Tivantinib (ARQ 197)

For research use only.

Catalog No.S2753

32 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 32 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 NH3iTFBMcW6jc3WgZZN{[Xl? MnuyglExKM7:TR?= M2XWWYlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MmPJNlA1QDRyMUi=
HT29 MUHLbY5ie2ViYYPzZZk> NIO5fI5,OTBizszN MVrpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MXiyNFQ5PDBzOB?=
MDA-MB-231 M{TKUGtqdmG|ZTDhd5NigQ>? MXT+NVAh|ryP MVTpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MmfyNlA1QDRyMUi=
NCI-H441 M1PPWGtqdmG|ZTDhd5NigQ>? NHn0fZN,OTBizszN Ml;FbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MVqyNFQ5PDBzOB?=
SK-MEL-28 NEPlRYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWDkT4pWOzNizszN NYHYUFJwUUN3ME6zN{DPxE1? M1LhS|IxPDh2MEG4
NCI-H661 NFP6SlBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NE\xNYg{OyEQvF2= MWHJR|UxRjN|IN88US=> NX;0c2lFOjB2OESwNVg>
NCI-H446 M3juNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MonDN|Mh|ryP MW\JR|UxRTdizszN M3LhUFIxPDh2MEG4
MDA-MB-231 NVT3SHAxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUOzN{DPxE1? MYPJR|UxRTBwNUWg{txO MV2yNFQ5PDBzOB?=
DLD-1 MkDRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkjmN|Mh|ryP Mlq0TWM2OD1yLkWzJO69VQ>? MYKyNFQ5PDBzOB?=
A549 NUjYPWxpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmLMN|Mh|ryP NF\NeVVKSzVyPUCuOVkh|ryP NYHYNndKOjB2OESwNVg>
SK-OV-3 Mlf1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVizN{DPxE1? NVr2[WFJUUN3ME2wMlY3KM7:TR?= MnPTNlA1QDRyMUi=
NCI-H460 MnHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIjKfo0{OyEQvF2= NV7JXG1oUUN3ME2wMlYh|ryP MXeyNFQ5PDBzOB?=
A375 M{PmWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrKNGZjOzNizszN NILIR2VKSzVyPUCuOFIh|ryP NX;QdoNQOjB2OESwNVg>
NCI-H441 MojxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPhN|Mh|ryP NUe0[GxNUUN3ME2wMlMh|ryP NGjNPGozODR6NECxPC=>
HT29 NF;hW2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXyzN{DPxE1? NX\FTItMUUN3ME2wMlQ6KM7:TR?= NX;k[JlROjB2OESwNVg>
MKN-45 MmPBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mnn5N|Mh|ryP MkTNTWM2OD1yLkW4JO69VQ>? MXWyNFQ5PDBzOB?=
HT29 NWXlUJdySXCxcITvd4l{KGG|c3H5 M1nafp4yOCEQvF2= MWjzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NGPxNIczODR6NECxPC=>
MKN-45 Mn:1RZBweHSxc3nzJIF{e2G7 NYX5UJB4hjFyIN88US=> NF\OR3F{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= M3TFW|IxPDh2MEG4
MDA-MB-231 Mn7VRZBweHSxc3nzJIF{e2G7 M4TjN54yOCEQvF2= NEfsZndud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu MmPoNlA1QDRyMUi=
MDA-MB-231/TGL M1X6fWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkL2glExOCEQvF2= MWrHTVUxRTFwMjFOwG0> NGfxc40zOjB{N{[5NC=>
1833/TGL NIfxSndIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mm\rglExOCEQvF2= NVfCN4NKT0l3ME2zMlch|ryP NInTUZAzOjB{N{[5NC=>
EBC1 NWDaSI9tS3m2b4TvfIlkyqCjc4PhfS=> MVr+NVAh|ryP MWXpcohq[mm2czD0bIUh[2WubDDndo94fGhw MofhNlM2QTh{N{[=
SNU638 NYTTe5E2S3m2b4TvfIlkyqCjc4PhfS=> NHz5VmR,OTBizszN Mk\lbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= MXmyN|U6QDJ5Nh?=
A549 M4nyO2N6fG:2b4jpZ:Kh[XO|YYm= NYixe5RLhjFyIN88US=> M3TGWY5wfCCjZn\lZ5Q> MlO1NlM2QTh{N{[=
H460 MnnRR5l1d3SxeHnjxsBie3OjeR?= NIDQNG5,OTBizszN NIe2XI1vd3RiYX\m[YN1 NIXyUZgzOzV7OEK3Oi=>
HCC827 NVjQeIk3S3m2b4TvfIlkyqCjc4PhfS=> M3;ZVJ4yOCEQvF2= MYruc5Qh[W[oZXP0 M3LEPFI{PTl6Mke2
A549 M33tV2Z2dmO2aX;uJIF{e2G7 Mnz5NVAh|ryP M3:yN4Rqe3K3cITzJI1q[3KxdIXieYxm NHjOcWIzOzV7OEK3Oi=>
EBC1 NFHpd5VHfW6ldHnvckBie3OjeR?= NGLGXW4yOCEQvF2= MkDM[Il{enWydIOgcYlkem:2dXL1cIU> MkniNlM2QTh{N{[=
H460 NF\iOIZHfW6ldHnvckBie3OjeR?= NGG3SW8yOCEQvF2= MYHpcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v NWGzTGhZOjV|MUOwNVA>
K562/VCR MUHDfZRwfG:6aXRCpIF{e2G7 MXX+NVAh|ryP MWLzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NHzhVIUzPTNzM{CxNC=>
CEM/VBL NXO3eXlES3m2b4TvfIlkyqCjc4PhfS=> MkC3glExKM7:TR?= NXvad4Rke2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MYSyOVMyOzBzMB?=
U266 NWjxT4R5S3m2b4TvfIlkyqCjc4PhfS=> NGHaNGh,OyEQvF5CpC=> NE\Od4lKSzVyPUGuNUDPxE1? MVSyOVgyODBzMx?=
OPM-2 NV\3dZN4S3m2b4TvfIlkyqCjc4PhfS=> NELZe4F,OyEQvF5CpC=> NWrVO4RYUUN3ME2xMlgh|ryP M3jUbFI2QDFyMEGz
MM.1S NV\pR3B7S3m2b4TvfIlkyqCjc4PhfS=> NXLoV3Y{hjNizszNxsA> MVjJR|UxRTFwNjFOwG0> MVyyOVgyODBzMx?=
MM.1R MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{DVXFMh|ryPwrC= M3jqVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> MXWyOVgyODBzMx?=
RPMI-8226 NY\CWmtiS3m2b4TvfIlkyqCjc4PhfS=> M{Lk[J4{KM7:TdMg NFXqTFVKSzVyPUCuPUDPxE1? MnXtNlU5OTByMUO=
ANBL-6 Mle2R5l1d3SxeHnjxsBie3OjeR?= M2HmVVEh|ryPwrC= MV\pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NWfaZlVLOjV6MUCwNVM>
ANLB-6/V10R M13wXmN6fG:2b4jpZ:Kh[XO|YYm= NHrxc20yKM7:TdMg M4O2[Ilv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NIHjZ3QzPThzMECxNy=>
KAS-6/1 M2HPZWN6fG:2b4jpZ:Kh[XO|YYm= Mkn4NUDPxE4EoB?= MYLpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MlnhNlU5OTByMUO=
KAS-6/V10R NE\kc5NEgXSxdH;4bYPDqGG|c3H5 M373TlEh|ryPwrC= M3PlSIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NX7SUJYxOjV6MUCwNVM>
KAS-6/R10R MVLDfZRwfG:6aXRCpIF{e2G7 MmTTNUDPxE4EoB?= MXrpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NFL3XFIzPThzMECxNy=>
8226/S Mmr6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWOzJO69VcLi Mn3xbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl MY[yOVgyODBzMx?=
8226/LR-5 NID6ZpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWTjSWw4OyEQvF5CpC=> NXq1R5hVcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm M{C5eFI2QDFyMEGz
Huh7 M{PDe2N6fG:2b4jpZ:Kh[XO|YYm= MojTglQvQCEQvF5CpC=> NH3OU2ZFVVOR MXTJR|UxRTlwOTDuUS=> NUn6bWx{OjZ{NUmyOVA>
Hep3B NH3vb4lEgXSxdH;4bYPDqGG|c3H5 NGL5W5p,PC56IN88UeKh MkHCSG1UVw>? Mmq3TWM2OD12NEiuO{BvVQ>? MYOyOlI2QTJ3MB?=
HepG2 MXPDfZRwfG:6aXRCpIF{e2G7 NET5NGV,PC56IN88UeKh NH;hbFZFVVOR Ml20TWM2OD1zM{muO|chdk1? MVqyOlI2QTJ3MB?=
Chang NWf6UHhbS3m2b4TvfIlkyqCjc4PhfS=> MkOxglQvQCEQvF5CpC=> M365N2ROW09? MYTJR|UxRTR2OD63JI5O MmPHNlYzPTl{NUC=
Huh7 MYXGeY5kfGmxbjDhd5NigQ>? MWqxMlYh|ryPwrC= NUS4OXNvTE2VTx?= MojpZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NGnYOIYzPjJ3OUK1NC=>
Hep3B MV\GeY5kfGmxbjDhd5NigQ>? NFrh[lkyNjZizszNxsA> MlfySG1UVw>? NWqzS|RC[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= Mnr5NlYzPTl{NUC=
HepG2 NHzZSmlHfW6ldHnvckBie3OjeR?= NIfPeJMyNjZizszNxsA> NYrpcpdiTE2VTx?= NHzSPYlk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MmfRNlYzPTl{NUC=
Chang NV3Qb4pWTnWwY4Tpc44h[XO|YYm= MWKxMlYh|ryPwrC= NWTxXpdbTE2VTx?= NX[3RXBx[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= Mn3xNlYzPTl{NUC=
MHCC97L MmjSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVzkO45rhjFyIN88US=> MnzVSG1UVw>? MlrxTWM2OD1|MUWgcm0> MUWyOlQ2QDl3Mx?=
MHCC97H NGnyfGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFnyS5p,OTBizszN NX;IcpA5TE2VTx?= NV7PPXN{UUN3ME2zOljjiIlibl2= M3G0PFI3PDV6OUWz
Huh7 MkmzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4\nbp4yOCEQvF2= M4PUSmROW09? MkTuTWM2OD1{NkWgcm0> NWDtRZF7OjZ2NUi5OVM>
HepG2 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWf+NVAh|ryP M{e4[WROW09? NVy0c|l{UUN3ME2zPVIhdk1? M2nqSlI3PDV6OUWz
MHCC97L M3HPOGZ2dmO2aX;uJIF{e2G7 MY[xJO69VcLi MkfQSG1UVw>? NW\sbGdmcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NVvndYF4OjZ2NUi5OVM>
Huh7 NYi2[44yTnWwY4Tpc44h[XO|YYm= NHfZRZIyKM7:TdMg NV\qN2NDTE2VTx?= NWfQV4pqcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NGXz[WozPjR3OEm1Ny=>
MHCC97L MnfORZBweHSxc3nzJIF{e2G7 Mof4NUDPxE4EoB?= NHG2OJFFVVOR NXHxS4ozcW6mdXPld{BieG:ydH;zbZM> NF6zUokzPjR3OEm1Ny=>
Huh7 M{KzXGFxd3C2b4Ppd{Bie3OjeR?= MnT3NUDPxE4EoB?= NYmwVlJjTE2VTx?= NGfHZ3ZqdmS3Y3XzJIFxd3C2b4Ppdy=> MVWyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts NWexNolvU2mwYYPlJIF{e2G7 M2jnVlI2KM7:TR?= MWjEUXNQ M2P6e5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> NXf2VXhUOjB3M{SzOFU>
H23 NE[2PFdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{fs[FI2KM7:TR?= Mmq1SG1UVw>? Mm\Gd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MVSyNFU{PDN2NR?=
WM35 M1XDbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NETNNJMyOCEQvF2= M13ydmROW09? MYXzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= M3\WXVIxPTN2M{S1
NIH 3T3 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4nWV|ExKM7:TR?= Mmn1SG1UVw>? MYXkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= M3LEOVIxPTN2M{S1
H838 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV[xNEDPxE1? NIe5UItFVVOR NHHodlNld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NGT2c4gzODV|NEO0OS=>
H1395 NWrYSWVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFW4dVkyOCEQvF2= NUTyV2VyTE2VTx?= NGq5blNld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NF\RWlczODV|NEO0OS=>
Quiescent S2 M37FVWtqdmG|ZTDhd5NigQ>? Mn\XN|Ah|ryP MoLOSG1UVw>? M4TUcoNwdXCuZYTlcJkh[WK{b3fheIV{KFSVQT3pcoR2[2WmIHj5dIVz[WOndInsZZRqd25ib3[gTFNMPG2nMzDobZN1d26ncx?= NE\5SFAzOTVzOEmxOS=>
PC3 NW\UVY97SXCxcITvd4l{KGG|c3H5 MmjXNlAh|ryP MXfEUXNQ MlHSbY5lfWOnczDhdI9xfG:|aYO= MWmyNVcxQTF|MB?=
Du145 NFjI[3RCeG:ydH;zbZMh[XO|YYm= NIC4XpkzOCEQvF2= MWTEUXNQ M1rRd4lv\HWlZYOgZZBweHSxc3nz M4XYe|IyPzB7MUOw
LNCaP NYDMSmprSXCxcITvd4l{KGG|c3H5 MWSyNEDPxE1? MVvEUXNQ M1LHR4lv\HWlZYOgZZBweHSxc3nz Mk\6NlE4ODlzM{C=
LAPC-4 MoLTRZBweHSxc3nzJIF{e2G7 MWKyNEDPxE1? M1LS[2ROW09? NXjNSFNKcW6mdXPld{BieG:ydH;zbZM> Ml;DNlE4ODlzM{C=
LNCaP NFOydFZHfW6ldHnvckBie3OjeR?= NFviSXgzOCEQvF2= MoXISG1UVw>? M1zYdoRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NUHqV|Z1OjF5MEmxN|A>
LAPC-4 MkjlSpVv[3Srb36gZZN{[Xl? NGnpUG4zOCEQvF2= MU\EUXNQ MkLG[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NWK2THRFOjF5MEmxN|A>
Kasumi-1 NYHId2JVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2DjT542OCEQvF2= NEjTZllFVVOR NEX2R|VqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MXWyN|M6ODV|Nh?=
SKNO-1 MmLtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnnvglUxKM7:TR?= NWPS[5FlTE2VTx?= NU\XdohbcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MV2yN|M6ODV|Nh?=
Kasumi-1 Ml\xT4lv[XOnIHHzd4F6 NEL6N3F,OTBizszN MnX0SG1UVw>? M3r1c5Jm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> MkPpNlM{QTB3M{[=
SKNO-1 NWPjZYVOU2mwYYPlJIF{e2G7 MWL+NVAh|ryP M1jFV2ROW09? NUjQb2FFemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z MlrUNlM{QTB3M{[=
A549 NIXjNFZHfW6ldHnvckBie3OjeR?= MUSxNEDPxE1? MkXWSG1UVw>? NGH0V5dmdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm MXiyOFc1PjV5NB?=
NRK-52E M{DvR2Z2dmO2aX;uJIF{e2G7 MUKxNEDPxE1? M{T0RmROW09? NHHLRXlqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDTWGFVOyCwdXPs[YFzKHS{YX7zcI9k[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKFSJRj5OtlEtKGOxbHzh[4VvKEmYIHHu[EBncWK{b37lZ5Rqdg>? M4LxPVI2ODh6MECy
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RCH-ACV M{XXSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2TjXFExKM7:TR?= NYXG[XFNTE2VTx?= M1f5VmVEPTB;MUWyJI5O M2jVc|E6ODZ2N{Ow
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800000 NVfxe2VnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2nCdVExKM7:TR?= Mn7ESG1UVw>? NVfEZY1nTUN3ME2xOlMhdk1? NGPEfYsyQTB4NEezNC=>
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CHLA-10 NUC0SmE{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWexNEDPxE1? MVzJR|UxRTFyMjDuUS=> NXHhR5hXOjB5NEC2NlM>
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H1299 M4HCfmtqdmG|ZTDhd5NigQ>? M1rIT|ExKM7:TR?= M134RYlvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> MmPkNlE6ODh4MU[=

... 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 Completed 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 Inc. (a wholly owned subsidiary of Merck Sharp and Dohme a subsidiary of Merck & Co. Inc.) 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

Tel: +1-832-582-8158 Ext:3

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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