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 M3vHNWtqdmG|ZTDhd5NigQ>? NYfnVpBUhjFyIN88US=> Ml\3bY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NHjwcXIzODR6NECxPC=>
HT29 Ml3ET4lv[XOnIHHzd4F6 MmHzglExKM7:TR?= MofGbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MWCyNFQ5PDBzOB?=
MDA-MB-231 M4r1emtqdmG|ZTDhd5NigQ>? MYP+NVAh|ryP MUfpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M4q2V|IxPDh2MEG4
NCI-H441 NVHwRolpU2mwYYPlJIF{e2G7 MmC3glExKM7:TR?= MnLlbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NVPzc|FyOjB2OESwNVg>
SK-MEL-28 NITRdWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXzTc|BNOzNizszN NWHNcWlnUUN3ME6zN{DPxE1? MVKyNFQ5PDBzOB?=
NCI-H661 MoHFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmnPN|Mh|ryP MlnQTWM2OD5|MzFOwG0> MoLINlA1QDRyMUi=
NCI-H446 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYnxe3FDOzNizszN M1jGc2lEPTB;NzFOwG0> MXGyNFQ5PDBzOB?=
MDA-MB-231 M1;sT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIrGNJk{OyEQvF2= NEX0[phKSzVyPUCuOVUh|ryP M4rycFIxPDh2MEG4
DLD-1 MkC0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUK0[nZTOzNizszN NIHhN2xKSzVyPUCuOVMh|ryP NITW[IozODR6NECxPC=>
A549 M1L3e2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDSN|Mh|ryP NUXFcI14UUN3ME2wMlU6KM7:TR?= NEDEPIgzODR6NECxPC=>
SK-OV-3 M3uySmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{TQZVM{KM7:TR?= NEjBRm5KSzVyPUCuOlYh|ryP NHLFXVIzODR6NECxPC=>
NCI-H460 MmX4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY[zN{DPxE1? M{LwNGlEPTB;MD62JO69VQ>? MXyyNFQ5PDBzOB?=
A375 MnrES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYWzN{DPxE1? MVrJR|UxRTBwNEKg{txO NWDye5JqOjB2OESwNVg>
NCI-H441 NXX0WZhsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M32zeVM{KM7:TR?= NX2yOopVUUN3ME2wMlMh|ryP NFqye|QzODR6NECxPC=>
HT29 NXO2XHBkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYr2PFRyOzNizszN NH7GZ3ZKSzVyPUCuOFkh|ryP NVzROZpHOjB2OESwNVg>
MKN-45 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLTbZlJOzNizszN M4CxR2lEPTB;MD61PEDPxE1? NXv3[|dtOjB2OESwNVg>
HT29 MVrBdI9xfG:|aYOgZZN{[Xl? M4fXTZ4yOCEQvF2= MmG2d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw M4PtU|IxPDh2MEG4
MKN-45 MnrqRZBweHSxc3nzJIF{e2G7 MoTvglExKM7:TR?= M4n6d5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NXvJbWJkOjB2OESwNVg>
MDA-MB-231 M4PwTmFxd3C2b4Ppd{Bie3OjeR?= NHzBcWV,OTBizszN NFXLUI1ud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu NXLIOmg3OjB2OESwNVg>
MDA-MB-231/TGL MknoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M17NS54yODBizszN NV;HSXkyT0l3ME2xMlIh|ryP M4GyRlIzODJ5Nkmw
1833/TGL NIjrWFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYTJSXVLhjFyMDFOwG0> MWDHTVUxRTNwNzFOwG0> M2nQfVIzODJ5Nkmw
EBC1 NHT6R|BEgXSxdH;4bYPDqGG|c3H5 M1L0cp4yOCEQvF2= M{TrWolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= M4m4RVI{PTl6Mke2
SNU638 M2n0XWN6fG:2b4jpZ:Kh[XO|YYm= MmHBglExKM7:TR?= M{PIeIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= M4PkSVI{PTl6Mke2
A549 NXXlfo5TS3m2b4TvfIlkyqCjc4PhfS=> MYD+NVAh|ryP NUTtXmh4dm:2IHHm[oVkfA>? MYOyN|U6QDJ5Nh?=
H460 MVnDfZRwfG:6aXRCpIF{e2G7 NX\keYF2hjFyIN88US=> NG[4dVlvd3RiYX\m[YN1 M3i2[VI{PTl6Mke2
HCC827 NGLOdYtEgXSxdH;4bYPDqGG|c3H5 NIfQcZF,OTBizszN MYDuc5Qh[W[oZXP0 MUKyN|U6QDJ5Nh?=
A549 NXOzeGxGTnWwY4Tpc44h[XO|YYm= NHXaR|YyOCEQvF2= M{SxcoRqe3K3cITzJI1q[3KxdIXieYxm M4fM[VI{PTl6Mke2
EBC1 NXuzbI44TnWwY4Tpc44h[XO|YYm= Ml7jNVAh|ryP M3HxSoRqe3K3cITzJI1q[3KxdIXieYxm MX[yN|U6QDJ5Nh?=
H460 MWnGeY5kfGmxbjDhd5NigQ>? NFLNfY0yOCEQvF2= M3;kUIlvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? M4XmeVI2OzF|MEGw
K562/VCR M2PDVWN6fG:2b4jpZ:Kh[XO|YYm= M3vod54yOCEQvF2= NEXyPWR{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= MVGyOVMyOzBzMB?=
CEM/VBL MUPDfZRwfG:6aXRCpIF{e2G7 NH72NJh,OTBizszN MYfzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NGS2c|YzPTNzM{CxNC=>
U266 M1qzZmN6fG:2b4jpZ:Kh[XO|YYm= Mmq5glMh|ryPwrC= NUjRUVdYUUN3ME2xMlEh|ryP MnmwNlU5OTByMUO=
OPM-2 MXrDfZRwfG:6aXRCpIF{e2G7 NWPjXHI{hjNizszNxsA> MlvYTWM2OD1zLkig{txO MlnsNlU5OTByMUO=
MM.1S MkK4R5l1d3SxeHnjxsBie3OjeR?= M3rsXZ4{KM7:TdMg NEnCfm9KSzVyPUGuOkDPxE1? NH;hc3IzPThzMECxNy=>
MM.1R NVrC[phET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;Hc5pPOyEQvF5CpC=> NHnwVotqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> NFrHZ4QzPThzMECxNy=>
RPMI-8226 MmrIR5l1d3SxeHnjxsBie3OjeR?= NXzjS5hNhjNizszNxsA> MYTJR|UxRTBwOTFOwG0> NYKx[nhtOjV6MUCwNVM>
ANBL-6 M{iycmN6fG:2b4jpZ:Kh[XO|YYm= NEfqV5YyKM7:TdMg MY\pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NGHzepIzPThzMECxNy=>
ANLB-6/V10R NGnaTZNEgXSxdH;4bYPDqGG|c3H5 MoXHNUDPxE4EoB?= MUXpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= M3q4U|I2QDFyMEGz
KAS-6/1 NWXaO5UxS3m2b4TvfIlkyqCjc4PhfS=> MnLvNUDPxE4EoB?= NUPrV3ZtcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NV;C[5IxOjV6MUCwNVM>
KAS-6/V10R M2rpV2N6fG:2b4jpZ:Kh[XO|YYm= MUOxJO69VcLi NW\0S4ZJcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NYDoVXA3OjV6MUCwNVM>
KAS-6/R10R MYrDfZRwfG:6aXRCpIF{e2G7 M{OxTlEh|ryPwrC= M4\jdYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MV[yOVgyODBzMx?=
8226/S M1LOOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUWzJO69VcLi MWnpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NVTDfGI2OjV6MUCwNVM>
8226/LR-5 NHXrcmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWTmRVhvOyEQvF5CpC=> M2HyN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MlLYNlU5OTByMUO=
Huh7 MVjDfZRwfG:6aXRCpIF{e2G7 M3\Dep41NjhizszNxsA> NGHDWnpFVVOR MUXJR|UxRTlwOTDuUS=> MVqyOlI2QTJ3MB?=
Hep3B NGrMRXlEgXSxdH;4bYPDqGG|c3H5 M4r1e541NjhizszNxsA> MXvEUXNQ M{X3SGlEPTB;NES4Mlchdk1? NF7rNWszPjJ3OUK1NC=>
HepG2 NGG3R3hEgXSxdH;4bYPDqGG|c3H5 NVPxeopQhjRwODFOwG3DqA>? M4HOdmROW09? MojtTWM2OD1zM{muO|chdk1? M2DTOlI3OjV7MkWw
Chang NFfRPYNEgXSxdH;4bYPDqGG|c3H5 NIHRd2d,PC56IN88UeKh Mlm4SG1UVw>? Mm\BTWM2OD12NEiuO{BvVQ>? NEDPfogzPjJ3OUK1NC=>
Huh7 NGXs[mRHfW6ldHnvckBie3OjeR?= NH[yPFQyNjZizszNxsA> NUH4S3BSTE2VTx?= M2rNWYNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NVLne2N3OjZ{NUmyOVA>
Hep3B MYXGeY5kfGmxbjDhd5NigQ>? M2W3Z|EvPiEQvF5CpC=> MnvJSG1UVw>? NX7uWpJD[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M3LnUVI3OjV7MkWw
HepG2 M{jHVWZ2dmO2aX;uJIF{e2G7 NWHaSFdiOS54IN88UeKh M3;oTGROW09? MonmZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Mo\VNlYzPTl{NUC=
Chang MWnGeY5kfGmxbjDhd5NigQ>? MVixMlYh|ryPwrC= M3vET2ROW09? MX3jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M2DReVI3OjV7MkWw
MHCC97L MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MY\+NVAh|ryP MoLPSG1UVw>? MXXJR|UxRTNzNTDuUS=> NF21SVkzPjR3OEm1Ny=>
MHCC97H MmTyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVr+NVAh|ryP NYfLTWJCTE2VTx?= M37Pb2lEPTB;M{[45qCKKG6P NXTa[4tHOjZ2NUi5OVM>
Huh7 NWjacWtPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYW4ZlBRhjFyIN88US=> MUnEUXNQ NHj2VmxKSzVyPUK2OUBvVQ>? NXzL[m4xOjZ2NUi5OVM>
HepG2 M37uOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4LzNZ4yOCEQvF2= M{faSmROW09? M2fRbmlEPTB;M{myJI5O MVmyOlQ2QDl3Mx?=
MHCC97L MXPGeY5kfGmxbjDhd5NigQ>? NGDJZWkyKM7:TdMg M3rFV2ROW09? MmG4bY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NEPGOoYzPjR3OEm1Ny=>
Huh7 NF\zOnlHfW6ldHnvckBie3OjeR?= MnP6NUDPxE4EoB?= MmftSG1UVw>? NIjUZ5hqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v NGXKV2EzPjR3OEm1Ny=>
MHCC97L NGm4XnNCeG:ydH;zbZMh[XO|YYm= MUSxJO69VcLi NEjOSXBFVVOR M4C5Oolv\HWlZYOgZZBweHSxc3nz MV[yOlQ2QDl3Mx?=
Huh7 Mlr3RZBweHSxc3nzJIF{e2G7 M{PaXFEh|ryPwrC= MYXEUXNQ MULpcoR2[2W|IHHwc5B1d3Orcx?= NXz2RnhnOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts M1:5eWtqdmG|ZTDhd5NigQ>? NHewe4wzPSEQvF2= NYr2OWRRTE2VTx?= MY\y[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg M{f6XVIxPTN2M{S1
H23 M3;0bWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4rpTlI2KM7:TR?= MV;EUXNQ NXz2TlFYe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> Mm\ONlA2OzR|NEW=
WM35 NWjYU5pRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWSxNEDPxE1? M3;tSWROW09? NETl[4F{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NVvq[GdMOjB3M{SzOFU>
NIH 3T3 M4Dqemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUX6WHdSOTBizszN MkCwSG1UVw>? NXv4W4pt\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NYHSSGd5OjB3M{SzOFU>
H838 NF\QSWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4nrWlExKM7:TR?= MXPEUXNQ M33hWYRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NEDuUWczODV|NEO0OS=>
H1395 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHmNVAh|ryP MkW4SG1UVw>? MlTG[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MVmyNFU{PDN2NR?=
Quiescent S2 NVXW[It1U2mwYYPlJIF{e2G7 NFTXcZU{OCEQvF2= M{XOW2ROW09? NXr2bmNP[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz Mlq5NlE2OTh7MUW=
PC3 NFj0XWxCeG:ydH;zbZMh[XO|YYm= NUL3RpVsOjBizszN NUDUTIFmTE2VTx?= MVXpcoR2[2W|IHHwc5B1d3Orcx?= NV34VINEOjF5MEmxN|A>
Du145 NIHRdIZCeG:ydH;zbZMh[XO|YYm= MlPzNlAh|ryP NGm1elVFVVOR NVzHeVdKcW6mdXPld{BieG:ydH;zbZM> MUiyNVcxQTF|MB?=
LNCaP MkXTRZBweHSxc3nzJIF{e2G7 NWLIPVZnOjBizszN NXraOXdUTE2VTx?= MWLpcoR2[2W|IHHwc5B1d3Orcx?= MVuyNVcxQTF|MB?=
LAPC-4 M3jod2Fxd3C2b4Ppd{Bie3OjeR?= NULGXINkOjBizszN NV:4SHZ[TE2VTx?= Moq4bY5lfWOnczDhdI9xfG:|aYO= NGLobJYzOTdyOUGzNC=>
LNCaP MnrISpVv[3Srb36gZZN{[Xl? MVKyNEDPxE1? NVXielZvTE2VTx?= MX\k[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ MUGyNVcxQTF|MB?=
LAPC-4 M3TKVmZ2dmO2aX;uJIF{e2G7 NWWwd4ZIOjBizszN NGPH[IhFVVOR MYLk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ MX[yNVcxQTF|MB?=
Kasumi-1 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIXI[pZ,PTBizszN NEDqTFdFVVOR Ml3VbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M2f5XFI{OzlyNUO2
SKNO-1 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3y1PJ42OCEQvF2= MmjDSG1UVw>? MYLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MmSzNlM{QTB3M{[=
Kasumi-1 NVvzRXZlU2mwYYPlJIF{e2G7 MlfHglExKM7:TR?= M2LTVWROW09? MkfXdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y M{f4SFI{OzlyNUO2
SKNO-1 MVPLbY5ie2ViYYPzZZk> MWT+NVAh|ryP M4nPe2ROW09? NIHYV29z\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MVmyN|M6ODV|Nh?=
A549 MontSpVv[3Srb36gZZN{[Xl? NYrCd3JrOTBizszN NVLZb2FxTE2VTx?= MXzlcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl MW[yOFc1PjV5NB?=
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Ramos-RA1 NGDnS4dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUGxNEDPxE1? NEDk[IZKSzVyPUeuN|Uh|ryP NGHsNHMzODd2ME[yNy=>
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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
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
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
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3

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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