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)は初めの非ATP競争性的なc-Met阻害剤で、無細胞実験でKi値が0.355 μMです。Tivantinib (ARQ 197)はRonに作用する活性が殆どなくて、EGFR、InsR、PDGFRαとFGFR1/4を抑制する作用がありません。臨床3期。

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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. 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)は初めの非ATP競争性的なc-Met阻害剤で、無細胞実験でKi値が0.355 μMです。Tivantinib (ARQ 197)はRonに作用する活性が殆どなくて、EGFR、InsR、PDGFRαとFGFR1/4を抑制する作用がありません。臨床3期。
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 MVnLbY5ie2ViYYPzZZk> NFHOXZV,OTBizszN NVvEVHRJcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MmHONlA1QDRyMUi=
HT29 MnHqT4lv[XOnIHHzd4F6 MnvWglExKM7:TR?= NEjtTWxqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MkTMNlA1QDRyMUi=
MDA-MB-231 NWjDUWt1U2mwYYPlJIF{e2G7 Mm\LglExKM7:TR?= Mm[5bY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MnO2NlA1QDRyMUi=
NCI-H441 M1fwZ2tqdmG|ZTDhd5NigQ>? NYX6Uld1hjFyIN88US=> MWTpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NVXoNoFwOjB2OESwNVg>
SK-MEL-28 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4D3VVM{KM7:TR?= MkTVTWM2OD5|MzFOwG0> MmjFNlA1QDRyMUi=
NCI-H661 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWKzN{DPxE1? NHjRWYtKSzVyPkOzJO69VQ>? NH;DTZAzODR6NECxPC=>
NCI-H446 M3mzZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFjtV|I{OyEQvF2= M1rsd2lEPTB;NzFOwG0> M3j5NVIxPDh2MEG4
MDA-MB-231 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{jUSFM{KM7:TR?= MWXJR|UxRTBwNUWg{txO M4DzRlIxPDh2MEG4
DLD-1 M1Oxcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIDRWlY{OyEQvF2= M4PldWlEPTB;MD61N{DPxE1? NYHXVHNtOjB2OESwNVg>
A549 M3nVS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV7NUpl7OzNizszN M2\oTWlEPTB;MD61PUDPxE1? NFvGRZIzODR6NECxPC=>
SK-OV-3 NYfvNVZxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV2zN{DPxE1? NXizNY1GUUN3ME2wMlY3KM7:TR?= NIjMNIMzODR6NECxPC=>
NCI-H460 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHKN|Mh|ryP MmX3TWM2OD1yLk[g{txO NF3GUlczODR6NECxPC=>
A375 NGr4U2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3TrXlM{KM7:TR?= MlvKTWM2OD1yLkSyJO69VQ>? Mki0NlA1QDRyMUi=
NCI-H441 MlXDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnfxN|Mh|ryP MmHOTWM2OD1yLkOg{txO MYGyNFQ5PDBzOB?=
HT29 NWO0RYJpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXqzN{DPxE1? NUC1XYY6UUN3ME2wMlQ6KM7:TR?= MVGyNFQ5PDBzOB?=
MKN-45 M{Lq[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{TTV|M{KM7:TR?= NVjyUnJEUUN3ME2wMlU5KM7:TR?= MnPhNlA1QDRyMUi=
HT29 MWLBdI9xfG:|aYOgZZN{[Xl? M1PybJ4yOCEQvF2= M{fPc5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NIX3[2wzODR6NECxPC=>
MKN-45 NEPjNVdCeG:ydH;zbZMh[XO|YYm= MY\+NVAh|ryP MYHzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? M1\VT|IxPDh2MEG4
MDA-MB-231 NXHYPYVFSXCxcITvd4l{KGG|c3H5 MnjxglExKM7:TR?= MUntc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw M{\VeVIxPDh2MEG4
MDA-MB-231/TGL MlPFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVTSbXFIhjFyMDFOwG0> NUW2[FNKT0l3ME2xMlIh|ryP MV2yNlAzPzZ7MB?=
1833/TGL MoLFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWXVdGZ5hjFyMDFOwG0> NGLq[W9IUTVyPUOuO{DPxE1? MU[yNlAzPzZ7MB?=
EBC1 NXjWVYdjS3m2b4TvfIlkyqCjc4PhfS=> NFHzbWJ,OTBizszN NViwfoxwcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> M2rYOlI{PTl6Mke2
SNU638 MWDDfZRwfG:6aXRCpIF{e2G7 M2nEU54yOCEQvF2= MkHKbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= NYn5OlZqOjN3OUiyO|Y>
A549 MUfDfZRwfG:6aXRCpIF{e2G7 NVzXSXdmhjFyIN88US=> Mmjqco91KGGoZnXjeC=> MV:yN|U6QDJ5Nh?=
H460 MV;DfZRwfG:6aXRCpIF{e2G7 NX\LVHlVhjFyIN88US=> M1TXcY5wfCCjZn\lZ5Q> MlH2NlM2QTh{N{[=
HCC827 NFe3c41EgXSxdH;4bYPDqGG|c3H5 NVHrRXVJhjFyIN88US=> Momxco91KGGoZnXjeC=> M{fUNlI{PTl6Mke2
A549 NGfGTW9HfW6ldHnvckBie3OjeR?= MVOxNEDPxE1? MYfkbZNzfXC2czDtbYNzd3S3YoXs[S=> MYqyN|U6QDJ5Nh?=
EBC1 NITxPJNHfW6ldHnvckBie3OjeR?= M1fxbFExKM7:TR?= NUDacJgx\Gm|coXweJMhdWmlcn;0eYJ2dGV? Ml7sNlM2QTh{N{[=
H460 MWXGeY5kfGmxbjDhd5NigQ>? MVSxNEDPxE1? NYjpUlJlcW6qaXLpeJMhfHWkdXzpckBxd2y7bXXybZpifGmxbh?= MWGyOVMyOzBzMB?=
K562/VCR Mo\ZR5l1d3SxeHnjxsBie3OjeR?= NVPtd4FXhjFyIN88US=> NYj0UVNpe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MmPENlU{OTNyMUC=
CEM/VBL Mke0R5l1d3SxeHnjxsBie3OjeR?= M4W3cZ4yOCEQvF2= Mn3Ud4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 M4HmRlI2OzF|MEGw
U266 NHn2c3ZEgXSxdH;4bYPDqGG|c3H5 MUH+N{DPxE4EoB?= MlX3TWM2OD1zLkGg{txO M1nzb|I2QDFyMEGz
OPM-2 NYO4W3pyS3m2b4TvfIlkyqCjc4PhfS=> NIqwcmd,OyEQvF5CpC=> NIfyWHpKSzVyPUGuPEDPxE1? MV[yOVgyODBzMx?=
MM.1S MUDDfZRwfG:6aXRCpIF{e2G7 M{m2Op4{KM7:TdMg Mo\RTWM2OD1zLk[g{txO MViyOVgyODBzMx?=
MM.1R NUfjOYxvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYOwOpltOyEQvF5CpC=> Mor0bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml NF35VY8zPThzMECxNy=>
RPMI-8226 NFfvfZpEgXSxdH;4bYPDqGG|c3H5 MmHLglMh|ryPwrC= M2fXd2lEPTB;MD65JO69VQ>? NH3SOIozPThzMECxNy=>
ANBL-6 MUjDfZRwfG:6aXRCpIF{e2G7 MoPuNUDPxE4EoB?= NEDpe|JqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MoLGNlU5OTByMUO=
ANLB-6/V10R MlS2R5l1d3SxeHnjxsBie3OjeR?= NGfXPWEyKM7:TdMg NV7SXnc3cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NUnEcmdkOjV6MUCwNVM>
KAS-6/1 MlrER5l1d3SxeHnjxsBie3OjeR?= MnHHNUDPxE4EoB?= NHeydINqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MVSyOVgyODBzMx?=
KAS-6/V10R NYO4W5Y1S3m2b4TvfIlkyqCjc4PhfS=> NFjydZAyKM7:TdMg NE\ndXFqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MnHwNlU5OTByMUO=
KAS-6/R10R M2iwbWN6fG:2b4jpZ:Kh[XO|YYm= MU[xJO69VcLi Mni0bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MoTvNlU5OTByMUO=
8226/S NGe2TGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYmzJO69VcLi MX\pcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NVnpeHBJOjV6MUCwNVM>
8226/LR-5 Mn\aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkW0N{DPxE4EoB?= M2rae4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MWSyOVgyODBzMx?=
Huh7 MoTRR5l1d3SxeHnjxsBie3OjeR?= MnvsglQvQCEQvF5CpC=> NIPQfIRFVVOR NGn2bJZKSzVyPUmuPUBvVQ>? NV;ZZW9POjZ{NUmyOVA>
Hep3B M2jUcGN6fG:2b4jpZ:Kh[XO|YYm= MUH+OE45KM7:TdMg M3fXe2ROW09? M1[xU2lEPTB;NES4Mlchdk1? NHXqXZMzPjJ3OUK1NC=>
HepG2 NGL4UYFEgXSxdH;4bYPDqGG|c3H5 MXT+OE45KM7:TdMg NXe2ZYloTE2VTx?= NYH3bVhuUUN3ME2xN|kvPzdibl2= MXmyOlI2QTJ3MB?=
Chang M3GxbWN6fG:2b4jpZ:Kh[XO|YYm= M2TGSZ41NjhizszNxsA> M2r5[WROW09? MVnJR|UxRTR2OD63JI5O M3;Fe|I3OjV7MkWw
Huh7 NV;uTXplTnWwY4Tpc44h[XO|YYm= NHLuZ|gyNjZizszNxsA> M{DpRWROW09? MUXjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NXTISYU{OjZ{NUmyOVA>
Hep3B MYrGeY5kfGmxbjDhd5NigQ>? MnnyNU43KM7:TdMg NHno[W1FVVOR MWjjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MonoNlYzPTl{NUC=
HepG2 M3zST2Z2dmO2aX;uJIF{e2G7 Ml70NU43KM7:TdMg NETDWIRFVVOR NFLDdopk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MkjzNlYzPTl{NUC=
Chang NHjGRppHfW6ldHnvckBie3OjeR?= MljxNU43KM7:TdMg M3LoPGROW09? NEPsN5pk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 Mn3lNlYzPTl{NUC=
MHCC97L MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4Tmdp4yOCEQvF2= M2H6emROW09? NYrYRlN1UUN3ME2zNVUhdk1? MkTpNlY1PTh7NUO=
MHCC97H MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmO5glExKM7:TR?= NYjJW3pXTE2VTx?= MVvJR|UxRTN4OPMAjUBvVQ>? Ml:2NlY1PTh7NUO=
Huh7 M4jCcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYfPWYR5hjFyIN88US=> MlnLSG1UVw>? MVPJR|UxRTJ4NTDuUS=> NVflfHQ4OjZ2NUi5OVM>
HepG2 NYrLWFFUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUH+NVAh|ryP MoCwSG1UVw>? MoGzTWM2OD1|OUKgcm0> NYD5TZNVOjZ2NUi5OVM>
MHCC97L NEfmVG5HfW6ldHnvckBie3OjeR?= NF3Q[4cyKM7:TdMg MXXEUXNQ MlLXbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NXz4cIl3OjZ2NUi5OVM>
Huh7 NGXTOZNHfW6ldHnvckBie3OjeR?= MnzDNUDPxE4EoB?= NGThWYxFVVOR MV\pcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u MVqyOlQ2QDl3Mx?=
MHCC97L NX:0SINjSXCxcITvd4l{KGG|c3H5 NES4OWoyKM7:TdMg NHLNTFdFVVOR MV;pcoR2[2W|IHHwc5B1d3Orcx?= MWGyOlQ2QDl3Mx?=
Huh7 NX73XWxSSXCxcITvd4l{KGG|c3H5 NVXqSlNJOSEQvF5CpC=> NFTBSIxFVVOR MW\pcoR2[2W|IHHwc5B1d3Orcx?= M1;CO|I3PDV6OUWz
C3H 10T1/2 mouse fibroblasts M3vFN2tqdmG|ZTDhd5NigQ>? NF;WO4QzPSEQvF2= M{H1RWROW09? NXPr[ppCemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? NGnJXXAzODV|NEO0OS=>
H23 MnXCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYjwW45SOjVizszN MVTEUXNQ M1vsc5Nq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NEX6fGEzODV|NEO0OS=>
WM35 M1rMNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWexNEDPxE1? NXvTeZp{TE2VTx?= M1\iXZNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NIra[5gzODV|NEO0OS=>
NIH 3T3 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVjvOYxlOTBizszN M3\0eWROW09? NELP[W9ld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NY\uXW06OjB3M{SzOFU>
H838 NVm2eVFOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfXNVAh|ryP MX3EUXNQ NHnJRXZld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NVi3Z4w{OjB3M{SzOFU>
H1395 NH7zO4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkPZNVAh|ryP M4jRZWROW09? NWi1TIF4\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MkLBNlA2OzR|NEW=
Quiescent S2 NI\sd3RMcW6jc3WgZZN{[Xl? NGLKPZQ{OCEQvF2= NWDiNnBmTE2VTx?= MkDGZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| MlPrNlE2OTh7MUW=
PC3 M1jySWFxd3C2b4Ppd{Bie3OjeR?= NFnNTFMzOCEQvF2= M{\Vd2ROW09? NF\EUZhqdmS3Y3XzJIFxd3C2b4Ppdy=> M1rldFIyPzB7MUOw
Du145 NXXvSFUySXCxcITvd4l{KGG|c3H5 NUDLZ2tEOjBizszN NG\PWIZFVVOR NV6wPXRrcW6mdXPld{BieG:ydH;zbZM> NH\GXY0zOTdyOUGzNC=>
LNCaP M1vyNWFxd3C2b4Ppd{Bie3OjeR?= NW\MfJl4OjBizszN Mlr4SG1UVw>? NVS0[GNYcW6mdXPld{BieG:ydH;zbZM> NHn3bI4zOTdyOUGzNC=>
LAPC-4 NX;C[2JnSXCxcITvd4l{KGG|c3H5 M4LJUlIxKM7:TR?= MkmySG1UVw>? MV;pcoR2[2W|IHHwc5B1d3Orcx?= M1\ZWVIyPzB7MUOw
LNCaP MVfGeY5kfGmxbjDhd5NigQ>? M3vpcVIxKM7:TR?= MULEUXNQ NUHGbJZO\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= NVzYTIFEOjF5MEmxN|A>
LAPC-4 M3ixT2Z2dmO2aX;uJIF{e2G7 NFvTRlkzOCEQvF2= NVy0ZW9pTE2VTx?= MUXk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ M4\PfFIyPzB7MUOw
Kasumi-1 MkTXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUf+OVAh|ryP MlrhSG1UVw>? M2XZUYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M3HwVlI{OzlyNUO2
SKNO-1 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2DaSp42OCEQvF2= M{fXfGROW09? NET3UmRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NXK3OWlQOjN|OUC1N|Y>
Kasumi-1 M3Hkc2tqdmG|ZTDhd5NigQ>? NGHrSWF,OTBizszN MXLEUXNQ M{fuXZJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> MoD2NlM{QTB3M{[=
SKNO-1 NFGxRXFMcW6jc3WgZZN{[Xl? MUj+NVAh|ryP M{DRXWROW09? Mm\3doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y MoLKNlM{QTB3M{[=
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Ramos-RA1 NV[4NGdOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLqSJhUOTBizszN NUHNPXhlUUN3ME23MlM2KM7:TR?= MVeyNFc1ODZ{Mx?=
H1299 MYPLbY5ie2ViYYPzZZk> MX2xNEDPxE1? MnLTbY5pcWKrdIOgTWtDU0VvaX7keYNm\CCDa4SgRYN1cX[jdHnvci=> MkDnNlE6ODh4MU[=

多くの細胞株試験データを見る場合、クリックしてください

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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 24, 2011 Phase 1
NCT02608411 Recruiting 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 Recruiting Liver Cancer Kyowa Hakko Kirin Co., Ltd January 2014 Phase 3
NCT01892527 Active, not recruiting 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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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信号経路図

c-Met Inhibitors with Unique Features

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