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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1 Customer Review

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NVvUcmdPU2mwYYPlJIF{e2G7 NEPOfWl,OTBizszN MX\pcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NYjZZpFnOjB2OESwNVg>
HT29 NYDRdnVyU2mwYYPlJIF{e2G7 MnHqglExKM7:TR?= MUnpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M1TXW|IxPDh2MEG4
MDA-MB-231 MkC2T4lv[XOnIHHzd4F6 NWjGd2dXhjFyIN88US=> Mom2bY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MVqyNFQ5PDBzOB?=
NCI-H441 MmnYT4lv[XOnIHHzd4F6 MX;+NVAh|ryP M4TtTolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NFvY[5IzODR6NECxPC=>
SK-MEL-28 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHzIOGU{OyEQvF2= NHL1RXdKSzVyPkOzJO69VQ>? M3XBW|IxPDh2MEG4
NCI-H661 NXnK[Y1vT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NE\RW4E{OyEQvF2= NE[zfFBKSzVyPkOzJO69VQ>? NU\3UZdFOjB2OESwNVg>
NCI-H446 NUT1cVB6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWXyPYp5OzNizszN NHLGdIhKSzVyPUeg{txO MWCyNFQ5PDBzOB?=
MDA-MB-231 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIrGVGQ{OyEQvF2= NYHacphIUUN3ME2wMlU2KM7:TR?= NEfQTm0zODR6NECxPC=>
DLD-1 NHTyXHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{fKSlM{KM7:TR?= MmiwTWM2OD1yLkWzJO69VQ>? MXqyNFQ5PDBzOB?=
A549 NIPXelBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUjORWl1OzNizszN NYTaTmFRUUN3ME2wMlU6KM7:TR?= MXiyNFQ5PDBzOB?=
SK-OV-3 M{DqTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnTLN|Mh|ryP Mmj1TWM2OD1yLk[2JO69VQ>? NILk[ZQzODR6NECxPC=>
NCI-H460 NYG2NJRMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrYWFZ5OzNizszN NILNbWRKSzVyPUCuOkDPxE1? MVmyNFQ5PDBzOB?=
A375 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkO1N|Mh|ryP M{fse2lEPTB;MD60NkDPxE1? NI\lUmkzODR6NECxPC=>
NCI-H441 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHLhSHk{OyEQvF2= MlzPTWM2OD1yLkOg{txO M4HNN|IxPDh2MEG4
HT29 MmrYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIO2S3I{OyEQvF2= M{fH[mlEPTB;MD60PUDPxE1? NHjwfJczODR6NECxPC=>
MKN-45 NUjiT2hrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmHIN|Mh|ryP MoP5TWM2OD1yLkW4JO69VQ>? MWWyNFQ5PDBzOB?=
HT29 NW\pWYxSSXCxcITvd4l{KGG|c3H5 MWH+NVAh|ryP M3PIRpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NUHnZVhkOjB2OESwNVg>
MKN-45 MX3BdI9xfG:|aYOgZZN{[Xl? NFzxXZR,OTBizszN MYXzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NVXHOm06OjB2OESwNVg>
MDA-MB-231 MlHVRZBweHSxc3nzJIF{e2G7 MWn+NVAh|ryP NH33OZdud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu MlPINlA1QDRyMUi=
MDA-MB-231/TGL MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\SbJ4yODBizszN NV;HcWlLT0l3ME2xMlIh|ryP M1TicVIzODJ5Nkmw
1833/TGL NHjGem1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYH+NVAxKM7:TR?= MlHRS2k2OD1|Lkeg{txO NXXObHc4OjJyMke2PVA>
EBC1 MYfDfZRwfG:6aXRCpIF{e2G7 Mom1glExKM7:TR?= MmPJbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= MnXONlM2QTh{N{[=
SNU638 MX7DfZRwfG:6aXRCpIF{e2G7 M4LK[p4yOCEQvF2= MoXibY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= M{nXUVI{PTl6Mke2
A549 NYHpfItmS3m2b4TvfIlkyqCjc4PhfS=> NGnXdW5,OTBizszN MWruc5Qh[W[oZXP0 NF3xWWwzOzV7OEK3Oi=>
H460 MnrtR5l1d3SxeHnjxsBie3OjeR?= NHPiXGZ,OTBizszN NVfMOpMxdm:2IHHm[oVkfA>? NGnVWVMzOzV7OEK3Oi=>
HCC827 M2H2UWN6fG:2b4jpZ:Kh[XO|YYm= NYfoVWVthjFyIN88US=> M2TyUY5wfCCjZn\lZ5Q> MVqyN|U6QDJ5Nh?=
A549 Mkn5SpVv[3Srb36gZZN{[Xl? M3;Ie|ExKM7:TR?= MmLq[Il{enWydIOgcYlkem:2dXL1cIU> NIHWOGEzOzV7OEK3Oi=>
EBC1 M4rUT2Z2dmO2aX;uJIF{e2G7 MmXxNVAh|ryP NXPjU|E3\Gm|coXweJMhdWmlcn;0eYJ2dGV? MljNNlM2QTh{N{[=
H460 Mk\SSpVv[3Srb36gZZN{[Xl? NFTIXmEyOCEQvF2= MoPabY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? MUeyOVMyOzBzMB?=
K562/VCR NUnBW5Q4S3m2b4TvfIlkyqCjc4PhfS=> MXf+NVAh|ryP NVTic5I2e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NFXscXEzPTNzM{CxNC=>
CEM/VBL MX\DfZRwfG:6aXRCpIF{e2G7 NGDyPIR,OTBizszN Mn\Kd4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 M4fwVlI2OzF|MEGw
U266 NVHvfG94S3m2b4TvfIlkyqCjc4PhfS=> MXL+N{DPxE4EoB?= NWTsbpJzUUN3ME2xMlEh|ryP NFPWOpozPThzMECxNy=>
OPM-2 NWTJV5Q3S3m2b4TvfIlkyqCjc4PhfS=> MkLSglMh|ryPwrC= NIL5eJVKSzVyPUGuPEDPxE1? M{\jRlI2QDFyMEGz
MM.1S NEXLW5lEgXSxdH;4bYPDqGG|c3H5 NVXjRVlXhjNizszNxsA> MULJR|UxRTFwNjFOwG0> NUXqXHRVOjV6MUCwNVM>
MM.1R M{LUVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHv2bIM{KM7:TdMg M4nxNYlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> M3;GblI2QDFyMEGz
RPMI-8226 MkXER5l1d3SxeHnjxsBie3OjeR?= NEjmN4V,OyEQvF5CpC=> M4TC[WlEPTB;MD65JO69VQ>? NV3pdIxqOjV6MUCwNVM>
ANBL-6 NHLsd|REgXSxdH;4bYPDqGG|c3H5 MoDUNUDPxE4EoB?= M2W3TIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MonFNlU5OTByMUO=
ANLB-6/V10R MnXHR5l1d3SxeHnjxsBie3OjeR?= NV\OZ25iOSEQvF5CpC=> NHPifmNqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MXGyOVgyODBzMx?=
KAS-6/1 MoXYR5l1d3SxeHnjxsBie3OjeR?= MY[xJO69VcLi NX\qW2hpcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NF;zRoszPThzMECxNy=>
KAS-6/V10R MXzDfZRwfG:6aXRCpIF{e2G7 M1HlRlEh|ryPwrC= MXXpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NECxZoozPThzMECxNy=>
KAS-6/R10R MUHDfZRwfG:6aXRCpIF{e2G7 NFT6UIQyKM7:TdMg MkTubY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= Mm\SNlU5OTByMUO=
8226/S MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUf5N4Z3OyEQvF5CpC=> M3P0WolvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> NWfMN3RVOjV6MUCwNVM>
8226/LR-5 M4n4Xmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXPpZYZVOyEQvF5CpC=> NWTkRotPcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm NGjwUpgzPThzMECxNy=>
Huh7 MYXDfZRwfG:6aXRCpIF{e2G7 MkXPglQvQCEQvF5CpC=> MkTwSG1UVw>? MmrLTWM2OD17Lkmgcm0> M4DQS|I3OjV7MkWw
Hep3B NF75bJVEgXSxdH;4bYPDqGG|c3H5 M2\qZp41NjhizszNxsA> MorOSG1UVw>? NUm3fZJbUUN3ME20OFgvPyCwTR?= MmHiNlYzPTl{NUC=
HepG2 NEfXenZEgXSxdH;4bYPDqGG|c3H5 MUL+OE45KM7:TdMg MnrkSG1UVw>? MmLDTWM2OD1zM{muO|chdk1? M1ftSlI3OjV7MkWw
Chang MnrnR5l1d3SxeHnjxsBie3OjeR?= MXP+OE45KM7:TdMg NYOwXJNjTE2VTx?= MkHzTWM2OD12NEiuO{BvVQ>? NGHWWoozPjJ3OUK1NC=>
Huh7 NYPpXHFqTnWwY4Tpc44h[XO|YYm= MnLaNU43KM7:TdMg NIm4OohFVVOR NHjTb5Zk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NYfmToNtOjZ{NUmyOVA>
Hep3B MlP3SpVv[3Srb36gZZN{[Xl? MnPiNU43KM7:TdMg NXLNUZI4TE2VTx?= MlXMZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Mn7lNlYzPTl{NUC=
HepG2 MVXGeY5kfGmxbjDhd5NigQ>? NVrVd2J6OS54IN88UeKh NFXTbolFVVOR M2GyOoNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NWLSUIxuOjZ{NUmyOVA>
Chang NWjrVFNVTnWwY4Tpc44h[XO|YYm= MlTiNU43KM7:TdMg MU\EUXNQ MYDjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NXfnNohNOjZ{NUmyOVA>
MHCC97L M1vMRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGDI[GJ,OTBizszN M1fob2ROW09? MkDzTWM2OD1|MUWgcm0> MnfINlY1PTh7NUO=
MHCC97H M1\nTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIjMUld,OTBizszN MkHGSG1UVw>? MmPVTWM2OD1|NklihKkhdk1? M2rD[lI3PDV6OUWz
Huh7 M{LHdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4SzbJ4yOCEQvF2= MWXEUXNQ MnLETWM2OD1{NkWgcm0> M4frUlI3PDV6OUWz
HepG2 NEfGNYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLUZXFEhjFyIN88US=> M3\PTWROW09? NUPmXolOUUN3ME2zPVIhdk1? NV;WTIFGOjZ2NUi5OVM>
MHCC97L MX\GeY5kfGmxbjDhd5NigQ>? NIXHWngyKM7:TdMg NFXv[pVFVVOR MoXxbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NX;3dGE1OjZ2NUi5OVM>
Huh7 NHLXUHhHfW6ldHnvckBie3OjeR?= MkXDNUDPxE4EoB?= NXnxe4QxTE2VTx?= NUXt[Yc5cW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? MVyyOlQ2QDl3Mx?=
MHCC97L NEXjNY5CeG:ydH;zbZMh[XO|YYm= NVXacXpXOSEQvF5CpC=> MkThSG1UVw>? NWC3c2FncW6mdXPld{BieG:ydH;zbZM> NFPvXZQzPjR3OEm1Ny=>
Huh7 NGrpbIhCeG:ydH;zbZMh[XO|YYm= M2TNNVEh|ryPwrC= MWDEUXNQ MY\pcoR2[2W|IHHwc5B1d3Orcx?= MUSyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts MYnLbY5ie2ViYYPzZZk> MVeyOUDPxE1? NFn0SnNFVVOR NXvBOoMzemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? NYnyRZd1OjB3M{SzOFU>
H23 MoL5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1zaV|I2KM7:TR?= MULEUXNQ NGfhOWF{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NUXJbJZ2OjB3M{SzOFU>
WM35 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml75NVAh|ryP M4POPGROW09? NV;OeINNe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MkT5NlA2OzR|NEW=
NIH 3T3 M4T5Z2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlPuNVAh|ryP NHXLNGhFVVOR MmLE[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NIjJNHozODV|NEO0OS=>
H838 M3jGV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGn4NHEyOCEQvF2= NUe4Z5N6TE2VTx?= MXLkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= Mmi1NlA2OzR|NEW=
H1395 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUP3S2FHOTBizszN NHHGUWRFVVOR MlrT[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MXGyNFU{PDN2NR?=
Quiescent S2 NFq4OZlMcW6jc3WgZZN{[Xl? MVyzNEDPxE1? NFTNWYRFVVOR M165XINwdXCuZYTlcJkh[WK{b3fheIV{KFSVQT3pcoR2[2WmIHj5dIVz[WOndInsZZRqd25ib3[gTFNMPG2nMzDobZN1d26ncx?= MXGyNVUyQDlzNR?=
PC3 NYfWe2c3SXCxcITvd4l{KGG|c3H5 MUGyNEDPxE1? NW\1[odjTE2VTx?= NF7Sb25qdmS3Y3XzJIFxd3C2b4Ppdy=> M3PDV|IyPzB7MUOw
Du145 MV;BdI9xfG:|aYOgZZN{[Xl? NETkfIMzOCEQvF2= NF\EXIpFVVOR NEnyeoNqdmS3Y3XzJIFxd3C2b4Ppdy=> MYGyNVcxQTF|MB?=
LNCaP MWrBdI9xfG:|aYOgZZN{[Xl? NXLwTFdXOjBizszN M1rKNmROW09? MljHbY5lfWOnczDhdI9xfG:|aYO= NEDkeIczOTdyOUGzNC=>
LAPC-4 Mm\ORZBweHSxc3nzJIF{e2G7 M1XCPVIxKM7:TR?= MXXEUXNQ MnXkbY5lfWOnczDhdI9xfG:|aYO= MYGyNVcxQTF|MB?=
LNCaP NXTFfZJtTnWwY4Tpc44h[XO|YYm= NGTxT2EzOCEQvF2= M1rEW2ROW09? MlL0[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MXmyNVcxQTF|MB?=
LAPC-4 NIC2N5JHfW6ldHnvckBie3OjeR?= M4nnOFIxKM7:TR?= MWHEUXNQ M3rBU4Rm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? MXKyNVcxQTF|MB?=
Kasumi-1 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVHEVpZqhjVyIN88US=> MXXEUXNQ Mn3nbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NYHuPFNHOjN|OUC1N|Y>
SKNO-1 NHvheHJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoLaglUxKM7:TR?= NFfHSFBFVVOR M325XIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M{\UNlI{OzlyNUO2
Kasumi-1 MWDLbY5ie2ViYYPzZZk> NYL1OVdHhjFyIN88US=> NHfJVHpFVVOR NIXTbYFz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MVyyN|M6ODV|Nh?=
SKNO-1 NV71fmJFU2mwYYPlJIF{e2G7 NWT3e4R5hjFyIN88US=> NHvLcGNFVVOR M17yN5Jm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> M2TuNFI{OzlyNUO2
A549 MX\GeY5kfGmxbjDhd5NigQ>? Ml\rNVAh|ryP M4fMdmROW09? NWT5XJJ3\W6qYX7j[ZMhdWm2b4TpZ{Bk[XSjc4Tyc5Bp\Q>? NYLKPGFPOjR5NE[1O|Q>
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PC12 NYCxSJBOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWr+NVIvPSEQvF2= NILEdJBFVVOR NFXFbHhxemW4ZX70d{BVW0FvaX7keYNm\CCwZYXybZRmKG[xcn3heIlwdg>? NIXqbnQzPTF{OEO4Oi=>
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Karpas-299 Mn7rS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml;rNVAh|ryP MUjJR|UxRTJwOUOg{txO MXuyNFc1ODZ{Mx?=
Ramos-RA1 NV;ifWtYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{XsclExKM7:TR?= MmPZTWM2OD15LkO1JO69VQ>? M2XxeFIxPzRyNkKz
H1299 MXLLbY5ie2ViYYPzZZk> M4LZWVExKM7:TR?= NUHkNmF3cW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? NGL1RXozOTlyOE[xOi=>

... 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]
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 24, 2011 Phase 1
NCT02608411 Recruiting 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
NCT02029157 Recruiting Liver Cancer Kyowa Hakko Kirin Co., Ltd January 2014 Phase 3
NCT01892527 Active, not recruiting Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro, MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Active, not recruiting 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID