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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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 M4\l[GtqdmG|ZTDhd5NigQ>? M{fxO54yOCEQvF2= NVz3[49GcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NYX1eHZjOjB2OESwNVg>
HT29 MX;LbY5ie2ViYYPzZZk> M{X3Tp4yOCEQvF2= NYP2em1LcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MoC2NlA1QDRyMUi=
MDA-MB-231 NEjMSFFMcW6jc3WgZZN{[Xl? Mn\3glExKM7:TR?= MmDYbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NHLldY0zODR6NECxPC=>
NCI-H441 MnTVT4lv[XOnIHHzd4F6 NX[zPIVChjFyIN88US=> NUDTcJRicW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MUWyNFQ5PDBzOB?=
SK-MEL-28 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIG0d2Q{OyEQvF2= NF63dYhKSzVyPkOzJO69VQ>? M3fNeFIxPDh2MEG4
NCI-H661 MlzFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUSyfm1uOzNizszN M{HNOWlEPTB-M{Og{txO NX7tb4ZOOjB2OESwNVg>
NCI-H446 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LyR|M{KM7:TR?= M{TiWGlEPTB;NzFOwG0> NGnNVFkzODR6NECxPC=>
MDA-MB-231 M2fJPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnnBN|Mh|ryP M3fwZmlEPTB;MD61OUDPxE1? NEfIUJkzODR6NECxPC=>
DLD-1 M2O4Rmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmLpN|Mh|ryP NULTUWl5UUN3ME2wMlU{KM7:TR?= MXSyNFQ5PDBzOB?=
A549 NXnafGs2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYjzW|NuOzNizszN MV\JR|UxRTBwNUmg{txO Mn6xNlA1QDRyMUi=
SK-OV-3 M{jVRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Moj0N|Mh|ryP NVO0NWJNUUN3ME2wMlY3KM7:TR?= NVT4Nnc3OjB2OESwNVg>
NCI-H460 Ml70S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoXpN|Mh|ryP NGnRSHZKSzVyPUCuOkDPxE1? MUGyNFQ5PDBzOB?=
A375 NXv6UVgyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;tSVQ{OyEQvF2= NHHkZmlKSzVyPUCuOFIh|ryP Mo[zNlA1QDRyMUi=
NCI-H441 NUS5[oJ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXezN{DPxE1? MVnJR|UxRTBwMzFOwG0> NGLWPVUzODR6NECxPC=>
HT29 MnjPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVqzN{DPxE1? NYPDT3JZUUN3ME2wMlQ6KM7:TR?= M{fUWFIxPDh2MEG4
MKN-45 M1nwRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYmzN{DPxE1? MXzJR|UxRTBwNUig{txO MmTwNlA1QDRyMUi=
HT29 MYfBdI9xfG:|aYOgZZN{[Xl? MXX+NVAh|ryP M2jPbJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MlLJNlA1QDRyMUi=
MKN-45 MX7BdI9xfG:|aYOgZZN{[Xl? NHHTWJp,OTBizszN M{X6eZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NGPE[3AzODR6NECxPC=>
MDA-MB-231 MWTBdI9xfG:|aYOgZZN{[Xl? NFL6d|F,OTBizszN MXHtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw Mn3tNlA1QDRyMUi=
MDA-MB-231/TGL NWHJSlljT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFXQNpp,OTByIN88US=> M3eyWmdKPTB;MT6yJO69VQ>? NYLVe|BJOjJyMke2PVA>
1833/TGL NXG1dJZ7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfyglExOCEQvF2= NYX1R|BRT0l3ME2zMlch|ryP Mni1NlIxOjd4OUC=
EBC1 NX3Tc3lmS3m2b4TvfIlkyqCjc4PhfS=> MWD+NVAh|ryP MofrbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= NGLuU4MzOzV7OEK3Oi=>
SNU638 NV3QTI1FS3m2b4TvfIlkyqCjc4PhfS=> NX\TblFvhjFyIN88US=> NUWzTmZHcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> MV2yN|U6QDJ5Nh?=
A549 NFPkPWREgXSxdH;4bYPDqGG|c3H5 NFHtbml,OTBizszN MXfuc5Qh[W[oZXP0 MYCyN|U6QDJ5Nh?=
H460 NFO5[GFEgXSxdH;4bYPDqGG|c3H5 MmLFglExKM7:TR?= Ml7Qco91KGGoZnXjeC=> MljDNlM2QTh{N{[=
HCC827 NXzsW3dYS3m2b4TvfIlkyqCjc4PhfS=> M1;rUJ4yOCEQvF2= MnK0co91KGGoZnXjeC=> MYWyN|U6QDJ5Nh?=
A549 NWfqN5J2TnWwY4Tpc44h[XO|YYm= NIqyTJUyOCEQvF2= MUfkbZNzfXC2czDtbYNzd3S3YoXs[S=> MXuyN|U6QDJ5Nh?=
EBC1 NGPNdFBHfW6ldHnvckBie3OjeR?= MljqNVAh|ryP MX\kbZNzfXC2czDtbYNzd3S3YoXs[S=> M3rmWVI{PTl6Mke2
H460 NIfCTVNHfW6ldHnvckBie3OjeR?= M2HQfFExKM7:TR?= Mn\5bY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? NX7YTlVKOjV|MUOwNVA>
K562/VCR NVXkOXMxS3m2b4TvfIlkyqCjc4PhfS=> M1uxbJ4yOCEQvF2= MUfzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NYftVoVlOjV|MUOwNVA>
CEM/VBL MmrJR5l1d3SxeHnjxsBie3OjeR?= NF\WZVN,OTBizszN MYrzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NHzWd3AzPTNzM{CxNC=>
U266 NIW2Z5JEgXSxdH;4bYPDqGG|c3H5 M4rXVp4{KM7:TdMg MWDJR|UxRTFwMTFOwG0> MlmwNlU5OTByMUO=
OPM-2 MXLDfZRwfG:6aXRCpIF{e2G7 MU\+N{DPxE4EoB?= NHTnPJVKSzVyPUGuPEDPxE1? NVjjcZQyOjV6MUCwNVM>
MM.1S Mk\ZR5l1d3SxeHnjxsBie3OjeR?= MkX3glMh|ryPwrC= M4frW2lEPTB;MT62JO69VQ>? NGLZUGEzPThzMECxNy=>
MM.1R NUntOFg2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYKzJO69VcLi Mkf0bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml NFvDNVEzPThzMECxNy=>
RPMI-8226 NUHNW3JTS3m2b4TvfIlkyqCjc4PhfS=> NEDTe|Z,OyEQvF5CpC=> MnHzTWM2OD1yLkmg{txO MmjPNlU5OTByMUO=
ANBL-6 MmD2R5l1d3SxeHnjxsBie3OjeR?= NVTvd4ZVOSEQvF5CpC=> NWHrPYZKcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NGDPU3AzPThzMECxNy=>
ANLB-6/V10R NHG3WYdEgXSxdH;4bYPDqGG|c3H5 M3joN|Eh|ryPwrC= M3PZZolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MkDGNlU5OTByMUO=
KAS-6/1 MlrTR5l1d3SxeHnjxsBie3OjeR?= MnrJNUDPxE4EoB?= NFOwWFJqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NVG4UY1UOjV6MUCwNVM>
KAS-6/V10R NX3zenkxS3m2b4TvfIlkyqCjc4PhfS=> M{XUdVEh|ryPwrC= NGKxNZhqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MWWyOVgyODBzMx?=
KAS-6/R10R NIr0bYVEgXSxdH;4bYPDqGG|c3H5 NWSwfmhWOSEQvF5CpC=> MVvpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MkHONlU5OTByMUO=
8226/S NY\Z[4o5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV6zJO69VcLi M2HJR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MVuyOVgyODBzMx?=
8226/LR-5 M4XGNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlXSN{DPxE4EoB?= NUnZOnFFcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm MWqyOVgyODBzMx?=
Huh7 MUXDfZRwfG:6aXRCpIF{e2G7 NXrEZ4FvhjRwODFOwG3DqA>? NGjueJJFVVOR MXnJR|UxRTlwOTDuUS=> MUOyOlI2QTJ3MB?=
Hep3B MYrDfZRwfG:6aXRCpIF{e2G7 M1vpZZ41NjhizszNxsA> NG\UVYtFVVOR M2O2dmlEPTB;NES4Mlchdk1? MYSyOlI2QTJ3MB?=
HepG2 M{W0OmN6fG:2b4jpZ:Kh[XO|YYm= MWr+OE45KM7:TdMg M4i0WmROW09? NGfvUpRKSzVyPUGzPU44PyCwTR?= MVmyOlI2QTJ3MB?=
Chang M3y1fWN6fG:2b4jpZ:Kh[XO|YYm= NVzmeFhkhjRwODFOwG3DqA>? MWTEUXNQ MoLiTWM2OD12NEiuO{BvVQ>? MXuyOlI2QTJ3MB?=
Huh7 NX;2cWQxTnWwY4Tpc44h[XO|YYm= NHPDVYgyNjZizszNxsA> MoP5SG1UVw>? NF;mV3Bk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MXSyOlI2QTJ3MB?=
Hep3B M176b2Z2dmO2aX;uJIF{e2G7 MXOxMlYh|ryPwrC= MUHEUXNQ NHm5doxk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MnXUNlYzPTl{NUC=
HepG2 NUXCbpU4TnWwY4Tpc44h[XO|YYm= NGDqb2wyNjZizszNxsA> M{nxbGROW09? NVLHNIdk[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= MWGyOlI2QTJ3MB?=
Chang NVzlcHpXTnWwY4Tpc44h[XO|YYm= NYLRfHRkOS54IN88UeKh Mo\iSG1UVw>? MX;jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NYnlVW1GOjZ{NUmyOVA>
MHCC97L NV\MN3hST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2C3Op4yOCEQvF2= M4rtbWROW09? MoW0TWM2OD1|MUWgcm0> Mne4NlY1PTh7NUO=
MHCC97H NXr6UoR7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUnITXlshjFyIN88US=> MlzHSG1UVw>? NEjrToNKSzVyPUO2PQKBkSCwTR?= NXfUV|NPOjZ2NUi5OVM>
Huh7 NWHFSGcxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfqWHh,OTBizszN NYrsNHBETE2VTx?= NGHC[JVKSzVyPUK2OUBvVQ>? MV:yOlQ2QDl3Mx?=
HepG2 MlKwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4rMZ54yOCEQvF2= MnPWSG1UVw>? M4fwUmlEPTB;M{myJI5O MXeyOlQ2QDl3Mx?=
MHCC97L NYTrcnRKTnWwY4Tpc44h[XO|YYm= M33SblEh|ryPwrC= MVHEUXNQ MYHpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u MoTPNlY1PTh7NUO=
Huh7 MXPGeY5kfGmxbjDhd5NigQ>? MoqyNUDPxE4EoB?= MlXLSG1UVw>? NV70VZF5cW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? MXiyOlQ2QDl3Mx?=
MHCC97L MVrBdI9xfG:|aYOgZZN{[Xl? NGP0PGoyKM7:TdMg NHXZUm9FVVOR M4D0[4lv\HWlZYOgZZBweHSxc3nz MX2yOlQ2QDl3Mx?=
Huh7 NH3HV2VCeG:ydH;zbZMh[XO|YYm= M{HMWlEh|ryPwrC= NFXs[VZFVVOR MUnpcoR2[2W|IHHwc5B1d3Orcx?= MWqyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts M4fqR2tqdmG|ZTDhd5NigQ>? MUCyOUDPxE1? NIe0UYpFVVOR MWTy[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg NVzSSXJZOjB3M{SzOFU>
H23 MnfwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV2yOUDPxE1? M33yfmROW09? NYn4W|E{e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NHzxNYYzODV|NEO0OS=>
WM35 NHnHVYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHy5UoMyOCEQvF2= M3PPNWROW09? MVzzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MUeyNFU{PDN2NR?=
NIH 3T3 NVvIVFZQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml[5NVAh|ryP NFjtbmZFVVOR MVvkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= NIq3TYMzODV|NEO0OS=>
H838 M1PWUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1HRflExKM7:TR?= MYLEUXNQ M3TB[oRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NH;aXpYzODV|NEO0OS=>
H1395 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXixNEDPxE1? M4LTZ2ROW09? Mn7L[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MoPtNlA2OzR|NEW=
Quiescent S2 NI\5VJBMcW6jc3WgZZN{[Xl? M4DFbFMxKM7:TR?= NW[2WFhNTE2VTx?= MYfjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? MnzrNlE2OTh7MUW=
PC3 MYTBdI9xfG:|aYOgZZN{[Xl? MVyyNEDPxE1? Mk\5SG1UVw>? M4HsVIlv\HWlZYOgZZBweHSxc3nz Mnv6NlE4ODlzM{C=
Du145 NVmzZmRmSXCxcITvd4l{KGG|c3H5 M{jzO|IxKM7:TR?= NIXkdXJFVVOR M1LRVIlv\HWlZYOgZZBweHSxc3nz MX[yNVcxQTF|MB?=
LNCaP Mmj6RZBweHSxc3nzJIF{e2G7 MkD2NlAh|ryP NGXVdWlFVVOR NXvYOXBKcW6mdXPld{BieG:ydH;zbZM> M4DCcVIyPzB7MUOw
LAPC-4 NYjQcWNxSXCxcITvd4l{KGG|c3H5 MnjmNlAh|ryP MYfEUXNQ MlOzbY5lfWOnczDhdI9xfG:|aYO= M1zQV|IyPzB7MUOw
LNCaP MWXGeY5kfGmxbjDhd5NigQ>? MV:yNEDPxE1? NXHZSYROTE2VTx?= M4m1[YRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NXG5ZnJzOjF5MEmxN|A>
LAPC-4 M1fsU2Z2dmO2aX;uJIF{e2G7 NWXHWVBKOjBizszN M33C[2ROW09? MX7k[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ NVLabldMOjF5MEmxN|A>
Kasumi-1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH;WRXN,PTBizszN M1;rVmROW09? NGnZd3FqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NH;6e5czOzN7MEWzOi=>
SKNO-1 NWf4Now5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVH+OVAh|ryP MUnEUXNQ MlzFbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NI\vW3EzOzN7MEWzOi=>
Kasumi-1 MnzHT4lv[XOnIHHzd4F6 MlrBglExKM7:TR?= NXHFOWt1TE2VTx?= MkS1doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y M{LEdlI{OzlyNUO2
SKNO-1 NV3uWmdMU2mwYYPlJIF{e2G7 NWnXZpRphjFyIN88US=> M2fEbWROW09? Ml2zdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y MlOxNlM{QTB3M{[=
A549 NWr6PINvTnWwY4Tpc44h[XO|YYm= M1:5RlExKM7:TR?= NF3rPVlFVVOR NFfrO2FmdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm M2LnOlI1PzR4NUe0
NRK-52E M{X1SWZ2dmO2aX;uJIF{e2G7 NWXNOmVZOTBizszN NUX4dYRFTE2VTx?= M1zlN4lvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv MWOyOVA5QDByMh?=
PC12 MmGyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml\pglEzNjVizszN NHTrNZVFVVOR NIX5cZZxemW4ZX70d{BVW0FvaX7keYNm\CCwZYXybZRmKG[xcn3heIlwdg>? M3ziS|I2OTJ6M{i2
HPMCs NV\SNYt3TnWwY4Tpc44h[XO|YYm= M3\ubpJmfmW{c3XzJIVxcXSqZXzpZYwhfG9ibXXz[Y5kcHmvYXygeJJidnOrdHnvckBw\iCqdX3hckBx\XKrdH;u[YFtKG2nc3;0bIVtcWGuIHPlcIx{ NHzp[ogzPjB2NUe4NC=>
A549 M2L0WWZ2dmO2aX;uJIF{e2G7 M3vCdp42OCEQvF2= NGnlbWlFVVOR Mn7uZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> MYCyOlcyOTd2OB?=
RAW264.7 NXHs[GFSTnWwY4Tpc44h[XO|YYm= NEXhdoV,OzBizszN MU\EUXNQ NHPrW2Nz\WS3Y3XzJJBzdy2rbn\sZY1u[XSxcomg[4Vv\SCneIDy[ZN{cW:w NWrVNJp5OjZ5MUi1PFY>
MEMM M1voeWtqdmG|ZTDhd5NigQ>? MW[xOUDDvU1? MYPEUXNQ M3XPOIRm[3KnYYPld{Bi[2W2eXzheIlwdiCxZjDobZN1d26nIFiz NVHj[VVPOjZ7MkG1NFY>
MEMM MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLZVXp,OjBiwsXN NH7SVWNFVVOR NYXTd4ZbcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NXraSldUOjZ7MkG1NFY>
MEMM M3nwXWFxd3C2b4Ppd{Bie3OjeR?= MkPINVUhyrWP NWHWcIo{TE2VTx?= M1\QU4lv\HWlZYOgeIhmKHC{ZYPlcoNmKG:oIITo[UBieG:ydH;zbZMheHKxdHXpckwh[2ynYY\l[EBE[XOyYYPlMVM> MmLrNlY6OjF3ME[=
T47D MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn;yNVAh|ryP MnHESG1UVw>? NYfRVGgzUUN3ME23NkBvVQ>? M1PTV|E5OzhzNES0
ZR-75-1 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXnROo9bOTBizszN M{TJbWROW09? M3fhXWlEPTB;N{mgcm0> M{fkNFE5OzhzNES0
BT474 MkTzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGSwWm0yOCEQvF2= NF7NXVhFVVOR MYPJR|UxRTh4IH7N NYnTTGFWOTh|OEG0OFQ>
HCC1954 MmLLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFXnSVYyOCEQvF2= NX;NSJdlTE2VTx?= Mne3TWM2OD1zMUmgcm0> M4mzbVE5OzhzNES0
MDA-MB-453 NFvTc5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWixNEDPxE1? Mn7vSG1UVw>? NYT0UpcxUUN3ME25O|Uhdk1? NYrENGFvOTh|OEG0OFQ>
MDA-MB-468 M{WyXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV3OdI9VOTBizszN NHrSd3RFVVOR M1iwS2lEPTB;M{KwPEBvVQ>? M4rSblE5OzhzNES0
SkBr3 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkLsNVAh|ryP NI\sbGtFVVOR NIjGOZlKSzVyPkGwMFAxOCCwTR?= MYSxPFM5OTR2NB?=
MDA-MB-231 M1:zOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2PGS|ExKM7:TR?= NGn5WYdFVVOR MmLSTWM2OD5zMDywNFAhdk1? M{jp[|E5OzhzNES0
HCT116 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUL4[GRWOTBizszN NYq4SlV3TE2VTx?= NF3hdJlKSzVyPUW4N|Yhdk1? M4j5blE5OzhzNES0
HT29 MkHjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH7pUmcyOCEQvF2= NFPD[VVFVVOR MYfJR|UxRjFyLECwNEBvVQ>? NWXLSI82OTh|OEG0OFQ>
HFF M2TRW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml3mNVAh|ryP MYXEUXNQ NU\N[XdyUUN3ME23OlE2KG6P MmK4NVg{QDF2NES=
HN5 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGPiSnAyOCEQvF2= NUnyZ4lGTE2VTx?= NEjZUnBKSzVyPkGwMFAxOCCwTR?= MnjSNVg{QDF2NES=
786-0 M2i0fWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkfWNVAh|ryP MUnEUXNQ M33pV2lEPTB;NECwPUBvVQ>? NHizR2syQDN6MUS0OC=>
H157 NXjGXo45T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUDRUIozOTBizszN NIfCUWZFVVOR NH3QXYZKSzVyPUK2OFIhdk1? NEH4bpUyQDN6MUS0OC=>
NCI-H460 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVnzNWR6OTBizszN Mn;3SG1UVw>? MUPJR|UxRjJuNUCwJI5O NVnXVVNpOTh|OEG0OFQ>
SKOV-3 NEDyWIVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFf0dWMyOCEQvF2= NWD4[nJrTE2VTx?= NHrVe5ZKSzVyPUKxNlYhdk1? M3H4N|E5OzhzNES0
OVCAR-3 MnnxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXOxNEDPxE1? M4Sz[2ROW09? MW\JR|UxRTJ7MUigcm0> M3zwSVE5OzhzNES0
BXPC3 MmHQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mlr5NVAh|ryP MUfEUXNQ NHy2cVRKSzVyPUOxOFEhdk1? NX3kPJFEOTh|OEG0OFQ>
MiaPaCa NY[1bII4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHOyU3EyOCEQvF2= NFj6d|hFVVOR MVfJR|UxRTV2M{Ogcm0> MkKxNVg{QDF2NES=
PANC-1 NFj1VIxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEHrNI8yOCEQvF2= MlLxSG1UVw>? NXvFcWZ3UUN3ME24OlgyKG6P MlnyNVg{QDF2NES=
LNCaP NX7vVmQxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVPBeJdwOTBizszN MUXEUXNQ M{XNe2lEPTB;MUS3JI5O MljDNVg{QDF2NES=
DU145 M2e1eGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXmxNEDPxE1? NELzPVRFVVOR MYfJR|UxRTN6MUKgcm0> NYSzWHRVOTh|OEG0OFQ>
PC3 M3GwZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlGxNVAh|ryP NEnoXJRFVVOR Mn\CTWM2OD5zMDywNFAhdk1? M1q3SlE5OzhzNES0
BT474 NHfoZlZMcW6jc3WgZZN{[Xl? Mn7lNVAh|ryP MWjEUXNQ M3HWbYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF4MDDuUS=> MoXrNVg{QDF2NES=
786-0 MoXFT4lv[XOnIHHzd4F6 NITuSZkyOCEQvF2= NEHjXVFFVVOR M{i2fYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> M4nHdlE5OzhzNES0
LNCaP M1e1TWtqdmG|ZTDhd5NigQ>? MmX6NVAh|ryP NV;QV40xTE2VTx?= MYjpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1OyCwTR?= NIXYSWEyQDN6MUS0OC=>
PC3 NWf5PVd7U2mwYYPlJIF{e2G7 M4fuXVExKM7:TR?= M{W1eGROW09? Mlr1bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDlibl2= NIjLepoyQDN6MUS0OC=>
KARPAS-231 NELZe4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3e2ZVExKM7:TR?= NHvnWVVFVVOR NYHneFgzTUN3ME20NUBvVQ>? NYfnV246OTlyNkS3N|A>
CCRFSB NIPmeG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rSSFExKM7:TR?= NHfNfmhFVVOR Mn3lSWM2OD1zNUWgcm0> NFu3WHgyQTB4NEezNC=>
SUP B15 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXuxNEDPxE1? MnzzSG1UVw>? NX\4ToJITUN3ME2xPVchdk1? NHPPXmMyQTB4NEezNC=>
SD-1 NVPDTItxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWOxNEDPxE1? MmLrSG1UVw>? MlXzSWM2OD1|MkCgcm0> MXqxPVA3PDd|MB?=
RS4;11 M2LkXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYexNEDPxE1? NHHwbZNFVVOR M4LFc2VEPTB;NkW0JI5O M2CzdFE6ODZ2N{Ow
MN-60 M3:0Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIDSTXMyOCEQvF2= M2q4Z2ROW09? NUP5do84TUN3ME2zOlAzKG6P MYSxPVA3PDd|MB?=
Tanoue Mmf3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFjEVHUyOCEQvF2= M2Tq[GROW09? MVLFR|UxRTR3MUegcm0> MYexPVA3PDd|MB?=
RCH-ACV M4LJTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnP3NVAh|ryP MYfEUXNQ NEPQZopGSzVyPUG1NkBvVQ>? NXHIUFdXOTlyNkS3N|A>
SEM NYrSR|FbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MorENVAh|ryP NFrLdGNFVVOR Mn;tSWM2OD1{MEKgcm0> MWexPVA3PDd|MB?=
KASUMI-2 M2HHRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX\u[FZvOTBizszN MVvEUXNQ MVnFR|UxRTJ{NTDuUS=> MYixPVA3PDd|MB?=
REH NHv2Z2JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVXyUnR1OTBizszN NIDwNHpFVVOR NWq3NJBqTUN3ME2yPFghdk1? MWexPVA3PDd|MB?=
697 Mnf6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFL1V|kyOCEQvF2= M2HT[mROW09? NEOyN2FGSzVyPUOzPEBvVQ>? NFTUWVAyQTB4NEezNC=>
NALM-6 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2H5WFExKM7:TR?= MmG2SG1UVw>? M2nOSWVEPTB;NEKxJI5O MkL4NVkxPjR5M{C=
MHH-CALL–3 NULaSHp2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{n2cFExKM7:TR?= MnLCSG1UVw>? Mk[2SWM2OD16MUKgcm0> NWHvc4NGOTlyNkS3N|A>
MHH-CALL–2 NFuydFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkXFNVAh|ryP M4LIRWROW09? M1rFV2VEPTB;MkGxOEBvVQ>? MX:xPVA3PDd|MB?=
J.GAMMA-1 MlnIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEDlbpUyOCEQvF2= M4mzOGROW09? M4rpXWVEPTB;NkWgcm0> NXjhcFVSOTlyNkS3N|A>
JR45.01 NGHXZ2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHvJb4kyOCEQvF2= MVXEUXNQ MoTpSWM2OD14ODDuUS=> NEKxW5gyQTB4NEezNC=>
A3 NHPzTlNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoK2NVAh|ryP Ml7ESG1UVw>? MmT1SWM2OD14OTDuUS=> NYHDSXk5OTlyNkS3N|A>
I 2.1 NXm0dFl{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV2xNEDPxE1? NIjYeoFFVVOR MlzzSWM2OD15MzDuUS=> M3nmNVE6ODZ2N{Ow
MOLT-3 MnTHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXmxNEDPxE1? NEC1fVJFVVOR M2PGUGVEPTB;N{Sgcm0> MXmxPVA3PDd|MB?=
P116 NWXCcmg5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVPKSHlyOTBizszN M2rRcWROW09? MYLFR|UxRTd6IH7N MkjJNVkxPjR5M{C=
J.Cam1.6 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVOxNEDPxE1? NEXPeZJFVVOR MnyySWM2OD15OTDuUS=> NXXvUY9EOTlyNkS3N|A>
I 9.2 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXaNVAh|ryP M4\jW2ROW09? M4TmfmVEPTB;OECgcm0> NGfucm0yQTB4NEezNC=>
LOUCY NH\wSmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH36[pEyOCEQvF2= NEjCTWhFVVOR MmfVSWM2OD1zMUegcm0> NILweZYyQTB4NEezNC=>
J.RT3-T3.5 MoCxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml7JNVAh|ryP NWP4UFlyTE2VTx?= Mnm1SWM2OD1zMkOgcm0> MkXCNVkxPjR5M{C=
800000 NYPFTHJRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXrfWhwOTBizszN M{DVe2ROW09? MUXFR|UxRTF4MzDuUS=> MVmxPVA3PDd|MB?=
Jurkat MnzCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{SzfVExKM7:TR?= Mm[wSG1UVw>? MXnFR|UxRTJ{NTDuUS=> M{[5XVE6ODZ2N{Ow
MOLT-4 M2X0bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUC2O3AyOTBizszN NEnlUVFFVVOR NUD5T3hFTUN3ME2yN|Ihdk1? MYSxPVA3PDd|MB?=
Molt-16 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHzNVAh|ryP M4L1UmROW09? MmTFSWM2OD1{NEGgcm0> NWnG[VJHOTlyNkS3N|A>
CEM/C3 NIHRcFZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3LYWlExKM7:TR?= NIXXZ5JFVVOR NXu0XI5lTUN3ME2yOVchdk1? MVWxPVA3PDd|MB?=
CEM/C2 NGHzbWdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGLKV2YyOCEQvF2= MnywSG1UVw>? MWXFR|UxRTJ5MTDuUS=> MW[xPVA3PDd|MB?=
CCRFCEM NIHUTFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3exSVExKM7:TR?= MlnPSG1UVw>? NYm1VXoyTUN3ME2zNlchdk1? MXSxPVA3PDd|MB?=
CEM/C1 NFH6UHRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkLYNVAh|ryP MYDEUXNQ M1ztVWVEPTB;M{iyJI5O NVX0UYdTOTlyNkS3N|A>
SUPTI[VB] NVTwNFdRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlfDNVAh|ryP MnvmSG1UVw>? M1HHdmVEPTB;NkG5JI5O M4raTVE6ODZ2N{Ow
CCRF–HSB-2 M1HUcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYS5VVhoOTBizszN M3\1UWROW09? M{XFPWVEPTB;MkGxO{BvVQ>? Mo\UNVkxPjR5M{C=
I 2.1 NIHvXWJCeG:ydH;zbZMh[XO|YYm= NX3Ve3pTOTBizszN NX\TVms5TE2VTx?= NWf2VJhvcW6mdXPld{BieG:ydH;zbZM> M2LZeVE6ODZ2N{Ow
I 9.2 NUH5UYR7SXCxcITvd4l{KGG|c3H5 Ml24NVAh|ryP MXTEUXNQ NHnmS3NqdmS3Y3XzJIFxd3C2b4Ppdy=> MYOxPVA3PDd|MB?=
A3 MmG3RZBweHSxc3nzJIF{e2G7 NH35ZYEyOCEQvF2= MV\EUXNQ NF72WVRqdmS3Y3XzJIFxd3C2b4Ppdy=> M1zIeFE6ODZ2N{Ow
RD MnXjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVixNEDPxE1? NGrPN3BKSzVyPkGwJO69VQ>? Mn:5NlA4PDB4MkO=
Rh41 NXfmOW9OT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2T6NFExKM7:TR?= NY\qNIRsUUN3ME2zN{45KG6P MVGyNFc1ODZ{Mx?=
Rh18 M3f6PWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWSxNEDPxE1? NEHKbGRKSzVyPUOwN{BvVQ>? Mn3CNlA4PDB4MkO=
Rh30 NGHUZnZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmDzNVAh|ryP Ml34TWM2OD12LkixJO69VQ>? MWWyNFc1ODZ{Mx?=
BT-12 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1fodlExKM7:TR?= NHzZNWFKSzVyPkGwJO69VQ>? MUeyNFc1ODZ{Mx?=
CHLA-266 NUjBbZRIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGT4XooyOCEQvF2= MkjNTWM2OD1zLkKyJO69VQ>? MXSyNFc1ODZ{Mx?=
TC-71 NUnmbGl6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3rGNlExKM7:TR?= NHrReHlKSzVyPUKuOVIh|ryP M{juUVIxPzRyNkKz
CHLA-9 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NG\CWVgyOCEQvF2= MWfJR|UxRTV7MTDuUS=> MXOyNFc1ODZ{Mx?=
CHLA-10 M3;Ubmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NILBNGMyOCEQvF2= MoT2TWM2OD1zMEKgcm0> NVm2fJlKOjB5NEC2NlM>
CHLA-258 M{K5UWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHroPYEyOCEQvF2= M1jMPGlEPTB;MT6wOUDPxE1? M1[1OVIxPzRyNkKz
GBM2 NF6yfJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYCxNEDPxE1? NF7WVlZKSzVyPUmuNVUh|ryP MkLMNlA4PDB4MkO=
NB-1643 NXTFWGVDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW[xNEDPxE1? NHzib5JKSzVyPUWuOEDPxE1? MnHlNlA4PDB4MkO=
NB-Ebc1 MnXhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLBXmVHOTBizszN NIXkVm9KSzVyPkGwJO69VQ>? MVKyNFc1ODZ{Mx?=
CHLA-90 NW\OVFUzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3jSblExKM7:TR?= MnPXTWM2OD5zMDFOwG0> NV3Db4lIOjB5NEC2NlM>
CHLA-136 NGHC[pdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3qw[FExKM7:TR?= MUHJR|UxRjFyIN88US=> NEnycZIzODd2ME[yNy=>
NALM-6 M3e1ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4DoSlExKM7:TR?= NFzseG5KSzVyPUK2OUBvVQ>? NUntPGR5OjB5NEC2NlM>
COG-LL-317 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHT6S3gyOCEQvF2= MWHJR|UxRTZwNEmgcm0> MlzINlA4PDB4MkO=
RS4;11 MnvpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NW[4WlFFOTBizszN MYTJR|UxRTF2NzDuUS=> NFfzVm8zODd2ME[yNy=>
MOLT-4 M{L4fGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1W3d|ExKM7:TR?= MY\JR|UxRTRyIH7N MXiyNFc1ODZ{Mx?=
CCRF-CEM MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLzeYEyOCEQvF2= NHrYVHhKSzVyPUK2PEBvVQ>? MWqyNFc1ODZ{Mx?=
Kasumi-1 NHjabIJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXv4TGNvOTBizszN Mlr2TWM2OD1zMEegcm0> NEnlPWYzODd2ME[yNy=>
Karpas-299 NIX1c49Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLiUWY3OTBizszN NGXxXpNKSzVyPUKuPVMh|ryP NWHZVJR[OjB5NEC2NlM>
Ramos-RA1 NH;GSW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn3rNVAh|ryP NVz3cWVtUUN3ME23MlM2KM7:TR?= NYH6OnI5OjB5NEC2NlM>
H1299 NGfjZnJMcW6jc3WgZZN{[Xl? M{K2dVExKM7:TR?= NWXvPXVNcW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? MlrUNlE6ODh4MU[=

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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
  • 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 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01749384 Completed Solid Neoplasm National Cancer Institute (NCI) December 6 2012 Phase 1
NCT01755767 Completed Hepatocellular Carcinoma Daiichi Sankyo Inc.|ArQule December 27 2012 Phase 3
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 25 2011 Phase 1
NCT01654965 Completed Adult Solid Neoplasm National Cancer Institute (NCI) July 24 2012 Phase 1
NCT02608411 Terminated 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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

  • Answer:

    S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.

c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID