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 NED2VFlMcW6jc3WgZZN{[Xl? Ml3DglExKM7:TR?= M4j4[YlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MX[yNFQ5PDBzOB?=
HT29 MWXLbY5ie2ViYYPzZZk> MkL4glExKM7:TR?= NWPCcohkcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NHjMWoczODR6NECxPC=>
MDA-MB-231 NFe1UVJMcW6jc3WgZZN{[Xl? MoPtglExKM7:TR?= MVXpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NF;YVGEzODR6NECxPC=>
NCI-H441 NF;0NJRMcW6jc3WgZZN{[Xl? NELsb5p,OTBizszN NVPmWXNIcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MWCyNFQ5PDBzOB?=
SK-MEL-28 NG\vb|BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFzwOGQ{OyEQvF2= M1fH[mlEPTB-M{Og{txO NGnqUlUzODR6NECxPC=>
NCI-H661 NVPjblNzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmTFN|Mh|ryP Mn;YTWM2OD5|MzFOwG0> M1jDN|IxPDh2MEG4
NCI-H446 NXfa[Id1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4K0d|M{KM7:TR?= M3n6XWlEPTB;NzFOwG0> MoLRNlA1QDRyMUi=
MDA-MB-231 NH;1WZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mo\1N|Mh|ryP Ml[0TWM2OD1yLkW1JO69VQ>? NH;GflEzODR6NECxPC=>
DLD-1 NVX1XYw3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVezN{DPxE1? NWCyfZluUUN3ME2wMlU{KM7:TR?= MYSyNFQ5PDBzOB?=
A549 NXXvWYhIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3LiTFM{KM7:TR?= MU\JR|UxRTBwNUmg{txO NF7OVm0zODR6NECxPC=>
SK-OV-3 NVq5UnA6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVfQcpFYOzNizszN M3fsUGlEPTB;MD62OkDPxE1? MnKzNlA1QDRyMUi=
NCI-H460 MoPlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4jNfVM{KM7:TR?= MXzJR|UxRTBwNjFOwG0> NVGyZ|FTOjB2OESwNVg>
A375 NXzubJJET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFzBUVc{OyEQvF2= MU\JR|UxRTBwNEKg{txO NG\3Xm8zODR6NECxPC=>
NCI-H441 MmeyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEHjWlE{OyEQvF2= NFPKPXVKSzVyPUCuN{DPxE1? NGj6TIkzODR6NECxPC=>
HT29 NXnBN|IzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVzrd4UzOzNizszN MVvJR|UxRTBwNEmg{txO NEftPGkzODR6NECxPC=>
MKN-45 NInWTHNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXTScHd7OzNizszN M4P3VWlEPTB;MD61PEDPxE1? NFrEbYYzODR6NECxPC=>
HT29 MWPBdI9xfG:|aYOgZZN{[Xl? M1fjZ54yOCEQvF2= NVKxVWVXe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NYfUfWdNOjB2OESwNVg>
MKN-45 NX\Kd24zSXCxcITvd4l{KGG|c3H5 MVr+NVAh|ryP M4TiRpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NYC3T3pNOjB2OESwNVg>
MDA-MB-231 NXrZRZI5SXCxcITvd4l{KGG|c3H5 M{TpTp4yOCEQvF2= NVG1dmpXdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> NXnkVHlIOjB2OESwNVg>
MDA-MB-231/TGL MojZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoPKglExOCEQvF2= NUX1bpJWT0l3ME2xMlIh|ryP NW\UeWVLOjJyMke2PVA>
1833/TGL NYPyfmJ1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVjKd5IzhjFyMDFOwG0> NVfGUotRT0l3ME2zMlch|ryP NIO3TGUzOjB{N{[5NC=>
EBC1 MmLsR5l1d3SxeHnjxsBie3OjeR?= MX3+NVAh|ryP MnXvbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= NEfkfFgzOzV7OEK3Oi=>
SNU638 NFW5W2JEgXSxdH;4bYPDqGG|c3H5 MYD+NVAh|ryP NX\KW4FEcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> MUWyN|U6QDJ5Nh?=
A549 M2G2SWN6fG:2b4jpZ:Kh[XO|YYm= NUPGNYZihjFyIN88US=> M1ex[45wfCCjZn\lZ5Q> NHfFe40zOzV7OEK3Oi=>
H460 MWHDfZRwfG:6aXRCpIF{e2G7 M4\XTZ4yOCEQvF2= M3q5d45wfCCjZn\lZ5Q> MnLvNlM2QTh{N{[=
HCC827 NV7SfFhlS3m2b4TvfIlkyqCjc4PhfS=> MX3+NVAh|ryP MYLuc5Qh[W[oZXP0 M3\GWlI{PTl6Mke2
A549 MVLGeY5kfGmxbjDhd5NigQ>? MWKxNEDPxE1? M{juN4Rqe3K3cITzJI1q[3KxdIXieYxm MoHDNlM2QTh{N{[=
EBC1 NFHHNmlHfW6ldHnvckBie3OjeR?= NFHne4YyOCEQvF2= NUS5N4hv\Gm|coXweJMhdWmlcn;0eYJ2dGV? Ml[1NlM2QTh{N{[=
H460 NUnzfIJLTnWwY4Tpc44h[XO|YYm= MnXtNVAh|ryP M1T2ZYlvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? Mmf2NlU{OTNyMUC=
K562/VCR NEDoTWFEgXSxdH;4bYPDqGG|c3H5 M2\me54yOCEQvF2= MnXZd4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 Mn\rNlU{OTNyMUC=
CEM/VBL M1HJemN6fG:2b4jpZ:Kh[XO|YYm= NWXaWFdFhjFyIN88US=> M4m5SZNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= M{HiZVI2OzF|MEGw
U266 NWr3cIFlS3m2b4TvfIlkyqCjc4PhfS=> NEfvR2p,OyEQvF5CpC=> M1n1UGlEPTB;MT6xJO69VQ>? M1i4SlI2QDFyMEGz
OPM-2 MlexR5l1d3SxeHnjxsBie3OjeR?= MXv+N{DPxE4EoB?= M{HWdWlEPTB;MT64JO69VQ>? MljKNlU5OTByMUO=
MM.1S M4foZmN6fG:2b4jpZ:Kh[XO|YYm= NHj6PGR,OyEQvF5CpC=> MmrJTWM2OD1zLk[g{txO M2rkb|I2QDFyMEGz
MM.1R MkXmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmPWN{DPxE4EoB?= MUDpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= MoW0NlU5OTByMUO=
RPMI-8226 MoX4R5l1d3SxeHnjxsBie3OjeR?= NWDkc|FwhjNizszNxsA> NFrYSJNKSzVyPUCuPUDPxE1? M1Xqe|I2QDFyMEGz
ANBL-6 NH71fnhEgXSxdH;4bYPDqGG|c3H5 M1jGXVEh|ryPwrC= MkjkbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= M3H5RVI2QDFyMEGz
ANLB-6/V10R MmfoR5l1d3SxeHnjxsBie3OjeR?= NWfLVWJzOSEQvF5CpC=> NH3TeWdqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MWmyOVgyODBzMx?=
KAS-6/1 NVPaXoJCS3m2b4TvfIlkyqCjc4PhfS=> M2e2bVEh|ryPwrC= NXfXe2RYcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M2iwT|I2QDFyMEGz
KAS-6/V10R MonxR5l1d3SxeHnjxsBie3OjeR?= MWexJO69VcLi M{flW4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NUjxTnV6OjV6MUCwNVM>
KAS-6/R10R M1;ZOGN6fG:2b4jpZ:Kh[XO|YYm= MWqxJO69VcLi M3LhTolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NWfEWWhKOjV6MUCwNVM>
8226/S NFnXR2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfkSYFzOyEQvF5CpC=> NUHCWYVjcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm M4OxdFI2QDFyMEGz
8226/LR-5 NVXQdGl{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF36VnI{KM7:TdMg NIPqSndqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> NUDjUmtXOjV6MUCwNVM>
Huh7 MVjDfZRwfG:6aXRCpIF{e2G7 M4DZe541NjhizszNxsA> NFfMOZhFVVOR MVTJR|UxRTlwOTDuUS=> NUfjcIVuOjZ{NUmyOVA>
Hep3B MoD4R5l1d3SxeHnjxsBie3OjeR?= NUTSVmF3hjRwODFOwG3DqA>? M17P[WROW09? MUnJR|UxRTR2OD63JI5O MYqyOlI2QTJ3MB?=
HepG2 MWXDfZRwfG:6aXRCpIF{e2G7 Mn63glQvQCEQvF5CpC=> MVTEUXNQ MY\JR|UxRTF|OT63O{BvVQ>? NWfzems5OjZ{NUmyOVA>
Chang NVHXS2JIS3m2b4TvfIlkyqCjc4PhfS=> MYn+OE45KM7:TdMg MWXEUXNQ M1HwT2lEPTB;NES4Mlchdk1? NGPrcW8zPjJ3OUK1NC=>
Huh7 NGqzTnhHfW6ldHnvckBie3OjeR?= MV[xMlYh|ryPwrC= Mn\2SG1UVw>? NEHMTFNk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M2TJTFI3OjV7MkWw
Hep3B MXvGeY5kfGmxbjDhd5NigQ>? NYXXVHJ6OS54IN88UeKh NYXaclJDTE2VTx?= Mk\1Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Mn;pNlYzPTl{NUC=
HepG2 MkjRSpVv[3Srb36gZZN{[Xl? NHHDbpAyNjZizszNxsA> Mlf4SG1UVw>? M{O3eINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NXHLeod2OjZ{NUmyOVA>
Chang MVzGeY5kfGmxbjDhd5NigQ>? MVmxMlYh|ryPwrC= MlrPSG1UVw>? MoD5Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MVOyOlI2QTJ3MB?=
MHCC97L Ml3yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4XrV54yOCEQvF2= NIq1ZohFVVOR MVPJR|UxRTNzNTDuUS=> MVKyOlQ2QDl3Mx?=
MHCC97H MkKxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4fi[J4yOCEQvF2= Mn75SG1UVw>? M2\GPWlEPTB;M{[45qCKKG6P NYjRU|BlOjZ2NUi5OVM>
Huh7 MlLPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlfQglExKM7:TR?= NIHybVBFVVOR NVPBOZl3UUN3ME2yOlUhdk1? NYjtUZNbOjZ2NUi5OVM>
HepG2 NUnaO2g6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NETjPIt,OTBizszN MoTSSG1UVw>? NHLkSXVKSzVyPUO5NkBvVQ>? NHjDbVgzPjR3OEm1Ny=>
MHCC97L NEDhTI5HfW6ldHnvckBie3OjeR?= M3XQdFEh|ryPwrC= NHrHfVVFVVOR Mn\0bY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NXrRbnU5OjZ2NUi5OVM>
Huh7 NIj6WZFHfW6ldHnvckBie3OjeR?= MmfMNUDPxE4EoB?= Mli5SG1UVw>? MUTpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u M2PqUVI3PDV6OUWz
MHCC97L NE\FWolCeG:ydH;zbZMh[XO|YYm= MX:xJO69VcLi MVfEUXNQ MUDpcoR2[2W|IHHwc5B1d3Orcx?= M1G5[lI3PDV6OUWz
Huh7 MYHBdI9xfG:|aYOgZZN{[Xl? MVKxJO69VcLi NWXRZ|VzTE2VTx?= NHTQdXBqdmS3Y3XzJIFxd3C2b4Ppdy=> NIXHSVYzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts NInUS5ZMcW6jc3WgZZN{[Xl? M4XYcVI2KM7:TR?= NGrJcppFVVOR M13je5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> NYrSWnlFOjB3M{SzOFU>
H23 M2ry[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnPLNlUh|ryP NULEWlVbTE2VTx?= MmfMd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NW[xRlNVOjB3M{SzOFU>
WM35 M{T4Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NI\hTVYyOCEQvF2= NX\Tc4VSTE2VTx?= NEP3V5B{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M4\G[VIxPTN2M{S1
NIH 3T3 MnnDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGTFcnYyOCEQvF2= MkPxSG1UVw>? NXnFZ|g5\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MVmyNFU{PDN2NR?=
H838 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUHQdWxpOTBizszN MVLEUXNQ MnLz[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NYjJXpR{OjB3M{SzOFU>
H1395 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1zYR|ExKM7:TR?= NVnW[XJqTE2VTx?= NWnFUYlp\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NFnTS|kzODV|NEO0OS=>
Quiescent S2 NVjCWHJWU2mwYYPlJIF{e2G7 MlniN|Ah|ryP M3;McmROW09? NXXwfHpY[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz NEnHTWMzOTVzOEmxOS=>
PC3 NVzDRnZrSXCxcITvd4l{KGG|c3H5 M1jQdlIxKM7:TR?= MYnEUXNQ NIrRZXNqdmS3Y3XzJIFxd3C2b4Ppdy=> NVjwU29GOjF5MEmxN|A>
Du145 M3Kx[mFxd3C2b4Ppd{Bie3OjeR?= M3PCSFIxKM7:TR?= MWrEUXNQ M{izcIlv\HWlZYOgZZBweHSxc3nz MVSyNVcxQTF|MB?=
LNCaP MoPtRZBweHSxc3nzJIF{e2G7 NVS4[YpuOjBizszN NX\yZ3RbTE2VTx?= Mor0bY5lfWOnczDhdI9xfG:|aYO= NWjaU486OjF5MEmxN|A>
LAPC-4 NHfQXXdCeG:ydH;zbZMh[XO|YYm= NGi1S40zOCEQvF2= NWLNNnplTE2VTx?= M{PsW4lv\HWlZYOgZZBweHSxc3nz MYeyNVcxQTF|MB?=
LNCaP M3PXe2Z2dmO2aX;uJIF{e2G7 M3P6ZlIxKM7:TR?= MmHWSG1UVw>? NX;qeYlp\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= M1jmSVIyPzB7MUOw
LAPC-4 MmDnSpVv[3Srb36gZZN{[Xl? M4LQWFIxKM7:TR?= NI\1O4hFVVOR MUHk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ NXTJNZlDOjF5MEmxN|A>
Kasumi-1 Mo\1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1vyTZ42OCEQvF2= M160d2ROW09? M3S1PYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Ml3RNlM{QTB3M{[=
SKNO-1 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHnelQ3hjVyIN88US=> MnvrSG1UVw>? MUfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NGfPcW8zOzN7MEWzOi=>
Kasumi-1 MYrLbY5ie2ViYYPzZZk> MVP+NVAh|ryP MXPEUXNQ NEDpcXRz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> Mon3NlM{QTB3M{[=
SKNO-1 M3vHVWtqdmG|ZTDhd5NigQ>? NFjoNHJ,OTBizszN MUfEUXNQ NEDBW41z\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> NYPVbG1vOjN|OUC1N|Y>
A549 NF3iS45HfW6ldHnvckBie3OjeR?= NV\5WFFxOTBizszN MoHxSG1UVw>? MVjlcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl MYKyOFc1PjV5NB?=
NRK-52E MWHGeY5kfGmxbjDhd5NigQ>? MoDMNVAh|ryP NUiwd5JZTE2VTx?= M3vCRolvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv MXqyOVA5QDByMh?=
PC12 MoDOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mlu3glEzNjVizszN M3fTfGROW09? MofmdJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> MlHqNlUyOjh|OE[=
HPMCs NWPhUlBUTnWwY4Tpc44h[XO|YYm= NEDkdVNz\X[ncoPld{BmeGm2aHXsbYFtKHSxIH3ld4Vv[2i7bXHsJJRz[W6|aYTpc44hd2ZiaIXtZY4heGW{aYTvcoVidCCvZYPveIhmdGmjbDDj[Yxtew>? NHKyOpAzPjB2NUe4NC=>
A549 NVXMRoJCTnWwY4Tpc44h[XO|YYm= MVP+OVAh|ryP M2nZ[2ROW09? NWfCR5B7[W[oZXP0d{B1cGVidnnyZYwhdGmoZTDjfYNt\SCjbnSgbI9{fCC{ZYPwc45{\Q>? M4fjPFI3PzFzN{S4
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H1299 NXHmbJF{U2mwYYPlJIF{e2G7 MX:xNEDPxE1? NWTnUnU1cW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? M3zVTVIyQTB6NkG2

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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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