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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Cited by 12 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 NWjKW3czU2mwYYPlJIF{e2G7 M2HZSZ4yOCEQvF2= MoHBbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= M2H4V|IxPDh2MEG4
HT29 M4XzU2tqdmG|ZTDhd5NigQ>? Ml\NglExKM7:TR?= NWDBcJF3cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NHfXSVkzODR6NECxPC=>
MDA-MB-231 MX7LbY5ie2ViYYPzZZk> MmrMglExKM7:TR?= NFnpXXVqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MX:yNFQ5PDBzOB?=
NCI-H441 Ml71T4lv[XOnIHHzd4F6 MUT+NVAh|ryP MoHYbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NULmdYp{OjB2OESwNVg>
SK-MEL-28 NH;HcJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYqzN{DPxE1? M{LORmlEPTB-M{Og{txO Mly4NlA1QDRyMUi=
NCI-H661 Mkj4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV[zN{DPxE1? MmrMTWM2OD5|MzFOwG0> NH65WY4zODR6NECxPC=>
NCI-H446 NIjYV2hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPKdoQ{OyEQvF2= MYTJR|UxRTdizszN Mni5NlA1QDRyMUi=
MDA-MB-231 MlvtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjUNY1VOzNizszN M4rC[2lEPTB;MD61OUDPxE1? NFr5Z|UzODR6NECxPC=>
DLD-1 MmK4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXtN|Mh|ryP M2XWVGlEPTB;MD61N{DPxE1? NInGenozODR6NECxPC=>
A549 NHLlR2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4rtRVM{KM7:TR?= M3qxe2lEPTB;MD61PUDPxE1? M4TJZlIxPDh2MEG4
SK-OV-3 MoHuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M324PFM{KM7:TR?= NHrycGhKSzVyPUCuOlYh|ryP M3jFZlIxPDh2MEG4
NCI-H460 MkDLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFrSSlU{OyEQvF2= M4LkOWlEPTB;MD62JO69VQ>? MYWyNFQ5PDBzOB?=
A375 NYfCWXRkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVHqPGp2OzNizszN MkG0TWM2OD1yLkSyJO69VQ>? NX[wbpZQOjB2OESwNVg>
NCI-H441 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXizN{DPxE1? M4DYbWlEPTB;MD6zJO69VQ>? M{fXeFIxPDh2MEG4
HT29 NES5bnFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVO5[YZzOzNizszN NE\YdWxKSzVyPUCuOFkh|ryP NH;ZdXMzODR6NECxPC=>
MKN-45 NE\0dmdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGm4b40{OyEQvF2= NFTwbHhKSzVyPUCuOVgh|ryP MmLzNlA1QDRyMUi=
HT29 MlroRZBweHSxc3nzJIF{e2G7 Mof3glExKM7:TR?= M1;OOJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= NV:2eWM4OjB2OESwNVg>
MKN-45 MXjBdI9xfG:|aYOgZZN{[Xl? M3n6VJ4yOCEQvF2= M4TmPJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= M3naSlIxPDh2MEG4
MDA-MB-231 NWjlN|dlSXCxcITvd4l{KGG|c3H5 M2DUT54yOCEQvF2= NGXOO|lud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu NGeyO5UzODR6NECxPC=>
MDA-MB-231/TGL Mnj5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvDTmF,OTByIN88US=> NHf0UYtIUTVyPUGuNkDPxE1? M2HoOlIzODJ5Nkmw
1833/TGL MmHhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorhglExOCEQvF2= MVnHTVUxRTNwNzFOwG0> MkX5NlIxOjd4OUC=
EBC1 NHfuRphEgXSxdH;4bYPDqGG|c3H5 NGjyR4N,OTBizszN MlHQbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= Ml3yNlM2QTh{N{[=
SNU638 NX:2XotCS3m2b4TvfIlkyqCjc4PhfS=> Mm\HglExKM7:TR?= MmLRbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= NHT3b3kzOzV7OEK3Oi=>
A549 NETDTVhEgXSxdH;4bYPDqGG|c3H5 M{DXdZ4yOCEQvF2= M4\HWo5wfCCjZn\lZ5Q> NXj0UIhNOjN3OUiyO|Y>
H460 MVTDfZRwfG:6aXRCpIF{e2G7 M{DQZZ4yOCEQvF2= MlL3co91KGGoZnXjeC=> NEDCfZozOzV7OEK3Oi=>
HCC827 NHHidWtEgXSxdH;4bYPDqGG|c3H5 MlrBglExKM7:TR?= M4\WfY5wfCCjZn\lZ5Q> NV6xTJBTOjN3OUiyO|Y>
A549 NFrlcnJHfW6ldHnvckBie3OjeR?= MX2xNEDPxE1? NFvze4JlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? MkKyNlM2QTh{N{[=
EBC1 NWjtWIh7TnWwY4Tpc44h[XO|YYm= NFPad|EyOCEQvF2= NWPsWHhu\Gm|coXweJMhdWmlcn;0eYJ2dGV? NVzoPFZuOjN3OUiyO|Y>
H460 M4XPXmZ2dmO2aX;uJIF{e2G7 NUHwc|BEOTBizszN NIrzUGRqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w NW\KS2E2OjV|MUOwNVA>
K562/VCR NUPaUVE6S3m2b4TvfIlkyqCjc4PhfS=> MWf+NVAh|ryP NU\0T4tQe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MoLiNlU{OTNyMUC=
CEM/VBL MnjkR5l1d3SxeHnjxsBie3OjeR?= NG\5bWJ,OTBizszN NXTS[pd7e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MoTuNlU{OTNyMUC=
U266 M1TkVWN6fG:2b4jpZ:Kh[XO|YYm= M1nJdZ4{KM7:TdMg NVLxTWd4UUN3ME2xMlEh|ryP M1TOeFI2QDFyMEGz
OPM-2 Mkj5R5l1d3SxeHnjxsBie3OjeR?= NUjD[JVqhjNizszNxsA> M3LDVmlEPTB;MT64JO69VQ>? MkC3NlU5OTByMUO=
MM.1S NULJUJp7S3m2b4TvfIlkyqCjc4PhfS=> Mm\hglMh|ryPwrC= NYnVSoc1UUN3ME2xMlYh|ryP MmfxNlU5OTByMUO=
MM.1R NVn5foFoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXGzJO69VcLi Mmf5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml MnmwNlU5OTByMUO=
RPMI-8226 MoLER5l1d3SxeHnjxsBie3OjeR?= MWD+N{DPxE4EoB?= MnjPTWM2OD1yLkmg{txO NETyZWozPThzMECxNy=>
ANBL-6 NWfHfG51S3m2b4TvfIlkyqCjc4PhfS=> M4jZ[FEh|ryPwrC= NYHQemJ5cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NGL3[IszPThzMECxNy=>
ANLB-6/V10R NFnET4dEgXSxdH;4bYPDqGG|c3H5 M37IOlEh|ryPwrC= NUPCVI5tcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MlHINlU5OTByMUO=
KAS-6/1 NX\KVJpiS3m2b4TvfIlkyqCjc4PhfS=> MlTQNUDPxE4EoB?= MXnpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MkG1NlU5OTByMUO=
KAS-6/V10R M2nmdWN6fG:2b4jpZ:Kh[XO|YYm= M3jpb|Eh|ryPwrC= MkHIbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NFO5TJYzPThzMECxNy=>
KAS-6/R10R NGTIPWJEgXSxdH;4bYPDqGG|c3H5 MlHONUDPxE4EoB?= NG[4R5ZqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> M{\ndFI2QDFyMEGz
8226/S NWnMdGtWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVezJO69VcLi M{jKSolvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> NWKwbVJkOjV6MUCwNVM>
8226/LR-5 NH3YR|lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2nPO|Mh|ryPwrC= NFuyVpJqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> NFvqRZMzPThzMECxNy=>
Huh7 Ml3nR5l1d3SxeHnjxsBie3OjeR?= M3e2cZ41NjhizszNxsA> NIflXFFFVVOR MkDMTWM2OD17Lkmgcm0> MnX2NlYzPTl{NUC=
Hep3B M4DOXGN6fG:2b4jpZ:Kh[XO|YYm= NWTqfmwzhjRwODFOwG3DqA>? M17jWWROW09? NXXHVXE3UUN3ME20OFgvPyCwTR?= MYmyOlI2QTJ3MB?=
HepG2 MlT0R5l1d3SxeHnjxsBie3OjeR?= NG[3UoN,PC56IN88UeKh NH3BWHNFVVOR MUXJR|UxRTF|OT63O{BvVQ>? M4iyOVI3OjV7MkWw
Chang MofiR5l1d3SxeHnjxsBie3OjeR?= MW\+OE45KM7:TdMg M3znNGROW09? NEjGeFBKSzVyPUS0PE44KG6P MlvnNlYzPTl{NUC=
Huh7 MUfGeY5kfGmxbjDhd5NigQ>? NH3UTpcyNjZizszNxsA> MVzEUXNQ M{KxVoNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MWOyOlI2QTJ3MB?=
Hep3B M3vmUWZ2dmO2aX;uJIF{e2G7 MnS1NU43KM7:TdMg NFr6dotFVVOR MWDjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 Mn76NlYzPTl{NUC=
HepG2 NH7yT|hHfW6ldHnvckBie3OjeR?= NIK5WpoyNjZizszNxsA> Ml7MSG1UVw>? MV7jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M{TZcVI3OjV7MkWw
Chang M{DxXWZ2dmO2aX;uJIF{e2G7 MnHyNU43KM7:TdMg NYLUS5V{TE2VTx?= NWX3SopF[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= MmnqNlYzPTl{NUC=
MHCC97L M{HE[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVX+NVAh|ryP NWDoOVZwTE2VTx?= MYPJR|UxRTNzNTDuUS=> NF\CdIwzPjR3OEm1Ny=>
MHCC97H MlGxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPuglExKM7:TR?= MYPEUXNQ MlvrTWM2OD1|NklihKkhdk1? Mnr1NlY1PTh7NUO=
Huh7 NXHm[JpoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2H1dJ4yOCEQvF2= Mn\qSG1UVw>? M1fCVWlEPTB;Mk[1JI5O MlO3NlY1PTh7NUO=
HepG2 NVHVb|k{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX3nUFlDhjFyIN88US=> MnjpSG1UVw>? MlHyTWM2OD1|OUKgcm0> NEHQT|QzPjR3OEm1Ny=>
MHCC97L M{Pp[2Z2dmO2aX;uJIF{e2G7 MVmxJO69VcLi MlG0SG1UVw>? NGeyNlJqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v NXLre41HOjZ2NUi5OVM>
Huh7 MmXWSpVv[3Srb36gZZN{[Xl? M1jV[|Eh|ryPwrC= NVr4TGI5TE2VTx?= NXrzd4VTcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NHfNO28zPjR3OEm1Ny=>
MHCC97L M{DZWGFxd3C2b4Ppd{Bie3OjeR?= M{S0NFEh|ryPwrC= NX\6cmR1TE2VTx?= NEn4OHRqdmS3Y3XzJIFxd3C2b4Ppdy=> Mn\PNlY1PTh7NUO=
Huh7 NEHBW2ZCeG:ydH;zbZMh[XO|YYm= M3u0[VEh|ryPwrC= NILYeotFVVOR NXrBNJFMcW6mdXPld{BieG:ydH;zbZM> NYG5ZVhNOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts MoDUT4lv[XOnIHHzd4F6 NXXlR45FOjVizszN MWXEUXNQ NEnZ[|lz\WS3Y3XzJGhqe3SxbnWgTFMh[W6mIFi0JIFk\XS7bHH0bY9vKGyndnXsd:Kh NHOwOXAzODV|NEO0OS=>
H23 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWCyOUDPxE1? NHPQVXRFVVOR MmTCd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MYiyNFU{PDN2NR?=
WM35 M4LD[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEjwT4EyOCEQvF2= MWjEUXNQ MYPzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MY[yNFU{PDN2NR?=
NIH 3T3 MmrRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml;4NVAh|ryP Mlf5SG1UVw>? MYjkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= M4PX[FIxPTN2M{S1
H838 MlHuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnjSNVAh|ryP M{PBOWROW09? M{LpXIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> Mn2zNlA2OzR|NEW=
H1395 MoD0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3FbI0yOCEQvF2= MVLEUXNQ M2H3Z4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NF;UO3UzODV|NEO0OS=>
Quiescent S2 NGP4bnVMcW6jc3WgZZN{[Xl? MVuzNEDPxE1? NH7LUlJFVVOR MnvrZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| M3HE[VIyPTF6OUG1
PC3 MV7BdI9xfG:|aYOgZZN{[Xl? NEWwVWwzOCEQvF2= M1rGb2ROW09? NYDKcmd{cW6mdXPld{BieG:ydH;zbZM> MVqyNVcxQTF|MB?=
Du145 NHPCcGNCeG:ydH;zbZMh[XO|YYm= NWDrfZl[OjBizszN MXvEUXNQ NXOzRXh4cW6mdXPld{BieG:ydH;zbZM> M3;tOFIyPzB7MUOw
LNCaP Mo\uRZBweHSxc3nzJIF{e2G7 NE\MNnozOCEQvF2= M3PWVmROW09? MUDpcoR2[2W|IHHwc5B1d3Orcx?= NE\0bpYzOTdyOUGzNC=>
LAPC-4 MWXBdI9xfG:|aYOgZZN{[Xl? NVzMcGVTOjBizszN MlPVSG1UVw>? NE\0WY9qdmS3Y3XzJIFxd3C2b4Ppdy=> NVHwPIhEOjF5MEmxN|A>
LNCaP MnS2SpVv[3Srb36gZZN{[Xl? NFHjfIwzOCEQvF2= M1XYPWROW09? MmTL[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NWHxbJJJOjF5MEmxN|A>
LAPC-4 NUTWcHkyTnWwY4Tpc44h[XO|YYm= MYGyNEDPxE1? MkLOSG1UVw>? NFfBeFVl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NF;UZY0zOTdyOUGzNC=>
Kasumi-1 M2rOcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYjIXZFshjVyIN88US=> MVvEUXNQ NWrBNHY3cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M2H0SFI{OzlyNUO2
SKNO-1 Mmi1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVj+OVAh|ryP MkTySG1UVw>? MV;pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MV6yN|M6ODV|Nh?=
Kasumi-1 MXvLbY5ie2ViYYPzZZk> M{nWcZ4yOCEQvF2= MljXSG1UVw>? NXyzOI9jemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z MorhNlM{QTB3M{[=
SKNO-1 Mn[4T4lv[XOnIHHzd4F6 MYf+NVAh|ryP MV;EUXNQ NF;SNVVz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> NIDJcokzOzN7MEWzOi=>
A549 MXXGeY5kfGmxbjDhd5NigQ>? MV:xNEDPxE1? M3ywTmROW09? M4jsSYVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> NXLVdoFiOjR5NE[1O|Q>
NRK-52E MYnGeY5kfGmxbjDhd5NigQ>? M3;rNFExKM7:TR?= MV;EUXNQ NEXmZoFqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDTWGFVOyCwdXPs[YFzKHS{YX7zcI9k[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKFSJRj5OtlEtKGOxbHzh[4VvKEmYIHHu[EBncWK{b37lZ5Rqdg>? NWjPbmpCOjVyOEiwNFI>
PC12 NIq0dIpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1my[54yOi53IN88US=> NXj5R5hETE2VTx?= MmDrdJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> MoTmNlUyOjh|OE[=
HPMCs NHLhbppHfW6ldHnvckBie3OjeR?= M4T5ZZJmfmW{c3XzJIVxcXSqZXzpZYwhfG9ibXXz[Y5kcHmvYXygeJJidnOrdHnvckBw\iCqdX3hckBx\XKrdH;u[YFtKG2nc3;0bIVtcWGuIHPlcIx{ NYHCZ21MOjZyNEW3PFA>
A549 MnnhSpVv[3Srb36gZZN{[Xl? M2G2S542OCEQvF2= M1y5OWROW09? Mn7zZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> Ml3PNlY4OTF5NEi=
RAW264.7 NY[yWnM3TnWwY4Tpc44h[XO|YYm= MlvqglMxKM7:TR?= M3j4UGROW09? Ml\vdoVlfWOnczDwdo8ucW6obHHtcYF1d3K7IHflcoUh\XiycnXzd4lwdg>? NVzSVW41OjZ5MUi1PFY>
MEMM MkX6T4lv[XOnIHHzd4F6 NE\SeXkyPSEEtV2= NHXqbVhFVVOR NIHxW4dl\WO{ZXHz[ZMh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINy=> M1vk[FI3QTJzNUC2
MEMM NFywOW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rSRp4zOCEEtV2= MV3EUXNQ NWHDfIxXcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M1;rUVI3QTJzNUC2
MEMM Mme4RZBweHSxc3nzJIF{e2G7 M2LFc|E2KML3TR?= MmXpSG1UVw>? NVrmVphscW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? M2HsdVI3QTJzNUC2
T47D MofGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXWxNEDPxE1? M2m4V2ROW09? MkPMTWM2OD15MjDuUS=> NFzEbmgyQDN6MUS0OC=>
ZR-75-1 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUDMPYhpOTBizszN NVTqUJFiTE2VTx?= M{HRUmlEPTB;N{mgcm0> NYT5U|hwOTh|OEG0OFQ>
BT474 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF7qZowyOCEQvF2= NF3SbWZFVVOR NFvwNldKSzVyPUi2JI5O MofGNVg{QDF2NES=
HCC1954 NUj2R2JiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYqxNEDPxE1? NUjpVItoTE2VTx?= MmrxTWM2OD1zMUmgcm0> MnS2NVg{QDF2NES=
MDA-MB-453 NGrPd2pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkK1NVAh|ryP Mo[xSG1UVw>? M4PkdGlEPTB;OUe1JI5O MYOxPFM5OTR2NB?=
MDA-MB-468 M2jY[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MU[xNEDPxE1? MXzEUXNQ NUXEVXR3UUN3ME2zNlA5KG6P MnTzNVg{QDF2NES=
SkBr3 M{PI[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYWxNEDPxE1? MWnEUXNQ NV\ZUWdOUUN3ME6xNEwxODBibl2= MWCxPFM5OTR2NB?=
MDA-MB-231 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmfhNVAh|ryP MYDEUXNQ NYrOd5RxUUN3ME6xNEwxODBibl2= MlrMNVg{QDF2NES=
HCT116 M4j6c2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;NOVYyOCEQvF2= NXzHS41nTE2VTx?= MkfMTWM2OD13OEO2JI5O NESyV20yQDN6MUS0OC=>
HT29 NGr6U4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXSxNEDPxE1? MXfEUXNQ NF\wdYlKSzVyPkGwMFAxOCCwTR?= NVXWUGNZOTh|OEG0OFQ>
HFF M2niUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIHZNXIyOCEQvF2= M3rVXmROW09? MWXJR|UxRTd4MUWgcm0> NYfUU|ZNOTh|OEG0OFQ>
HN5 NWDoWVFLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zPcVExKM7:TR?= MYnEUXNQ MYLJR|UxRjFyLECwNEBvVQ>? MnnNNVg{QDF2NES=
786-0 MnHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3HKOlExKM7:TR?= MWrEUXNQ NH;4ZWtKSzVyPUSwNFkhdk1? Mo\WNVg{QDF2NES=
H157 M4L1Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm\ENVAh|ryP Mm\TSG1UVw>? M1jJfGlEPTB;Mk[0NkBvVQ>? MWmxPFM5OTR2NB?=
NCI-H460 NV\seoZvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{O3d|ExKM7:TR?= Mni1SG1UVw>? M1\2PGlEPTB-Mjy1NFAhdk1? NGD5S4oyQDN6MUS0OC=>
SKOV-3 MlOxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYmxNEDPxE1? MlrkSG1UVw>? MUjJR|UxRTJzMk[gcm0> NHT3d3oyQDN6MUS0OC=>
OVCAR-3 NIjyXGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1TiXFExKM7:TR?= MYjEUXNQ M2n6OWlEPTB;MkmxPEBvVQ>? MoTSNVg{QDF2NES=
BXPC3 NF\rTmZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlTNNVAh|ryP NEHhVJBFVVOR NHPrSndKSzVyPUOxOFEhdk1? M3ewdlE5OzhzNES0
MiaPaCa MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3WxWlExKM7:TR?= NX7OepZPTE2VTx?= NHXn[GpKSzVyPUW0N|Mhdk1? NHfrfVkyQDN6MUS0OC=>
PANC-1 M{n0OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3:0eFExKM7:TR?= MU\EUXNQ NGThb2pKSzVyPUi2PFEhdk1? NFv1dJYyQDN6MUS0OC=>
LNCaP NFP6dGpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MW[xNEDPxE1? NI\jUmFFVVOR NXzVXll5UUN3ME2xOFchdk1? MmnjNVg{QDF2NES=
DU145 MoHtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\hbVExKM7:TR?= NVHPdmdQTE2VTx?= M{jScGlEPTB;M{ixNkBvVQ>? M{\pfFE5OzhzNES0
PC3 NVvIO2ZLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4fTcVExKM7:TR?= NHHLd5RFVVOR NUexVFhFUUN3ME6xNEwxODBibl2= MYWxPFM5OTR2NB?=
BT474 NFLYdW9McW6jc3WgZZN{[Xl? MW[xNEDPxE1? MkDrSG1UVw>? NWXNOo9mcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMU[wJI5O NULHWIg1OTh|OEG0OFQ>
786-0 NVTsUY5HU2mwYYPlJIF{e2G7 MV:xNEDPxE1? NFu1OJhFVVOR NWLOWoxmcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMUWwJI5O NXOzOY9iOTh|OEG0OFQ>
LNCaP MkHxT4lv[XOnIHHzd4F6 NH3FNWMyOCEQvF2= NHvwboFFVVOR MmTEbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDNibl2= NXLobZhHOTh|OEG0OFQ>
PC3 MVzLbY5ie2ViYYPzZZk> NVy3WW9mOTBizszN NFS3doxFVVOR MWTpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1QSCwTR?= NU\kdHdKOTh|OEG0OFQ>
KARPAS-231 NHj4TnRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEDMR5oyOCEQvF2= MX7EUXNQ MX;FR|UxRTRzIH7N MnjpNVkxPjR5M{C=
CCRFSB M3HofWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2iyeVExKM7:TR?= M{XYfmROW09? M1HXTWVEPTB;MUW1JI5O NHzKWIkyQTB4NEezNC=>
SUP B15 NYTlVZBRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIrQPIcyOCEQvF2= MYHEUXNQ NUexcIRSTUN3ME2xPVchdk1? MluzNVkxPjR5M{C=
SD-1 M3fVRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV7J[nVEOTBizszN NEP2ZphFVVOR NH3tUFZGSzVyPUOyNEBvVQ>? NFT1Z5QyQTB4NEezNC=>
RS4;11 MlGxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXzQW5RJOTBizszN M1O1OmROW09? NFnlfI9GSzVyPU[1OEBvVQ>? NXe5PI1WOTlyNkS3N|A>
MN-60 MknzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M165T|ExKM7:TR?= NFvwUmJFVVOR NES2ZolGSzVyPUO2NFIhdk1? MoTrNVkxPjR5M{C=
Tanoue NWPDdGtqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWDnRoZwOTBizszN Ml;0SG1UVw>? NGPlRmNGSzVyPUS1NVchdk1? MlXVNVkxPjR5M{C=
RCH-ACV NEf0[HdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoHyNVAh|ryP MVrEUXNQ MlP2SWM2OD1zNUKgcm0> NXLIW25lOTlyNkS3N|A>
SEM Moi2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1m1VFExKM7:TR?= M4jvZ2ROW09? Mn3mSWM2OD1{MEKgcm0> NWrDUIVGOTlyNkS3N|A>
KASUMI-2 MnTUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{[2UFExKM7:TR?= MkfZSG1UVw>? NITFd4pGSzVyPUKyOUBvVQ>? Mn3pNVkxPjR5M{C=
REH Moe0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGCye4YyOCEQvF2= M1L4OmROW09? MXHFR|UxRTJ6ODDuUS=> NG\xPJMyQTB4NEezNC=>
697 MoLaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHrRfoEyOCEQvF2= MlLNSG1UVw>? M3S4dWVEPTB;M{O4JI5O NFKzPW0yQTB4NEezNC=>
NALM-6 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEPaVIkyOCEQvF2= M{X0OWROW09? MmTlSWM2OD12MkGgcm0> NUn2fm5sOTlyNkS3N|A>
MHH-CALL–3 NVi0Sm4zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHW0Z4MyOCEQvF2= NFzINWhFVVOR MVTFR|UxRThzMjDuUS=> M13z[FE6ODZ2N{Ow
MHH-CALL–2 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXPtfXd2OTBizszN NUD1WlhzTE2VTx?= NHjaTHBGSzVyPUKxNVQhdk1? MUGxPVA3PDd|MB?=
J.GAMMA-1 NF;zSYtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmXaNVAh|ryP NELNUXRFVVOR MoG3SWM2OD14NTDuUS=> NVLDRVUyOTlyNkS3N|A>
JR45.01 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX7sWZVxOTBizszN NXHM[HRHTE2VTx?= NUnSeFB7TUN3ME22PEBvVQ>? NV;oXmQzOTlyNkS3N|A>
A3 NFPxcXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NY[2U4RPOTBizszN MUnEUXNQ MWPFR|UxRTZ7IH7N MUWxPVA3PDd|MB?=
I 2.1 NWX6flVpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkfLNVAh|ryP MXrEUXNQ MWTFR|UxRTd|IH7N NXvnUnZQOTlyNkS3N|A>
MOLT-3 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIXuRmwyOCEQvF2= Mlf2SG1UVw>? MkDuSWM2OD15NDDuUS=> M1\lcFE6ODZ2N{Ow
P116 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnnxNVAh|ryP NWnaSoM2TE2VTx?= MlXXSWM2OD15ODDuUS=> MonzNVkxPjR5M{C=
J.Cam1.6 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEK3WZMyOCEQvF2= M3\SXWROW09? NES3cZlGSzVyPUe5JI5O MlXDNVkxPjR5M{C=
I 9.2 NFv1SZFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkLBNVAh|ryP MUHEUXNQ MWrFR|UxRThyIH7N MoKxNVkxPjR5M{C=
LOUCY Mn7hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIrLXmgyOCEQvF2= MWDEUXNQ MWjFR|UxRTFzNzDuUS=> NILHbpQyQTB4NEezNC=>
J.RT3-T3.5 M2eyZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYOxNEDPxE1? NEj2VWVFVVOR M3;Id2VEPTB;MUKzJI5O M1fON|E6ODZ2N{Ow
800000 NXn0VIp2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnvKNVAh|ryP Mn3TSG1UVw>? M4\D[WVEPTB;MU[zJI5O MWqxPVA3PDd|MB?=
Jurkat NFTjS5VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFjoS|YyOCEQvF2= MUXEUXNQ MnzKSWM2OD1{MkWgcm0> NYS5T2hzOTlyNkS3N|A>
MOLT-4 M2TjeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkHXNVAh|ryP Mn3USG1UVw>? M2jOemVEPTB;MkOyJI5O NVzsRm5COTlyNkS3N|A>
Molt-16 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml2wNVAh|ryP M1rYTmROW09? NHLFcllGSzVyPUK0NUBvVQ>? MX2xPVA3PDd|MB?=
CEM/C3 NUP4NIdlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIjS[WsyOCEQvF2= Mor4SG1UVw>? MlzNSWM2OD1{NUegcm0> MnzDNVkxPjR5M{C=
CEM/C2 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn;5NVAh|ryP MmrESG1UVw>? MVjFR|UxRTJ5MTDuUS=> NG\2S5EyQTB4NEezNC=>
CCRFCEM MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVyxNEDPxE1? M1;ubmROW09? NVHWNHoxTUN3ME2zNlchdk1? MUexPVA3PDd|MB?=
CEM/C1 NY\Q[VAyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV6xNEDPxE1? M1;4dGROW09? NYPTTW84TUN3ME2zPFIhdk1? Mn24NVkxPjR5M{C=
SUPTI[VB] NVT4SJFNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2G4NFExKM7:TR?= M1;H[WROW09? NIj4eYZGSzVyPU[xPUBvVQ>? MYexPVA3PDd|MB?=
CCRF–HSB-2 M1P4TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHvLXIMyOCEQvF2= NF3RWJRFVVOR MUXFR|UxRTJzMUegcm0> M33jPFE6ODZ2N{Ow
I 2.1 M{G5W2Fxd3C2b4Ppd{Bie3OjeR?= M2r6NFExKM7:TR?= M1rUeWROW09? NFfOb5hqdmS3Y3XzJIFxd3C2b4Ppdy=> MkHwNVkxPjR5M{C=
I 9.2 NFzadGpCeG:ydH;zbZMh[XO|YYm= Mny1NVAh|ryP MkLhSG1UVw>? M4e0V4lv\HWlZYOgZZBweHSxc3nz MYGxPVA3PDd|MB?=
A3 MV3BdI9xfG:|aYOgZZN{[Xl? MUGxNEDPxE1? MV;EUXNQ MYfpcoR2[2W|IHHwc5B1d3Orcx?= NVjoOJV1OTlyNkS3N|A>
RD NIS3b2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1HOblExKM7:TR?= NHfUZmJKSzVyPkGwJO69VQ>? MX2yNFc1ODZ{Mx?=
Rh41 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVOxNEDPxE1? MlLkTWM2OD1|Mz64JI5O MXmyNFc1ODZ{Mx?=
Rh18 NELNUnNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUCxNEDPxE1? MnTXTWM2OD1|MEOgcm0> MlP2NlA4PDB4MkO=
Rh30 MmLwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\xO|ExKM7:TR?= M3vHSWlEPTB;ND64NUDPxE1? M3HmRlIxPzRyNkKz
BT-12 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXn5eXVHOTBizszN M4PCNGlEPTB-MUCg{txO NX7Qe2VrOjB5NEC2NlM>
CHLA-266 Mn7pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGe3clIyOCEQvF2= NXH1fGtyUUN3ME2xMlIzKM7:TR?= MYGyNFc1ODZ{Mx?=
TC-71 Mn;pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1;NbVExKM7:TR?= NHjBdm5KSzVyPUKuOVIh|ryP MYeyNFc1ODZ{Mx?=
CHLA-9 MoLnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV6xNEDPxE1? MnHJTWM2OD13OUGgcm0> MX6yNFc1ODZ{Mx?=
CHLA-10 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnrKNVAh|ryP MoCxTWM2OD1zMEKgcm0> M4DJWlIxPzRyNkKz
CHLA-258 M2[5Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3LTWlExKM7:TR?= MnPiTWM2OD1zLkC1JO69VQ>? M4T6ZlIxPzRyNkKz
GBM2 M33SWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoO5NVAh|ryP NVfzd5ZXUUN3ME25MlE2KM7:TR?= M3Hte|IxPzRyNkKz
NB-1643 NWftNJc2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1;GSVExKM7:TR?= M{HDcWlEPTB;NT60JO69VQ>? NFLlT|UzODd2ME[yNy=>
NB-Ebc1 Mm\uS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUe3[WRyOTBizszN NYGzdHZ5UUN3ME6xNEDPxE1? MXqyNFc1ODZ{Mx?=
CHLA-90 NGrqdFRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3nldFExKM7:TR?= MkTmTWM2OD5zMDFOwG0> M2TmXlIxPzRyNkKz
CHLA-136 NXPYdG9kT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXHKdFdVOTBizszN M4nIRWlEPTB-MUCg{txO MmrsNlA4PDB4MkO=
NALM-6 NXux[XVkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3e0VFExKM7:TR?= NELLV3RKSzVyPUK2OUBvVQ>? M3H0WVIxPzRyNkKz
COG-LL-317 MkTNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoXvNVAh|ryP M3Lvd2lEPTB;Nj60PUBvVQ>? M3npUVIxPzRyNkKz
RS4;11 M3TLfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm[xNVAh|ryP M4C4fWlEPTB;MUS3JI5O NVX2dHk{OjB5NEC2NlM>
MOLT-4 NFTR[2VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1j3PVExKM7:TR?= M2DwR2lEPTB;NECgcm0> M3jobFIxPzRyNkKz
CCRF-CEM MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEi2Z|MyOCEQvF2= NFPuXGxKSzVyPUK2PEBvVQ>? NVGydmZpOjB5NEC2NlM>
Kasumi-1 NI\vUZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3\Ve|ExKM7:TR?= NFf6R|VKSzVyPUGwO{BvVQ>? M3HuNFIxPzRyNkKz
Karpas-299 M4rad2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWLiblBTOTBizszN NYjKNIE4UUN3ME2yMlk{KM7:TR?= NWXFTZRzOjB5NEC2NlM>
Ramos-RA1 NYmxOpJET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUm0ZnJyOTBizszN MW\JR|UxRTdwM{Wg{txO Ml3UNlA4PDB4MkO=
H1299 NX\BNWVjU2mwYYPlJIF{e2G7 NVjKWpM4OTBizszN NWXxcXRWcW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? MXyyNVkxQDZzNh?=

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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
  • 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

Bio Calculators

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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.

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