Tivantinib (ARQ 197)

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)  
JPY 18260.00
JPY 78020.00

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 M{jlUGtqdmG|ZTDhd5NigQ>? M3K2[J4yOCEQvF2= MVHpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NYTNRYNoOjB2OESwNVg>
HT29 MXvLbY5ie2ViYYPzZZk> NGjSUmN,OTBizszN M17heIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MYqyNFQ5PDBzOB?=
MDA-MB-231 NE\KT|BMcW6jc3WgZZN{[Xl? NEjuPGN,OTBizszN NWr5XXk4cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> M2W3ZlIxPDh2MEG4
NCI-H441 MXPLbY5ie2ViYYPzZZk> MkjiglExKM7:TR?= Ml7obY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NILrPWEzODR6NECxPC=>
SK-MEL-28 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYizN{DPxE1? M4Xxd2lEPTB-M{Og{txO M3zHTlIxPDh2MEG4
NCI-H661 Mo\4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorTN|Mh|ryP M3vTSWlEPTB-M{Og{txO M3f3cVIxPDh2MEG4
NCI-H446 M{L5dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVKzN{DPxE1? NF\uXWhKSzVyPUeg{txO M3HjeVIxPDh2MEG4
MDA-MB-231 NIP5d5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M123OlM{KM7:TR?= MlnHTWM2OD1yLkW1JO69VQ>? MlWzNlA1QDRyMUi=
DLD-1 MmG2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXH3e2FZOzNizszN MX;JR|UxRTBwNUOg{txO MUmyNFQ5PDBzOB?=
A549 NUW5clNJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPSXng{OyEQvF2= MXTJR|UxRTBwNUmg{txO M4r3dFIxPDh2MEG4
SK-OV-3 NHy1dIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1HOOFM{KM7:TR?= NV7NRoc4UUN3ME2wMlY3KM7:TR?= MUSyNFQ5PDBzOB?=
NCI-H460 M4jOdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmXjN|Mh|ryP M3i3WGlEPTB;MD62JO69VQ>? MX6yNFQ5PDBzOB?=
A375 NGLxcZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3rrelM{KM7:TR?= NYHW[lNHUUN3ME2wMlQzKM7:TR?= NG\5N4szODR6NECxPC=>
NCI-H441 M3TPOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2TmUVM{KM7:TR?= NGHlZW1KSzVyPUCuN{DPxE1? NVv3O3RlOjB2OESwNVg>
HT29 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIH6eo4{OyEQvF2= NV;vXXJ[UUN3ME2wMlQ6KM7:TR?= MnTuNlA1QDRyMUi=
MKN-45 NIXHRXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUSzN{DPxE1? NH\o[GhKSzVyPUCuOVgh|ryP MVyyNFQ5PDBzOB?=
HT29 NGrFNIxCeG:ydH;zbZMh[XO|YYm= M2D1PJ4yOCEQvF2= MnrUd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MUeyNFQ5PDBzOB?=
MKN-45 M1KxW2Fxd3C2b4Ppd{Bie3OjeR?= NGSxdmV,OTBizszN MkS0d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NX;XeW96OjB2OESwNVg>
MDA-MB-231 MlXJRZBweHSxc3nzJIF{e2G7 MVf+NVAh|ryP NVTRdIFxdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> MoLlNlA1QDRyMUi=
MDA-MB-231/TGL M4XjWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{HHOZ4yODBizszN NHzM[YxIUTVyPUGuNkDPxE1? MXqyNlAzPzZ7MB?=
1833/TGL MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUD+NVAxKM7:TR?= NET6XpFIUTVyPUOuO{DPxE1? Mnm4NlIxOjd4OUC=
EBC1 NEf4WIVEgXSxdH;4bYPDqGG|c3H5 NYLtTWp4hjFyIN88US=> MXrpcohq[mm2czD0bIUh[2WubDDndo94fGhw MlTCNlM2QTh{N{[=
SNU638 MkfFR5l1d3SxeHnjxsBie3OjeR?= NGLVNYZ,OTBizszN M3LkSolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NEPyOIczOzV7OEK3Oi=>
A549 MVXDfZRwfG:6aXRCpIF{e2G7 M3\iT54yOCEQvF2= NHrHOXdvd3RiYX\m[YN1 MkHNNlM2QTh{N{[=
H460 NX\PNWlpS3m2b4TvfIlkyqCjc4PhfS=> M1u4Zp4yOCEQvF2= MljQco91KGGoZnXjeC=> NH7kNYwzOzV7OEK3Oi=>
HCC827 MXPDfZRwfG:6aXRCpIF{e2G7 MUj+NVAh|ryP NFmwb4Zvd3RiYX\m[YN1 MX6yN|U6QDJ5Nh?=
A549 M4fLXWZ2dmO2aX;uJIF{e2G7 MVOxNEDPxE1? NXrGW446\Gm|coXweJMhdWmlcn;0eYJ2dGV? NVrBU5ZzOjN3OUiyO|Y>
EBC1 NGnVUWpHfW6ldHnvckBie3OjeR?= NWnuelF[OTBizszN NW\0OIZI\Gm|coXweJMhdWmlcn;0eYJ2dGV? MlL4NlM2QTh{N{[=
H460 NH7CcldHfW6ldHnvckBie3OjeR?= MmjMNVAh|ryP MXrpcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v MkW4NlU{OTNyMUC=
K562/VCR NVy2[2d2S3m2b4TvfIlkyqCjc4PhfS=> NHfvTXd,OTBizszN M2PNSJNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= NYXYN4M2OjV|MUOwNVA>
CEM/VBL MYHDfZRwfG:6aXRCpIF{e2G7 NWS2fHF5hjFyIN88US=> NHzvPY1{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= NYfpPJpROjV|MUOwNVA>
U266 MX;DfZRwfG:6aXRCpIF{e2G7 NFjoW|Z,OyEQvF5CpC=> NVnYSXROUUN3ME2xMlEh|ryP NInG[oszPThzMECxNy=>
OPM-2 NIDxbWVEgXSxdH;4bYPDqGG|c3H5 NIPOUFB,OyEQvF5CpC=> M3vGVGlEPTB;MT64JO69VQ>? MmLoNlU5OTByMUO=
MM.1S MULDfZRwfG:6aXRCpIF{e2G7 MkH3glMh|ryPwrC= MYHJR|UxRTFwNjFOwG0> NF73SIozPThzMECxNy=>
MM.1R MoewS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVizJO69VcLi NGK1U4JqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> MXmyOVgyODBzMx?=
RPMI-8226 MXfDfZRwfG:6aXRCpIF{e2G7 MlO4glMh|ryPwrC= M{ewUmlEPTB;MD65JO69VQ>? M1vBVVI2QDFyMEGz
ANBL-6 MlP3R5l1d3SxeHnjxsBie3OjeR?= MnW3NUDPxE4EoB?= NUjMNnRMcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NEK3dXczPThzMECxNy=>
ANLB-6/V10R M3PtVWN6fG:2b4jpZ:Kh[XO|YYm= MX2xJO69VcLi M4fUbIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MlfMNlU5OTByMUO=
KAS-6/1 NWDtdmVHS3m2b4TvfIlkyqCjc4PhfS=> NYLoVHQyOSEQvF5CpC=> MlnjbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= M1rCfVI2QDFyMEGz
KAS-6/V10R NF3KPW9EgXSxdH;4bYPDqGG|c3H5 MUCxJO69VcLi MYnpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MUOyOVgyODBzMx?=
KAS-6/R10R M1[0OWN6fG:2b4jpZ:Kh[XO|YYm= NID3SmwyKM7:TdMg MYLpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NETC[JozPThzMECxNy=>
8226/S NYTuc29DT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXi1R5hnOyEQvF5CpC=> M3j4dolvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> NFnSbXAzPThzMECxNy=>
8226/LR-5 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWnlPYJCOyEQvF5CpC=> MVXpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= M1n3ZVI2QDFyMEGz
Huh7 NXvzcZFiS3m2b4TvfIlkyqCjc4PhfS=> M3PMVp41NjhizszNxsA> MV\EUXNQ NIXhc|JKSzVyPUmuPUBvVQ>? NGX3NWUzPjJ3OUK1NC=>
Hep3B MmjDR5l1d3SxeHnjxsBie3OjeR?= MX3+OE45KM7:TdMg MoHISG1UVw>? MlHtTWM2OD12NEiuO{BvVQ>? MXmyOlI2QTJ3MB?=
HepG2 Mn7RR5l1d3SxeHnjxsBie3OjeR?= NH\nTpZ,PC56IN88UeKh MXzEUXNQ MnzMTWM2OD1zM{muO|chdk1? NEnRU2MzPjJ3OUK1NC=>
Chang M1nqeGN6fG:2b4jpZ:Kh[XO|YYm= NUf3R|gyhjRwODFOwG3DqA>? M2jFZWROW09? MXLJR|UxRTR2OD63JI5O NIC1dJMzPjJ3OUK1NC=>
Huh7 NILXbWVHfW6ldHnvckBie3OjeR?= NYC1NZlSOS54IN88UeKh MV7EUXNQ M2W1cINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M1fmVFI3OjV7MkWw
Hep3B NHy0Rm9HfW6ldHnvckBie3OjeR?= NEez[o0yNjZizszNxsA> MX\EUXNQ NGP2cnZk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M3\XTlI3OjV7MkWw
HepG2 NH7wV4hHfW6ldHnvckBie3OjeR?= MoLnNU43KM7:TdMg MkmySG1UVw>? NFzUbHBk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NFS3TIszPjJ3OUK1NC=>
Chang M3;DXWZ2dmO2aX;uJIF{e2G7 NVvnZotrOS54IN88UeKh M4H6V2ROW09? M{n0[4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? Mnj0NlYzPTl{NUC=
MHCC97L NUfvfnhnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4HHOJ4yOCEQvF2= MnS3SG1UVw>? NVHwSZpLUUN3ME2zNVUhdk1? MnvGNlY1PTh7NUO=
MHCC97H MmLoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX;+NVAh|ryP NE\KS3BFVVOR Ml7MTWM2OD1|NklihKkhdk1? MXeyOlQ2QDl3Mx?=
Huh7 MmjxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3e4Tp4yOCEQvF2= NXPidohkTE2VTx?= M1\UXmlEPTB;Mk[1JI5O NHfJRlUzPjR3OEm1Ny=>
HepG2 MoH0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUCwSVhYhjFyIN88US=> MliySG1UVw>? NGLEUpJKSzVyPUO5NkBvVQ>? MXmyOlQ2QDl3Mx?=
MHCC97L M3f1bmZ2dmO2aX;uJIF{e2G7 MXSxJO69VcLi NH3STndFVVOR NGq3VWdqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v M4\JWFI3PDV6OUWz
Huh7 MorQSpVv[3Srb36gZZN{[Xl? M3\rOFEh|ryPwrC= M37odWROW09? NHfoV5ZqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MorUNlY1PTh7NUO=
MHCC97L MUjBdI9xfG:|aYOgZZN{[Xl? MlrKNUDPxE4EoB?= MlTMSG1UVw>? MVrpcoR2[2W|IHHwc5B1d3Orcx?= MkDKNlY1PTh7NUO=
Huh7 NHjuN5VCeG:ydH;zbZMh[XO|YYm= MmjHNUDPxE4EoB?= NGjJVmVFVVOR NFnlTXZqdmS3Y3XzJIFxd3C2b4Ppdy=> MVeyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts MmT6T4lv[XOnIHHzd4F6 MmjUNlUh|ryP MYHEUXNQ MX7y[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg NEfYOJozODV|NEO0OS=>
H23 NV:xXJhwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkGxNlUh|ryP MXnEUXNQ NVrIW5NVe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MlLaNlA2OzR|NEW=
WM35 NXHYZ3F{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlzTNVAh|ryP M3vOT2ROW09? MWnzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MWmyNFU{PDN2NR?=
NIH 3T3 NUnIdmg2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlTPNVAh|ryP MVfEUXNQ NWHxZ|Zs\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NU[4dWRsOjB3M{SzOFU>
H838 NXjleZJsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkjvNVAh|ryP M3fHcGROW09? NU\iO|dJ\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NVHLRXU6OjB3M{SzOFU>
H1395 NHW0RWxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{DscVExKM7:TR?= NYfjTJJQTE2VTx?= MXfkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= NF\TPW0zODV|NEO0OS=>
Quiescent S2 M3rObmtqdmG|ZTDhd5NigQ>? MnPEN|Ah|ryP M{fIOmROW09? MlfwZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| Mo\nNlE2OTh7MUW=
PC3 MXPBdI9xfG:|aYOgZZN{[Xl? NHnhR|kzOCEQvF2= M2XiVWROW09? MYLpcoR2[2W|IHHwc5B1d3Orcx?= M1K1TVIyPzB7MUOw
Du145 MU\BdI9xfG:|aYOgZZN{[Xl? MUCyNEDPxE1? M{TNbWROW09? M1y3b4lv\HWlZYOgZZBweHSxc3nz MYqyNVcxQTF|MB?=
LNCaP MV3BdI9xfG:|aYOgZZN{[Xl? MlfBNlAh|ryP NIfjc|FFVVOR NFPjN2FqdmS3Y3XzJIFxd3C2b4Ppdy=> MoPaNlE4ODlzM{C=
LAPC-4 MXLBdI9xfG:|aYOgZZN{[Xl? MnGyNlAh|ryP NGDPd3VFVVOR Mo\abY5lfWOnczDhdI9xfG:|aYO= MWWyNVcxQTF|MB?=
LNCaP MVjGeY5kfGmxbjDhd5NigQ>? M1HRcVIxKM7:TR?= MYDEUXNQ NGfZd4Vl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| Mo\wNlE4ODlzM{C=
LAPC-4 NYm4S2hQTnWwY4Tpc44h[XO|YYm= MWiyNEDPxE1? MUTEUXNQ M13wRoRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? MnnqNlE4ODlzM{C=
Kasumi-1 NYrhVHljT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoLWglUxKM7:TR?= M375d2ROW09? M2XpR4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NFezbpMzOzN7MEWzOi=>
SKNO-1 Mmf4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHmenJ,PTBizszN NVTIfo41TE2VTx?= NVjGNpBEcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MUmyN|M6ODV|Nh?=
Kasumi-1 NFvYWmpMcW6jc3WgZZN{[Xl? MVz+NVAh|ryP M3fQOGROW09? NUfaZY1bemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NF3FN2UzOzN7MEWzOi=>
SKNO-1 M4G3V2tqdmG|ZTDhd5NigQ>? NYjYc4c6hjFyIN88US=> NEL4SVdFVVOR NF\jVWNz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MVuyN|M6ODV|Nh?=
A549 MUXGeY5kfGmxbjDhd5NigQ>? M2TzNVExKM7:TR?= MWDEUXNQ NFXrV49mdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm M{HiNlI1PzR4NUe0
NRK-52E M2DWdGZ2dmO2aX;uJIF{e2G7 MorENVAh|ryP NWradGJDTE2VTx?= M{D6ZolvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv M1vscFI2ODh6MECy
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Jurkat MlnsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknoNVAh|ryP MmrYSG1UVw>? MknlSWM2OD1{MkWgcm0> M2T5eVE6ODZ2N{Ow
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CHLA-266 M{PsT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWWxNEDPxE1? MlG3TWM2OD1zLkKyJO69VQ>? MXSyNFc1ODZ{Mx?=
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H1299 M1v2O2tqdmG|ZTDhd5NigQ>? MoTjNVAh|ryP NHv0N4FqdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v M1PMUFIyQTB6NkG2

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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]
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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]
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  • 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]
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  • 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
    (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
保管
in solvent
別名 N/A

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 (g) = 濃度 (mol/L) x 体積 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02608411 Terminated Carcinoma Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3
NCT01892527 Unknown status Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Active not recruiting Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2
NCT01861301 Terminated Epithelioid Mesothelioma|Recurrent Malignant Mesothelioma|Sarcomatoid Mesothelioma|Stage II Pleural Mesothelioma|Stage III Pleural Mesothelioma|Stage IV Pleural Mesothelioma National Cancer Institute (NCI) January 2013 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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