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 NITlO3dMcW6jc3WgZZN{[Xl? Mnv5glExKM7:TR?= NWrnNllbcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> M3nTb|IxPDh2MEG4
HT29 MnjQT4lv[XOnIHHzd4F6 MYX+NVAh|ryP MVrpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MVeyNFQ5PDBzOB?=
MDA-MB-231 NEj2SZpMcW6jc3WgZZN{[Xl? NUH1Omx4hjFyIN88US=> M3fSeIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NYXGcWQzOjB2OESwNVg>
NCI-H441 MnT6T4lv[XOnIHHzd4F6 NFL5fYd,OTBizszN NXW5UVIxcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MlXHNlA1QDRyMUi=
SK-MEL-28 NXTWTFRrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXvad2w5OzNizszN MlHJTWM2OD5|MzFOwG0> MmLRNlA1QDRyMUi=
NCI-H661 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYXT[VQ5OzNizszN NYLzXXEzUUN3ME6zN{DPxE1? MViyNFQ5PDBzOB?=
NCI-H446 NHXvb4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfndYZFOzNizszN NEeydZhKSzVyPUeg{txO NELVPJkzODR6NECxPC=>
MDA-MB-231 NVz6XWY1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXWzN{DPxE1? NVnybFJrUUN3ME2wMlU2KM7:TR?= NVqxdGltOjB2OESwNVg>
DLD-1 NIHUc3lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIPXbpI{OyEQvF2= MmDDTWM2OD1yLkWzJO69VQ>? MWCyNFQ5PDBzOB?=
A549 M4LLcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml\YN|Mh|ryP M2nRSmlEPTB;MD61PUDPxE1? NVjhZnZ5OjB2OESwNVg>
SK-OV-3 MmnIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH;jVpg{OyEQvF2= MWrJR|UxRTBwNk[g{txO M3zWVFIxPDh2MEG4
NCI-H460 M3\uZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2npZ|M{KM7:TR?= M2SzR2lEPTB;MD62JO69VQ>? MkjPNlA1QDRyMUi=
A375 NGHPdoVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2jkSFM{KM7:TR?= MmraTWM2OD1yLkSyJO69VQ>? M13aVFIxPDh2MEG4
NCI-H441 M1L0[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWfqU3M4OzNizszN MVLJR|UxRTBwMzFOwG0> MmiyNlA1QDRyMUi=
HT29 NFXqe3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkTLN|Mh|ryP NFPnTXJKSzVyPUCuOFkh|ryP MmPLNlA1QDRyMUi=
MKN-45 Mn\iS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{f0PFM{KM7:TR?= MmTHTWM2OD1yLkW4JO69VQ>? M{PtUlIxPDh2MEG4
HT29 M4HP[WFxd3C2b4Ppd{Bie3OjeR?= NYP1S|FphjFyIN88US=> MUnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? MYCyNFQ5PDBzOB?=
MKN-45 NFj0OoRCeG:ydH;zbZMh[XO|YYm= M1;zbJ4yOCEQvF2= NYDDUYgxe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NEDvRYkzODR6NECxPC=>
MDA-MB-231 NI[5NIpCeG:ydH;zbZMh[XO|YYm= M4Xp[54yOCEQvF2= M{LMco1w\GW|dHz5JIlv\HWlZYOgZZBweHSxc3nzJIJ6KDN3JT6= Mn3UNlA1QDRyMUi=
MDA-MB-231/TGL NUXIZpA5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWfXcnVxhjFyMDFOwG0> MXLHTVUxRTFwMjFOwG0> M4DUWlIzODJ5Nkmw
1833/TGL M{fHXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+NVAxKM7:TR?= MWnHTVUxRTNwNzFOwG0> NHSyOFQzOjB{N{[5NC=>
EBC1 NWjkRYRrS3m2b4TvfIlkyqCjc4PhfS=> M4jWPJ4yOCEQvF2= MWPpcohq[mm2czD0bIUh[2WubDDndo94fGhw NWiwTY9YOjN3OUiyO|Y>
SNU638 NXX2Wpp7S3m2b4TvfIlkyqCjc4PhfS=> Mlf2glExKM7:TR?= M4XMe4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NHi0dpAzOzV7OEK3Oi=>
A549 NHLz[2REgXSxdH;4bYPDqGG|c3H5 NE\FNVl,OTBizszN MY\uc5Qh[W[oZXP0 NFu0UmQzOzV7OEK3Oi=>
H460 NYPjN41nS3m2b4TvfIlkyqCjc4PhfS=> NEjvPVZ,OTBizszN MVHuc5Qh[W[oZXP0 M{frN|I{PTl6Mke2
HCC827 MmPCR5l1d3SxeHnjxsBie3OjeR?= NGPKbGt,OTBizszN NG\1[|dvd3RiYX\m[YN1 NELTd4wzOzV7OEK3Oi=>
A549 M4LzRWZ2dmO2aX;uJIF{e2G7 MX:xNEDPxE1? M1L3PYRqe3K3cITzJI1q[3KxdIXieYxm NITqUpIzOzV7OEK3Oi=>
EBC1 NWD4S|JXTnWwY4Tpc44h[XO|YYm= NUP3enRPOTBizszN NHzlWW1lcXO{dYD0d{BucWO{b4T1ZpVt\Q>? MWCyN|U6QDJ5Nh?=
H460 MoLySpVv[3Srb36gZZN{[Xl? NVfodFlJOTBizszN M4\YUIlvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? NI\I[Y0zPTNzM{CxNC=>
K562/VCR NEWwZVREgXSxdH;4bYPDqGG|c3H5 MWH+NVAh|ryP NXy1UlF7e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MUmyOVMyOzBzMB?=
CEM/VBL NUi3PY5LS3m2b4TvfIlkyqCjc4PhfS=> Ml\lglExKM7:TR?= Moj0d4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 NF3ZVJozPTNzM{CxNC=>
U266 NHjxe|JEgXSxdH;4bYPDqGG|c3H5 NFKxenJ,OyEQvF5CpC=> M{XJRmlEPTB;MT6xJO69VQ>? MonkNlU5OTByMUO=
OPM-2 NEPYdXNEgXSxdH;4bYPDqGG|c3H5 NVHiUGU2hjNizszNxsA> M3nje2lEPTB;MT64JO69VQ>? MnSwNlU5OTByMUO=
MM.1S MkLWR5l1d3SxeHnjxsBie3OjeR?= NEHDTpZ,OyEQvF5CpC=> M3PlTWlEPTB;MT62JO69VQ>? MY[yOVgyODBzMx?=
MM.1R MnvIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV:xPXdCOyEQvF5CpC=> NH7JOnNqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> MWeyOVgyODBzMx?=
RPMI-8226 NGnNSI5EgXSxdH;4bYPDqGG|c3H5 M1zsTJ4{KM7:TdMg NEe2XmJKSzVyPUCuPUDPxE1? NW\RR2p5OjV6MUCwNVM>
ANBL-6 MYDDfZRwfG:6aXRCpIF{e2G7 NVzXbYlHOSEQvF5CpC=> MnvrbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= M1;5OFI2QDFyMEGz
ANLB-6/V10R NX\BW4I{S3m2b4TvfIlkyqCjc4PhfS=> MofYNUDPxE4EoB?= MnzibY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NH64S3IzPThzMECxNy=>
KAS-6/1 M2Dzd2N6fG:2b4jpZ:Kh[XO|YYm= NV3nblFCOSEQvF5CpC=> MXHpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NVrscHE5OjV6MUCwNVM>
KAS-6/V10R NYLlTlNjS3m2b4TvfIlkyqCjc4PhfS=> NF\oNnUyKM7:TdMg MWnpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NG\1S|UzPThzMECxNy=>
KAS-6/R10R M4XhNGN6fG:2b4jpZ:Kh[XO|YYm= MWOxJO69VcLi MV7pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NHW0OFYzPThzMECxNy=>
8226/S NUiz[JJlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYSzJO69VcLi NXz4[4hscW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm NVHKSXJLOjV6MUCwNVM>
8226/LR-5 Mn\zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkDoN{DPxE4EoB?= NEGwU2VqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> M4PG[|I2QDFyMEGz
Huh7 NFL4[|ZEgXSxdH;4bYPDqGG|c3H5 MXv+OE45KM7:TdMg NHnLZnNFVVOR MknYTWM2OD17Lkmgcm0> MViyOlI2QTJ3MB?=
Hep3B MXTDfZRwfG:6aXRCpIF{e2G7 NUDB[VlvhjRwODFOwG3DqA>? MU\EUXNQ Mne1TWM2OD12NEiuO{BvVQ>? MWmyOlI2QTJ3MB?=
HepG2 NVTMfHB3S3m2b4TvfIlkyqCjc4PhfS=> MXz+OE45KM7:TdMg NYX1dZdnTE2VTx?= MnLJTWM2OD1zM{muO|chdk1? MkOwNlYzPTl{NUC=
Chang MYDDfZRwfG:6aXRCpIF{e2G7 NV:5XGxkhjRwODFOwG3DqA>? MnnzSG1UVw>? Mn2zTWM2OD12NEiuO{BvVQ>? NXO0OmRmOjZ{NUmyOVA>
Huh7 M3XFPGZ2dmO2aX;uJIF{e2G7 M3fzZlEvPiEQvF5CpC=> MWHEUXNQ MlLiZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NFLTSWozPjJ3OUK1NC=>
Hep3B NV3IcXhCTnWwY4Tpc44h[XO|YYm= NEDSPYsyNjZizszNxsA> NXO1fHk1TE2VTx?= MW\jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NVfYephMOjZ{NUmyOVA>
HepG2 NHHybJVHfW6ldHnvckBie3OjeR?= MWSxMlYh|ryPwrC= MWfEUXNQ MYHjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MViyOlI2QTJ3MB?=
Chang NYrYT4R3TnWwY4Tpc44h[XO|YYm= NVH1O2tCOS54IN88UeKh NIjrRpZFVVOR NYXJb5Rb[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= MVyyOlI2QTJ3MB?=
MHCC97L MlnDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkK5glExKM7:TR?= M3zGVWROW09? M4PF[mlEPTB;M{G1JI5O MoHYNlY1PTh7NUO=
MHCC97H NV7ZcJBlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUD1OGk4hjFyIN88US=> M3vsT2ROW09? MmKxTWM2OD1|NklihKkhdk1? NEe3cY4zPjR3OEm1Ny=>
Huh7 M1HGc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFX6bWt,OTBizszN NHK3UpVFVVOR NF2wWYFKSzVyPUK2OUBvVQ>? MX:yOlQ2QDl3Mx?=
HepG2 NXnl[2l1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M37jW54yOCEQvF2= NEfKV3lFVVOR MnzMTWM2OD1|OUKgcm0> M1ixPVI3PDV6OUWz
MHCC97L NHf3bm5HfW6ldHnvckBie3OjeR?= M4noTlEh|ryPwrC= NVvGfolETE2VTx?= M2HMfolv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> Mkm1NlY1PTh7NUO=
Huh7 M3TBS2Z2dmO2aX;uJIF{e2G7 M2HpfFEh|ryPwrC= M2K4N2ROW09? MYLpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u NIrzRYQzPjR3OEm1Ny=>
MHCC97L MUXBdI9xfG:|aYOgZZN{[Xl? NHHtXYsyKM7:TdMg NHrmRmRFVVOR M1;iRYlv\HWlZYOgZZBweHSxc3nz NE\PfpEzPjR3OEm1Ny=>
Huh7 NYHid4FxSXCxcITvd4l{KGG|c3H5 M2XqWVEh|ryPwrC= MWjEUXNQ NX;UVmlwcW6mdXPld{BieG:ydH;zbZM> NH7sN2ozPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts NWTUO5lYU2mwYYPlJIF{e2G7 NXuzW5R2OjVizszN NUG3WIJZTE2VTx?= M{e5RZJm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MW[yNFU{PDN2NR?=
H23 NWLXWWROT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX\IVHN{OjVizszN NUTkZpdYTE2VTx?= Mmrqd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MkLpNlA2OzR|NEW=
WM35 M1raVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHn2T5MyOCEQvF2= MmL6SG1UVw>? M2\MU5Nq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu M2fhU|IxPTN2M{S1
NIH 3T3 MlXiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXixNEDPxE1? NUPTeY9kTE2VTx?= NE\id21ld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> M{fYOVIxPTN2M{S1
H838 Mk[zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4PWdlExKM7:TR?= M33tXWROW09? Mlv5[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MneyNlA2OzR|NEW=
H1395 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWfYb2pDOTBizszN NHGw[I9FVVOR M3SwRYRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M{HjOlIxPTN2M{S1
Quiescent S2 MVTLbY5ie2ViYYPzZZk> NHvWdpk{OCEQvF2= MYfEUXNQ M1fETYNwdXCuZYTlcJkh[WK{b3fheIV{KFSVQT3pcoR2[2WmIHj5dIVz[WOndInsZZRqd25ib3[gTFNMPG2nMzDobZN1d26ncx?= MXyyNVUyQDlzNR?=
PC3 NWTCdm0xSXCxcITvd4l{KGG|c3H5 MWSyNEDPxE1? MV;EUXNQ MoDZbY5lfWOnczDhdI9xfG:|aYO= MlnENlE4ODlzM{C=
Du145 NVzkd5h6SXCxcITvd4l{KGG|c3H5 NYDpb5F7OjBizszN NX[xSXdNTE2VTx?= M{XCSIlv\HWlZYOgZZBweHSxc3nz MlLsNlE4ODlzM{C=
LNCaP M1e2OWFxd3C2b4Ppd{Bie3OjeR?= NVrSOVg5OjBizszN NIDXbWlFVVOR NIniemRqdmS3Y3XzJIFxd3C2b4Ppdy=> NFLyOngzOTdyOUGzNC=>
LAPC-4 NIrne|JCeG:ydH;zbZMh[XO|YYm= MXWyNEDPxE1? NEf0W3FFVVOR NILUc|NqdmS3Y3XzJIFxd3C2b4Ppdy=> M4LmRlIyPzB7MUOw
LNCaP NI[1VGlHfW6ldHnvckBie3OjeR?= NF3Xd|gzOCEQvF2= Ml;FSG1UVw>? MmH1[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MWWyNVcxQTF|MB?=
LAPC-4 NWTXe2VCTnWwY4Tpc44h[XO|YYm= NX[3UFV1OjBizszN NEDkN2xFVVOR M1n2[IRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NULwNZNZOjF5MEmxN|A>
Kasumi-1 M4[wVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVzy[npjhjVyIN88US=> NYrlRZFFTE2VTx?= NW\rWnpDcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NELyTHIzOzN7MEWzOi=>
SKNO-1 NVfX[GV4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1HENZ42OCEQvF2= NHnsemVFVVOR NUTXZXdicW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHLUVpAzOzN7MEWzOi=>
Kasumi-1 MlPvT4lv[XOnIHHzd4F6 NX\kcXRyhjFyIN88US=> NIf0TJpFVVOR MUTy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NFuwTJIzOzN7MEWzOi=>
SKNO-1 MojXT4lv[XOnIHHzd4F6 MkDrglExKM7:TR?= M4nzOGROW09? Moi5doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NV;pcmtLOjN|OUC1N|Y>
A549 NELVdJVHfW6ldHnvckBie3OjeR?= NGHBV2IyOCEQvF2= MX\EUXNQ NF75c5NmdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm MknxNlQ4PDZ3N{S=
NRK-52E NIS5eFBHfW6ldHnvckBie3OjeR?= NFPXPJUyOCEQvF2= NYnLNY5vTE2VTx?= NWPkcHV1cW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgV3RCXDNiboXjcIVieiC2cnHud4xw[2G2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCWR1[t{tIyNCClb3zsZYdmdiCLVjDhcoQh\mmkcn;u[YN1cW5? NV3wOI13OjVyOEiwNFI>
PC12 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{Dx[p4yOi53IN88US=> MljCSG1UVw>? MXnwdoV3\W62czDUV2EucW6mdXPl[EBv\XW{aYTlJIZwem2jdHnvci=> MX[yOVEzQDN6Nh?=
HPMCs NWDqSZJDTnWwY4Tpc44h[XO|YYm= MWry[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> NV3xeoNiOjZyNEW3PFA>
A549 MYfGeY5kfGmxbjDhd5NigQ>? M2XTS542OCEQvF2= MmfuSG1UVw>? M4fuNoFn\mWldIOgeIhmKH[rcnHsJIxq\mViY4njcIUh[W6mIHjvd5QhemW|cH;ud4U> M1XjS|I3PzFzN{S4
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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

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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