Tivantinib (ARQ 197) 化学構造
分子量: 369.42

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製品説明

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    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 MmO3T4lv[XOnIHHzd4F6 MVT+NVAh|ryP NUm0U2tncW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MYqyNFQ5PDBzOB?=
HT29 M4LPdWtqdmG|ZTDhd5NigQ>? M4ro[Z4yOCEQvF2= M2TxOolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= Mo\tNlA1QDRyMUi=
MDA-MB-231 NW\4TIRSU2mwYYPlJIF{e2G7 NX;sSYhuhjFyIN88US=> NVjk[|NkcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MXKyNFQ5PDBzOB?=
NCI-H441 MlHuT4lv[XOnIHHzd4F6 MnzCglExKM7:TR?= Mmr1bY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NWDNUHd4OjB2OESwNVg>
SK-MEL-28 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFLRO3I{OyEQvF2= M4rUWmlEPTB-M{Og{txO M2XtZVIxPDh2MEG4
NCI-H661 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHe3U2Q{OyEQvF2= MYjJR|UxRjN|IN88US=> NE\DN4kzODR6NECxPC=>
NCI-H446 NUjjNlVHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2XFTFM{KM7:TR?= M3nC[WlEPTB;NzFOwG0> MlrtNlA1QDRyMUi=
MDA-MB-231 MofaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVnPRohMOzNizszN NHvDZZlKSzVyPUCuOVUh|ryP Mmr5NlA1QDRyMUi=
DLD-1 MnG4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXmzN{DPxE1? NEm1R|hKSzVyPUCuOVMh|ryP M1jZd|IxPDh2MEG4
A549 NHPTclFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2Xu[FM{KM7:TR?= NV7QRo9rUUN3ME2wMlU6KM7:TR?= NV7MdnpDOjB2OESwNVg>
SK-OV-3 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX;GO|Y1OzNizszN NX[4U21VUUN3ME2wMlY3KM7:TR?= M1LLZ|IxPDh2MEG4
NCI-H460 NYH6cmZmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NILucIQ{OyEQvF2= M3TiT2lEPTB;MD62JO69VQ>? MVyyNFQ5PDBzOB?=
A375 NFzKNmdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUWzN{DPxE1? MVPJR|UxRTBwNEKg{txO MV:yNFQ5PDBzOB?=
NCI-H441 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUmzN{DPxE1? MUDJR|UxRTBwMzFOwG0> MUCyNFQ5PDBzOB?=
HT29 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWqzN{DPxE1? NVLQb|Z6UUN3ME2wMlQ6KM7:TR?= NI\icVQzODR6NECxPC=>
MKN-45 NYXGVpNkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mme4N|Mh|ryP MojjTWM2OD1yLkW4JO69VQ>? M1XjRlIxPDh2MEG4
HT29 Ml;NRZBweHSxc3nzJIF{e2G7 MmfqglExKM7:TR?= M1;RNpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NYrHRY1yOjB2OESwNVg>
MKN-45 MoTtRZBweHSxc3nzJIF{e2G7 Mn;uglExKM7:TR?= MVHzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NWXiVZhWOjB2OESwNVg>
MDA-MB-231 NEToRW1CeG:ydH;zbZMh[XO|YYm= NXHRcWNIhjFyIN88US=> MUTtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw NHSzc|UzODR6NECxPC=>
MDA-MB-231/TGL M{exc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHXRNnd,OTByIN88US=> NFSz[IhIUTVyPUGuNkDPxE1? MlPINlIxOjd4OUC=
1833/TGL NWfS[XQzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUHTZnpIhjFyMDFOwG0> NIn6SotIUTVyPUOuO{DPxE1? MV[yNlAzPzZ7MB?=
EBC1 NUTzdmdyS3m2b4TvfIlkyqCjc4PhfS=> MmP3glExKM7:TR?= NYTVXWV5cW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> MXuyN|U6QDJ5Nh?=
SNU638 MoCxR5l1d3SxeHnjxsBie3OjeR?= MnTJglExKM7:TR?= M1nTR4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NF:xflIzOzV7OEK3Oi=>
A549 MWXDfZRwfG:6aXRCpIF{e2G7 NWnjbFN{hjFyIN88US=> NH7JbXVvd3RiYX\m[YN1 M4jJe|I{PTl6Mke2
H460 MmjvR5l1d3SxeHnjxsBie3OjeR?= MX\+NVAh|ryP MV\uc5Qh[W[oZXP0 MX6yN|U6QDJ5Nh?=
HCC827 NYTtS2gzS3m2b4TvfIlkyqCjc4PhfS=> NUDSbHhkhjFyIN88US=> NYHBOZVrdm:2IHHm[oVkfA>? MVeyN|U6QDJ5Nh?=
A549 MofOSpVv[3Srb36gZZN{[Xl? NGHPR|kyOCEQvF2= NF:zRXVlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? M3i1bVI{PTl6Mke2
EBC1 M4HS[2Z2dmO2aX;uJIF{e2G7 MUSxNEDPxE1? NGDnXotlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? MlHvNlM2QTh{N{[=
H460 Mlz1SpVv[3Srb36gZZN{[Xl? NXL0VnBpOTBizszN NXKyV4ZrcW6qaXLpeJMhfHWkdXzpckBxd2y7bXXybZpifGmxbh?= NVr5XnVOOjV|MUOwNVA>
K562/VCR MnG3R5l1d3SxeHnjxsBie3OjeR?= MlfhglExKM7:TR?= NF;hPFJ{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M2WyZVI2OzF|MEGw
CEM/VBL Ml7aR5l1d3SxeHnjxsBie3OjeR?= MVz+NVAh|ryP NV\4NpF7e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MmLQNlU{OTNyMUC=
U266 M3[0e2N6fG:2b4jpZ:Kh[XO|YYm= MWH+N{DPxE4EoB?= M4nnS2lEPTB;MT6xJO69VQ>? MnvjNlU5OTByMUO=
OPM-2 MUnDfZRwfG:6aXRCpIF{e2G7 MXv+N{DPxE4EoB?= MnTFTWM2OD1zLkig{txO MYqyOVgyODBzMx?=
MM.1S NYe1WHIyS3m2b4TvfIlkyqCjc4PhfS=> NFGyPG1,OyEQvF5CpC=> M2r1ZWlEPTB;MT62JO69VQ>? NEDPc4IzPThzMECxNy=>
MM.1R MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXvGZlhvOyEQvF5CpC=> MVnpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= NX\UNldmOjV6MUCwNVM>
RPMI-8226 M1jBdmN6fG:2b4jpZ:Kh[XO|YYm= M3rlbJ4{KM7:TdMg M2\DZ2lEPTB;MD65JO69VQ>? M37ScFI2QDFyMEGz
ANBL-6 NWTMZXo2S3m2b4TvfIlkyqCjc4PhfS=> MkWzNUDPxE4EoB?= MXPpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MUiyOVgyODBzMx?=
ANLB-6/V10R Mn7HR5l1d3SxeHnjxsBie3OjeR?= NVvP[ZE{OSEQvF5CpC=> NYCxWFZCcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> Mo\VNlU5OTByMUO=
KAS-6/1 NVTjeZNFS3m2b4TvfIlkyqCjc4PhfS=> M{PkXFEh|ryPwrC= MVjpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MWSyOVgyODBzMx?=
KAS-6/V10R M{XT[mN6fG:2b4jpZ:Kh[XO|YYm= NXTGe5RSOSEQvF5CpC=> M4TQWIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NUHjcm5xOjV6MUCwNVM>
KAS-6/R10R MWrDfZRwfG:6aXRCpIF{e2G7 NVzCPGVOOSEQvF5CpC=> M3\Hdolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MofBNlU5OTByMUO=
8226/S NGfqW|hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUSzJO69VcLi M1\udolvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> NIXtWXIzPThzMECxNy=>
8226/LR-5 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml:2N{DPxE4EoB?= MXXpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NEnoPIIzPThzMECxNy=>
Huh7 NXLDSlJCS3m2b4TvfIlkyqCjc4PhfS=> NXXBWXIzhjRwODFOwG3DqA>? NHPZ[3BFVVOR Mn3tTWM2OD17Lkmgcm0> MYKyOlI2QTJ3MB?=
Hep3B MX7DfZRwfG:6aXRCpIF{e2G7 MmjaglQvQCEQvF5CpC=> NFWyfo1FVVOR M2XQemlEPTB;NES4Mlchdk1? NHLJdm8zPjJ3OUK1NC=>
HepG2 MmrJR5l1d3SxeHnjxsBie3OjeR?= NU\LRmZthjRwODFOwG3DqA>? MVPEUXNQ NFfxcIxKSzVyPUGzPU44PyCwTR?= M{\CT|I3OjV7MkWw
Chang NWrLcnJZS3m2b4TvfIlkyqCjc4PhfS=> NHXiZpN,PC56IN88UeKh MVLEUXNQ NI\pNphKSzVyPUS0PE44KG6P NY\nNJFPOjZ{NUmyOVA>
Huh7 NHvac25HfW6ldHnvckBie3OjeR?= NICwSHEyNjZizszNxsA> NFnGXmRFVVOR MXHjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NInNNlUzPjJ3OUK1NC=>
Hep3B NEnXfXRHfW6ldHnvckBie3OjeR?= M{XNU|EvPiEQvF5CpC=> MVnEUXNQ MmLlZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MmfONlYzPTl{NUC=
HepG2 MYnGeY5kfGmxbjDhd5NigQ>? NX;SWYdYOS54IN88UeKh NWDxOXZsTE2VTx?= NY[zeplQ[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M2H6Z|I3OjV7MkWw
Chang M1W2cmZ2dmO2aX;uJIF{e2G7 NEfjOZoyNjZizszNxsA> NHriPZVFVVOR Ml;yZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MnL1NlYzPTl{NUC=
MHCC97L Ml;ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWfzcIxOhjFyIN88US=> Mk\qSG1UVw>? MVvJR|UxRTNzNTDuUS=> M2jQUVI3PDV6OUWz
MHCC97H NGnvZ2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWHmXnRThjFyIN88US=> NHzP[29FVVOR MUjJR|UxRTN4OPMAjUBvVQ>? NH;E[nIzPjR3OEm1Ny=>
Huh7 M{PGdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXu3TXpohjFyIN88US=> Mlv5SG1UVw>? NFX4dIZKSzVyPUK2OUBvVQ>? MljLNlY1PTh7NUO=
HepG2 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MojTglExKM7:TR?= MUTEUXNQ M4q0dmlEPTB;M{myJI5O MknLNlY1PTh7NUO=
MHCC97L M2\jXmZ2dmO2aX;uJIF{e2G7 MkX0NUDPxE4EoB?= NF3tfGVFVVOR NGL5eGRqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v NILzbHkzPjR3OEm1Ny=>
Huh7 M3nqb2Z2dmO2aX;uJIF{e2G7 NUnqeIRbOSEQvF5CpC=> NUfjW3hWTE2VTx?= MX7pcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u MXiyOlQ2QDl3Mx?=
MHCC97L M3S4U2Fxd3C2b4Ppd{Bie3OjeR?= MkPaNUDPxE4EoB?= M2PDSGROW09? MV7pcoR2[2W|IHHwc5B1d3Orcx?= MWmyOlQ2QDl3Mx?=
Huh7 MWDBdI9xfG:|aYOgZZN{[Xl? NF\k[YUyKM7:TdMg M4\FSWROW09? NG\XR|dqdmS3Y3XzJIFxd3C2b4Ppdy=> MUOyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts NX:2R|ZbU2mwYYPlJIF{e2G7 NYjkWllvOjVizszN MUTEUXNQ M3LzW5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MkXnNlA2OzR|NEW=
H23 M2TubWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHfHTIgzPSEQvF2= M2XUUmROW09? Mlu5d4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NF23cIQzODV|NEO0OS=>
WM35 M4C3bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mni5NVAh|ryP MWnEUXNQ NWPXUYV{e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MYCyNFU{PDN2NR?=
NIH 3T3 M2rGe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWKxNEDPxE1? NWPWR4xxTE2VTx?= M{fLSIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NHr1dHUzODV|NEO0OS=>
H838 NV\IU2FDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1HuVVExKM7:TR?= NHfvS|RFVVOR NWPHXpVs\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NXvTdGU3OjB3M{SzOFU>
H1395 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NInkSnAyOCEQvF2= Mon6SG1UVw>? NV34SlF{\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 Mmf2NlA2OzR|NEW=
Quiescent S2 MY\LbY5ie2ViYYPzZZk> NUnPVmoyOzBizszN MUXEUXNQ NYnufWd3[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz M3PmXVIyPTF6OUG1
PC3 M3jlWWFxd3C2b4Ppd{Bie3OjeR?= M1r5[VIxKM7:TR?= M33SZmROW09? M3Padolv\HWlZYOgZZBweHSxc3nz MlTQNlE4ODlzM{C=
Du145 NWjuXnkzSXCxcITvd4l{KGG|c3H5 NYjW[VF[OjBizszN M1nVRmROW09? NGTGcVNqdmS3Y3XzJIFxd3C2b4Ppdy=> NEXxd4MzOTdyOUGzNC=>
LNCaP MnO4RZBweHSxc3nzJIF{e2G7 MVmyNEDPxE1? NGPvU|FFVVOR MV3pcoR2[2W|IHHwc5B1d3Orcx?= MmCyNlE4ODlzM{C=
LAPC-4 Mk[1RZBweHSxc3nzJIF{e2G7 NECzb|AzOCEQvF2= M33kd2ROW09? MnzSbY5lfWOnczDhdI9xfG:|aYO= MoTZNlE4ODlzM{C=
LNCaP MUnGeY5kfGmxbjDhd5NigQ>? M1jVNVIxKM7:TR?= M17B[GROW09? NYHNUmpu\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= MV2yNVcxQTF|MB?=
LAPC-4 MY\GeY5kfGmxbjDhd5NigQ>? NIj5XHIzOCEQvF2= NIrveWVFVVOR M{TZTIRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NWO4NoV1OjF5MEmxN|A>
Kasumi-1 NV\sOFh[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1rkXp42OCEQvF2= MlXKSG1UVw>? Mm\DbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MnT0NlM{QTB3M{[=
SKNO-1 Ml\6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7EW4lphjVyIN88US=> NUPxS3AxTE2VTx?= M4TQc4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MUiyN|M6ODV|Nh?=
Kasumi-1 M3eyN2tqdmG|ZTDhd5NigQ>? M{[zXZ4yOCEQvF2= NHfTPJRFVVOR M2[xSpJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> M4PQPFI{OzlyNUO2
SKNO-1 MkPiT4lv[XOnIHHzd4F6 NWLDb4xWhjFyIN88US=> M3LNSGROW09? MlvCdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y MU[yN|M6ODV|Nh?=
A549 M1XqfGZ2dmO2aX;uJIF{e2G7 MoDnNVAh|ryP NH3TNHJFVVOR M3ftfYVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> Mlj1NlQ4PDZ3N{S=
NRK-52E NXvRRplqTnWwY4Tpc44h[XO|YYm= M13NWVExKM7:TR?= MX3EUXNQ M3XUR4lvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv NXzDcnF1OjVyOEiwNFI>
PC12 NWTtVolXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HBVp4yOi53IN88US=> M4PX[mROW09? MlvadJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> NIrFbm0zPTF{OEO4Oi=>
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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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