Tivantinib (ARQ 197)

For research use only.

Catalog No.S2753

24 publications

Tivantinib (ARQ 197) Chemical Structure

CAS No. 905854-02-6

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 24 publications

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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 MWDLbY5ie2ViYYPzZZk> NGPOd3l,OTBizszN MWDpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NXTPSGUzOjB2OESwNVg>
HT29 NIWyVZlMcW6jc3WgZZN{[Xl? M1LvTZ4yOCEQvF2= MVrpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M2TyUVIxPDh2MEG4
MDA-MB-231 M3TLb2tqdmG|ZTDhd5NigQ>? MkTlglExKM7:TR?= M2\4V4lvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= Moe5NlA1QDRyMUi=
NCI-H441 NU\3RmtGU2mwYYPlJIF{e2G7 M{HBO54yOCEQvF2= M2i4SIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NYjPdlBOOjB2OESwNVg>
SK-MEL-28 MlPrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWrjO2xOOzNizszN NUCzS5c1UUN3ME6zN{DPxE1? MV6yNFQ5PDBzOB?=
NCI-H661 NWPLOZMzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVSzN{DPxE1? M4CwdWlEPTB-M{Og{txO NFPxUJIzODR6NECxPC=>
NCI-H446 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWDGW4xmOzNizszN MnTWTWM2OD15IN88US=> NXnJd3ZOOjB2OESwNVg>
MDA-MB-231 NXKyV2NPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MonaN|Mh|ryP MWnJR|UxRTBwNUWg{txO M{K4WVIxPDh2MEG4
DLD-1 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1vrfFM{KM7:TR?= MXnJR|UxRTBwNUOg{txO NXrFW|FrOjB2OESwNVg>
A549 NWnBWGFoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLKUXk4OzNizszN M4\ZN2lEPTB;MD61PUDPxE1? MYSyNFQ5PDBzOB?=
SK-OV-3 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXSzN{DPxE1? MnPqTWM2OD1yLk[2JO69VQ>? MnXKNlA1QDRyMUi=
NCI-H460 M2TPdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYizN{DPxE1? M17iUGlEPTB;MD62JO69VQ>? M3zJelIxPDh2MEG4
A375 NVWwWJNyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlftN|Mh|ryP NV\6PY9YUUN3ME2wMlQzKM7:TR?= NF\6TpEzODR6NECxPC=>
NCI-H441 M{Dk[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYKzN{DPxE1? MofaTWM2OD1yLkOg{txO MnTWNlA1QDRyMUi=
HT29 Mk[3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV[zN{DPxE1? MXHJR|UxRTBwNEmg{txO MnLZNlA1QDRyMUi=
MKN-45 NEH5R5VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV60PWtLOzNizszN NU\BVmpHUUN3ME2wMlU5KM7:TR?= NYHNUGFsOjB2OESwNVg>
HT29 NWrlNlNOSXCxcITvd4l{KGG|c3H5 NG\6V3B,OTBizszN MUTzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NXWxN4FtOjB2OESwNVg>
MKN-45 NU\6R4ViSXCxcITvd4l{KGG|c3H5 MVv+NVAh|ryP Mmnqd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MofTNlA1QDRyMUi=
MDA-MB-231 NEewSXdCeG:ydH;zbZMh[XO|YYm= NWjIS2o5hjFyIN88US=> MkHacY9l\XO2bImgbY5lfWOnczDhdI9xfG:|aYOgZpkhOzVnLh?= M1TyOVIxPDh2MEG4
MDA-MB-231/TGL MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWH+NVAxKM7:TR?= MnTpS2k2OD1zLkKg{txO MoK4NlIxOjd4OUC=
1833/TGL NHvQVG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn6wglExOCEQvF2= NXvNT2dzT0l3ME2zMlch|ryP MkXwNlIxOjd4OUC=
EBC1 MXLDfZRwfG:6aXRCpIF{e2G7 NGrXXmN,OTBizszN NVnQ[Gd[cW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> NXywR|RuOjN3OUiyO|Y>
SNU638 NWPDc3ZsS3m2b4TvfIlkyqCjc4PhfS=> NWrVb5FUhjFyIN88US=> MWnpcohq[mm2czD0bIUh[2WubDDndo94fGhw MnyyNlM2QTh{N{[=
A549 MX\DfZRwfG:6aXRCpIF{e2G7 NWewd2E{hjFyIN88US=> NXLNVpVodm:2IHHm[oVkfA>? NXm3UJAyOjN3OUiyO|Y>
H460 M1\BPWN6fG:2b4jpZ:Kh[XO|YYm= MmLiglExKM7:TR?= MX3uc5Qh[W[oZXP0 NV\sW5VOOjN3OUiyO|Y>
HCC827 M2LDOGN6fG:2b4jpZ:Kh[XO|YYm= Moe5glExKM7:TR?= Mo\nco91KGGoZnXjeC=> NILWcFQzOzV7OEK3Oi=>
A549 M3:3[mZ2dmO2aX;uJIF{e2G7 NWezSY5ZOTBizszN Mo[2[Il{enWydIOgcYlkem:2dXL1cIU> MWSyN|U6QDJ5Nh?=
EBC1 NYfCR4xXTnWwY4Tpc44h[XO|YYm= NWrsW2hROTBizszN M2Dte4Rqe3K3cITzJI1q[3KxdIXieYxm MoHyNlM2QTh{N{[=
H460 NEXJVXhHfW6ldHnvckBie3OjeR?= NGXrRWYyOCEQvF2= NV\rVFZycW6qaXLpeJMhfHWkdXzpckBxd2y7bXXybZpifGmxbh?= NXrFPVU2OjV|MUOwNVA>
K562/VCR NFnnOJZEgXSxdH;4bYPDqGG|c3H5 NULnXXVVhjFyIN88US=> MYDzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MYOyOVMyOzBzMB?=
CEM/VBL MmDRR5l1d3SxeHnjxsBie3OjeR?= NWXwVFB1hjFyIN88US=> NFXSPHF{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= Moq0NlU{OTNyMUC=
U266 NVna[4l1S3m2b4TvfIlkyqCjc4PhfS=> NHjH[pR,OyEQvF5CpC=> MmHSTWM2OD1zLkGg{txO NGr3TGUzPThzMECxNy=>
OPM-2 M2fJfWN6fG:2b4jpZ:Kh[XO|YYm= MYD+N{DPxE4EoB?= MVTJR|UxRTFwODFOwG0> NFXZWHozPThzMECxNy=>
MM.1S NUHXVIk5S3m2b4TvfIlkyqCjc4PhfS=> M4HycZ4{KM7:TdMg Ml;JTWM2OD1zLk[g{txO MVqyOVgyODBzMx?=
MM.1R Ml\KS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLsb4ZoOyEQvF5CpC=> MmPmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml NELKT|czPThzMECxNy=>
RPMI-8226 NXntc4FUS3m2b4TvfIlkyqCjc4PhfS=> MmrGglMh|ryPwrC= NH;6[3JKSzVyPUCuPUDPxE1? M33iR|I2QDFyMEGz
ANBL-6 MnnjR5l1d3SxeHnjxsBie3OjeR?= NY\KXI97OSEQvF5CpC=> M4rjWIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M2HCOFI2QDFyMEGz
ANLB-6/V10R NV3MOIppS3m2b4TvfIlkyqCjc4PhfS=> M{TiNlEh|ryPwrC= MlvlbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= M1jDVFI2QDFyMEGz
KAS-6/1 NVLubnQyS3m2b4TvfIlkyqCjc4PhfS=> NVzEcY4xOSEQvF5CpC=> MoXJbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NFLveFYzPThzMECxNy=>
KAS-6/V10R MXrDfZRwfG:6aXRCpIF{e2G7 M4S5UVEh|ryPwrC= NU[0T4p2cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NXO5TodLOjV6MUCwNVM>
KAS-6/R10R NGfKXJdEgXSxdH;4bYPDqGG|c3H5 NEPiRm8yKM7:TdMg M{DEZ4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MnvvNlU5OTByMUO=
8226/S NWnoTHZxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVvG[GxMOyEQvF5CpC=> M1rjPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> Mo[0NlU5OTByMUO=
8226/LR-5 NX[1UpRpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIHDTmU{KM7:TdMg MlG5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl MX:yOVgyODBzMx?=
Huh7 M{fPdWN6fG:2b4jpZ:Kh[XO|YYm= NEnYc|h,PC56IN88UeKh M4f6dmROW09? MlqwTWM2OD17Lkmgcm0> MXGyOlI2QTJ3MB?=
Hep3B M1\kfGN6fG:2b4jpZ:Kh[XO|YYm= MXv+OE45KM7:TdMg NF3uRmNFVVOR NXXodY9ZUUN3ME20OFgvPyCwTR?= MnLGNlYzPTl{NUC=
HepG2 NHPa[3pEgXSxdH;4bYPDqGG|c3H5 MYf+OE45KM7:TdMg MmrISG1UVw>? MUHJR|UxRTF|OT63O{BvVQ>? MoPHNlYzPTl{NUC=
Chang NGT3eotEgXSxdH;4bYPDqGG|c3H5 NYCxfZBYhjRwODFOwG3DqA>? NYjndIdTTE2VTx?= M4\EWmlEPTB;NES4Mlchdk1? M371bFI3OjV7MkWw
Huh7 NUK5NHJkTnWwY4Tpc44h[XO|YYm= M{fFRVEvPiEQvF5CpC=> M2XDUWROW09? MlXVZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M2TNUFI3OjV7MkWw
Hep3B M4i2NWZ2dmO2aX;uJIF{e2G7 M3;XWlEvPiEQvF5CpC=> MnfrSG1UVw>? NXHRNHlC[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= MnXpNlYzPTl{NUC=
HepG2 NGPHNnJHfW6ldHnvckBie3OjeR?= NGnlS|EyNjZizszNxsA> MnvtSG1UVw>? MmTEZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MmPCNlYzPTl{NUC=
Chang M3T5eWZ2dmO2aX;uJIF{e2G7 MXqxMlYh|ryPwrC= Mnv3SG1UVw>? M4LYd4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NGTzNZQzPjJ3OUK1NC=>
MHCC97L MlrNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml3pglExKM7:TR?= MlrpSG1UVw>? MXPJR|UxRTNzNTDuUS=> NYnYSZI{OjZ2NUi5OVM>
MHCC97H NGfOOGpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn\MglExKM7:TR?= M2D6SWROW09? NYXCenJkUUN3ME2zOljjiIlibl2= MU[yOlQ2QDl3Mx?=
Huh7 NHXZT5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MonlglExKM7:TR?= NHjPNWtFVVOR M3Hre2lEPTB;Mk[1JI5O NUK1UWFNOjZ2NUi5OVM>
HepG2 M{e2Xmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHjvToZ,OTBizszN M4\TRmROW09? Mn\yTWM2OD1|OUKgcm0> MYiyOlQ2QDl3Mx?=
MHCC97L MV3GeY5kfGmxbjDhd5NigQ>? NH;kSVUyKM7:TdMg MXvEUXNQ MVnpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u NWDufXRbOjZ2NUi5OVM>
Huh7 NHHQOmpHfW6ldHnvckBie3OjeR?= NV\hTWFbOSEQvF5CpC=> M3e5VGROW09? MVHpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u MoLpNlY1PTh7NUO=
MHCC97L MkPnRZBweHSxc3nzJIF{e2G7 NF7WOGMyKM7:TdMg MWXEUXNQ M{\STYlv\HWlZYOgZZBweHSxc3nz M2TOTVI3PDV6OUWz
Huh7 MUHBdI9xfG:|aYOgZZN{[Xl? NHnPRWcyKM7:TdMg NVGxSWY1TE2VTx?= NGr0TXFqdmS3Y3XzJIFxd3C2b4Ppdy=> M1XCNlI3PDV6OUWz
C3H 10T1/2 mouse fibroblasts MoSyT4lv[XOnIHHzd4F6 M3nGVVI2KM7:TR?= M3u4R2ROW09? MWry[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg MWqyNFU{PDN2NR?=
H23 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXWyOUDPxE1? NXPxUnlnTE2VTx?= MmTJd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= M3:wO|IxPTN2M{S1
WM35 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYGxNEDPxE1? MoLpSG1UVw>? MWPzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MUKyNFU{PDN2NR?=
NIH 3T3 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHzHXHEyOCEQvF2= NILhW|FFVVOR MXnkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= Mlz0NlA2OzR|NEW=
H838 NFnYV3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkjXNVAh|ryP MlfUSG1UVw>? NInhNWNld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NIjHTHkzODV|NEO0OS=>
H1395 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\MN|ExKM7:TR?= MUHEUXNQ M2jhVIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M4LCOFIxPTN2M{S1
Quiescent S2 M2HHXWtqdmG|ZTDhd5NigQ>? MojsN|Ah|ryP NFfIUWZFVVOR NUWydJAx[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz Mo\xNlE2OTh7MUW=
PC3 M{Cw[2Fxd3C2b4Ppd{Bie3OjeR?= MWCyNEDPxE1? MmKzSG1UVw>? MXPpcoR2[2W|IHHwc5B1d3Orcx?= NH7JVnAzOTdyOUGzNC=>
Du145 M1j5NmFxd3C2b4Ppd{Bie3OjeR?= M3PoVlIxKM7:TR?= MUPEUXNQ NVPZUHpxcW6mdXPld{BieG:ydH;zbZM> M1n0[lIyPzB7MUOw
LNCaP NGfkb4lCeG:ydH;zbZMh[XO|YYm= MWKyNEDPxE1? NVj0OmZXTE2VTx?= M{XhbYlv\HWlZYOgZZBweHSxc3nz MmDlNlE4ODlzM{C=
LAPC-4 MlrKRZBweHSxc3nzJIF{e2G7 MXqyNEDPxE1? MkjtSG1UVw>? Mm\EbY5lfWOnczDhdI9xfG:|aYO= NYW4fJpkOjF5MEmxN|A>
LNCaP MVXGeY5kfGmxbjDhd5NigQ>? M3XZfVIxKM7:TR?= NY\kPWpOTE2VTx?= MmKz[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MmHxNlE4ODlzM{C=
LAPC-4 M1ezPGZ2dmO2aX;uJIF{e2G7 NGTJW4ozOCEQvF2= MnnESG1UVw>? MWPk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ NHWx[2kzOTdyOUGzNC=>
Kasumi-1 NU\tTIhsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX\+OVAh|ryP NUHMNoFxTE2VTx?= M1PKfIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NHnLd5MzOzN7MEWzOi=>
SKNO-1 NX3ydopsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLJd3ZXhjVyIN88US=> MWrEUXNQ NEi4emlqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MmTlNlM{QTB3M{[=
Kasumi-1 NVG2VpFpU2mwYYPlJIF{e2G7 NIL6enR,OTBizszN M3fibWROW09? NUHvfY9DemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NYH5fYtiOjN|OUC1N|Y>
SKNO-1 MU\LbY5ie2ViYYPzZZk> M{HZb54yOCEQvF2= MW\EUXNQ MVPy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NV\xN4R6OjN|OUC1N|Y>
A549 MlfPSpVv[3Srb36gZZN{[Xl? MljuNVAh|ryP M2XhNGROW09? Mn3G[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> M3;uelI1PzR4NUe0
NRK-52E MlvDSpVv[3Srb36gZZN{[Xl? M17hfVExKM7:TR?= MlLXSG1UVw>? NUn1SohucW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgV3RCXDNiboXjcIVieiC2cnHud4xw[2G2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCWR1[t{tIyNCClb3zsZYdmdiCLVjDhcoQh\mmkcn;u[YN1cW5? M4HvXFI2ODh6MECy
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... 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 C1CC2=C3C(=CC=C2)C(=CN3C1)C4C(C(=O)NC4=O)C5=CNC6=CC=CC=C65

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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
NCT01755767 Completed Drug: Tivantinib|Drug: Placebo Hepatocellular Carcinoma Daiichi Sankyo Inc.|ArQule December 27 2012 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID