Tivantinib (ARQ 197)

For research use only.

Catalog No.S2753

29 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 29 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 NWj3em1nU2mwYYPlJIF{e2G7 MVX+NVAh|ryP NYHBb4NvcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NGLsNWMzODR6NECxPC=>
HT29 MUXLbY5ie2ViYYPzZZk> MUD+NVAh|ryP NEW3fodqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MVKyNFQ5PDBzOB?=
MDA-MB-231 M17Z[WtqdmG|ZTDhd5NigQ>? NXfsemtxhjFyIN88US=> NXuyUo5ocW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MXuyNFQ5PDBzOB?=
NCI-H441 M4\4OWtqdmG|ZTDhd5NigQ>? MXz+NVAh|ryP MULpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MoGzNlA1QDRyMUi=
SK-MEL-28 MlriS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXSzN{DPxE1? NEHp[45KSzVyPkOzJO69VQ>? M2nCdlIxPDh2MEG4
NCI-H661 M4PjZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXu4UJp3OzNizszN NHvkNJBKSzVyPkOzJO69VQ>? MX:yNFQ5PDBzOB?=
NCI-H446 MmTFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSzN{DPxE1? MoTTTWM2OD15IN88US=> NGrTNVYzODR6NECxPC=>
MDA-MB-231 NVjMXoY3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYSzN{DPxE1? M1rlNWlEPTB;MD61OUDPxE1? NH;rXokzODR6NECxPC=>
DLD-1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXy4b|kzOzNizszN NV7sTGxbUUN3ME2wMlU{KM7:TR?= MlLZNlA1QDRyMUi=
A549 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NW\zNm5WOzNizszN MX\JR|UxRTBwNUmg{txO NULiOW1ZOjB2OESwNVg>
SK-OV-3 NXrRT|g4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVuzN{DPxE1? M1[3WmlEPTB;MD62OkDPxE1? M4TmXlIxPDh2MEG4
NCI-H460 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH[0T|E{OyEQvF2= M3LrVmlEPTB;MD62JO69VQ>? NGfQUmYzODR6NECxPC=>
A375 NGnG[oRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jjSVM{KM7:TR?= NHzWd2hKSzVyPUCuOFIh|ryP NI[4UYgzODR6NECxPC=>
NCI-H441 MoTiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVTxT5NYOzNizszN Mk\ITWM2OD1yLkOg{txO NUDOXHBtOjB2OESwNVg>
HT29 NV7jUGlDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{L2fVM{KM7:TR?= MX3JR|UxRTBwNEmg{txO MVeyNFQ5PDBzOB?=
MKN-45 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmO3N|Mh|ryP MmnFTWM2OD1yLkW4JO69VQ>? MnXvNlA1QDRyMUi=
HT29 NHrp[npCeG:ydH;zbZMh[XO|YYm= NF3FXWV,OTBizszN M1n2NJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NF\TcJAzODR6NECxPC=>
MKN-45 NFz2UZhCeG:ydH;zbZMh[XO|YYm= MoXQglExKM7:TR?= NWfmZlhje2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NVPOTnN{OjB2OESwNVg>
MDA-MB-231 MmfmRZBweHSxc3nzJIF{e2G7 NEXY[Y1,OTBizszN NV7tfZhtdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> M3jLVFIxPDh2MEG4
MDA-MB-231/TGL Ml\LS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLF[mVzhjFyMDFOwG0> MYTHTVUxRTFwMjFOwG0> MXGyNlAzPzZ7MB?=
1833/TGL NVLCem1jT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXr+NVAxKM7:TR?= M{LmbGdKPTB;Mz63JO69VQ>? NF[2XGkzOjB{N{[5NC=>
EBC1 NH3sU4JEgXSxdH;4bYPDqGG|c3H5 NF6ycGp,OTBizszN M{\Fc4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= MWWyN|U6QDJ5Nh?=
SNU638 NVnieHZLS3m2b4TvfIlkyqCjc4PhfS=> M1;yVZ4yOCEQvF2= M1zvSolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NWq3PJY6OjN3OUiyO|Y>
A549 NVP5bFNPS3m2b4TvfIlkyqCjc4PhfS=> NVS4[IRwhjFyIN88US=> Mn;uco91KGGoZnXjeC=> M2riS|I{PTl6Mke2
H460 NVnZSmtwS3m2b4TvfIlkyqCjc4PhfS=> M4PlWJ4yOCEQvF2= MX3uc5Qh[W[oZXP0 NUPY[WllOjN3OUiyO|Y>
HCC827 NWTEVJhmS3m2b4TvfIlkyqCjc4PhfS=> MWD+NVAh|ryP MWDuc5Qh[W[oZXP0 NIe0R|AzOzV7OEK3Oi=>
A549 MY\GeY5kfGmxbjDhd5NigQ>? NHXtZm4yOCEQvF2= NVvyfYhL\Gm|coXweJMhdWmlcn;0eYJ2dGV? MVKyN|U6QDJ5Nh?=
EBC1 M{WzV2Z2dmO2aX;uJIF{e2G7 MW[xNEDPxE1? Mn;t[Il{enWydIOgcYlkem:2dXL1cIU> Ml;kNlM2QTh{N{[=
H460 NW\Me2xETnWwY4Tpc44h[XO|YYm= Ml;2NVAh|ryP M1fIOYlvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? MkXINlU{OTNyMUC=
K562/VCR MWLDfZRwfG:6aXRCpIF{e2G7 M3:4bZ4yOCEQvF2= NG\EW5J{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= NXPDeI4xOjV|MUOwNVA>
CEM/VBL Mlr0R5l1d3SxeHnjxsBie3OjeR?= MX3+NVAh|ryP MoX6d4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 NIXpOWEzPTNzM{CxNC=>
U266 Mm\wR5l1d3SxeHnjxsBie3OjeR?= MkXVglMh|ryPwrC= NVzCPWhHUUN3ME2xMlEh|ryP MV[yOVgyODBzMx?=
OPM-2 NGrWVHpEgXSxdH;4bYPDqGG|c3H5 NEnrSWl,OyEQvF5CpC=> MYXJR|UxRTFwODFOwG0> NUfWXYVWOjV6MUCwNVM>
MM.1S NHv1TmdEgXSxdH;4bYPDqGG|c3H5 NFTTXpF,OyEQvF5CpC=> M{T2TGlEPTB;MT62JO69VQ>? MX:yOVgyODBzMx?=
MM.1R NVn4fYNmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoW2N{DPxE4EoB?= Ml3obY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml NIPTV|MzPThzMECxNy=>
RPMI-8226 NFzZUFVEgXSxdH;4bYPDqGG|c3H5 MWX+N{DPxE4EoB?= NIDCO5ZKSzVyPUCuPUDPxE1? NYX2TWh6OjV6MUCwNVM>
ANBL-6 NGT0e2JEgXSxdH;4bYPDqGG|c3H5 M4mzOVEh|ryPwrC= NFPidIRqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M3y3XVI2QDFyMEGz
ANLB-6/V10R Mke4R5l1d3SxeHnjxsBie3OjeR?= NEHYXI4yKM7:TdMg M1rFW4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MXKyOVgyODBzMx?=
KAS-6/1 MmCxR5l1d3SxeHnjxsBie3OjeR?= MlvPNUDPxE4EoB?= NGXle25qdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NEK1fo4zPThzMECxNy=>
KAS-6/V10R MoH1R5l1d3SxeHnjxsBie3OjeR?= NIjRRpkyKM7:TdMg NXLVTo9FcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NHXMV5IzPThzMECxNy=>
KAS-6/R10R M2\0e2N6fG:2b4jpZ:Kh[XO|YYm= Mlj2NUDPxE4EoB?= MX;pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NHHCdHYzPThzMECxNy=>
8226/S MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NETTPFI{KM7:TdMg M13id4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> M1zlW|I2QDFyMEGz
8226/LR-5 M4\tV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NELkTJE{KM7:TdMg M2DRZolvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MnHwNlU5OTByMUO=
Huh7 MUXDfZRwfG:6aXRCpIF{e2G7 NVGzbYJNhjRwODFOwG3DqA>? NInLfIFFVVOR MWTJR|UxRTlwOTDuUS=> NXnLWFdZOjZ{NUmyOVA>
Hep3B NUL2b3U1S3m2b4TvfIlkyqCjc4PhfS=> MUj+OE45KM7:TdMg MnHLSG1UVw>? M1LEUGlEPTB;NES4Mlchdk1? NV\DTIR7OjZ{NUmyOVA>
HepG2 NWTPPHlGS3m2b4TvfIlkyqCjc4PhfS=> MVH+OE45KM7:TdMg MV7EUXNQ NYnSPJBuUUN3ME2xN|kvPzdibl2= MXSyOlI2QTJ3MB?=
Chang NVzQb|NUS3m2b4TvfIlkyqCjc4PhfS=> MmGzglQvQCEQvF5CpC=> MnvKSG1UVw>? NYS0OZJwUUN3ME20OFgvPyCwTR?= NVK2RpU2OjZ{NUmyOVA>
Huh7 MUPGeY5kfGmxbjDhd5NigQ>? MVmxMlYh|ryPwrC= MVfEUXNQ MnzHZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MWWyOlI2QTJ3MB?=
Hep3B M36ybGZ2dmO2aX;uJIF{e2G7 MkTWNU43KM7:TdMg NHjnRmlFVVOR MkLzZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MmXiNlYzPTl{NUC=
HepG2 M3zYe2Z2dmO2aX;uJIF{e2G7 MV[xMlYh|ryPwrC= NEDpWG1FVVOR MYLjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M3fnSFI3OjV7MkWw
Chang NVjYNGJlTnWwY4Tpc44h[XO|YYm= M1XUdFEvPiEQvF5CpC=> NG\jW5hFVVOR NFvxUm1k[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MXSyOlI2QTJ3MB?=
MHCC97L NGHhe2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXvZNHpIhjFyIN88US=> MYLEUXNQ MUTJR|UxRTNzNTDuUS=> MorXNlY1PTh7NUO=
MHCC97H M4nue2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MljHglExKM7:TR?= MWTEUXNQ NFi1N4ZKSzVyPUO2PQKBkSCwTR?= MWCyOlQ2QDl3Mx?=
Huh7 M1HHUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEe4SZF,OTBizszN NUPieYFjTE2VTx?= NVrwVWNOUUN3ME2yOlUhdk1? NHPTXFUzPjR3OEm1Ny=>
HepG2 NGnnW3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGHYSoR,OTBizszN M2HlVWROW09? M1Tkd2lEPTB;M{myJI5O NX7LXlQ5OjZ2NUi5OVM>
MHCC97L M1LyPGZ2dmO2aX;uJIF{e2G7 NEf2TmcyKM7:TdMg NVvGTWF7TE2VTx?= M4DUZYlv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NIC1[HIzPjR3OEm1Ny=>
Huh7 M4jPUmZ2dmO2aX;uJIF{e2G7 MlL6NUDPxE4EoB?= MnzzSG1UVw>? M3Pi[4lv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NFv4N2kzPjR3OEm1Ny=>
MHCC97L MVHBdI9xfG:|aYOgZZN{[Xl? MVixJO69VcLi NIPKOVRFVVOR NIPyenVqdmS3Y3XzJIFxd3C2b4Ppdy=> MmHQNlY1PTh7NUO=
Huh7 MknyRZBweHSxc3nzJIF{e2G7 NEP1[HYyKM7:TdMg NELiPVJFVVOR M4P0fYlv\HWlZYOgZZBweHSxc3nz NUfNboU{OjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts MmfiT4lv[XOnIHHzd4F6 NGjHVnAzPSEQvF2= MYXEUXNQ NG\qfmpz\WS3Y3XzJGhqe3SxbnWgTFMh[W6mIFi0JIFk\XS7bHH0bY9vKGyndnXsd:Kh MnLMNlA2OzR|NEW=
H23 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2LHbVI2KM7:TR?= MXXEUXNQ M4HEPJNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MVWyNFU{PDN2NR?=
WM35 MonLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnnhNVAh|ryP M4XEW2ROW09? M1TmRZNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MUOyNFU{PDN2NR?=
NIH 3T3 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXzQUJoxOTBizszN Ml;BSG1UVw>? M{fxdIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MnLnNlA2OzR|NEW=
H838 MoHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1W3VlExKM7:TR?= NVHXOYdUTE2VTx?= M2TaRoRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M4i0VlIxPTN2M{S1
H1395 MmjVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXHDSVdXOTBizszN NEHOS3FFVVOR MoLv[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NHHU[mkzODV|NEO0OS=>
Quiescent S2 NUn5XpNGU2mwYYPlJIF{e2G7 MmDxN|Ah|ryP M33ZO2ROW09? NFPie41kd22ybHX0[Yx6KGGkcn;nZZRmeyCWU1GtbY5lfWOnZDDofZBmemGlZYT5cIF1cW:wIH;mJGg{UzSvZUOgbIl{fG:wZYO= NX3qV5I3OjF3MUi5NVU>
PC3 M4XpfmFxd3C2b4Ppd{Bie3OjeR?= MV:yNEDPxE1? NULNdIlnTE2VTx?= MX\pcoR2[2W|IHHwc5B1d3Orcx?= MUCyNVcxQTF|MB?=
Du145 NIDEWlZCeG:ydH;zbZMh[XO|YYm= NX7MZXhmOjBizszN MlLySG1UVw>? M1mxVolv\HWlZYOgZZBweHSxc3nz NEHtcJUzOTdyOUGzNC=>
LNCaP NUToXZA5SXCxcITvd4l{KGG|c3H5 M1;vbVIxKM7:TR?= NYrhUXpjTE2VTx?= MWTpcoR2[2W|IHHwc5B1d3Orcx?= Ml7iNlE4ODlzM{C=
LAPC-4 MYHBdI9xfG:|aYOgZZN{[Xl? Mk\XNlAh|ryP NUHkSXdETE2VTx?= M1PHZolv\HWlZYOgZZBweHSxc3nz MkKxNlE4ODlzM{C=
LNCaP Ml\iSpVv[3Srb36gZZN{[Xl? MWOyNEDPxE1? NUDoOGxETE2VTx?= NFyzOmNl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NUPNNHVPOjF5MEmxN|A>
LAPC-4 MmXBSpVv[3Srb36gZZN{[Xl? MmPpNlAh|ryP M1XLfWROW09? NWKyUYVF\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= MYWyNVcxQTF|MB?=
Kasumi-1 NXnoNY43T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV3SWJp7hjVyIN88US=> NYHGfXZsTE2VTx?= MXvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MnrYNlM{QTB3M{[=
SKNO-1 MkPSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWTrclN2hjVyIN88US=> NFn1RodFVVOR MUDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MYCyN|M6ODV|Nh?=
Kasumi-1 MkjVT4lv[XOnIHHzd4F6 NHnTSGZ,OTBizszN NEDX[GJFVVOR NGXxU3Fz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MYKyN|M6ODV|Nh?=
SKNO-1 NWTOXIZ6U2mwYYPlJIF{e2G7 MUH+NVAh|ryP NYXQSFJCTE2VTx?= NWrZR5ZYemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NFryTngzOzN7MEWzOi=>
A549 MV;GeY5kfGmxbjDhd5NigQ>? NHHSS28yOCEQvF2= NV7rfld5TE2VTx?= Mlza[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> MXOyOFc1PjV5NB?=
NRK-52E MlfCSpVv[3Srb36gZZN{[Xl? MlLMNVAh|ryP NYnwfnNKTE2VTx?= M17YXIlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv NFrqT|gzPTB6OECwNi=>
PC12 NFS3OI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXHyPII2hjF{LkWg{txO MnvBSG1UVw>? NYLuOWlReHKndnXueJMhXFODLXnu[JVk\WRibnX1dol1\SCob4LtZZRqd25? M1vO[|I2OTJ6M{i2
HPMCs MU\GeY5kfGmxbjDhd5NigQ>? MX;y[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> M4q2R|I3ODR3N{iw
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DU145 NFPPOXlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF74T|QyOCEQvF2= NYHLb|Q2TE2VTx?= M1j6R2lEPTB;M{ixNkBvVQ>? MlPiNVg{QDF2NES=
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BT474 NEjRPIdMcW6jc3WgZZN{[Xl? NWDkUYRCOTBizszN MX\EUXNQ NFTL[WlqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNkCgcm0> NVnkV4dtOTh|OEG0OFQ>
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PC3 NV[0boZpU2mwYYPlJIF{e2G7 NGrOfXMyOCEQvF2= NH7GVotFVVOR MWTpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1QSCwTR?= MVmxPFM5OTR2NB?=
KARPAS-231 MnzhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYXLPFc5OTBizszN M{myNWROW09? NH\QcHhGSzVyPUSxJI5O Ml;RNVkxPjR5M{C=
CCRFSB NI\iTmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWLu[lFCOTBizszN NFvLWWdFVVOR M{T1cWVEPTB;MUW1JI5O NHfpdo0yQTB4NEezNC=>
SUP B15 NF\MWIJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV6xNEDPxE1? NHzhZ|JFVVOR M1;k[mVEPTB;MUm3JI5O NFHx[FcyQTB4NEezNC=>
SD-1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4nxeVExKM7:TR?= MUHEUXNQ M3vueGVEPTB;M{KwJI5O NFvkR5EyQTB4NEezNC=>
RS4;11 M3z4OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHXZcYUyOCEQvF2= M4rIe2ROW09? MXXFR|UxRTZ3NDDuUS=> NWLxVVQ3OTlyNkS3N|A>
MN-60 Mkm1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXf6dWdPOTBizszN MYnEUXNQ MVfFR|UxRTN4MEKgcm0> NYq4cnZOOTlyNkS3N|A>
Tanoue M1jUV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3y2NlExKM7:TR?= MkLKSG1UVw>? Mn\LSWM2OD12NUG3JI5O M1vSbFE6ODZ2N{Ow
RCH-ACV MnvVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M33PNVExKM7:TR?= NUPHVGE3TE2VTx?= MX\FR|UxRTF3MjDuUS=> MWWxPVA3PDd|MB?=
SEM NEHEW|ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX2xNEDPxE1? MWjEUXNQ M2q4TGVEPTB;MkCyJI5O MVKxPVA3PDd|MB?=
KASUMI-2 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkXnNVAh|ryP NHv3UnhFVVOR MVPFR|UxRTJ{NTDuUS=> NI\KU|cyQTB4NEezNC=>
REH M1zROmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm\jNVAh|ryP M3LWWWROW09? MkjqSWM2OD1{OEigcm0> MUGxPVA3PDd|MB?=
697 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Moe1NVAh|ryP NWiyXXZOTE2VTx?= M{O0[WVEPTB;M{O4JI5O NWrFRW9SOTlyNkS3N|A>
NALM-6 M1LKVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkTENVAh|ryP NITUd5RFVVOR NH7MZYhGSzVyPUSyNUBvVQ>? M3i5WVE6ODZ2N{Ow
MHH-CALL–3 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mmf0NVAh|ryP Mkf1SG1UVw>? NEjZd3RGSzVyPUixNkBvVQ>? NXjLd|A{OTlyNkS3N|A>
MHH-CALL–2 NVfPeoZ7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlzaNVAh|ryP M1T4O2ROW09? NVfo[YdzTUN3ME2yNVE1KG6P NUfreHBDOTlyNkS3N|A>
J.GAMMA-1 MlnaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH22N2UyOCEQvF2= M1fKWWROW09? NGXLSmdGSzVyPU[1JI5O MnLDNVkxPjR5M{C=
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A3 NHvIZZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4DkNVExKM7:TR?= Ml\6SG1UVw>? M4rQSmVEPTB;Nkmgcm0> M3rCR|E6ODZ2N{Ow
I 2.1 NXXOTYNvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1jkVFExKM7:TR?= NI\2bmtFVVOR M1uybGVEPTB;N{Ogcm0> NETXOHIyQTB4NEezNC=>
MOLT-3 NXvsSmFmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFjVVVYyOCEQvF2= MVjEUXNQ Mk\qSWM2OD15NDDuUS=> NF3qcJMyQTB4NEezNC=>
P116 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHnpdHoyOCEQvF2= M3SyVWROW09? NV:0U|dUTUN3ME23PEBvVQ>? MnHHNVkxPjR5M{C=
J.Cam1.6 Ml7CS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGjtTWgyOCEQvF2= M{fVbWROW09? NVrX[FBDTUN3ME23PUBvVQ>? MY[xPVA3PDd|MB?=
I 9.2 M1LCSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEDYVnEyOCEQvF2= NGLUbI9FVVOR MWrFR|UxRThyIH7N MkTnNVkxPjR5M{C=
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J.RT3-T3.5 NWi4WGF3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYSxNEDPxE1? NIjxWGlFVVOR MW\FR|UxRTF{MzDuUS=> NYfnZnV7OTlyNkS3N|A>
800000 M2O3fWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlfaNVAh|ryP NFzRSYVFVVOR NEjtdGJGSzVyPUG2N{BvVQ>? NGHESWIyQTB4NEezNC=>
Jurkat NXX4XGRKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWSxNEDPxE1? NXPpc3ZNTE2VTx?= M1q2cGVEPTB;MkK1JI5O M2nye|E6ODZ2N{Ow
MOLT-4 NGX1em9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWPhTnh2OTBizszN NVjLW5pZTE2VTx?= NYmzWVdnTUN3ME2yN|Ihdk1? MXixPVA3PDd|MB?=
Molt-16 NFTFWmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVzKcYQ3OTBizszN Mk\hSG1UVw>? NGrpd5JGSzVyPUK0NUBvVQ>? Ml21NVkxPjR5M{C=
CEM/C3 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NE\Uco0yOCEQvF2= NG[4WGhFVVOR M1;vZmVEPTB;MkW3JI5O MVqxPVA3PDd|MB?=
CEM/C2 MlfYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4XBWVExKM7:TR?= NU[zfFBWTE2VTx?= NVPKcW41TUN3ME2yO|Ehdk1? M17uSlE6ODZ2N{Ow
CCRFCEM NW\t[Gx1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIPHNIUyOCEQvF2= NFniTHVFVVOR NX\Xe3hWTUN3ME2zNlchdk1? M1;OVVE6ODZ2N{Ow
CEM/C1 Mnq5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1i4V|ExKM7:TR?= MXrEUXNQ NWjaRW8{TUN3ME2zPFIhdk1? MUixPVA3PDd|MB?=
SUPTI[VB] MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWjWZ|E3OTBizszN Mkn1SG1UVw>? NIDkdHBGSzVyPU[xPUBvVQ>? M2HCPFE6ODZ2N{Ow
CCRF–HSB-2 MmLaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXrSbXR6OTBizszN NUXtbYVWTE2VTx?= NVHFOFFnTUN3ME2yNVE4KG6P NFvTXWEyQTB4NEezNC=>
I 2.1 MkTpRZBweHSxc3nzJIF{e2G7 MXqxNEDPxE1? MXXEUXNQ MlKwbY5lfWOnczDhdI9xfG:|aYO= NUKzZ2xjOTlyNkS3N|A>
I 9.2 NFjYR|dCeG:ydH;zbZMh[XO|YYm= NUK5VWprOTBizszN MkLuSG1UVw>? MWnpcoR2[2W|IHHwc5B1d3Orcx?= NYexPGxCOTlyNkS3N|A>
A3 NFPlO5BCeG:ydH;zbZMh[XO|YYm= MXWxNEDPxE1? NVrFTJNZTE2VTx?= MlnzbY5lfWOnczDhdI9xfG:|aYO= NIX5[4gyQTB4NEezNC=>
RD NHPWWXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEf6b|kyOCEQvF2= M{nieGlEPTB-MUCg{txO NV21WpFmOjB5NEC2NlM>
Rh41 M3\QR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVjWRnpCOTBizszN MXjJR|UxRTN|Lkigcm0> NGjQUVQzODd2ME[yNy=>
Rh18 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1v5[VExKM7:TR?= Mor6TWM2OD1|MEOgcm0> NVr6V2VYOjB5NEC2NlM>
Rh30 NGOyeGNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkTmNVAh|ryP NGCyNVhKSzVyPUSuPFEh|ryP MmTINlA4PDB4MkO=
BT-12 M1LINWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW[xNEDPxE1? M2O1RWlEPTB-MUCg{txO M2HYNlIxPzRyNkKz
CHLA-266 M17BO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkH5NVAh|ryP NUnqUmQ4UUN3ME2xMlIzKM7:TR?= MknENlA4PDB4MkO=
TC-71 MlTpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknVNVAh|ryP MXfJR|UxRTJwNUKg{txO NX;NNmx3OjB5NEC2NlM>
CHLA-9 MoXES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGDDfYUyOCEQvF2= MVXJR|UxRTV7MTDuUS=> NWLlRmFrOjB5NEC2NlM>
CHLA-10 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUHCd5dXOTBizszN MkK2TWM2OD1zMEKgcm0> M3f5[|IxPzRyNkKz
CHLA-258 NHnmO3BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVf4S2xwOTBizszN NV\oPVQ6UUN3ME2xMlA2KM7:TR?= NFXkRlIzODd2ME[yNy=>
GBM2 NUDHNZhtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmHkNVAh|ryP MYXJR|UxRTlwMUWg{txO NGi3b5czODd2ME[yNy=>
NB-1643 NHj4WnJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWqxNEDPxE1? NUKzR4JDUUN3ME21MlQh|ryP MVWyNFc1ODZ{Mx?=
NB-Ebc1 Mk\FS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU[xNEDPxE1? NIG5UGFKSzVyPkGwJO69VQ>? MkXVNlA4PDB4MkO=
CHLA-90 MnLDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1Xp[lExKM7:TR?= NWXyT3p3UUN3ME6xNEDPxE1? NHzEdmszODd2ME[yNy=>
CHLA-136 MlfJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnexNVAh|ryP NHzXOGpKSzVyPkGwJO69VQ>? NV;YNYkxOjB5NEC2NlM>
NALM-6 MmDlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnjxNVAh|ryP MlzVTWM2OD1{NkWgcm0> Mm[0NlA4PDB4MkO=
COG-LL-317 Mn6yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4fzfVExKM7:TR?= NHrXe4ZKSzVyPU[uOFkhdk1? MkHKNlA4PDB4MkO=
RS4;11 MnfPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV\GfXIzOTBizszN MWPJR|UxRTF2NzDuUS=> MYqyNFc1ODZ{Mx?=
MOLT-4 NIPzZm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWnpbnR7OTBizszN M{DTcWlEPTB;NECgcm0> MnzTNlA4PDB4MkO=
CCRF-CEM MnTwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVrVVlNzOTBizszN NHr6eItKSzVyPUK2PEBvVQ>? M330OlIxPzRyNkKz
Kasumi-1 M3\qPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkSxNVAh|ryP NVnCbYg6UUN3ME2xNFchdk1? NXjWSnoxOjB5NEC2NlM>
Karpas-299 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4TRNFExKM7:TR?= MmDrTWM2OD1{LkmzJO69VQ>? NFTnNVMzODd2ME[yNy=>
Ramos-RA1 M13pSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIrNd2syOCEQvF2= NHzNOIhKSzVyPUeuN|Uh|ryP NIHVXIczODd2ME[yNy=>
H1299 NF31ZXJMcW6jc3WgZZN{[Xl? MX[xNEDPxE1? MXPpcohq[mm2czDJT2JMTS2rbnT1Z4VlKEGtdDDBZ5RqfmG2aX;u M2nudFIyQTB6NkG2

... 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID