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 MkXzT4lv[XOnIHHzd4F6 NU\UcW1MhjFyIN88US=> NYXkTWJPcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NVzzfXE5OjB2OESwNVg>
HT29 M1vkU2tqdmG|ZTDhd5NigQ>? M4POdJ4yOCEQvF2= M1fufolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= M3z3TVIxPDh2MEG4
MDA-MB-231 MlroT4lv[XOnIHHzd4F6 MX;+NVAh|ryP NEfRU|lqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NVf3[IduOjB2OESwNVg>
NCI-H441 MUjLbY5ie2ViYYPzZZk> NFLseYx,OTBizszN MYrpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MnKxNlA1QDRyMUi=
SK-MEL-28 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml;XN|Mh|ryP NXKzcWZLUUN3ME6zN{DPxE1? MYeyNFQ5PDBzOB?=
NCI-H661 MlntS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWCzN{DPxE1? M4[5bGlEPTB-M{Og{txO M1LwWFIxPDh2MEG4
NCI-H446 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXizN{DPxE1? NHuyU5hKSzVyPUeg{txO M336S|IxPDh2MEG4
MDA-MB-231 Ml\kS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoDHN|Mh|ryP MV;JR|UxRTBwNUWg{txO NHvsT4IzODR6NECxPC=>
DLD-1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkjtN|Mh|ryP MXLJR|UxRTBwNUOg{txO MY[yNFQ5PDBzOB?=
A549 Mn;lS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;6OlU{OyEQvF2= MUnJR|UxRTBwNUmg{txO M2L4ZVIxPDh2MEG4
SK-OV-3 NIrIZlZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXGzN{DPxE1? M2PDdmlEPTB;MD62OkDPxE1? NWq2dmdOOjB2OESwNVg>
NCI-H460 NHn3NGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVOzN{DPxE1? M{TjcWlEPTB;MD62JO69VQ>? MV:yNFQ5PDBzOB?=
A375 NV25VVA4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmjuN|Mh|ryP M1vCT2lEPTB;MD60NkDPxE1? M13ZeVIxPDh2MEG4
NCI-H441 NX:3NnV{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkPzN|Mh|ryP NYLDcIhpUUN3ME2wMlMh|ryP NYTWSpFIOjB2OESwNVg>
HT29 M4C4TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFTyNYo{OyEQvF2= NETnOZVKSzVyPUCuOFkh|ryP MWiyNFQ5PDBzOB?=
MKN-45 Mm\0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV\iTlBROzNizszN NInQW3ZKSzVyPUCuOVgh|ryP M4i2OVIxPDh2MEG4
HT29 NVK0OWdwSXCxcITvd4l{KGG|c3H5 NFe3Oo9,OTBizszN Ml\id4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw M4DNPVIxPDh2MEG4
MKN-45 MkmzRZBweHSxc3nzJIF{e2G7 MXf+NVAh|ryP MonRd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw M1HyfVIxPDh2MEG4
MDA-MB-231 MXXBdI9xfG:|aYOgZZN{[Xl? NHTNe5F,OTBizszN NF3qc3lud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu MYSyNFQ5PDBzOB?=
MDA-MB-231/TGL MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWrTSYE5hjFyMDFOwG0> NEDaNWVIUTVyPUGuNkDPxE1? M{TMb|IzODJ5Nkmw
1833/TGL MnryS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXvglExOCEQvF2= MmfuS2k2OD1|Lkeg{txO NHHRO|kzOjB{N{[5NC=>
EBC1 MlHIR5l1d3SxeHnjxsBie3OjeR?= M3zDPJ4yOCEQvF2= M3PXS4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= MorLNlM2QTh{N{[=
SNU638 MoTmR5l1d3SxeHnjxsBie3OjeR?= NYrnUmRIhjFyIN88US=> NXLZTW44cW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> NYTuZVhwOjN3OUiyO|Y>
A549 MV\DfZRwfG:6aXRCpIF{e2G7 NYPrZ3JzhjFyIN88US=> NG\C[GNvd3RiYX\m[YN1 Mmq5NlM2QTh{N{[=
H460 Mn\ER5l1d3SxeHnjxsBie3OjeR?= MYH+NVAh|ryP NXnPd4FJdm:2IHHm[oVkfA>? MYGyN|U6QDJ5Nh?=
HCC827 NHnGZZlEgXSxdH;4bYPDqGG|c3H5 NUX3dGE4hjFyIN88US=> MX\uc5Qh[W[oZXP0 M3LDcFI{PTl6Mke2
A549 MX\GeY5kfGmxbjDhd5NigQ>? NHLZUpIyOCEQvF2= M4r4foRqe3K3cITzJI1q[3KxdIXieYxm M1ToWVI{PTl6Mke2
EBC1 MlfwSpVv[3Srb36gZZN{[Xl? NWTlfHJUOTBizszN M2nPboRqe3K3cITzJI1q[3KxdIXieYxm M1XXV|I{PTl6Mke2
H460 MVXGeY5kfGmxbjDhd5NigQ>? MXOxNEDPxE1? M4nyeolvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? NVztc|cxOjV|MUOwNVA>
K562/VCR Mmq4R5l1d3SxeHnjxsBie3OjeR?= MX\+NVAh|ryP NHvsTo9{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= MoX6NlU{OTNyMUC=
CEM/VBL NV\UU2FDS3m2b4TvfIlkyqCjc4PhfS=> MU\+NVAh|ryP NWHKRVg6e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 M4LheVI2OzF|MEGw
U266 NX\IWpRjS3m2b4TvfIlkyqCjc4PhfS=> MWj+N{DPxE4EoB?= NY[2NZRUUUN3ME2xMlEh|ryP MkDrNlU5OTByMUO=
OPM-2 NXKzeZVKS3m2b4TvfIlkyqCjc4PhfS=> MYH+N{DPxE4EoB?= M2HFbWlEPTB;MT64JO69VQ>? NX3aXm1wOjV6MUCwNVM>
MM.1S M4LzXGN6fG:2b4jpZ:Kh[XO|YYm= NGX2S5d,OyEQvF5CpC=> NV\sPFZNUUN3ME2xMlYh|ryP NXrpfnd4OjV6MUCwNVM>
MM.1R Ml22S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVqzJO69VcLi M2S0folvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> NY\VS3hqOjV6MUCwNVM>
RPMI-8226 NGDEWoFEgXSxdH;4bYPDqGG|c3H5 M3Lwd54{KM7:TdMg NX;MOpFoUUN3ME2wMlkh|ryP MW[yOVgyODBzMx?=
ANBL-6 MkXsR5l1d3SxeHnjxsBie3OjeR?= Mm\HNUDPxE4EoB?= M3HFN4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MX2yOVgyODBzMx?=
ANLB-6/V10R MnrLR5l1d3SxeHnjxsBie3OjeR?= M4fjeVEh|ryPwrC= M1\jVolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NGfL[|kzPThzMECxNy=>
KAS-6/1 MX\DfZRwfG:6aXRCpIF{e2G7 NV:0e3NTOSEQvF5CpC=> NIXGR2tqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M4\2clI2QDFyMEGz
KAS-6/V10R M3HmUWN6fG:2b4jpZ:Kh[XO|YYm= MXGxJO69VcLi NEm2[|RqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M1rFWlI2QDFyMEGz
KAS-6/R10R MV3DfZRwfG:6aXRCpIF{e2G7 MkPvNUDPxE4EoB?= NYDsTo0xcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MWmyOVgyODBzMx?=
8226/S MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkexN{DPxE4EoB?= NWjpWHdqcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm Mlq3NlU5OTByMUO=
8226/LR-5 NEfqempIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWmzJO69VcLi NVPESYhwcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm M2LvcVI2QDFyMEGz
Huh7 MkHMR5l1d3SxeHnjxsBie3OjeR?= M3H6T541NjhizszNxsA> NFjydGdFVVOR NFjhPFVKSzVyPUmuPUBvVQ>? MnfENlYzPTl{NUC=
Hep3B MkTDR5l1d3SxeHnjxsBie3OjeR?= Mn;4glQvQCEQvF5CpC=> MXrEUXNQ NFq1RlRKSzVyPUS0PE44KG6P MVKyOlI2QTJ3MB?=
HepG2 NIfKTFBEgXSxdH;4bYPDqGG|c3H5 NH;tb2p,PC56IN88UeKh Mn\mSG1UVw>? M1rTSWlEPTB;MUO5Mlc4KG6P NF\ldm8zPjJ3OUK1NC=>
Chang M{DNSWN6fG:2b4jpZ:Kh[XO|YYm= Mm\zglQvQCEQvF5CpC=> MWXEUXNQ MlPkTWM2OD12NEiuO{BvVQ>? MmfVNlYzPTl{NUC=
Huh7 NWfWd3dUTnWwY4Tpc44h[XO|YYm= NFO5SoYyNjZizszNxsA> MnnCSG1UVw>? Ml\pZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MV6yOlI2QTJ3MB?=
Hep3B NX;jSlBuTnWwY4Tpc44h[XO|YYm= NFTZN2EyNjZizszNxsA> M{fzRWROW09? NXzTV4tm[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= MlzLNlYzPTl{NUC=
HepG2 NF;xTlBHfW6ldHnvckBie3OjeR?= Mn\sNU43KM7:TdMg NIL5OVhFVVOR NFz3UFRk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MmHVNlYzPTl{NUC=
Chang NF7xeY1HfW6ldHnvckBie3OjeR?= MlTpNU43KM7:TdMg MUHEUXNQ MV3jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M4DJd|I3OjV7MkWw
MHCC97L NEGwc3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHrDU45,OTBizszN MV;EUXNQ Ml7ZTWM2OD1|MUWgcm0> M3XXOFI3PDV6OUWz
MHCC97H MofXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml3rglExKM7:TR?= M1G4PGROW09? NHmyTphKSzVyPUO2PQKBkSCwTR?= NWrBXJU2OjZ2NUi5OVM>
Huh7 NFXifpFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3K5Rp4yOCEQvF2= M2HYcWROW09? MUjJR|UxRTJ4NTDuUS=> M{L5TlI3PDV6OUWz
HepG2 NF\GWWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXvDbWRQhjFyIN88US=> M3ntbmROW09? NXnVSGtEUUN3ME2zPVIhdk1? NXfKSFhLOjZ2NUi5OVM>
MHCC97L M360PWZ2dmO2aX;uJIF{e2G7 MXKxJO69VcLi MlnGSG1UVw>? NVLRSZBzcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? MkPTNlY1PTh7NUO=
Huh7 MoTCSpVv[3Srb36gZZN{[Xl? NITzcJgyKM7:TdMg Mlf2SG1UVw>? MoTubY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NGT6XWgzPjR3OEm1Ny=>
MHCC97L NXvhN4lUSXCxcITvd4l{KGG|c3H5 M2HNNVEh|ryPwrC= M3rwdmROW09? NW[wbFUzcW6mdXPld{BieG:ydH;zbZM> Mmm4NlY1PTh7NUO=
Huh7 NV2yTIQ1SXCxcITvd4l{KGG|c3H5 MVGxJO69VcLi Ml;2SG1UVw>? NUjybo1vcW6mdXPld{BieG:ydH;zbZM> MmH6NlY1PTh7NUO=
C3H 10T1/2 mouse fibroblasts NWTVXXBrU2mwYYPlJIF{e2G7 MVmyOUDPxE1? MmfZSG1UVw>? MVfy[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg MU[yNFU{PDN2NR?=
H23 M4rCR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3E[HNVOjVizszN MVjEUXNQ MVTzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MWKyNFU{PDN2NR?=
WM35 NE\QZZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlWyNVAh|ryP M{j2eWROW09? M{PmPZNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NV3o[I82OjB3M{SzOFU>
NIH 3T3 M4PKOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGP6c4syOCEQvF2= MX;EUXNQ NUHjfIti\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 M1zabVIxPTN2M{S1
H838 NGXTXnhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoTXNVAh|ryP M1T2O2ROW09? MWHkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= MYGyNFU{PDN2NR?=
H1395 MoXnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M37uNFExKM7:TR?= NFLO[pRFVVOR NY[zW2xy\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 Mn\pNlA2OzR|NEW=
Quiescent S2 NEH3SJRMcW6jc3WgZZN{[Xl? M3O1SlMxKM7:TR?= M2CyTWROW09? MVnjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? M4\melIyPTF6OUG1
PC3 MVrBdI9xfG:|aYOgZZN{[Xl? M3HOUlIxKM7:TR?= MWLEUXNQ MX3pcoR2[2W|IHHwc5B1d3Orcx?= NFjwRZozOTdyOUGzNC=>
Du145 MnPpRZBweHSxc3nzJIF{e2G7 NFXSWFIzOCEQvF2= MnTESG1UVw>? M{\mZYlv\HWlZYOgZZBweHSxc3nz MX:yNVcxQTF|MB?=
LNCaP MmHJRZBweHSxc3nzJIF{e2G7 M3v0VFIxKM7:TR?= NUTQSWpzTE2VTx?= NIrHfmFqdmS3Y3XzJIFxd3C2b4Ppdy=> M130clIyPzB7MUOw
LAPC-4 NXfM[oFRSXCxcITvd4l{KGG|c3H5 NVPQSnRrOjBizszN NUWwTHg5TE2VTx?= NVfnW2tWcW6mdXPld{BieG:ydH;zbZM> MkL5NlE4ODlzM{C=
LNCaP NXLOOnV[TnWwY4Tpc44h[XO|YYm= M4\rXFIxKM7:TR?= MnTISG1UVw>? M162RoRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NYjR[HJUOjF5MEmxN|A>
LAPC-4 NHjOXnhHfW6ldHnvckBie3OjeR?= M2TjOFIxKM7:TR?= NYfocXlvTE2VTx?= NXHadolR\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= Mn3PNlE4ODlzM{C=
Kasumi-1 NVu0VY0{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXfwdFhXhjVyIN88US=> MlnKSG1UVw>? MlrHbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NUPVN|hOOjN|OUC1N|Y>
SKNO-1 M2Lub2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVX+OVAh|ryP NYmwfFQ{TE2VTx?= Mlf5bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MVeyN|M6ODV|Nh?=
Kasumi-1 M1y4ZmtqdmG|ZTDhd5NigQ>? NYD6Wnp7hjFyIN88US=> NISybGtFVVOR MXfy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= MlraNlM{QTB3M{[=
SKNO-1 MYTLbY5ie2ViYYPzZZk> NUf2bGRrhjFyIN88US=> M3H4UGROW09? MmLVdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y M3e4e|I{OzlyNUO2
A549 MV\GeY5kfGmxbjDhd5NigQ>? NFzwbVIyOCEQvF2= MV7EUXNQ Mkf3[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> Mm\TNlQ4PDZ3N{S=
NRK-52E M3L2VWZ2dmO2aX;uJIF{e2G7 MYexNEDPxE1? MYXEUXNQ M1\DcIlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv NHPuc5AzPTB6OECwNi=>
PC12 MlHuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlWxglEzNjVizszN NYrFfpRxTE2VTx?= MkXJdJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> NUG2c|VpOjVzMkizPFY>
HPMCs NInkXIZHfW6ldHnvckBie3OjeR?= MXzy[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> MXGyOlA1PTd6MB?=
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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 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

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Source , , PLoS One, 2014, 9(9): e105919. Tivantinib (ARQ 197) purchased from Selleck
Method Western Blot
Cell Lines H513 cells
Concentrations 0-0.5 μM
Incubation Time 48 h
Results The levels of cyclin D1, which is a G0/G1 cell cycle regulator were decreased in cells treated with ARQ 197, GDC-0980 or NVP-BEZ235, in a dose dependent manner. In the case of NVP-BEZ235 the effect was much more pronounced in H513 cells. The combinatorial treatment of ARQ 197/GDC-0980 and ARQ 197/NVP-BEZ235 however induced significant levels of cleaved PARP in both MPM cell lines. Individual treatment with GDC-0980 or NVP-BEZ235 had little effect as evidenced from cleaved PARP levels.

文献中の引用 (4)

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