Tivantinib (ARQ 197) 化学構造
分子量: 369.42

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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 MkjKT4lv[XOnIHHzd4F6 NXLDUXEzhjFyIN88US=> NETnZ29qdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MVuyNFQ5PDBzOB?=
HT29 MYrLbY5ie2ViYYPzZZk> MlPOglExKM7:TR?= MVTpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NInK[ZUzODR6NECxPC=>
MDA-MB-231 Mnz4T4lv[XOnIHHzd4F6 NIfsVVV,OTBizszN M4rBWolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MWqyNFQ5PDBzOB?=
NCI-H441 MkTUT4lv[XOnIHHzd4F6 NYjye3NXhjFyIN88US=> MnnJbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MUiyNFQ5PDBzOB?=
SK-MEL-28 NGX0NZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYnGeIpOOzNizszN MmfsTWM2OD5|MzFOwG0> MmXnNlA1QDRyMUi=
NCI-H661 NH7BVHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGnw[Fc{OyEQvF2= MVHJR|UxRjN|IN88US=> NHTzN2wzODR6NECxPC=>
NCI-H446 NIfIUJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1[4NFM{KM7:TR?= NFTFPXVKSzVyPUeg{txO MkLkNlA1QDRyMUi=
MDA-MB-231 NVPoe5h2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFHFcZo{OyEQvF2= M3Xz[mlEPTB;MD61OUDPxE1? NXHoSlNOOjB2OESwNVg>
DLD-1 NEnFZm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHTJ[3A{OyEQvF2= MoDmTWM2OD1yLkWzJO69VQ>? NYfOZY41OjB2OESwNVg>
A549 MkmwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXj3eIZLOzNizszN M4rKbWlEPTB;MD61PUDPxE1? NHHZdYEzODR6NECxPC=>
SK-OV-3 NUew[YROT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1jtTFM{KM7:TR?= MVfJR|UxRTBwNk[g{txO NH3mbZYzODR6NECxPC=>
NCI-H460 NXTCW5I6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYSzN{DPxE1? M{X4WmlEPTB;MD62JO69VQ>? MXuyNFQ5PDBzOB?=
A375 NH;kZW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFrLfIs{OyEQvF2= NV[yNoc1UUN3ME2wMlQzKM7:TR?= MmPhNlA1QDRyMUi=
NCI-H441 Mni5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVizN{DPxE1? NHfPbZpKSzVyPUCuN{DPxE1? NFHGU2kzODR6NECxPC=>
HT29 Mn;HS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn:wN|Mh|ryP M2TkS2lEPTB;MD60PUDPxE1? M3z3NlIxPDh2MEG4
MKN-45 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MljyN|Mh|ryP MmKzTWM2OD1yLkW4JO69VQ>? MlfGNlA1QDRyMUi=
HT29 MojqRZBweHSxc3nzJIF{e2G7 NIjWOHJ,OTBizszN NULWXpNCe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu MmLpNlA1QDRyMUi=
MKN-45 NG\kRWlCeG:ydH;zbZMh[XO|YYm= NYLHOZVnhjFyIN88US=> M33ad5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MkPHNlA1QDRyMUi=
MDA-MB-231 M1fpdWFxd3C2b4Ppd{Bie3OjeR?= MVn+NVAh|ryP Mn3qcY9l\XO2bImgbY5lfWOnczDhdI9xfG:|aYOgZpkhOzVnLh?= Mn\XNlA1QDRyMUi=
MDA-MB-231/TGL MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1zRcJ4yODBizszN NXXlUYp6T0l3ME2xMlIh|ryP Mo\UNlIxOjd4OUC=
1833/TGL MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIPX[oF,OTByIN88US=> NGnCbGFIUTVyPUOuO{DPxE1? Mly4NlIxOjd4OUC=
EBC1 M3\nUGN6fG:2b4jpZ:Kh[XO|YYm= Ml72glExKM7:TR?= MVHpcohq[mm2czD0bIUh[2WubDDndo94fGhw NHjxeY8zOzV7OEK3Oi=>
SNU638 MWnDfZRwfG:6aXRCpIF{e2G7 M2jmVp4yOCEQvF2= M{\IcYlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= MmXoNlM2QTh{N{[=
A549 NGXtVGlEgXSxdH;4bYPDqGG|c3H5 MVX+NVAh|ryP MUTuc5Qh[W[oZXP0 MnGwNlM2QTh{N{[=
H460 M3XFdWN6fG:2b4jpZ:Kh[XO|YYm= MVP+NVAh|ryP NXrqOWV[dm:2IHHm[oVkfA>? M2e5TFI{PTl6Mke2
HCC827 MmXrR5l1d3SxeHnjxsBie3OjeR?= MoTrglExKM7:TR?= M4jFeY5wfCCjZn\lZ5Q> MYCyN|U6QDJ5Nh?=
A549 NH\JbIpHfW6ldHnvckBie3OjeR?= M{DPblExKM7:TR?= MXLkbZNzfXC2czDtbYNzd3S3YoXs[S=> MYeyN|U6QDJ5Nh?=
EBC1 MWHGeY5kfGmxbjDhd5NigQ>? M1vBblExKM7:TR?= NVWyW21o\Gm|coXweJMhdWmlcn;0eYJ2dGV? NWPMTHE{OjN3OUiyO|Y>
H460 MonDSpVv[3Srb36gZZN{[Xl? NX;Hd|ExOTBizszN NI\WSYdqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w NFnDPW0zPTNzM{CxNC=>
K562/VCR MkHMR5l1d3SxeHnjxsBie3OjeR?= NGjNPHJ,OTBizszN M1PPOZNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= MUmyOVMyOzBzMB?=
CEM/VBL NY\QVog4S3m2b4TvfIlkyqCjc4PhfS=> NGLNNVR,OTBizszN M3m0SJNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= MkHBNlU{OTNyMUC=
U266 MUXDfZRwfG:6aXRCpIF{e2G7 NGnwRWx,OyEQvF5CpC=> MYPJR|UxRTFwMTFOwG0> NYXjUnRXOjV6MUCwNVM>
OPM-2 NUWyXZNmS3m2b4TvfIlkyqCjc4PhfS=> M{G0XJ4{KM7:TdMg NEftRVZKSzVyPUGuPEDPxE1? M4\QTlI2QDFyMEGz
MM.1S NFTt[mZEgXSxdH;4bYPDqGG|c3H5 MYj+N{DPxE4EoB?= M1ruU2lEPTB;MT62JO69VQ>? M{G0WVI2QDFyMEGz
MM.1R NGO2UYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4XNOVMh|ryPwrC= M1XSeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> MlPINlU5OTByMUO=
RPMI-8226 MVzDfZRwfG:6aXRCpIF{e2G7 M3f1Sp4{KM7:TdMg NXHZN3ZPUUN3ME2wMlkh|ryP MUeyOVgyODBzMx?=
ANBL-6 NESweJBEgXSxdH;4bYPDqGG|c3H5 NXvVTndGOSEQvF5CpC=> M3rH[Ilv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MWCyOVgyODBzMx?=
ANLB-6/V10R MoPoR5l1d3SxeHnjxsBie3OjeR?= MUOxJO69VcLi NFi5TVBqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M3rTVVI2QDFyMEGz
KAS-6/1 NUTrZlEzS3m2b4TvfIlkyqCjc4PhfS=> NHzyXncyKM7:TdMg M4T5Wolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M3j5eFI2QDFyMEGz
KAS-6/V10R MWjDfZRwfG:6aXRCpIF{e2G7 MlLXNUDPxE4EoB?= NVTEWZRlcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M1G5bVI2QDFyMEGz
KAS-6/R10R MUjDfZRwfG:6aXRCpIF{e2G7 NIK3XIIyKM7:TdMg NYnie|dlcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NVXPeG1IOjV6MUCwNVM>
8226/S MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHHoco8{KM7:TdMg NUP4RXI{cW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm NGq0eHUzPThzMECxNy=>
8226/LR-5 NX7YZYRQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX:zJO69VcLi Mkn3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl M3;vb|I2QDFyMEGz
Huh7 NUjnR|UxS3m2b4TvfIlkyqCjc4PhfS=> MXL+OE45KM7:TdMg MVLEUXNQ MoT2TWM2OD17Lkmgcm0> NF;pT5kzPjJ3OUK1NC=>
Hep3B NUXtSJR6S3m2b4TvfIlkyqCjc4PhfS=> NFrRVoV,PC56IN88UeKh MmjsSG1UVw>? MojRTWM2OD12NEiuO{BvVQ>? NX7JfWxNOjZ{NUmyOVA>
HepG2 NVHlfVVDS3m2b4TvfIlkyqCjc4PhfS=> NUHkTnJNhjRwODFOwG3DqA>? MVTEUXNQ M3\EbmlEPTB;MUO5Mlc4KG6P M3;0S|I3OjV7MkWw
Chang NVq3blQ3S3m2b4TvfIlkyqCjc4PhfS=> NFLkOWN,PC56IN88UeKh M{ize2ROW09? MWnJR|UxRTR2OD63JI5O MXyyOlI2QTJ3MB?=
Huh7 NIK5[YxHfW6ldHnvckBie3OjeR?= NHLOdWwyNjZizszNxsA> M3\ObmROW09? M1i0SINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MnXQNlYzPTl{NUC=
Hep3B M{my[WZ2dmO2aX;uJIF{e2G7 MonzNU43KM7:TdMg NF65cGVFVVOR MV;jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MoDZNlYzPTl{NUC=
HepG2 NHnWOVVHfW6ldHnvckBie3OjeR?= M4i2cFEvPiEQvF5CpC=> MXPEUXNQ M3nxNINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NYTBb2FbOjZ{NUmyOVA>
Chang MWXGeY5kfGmxbjDhd5NigQ>? NITSPGkyNjZizszNxsA> MVTEUXNQ MmrDZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MVqyOlI2QTJ3MB?=
MHCC97L NHzEbpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mk\SglExKM7:TR?= MkLsSG1UVw>? MkTXTWM2OD1|MUWgcm0> MnXrNlY1PTh7NUO=
MHCC97H MlTJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHfRNXB,OTBizszN NHLnNWxFVVOR NEfUOlNKSzVyPUO2PQKBkSCwTR?= M4PiOFI3PDV6OUWz
Huh7 M2LlUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWj+NVAh|ryP MoTlSG1UVw>? MmPKTWM2OD1{NkWgcm0> NF3L[nUzPjR3OEm1Ny=>
HepG2 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH7vU2J,OTBizszN M4LsV2ROW09? NWfJbolqUUN3ME2zPVIhdk1? MXOyOlQ2QDl3Mx?=
MHCC97L NWT2R|JOTnWwY4Tpc44h[XO|YYm= M1nkZlEh|ryPwrC= MU\EUXNQ NEjSNINqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v Mlv2NlY1PTh7NUO=
Huh7 MkexSpVv[3Srb36gZZN{[Xl? NHTSOmcyKM7:TdMg MX3EUXNQ NWPPUpV2cW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? MWiyOlQ2QDl3Mx?=
MHCC97L M2DMOGFxd3C2b4Ppd{Bie3OjeR?= NFzQW4syKM7:TdMg NWTidGpzTE2VTx?= M3vyfIlv\HWlZYOgZZBweHSxc3nz MVmyOlQ2QDl3Mx?=
Huh7 M{CyUmFxd3C2b4Ppd{Bie3OjeR?= MX2xJO69VcLi NYrWcHZtTE2VTx?= NV;ue3FTcW6mdXPld{BieG:ydH;zbZM> NXraU49YOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts M3z3cWtqdmG|ZTDhd5NigQ>? NYC2THF{OjVizszN NFLTXnZFVVOR NIfTfGFz\WS3Y3XzJGhqe3SxbnWgTFMh[W6mIFi0JIFk\XS7bHH0bY9vKGyndnXsd:Kh MV2yNFU{PDN2NR?=
H23 NFy0doZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkD1NlUh|ryP NXnMeVhHTE2VTx?= M3\jepNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MmPHNlA2OzR|NEW=
WM35 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPwNVAh|ryP M3LsdmROW09? Mn7Nd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NGjF[lkzODV|NEO0OS=>
NIH 3T3 M2DKSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWSxNEDPxE1? MVvEUXNQ MV3kc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= Mn\nNlA2OzR|NEW=
H838 NWHuSVZHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX\4Vmh[OTBizszN MVLEUXNQ M1X6RoRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MkTINlA2OzR|NEW=
H1395 MnvLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH3kNpYyOCEQvF2= MX3EUXNQ NF;BeGFld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NGDNRoIzODV|NEO0OS=>
Quiescent S2 NEizeGFMcW6jc3WgZZN{[Xl? MVGzNEDPxE1? NF\ndYtFVVOR M4HuNINwdXCuZYTlcJkh[WK{b3fheIV{KFSVQT3pcoR2[2WmIHj5dIVz[WOndInsZZRqd25ib3[gTFNMPG2nMzDobZN1d26ncx?= NXPJUVI3OjF3MUi5NVU>
PC3 NEHGd3FCeG:ydH;zbZMh[XO|YYm= NUm1VlI5OjBizszN MlHBSG1UVw>? MXTpcoR2[2W|IHHwc5B1d3Orcx?= M4ezOVIyPzB7MUOw
Du145 NF;Pe29CeG:ydH;zbZMh[XO|YYm= MYiyNEDPxE1? MXjEUXNQ M{TsN4lv\HWlZYOgZZBweHSxc3nz M4fwVlIyPzB7MUOw
LNCaP MY\BdI9xfG:|aYOgZZN{[Xl? NUmzN41GOjBizszN MWXEUXNQ NX;DdpZZcW6mdXPld{BieG:ydH;zbZM> MX2yNVcxQTF|MB?=
LAPC-4 NGLF[GRCeG:ydH;zbZMh[XO|YYm= MYGyNEDPxE1? M{j2WGROW09? Mn;GbY5lfWOnczDhdI9xfG:|aYO= MV:yNVcxQTF|MB?=
LNCaP MlH4SpVv[3Srb36gZZN{[Xl? NEnF[XgzOCEQvF2= Mn7CSG1UVw>? NV\icI1l\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= NV:0b5ZGOjF5MEmxN|A>
LAPC-4 NIDyPG9HfW6ldHnvckBie3OjeR?= NWXkNFF3OjBizszN MXfEUXNQ MUHk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ MoTxNlE4ODlzM{C=
Kasumi-1 NYrOWINQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4PVSJ42OCEQvF2= NYDSW5V5TE2VTx?= NIPPXHdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NHHWWGszOzN7MEWzOi=>
SKNO-1 M{LpSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXj+OVAh|ryP Mn\USG1UVw>? NITGeZdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MkDLNlM{QTB3M{[=
Kasumi-1 MYjLbY5ie2ViYYPzZZk> M1TFN54yOCEQvF2= M2\uW2ROW09? MVfy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NIrjTGQzOzN7MEWzOi=>
SKNO-1 MXfLbY5ie2ViYYPzZZk> NVvRW4F2hjFyIN88US=> NVfSXnJiTE2VTx?= NYTN[YhlemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NFv2bFIzOzN7MEWzOi=>
A549 M{fpR2Z2dmO2aX;uJIF{e2G7 NWjnUHlPOTBizszN MVXEUXNQ MmfC[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> Ml7HNlQ4PDZ3N{S=
NRK-52E M{\WW2Z2dmO2aX;uJIF{e2G7 NHTPN2YyOCEQvF2= MU\EUXNQ M4PpdolvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv M2iwV|I2ODh6MECy
PC12 NUDFSXZxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4\kfp4yOi53IN88US=> M13BbGROW09? MnHxdJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> NXO2RZd{OjVzMkizPFY>
HPMCs M2\IV2Z2dmO2aX;uJIF{e2G7 NW\oeng6emW4ZYLz[ZMh\XCrdHjlcIlidCC2bzDt[ZNmdmOqeX3hcEB1emGwc3n0bY9vKG:oIHj1cYFvKHCncnn0c45m[WxibXXzc5Rp\WyrYXygZ4VtdHN? MnWwNlYxPDV5OEC=
A549 NW\5flNETnWwY4Tpc44h[XO|YYm= NWPwWGtjhjVyIN88US=> M{jzT2ROW09? M2GyboFn\mWldIOgeIhmKH[rcnHsJIxq\mViY4njcIUh[W6mIHjvd5QhemW|cH;ud4U> MYWyOlcyOTd2OB?=
RAW264.7 NGLMPVBHfW6ldHnvckBie3OjeR?= NYTndG1ShjNyIN88US=> NWjISHN1TE2VTx?= M1LjdpJm\HWlZYOgdJJwNWmwZnzhcY1ifG:{eTDn[Y5mKGW6cILld5Nqd25? MXKyOlcyQDV6Nh?=
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... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 73 mg/mL (197.6 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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.

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