Tivantinib (ARQ 197)

For research use only.

Catalog No.S2753

18 publications

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. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. Phase 3.

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Selleck's Tivantinib (ARQ 197) has been cited by 18 publications

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  • 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.

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. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. 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 NHvwe5BMcW6jc3WgZZN{[Xl? NHzFZWJ,OTBizszN MWLpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M3TPTlIxPDh2MEG4
HT29 MoXXT4lv[XOnIHHzd4F6 NXjRS2NEhjFyIN88US=> NYeyfG17cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MYmyNFQ5PDBzOB?=
MDA-MB-231 MX;LbY5ie2ViYYPzZZk> M3LsN54yOCEQvF2= M3zpTYlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= M17IV|IxPDh2MEG4
NCI-H441 Mmr3T4lv[XOnIHHzd4F6 Mmj5glExKM7:TR?= NUDhOWRrcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NWG4eGRmOjB2OESwNVg>
SK-MEL-28 M3iyNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mo\DN|Mh|ryP MorFTWM2OD5|MzFOwG0> NFexbm4zODR6NECxPC=>
NCI-H661 M3j3PGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4PN[|M{KM7:TR?= M2jnVmlEPTB-M{Og{txO NFzwW|UzODR6NECxPC=>
NCI-H446 NVz2bIRpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3[5WFM{KM7:TR?= M2XRXmlEPTB;NzFOwG0> MXWyNFQ5PDBzOB?=
MDA-MB-231 MkHlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3zDRlM{KM7:TR?= M{m2VGlEPTB;MD61OUDPxE1? NG[2eZAzODR6NECxPC=>
DLD-1 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkTyN|Mh|ryP MX7JR|UxRTBwNUOg{txO M{jxT|IxPDh2MEG4
A549 NFjYcGxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPlRoI{OyEQvF2= MojiTWM2OD1yLkW5JO69VQ>? M4PKXFIxPDh2MEG4
SK-OV-3 NIe5NoFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkDlN|Mh|ryP NX3yeoI4UUN3ME2wMlY3KM7:TR?= MX6yNFQ5PDBzOB?=
NCI-H460 MnzWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV20[mREOzNizszN NYW5UFNJUUN3ME2wMlYh|ryP NVy5PGRjOjB2OESwNVg>
A375 NFK3N4VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH\1VlA{OyEQvF2= MkHFTWM2OD1yLkSyJO69VQ>? MkPlNlA1QDRyMUi=
NCI-H441 NFjy[5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYOzN{DPxE1? Mmr6TWM2OD1yLkOg{txO NXy4RZpwOjB2OESwNVg>
HT29 MnvaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGi0dVk{OyEQvF2= NYnwOIJtUUN3ME2wMlQ6KM7:TR?= NUD5WJE3OjB2OESwNVg>
MKN-45 MmDkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWnBcm9UOzNizszN NVvPV4NrUUN3ME2wMlU5KM7:TR?= NI[2SnYzODR6NECxPC=>
HT29 NVzRfnk4SXCxcITvd4l{KGG|c3H5 MXr+NVAh|ryP Mm\xd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MV:yNFQ5PDBzOB?=
MKN-45 NEHQe25CeG:ydH;zbZMh[XO|YYm= NFfUVm5,OTBizszN MmPSd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw Mn\INlA1QDRyMUi=
MDA-MB-231 NWDpcnE6SXCxcITvd4l{KGG|c3H5 M3nWNZ4yOCEQvF2= NFfKPXhud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu MnWxNlA1QDRyMUi=
MDA-MB-231/TGL NHXQcGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUTR[Gc6hjFyMDFOwG0> NIrYNYVIUTVyPUGuNkDPxE1? MlLENlIxOjd4OUC=
1833/TGL MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1HLXp4yODBizszN MUXHTVUxRTNwNzFOwG0> Mnz4NlIxOjd4OUC=
EBC1 NIK2XnVEgXSxdH;4bYPDqGG|c3H5 NUizTo11hjFyIN88US=> NEHMSFRqdmirYnn0d{B1cGViY3XscEBoem:5dHiu MUmyN|U6QDJ5Nh?=
SNU638 NGnKW5hEgXSxdH;4bYPDqGG|c3H5 NGL0c2R,OTBizszN M3SxWolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= M1z3OFI{PTl6Mke2
A549 MoLZR5l1d3SxeHnjxsBie3OjeR?= NV;CfnFnhjFyIN88US=> Ml;xco91KGGoZnXjeC=> NInPSmUzOzV7OEK3Oi=>
H460 Ml3PR5l1d3SxeHnjxsBie3OjeR?= MkXJglExKM7:TR?= NIrTZ5Rvd3RiYX\m[YN1 M2i2blI{PTl6Mke2
HCC827 NWq0R3VOS3m2b4TvfIlkyqCjc4PhfS=> M2PTV54yOCEQvF2= Ml\oco91KGGoZnXjeC=> M{PjcVI{PTl6Mke2
A549 NX3xVog2TnWwY4Tpc44h[XO|YYm= M4K0d|ExKM7:TR?= MU\kbZNzfXC2czDtbYNzd3S3YoXs[S=> M13oU|I{PTl6Mke2
EBC1 MmHtSpVv[3Srb36gZZN{[Xl? MUSxNEDPxE1? Monx[Il{enWydIOgcYlkem:2dXL1cIU> MX:yN|U6QDJ5Nh?=
H460 NYfObWd1TnWwY4Tpc44h[XO|YYm= MWWxNEDPxE1? MUTpcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v Mmq2NlU{OTNyMUC=
K562/VCR NE\TXZJEgXSxdH;4bYPDqGG|c3H5 M2r6UZ4yOCEQvF2= MWLzbI94eyCleYTveI95cWNiYXP0bZZqfHl? Ml63NlU{OTNyMUC=
CEM/VBL MVzDfZRwfG:6aXRCpIF{e2G7 NFLlVFd,OTBizszN NHHrd2N{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= NFz2PXUzPTNzM{CxNC=>
U266 MnzZR5l1d3SxeHnjxsBie3OjeR?= M3e3S54{KM7:TdMg M2fyZ2lEPTB;MT6xJO69VQ>? NH3iRpIzPThzMECxNy=>
OPM-2 M{LTU2N6fG:2b4jpZ:Kh[XO|YYm= NF23[Jl,OyEQvF5CpC=> NUj3O5o4UUN3ME2xMlgh|ryP NYjUN|A{OjV6MUCwNVM>
MM.1S NUj6W45uS3m2b4TvfIlkyqCjc4PhfS=> NILESnd,OyEQvF5CpC=> Ml33TWM2OD1zLk[g{txO NV;OdI5FOjV6MUCwNVM>
MM.1R MnvlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEnkfZo{KM7:TdMg MmW3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml MWiyOVgyODBzMx?=
RPMI-8226 M4fTdGN6fG:2b4jpZ:Kh[XO|YYm= M1PBXp4{KM7:TdMg MlrHTWM2OD1yLkmg{txO NWS5V29POjV6MUCwNVM>
ANBL-6 NG\heHlEgXSxdH;4bYPDqGG|c3H5 M3XlOVEh|ryPwrC= NE\tPXRqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NVe4d5hROjV6MUCwNVM>
ANLB-6/V10R MVzDfZRwfG:6aXRCpIF{e2G7 M4\SSFEh|ryPwrC= NIno[4pqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NGf2S2wzPThzMECxNy=>
KAS-6/1 MXHDfZRwfG:6aXRCpIF{e2G7 M{XkNVEh|ryPwrC= MWnpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NUPkRnY5OjV6MUCwNVM>
KAS-6/V10R M{DqSGN6fG:2b4jpZ:Kh[XO|YYm= M3jyVFEh|ryPwrC= NYqxWYRUcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MV6yOVgyODBzMx?=
KAS-6/R10R NEfETZNEgXSxdH;4bYPDqGG|c3H5 NYXKSmdTOSEQvF5CpC=> NWPSNFNHcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M1W5UFI2QDFyMEGz
8226/S NUC3WFFST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWqzJO69VcLi NEDxVWpqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> M2radFI2QDFyMEGz
8226/LR-5 MkH3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{HwZVMh|ryPwrC= MYHpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= MnjUNlU5OTByMUO=
Huh7 NF7zc4xEgXSxdH;4bYPDqGG|c3H5 M1noUp41NjhizszNxsA> NWPZUlhoTE2VTx?= M{fq[GlEPTB;OT65JI5O M3Pab|I3OjV7MkWw
Hep3B NFvuN3dEgXSxdH;4bYPDqGG|c3H5 MkL1glQvQCEQvF5CpC=> MULEUXNQ NWnjRXk5UUN3ME20OFgvPyCwTR?= Mni4NlYzPTl{NUC=
HepG2 NUXhXXRVS3m2b4TvfIlkyqCjc4PhfS=> MUH+OE45KM7:TdMg MX;EUXNQ MYPJR|UxRTF|OT63O{BvVQ>? NX\GWnE6OjZ{NUmyOVA>
Chang M{W2fWN6fG:2b4jpZ:Kh[XO|YYm= NWj2UnlshjRwODFOwG3DqA>? NEj5dolFVVOR M{PWVmlEPTB;NES4Mlchdk1? M1HlUVI3OjV7MkWw
Huh7 M4qxWWZ2dmO2aX;uJIF{e2G7 NEH5VooyNjZizszNxsA> M2TqXmROW09? MWjjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MXGyOlI2QTJ3MB?=
Hep3B NXXB[4FqTnWwY4Tpc44h[XO|YYm= NFy3R|EyNjZizszNxsA> NHj4N4RFVVOR NFLNT4Fk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MYiyOlI2QTJ3MB?=
HepG2 MVTGeY5kfGmxbjDhd5NigQ>? NH;0NXAyNjZizszNxsA> NFnsSGtFVVOR MXTjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MoftNlYzPTl{NUC=
Chang NVHCZ3dMTnWwY4Tpc44h[XO|YYm= NIDMdJoyNjZizszNxsA> NYHnUGhWTE2VTx?= M1\VW4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NV[zUWV[OjZ{NUmyOVA>
MHCC97L NHq4SmFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF;JcVR,OTBizszN NIOzUnNFVVOR MUXJR|UxRTNzNTDuUS=> MUeyOlQ2QDl3Mx?=
MHCC97H Mk\DS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYKz[WtIhjFyIN88US=> NXTHN49ITE2VTx?= NInneGlKSzVyPUO2PQKBkSCwTR?= M3PUPVI3PDV6OUWz
Huh7 MkjtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH7R[5h,OTBizszN NV3JXow5TE2VTx?= NEfySYpKSzVyPUK2OUBvVQ>? M2jnS|I3PDV6OUWz
HepG2 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXP+NVAh|ryP M1jCbGROW09? NEnXTm1KSzVyPUO5NkBvVQ>? M2Dyb|I3PDV6OUWz
MHCC97L MmG0SpVv[3Srb36gZZN{[Xl? NWPETYNGOSEQvF5CpC=> NXjCboo4TE2VTx?= MWTpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u MmHRNlY1PTh7NUO=
Huh7 M3u0fWZ2dmO2aX;uJIF{e2G7 NW\Tb5FOOSEQvF5CpC=> MUjEUXNQ Mom5bY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> M4HUclI3PDV6OUWz
MHCC97L NUnnXJBCSXCxcITvd4l{KGG|c3H5 NXXBO|N4OSEQvF5CpC=> NVvHUXA{TE2VTx?= MV7pcoR2[2W|IHHwc5B1d3Orcx?= M1XNfVI3PDV6OUWz
Huh7 MUTBdI9xfG:|aYOgZZN{[Xl? MYqxJO69VcLi NWLKN3N4TE2VTx?= M3TyZYlv\HWlZYOgZZBweHSxc3nz NVyyRXdlOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts MYfLbY5ie2ViYYPzZZk> MWqyOUDPxE1? MmHESG1UVw>? NWTB[pIxemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? NVLjPJFFOjB3M{SzOFU>
H23 MoK4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mor6NlUh|ryP NGDYbJJFVVOR Mnzrd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= M1PGclIxPTN2M{S1
WM35 NH7PPJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYSxNEDPxE1? NYK0Vm5yTE2VTx?= MoP2d4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NWDWbZdQOjB3M{SzOFU>
NIH 3T3 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWOxNEDPxE1? M2C0OmROW09? NWHmXoM2\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 M{\sdVIxPTN2M{S1
H838 NWi1SIozT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXPBTFVDOTBizszN MUjEUXNQ NVfzRYw2\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NXKxSHdWOjB3M{SzOFU>
H1395 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmniNVAh|ryP NGH2eVlFVVOR M4n4XoRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NXL3[ZkxOjB3M{SzOFU>
Quiescent S2 M2[xN2tqdmG|ZTDhd5NigQ>? MkDRN|Ah|ryP MUDEUXNQ MV;jc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? Mn7MNlE2OTh7MUW=
PC3 MXvBdI9xfG:|aYOgZZN{[Xl? MkfHNlAh|ryP MVHEUXNQ MUXpcoR2[2W|IHHwc5B1d3Orcx?= NXzFVpNyOjF5MEmxN|A>
Du145 NXTjXGpoSXCxcITvd4l{KGG|c3H5 MlLSNlAh|ryP M3v3emROW09? NFXzOHZqdmS3Y3XzJIFxd3C2b4Ppdy=> MXiyNVcxQTF|MB?=
LNCaP NVnpOFNFSXCxcITvd4l{KGG|c3H5 MUCyNEDPxE1? MV7EUXNQ MmLHbY5lfWOnczDhdI9xfG:|aYO= NEDTU3gzOTdyOUGzNC=>
LAPC-4 Mo\FRZBweHSxc3nzJIF{e2G7 M2fXVFIxKM7:TR?= NXfFOmhJTE2VTx?= M4m2W4lv\HWlZYOgZZBweHSxc3nz Mn3iNlE4ODlzM{C=
LNCaP MonaSpVv[3Srb36gZZN{[Xl? NG\WPVUzOCEQvF2= MXLEUXNQ M3nuUIRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? MX2yNVcxQTF|MB?=
LAPC-4 M2jzU2Z2dmO2aX;uJIF{e2G7 NHrGenAzOCEQvF2= NEP1SlFFVVOR MmDs[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NGTXT2czOTdyOUGzNC=>
Kasumi-1 NGmzXmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVHI[IJRhjVyIN88US=> MnTwSG1UVw>? M{nhVYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MkfSNlM{QTB3M{[=
SKNO-1 MojYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2TNZZ42OCEQvF2= NWHCZW9STE2VTx?= NVnHcGNscW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnrTNlM{QTB3M{[=
Kasumi-1 NEjtXnFMcW6jc3WgZZN{[Xl? MX\+NVAh|ryP NUm0SnpmTE2VTx?= M2HYNpJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> NYPyeXhKOjN|OUC1N|Y>
SKNO-1 MoP3T4lv[XOnIHHzd4F6 NHnmU3V,OTBizszN MlnuSG1UVw>? NGj2Nlhz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MVmyN|M6ODV|Nh?=
A549 NYH5bVRxTnWwY4Tpc44h[XO|YYm= NWnrNXZXOTBizszN MWjEUXNQ NVW5bYNU\W6qYX7j[ZMhdWm2b4TpZ{Bk[XSjc4Tyc5Bp\Q>? MXSyOFc1PjV5NB?=
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Karpas-299 NXy4NnBTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVjQNnRYOTBizszN MkL5TWM2OD1{LkmzJO69VQ>? M4O0OlIxPzRyNkKz
Ramos-RA1 NFP3WHJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnLDNVAh|ryP NX;VNI1{UUN3ME23MlM2KM7:TR?= NFruNo0zODd2ME[yNy=>
H1299 M4G5WmtqdmG|ZTDhd5NigQ>? MmfSNVAh|ryP MnOxbY5pcWKrdIOgTWtDU0VvaX7keYNm\CCDa4SgRYN1cX[jdHnvci=> M{LxdVIyQTB6NkG2

... Click to View More Cell Line Experimental Data

Assay
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
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]
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  • Animal Models: Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
  • 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
in solvent
Synonyms N/A
Smiles O=C1NC(=O)C(C1C2=C[NH]C3=C2C=CC=C3)C4=C[N]5CCCC6=CC=CC4=C56

In vivo Formulation Calculator (Clear solution)

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Clinical Trial Information

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

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.

Handling Instructions

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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.

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID