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 5 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 M17VWmtqdmG|ZTDhd5NigQ>? NHvpdnl,OTBizszN NI[xclhqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MoToNlA1QDRyMUi=
HT29 M1rTUWtqdmG|ZTDhd5NigQ>? NXz6[o9KhjFyIN88US=> NXLo[Wc4cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> M3LZOFIxPDh2MEG4
MDA-MB-231 MkW2T4lv[XOnIHHzd4F6 M3f1VJ4yOCEQvF2= M1T6XolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NH;OdIQzODR6NECxPC=>
NCI-H441 Mke0T4lv[XOnIHHzd4F6 M3nXbJ4yOCEQvF2= MnrKbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NGHnPHczODR6NECxPC=>
SK-MEL-28 NYfJUpR3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX[zN{DPxE1? NEPjWZZKSzVyPkOzJO69VQ>? MWqyNFQ5PDBzOB?=
NCI-H661 M2i1UWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWKzN{DPxE1? NUHac2oyUUN3ME6zN{DPxE1? M1;vU|IxPDh2MEG4
NCI-H446 M3fQW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV;ZRo5OOzNizszN MV;JR|UxRTdizszN NVuwXFJyOjB2OESwNVg>
MDA-MB-231 NYHze3ptT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkezN|Mh|ryP NGqxOWxKSzVyPUCuOVUh|ryP NHTHSJczODR6NECxPC=>
DLD-1 NXe4XWt6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVixe|dQOzNizszN MkHNTWM2OD1yLkWzJO69VQ>? NXXRcXdNOjB2OESwNVg>
A549 MmfFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX6zN{DPxE1? MYfJR|UxRTBwNUmg{txO MknCNlA1QDRyMUi=
SK-OV-3 MkTQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmG0N|Mh|ryP NEnw[3NKSzVyPUCuOlYh|ryP MnTBNlA1QDRyMUi=
NCI-H460 NFzFNGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYK5c|F5OzNizszN M1rYemlEPTB;MD62JO69VQ>? Ml7GNlA1QDRyMUi=
A375 M2LjZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX6zN{DPxE1? M3PU[WlEPTB;MD60NkDPxE1? NGXMSmszODR6NECxPC=>
NCI-H441 M4nRbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW\wUW1qOzNizszN NUjTOZFHUUN3ME2wMlMh|ryP MnPmNlA1QDRyMUi=
HT29 Mk\PS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MofTN|Mh|ryP M2q3bGlEPTB;MD60PUDPxE1? MlT5NlA1QDRyMUi=
MKN-45 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LMS|M{KM7:TR?= NG\3UY9KSzVyPUCuOVgh|ryP Mk\WNlA1QDRyMUi=
HT29 NE\3OpJCeG:ydH;zbZMh[XO|YYm= MX7+NVAh|ryP MnHid4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NGnNe4wzODR6NECxPC=>
MKN-45 NF[2SpRCeG:ydH;zbZMh[XO|YYm= NILvVm1,OTBizszN Mn7id4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NEnOOnIzODR6NECxPC=>
MDA-MB-231 M2rvcWFxd3C2b4Ppd{Bie3OjeR?= MXH+NVAh|ryP M4PVVI1w\GW|dHz5JIlv\HWlZYOgZZBweHSxc3nzJIJ6KDN3JT6= MX2yNFQ5PDBzOB?=
MDA-MB-231/TGL M3PVNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1KzfJ4yODBizszN NGHSW5RIUTVyPUGuNkDPxE1? M17yT|IzODJ5Nkmw
1833/TGL M2\i[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVjQfnhqhjFyMDFOwG0> M3u5XmdKPTB;Mz63JO69VQ>? MYKyNlAzPzZ7MB?=
EBC1 M{HTWWN6fG:2b4jpZ:Kh[XO|YYm= MWH+NVAh|ryP MmDYbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= MVGyN|U6QDJ5Nh?=
SNU638 MonRR5l1d3SxeHnjxsBie3OjeR?= MYT+NVAh|ryP NWjUO3ppcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> MlHZNlM2QTh{N{[=
A549 Mm[yR5l1d3SxeHnjxsBie3OjeR?= MlHyglExKM7:TR?= MnTOco91KGGoZnXjeC=> NIrqSIszOzV7OEK3Oi=>
H460 M{LHO2N6fG:2b4jpZ:Kh[XO|YYm= NXnSeoFrhjFyIN88US=> NF\r[oFvd3RiYX\m[YN1 NULKfGNuOjN3OUiyO|Y>
HCC827 MXjDfZRwfG:6aXRCpIF{e2G7 NWTSV2JFhjFyIN88US=> NHTyeHFvd3RiYX\m[YN1 M{TVTVI{PTl6Mke2
A549 MojOSpVv[3Srb36gZZN{[Xl? MV:xNEDPxE1? Mk\p[Il{enWydIOgcYlkem:2dXL1cIU> MWmyN|U6QDJ5Nh?=
EBC1 NX\zO2o{TnWwY4Tpc44h[XO|YYm= MkT6NVAh|ryP MVvkbZNzfXC2czDtbYNzd3S3YoXs[S=> MoTPNlM2QTh{N{[=
H460 M3HNWmZ2dmO2aX;uJIF{e2G7 MYixNEDPxE1? NUf6cJJQcW6qaXLpeJMhfHWkdXzpckBxd2y7bXXybZpifGmxbh?= MnH2NlU{OTNyMUC=
K562/VCR NVTUcJJSS3m2b4TvfIlkyqCjc4PhfS=> MkjEglExKM7:TR?= NGrHT2N{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M1vKPFI2OzF|MEGw
CEM/VBL MVXDfZRwfG:6aXRCpIF{e2G7 NYK2VIhRhjFyIN88US=> NYPC[nZMe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NEW3UWkzPTNzM{CxNC=>
U266 NXq5XHRrS3m2b4TvfIlkyqCjc4PhfS=> MlHiglMh|ryPwrC= MUDJR|UxRTFwMTFOwG0> MkPoNlU5OTByMUO=
OPM-2 NXHJRYtiS3m2b4TvfIlkyqCjc4PhfS=> MmTGglMh|ryPwrC= NE\MTnNKSzVyPUGuPEDPxE1? M3nlfVI2QDFyMEGz
MM.1S M4\JVGN6fG:2b4jpZ:Kh[XO|YYm= M1HZZ54{KM7:TdMg MULJR|UxRTFwNjFOwG0> NHvaOnEzPThzMECxNy=>
MM.1R NYHNN445T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4PhTVMh|ryPwrC= MW\pcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= NXHpcoh3OjV6MUCwNVM>
RPMI-8226 M{nDe2N6fG:2b4jpZ:Kh[XO|YYm= MljrglMh|ryPwrC= NGi2VolKSzVyPUCuPUDPxE1? M1LRSVI2QDFyMEGz
ANBL-6 NXXlfFdpS3m2b4TvfIlkyqCjc4PhfS=> M4q4[lEh|ryPwrC= M3TUSolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NVzVcHlLOjV6MUCwNVM>
ANLB-6/V10R Ml[xR5l1d3SxeHnjxsBie3OjeR?= M{PTN|Eh|ryPwrC= M2HqXYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NUj0c4ZqOjV6MUCwNVM>
KAS-6/1 M3uwRmN6fG:2b4jpZ:Kh[XO|YYm= NUW1fHh6OSEQvF5CpC=> MX3pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NHzMZWczPThzMECxNy=>
KAS-6/V10R MkXxR5l1d3SxeHnjxsBie3OjeR?= NIHMcogyKM7:TdMg NXfHd|RScW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MUiyOVgyODBzMx?=
KAS-6/R10R NXjDfFIyS3m2b4TvfIlkyqCjc4PhfS=> MlPRNUDPxE4EoB?= M17LVolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MonvNlU5OTByMUO=
8226/S MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M13LS|Mh|ryPwrC= NFT1U|hqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> MnPBNlU5OTByMUO=
8226/LR-5 NIrFNIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXuzJO69VcLi M17KN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> Ml3NNlU5OTByMUO=
Huh7 M3:4SmN6fG:2b4jpZ:Kh[XO|YYm= M4[1VZ41NjhizszNxsA> NFvyXYpFVVOR NYfkR4w6UUN3ME25Mlkhdk1? MnLONlYzPTl{NUC=
Hep3B NVezemw5S3m2b4TvfIlkyqCjc4PhfS=> NEe0XXJ,PC56IN88UeKh M4HWZ2ROW09? Mn36TWM2OD12NEiuO{BvVQ>? NIrNUZgzPjJ3OUK1NC=>
HepG2 NFiyNWREgXSxdH;4bYPDqGG|c3H5 NFnHdmd,PC56IN88UeKh M3z3bGROW09? NEP0cmNKSzVyPUGzPU44PyCwTR?= M36yNVI3OjV7MkWw
Chang NGqz[mtEgXSxdH;4bYPDqGG|c3H5 NFztSmZ,PC56IN88UeKh NVPUdplCTE2VTx?= MYjJR|UxRTR2OD63JI5O NHHuVXEzPjJ3OUK1NC=>
Huh7 MlK3SpVv[3Srb36gZZN{[Xl? NH3IOJkyNjZizszNxsA> MWfEUXNQ MnjYZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NFnyOGgzPjJ3OUK1NC=>
Hep3B NIfXem1HfW6ldHnvckBie3OjeR?= M{LQflEvPiEQvF5CpC=> MkDXSG1UVw>? NIroWnVk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NFTOUIQzPjJ3OUK1NC=>
HepG2 NI\udJRHfW6ldHnvckBie3OjeR?= MUCxMlYh|ryPwrC= NF\VR3VFVVOR MXnjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NEfVbXQzPjJ3OUK1NC=>
Chang MlzzSpVv[3Srb36gZZN{[Xl? MkfMNU43KM7:TdMg MV;EUXNQ MmDkZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NHHCc|AzPjJ3OUK1NC=>
MHCC97L Mn\GS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUL+NVAh|ryP M4n0NGROW09? NF3w[pBKSzVyPUOxOUBvVQ>? MoLtNlY1PTh7NUO=
MHCC97H NVvzfnRwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlr3glExKM7:TR?= NVHYSGE{TE2VTx?= MkjMTWM2OD1|NklihKkhdk1? M1HMOFI3PDV6OUWz
Huh7 NHvFc|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUD+NVAh|ryP MoLtSG1UVw>? MlTFTWM2OD1{NkWgcm0> NEj4TZMzPjR3OEm1Ny=>
HepG2 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVX+NVAh|ryP Ml\WSG1UVw>? Ml7wTWM2OD1|OUKgcm0> NV75e21QOjZ2NUi5OVM>
MHCC97L NFnUWVlHfW6ldHnvckBie3OjeR?= NFe5VVIyKM7:TdMg M2LoXWROW09? M{TXcolv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NYHaeJA{OjZ2NUi5OVM>
Huh7 MlqzSpVv[3Srb36gZZN{[Xl? M{Dj[VEh|ryPwrC= MYXEUXNQ MWjpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u NEPwU5czPjR3OEm1Ny=>
MHCC97L NVPhTph{SXCxcITvd4l{KGG|c3H5 NFHUNooyKM7:TdMg NHfH[IhFVVOR M4rDeolv\HWlZYOgZZBweHSxc3nz MnX5NlY1PTh7NUO=
Huh7 NUHHbmhjSXCxcITvd4l{KGG|c3H5 NUTrWldqOSEQvF5CpC=> NGLn[GJFVVOR NV3ybVZOcW6mdXPld{BieG:ydH;zbZM> MU[yOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts M4rqS2tqdmG|ZTDhd5NigQ>? MX[yOUDPxE1? M2L1[WROW09? NUXtZ|IzemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? NE\HUI8zODV|NEO0OS=>
H23 NYfoXG5qT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFLWN|EzPSEQvF2= M1Pn[GROW09? MW\zbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NGjRPFczODV|NEO0OS=>
WM35 Ml\kS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NESyXIoyOCEQvF2= NH75bI9FVVOR NYfOe|hNe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MnrONlA2OzR|NEW=
NIH 3T3 NWTOdoRIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYmxNEDPxE1? MUfEUXNQ MWrkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= NEHmU5gzODV|NEO0OS=>
H838 NID4cJdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWSxNEDPxE1? M1HtXWROW09? MkKz[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MlHZNlA2OzR|NEW=
H1395 NH3VeVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmXmNVAh|ryP MmXPSG1UVw>? NX\scZNL\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MkHTNlA2OzR|NEW=
Quiescent S2 MkS0T4lv[XOnIHHzd4F6 MXGzNEDPxE1? NEnDZmxFVVOR NX\sUWNS[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz M{H0T|IyPTF6OUG1
PC3 MoTtRZBweHSxc3nzJIF{e2G7 NGTxcJozOCEQvF2= NUK0SpdpTE2VTx?= Mmr6bY5lfWOnczDhdI9xfG:|aYO= NI\F[oYzOTdyOUGzNC=>
Du145 NG\z[GdCeG:ydH;zbZMh[XO|YYm= NVm3NZVNOjBizszN M3PkcGROW09? M1zlU4lv\HWlZYOgZZBweHSxc3nz NHrvZ5UzOTdyOUGzNC=>
LNCaP NXzmVYdjSXCxcITvd4l{KGG|c3H5 Mo\2NlAh|ryP MV\EUXNQ M4TBe4lv\HWlZYOgZZBweHSxc3nz M2n3R|IyPzB7MUOw
LAPC-4 MUHBdI9xfG:|aYOgZZN{[Xl? NEPNZ3EzOCEQvF2= MlrHSG1UVw>? M3joU4lv\HWlZYOgZZBweHSxc3nz M4DnZ|IyPzB7MUOw
LNCaP Mnq3SpVv[3Srb36gZZN{[Xl? M1PPT|IxKM7:TR?= M4rj[mROW09? M4\ndoRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NVLESJV3OjF5MEmxN|A>
LAPC-4 M{[wNGZ2dmO2aX;uJIF{e2G7 MoSyNlAh|ryP MVrEUXNQ NGDWZ4xl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| MYSyNVcxQTF|MB?=
Kasumi-1 MonVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\MXlR,PTBizszN M3\lUWROW09? NX7hU|BucW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NGTh[WkzOzN7MEWzOi=>
SKNO-1 MoTyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnnqglUxKM7:TR?= MmHXSG1UVw>? M4rObolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NYTxcVlxOjN|OUC1N|Y>
Kasumi-1 NYXa[GNsU2mwYYPlJIF{e2G7 NHO4SGZ,OTBizszN MnLCSG1UVw>? NXfvcYM3emWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NF3rUmkzOzN7MEWzOi=>
SKNO-1 NIK3RYZMcW6jc3WgZZN{[Xl? NYW4[VFShjFyIN88US=> MVHEUXNQ MUDy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= M2qwWFI{OzlyNUO2
A549 MUnGeY5kfGmxbjDhd5NigQ>? MkHNNVAh|ryP NFrnZ29FVVOR MV;lcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl M{j5VVI1PzR4NUe0
NRK-52E MmHWSpVv[3Srb36gZZN{[Xl? NVzSPWtmOTBizszN NWfHXGNVTE2VTx?= M1rB[YlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv NWLK[Gh2OjVyOEiwNFI>
PC12 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYH+NVIvPSEQvF2= Mo\CSG1UVw>? NWiye|AyeHKndnXueJMhXFODLXnu[JVk\WRibnX1dol1\SCob4LtZZRqd25? M{nG[lI2OTJ6M{i2
HPMCs NHfVZZhHfW6ldHnvckBie3OjeR?= M4jq[5JmfmW{c3XzJIVxcXSqZXzpZYwhfG9ibXXz[Y5kcHmvYXygeJJidnOrdHnvckBw\iCqdX3hckBx\XKrdH;u[YFtKG2nc3;0bIVtcWGuIHPlcIx{ NYGwNnN7OjZyNEW3PFA>
A549 M1HHVmZ2dmO2aX;uJIF{e2G7 NVvtUINQhjVyIN88US=> MXTEUXNQ MmmzZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> MXiyOlcyOTd2OB?=
RAW264.7 Mkn6SpVv[3Srb36gZZN{[Xl? NXfHWHVKhjNyIN88US=> NXL1b2d6TE2VTx?= MmX3doVlfWOnczDwdo8ucW6obHHtcYF1d3K7IHflcoUh\XiycnXzd4lwdg>? MkfVNlY4OTh3OE[=
MEMM MWLLbY5ie2ViYYPzZZk> NUHnNW1GOTViwsXN MVvEUXNQ NUWzU3Nm\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> MUWyOlkzOTVyNh?=
MEMM MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1v5e54zOCEEtV2= MVvEUXNQ NWTE[XBTcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnPZNlY6OjF3ME[=
MEMM M2HvWGFxd3C2b4Ppd{Bie3OjeR?= NWTBb4JnOTViwsXN MWLEUXNQ NIPWT|RqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ NEPVfHQzPjl{MUWwOi=>
T47D MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoTjNVAh|ryP MVfEUXNQ MlPITWM2OD15MjDuUS=> NVLaV3d5OTh|OEG0OFQ>
ZR-75-1 M3S1S2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3\YZlExKM7:TR?= NVHa[GFqTE2VTx?= MY\JR|UxRTd7IH7N NHe1e5gyQDN6MUS0OC=>
BT474 Ml\JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M17jblExKM7:TR?= MV\EUXNQ M3fiO2lEPTB;OE[gcm0> M3jYU|E5OzhzNES0
HCC1954 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUHndYxrOTBizszN MVTEUXNQ NWrRdGlIUUN3ME2xNVkhdk1? NHO5WGYyQDN6MUS0OC=>
MDA-MB-453 NXrTRnhuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3vjblExKM7:TR?= M2rGcWROW09? NIj5Z49KSzVyPUm3OUBvVQ>? NYnHW3AyOTh|OEG0OFQ>
MDA-MB-468 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3TibVExKM7:TR?= MX\EUXNQ M3O4VGlEPTB;M{KwPEBvVQ>? MnvENVg{QDF2NES=
SkBr3 NFjVRW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1XyRVExKM7:TR?= NW\kVWF[TE2VTx?= MnfrTWM2OD5zMDywNFAhdk1? MlOyNVg{QDF2NES=
MDA-MB-231 Mn;JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUniSWRFOTBizszN NVXmZYJuTE2VTx?= MYrJR|UxRjFyLECwNEBvVQ>? NVWxWGFOOTh|OEG0OFQ>
HCT116 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{nCXlExKM7:TR?= Mlj4SG1UVw>? NE\Kb2NKSzVyPUW4N|Yhdk1? MoX1NVg{QDF2NES=
HT29 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEjObGIyOCEQvF2= MVTEUXNQ NXfuUoRUUUN3ME6xNEwxODBibl2= NYKwVnF1OTh|OEG0OFQ>
HFF MmjPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3vUS|ExKM7:TR?= NGTyVWpFVVOR M{PZd2lEPTB;N{[xOUBvVQ>? MlX3NVg{QDF2NES=
HN5 NHvDU2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn\hNVAh|ryP M4DBS2ROW09? NX;1[o1FUUN3ME6xNEwxODBibl2= NFqyNG0yQDN6MUS0OC=>
786-0 MmXOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSxNEDPxE1? M1P0eWROW09? NFz5b2dKSzVyPUSwNFkhdk1? MmLWNVg{QDF2NES=
H157 NYn2Rph4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HWeVExKM7:TR?= NEnoTnFFVVOR NED1WIlKSzVyPUK2OFIhdk1? NEX2U2QyQDN6MUS0OC=>
NCI-H460 NFPN[nZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFTWRmgyOCEQvF2= NEjOdHBFVVOR MlzjTWM2OD5{LEWwNEBvVQ>? NVKw[3l6OTh|OEG0OFQ>
SKOV-3 NEm4OYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWKxNEDPxE1? MUPEUXNQ Mnv5TWM2OD1{MUK2JI5O Ml;INVg{QDF2NES=
OVCAR-3 NIHrfXFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn;RNVAh|ryP M4jwVmROW09? NHK0eGNKSzVyPUK5NVghdk1? M1j2TlE5OzhzNES0
BXPC3 M2jtemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWXpR2UyOTBizszN M3rGe2ROW09? NFjFWldKSzVyPUOxOFEhdk1? NFvmR3IyQDN6MUS0OC=>
MiaPaCa NELzN5ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NE\FZ5gyOCEQvF2= MnfHSG1UVw>? M2LnO2lEPTB;NUSzN{BvVQ>? NYDjeZpwOTh|OEG0OFQ>
PANC-1 NYHiV5NzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{PIc|ExKM7:TR?= M2S5SmROW09? NWnNXo1JUUN3ME24OlgyKG6P NVz4Zpl6OTh|OEG0OFQ>
LNCaP MljCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYqxNEDPxE1? MmrTSG1UVw>? MVrJR|UxRTF2NzDuUS=> MnXtNVg{QDF2NES=
DU145 NYf6b3JpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIi1RmUyOCEQvF2= MXzEUXNQ NWnBWlJFUUN3ME2zPFEzKG6P MWKxPFM5OTR2NB?=
PC3 MoTBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVGxNEDPxE1? M2DoNWROW09? MYDJR|UxRjFyLECwNEBvVQ>? MmCxNVg{QDF2NES=
BT474 NHK0Z2JMcW6jc3WgZZN{[Xl? NUHFPXZrOTBizszN NHXINYFFVVOR NVrLNHlMcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMU[wJI5O M{HEZVE5OzhzNES0
786-0 NIWyOZJMcW6jc3WgZZN{[Xl? MUGxNEDPxE1? M4PGcmROW09? MWXpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kAyPTBibl2= NWrhe2VUOTh|OEG0OFQ>
LNCaP NFnhV3NMcW6jc3WgZZN{[Xl? NYTrcYdiOTBizszN M4fVOWROW09? NHfHOpBqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2MzDuUS=> M3rYd|E5OzhzNES0
PC3 NFvCT3ZMcW6jc3WgZZN{[Xl? MX2xNEDPxE1? Mkn5SG1UVw>? M{nndYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR7IH7N M4H0VFE5OzhzNES0
KARPAS-231 NXzaVHFLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NU[4SpRJOTBizszN NH[zTGdFVVOR M4G0[WVEPTB;NEGgcm0> NHLHSmgyQTB4NEezNC=>
CCRFSB NWD1Z|V1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF\hR3gyOCEQvF2= NYexNYIyTE2VTx?= MYHFR|UxRTF3NTDuUS=> MVKxPVA3PDd|MB?=
SUP B15 M2f2Rmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4\UeFExKM7:TR?= NV7JbWRFTE2VTx?= NVWyfY1xTUN3ME2xPVchdk1? MnTVNVkxPjR5M{C=
SD-1 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLQVYhqOTBizszN MmftSG1UVw>? MVrFR|UxRTN{MDDuUS=> NW\nS4VlOTlyNkS3N|A>
RS4;11 M33RR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXK5UVF[OTBizszN NFfHXnVFVVOR MVvFR|UxRTZ3NDDuUS=> M4O2flE6ODZ2N{Ow
MN-60 NWnxR2lZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{jEelExKM7:TR?= M2S4U2ROW09? NYi0fmJsTUN3ME2zOlAzKG6P M3LZOFE6ODZ2N{Ow
Tanoue M4ewTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFj3OpQyOCEQvF2= MkfzSG1UVw>? MljUSWM2OD12NUG3JI5O NWHlN4U4OTlyNkS3N|A>
RCH-ACV M1q4T2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn3FNVAh|ryP MlztSG1UVw>? M2e3emVEPTB;MUWyJI5O MkK0NVkxPjR5M{C=
SEM M3q2Zmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHjIcnYyOCEQvF2= MX7EUXNQ NYK2eGNyTUN3ME2yNFIhdk1? M2m4fVE6ODZ2N{Ow
KASUMI-2 MorhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHi1RZEyOCEQvF2= M1\SeWROW09? MXXFR|UxRTJ{NTDuUS=> MVqxPVA3PDd|MB?=
REH MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4rR[FExKM7:TR?= MUTEUXNQ NGjDSZRGSzVyPUK4PEBvVQ>? M2TRXVE6ODZ2N{Ow
697 NEHIRolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYrReVR7OTBizszN Moj3SG1UVw>? NV;0XnJRTUN3ME2zN|ghdk1? M4myT|E6ODZ2N{Ow
NALM-6 NIrlRYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2DSS|ExKM7:TR?= M3X2XGROW09? MWLFR|UxRTR{MTDuUS=> MYmxPVA3PDd|MB?=
MHH-CALL–3 MnjVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1zw[lExKM7:TR?= NXfTRpZSTE2VTx?= NWDEOpk6TUN3ME24NVIhdk1? MoK4NVkxPjR5M{C=
MHH-CALL–2 M2foNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYqxNEDPxE1? NXrQSoRrTE2VTx?= NH34XZFGSzVyPUKxNVQhdk1? MmnHNVkxPjR5M{C=
J.GAMMA-1 MnzwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1fSfVExKM7:TR?= MVfEUXNQ NV;FdJYzTUN3ME22OUBvVQ>? NWfpc3JYOTlyNkS3N|A>
JR45.01 NXXCZpFNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYDMTYxvOTBizszN NHjDcYlFVVOR NETD[JhGSzVyPU[4JI5O MmLzNVkxPjR5M{C=
A3 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYWxNEDPxE1? NGq1dFJFVVOR MY\FR|UxRTZ7IH7N NGq5Z5gyQTB4NEezNC=>
I 2.1 Ml3BS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUKxNEDPxE1? MnjXSG1UVw>? NYDTPWdzTUN3ME23N{BvVQ>? NWT5eIc{OTlyNkS3N|A>
MOLT-3 NHHJcllIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXPwflh[OTBizszN NIGxVIZFVVOR NVnhfpdwTUN3ME23OEBvVQ>? M4LyWVE6ODZ2N{Ow
P116 M2r2XWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWSxNEDPxE1? MnzuSG1UVw>? NGX0So9GSzVyPUe4JI5O M3jSPFE6ODZ2N{Ow
J.Cam1.6 M{X0[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXWxNEDPxE1? MmrTSG1UVw>? NUDWcnVlTUN3ME23PUBvVQ>? NYP4e3p[OTlyNkS3N|A>
I 9.2 NYrRO|dIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHi5RVUyOCEQvF2= MWrEUXNQ MV\FR|UxRThyIH7N NGLzbY8yQTB4NEezNC=>
LOUCY NHjGZYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYqyV2FIOTBizszN NFjYNJRFVVOR MWjFR|UxRTFzNzDuUS=> M2jKTVE6ODZ2N{Ow
J.RT3-T3.5 NHXscndIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVPjV4lMOTBizszN NWe4O4oxTE2VTx?= MlfCSWM2OD1zMkOgcm0> NXf2[3VOOTlyNkS3N|A>
800000 NYLVVWlbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mm\0NVAh|ryP M3jGNGROW09? M1nRNmVEPTB;MU[zJI5O NFrjOoIyQTB4NEezNC=>
Jurkat NGrGfmhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHHj[FkyOCEQvF2= NYfNcHk{TE2VTx?= M1z2XGVEPTB;MkK1JI5O NYXwOWpDOTlyNkS3N|A>
MOLT-4 NX\uVmNQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NET3SGoyOCEQvF2= NVjwc5F1TE2VTx?= MY\FR|UxRTJ|MjDuUS=> M2GxOVE6ODZ2N{Ow
Molt-16 NHK5SWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{Dt[|ExKM7:TR?= NHvke4VFVVOR MULFR|UxRTJ2MTDuUS=> MVuxPVA3PDd|MB?=
CEM/C3 NUH3NXJmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3rGXFExKM7:TR?= M3zaXGROW09? NH65Oo1GSzVyPUK1O{BvVQ>? MWmxPVA3PDd|MB?=
CEM/C2 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmrNNVAh|ryP M17kT2ROW09? NUTmenBuTUN3ME2yO|Ehdk1? MmD0NVkxPjR5M{C=
CCRFCEM MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoGwNVAh|ryP NF\QUZFFVVOR NWWzPJdKTUN3ME2zNlchdk1? MkXTNVkxPjR5M{C=
CEM/C1 M2P2Wmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWCxNEDPxE1? MVHEUXNQ NEPlfJVGSzVyPUO4NkBvVQ>? MYOxPVA3PDd|MB?=
SUPTI[VB] M3zWNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmSxNVAh|ryP NVnxU4FxTE2VTx?= NWrvTFNCTUN3ME22NVkhdk1? NWrrZ|N7OTlyNkS3N|A>
CCRF–HSB-2 NYnLdWRPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFjmXlEyOCEQvF2= NXjaV4VjTE2VTx?= Mmn1SWM2OD1{MUG3JI5O MWmxPVA3PDd|MB?=
I 2.1 NUHFWlZ4SXCxcITvd4l{KGG|c3H5 NG\mSnIyOCEQvF2= NF3qO5JFVVOR MXrpcoR2[2W|IHHwc5B1d3Orcx?= MXexPVA3PDd|MB?=
I 9.2 M{nkb2Fxd3C2b4Ppd{Bie3OjeR?= NUfwRoJTOTBizszN NUOzcVNxTE2VTx?= NHrUc4VqdmS3Y3XzJIFxd3C2b4Ppdy=> NGTtNFQyQTB4NEezNC=>
A3 MWjBdI9xfG:|aYOgZZN{[Xl? M1r6TFExKM7:TR?= MonZSG1UVw>? MUPpcoR2[2W|IHHwc5B1d3Orcx?= NEjiToMyQTB4NEezNC=>
RD MofGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{fRZlExKM7:TR?= NF\jOYlKSzVyPkGwJO69VQ>? M4XjV|IxPzRyNkKz
Rh41 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NG[xOm8yOCEQvF2= M3f3NGlEPTB;M{OuPEBvVQ>? NGPTRYczODd2ME[yNy=>
Rh18 NHPt[mZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4PN[FExKM7:TR?= MXvJR|UxRTNyMzDuUS=> MYiyNFc1ODZ{Mx?=
Rh30 M3zUPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkXkNVAh|ryP MWLJR|UxRTRwOEGg{txO MmrBNlA4PDB4MkO=
BT-12 MojCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1S4XVExKM7:TR?= NEnZe|FKSzVyPkGwJO69VQ>? M{fU[VIxPzRyNkKz
CHLA-266 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlLwNVAh|ryP MWXJR|UxRTFwMkKg{txO MUSyNFc1ODZ{Mx?=
TC-71 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF:yVWkyOCEQvF2= M{\0SWlEPTB;Mj61NkDPxE1? MXqyNFc1ODZ{Mx?=
CHLA-9 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnrINVAh|ryP Mnr4TWM2OD13OUGgcm0> M{jJN|IxPzRyNkKz
CHLA-10 NF:x[I1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF;6eHMyOCEQvF2= M17ISmlEPTB;MUCyJI5O Mn\4NlA4PDB4MkO=
CHLA-258 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLITHh2OTBizszN M{PzUWlEPTB;MT6wOUDPxE1? M{jVTFIxPzRyNkKz
GBM2 M{\mfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIr2dm0yOCEQvF2= MljyTWM2OD17LkG1JO69VQ>? NVjIPGdGOjB5NEC2NlM>
NB-1643 Mn;US5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW[xNEDPxE1? NUDKSHp[UUN3ME21MlQh|ryP NEHISlczODd2ME[yNy=>
NB-Ebc1 M1raSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlzqNVAh|ryP NGDqNINKSzVyPkGwJO69VQ>? MoPkNlA4PDB4MkO=
CHLA-90 NHnsUm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV2xNEDPxE1? MXPJR|UxRjFyIN88US=> MnPxNlA4PDB4MkO=
CHLA-136 M4TaS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmX2NVAh|ryP NYXCNWdjUUN3ME6xNEDPxE1? NHPCO5gzODd2ME[yNy=>
NALM-6 NFjmUoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUCxNEDPxE1? MV\JR|UxRTJ4NTDuUS=> MmL0NlA4PDB4MkO=
COG-LL-317 NHzZZ21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4DlblExKM7:TR?= NVn2PXNuUUN3ME22MlQ6KG6P NWXSc5dUOjB5NEC2NlM>
RS4;11 NGPSbZFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3i0eVExKM7:TR?= M4LzdmlEPTB;MUS3JI5O MkLoNlA4PDB4MkO=
MOLT-4 M1\RV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWHvfHF3OTBizszN MV3JR|UxRTRyIH7N MmHWNlA4PDB4MkO=
CCRF-CEM NIrDfI1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVnMenpyOTBizszN NHHKXG1KSzVyPUK2PEBvVQ>? M33jUFIxPzRyNkKz
Kasumi-1 NIXWdZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkLpNVAh|ryP NIDSWmNKSzVyPUGwO{BvVQ>? MXeyNFc1ODZ{Mx?=
Karpas-299 NW[wd5kxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1rRU|ExKM7:TR?= MXrJR|UxRTJwOUOg{txO MkO1NlA4PDB4MkO=
Ramos-RA1 NF\wV4pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXuxNEDPxE1? NEXi[VNKSzVyPUeuN|Uh|ryP M3[3VlIxPzRyNkKz
H1299 NVXyXmNDU2mwYYPlJIF{e2G7 MlLTNVAh|ryP NHnQOnJqdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v MnPZNlE6ODh4MU[=

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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]
+ Expand
  • Animal Models: Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
  • Formulation: In polyethylene glycol 400/20% Vitamin E tocopheryl polyethylene glycol succinate (60:40) 30 mg/mL
  • Dosages: 200 mg/kg
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (197.6 mM)
Water 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
NCT02608411 Terminated Carcinoma Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
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
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3

Tech Support

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

Handling Instructions

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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

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID