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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Cited by 6 Publications

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, 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. 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 MYHLbY5ie2ViYYPzZZk> MXT+NVAh|ryP NF3lRplqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NY[zU3RlOjB2OESwNVg>
HT29 NHP6ZpBMcW6jc3WgZZN{[Xl? NEDGSpJ,OTBizszN M{KwTolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NYT0OI9QOjB2OESwNVg>
MDA-MB-231 M{\KVWtqdmG|ZTDhd5NigQ>? NIP1e5Z,OTBizszN M4X2SIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= Mo[zNlA1QDRyMUi=
NCI-H441 M1O4[mtqdmG|ZTDhd5NigQ>? MUT+NVAh|ryP NV:yO49lcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> M3flZ|IxPDh2MEG4
SK-MEL-28 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkfmN|Mh|ryP MXXJR|UxRjN|IN88US=> NWnXeI9oOjB2OESwNVg>
NCI-H661 NXH6dVNlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnuyN|Mh|ryP NYjkd3VRUUN3ME6zN{DPxE1? MWSyNFQ5PDBzOB?=
NCI-H446 NXzp[IE6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkHTN|Mh|ryP M{PqOmlEPTB;NzFOwG0> M{CwUFIxPDh2MEG4
MDA-MB-231 NEnXNWdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEewVZQ{OyEQvF2= NFnQbmdKSzVyPUCuOVUh|ryP MV2yNFQ5PDBzOB?=
DLD-1 NYL3[2ZwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFy4V5o{OyEQvF2= M4LMT2lEPTB;MD61N{DPxE1? MmLWNlA1QDRyMUi=
A549 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEPzTWY{OyEQvF2= NXfuOVVoUUN3ME2wMlU6KM7:TR?= NIHs[YQzODR6NECxPC=>
SK-OV-3 NVexNZh[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NInzWHA{OyEQvF2= MlnJTWM2OD1yLk[2JO69VQ>? NVv0NWtGOjB2OESwNVg>
NCI-H460 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnLTN|Mh|ryP Mn3CTWM2OD1yLk[g{txO NWTPXpBROjB2OESwNVg>
A375 M4XOdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEPzUJo{OyEQvF2= MkCyTWM2OD1yLkSyJO69VQ>? NY\hcpZoOjB2OESwNVg>
NCI-H441 NFv5UlBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3zCflM{KM7:TR?= M13nbmlEPTB;MD6zJO69VQ>? Ml;KNlA1QDRyMUi=
HT29 M1XiRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NITKd4Q{OyEQvF2= M13KTmlEPTB;MD60PUDPxE1? MlHCNlA1QDRyMUi=
MKN-45 NUPJdpFIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFmyRms{OyEQvF2= MV3JR|UxRTBwNUig{txO M3r6cFIxPDh2MEG4
HT29 NHLKb4dCeG:ydH;zbZMh[XO|YYm= MX3+NVAh|ryP M4HWXZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NFXaT3MzODR6NECxPC=>
MKN-45 MVLBdI9xfG:|aYOgZZN{[Xl? NIjUT2R,OTBizszN NUjaZ|Bqe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu MnT1NlA1QDRyMUi=
MDA-MB-231 NHPXTZRCeG:ydH;zbZMh[XO|YYm= NXTJXlVYhjFyIN88US=> MoLlcY9l\XO2bImgbY5lfWOnczDhdI9xfG:|aYOgZpkhOzVnLh?= MnXGNlA1QDRyMUi=
MDA-MB-231/TGL Ml3vS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmPRglExOCEQvF2= NFjIWmpIUTVyPUGuNkDPxE1? M{nVcVIzODJ5Nkmw
1833/TGL M2HYV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2H3TJ4yODBizszN NITFe|VIUTVyPUOuO{DPxE1? MVqyNlAzPzZ7MB?=
EBC1 M3u4dWN6fG:2b4jpZ:Kh[XO|YYm= NHm3eXZ,OTBizszN MlPMbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= M3O5OlI{PTl6Mke2
SNU638 MnWzR5l1d3SxeHnjxsBie3OjeR?= NYnqS5NrhjFyIN88US=> NWGw[XhxcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> NXHkU2FROjN3OUiyO|Y>
A549 MUXDfZRwfG:6aXRCpIF{e2G7 NX7TR|dbhjFyIN88US=> M3TQXI5wfCCjZn\lZ5Q> MkjYNlM2QTh{N{[=
H460 NF3XNWREgXSxdH;4bYPDqGG|c3H5 MVf+NVAh|ryP NX7qWXlwdm:2IHHm[oVkfA>? NXHKUVRzOjN3OUiyO|Y>
HCC827 MWjDfZRwfG:6aXRCpIF{e2G7 NIjCVpN,OTBizszN NHrje2xvd3RiYX\m[YN1 NWPXSYVTOjN3OUiyO|Y>
A549 MUPGeY5kfGmxbjDhd5NigQ>? MV2xNEDPxE1? MUjkbZNzfXC2czDtbYNzd3S3YoXs[S=> NHrGcnQzOzV7OEK3Oi=>
EBC1 M{jGPGZ2dmO2aX;uJIF{e2G7 NWTJSZpVOTBizszN NH\le2xlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? NX;wSZRxOjN3OUiyO|Y>
H460 NXq4RlZvTnWwY4Tpc44h[XO|YYm= MVixNEDPxE1? MlvibY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? NGPFR4IzPTNzM{CxNC=>
K562/VCR NXG3XIx1S3m2b4TvfIlkyqCjc4PhfS=> MYD+NVAh|ryP MXPzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MX[yOVMyOzBzMB?=
CEM/VBL M4rWfWN6fG:2b4jpZ:Kh[XO|YYm= NIXVU2h,OTBizszN NVLVc2tDe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NHLsZ2MzPTNzM{CxNC=>
U266 NFLIO2NEgXSxdH;4bYPDqGG|c3H5 NXnTS4plhjNizszNxsA> MYDJR|UxRTFwMTFOwG0> NUnBXYZyOjV6MUCwNVM>
OPM-2 M1fpUmN6fG:2b4jpZ:Kh[XO|YYm= NE\pSXB,OyEQvF5CpC=> NXrj[443UUN3ME2xMlgh|ryP MWSyOVgyODBzMx?=
MM.1S MXjDfZRwfG:6aXRCpIF{e2G7 NU[yRYlMhjNizszNxsA> NWHzUXQ6UUN3ME2xMlYh|ryP MnywNlU5OTByMUO=
MM.1R M{PCW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3jBN|Mh|ryPwrC= MW\pcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= MnnXNlU5OTByMUO=
RPMI-8226 NFzESHJEgXSxdH;4bYPDqGG|c3H5 M4TEW54{KM7:TdMg NWn3UI9QUUN3ME2wMlkh|ryP M1rmSFI2QDFyMEGz
ANBL-6 NEmzRoJEgXSxdH;4bYPDqGG|c3H5 MW[xJO69VcLi NYnT[oY1cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MonVNlU5OTByMUO=
ANLB-6/V10R NGraTVlEgXSxdH;4bYPDqGG|c3H5 MVmxJO69VcLi NWSyVmtXcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M1\WfFI2QDFyMEGz
KAS-6/1 NWLjSmVTS3m2b4TvfIlkyqCjc4PhfS=> MlnJNUDPxE4EoB?= MkLnbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MkLmNlU5OTByMUO=
KAS-6/V10R MVPDfZRwfG:6aXRCpIF{e2G7 MVWxJO69VcLi NFzUfnlqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NVzPRVZWOjV6MUCwNVM>
KAS-6/R10R MUDDfZRwfG:6aXRCpIF{e2G7 MYqxJO69VcLi NW[1NYQzcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NE\0RpgzPThzMECxNy=>
8226/S M2X4d2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXezJO69VcLi M{jaPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> NU[0ZmlpOjV6MUCwNVM>
8226/LR-5 NWDSbYk4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXSzJO69VcLi MXzpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NIXvTpIzPThzMECxNy=>
Huh7 M4PhUWN6fG:2b4jpZ:Kh[XO|YYm= MUT+OE45KM7:TdMg MXPEUXNQ MlPnTWM2OD17Lkmgcm0> NHHP[pkzPjJ3OUK1NC=>
Hep3B M13TbGN6fG:2b4jpZ:Kh[XO|YYm= Ml76glQvQCEQvF5CpC=> NHvpVYtFVVOR NELydnZKSzVyPUS0PE44KG6P MUSyOlI2QTJ3MB?=
HepG2 M{nDPWN6fG:2b4jpZ:Kh[XO|YYm= MVP+OE45KM7:TdMg NIm3V2tFVVOR M3j1bGlEPTB;MUO5Mlc4KG6P NELPSWgzPjJ3OUK1NC=>
Chang NIrIXIhEgXSxdH;4bYPDqGG|c3H5 NYKzU45NhjRwODFOwG3DqA>? NF;E[|RFVVOR MmLPTWM2OD12NEiuO{BvVQ>? MnyxNlYzPTl{NUC=
Huh7 NIr5dolHfW6ldHnvckBie3OjeR?= MkjZNU43KM7:TdMg M1rUOWROW09? M4n5N4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M4LMUlI3OjV7MkWw
Hep3B MoKwSpVv[3Srb36gZZN{[Xl? M4n2RlEvPiEQvF5CpC=> MXLEUXNQ NGC1dINk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MlniNlYzPTl{NUC=
HepG2 NWC3S|ZoTnWwY4Tpc44h[XO|YYm= M3nadlEvPiEQvF5CpC=> MonBSG1UVw>? M3rre4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M4q5ZlI3OjV7MkWw
Chang MULGeY5kfGmxbjDhd5NigQ>? M1e4WFEvPiEQvF5CpC=> NX;xbHhGTE2VTx?= NELsXW5k[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NILyXZMzPjJ3OUK1NC=>
MHCC97L NIXOcYhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGf4UHh,OTBizszN NEXm[4xFVVOR NV;yTo86UUN3ME2zNVUhdk1? MmOwNlY1PTh7NUO=
MHCC97H NVnPOG1rT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYTqbmoxhjFyIN88US=> MoHhSG1UVw>? NFLXWIRKSzVyPUO2PQKBkSCwTR?= MmLYNlY1PTh7NUO=
Huh7 MnjSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVH+NVAh|ryP NInBTW1FVVOR MkXWTWM2OD1{NkWgcm0> NWrJOYRlOjZ2NUi5OVM>
HepG2 NIq0NoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M372cp4yOCEQvF2= NEXPUFFFVVOR MYfJR|UxRTN7MjDuUS=> M{HpRVI3PDV6OUWz
MHCC97L NYrHSo1uTnWwY4Tpc44h[XO|YYm= Mkn4NUDPxE4EoB?= NFXIWIxFVVOR NV\GbppqcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? M{TEXVI3PDV6OUWz
Huh7 NFe3WZpHfW6ldHnvckBie3OjeR?= NYDHPJhWOSEQvF5CpC=> M1fPTGROW09? NGG1dXdqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MWKyOlQ2QDl3Mx?=
MHCC97L MVzBdI9xfG:|aYOgZZN{[Xl? Ml\iNUDPxE4EoB?= NWO1O3ZQTE2VTx?= MnPvbY5lfWOnczDhdI9xfG:|aYO= NUXKNXp4OjZ2NUi5OVM>
Huh7 MknuRZBweHSxc3nzJIF{e2G7 NIHublgyKM7:TdMg M4TMTWROW09? MXXpcoR2[2W|IHHwc5B1d3Orcx?= M3q2bFI3PDV6OUWz
C3H 10T1/2 mouse fibroblasts MYDLbY5ie2ViYYPzZZk> NU\ZTWlHOjVizszN Ml[1SG1UVw>? MoDydoVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> NUT2VFREOjB3M{SzOFU>
H23 M{nlVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYeyOUDPxE1? M{O2XGROW09? Ml7id4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NVr5[oFzOjB3M{SzOFU>
WM35 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX2xNEDPxE1? MnfOSG1UVw>? MYHzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NWSye2ZOOjB3M{SzOFU>
NIH 3T3 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlzzNVAh|ryP MoOzSG1UVw>? Mmnp[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MkXrNlA2OzR|NEW=
H838 NFPFbpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MofDNVAh|ryP NVOw[21TTE2VTx?= M4TGS4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MWmyNFU{PDN2NR?=
H1395 Mn\ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1rwSVExKM7:TR?= NX;3NohSTE2VTx?= M4exO4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MV2yNFU{PDN2NR?=
Quiescent S2 NHnxUHVMcW6jc3WgZZN{[Xl? MmrQN|Ah|ryP MWrEUXNQ M4THOINwdXCuZYTlcJkh[WK{b3fheIV{KFSVQT3pcoR2[2WmIHj5dIVz[WOndInsZZRqd25ib3[gTFNMPG2nMzDobZN1d26ncx?= Mm\rNlE2OTh7MUW=
PC3 NEfScphCeG:ydH;zbZMh[XO|YYm= MYmyNEDPxE1? M1TnSGROW09? NUHvNGJJcW6mdXPld{BieG:ydH;zbZM> NUXZTmt4OjF5MEmxN|A>
Du145 NIe5SGJCeG:ydH;zbZMh[XO|YYm= NHzsR2czOCEQvF2= M3;Ib2ROW09? M2rtSYlv\HWlZYOgZZBweHSxc3nz NELZOXAzOTdyOUGzNC=>
LNCaP Ml3MRZBweHSxc3nzJIF{e2G7 NYrmUVdUOjBizszN MUfEUXNQ MXzpcoR2[2W|IHHwc5B1d3Orcx?= NGLXd5MzOTdyOUGzNC=>
LAPC-4 MmHYRZBweHSxc3nzJIF{e2G7 Mor2NlAh|ryP MlzkSG1UVw>? M2W4dIlv\HWlZYOgZZBweHSxc3nz NHTwV3UzOTdyOUGzNC=>
LNCaP NGXyXnlHfW6ldHnvckBie3OjeR?= Mlq4NlAh|ryP NFPxS4JFVVOR NI\BXHpl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NGXsRpozOTdyOUGzNC=>
LAPC-4 M1L5ZWZ2dmO2aX;uJIF{e2G7 MnfGNlAh|ryP NX;wNo5oTE2VTx?= NWDvVHJk\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= MofQNlE4ODlzM{C=
Kasumi-1 NF;wcplIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M37qep42OCEQvF2= MnvPSG1UVw>? MYTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MnzoNlM{QTB3M{[=
SKNO-1 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NInCe|J,PTBizszN MmW1SG1UVw>? MU\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MnnONlM{QTB3M{[=
Kasumi-1 NF7BXplMcW6jc3WgZZN{[Xl? NWXIZVBOhjFyIN88US=> NIHBfWpFVVOR MmX2doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y M1qwXVI{OzlyNUO2
SKNO-1 NIHT[HVMcW6jc3WgZZN{[Xl? M3nUUp4yOCEQvF2= NYHFTpp{TE2VTx?= MYTy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NV\QTI1TOjN|OUC1N|Y>
A549 NVPk[Gl2TnWwY4Tpc44h[XO|YYm= M{nRS|ExKM7:TR?= MonYSG1UVw>? NW\Te|VU\W6qYX7j[ZMhdWm2b4TpZ{Bk[XSjc4Tyc5Bp\Q>? M1nKVlI1PzR4NUe0
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... 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]
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  • 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
in solvent
Synonyms N/A

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Clinical Trial Information

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

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