Tivantinib (ARQ 197)

For research use only.

Catalog No.S2753

15 publications

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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Selleck's Tivantinib (ARQ 197) has been cited by 15 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 NEHJToJMcW6jc3WgZZN{[Xl? MlO5glExKM7:TR?= MlrsbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NFPBWowzODR6NECxPC=>
HT29 M2nGcGtqdmG|ZTDhd5NigQ>? NV3zRXg2hjFyIN88US=> MWnpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NF;yd3YzODR6NECxPC=>
MDA-MB-231 MX\LbY5ie2ViYYPzZZk> M1K3dZ4yOCEQvF2= M1\nPIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MlfGNlA1QDRyMUi=
NCI-H441 NV[xXnQ3U2mwYYPlJIF{e2G7 MUD+NVAh|ryP MnHZbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NVrvSpdYOjB2OESwNVg>
SK-MEL-28 MkfHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUPLNJpWOzNizszN Ml[2TWM2OD5|MzFOwG0> NHj0V3EzODR6NECxPC=>
NCI-H661 NIfkb3RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1Sxb|M{KM7:TR?= NXmzUVN5UUN3ME6zN{DPxE1? NGWzOY4zODR6NECxPC=>
NCI-H446 MmLWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFP4cHc{OyEQvF2= NXLRTXk{UUN3ME23JO69VQ>? NF7NTWUzODR6NECxPC=>
MDA-MB-231 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mnv4N|Mh|ryP NVLLbJVnUUN3ME2wMlU2KM7:TR?= M4nwPFIxPDh2MEG4
DLD-1 M{DGRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoCyN|Mh|ryP MWPJR|UxRTBwNUOg{txO M2CwRVIxPDh2MEG4
A549 NWDLNGxbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXmzN{DPxE1? MXLJR|UxRTBwNUmg{txO MYiyNFQ5PDBzOB?=
SK-OV-3 MmD4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1fPTlM{KM7:TR?= MYrJR|UxRTBwNk[g{txO NH3UXmgzODR6NECxPC=>
NCI-H460 NFGxbFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn6yN|Mh|ryP NXK2O3U2UUN3ME2wMlYh|ryP NYjrRYxVOjB2OESwNVg>
A375 NGHPUmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGrm[mM{OyEQvF2= NEmwNWJKSzVyPUCuOFIh|ryP NUTWO3c3OjB2OESwNVg>
NCI-H441 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWT6[5VoOzNizszN NHLibo5KSzVyPUCuN{DPxE1? M4TtXFIxPDh2MEG4
HT29 M1zkSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn73N|Mh|ryP MW\JR|UxRTBwNEmg{txO M{TkUFIxPDh2MEG4
MKN-45 M{jZVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXO5UWlKOzNizszN M1LCUGlEPTB;MD61PEDPxE1? Mn;BNlA1QDRyMUi=
HT29 NWGwepdRSXCxcITvd4l{KGG|c3H5 NUPuWmpHhjFyIN88US=> NEPLTFh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= M4nuUVIxPDh2MEG4
MKN-45 MXjBdI9xfG:|aYOgZZN{[Xl? M2Lpfp4yOCEQvF2= M4nRbZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MXOyNFQ5PDBzOB?=
MDA-MB-231 MoCxRZBweHSxc3nzJIF{e2G7 M3HFfZ4yOCEQvF2= MWXtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw MoH2NlA1QDRyMUi=
MDA-MB-231/TGL MmPjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHv3Vnh,OTByIN88US=> MUXHTVUxRTFwMjFOwG0> NHPBeIszOjB{N{[5NC=>
1833/TGL Mnf1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3rRUJ4yODBizszN NILhN5ZIUTVyPUOuO{DPxE1? MkLYNlIxOjd4OUC=
EBC1 MoLwR5l1d3SxeHnjxsBie3OjeR?= M{XwWZ4yOCEQvF2= MmDHbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= MkjkNlM2QTh{N{[=
SNU638 M{PXS2N6fG:2b4jpZ:Kh[XO|YYm= NV2yWGpbhjFyIN88US=> MliwbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= NXX1[mdQOjN3OUiyO|Y>
A549 NV\sfHhHS3m2b4TvfIlkyqCjc4PhfS=> MkDOglExKM7:TR?= NHfqN5Nvd3RiYX\m[YN1 NX;iVJdPOjN3OUiyO|Y>
H460 NYHpS4JlS3m2b4TvfIlkyqCjc4PhfS=> NG\CVGd,OTBizszN NFXnbmpvd3RiYX\m[YN1 M3rlVVI{PTl6Mke2
HCC827 MnfMR5l1d3SxeHnjxsBie3OjeR?= MXj+NVAh|ryP M4m0So5wfCCjZn\lZ5Q> MlrMNlM2QTh{N{[=
A549 Mlr0SpVv[3Srb36gZZN{[Xl? MYixNEDPxE1? MnPl[Il{enWydIOgcYlkem:2dXL1cIU> NF[zcZczOzV7OEK3Oi=>
EBC1 MUHGeY5kfGmxbjDhd5NigQ>? NWjUUpZEOTBizszN M4jEN4Rqe3K3cITzJI1q[3KxdIXieYxm M4DlZlI{PTl6Mke2
H460 NGn2bIFHfW6ldHnvckBie3OjeR?= NHPw[IQyOCEQvF2= MmjibY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? MmnvNlU{OTNyMUC=
K562/VCR MXzDfZRwfG:6aXRCpIF{e2G7 M3jGU54yOCEQvF2= NEfTZ|F{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M3\TN|I2OzF|MEGw
CEM/VBL NXnBV4hmS3m2b4TvfIlkyqCjc4PhfS=> NVTCSYIxhjFyIN88US=> MmT0d4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 MY[yOVMyOzBzMB?=
U266 MWXDfZRwfG:6aXRCpIF{e2G7 NY\2ZYFohjNizszNxsA> MlvrTWM2OD1zLkGg{txO MVeyOVgyODBzMx?=
OPM-2 MVjDfZRwfG:6aXRCpIF{e2G7 MWf+N{DPxE4EoB?= M{jvXmlEPTB;MT64JO69VQ>? M1fsXVI2QDFyMEGz
MM.1S MVXDfZRwfG:6aXRCpIF{e2G7 NWDlbW1rhjNizszNxsA> MoPjTWM2OD1zLk[g{txO NHLQemIzPThzMECxNy=>
MM.1R MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPDN{DPxE4EoB?= NF23fmdqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> Mn\tNlU5OTByMUO=
RPMI-8226 NF61WmVEgXSxdH;4bYPDqGG|c3H5 NH7UOZd,OyEQvF5CpC=> NIO1U2FKSzVyPUCuPUDPxE1? MYmyOVgyODBzMx?=
ANBL-6 NFHqe2xEgXSxdH;4bYPDqGG|c3H5 NVewcJNuOSEQvF5CpC=> NYHjemhbcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NYDPRnBGOjV6MUCwNVM>
ANLB-6/V10R NYS0cZM1S3m2b4TvfIlkyqCjc4PhfS=> NVPjNWJtOSEQvF5CpC=> NUjDVZRNcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NGHCXVQzPThzMECxNy=>
KAS-6/1 MXTDfZRwfG:6aXRCpIF{e2G7 NH3qR|QyKM7:TdMg NV7pNJd6cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NXTyPW5jOjV6MUCwNVM>
KAS-6/V10R NHy5NohEgXSxdH;4bYPDqGG|c3H5 NULIS4xJOSEQvF5CpC=> M37Gd4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M4fiSFI2QDFyMEGz
KAS-6/R10R MVLDfZRwfG:6aXRCpIF{e2G7 NUfXW5ltOSEQvF5CpC=> MV;pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MlflNlU5OTByMUO=
8226/S MnnDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlK2N{DPxE4EoB?= MYXpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= MUeyOVgyODBzMx?=
8226/LR-5 MlLIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2jnd|Mh|ryPwrC= NHrvTFJqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> NX;CflBbOjV6MUCwNVM>
Huh7 NGnjeWdEgXSxdH;4bYPDqGG|c3H5 NFjXOFJ,PC56IN88UeKh M370bGROW09? MVnJR|UxRTlwOTDuUS=> NFXpWnkzPjJ3OUK1NC=>
Hep3B M33x[2N6fG:2b4jpZ:Kh[XO|YYm= NVLRRm5rhjRwODFOwG3DqA>? NXXtUJlyTE2VTx?= MmjnTWM2OD12NEiuO{BvVQ>? MW[yOlI2QTJ3MB?=
HepG2 Mmf2R5l1d3SxeHnjxsBie3OjeR?= M1X3TZ41NjhizszNxsA> NFPHfGVFVVOR MojaTWM2OD1zM{muO|chdk1? NGHWdZUzPjJ3OUK1NC=>
Chang NXHZZ29iS3m2b4TvfIlkyqCjc4PhfS=> NYW1NG9MhjRwODFOwG3DqA>? NHTmNZFFVVOR NGLBR5dKSzVyPUS0PE44KG6P MVOyOlI2QTJ3MB?=
Huh7 NEfYZW9HfW6ldHnvckBie3OjeR?= NFThWVUyNjZizszNxsA> MVXEUXNQ MU\jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NYP4O2FmOjZ{NUmyOVA>
Hep3B NF3uTmJHfW6ldHnvckBie3OjeR?= MnS1NU43KM7:TdMg NETSXmRFVVOR NGPBVlBk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M{XJN|I3OjV7MkWw
HepG2 NFy0T21HfW6ldHnvckBie3OjeR?= M3;0c|EvPiEQvF5CpC=> NUK1dIY2TE2VTx?= NWnVN3NI[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M1O3VFI3OjV7MkWw
Chang MlqwSpVv[3Srb36gZZN{[Xl? MkjFNU43KM7:TdMg MVrEUXNQ NHT3bG5k[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M3rSTlI3OjV7MkWw
MHCC97L NGrFT41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWDJbpNLhjFyIN88US=> M2nscWROW09? NHm0[IpKSzVyPUOxOUBvVQ>? NH7FNZkzPjR3OEm1Ny=>
MHCC97H M{nFOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVPW[2pmhjFyIN88US=> MnLYSG1UVw>? MWHJR|UxRTN4OPMAjUBvVQ>? MYOyOlQ2QDl3Mx?=
Huh7 NFHMOGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUP+NVAh|ryP NWLLUYxQTE2VTx?= MnHnTWM2OD1{NkWgcm0> MYWyOlQ2QDl3Mx?=
HepG2 NFH2O45Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHfh[5J,OTBizszN NXTKPIw1TE2VTx?= NFHqVnJKSzVyPUO5NkBvVQ>? MWSyOlQ2QDl3Mx?=
MHCC97L NYP6UIFwTnWwY4Tpc44h[XO|YYm= M1[wflEh|ryPwrC= MX7EUXNQ M2HVbIlv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> M1;od|I3PDV6OUWz
Huh7 Mk\ESpVv[3Srb36gZZN{[Xl? M2H5flEh|ryPwrC= Mn7wSG1UVw>? MXTpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u M1fweFI3PDV6OUWz
MHCC97L NYTaU2FHSXCxcITvd4l{KGG|c3H5 NFTa[HMyKM7:TdMg NFnLUZhFVVOR MVrpcoR2[2W|IHHwc5B1d3Orcx?= NUXGS41qOjZ2NUi5OVM>
Huh7 MWPBdI9xfG:|aYOgZZN{[Xl? NXe3Z4ZSOSEQvF5CpC=> NH;VeFVFVVOR MUnpcoR2[2W|IHHwc5B1d3Orcx?= NGfDWlgzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts MV3LbY5ie2ViYYPzZZk> NYjYU2ZTOjVizszN NIHpTo1FVVOR NELYZ|Fz\WS3Y3XzJGhqe3SxbnWgTFMh[W6mIFi0JIFk\XS7bHH0bY9vKGyndnXsd:Kh M2q0eVIxPTN2M{S1
H23 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4SzXlI2KM7:TR?= NVTFT4RPTE2VTx?= M37XXpNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu M{P3XVIxPTN2M{S1
WM35 NUnkVmhHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MU[xNEDPxE1? M3PUNGROW09? MUXzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NFS1OoIzODV|NEO0OS=>
NIH 3T3 NXnnZWZpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUTjVZBIOTBizszN NWLkW3FMTE2VTx?= NGnWUIRld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NYPXUWhrOjB3M{SzOFU>
H838 NYe3N3NuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVuxNEDPxE1? NFXZPFlFVVOR NFfGTHZld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> Mnm3NlA2OzR|NEW=
H1395 M2nidGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M17NXFExKM7:TR?= MYXEUXNQ MUDkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= M1zZN|IxPTN2M{S1
Quiescent S2 NXPsO4o{U2mwYYPlJIF{e2G7 NYHIVG5wOzBizszN M4[3bmROW09? MnrJZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| M4TZeFIyPTF6OUG1
PC3 NF\LXGhCeG:ydH;zbZMh[XO|YYm= NWXCOGZSOjBizszN NFrZXVdFVVOR NXHES21vcW6mdXPld{BieG:ydH;zbZM> NWXxWpg6OjF5MEmxN|A>
Du145 NYHFW5F6SXCxcITvd4l{KGG|c3H5 MonPNlAh|ryP NVOzSVlvTE2VTx?= M1TYeYlv\HWlZYOgZZBweHSxc3nz Mn;jNlE4ODlzM{C=
LNCaP MVXBdI9xfG:|aYOgZZN{[Xl? NFzKT4UzOCEQvF2= Ml;KSG1UVw>? M4nybYlv\HWlZYOgZZBweHSxc3nz MUSyNVcxQTF|MB?=
LAPC-4 MV3BdI9xfG:|aYOgZZN{[Xl? MVmyNEDPxE1? MVnEUXNQ NVW2UnU1cW6mdXPld{BieG:ydH;zbZM> MWGyNVcxQTF|MB?=
LNCaP MnX4SpVv[3Srb36gZZN{[Xl? NI\OT5gzOCEQvF2= MVnEUXNQ M3vqNYRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? M2XZe|IyPzB7MUOw
LAPC-4 NEfhd4hHfW6ldHnvckBie3OjeR?= Mnj1NlAh|ryP NFziXHlFVVOR NVLtOlEy\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= MVmyNVcxQTF|MB?=
Kasumi-1 NX\kZmgzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGm0NXd,PTBizszN M4SxXWROW09? M3vubYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MlTDNlM{QTB3M{[=
SKNO-1 MmnwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{\KcJ42OCEQvF2= MYTEUXNQ M2XHOolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M3naeVI{OzlyNUO2
Kasumi-1 MYjLbY5ie2ViYYPzZZk> M3Pwd54yOCEQvF2= MVPEUXNQ NIG0eodz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MkfONlM{QTB3M{[=
SKNO-1 MV3LbY5ie2ViYYPzZZk> NVPLU3I1hjFyIN88US=> MmT3SG1UVw>? NWPtTHo4emWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NFHGbHUzOzN7MEWzOi=>
A549 NGLxSJVHfW6ldHnvckBie3OjeR?= M2jlV|ExKM7:TR?= NWDaToNGTE2VTx?= MVLlcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl MmnONlQ4PDZ3N{S=
NRK-52E NF\uZWVHfW6ldHnvckBie3OjeR?= NF;kPZcyOCEQvF2= MlrhSG1UVw>? MnXRbY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiU2TBWFMhdnWlbHXhdkB1emGwc3zvZ4F1cW:wIHHu[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEBkd2yuYXflckBKXiCjbnSg[oljem:wZXP0bY4> Mo\lNlUxQDhyMEK=
PC12 NVvwcYJXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mk\1glEzNjVizszN NVHOZnF1TE2VTx?= MVzwdoV3\W62czDUV2EucW6mdXPl[EBv\XW{aYTlJIZwem2jdHnvci=> M4LoeVI2OTJ6M{i2
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MEMM NF[wdFVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXX+NlAhyrWP NWrZdI5KTE2VTx?= NUHyXldLcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MlOwNlY6OjF3ME[=
MEMM MXrBdI9xfG:|aYOgZZN{[Xl? MlXMNVUhyrWP MXvEUXNQ NHTGN4VqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ MknDNlY6OjF3ME[=
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ZR-75-1 M174Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYexNEDPxE1? NYXkWlRtTE2VTx?= NYnsSHY5UUN3ME23PUBvVQ>? M1;aNVE5OzhzNES0
BT474 M1Pzfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYGxNEDPxE1? M17QVGROW09? MkC1TWM2OD16NjDuUS=> NVexVlBqOTh|OEG0OFQ>
HCC1954 MmewS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mnr1NVAh|ryP MorzSG1UVw>? M4\jW2lEPTB;MUG5JI5O M{G5eVE5OzhzNES0
MDA-MB-453 M2[3Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnewNVAh|ryP M{nTZmROW09? NVOxbWd6UUN3ME25O|Uhdk1? NWLlSHJmOTh|OEG0OFQ>
MDA-MB-468 NImyTItIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkXKNVAh|ryP MULEUXNQ NXvmU|J4UUN3ME2zNlA5KG6P NVvqWWtDOTh|OEG0OFQ>
SkBr3 NFTxWYhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUWxNEDPxE1? NX7NUmxlTE2VTx?= NID6cnVKSzVyPkGwMFAxOCCwTR?= MXixPFM5OTR2NB?=
MDA-MB-231 MoLPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmn5NVAh|ryP M{nBdGROW09? MU\JR|UxRjFyLECwNEBvVQ>? M{\rWVE5OzhzNES0
HCT116 NEjKN4tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3X0flExKM7:TR?= M125TGROW09? NIDvemlKSzVyPUW4N|Yhdk1? M4nMclE5OzhzNES0
HT29 Mm\vS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXrNVAh|ryP NGHGN2ZFVVOR MY\JR|UxRjFyLECwNEBvVQ>? MVKxPFM5OTR2NB?=
HFF M3rqNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF\QZ|YyOCEQvF2= NF3OTVRFVVOR MXnJR|UxRTd4MUWgcm0> Mmq3NVg{QDF2NES=
HN5 NFzMOpVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVWxNEDPxE1? MYLEUXNQ M2XuZmlEPTB-MUCsNFAxKG6P MWGxPFM5OTR2NB?=
786-0 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M375WVExKM7:TR?= NFK5bZNFVVOR NH76b3VKSzVyPUSwNFkhdk1? M2LmUFE5OzhzNES0
H157 MlHBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlTUNVAh|ryP MVvEUXNQ NYDSWJlJUUN3ME2yOlQzKG6P MYGxPFM5OTR2NB?=
NCI-H460 NH7TPWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPJU5YyOCEQvF2= NWS3NI96TE2VTx?= MU\JR|UxRjJuNUCwJI5O MmX5NVg{QDF2NES=
SKOV-3 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NITaeIwyOCEQvF2= M2fkN2ROW09? MmnWTWM2OD1{MUK2JI5O NHTaRpgyQDN6MUS0OC=>
OVCAR-3 NV31eJhST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3GyT|ExKM7:TR?= MWPEUXNQ NUDLO285UUN3ME2yPVE5KG6P NIfLZokyQDN6MUS0OC=>
BXPC3 Mme3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX2xNEDPxE1? MXfEUXNQ MkG1TWM2OD1|MUSxJI5O NV;OT3RNOTh|OEG0OFQ>
MiaPaCa NH3GPINIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkfINVAh|ryP MWPEUXNQ MnO4TWM2OD13NEOzJI5O NWL5UXJmOTh|OEG0OFQ>
PANC-1 Mmn2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXrXcGFqOTBizszN Mn7VSG1UVw>? NHTOV49KSzVyPUi2PFEhdk1? NHT3dXIyQDN6MUS0OC=>
LNCaP MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3nMcFExKM7:TR?= Mn;TSG1UVw>? NYjMVWc{UUN3ME2xOFchdk1? NWfPbZM3OTh|OEG0OFQ>
DU145 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVexNEDPxE1? MWfEUXNQ MmDHTWM2OD1|OEGyJI5O M13XUFE5OzhzNES0
PC3 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVfPeFN7OTBizszN NHXrTYdFVVOR NY\4PHdGUUN3ME6xNEwxODBibl2= NX72SoxoOTh|OEG0OFQ>
BT474 MnTVT4lv[XOnIHHzd4F6 MoHZNVAh|ryP MXjEUXNQ NG\OZldqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNkCgcm0> NWTJd|NjOTh|OEG0OFQ>
786-0 MX7LbY5ie2ViYYPzZZk> NGXLdVUyOCEQvF2= MWHEUXNQ M3HWZYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> NHzsfGoyQDN6MUS0OC=>
LNCaP NH;Pd2ZMcW6jc3WgZZN{[Xl? M4LE[|ExKM7:TR?= MnzqSG1UVw>? NVHRb3RNcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEOgcm0> MXOxPFM5OTR2NB?=
PC3 MoPhT4lv[XOnIHHzd4F6 NWHwOGFXOTBizszN NHnzdG9FVVOR M3fSbIlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR7IH7N NVWy[2lIOTh|OEG0OFQ>
KARPAS-231 M1;QV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW\FeVhOOTBizszN NY\NfINpTE2VTx?= NEPlNIlGSzVyPUSxJI5O MVexPVA3PDd|MB?=
CCRFSB MnHUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnjTNVAh|ryP Mn7tSG1UVw>? M4TwOGVEPTB;MUW1JI5O NVuwO5VOOTlyNkS3N|A>
SUP B15 NEDVSYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2\tdFExKM7:TR?= MmDKSG1UVw>? M4G1dGVEPTB;MUm3JI5O NITPepIyQTB4NEezNC=>
SD-1 M4L6dWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{fKeFExKM7:TR?= MW\EUXNQ NWTyb|ZtTUN3ME2zNlAhdk1? NV6ybYxbOTlyNkS3N|A>
RS4;11 MlHwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml7ZNVAh|ryP M4PGW2ROW09? NUizTI1tTUN3ME22OVQhdk1? NXrne2lqOTlyNkS3N|A>
MN-60 M1P5dGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXSxNEDPxE1? NWXMOXh[TE2VTx?= MlL4SWM2OD1|NkCyJI5O M4nPOVE6ODZ2N{Ow
Tanoue NVfofWFkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mmm4NVAh|ryP MkC5SG1UVw>? MVLFR|UxRTR3MUegcm0> MXWxPVA3PDd|MB?=
RCH-ACV NWrNToFjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2jqVFExKM7:TR?= NEPvTo1FVVOR NIezVJJGSzVyPUG1NkBvVQ>? MYCxPVA3PDd|MB?=
SEM M1ruNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYmxNEDPxE1? NXfXdFhGTE2VTx?= M4\4e2VEPTB;MkCyJI5O M{fmW|E6ODZ2N{Ow
KASUMI-2 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVyxNEDPxE1? NHrYbWtFVVOR M4WybGVEPTB;MkK1JI5O M{Xoe|E6ODZ2N{Ow
REH NGPOR5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4jPblExKM7:TR?= NYfUeWNYTE2VTx?= MkH4SWM2OD1{OEigcm0> M2S4cVE6ODZ2N{Ow
697 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnvuNVAh|ryP MVPEUXNQ NYHSO203TUN3ME2zN|ghdk1? NVrmcmlkOTlyNkS3N|A>
NALM-6 M2TzSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGjNWWEyOCEQvF2= M2jzb2ROW09? Mo[ySWM2OD12MkGgcm0> NYDqOG9OOTlyNkS3N|A>
MHH-CALL–3 Mkn3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEf1emUyOCEQvF2= M1PUeGROW09? M4XCdWVEPTB;OEGyJI5O MX:xPVA3PDd|MB?=
MHH-CALL–2 MljuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV;uRohuOTBizszN NFK2[ZNFVVOR M2rXe2VEPTB;MkGxOEBvVQ>? NFPVc3IyQTB4NEezNC=>
J.GAMMA-1 M1nhXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHPaNWoyOCEQvF2= M2DGOGROW09? MUPFR|UxRTZ3IH7N NV3rPYpkOTlyNkS3N|A>
JR45.01 Mon0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXqxNEDPxE1? M3jFSmROW09? M{XDNmVEPTB;Nkigcm0> M{L5PFE6ODZ2N{Ow
A3 MmnYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1LPb|ExKM7:TR?= Mn3NSG1UVw>? MorJSWM2OD14OTDuUS=> NGXJT3IyQTB4NEezNC=>
I 2.1 NXTOZok4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX[xNEDPxE1? MmrBSG1UVw>? M{DtTWVEPTB;N{Ogcm0> NYTBOWRQOTlyNkS3N|A>
MOLT-3 NFPx[5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnHhNVAh|ryP M1XjTWROW09? MYrFR|UxRTd2IH7N NG\T[2QyQTB4NEezNC=>
P116 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUnDbFNnOTBizszN NWO5TWFVTE2VTx?= NVnDOmpHTUN3ME23PEBvVQ>? MoPRNVkxPjR5M{C=
J.Cam1.6 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYOxNEDPxE1? MUHEUXNQ MoO0SWM2OD15OTDuUS=> NFrNbpcyQTB4NEezNC=>
I 9.2 NVTGfoFYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1\DflExKM7:TR?= Mm\NSG1UVw>? MoHWSWM2OD16MDDuUS=> MVixPVA3PDd|MB?=
LOUCY NUDYVmtFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYjZN|dkOTBizszN MmnaSG1UVw>? MoSySWM2OD1zMUegcm0> NVv2eYNnOTlyNkS3N|A>
J.RT3-T3.5 MlzmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1jSeVExKM7:TR?= M{ficGROW09? MnTiSWM2OD1zMkOgcm0> MlO3NVkxPjR5M{C=
800000 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlL5NVAh|ryP NWTGS2xYTE2VTx?= M4j1VGVEPTB;MU[zJI5O NWTlOWlyOTlyNkS3N|A>
Jurkat M2TDemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFO0THkyOCEQvF2= NGrCc2dFVVOR NIDHfnFGSzVyPUKyOUBvVQ>? M2TzV|E6ODZ2N{Ow
MOLT-4 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml3BNVAh|ryP M3zTNWROW09? MknLSWM2OD1{M{Kgcm0> Mnf1NVkxPjR5M{C=
Molt-16 MnvGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3Xm[lExKM7:TR?= NH7PcI1FVVOR M1;qdWVEPTB;MkSxJI5O NWrvS2NwOTlyNkS3N|A>
CEM/C3 NGO0WItIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXH5WnFNOTBizszN MmDpSG1UVw>? Ml\XSWM2OD1{NUegcm0> MV6xPVA3PDd|MB?=
CEM/C2 NIP4NG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnXoNVAh|ryP Mn:wSG1UVw>? MYXFR|UxRTJ5MTDuUS=> MXexPVA3PDd|MB?=
CCRFCEM MojsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1HwRVExKM7:TR?= MVTEUXNQ NWC4RYhnTUN3ME2zNlchdk1? M2fnTFE6ODZ2N{Ow
CEM/C1 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4XtWVExKM7:TR?= NFzQeIhFVVOR M1HIT2VEPTB;M{iyJI5O M{PmUVE6ODZ2N{Ow
SUPTI[VB] MkmzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF7WfVMyOCEQvF2= NYnQVZgzTE2VTx?= M{HiTWVEPTB;NkG5JI5O NEXld2MyQTB4NEezNC=>
CCRF–HSB-2 NFHW[FBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoHoNVAh|ryP NUXjWWNVTE2VTx?= NIf0ZVRGSzVyPUKxNVchdk1? NVXPSFJoOTlyNkS3N|A>
I 2.1 NHjpVVNCeG:ydH;zbZMh[XO|YYm= MVmxNEDPxE1? MV7EUXNQ NVvWNZB5cW6mdXPld{BieG:ydH;zbZM> M3LjeFE6ODZ2N{Ow
I 9.2 NXjJPYUySXCxcITvd4l{KGG|c3H5 MkPKNVAh|ryP Mk\uSG1UVw>? M1;BPYlv\HWlZYOgZZBweHSxc3nz NX;XVnUyOTlyNkS3N|A>
A3 M2OzVGFxd3C2b4Ppd{Bie3OjeR?= NUPnSpZCOTBizszN MkPUSG1UVw>? M{PRVolv\HWlZYOgZZBweHSxc3nz NWC0[JFQOTlyNkS3N|A>
RD M3L5[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYexNEDPxE1? MkiyTWM2OD5zMDFOwG0> MmPFNlA4PDB4MkO=
Rh41 M2jsWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\F[o8yOCEQvF2= MWnJR|UxRTN|Lkigcm0> M4HhelIxPzRyNkKz
Rh18 MlXLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3hZ3IyOCEQvF2= NX3XcFBlUUN3ME2zNFMhdk1? MlrUNlA4PDB4MkO=
Rh30 M{\xXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX7lcJlROTBizszN MXvJR|UxRTRwOEGg{txO MmrZNlA4PDB4MkO=
BT-12 MnSwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGe1cI0yOCEQvF2= MYLJR|UxRjFyIN88US=> MWSyNFc1ODZ{Mx?=
CHLA-266 MlziS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH;JUZMyOCEQvF2= NXXZVYlJUUN3ME2xMlIzKM7:TR?= M{PBWlIxPzRyNkKz
TC-71 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGqxZlgyOCEQvF2= NGiyO|VKSzVyPUKuOVIh|ryP NFn4PXYzODd2ME[yNy=>
CHLA-9 NHPyWmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYexNEDPxE1? M2rTOmlEPTB;NUmxJI5O NWHMRnRZOjB5NEC2NlM>
CHLA-10 M2nFdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXyxNEDPxE1? NHHpeWZKSzVyPUGwNkBvVQ>? M{fQVlIxPzRyNkKz
CHLA-258 MnLaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{TDR|ExKM7:TR?= MWPJR|UxRTFwMEWg{txO NYXJeGl[OjB5NEC2NlM>
GBM2 NXHiWVRFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVqxNEDPxE1? NEjMZppKSzVyPUmuNVUh|ryP NX;KTpJSOjB5NEC2NlM>
NB-1643 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWixNEDPxE1? NVPQb3RnUUN3ME21MlQh|ryP MWOyNFc1ODZ{Mx?=
NB-Ebc1 NUXiO4JQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfWeWIyOCEQvF2= MkG3TWM2OD5zMDFOwG0> MorMNlA4PDB4MkO=
CHLA-90 MkDUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYi2VHRWOTBizszN MkfiTWM2OD5zMDFOwG0> MVmyNFc1ODZ{Mx?=
CHLA-136 MknjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFjaVoUyOCEQvF2= M1jFRmlEPTB-MUCg{txO MYiyNFc1ODZ{Mx?=
NALM-6 M2Twfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX[xNEDPxE1? MkjuTWM2OD1{NkWgcm0> Mm\lNlA4PDB4MkO=
COG-LL-317 NVP6XHpvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVixNEDPxE1? M1jrWWlEPTB;Nj60PUBvVQ>? NWrtVpd6OjB5NEC2NlM>
RS4;11 NWGyRYxHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVmxNEDPxE1? M1\vb2lEPTB;MUS3JI5O MmCwNlA4PDB4MkO=
MOLT-4 NVHYcWc6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4Tvc|ExKM7:TR?= NVn3SGhLUUN3ME20NEBvVQ>? NGCwRpMzODd2ME[yNy=>
CCRF-CEM MmiyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY[xNEDPxE1? Mmj6TWM2OD1{Nkigcm0> M{HCZlIxPzRyNkKz
Kasumi-1 MlK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1\zSlExKM7:TR?= Mnu1TWM2OD1zMEegcm0> NULWN3lTOjB5NEC2NlM>
Karpas-299 Mm[zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUmxNEDPxE1? NWLITVVJUUN3ME2yMlk{KM7:TR?= NFHTdVQzODd2ME[yNy=>
Ramos-RA1 M{\2bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVm4VXdjOTBizszN M1;X[WlEPTB;Nz6zOUDPxE1? M2rVbFIxPzRyNkKz
H1299 MXjLbY5ie2ViYYPzZZk> M2TK[|ExKM7:TR?= M3LsW4lvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> MVSyNVkxQDZzNh?=

... 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 O=C1NC(=O)C(C1C2=C[NH]C3=C2C=CC=C3)C4=C[N]5CCCC6=CC=CC4=C56

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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

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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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