Tivantinib (ARQ 197)

For research use only. Not for use in humans.

製品コードS2753

Tivantinib (ARQ 197)化学構造

分子量(MW):369.42

Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.

サイズ 価格(税別) 在庫  
JPY 20200 あり
JPY 80000 あり
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バルク問合せ

カスタマーフィードバック(2)

  • Effect of tivantinib on the mitotic index was compared with the antimitotic drugs paclitaxel and vinblastine after overnight treatment of the HLE cell line with two different concentrations of each drug

    Clin Cancer Res, 2017, 23(15):4364-4375. Tivantinib (ARQ 197) purchased from Selleck.

  • H513 cells were treated with ARQ 197, GDC-0980, NVP-BEZ235 alone and in combination for 48 h. Cell lysates were prepared and immunoblotted for total PARP, cleaved PARP, cyclin D1 and actin as a loading control.

    PLoS One, 2014, 9(9): e105919. Tivantinib (ARQ 197) purchased from Selleck.

製品安全説明書

c-Met阻害剤の選択性比較

生物活性

製品説明 Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.
特性 The first selective c-Met inhibitor to be advanced into human clinical trials.
ターゲット
c-Met [1]
(Cell-free assay)
0.355 μM(Ki)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 M1;VfmtqdmG|ZTDhd5NigQ>? MnPhglExKM7:TR?= NXHuWmI1cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MnXmNlA1QDRyMUi=
HT29 MnfkT4lv[XOnIHHzd4F6 NHLXVnB,OTBizszN NV7PcmZscW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MXOyNFQ5PDBzOB?=
MDA-MB-231 MnyzT4lv[XOnIHHzd4F6 M3fqeJ4yOCEQvF2= MVjpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NGLsN4QzODR6NECxPC=>
NCI-H441 NGrLWGhMcW6jc3WgZZN{[Xl? NFzFV2F,OTBizszN NVLQOnRFcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NFfCWWwzODR6NECxPC=>
SK-MEL-28 M2P3OGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NECz[JY{OyEQvF2= NUjMOGZwUUN3ME6zN{DPxE1? NVPVRZpbOjB2OESwNVg>
NCI-H661 MlzOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjWSpJSOzNizszN M1TlZ2lEPTB-M{Og{txO MYOyNFQ5PDBzOB?=
NCI-H446 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYGzN{DPxE1? M3PYVWlEPTB;NzFOwG0> NYPEN3VIOjB2OESwNVg>
MDA-MB-231 MkjZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NILicnI{OyEQvF2= MmLnTWM2OD1yLkW1JO69VQ>? NH36ZYczODR6NECxPC=>
DLD-1 NFLmRnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXv2dZpnOzNizszN MoDXTWM2OD1yLkWzJO69VQ>? MXGyNFQ5PDBzOB?=
A549 Mn\nS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoO2N|Mh|ryP NXvJfHNUUUN3ME2wMlU6KM7:TR?= NYHuV2FJOjB2OESwNVg>
SK-OV-3 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLqcYI5OzNizszN NUXofFVbUUN3ME2wMlY3KM7:TR?= M3PGO|IxPDh2MEG4
NCI-H460 M37QWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTCeGJQOzNizszN MoDQTWM2OD1yLk[g{txO MWCyNFQ5PDBzOB?=
A375 Mmq5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NI\xfWE{OyEQvF2= NILIOHVKSzVyPUCuOFIh|ryP M4jkRlIxPDh2MEG4
NCI-H441 M2e5cWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4S2TVM{KM7:TR?= NIK2d5RKSzVyPUCuN{DPxE1? MoP0NlA1QDRyMUi=
HT29 NEfWdo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIqxW3A{OyEQvF2= MmnITWM2OD1yLkS5JO69VQ>? MoHkNlA1QDRyMUi=
MKN-45 MoDUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoTCN|Mh|ryP M4TNd2lEPTB;MD61PEDPxE1? NIXYdYozODR6NECxPC=>
HT29 NUPYfGNwSXCxcITvd4l{KGG|c3H5 NWf6XZROhjFyIN88US=> NGjKdlR{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= MYCyNFQ5PDBzOB?=
MKN-45 NUDKS|IxSXCxcITvd4l{KGG|c3H5 NXTNTG9GhjFyIN88US=> Mnzsd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MmS5NlA1QDRyMUi=
MDA-MB-231 MmfiRZBweHSxc3nzJIF{e2G7 NIHJ[JZ,OTBizszN NFnJbmxud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu M3HtTFIxPDh2MEG4
MDA-MB-231/TGL NHPKTZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVv+NVAxKM7:TR?= NXH3U3dzT0l3ME2xMlIh|ryP NE[5NGwzOjB{N{[5NC=>
1833/TGL NY\jXGxmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkD5glExOCEQvF2= MkH3S2k2OD1|Lkeg{txO NWrSdXdYOjJyMke2PVA>
EBC1 M{jLe2N6fG:2b4jpZ:Kh[XO|YYm= MUn+NVAh|ryP MUDpcohq[mm2czD0bIUh[2WubDDndo94fGhw NHnufHIzOzV7OEK3Oi=>
SNU638 MlLhR5l1d3SxeHnjxsBie3OjeR?= NHe2eVZ,OTBizszN MW\pcohq[mm2czD0bIUh[2WubDDndo94fGhw NFT6W4UzOzV7OEK3Oi=>
A549 MlPuR5l1d3SxeHnjxsBie3OjeR?= Mln6glExKM7:TR?= NFfLSYRvd3RiYX\m[YN1 M3\ST|I{PTl6Mke2
H460 MkHuR5l1d3SxeHnjxsBie3OjeR?= MknhglExKM7:TR?= MXHuc5Qh[W[oZXP0 Ml;YNlM2QTh{N{[=
HCC827 MYnDfZRwfG:6aXRCpIF{e2G7 M4\5d54yOCEQvF2= MlWwco91KGGoZnXjeC=> Mn7jNlM2QTh{N{[=
A549 MX\GeY5kfGmxbjDhd5NigQ>? M1zRbVExKM7:TR?= NYT6d2h2\Gm|coXweJMhdWmlcn;0eYJ2dGV? NVfIdWx6OjN3OUiyO|Y>
EBC1 MmnQSpVv[3Srb36gZZN{[Xl? M3[xcVExKM7:TR?= MkXp[Il{enWydIOgcYlkem:2dXL1cIU> MUCyN|U6QDJ5Nh?=
H460 MYrGeY5kfGmxbjDhd5NigQ>? MmK1NVAh|ryP NG\xXo5qdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w MVeyOVMyOzBzMB?=
K562/VCR NEjCWY5EgXSxdH;4bYPDqGG|c3H5 MmjvglExKM7:TR?= NUXmNpVIe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MnjXNlU{OTNyMUC=
CEM/VBL NFjCd|lEgXSxdH;4bYPDqGG|c3H5 NH3nT5F,OTBizszN MmPYd4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 M4e4VFI2OzF|MEGw
U266 MWfDfZRwfG:6aXRCpIF{e2G7 MVH+N{DPxE4EoB?= MkS2TWM2OD1zLkGg{txO MnPRNlU5OTByMUO=
OPM-2 NVTBSWpVS3m2b4TvfIlkyqCjc4PhfS=> NYHjdFByhjNizszNxsA> NF72fmVKSzVyPUGuPEDPxE1? MW[yOVgyODBzMx?=
MM.1S NXPrZ5I5S3m2b4TvfIlkyqCjc4PhfS=> MXT+N{DPxE4EoB?= MkLBTWM2OD1zLk[g{txO NUjiNIx4OjV6MUCwNVM>
MM.1R NF;kclBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIftdXc{KM7:TdMg MX7pcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= MlPyNlU5OTByMUO=
RPMI-8226 MVnDfZRwfG:6aXRCpIF{e2G7 MkP6glMh|ryPwrC= MWnJR|UxRTBwOTFOwG0> MWeyOVgyODBzMx?=
ANBL-6 MVfDfZRwfG:6aXRCpIF{e2G7 NF3FfZgyKM7:TdMg NXzyTopmcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MoHRNlU5OTByMUO=
ANLB-6/V10R MkeyR5l1d3SxeHnjxsBie3OjeR?= MnniNUDPxE4EoB?= MljlbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NHvJXGYzPThzMECxNy=>
KAS-6/1 M4D5bGN6fG:2b4jpZ:Kh[XO|YYm= NVfmOZhHOSEQvF5CpC=> NEnWSHhqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M3XnZVI2QDFyMEGz
KAS-6/V10R M1PybGN6fG:2b4jpZ:Kh[XO|YYm= MYCxJO69VcLi NEPkeHRqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M17BdlI2QDFyMEGz
KAS-6/R10R M1G5NmN6fG:2b4jpZ:Kh[XO|YYm= MoL5NUDPxE4EoB?= M3XhW4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NEnZWW0zPThzMECxNy=>
8226/S Ml7ES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFnvd|I{KM7:TdMg M1\zOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> M4XoSVI2QDFyMEGz
8226/LR-5 NHOzOoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIPIRYo{KM7:TdMg NXr1XYc5cW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm NWPnUWp5OjV6MUCwNVM>
Huh7 NYjuXlh3S3m2b4TvfIlkyqCjc4PhfS=> MmLLglQvQCEQvF5CpC=> MXvEUXNQ MljyTWM2OD17Lkmgcm0> Mkf0NlYzPTl{NUC=
Hep3B MkTrR5l1d3SxeHnjxsBie3OjeR?= MmPpglQvQCEQvF5CpC=> NYXpZnZKTE2VTx?= NETsdWVKSzVyPUS0PE44KG6P NGDzfnEzPjJ3OUK1NC=>
HepG2 MoLzR5l1d3SxeHnjxsBie3OjeR?= MlHSglQvQCEQvF5CpC=> NHXp[IpFVVOR M2LWVmlEPTB;MUO5Mlc4KG6P NUfUT3IyOjZ{NUmyOVA>
Chang MYjDfZRwfG:6aXRCpIF{e2G7 MnXKglQvQCEQvF5CpC=> MmDoSG1UVw>? NY\GNnZzUUN3ME20OFgvPyCwTR?= NXPDXIxpOjZ{NUmyOVA>
Huh7 NXjKO4lITnWwY4Tpc44h[XO|YYm= M4TaclEvPiEQvF5CpC=> NUTPfIFSTE2VTx?= M1TPc4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NWOwUlBbOjZ{NUmyOVA>
Hep3B NGPrfVBHfW6ldHnvckBie3OjeR?= M1fIdlEvPiEQvF5CpC=> NVvtXFhVTE2VTx?= M{S5fINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MXuyOlI2QTJ3MB?=
HepG2 MmLDSpVv[3Srb36gZZN{[Xl? NXjZdI17OS54IN88UeKh M3vwVWROW09? M1Po[4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NVfzfllDOjZ{NUmyOVA>
Chang NITYTGFHfW6ldHnvckBie3OjeR?= NVPrZnpjOS54IN88UeKh MkXCSG1UVw>? MkTTZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MVGyOlI2QTJ3MB?=
MHCC97L MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rodZ4yOCEQvF2= MX7EUXNQ NIjCVnJKSzVyPUOxOUBvVQ>? NH7Ld5EzPjR3OEm1Ny=>
MHCC97H MnTBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYj+NVAh|ryP MW\EUXNQ MY\JR|UxRTN4OPMAjUBvVQ>? NGHZblMzPjR3OEm1Ny=>
Huh7 M1\pfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVXHWldyhjFyIN88US=> M33jd2ROW09? NGXmN4FKSzVyPUK2OUBvVQ>? MnLwNlY1PTh7NUO=
HepG2 M2\5V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4fDXp4yOCEQvF2= NWO4No91TE2VTx?= MU\JR|UxRTN7MjDuUS=> NITNb3czPjR3OEm1Ny=>
MHCC97L MmPDSpVv[3Srb36gZZN{[Xl? M1XoTlEh|ryPwrC= MlnaSG1UVw>? NV3kPVI4cW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? MkPxNlY1PTh7NUO=
Huh7 NGrYc2pHfW6ldHnvckBie3OjeR?= MX2xJO69VcLi NH\yemJFVVOR NHfYV4NqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MnzNNlY1PTh7NUO=
MHCC97L NHXKO4FCeG:ydH;zbZMh[XO|YYm= MoLqNUDPxE4EoB?= NEjmboZFVVOR NGfyWVdqdmS3Y3XzJIFxd3C2b4Ppdy=> Mom1NlY1PTh7NUO=
Huh7 NUjrR4JlSXCxcITvd4l{KGG|c3H5 M4\ubFEh|ryPwrC= MXLEUXNQ M2T6c4lv\HWlZYOgZZBweHSxc3nz MUeyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts NVLvTI5GU2mwYYPlJIF{e2G7 MlvtNlUh|ryP MlexSG1UVw>? MV7y[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg M3HseVIxPTN2M{S1
H23 MmDvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXHGXVRWOjVizszN MmrrSG1UVw>? M4nvdpNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NXLmbI55OjB3M{SzOFU>
WM35 NYGyd3V{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmDHNVAh|ryP MmToSG1UVw>? M1fBXJNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MkPQNlA2OzR|NEW=
NIH 3T3 NWPLNoh2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;X[HIyOCEQvF2= NWLUR|l7TE2VTx?= NWDpcWJ1\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NXPxelNOOjB3M{SzOFU>
H838 M1;sS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXyxNEDPxE1? MVrEUXNQ MlO4[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 M3nWU|IxPTN2M{S1
H1395 NIHucVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4XPVFExKM7:TR?= MnXUSG1UVw>? MXPkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= MUOyNFU{PDN2NR?=
Quiescent S2 NEPqPGpMcW6jc3WgZZN{[Xl? NVridIw2OzBizszN M2XEOGROW09? MUnjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? MVqyNVUyQDlzNR?=
PC3 NIPxcVVCeG:ydH;zbZMh[XO|YYm= MoXRNlAh|ryP M3WxN2ROW09? MlfRbY5lfWOnczDhdI9xfG:|aYO= Ml3zNlE4ODlzM{C=
Du145 NULUe4hTSXCxcITvd4l{KGG|c3H5 NUDye4t3OjBizszN NUDtR3ZkTE2VTx?= MX;pcoR2[2W|IHHwc5B1d3Orcx?= NIPwXGozOTdyOUGzNC=>
LNCaP M3HLO2Fxd3C2b4Ppd{Bie3OjeR?= NF7HcWozOCEQvF2= NEOyXJBFVVOR NYS1bFBGcW6mdXPld{BieG:ydH;zbZM> NHvKTVQzOTdyOUGzNC=>
LAPC-4 NID1WmFCeG:ydH;zbZMh[XO|YYm= NXu1[ZJtOjBizszN M4HjeGROW09? NVLqfpVHcW6mdXPld{BieG:ydH;zbZM> M1;P[|IyPzB7MUOw
LNCaP MUTGeY5kfGmxbjDhd5NigQ>? NXHLNHJ5OjBizszN NEntNHRFVVOR Mom0[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? Mn7QNlE4ODlzM{C=
LAPC-4 NHnHRlJHfW6ldHnvckBie3OjeR?= NVHnWZl5OjBizszN MUDEUXNQ NY[5[5h[\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= MoDlNlE4ODlzM{C=
Kasumi-1 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVX+OVAh|ryP M2DuUWROW09? M{DIdIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MYmyN|M6ODV|Nh?=
SKNO-1 NX;sOlFmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoLDglUxKM7:TR?= NF31WJVFVVOR M{DmVYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NXjF[oduOjN|OUC1N|Y>
Kasumi-1 NGrBcnNMcW6jc3WgZZN{[Xl? M4\2SZ4yOCEQvF2= MlvkSG1UVw>? Mmf1doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y M1PSRlI{OzlyNUO2
SKNO-1 NIf0dGtMcW6jc3WgZZN{[Xl? MmPBglExKM7:TR?= NELyWFRFVVOR MlO1doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y MXmyN|M6ODV|Nh?=
A549 NFe0RWpHfW6ldHnvckBie3OjeR?= NF3aeo4yOCEQvF2= MkH5SG1UVw>? M1XpSoVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> NFrWcJIzPDd2NkW3OC=>
NRK-52E M4Lzb2Z2dmO2aX;uJIF{e2G7 MV:xNEDPxE1? MUjEUXNQ NH3tPIxqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDTWGFVOyCwdXPs[YFzKHS{YX7zcI9k[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKFSJRj5OtlEtKGOxbHzh[4VvKEmYIHHu[EBncWK{b37lZ5Rqdg>? NWjWOG5iOjVyOEiwNFI>
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NALM-6 NXnZeYdzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NULzUIVXOTBizszN NYe2TGF1TE2VTx?= MUHFR|UxRTR{MTDuUS=> MXKxPVA3PDd|MB?=
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Jurkat MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\ySVExKM7:TR?= NH;1PXpFVVOR NX;yUnlvTUN3ME2yNlUhdk1? NIPLU3gyQTB4NEezNC=>
MOLT-4 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFTIdJcyOCEQvF2= MYDEUXNQ M2TE[2VEPTB;MkOyJI5O MmPiNVkxPjR5M{C=
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CEM/C3 M1fw[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEXLTGUyOCEQvF2= MVnEUXNQ MXfFR|UxRTJ3NzDuUS=> NWSwNGk2OTlyNkS3N|A>
CEM/C2 Mn3DS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX6xNEDPxE1? NWfBW5RzTE2VTx?= MlLnSWM2OD1{N{Ggcm0> MkjpNVkxPjR5M{C=
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CHLA-266 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVSxNEDPxE1? NYD1OYFGUUN3ME2xMlIzKM7:TR?= NEHvTY0zODd2ME[yNy=>
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CHLA-9 M{K2NWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF3B[FYyOCEQvF2= MonjTWM2OD13OUGgcm0> NVP6R5FJOjB5NEC2NlM>
CHLA-10 NF[xWG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXOxNEDPxE1? NFPDO|ZKSzVyPUGwNkBvVQ>? M2\wcFIxPzRyNkKz
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NB-1643 Ml2xS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmf1NVAh|ryP NG\uTVVKSzVyPUWuOEDPxE1? MXuyNFc1ODZ{Mx?=
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Kasumi-1 M4XuWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHq4XVMyOCEQvF2= MVPJR|UxRTFyNzDuUS=> NX3BV2d6OjB5NEC2NlM>
Karpas-299 NVvObXBST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGXjfY0yOCEQvF2= MYHJR|UxRTJwOUOg{txO NX7rU4lmOjB5NEC2NlM>
Ramos-RA1 M3\XNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXLaSWw1OTBizszN NF6xVmxKSzVyPUeuN|Uh|ryP M3HCZlIxPzRyNkKz
H1299 MoTqT4lv[XOnIHHzd4F6 NIq4V5EyOCEQvF2= M2q2ZolvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> MUGyNVkxQDZzNh?=

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アッセイ
Methods Test Index PMID
Western blot
cMET / p-cMET / p-AKT / p-ERK / p-rpS6 ; 

PubMed: 23022995     


A498 and 769P cell lines were treated with increasing concentrations of ARQ 197 for 24 h. Total c-Met expression remained relatively stable with drug treatment. Phosphorylated c-Met expression was highest in control (untreated cells) and was blocked with increasing concentrations of ARQ 197. Downstream changes in the c-Met pathway were seen predominantly in phosphorylated AKT, while decreased phosphorylated ERK1/2 and phosphorylated rpS6 (P70S6Kinase) occurred at higher c-Met inhibitor concentrations.

23022995
Growth inhibition assay
Cell viability; 

PubMed: 23598276     


Cells were treated with the increasing concentrations of tivantinib for 72 hr. Viable cells were assessed by CellTiter-Glo assay and were graphed relative to untreated cells. Experiments were carried out in sextuplet. The average values and SDs are shown. 

23598276
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

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.
細胞試験: [1]
- 合併
  • 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.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
  • 投薬量: 200 mg/kg
  • 投与方法: Orally administered
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 73 mg/mL (197.6 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 369.42
化学式

C23H19N3O2

CAS No. 905854-02-6
Storage powder
in solvent
別名 N/A
Smiles O=C1NC(=O)C(C1C2=C[NH]C3=C2C=CC=C3)C4=C[N]5CCCC6=CC=CC4=C56

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02150733 Completed Drug: Tivantinib Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT01892527 Unknown status Drug: Tivantinib (ARQ197) Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Unknown status Drug: Tivantinib Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

  • 回答:

    S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.

c-Metシグナル伝達経路

c-Met Inhibitors with Unique Features

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