Tivantinib (ARQ 197)

Catalog No.S2753

Tivantinib (ARQ 197) Chemical Structure

Molecular Weight(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.

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2 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective c-Met Inhibitors

Biological Activity

Description 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.
Features The first selective c-Met inhibitor to be advanced into human clinical trials.
Targets
c-Met [1]
(Cell-free assay)
0.355 μM(Ki)
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 NV7Nd3hGU2mwYYPlJIF{e2G7 M4fZTZ4yOCEQvF2= MoDmbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NVf4XFg3OjB2OESwNVg>
HT29 NVTCdY9xU2mwYYPlJIF{e2G7 M2PEVp4yOCEQvF2= MUPpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NH\Rd4IzODR6NECxPC=>
MDA-MB-231 NH\P[lFMcW6jc3WgZZN{[Xl? M4XBfp4yOCEQvF2= NGHk[3lqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NHHsXJczODR6NECxPC=>
NCI-H441 MlO5T4lv[XOnIHHzd4F6 NWXaN5J2hjFyIN88US=> MX\pcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MWWyNFQ5PDBzOB?=
SK-MEL-28 M{TZWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFrUdWw{OyEQvF2= Mke5TWM2OD5|MzFOwG0> MUCyNFQ5PDBzOB?=
NCI-H661 NU[0XXVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{e0O|M{KM7:TR?= MkW4TWM2OD5|MzFOwG0> Ml7sNlA1QDRyMUi=
NCI-H446 NHPQcHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEKzTGk{OyEQvF2= M4L3fWlEPTB;NzFOwG0> MoWwNlA1QDRyMUi=
MDA-MB-231 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlO0N|Mh|ryP MmHvTWM2OD1yLkW1JO69VQ>? M37rXVIxPDh2MEG4
DLD-1 M1T0PGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVmzN{DPxE1? NILsPY1KSzVyPUCuOVMh|ryP NUTud5N2OjB2OESwNVg>
A549 MmHRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{TCelM{KM7:TR?= NIq1Wo1KSzVyPUCuOVkh|ryP NXS1RYx6OjB2OESwNVg>
SK-OV-3 MmHLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3KR3c{OyEQvF2= MlL6TWM2OD1yLk[2JO69VQ>? MmDnNlA1QDRyMUi=
NCI-H460 NH3uPYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{\6U|M{KM7:TR?= M3zqd2lEPTB;MD62JO69VQ>? MVOyNFQ5PDBzOB?=
A375 NF\Ie2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUjaXIdlOzNizszN NYflOW9vUUN3ME2wMlQzKM7:TR?= M4nUe|IxPDh2MEG4
NCI-H441 NIfhTnpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MorCN|Mh|ryP MW\JR|UxRTBwMzFOwG0> NXvuWZpOOjB2OESwNVg>
HT29 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFvuR2Y{OyEQvF2= M3vQfWlEPTB;MD60PUDPxE1? MXyyNFQ5PDBzOB?=
MKN-45 M3;Hcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIfnNY4{OyEQvF2= Ml3VTWM2OD1yLkW4JO69VQ>? M1TzbVIxPDh2MEG4
HT29 Ml73RZBweHSxc3nzJIF{e2G7 NH;Hcld,OTBizszN M{fxSZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MlLNNlA1QDRyMUi=
MKN-45 NGjPd2NCeG:ydH;zbZMh[XO|YYm= M4K0b54yOCEQvF2= M3\lS5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NEXD[mczODR6NECxPC=>
MDA-MB-231 MWrBdI9xfG:|aYOgZZN{[Xl? MofqglExKM7:TR?= NELvNmFud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu M3;WbVIxPDh2MEG4
MDA-MB-231/TGL MlX1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4HjUZ4yODBizszN M1HkPGdKPTB;MT6yJO69VQ>? NU\ZdoVIOjJyMke2PVA>
1833/TGL NGXoXI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVX+NVAxKM7:TR?= M3fCWmdKPTB;Mz63JO69VQ>? MoTYNlIxOjd4OUC=
EBC1 NGnFRXdEgXSxdH;4bYPDqGG|c3H5 NF34[2x,OTBizszN NU\TV2JJcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> Ml3zNlM2QTh{N{[=
SNU638 M{TQN2N6fG:2b4jpZ:Kh[XO|YYm= MYf+NVAh|ryP M1\UdolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= M1:3dFI{PTl6Mke2
A549 NEPKclVEgXSxdH;4bYPDqGG|c3H5 M1rmXJ4yOCEQvF2= M2nxeI5wfCCjZn\lZ5Q> MlzsNlM2QTh{N{[=
H460 MXXDfZRwfG:6aXRCpIF{e2G7 MnrjglExKM7:TR?= M1fkTI5wfCCjZn\lZ5Q> NI\tU4EzOzV7OEK3Oi=>
HCC827 MlXIR5l1d3SxeHnjxsBie3OjeR?= NF\KZ|N,OTBizszN NVnNPVR2dm:2IHHm[oVkfA>? NEHlPZIzOzV7OEK3Oi=>
A549 NXvLXnVKTnWwY4Tpc44h[XO|YYm= NYG2dXg2OTBizszN M1rrPYRqe3K3cITzJI1q[3KxdIXieYxm NFHW[Y0zOzV7OEK3Oi=>
EBC1 NIHr[GZHfW6ldHnvckBie3OjeR?= NIT4UJEyOCEQvF2= MnrJ[Il{enWydIOgcYlkem:2dXL1cIU> NV7xTG9zOjN3OUiyO|Y>
H460 MV7GeY5kfGmxbjDhd5NigQ>? MU[xNEDPxE1? Ml3ibY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? MUCyOVMyOzBzMB?=
K562/VCR MVfDfZRwfG:6aXRCpIF{e2G7 M1vzdJ4yOCEQvF2= NUfqN4Z6e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NHXHb2QzPTNzM{CxNC=>
CEM/VBL MVzDfZRwfG:6aXRCpIF{e2G7 NXLqeI9QhjFyIN88US=> M4\nUJNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= M3;MSVI2OzF|MEGw
U266 NV7pUVRsS3m2b4TvfIlkyqCjc4PhfS=> NFjLSph,OyEQvF5CpC=> MmXXTWM2OD1zLkGg{txO M3\EcVI2QDFyMEGz
OPM-2 Mn62R5l1d3SxeHnjxsBie3OjeR?= MVX+N{DPxE4EoB?= NI\v[I9KSzVyPUGuPEDPxE1? M4jkO|I2QDFyMEGz
MM.1S MofJR5l1d3SxeHnjxsBie3OjeR?= NITnPYF,OyEQvF5CpC=> NFvYVmxKSzVyPUGuOkDPxE1? MmHCNlU5OTByMUO=
MM.1R MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWqzJO69VcLi NGrvbnVqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> NXTJeWU5OjV6MUCwNVM>
RPMI-8226 MmXwR5l1d3SxeHnjxsBie3OjeR?= M{D6O54{KM7:TdMg M3TBOGlEPTB;MD65JO69VQ>? NF\6foozPThzMECxNy=>
ANBL-6 MmjUR5l1d3SxeHnjxsBie3OjeR?= NH7ycnIyKM7:TdMg MUfpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MXqyOVgyODBzMx?=
ANLB-6/V10R MV3DfZRwfG:6aXRCpIF{e2G7 M2j1WVEh|ryPwrC= M2LI[Ylv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MV[yOVgyODBzMx?=
KAS-6/1 Ml:wR5l1d3SxeHnjxsBie3OjeR?= NGixZY0yKM7:TdMg NGn0fIhqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NYj0NYx6OjV6MUCwNVM>
KAS-6/V10R NI\tZlVEgXSxdH;4bYPDqGG|c3H5 NUPWS3VROSEQvF5CpC=> MVTpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NXvl[oo6OjV6MUCwNVM>
KAS-6/R10R MXPDfZRwfG:6aXRCpIF{e2G7 MVWxJO69VcLi NIfhVlVqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NEjsRoUzPThzMECxNy=>
8226/S M{HtXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIXo[FU{KM7:TdMg NYOzOIJGcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm MWmyOVgyODBzMx?=
8226/LR-5 M4XhW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHX1W4I{KM7:TdMg NWjLbYNHcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm MUmyOVgyODBzMx?=
Huh7 NUTHeHhGS3m2b4TvfIlkyqCjc4PhfS=> NUXSWpZOhjRwODFOwG3DqA>? NE\OW2FFVVOR NWryfZBLUUN3ME25Mlkhdk1? M2HuWVI3OjV7MkWw
Hep3B NUTkRZpbS3m2b4TvfIlkyqCjc4PhfS=> MmHnglQvQCEQvF5CpC=> NVfjfowyTE2VTx?= MmDpTWM2OD12NEiuO{BvVQ>? NV:wd2dFOjZ{NUmyOVA>
HepG2 MmW1R5l1d3SxeHnjxsBie3OjeR?= MVT+OE45KM7:TdMg NVPlepF2TE2VTx?= M4mxeWlEPTB;MUO5Mlc4KG6P MXyyOlI2QTJ3MB?=
Chang MoLBR5l1d3SxeHnjxsBie3OjeR?= MWf+OE45KM7:TdMg NVPyWoVRTE2VTx?= NX\HRZJMUUN3ME20OFgvPyCwTR?= MYmyOlI2QTJ3MB?=
Huh7 NIDacnZHfW6ldHnvckBie3OjeR?= NE[xXYYyNjZizszNxsA> NV7O[HptTE2VTx?= NV7nXG5t[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= NGr2T5YzPjJ3OUK1NC=>
Hep3B NH3O[lRHfW6ldHnvckBie3OjeR?= M4LTZlEvPiEQvF5CpC=> NES2WW5FVVOR MlfuZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M4Kxb|I3OjV7MkWw
HepG2 NIrYUXhHfW6ldHnvckBie3OjeR?= M4DWTlEvPiEQvF5CpC=> M4TFbGROW09? NHj1Wplk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MoTaNlYzPTl{NUC=
Chang NH7KVphHfW6ldHnvckBie3OjeR?= MYmxMlYh|ryPwrC= NUjwWI1wTE2VTx?= M1HGT4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M4X2cFI3OjV7MkWw
MHCC97L M2r1Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYPoVpRQhjFyIN88US=> NVO0[5NCTE2VTx?= MkLDTWM2OD1|MUWgcm0> NIjQ[nUzPjR3OEm1Ny=>
MHCC97H NIfOUJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2GzTJ4yOCEQvF2= NWr5O5VsTE2VTx?= MUfJR|UxRTN4OPMAjUBvVQ>? Mm\TNlY1PTh7NUO=
Huh7 M{XDcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NITZepB,OTBizszN NYGzZoRjTE2VTx?= NUDZSJhmUUN3ME2yOlUhdk1? NUnkd|FIOjZ2NUi5OVM>
HepG2 MmDYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mlf3glExKM7:TR?= NEL6eYJFVVOR NVL2dYtPUUN3ME2zPVIhdk1? NULnd3FsOjZ2NUi5OVM>
MHCC97L MnnaSpVv[3Srb36gZZN{[Xl? MVqxJO69VcLi NVznOXFUTE2VTx?= NIK4T49qdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MWKyOlQ2QDl3Mx?=
Huh7 NEO2RmJHfW6ldHnvckBie3OjeR?= NYfGPYk3OSEQvF5CpC=> Mo\2SG1UVw>? M3vqXolv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> MlH3NlY1PTh7NUO=
MHCC97L NHn1SllCeG:ydH;zbZMh[XO|YYm= M4fkT|Eh|ryPwrC= M1vwT2ROW09? MmTwbY5lfWOnczDhdI9xfG:|aYO= NF;NW4UzPjR3OEm1Ny=>
Huh7 NIjnVo9CeG:ydH;zbZMh[XO|YYm= NGfEcogyKM7:TdMg NFzF[|JFVVOR MnLwbY5lfWOnczDhdI9xfG:|aYO= MkTDNlY1PTh7NUO=
C3H 10T1/2 mouse fibroblasts Mn7TT4lv[XOnIHHzd4F6 NUG3TGxnOjVizszN MWPEUXNQ M1;2bJJm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> NHzRc2wzODV|NEO0OS=>
H23 NUHqXpJPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnfBNlUh|ryP M1rMS2ROW09? M1LrO5Nq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NYLKd3JOOjB3M{SzOFU>
WM35 NHP4em9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1TtblExKM7:TR?= NG\oTJRFVVOR MWDzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NIrXVZIzODV|NEO0OS=>
NIH 3T3 NV30RZE6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3[5PVExKM7:TR?= NXXQdFQ6TE2VTx?= MWjkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= MnLhNlA2OzR|NEW=
H838 NGDtO|dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYW1W41iOTBizszN NHvvU|BFVVOR MmPw[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MXiyNFU{PDN2NR?=
H1395 NEDCdWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVWxNEDPxE1? MYHEUXNQ NWexO3Ax\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NEHsZ44zODV|NEO0OS=>
Quiescent S2 MlH2T4lv[XOnIHHzd4F6 NXzRZm5pOzBizszN M3\VWmROW09? MlvSZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| M1nxfFIyPTF6OUG1
PC3 NYTUOnBTSXCxcITvd4l{KGG|c3H5 MVSyNEDPxE1? NVfkcoo2TE2VTx?= Ml3BbY5lfWOnczDhdI9xfG:|aYO= MnvFNlE4ODlzM{C=
Du145 MnjGRZBweHSxc3nzJIF{e2G7 MWCyNEDPxE1? MXTEUXNQ NGLIfWhqdmS3Y3XzJIFxd3C2b4Ppdy=> M2PzeFIyPzB7MUOw
LNCaP NUT0bIlESXCxcITvd4l{KGG|c3H5 MVKyNEDPxE1? M4D1NGROW09? M{f0dYlv\HWlZYOgZZBweHSxc3nz NXnhb3ZZOjF5MEmxN|A>
LAPC-4 NXzwN4ZwSXCxcITvd4l{KGG|c3H5 NF7CXFYzOCEQvF2= NUmxRVh5TE2VTx?= MV3pcoR2[2W|IHHwc5B1d3Orcx?= MVOyNVcxQTF|MB?=
LNCaP NEG0d3RHfW6ldHnvckBie3OjeR?= NF;0[lIzOCEQvF2= M1nFOGROW09? NIrnemVl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| MXSyNVcxQTF|MB?=
LAPC-4 NF7wUmJHfW6ldHnvckBie3OjeR?= MYGyNEDPxE1? MkjmSG1UVw>? M1ryOIRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NWrtPWs2OjF5MEmxN|A>
Kasumi-1 M1PQc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGLNdlh,PTBizszN NXrWd3gzTE2VTx?= NGL1NodqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MVWyN|M6ODV|Nh?=
SKNO-1 NXT0cW8yT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYPORXJnhjVyIN88US=> NU\LNmltTE2VTx?= MVjpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MUmyN|M6ODV|Nh?=
Kasumi-1 MYrLbY5ie2ViYYPzZZk> M{[ycZ4yOCEQvF2= NULs[o1STE2VTx?= NHfhdG9z\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MkfyNlM{QTB3M{[=
SKNO-1 M3GxXmtqdmG|ZTDhd5NigQ>? NUW2eZpXhjFyIN88US=> MkG2SG1UVw>? MlGzdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NYDlfIRDOjN|OUC1N|Y>
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NRK-52E MlfzSpVv[3Srb36gZZN{[Xl? NU\s[mo{OTBizszN MW\EUXNQ NWT3bnRjcW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgV3RCXDNiboXjcIVieiC2cnHud4xw[2G2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCWR1[t{tIyNCClb3zsZYdmdiCLVjDhcoQh\mmkcn;u[YN1cW5? NUL4RYpYOjVyOEiwNFI>
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Karpas-299 MofWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHLTfnIyOCEQvF2= NVW1RWc5UUN3ME2yMlk{KM7:TR?= MW[yNFc1ODZ{Mx?=
Ramos-RA1 Mn;GS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUexNEDPxE1? MlfmTWM2OD15LkO1JO69VQ>? NHzVOlEzODd2ME[yNy=>
H1299 MWXLbY5ie2ViYYPzZZk> MmS2NVAh|ryP M1fOO4lvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> M{LQSFIyQTB6NkG2

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[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.
Cell Research:[1]
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  • Cell lines: T29, MKN-45 and MDA-MB-231 cells
  • Concentrations: 0.03-10 μM
  • Incubation Time: 24, 32, and 48 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
  • Formulation: In polyethylene glycol 400/20% Vitamin E tocopheryl polyethylene glycol succinate (60:40) 30 mg/mL
  • Dosages: 200 mg/kg
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (197.6 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

CAS No. 905854-02-6
Storage powder
Synonyms N/A

Bio Calculators

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Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID