXxSFMzODd2ME[yNy=>
NALM-6 NWPUU4l1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkPsNVAh|ryP Mkf5TWM2OD1{NkWgcm0> M4fLWlIxPzRyNkKz
COG-LL-317 NUm3SHNmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3yzWlExKM7:TR?= NF\oN49KSzVyPU[uOFkhdk1? NXXQNXhEOjB5NEC2NlM>
RS4;11 NIn1NVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4XBXVExKM7:TR?= M1PUeGlEPTB;MUS3JI5O MkXnNlA4PDB4MkO=
MOLT-4 NFPnfIhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXOxNEDPxE1? NHXjT|NKSzVyPUSwJI5O MWiyNFc1ODZ{Mx?=
CCRF-CEM Ml\kS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYCxNEDPxE1? MlPRTWM2OD1{Nkigcm0> NGXnbGkzODd2ME[yNy=>
Kasumi-1 NUfhUWJMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUnudmFXOTBizszN MVvJR|UxRTFyNzDuUS=> MmTQNlA4PDB4MkO=
Karpas-299 M3izTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX2xNEDPxE1? NVXENYFTUUN3ME2yMlk{KM7:TR?= MXyyNFc1ODZ{Mx?=
Ramos-RA1 NInYdHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn\iNVAh|ryP NFLZbY5KSzVyPUeuN|Uh|ryP MV2yNFc1ODZ{Mx?=
H1299 MVrLbY5ie2ViYYPzZZk> NFz4RpIyOCEQvF2= M4PnRYlvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> MUCyNVkxQDZzNh?=

... Click to View More Cell Line Experimental Data

In vivo試験 All three xenograft models treated with ARQ-197 display reductions in tumor growth: 66% in the HT29 model, 45% in the MKN-45 model, and 79% in the MDA-MB-231 model. In these xenograft studies, no significant body weight changes following oral administration of ARQ-197 at 200 mg/kg are observed. Pharmacodynamically, the phosphorylation of c-Met in human colon xenograft tumors (HT29) is strongly inhibited by ARQ-197, as assessed by a dramatic reduction of c-Met autophosphorylation 24 hours after a single oral dose of 200 mg/kg of ARQ-197. This same dosage in mice exhibits that tumor xenografts are exposed to sustained plasma levels of ARQ-197, consistent with the observed pharmacodynamic inhibition of c-Met phosphorylation and inhibition of proliferation of c-Met harboring cancer cell lines. Plasma levels of ARQ-197 10 hours after dosing are determined to be 1.3 μM, more than 3-fold above the biochemical inhibitory constant of ARQ-197 for c-Met. Therefore, ARQ-197 is able to suppress its target in vivo in the xenografted human tumor tissue. In conclusion, ARQ-197 inhibits the growth of c-Met-dependent xenografted human tumors.[1]
臨床試験 ARQ 197 plus erlotinib is currently in Phase III study in subjects with locally advanced or metastatic non-squamous, non-small cell lung cancer who have received 1 or 2 prior systemic anti-cancer therapies.
特集 The first selective c-Met inhibitor to be advanced into human clinical trials.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

c-Met SDS-PAGE in vitro kinase assay Recombinant c-Met protein (100 ng) is preincubated with increasing concentrations of ARQ-197 for 30 minutes at room temperature. Following preincubation, 100 μM of poly-Glu-Tyr substrate and various concentrations of ATP containing 5 μCi of [γ-32P]ATP are added to the reaction mixture. The reaction is incubated for 5 minutes at room temperature and then stopped by the addition of 5 μL of SDS-polyacrylamide gel, reducing sample buffer. The samples are then loaded onto a 7.5% acrylamide gel and SDS-PAGE is performed. The phosphorylated poly-Glu-Tyr substrates are ultimately visualized by autoradiography. c-Met activity is quantified by densitometry.

細胞アッセイ: [1]

細胞株 T29, MKN-45 and MDA-MB-231 cells
濃度 0.03-10 μM
反応時間 24, 32, and 48 hours
実験の流れ HT29, MKN-45, and MDA-MB-231 cells are seeded in black 96-well plates at 5 × 103 cells per well overnight in a medium with 10% FBS. The next day, cells are treated with increasing concentrations of ARQ-197 (0.03-10 μM) for 24, 32, and 48 hours at 37 °C. After ARQ-197 treatment, the drug-containing medium is removed and cells are incubated for at least 10 minutes in a labeling solution (10 mM HEPES, 140 mM NaCl, and 6 mM CaCl2) containing 2 μg/mL Hoescht 33342 (blue channel), 500-times diluted Annexin V-FITC (green channel), and 1 μg/mL propidium iodide (red channel). High-content image acquisition and analysis are carried out. The program is set to take four images per well. The exposure time is set at 16.7 ms/10% gain, 500 ms/35% gain, and 300 ms/30% gain for the 4,6-diamidino-2-phenylindole, FITC, and rhodamine channels, respectively. Images are processed and the numbers of positive cells for each channel and each condition are determined. In addition, HT29 cells are treated with increasing concentrations of ARQ-197 for 32 hours in the absence or the presence of 25, 50, and 100 μM ZvAD-FMK (irreversible general caspase inhibitor), and the same procedures are undertaken. All experiments are done in triplicate. To determine whether the apoptotic effect is due to c-Met inhibition, the effect of ARQ-197 when glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and c-Met are knocked down using siRNA is investigated. HT29, MKN-45, and MDA-MB-231 cells are transfected with a nontargeted control siRNA, a gapgh-targeted control siRNA, or a met-targeted siRNA. After 3 days, c-Met, GAPDH, and β-actin expression levels are determined using specific antibodies. To determine if the effect is caspase dependent, HT29, MKN-45, and MDA-MB-231 cells are transfected with a met-targeted siRNA for 2 days and incubated in the absence or the presence of increasing concentrations of ZvAD-FMK for 1 additional day. A nontargeted siRNA and a gapgh-targeted siRNA (siRNA GAPDH) are also transfected in parallel, as controls. Cells are then stained with Annexin V-FITC and propidium iodide, and the percentage of apoptotic cells is determined.

動物実験: [1]

動物モデル Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
製剤 In polyethylene glycol 400/20% Vitamin E tocopheryl polyethylene glycol succinate (60:40) 30 mg/mL
投薬量 200 mg/kg
投与方法 Orally administered

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Tivantinib (ARQ 197) SDF
分子量 369.42
化学式

C23H19N3O2

CAS No. 905854-02-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 73 mg/mL (197.6 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 (3R,4R)-3-(2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione

文献中の引用 (4)

Frequently Asked Questions

  • Question 1
    Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

    Answer: S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related c-Met 阻害剤

  • NPS-1034

    NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324)

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.

  • Crizotinib (PF-02341066)

    Crizotinib (PF-02341066) は1種の有効な小分子の卵白の阻害剤の再編人プロテインキナーゼ、 Kiが 4 nM。

  • Foretinib (GSK1363089)

    Foretinib (GSK1363089)は、目標が会ったATP競争的活性部位阻害剤とKDRで、IC50がそれぞれ0.4 nM と 0.9 nMです。

  • Capmatinib (INCB28060)

    Capmatinib (INCB28060)は、IC50が0.13nMによりあるc-METキナーゼの新しい、ATP競争的阻害剤です。

    Features:Inactive against RONβ, another member of the c-MET RTK family, as well as EGFR and HER-3 (members of the EGFR RTK family).

  • PHA-665752

    PHA-665752は、9nMのIC50による強力で、選択的で、ATP競争的c-Met阻害剤です。

  • BMS-777607

    BMS777607は分子が小さいMet関連キナーゼ阻害剤、c-Met, Axl, Ron 、Tyro3に作用する時、IC50がそれぞれ3.9nM、1.1nM、1.8nMと4.3nMになる。

    Features:A potent inhibitor of the Met family, and >40-fold selectivity vs. Lck, VEGFR2, and TrkA/B and >500-fold selective vs. other receptor and non-receptor kinases.

最近チェックしたアイテム

Tags: Tivantinib (ARQ 197)を買う | Tivantinib (ARQ 197)供給者 | Tivantinib (ARQ 197)を購入する | Tivantinib (ARQ 197)費用 | Tivantinib (ARQ 197)生産者 | オーダーTivantinib (ARQ 197) | Tivantinib (ARQ 197)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ