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 MkK2T4lv[XOnIHHzd4F6 MoDSglExKM7:TR?= Ml\RbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MkPHNlA1QDRyMUi=
HT29 NX\j[YtTU2mwYYPlJIF{e2G7 NGnRVoR,OTBizszN NFnuepNqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NWDqVI1nOjB2OESwNVg>
MDA-MB-231 MV\LbY5ie2ViYYPzZZk> M4f6Tp4yOCEQvF2= NUH6UIVrcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MYqyNFQ5PDBzOB?=
NCI-H441 NWSzdVl1U2mwYYPlJIF{e2G7 NG\QdW1,OTBizszN MknlbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NWP2[45kOjB2OESwNVg>
SK-MEL-28 M2C3[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1TwU|M{KM7:TR?= NES0[3RKSzVyPkOzJO69VQ>? MYKyNFQ5PDBzOB?=
NCI-H661 NHPNR|RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV7ze5JpOzNizszN Mn;0TWM2OD5|MzFOwG0> M3fmRlIxPDh2MEG4
NCI-H446 NG\1fG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUWzN{DPxE1? MmnRTWM2OD15IN88US=> Ml;RNlA1QDRyMUi=
MDA-MB-231 MnvmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\jZVM{KM7:TR?= NV\IfplqUUN3ME2wMlU2KM7:TR?= NWiwXVZJOjB2OESwNVg>
DLD-1 NEjTcJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVnJXG5zOzNizszN MoC0TWM2OD1yLkWzJO69VQ>? NWPDfZF3OjB2OESwNVg>
A549 MmHES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4DUWVM{KM7:TR?= MnPnTWM2OD1yLkW5JO69VQ>? MVyyNFQ5PDBzOB?=
SK-OV-3 NYK5UG0zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4jWZlM{KM7:TR?= NGLr[45KSzVyPUCuOlYh|ryP NX;1ZZVSOjB2OESwNVg>
NCI-H460 NHLDemFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYqzN{DPxE1? NI[4eYtKSzVyPUCuOkDPxE1? M{TWRVIxPDh2MEG4
A375 M3e4emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{\GU|M{KM7:TR?= NFT6cXpKSzVyPUCuOFIh|ryP NVPXbmU4OjB2OESwNVg>
NCI-H441 NXzoR2dlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmXhN|Mh|ryP NU\vOldPUUN3ME2wMlMh|ryP M{jIN|IxPDh2MEG4
HT29 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDGRm4{OyEQvF2= Mme5TWM2OD1yLkS5JO69VQ>? MmfSNlA1QDRyMUi=
MKN-45 M3PSRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFXIT3U{OyEQvF2= NGT2XoJKSzVyPUCuOVgh|ryP NXfXc25WOjB2OESwNVg>
HT29 NFfvfoVCeG:ydH;zbZMh[XO|YYm= MlnmglExKM7:TR?= NUH2[ZJie2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu M1zFe|IxPDh2MEG4
MKN-45 MXzBdI9xfG:|aYOgZZN{[Xl? MlvTglExKM7:TR?= MUDzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? M4jWdVIxPDh2MEG4
MDA-MB-231 NFXmc|lCeG:ydH;zbZMh[XO|YYm= NIC2TnJ,OTBizszN NHjZRVJud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu MYeyNFQ5PDBzOB?=
MDA-MB-231/TGL MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlvLglExOCEQvF2= NXnqNFJQT0l3ME2xMlIh|ryP NULqSoV2OjJyMke2PVA>
1833/TGL MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX\MXnF4hjFyMDFOwG0> MUfHTVUxRTNwNzFOwG0> Mm\INlIxOjd4OUC=
EBC1 M3\OR2N6fG:2b4jpZ:Kh[XO|YYm= MmDuglExKM7:TR?= M{XsS4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= MlfrNlM2QTh{N{[=
SNU638 MnrlR5l1d3SxeHnjxsBie3OjeR?= M{i3N54yOCEQvF2= MmjNbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= NXTtb5RZOjN3OUiyO|Y>
A549 M3[wZ2N6fG:2b4jpZ:Kh[XO|YYm= NVzyemJthjFyIN88US=> MYHuc5Qh[W[oZXP0 NVKwTlVPOjN3OUiyO|Y>
H460 NEjTNoVEgXSxdH;4bYPDqGG|c3H5 NFXFZm5,OTBizszN NXTWcll2dm:2IHHm[oVkfA>? NVLDVHJFOjN3OUiyO|Y>
HCC827 MlnLR5l1d3SxeHnjxsBie3OjeR?= MYL+NVAh|ryP NIrle5Fvd3RiYX\m[YN1 NEnucVMzOzV7OEK3Oi=>
A549 NXTqUGI2TnWwY4Tpc44h[XO|YYm= NYXGWFd5OTBizszN Ml7I[Il{enWydIOgcYlkem:2dXL1cIU> M4qyT|I{PTl6Mke2
EBC1 Ml3MSpVv[3Srb36gZZN{[Xl? Ml;xNVAh|ryP NWrh[YRn\Gm|coXweJMhdWmlcn;0eYJ2dGV? NVzNWHNIOjN3OUiyO|Y>
H460 MkC3SpVv[3Srb36gZZN{[Xl? NF\PeHkyOCEQvF2= MnOxbY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? NVG2TZJVOjV|MUOwNVA>
K562/VCR NEjT[5JEgXSxdH;4bYPDqGG|c3H5 NVvi[JhmhjFyIN88US=> NFrHNnh{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= MUOyOVMyOzBzMB?=
CEM/VBL M2jod2N6fG:2b4jpZ:Kh[XO|YYm= NFOzRoZ,OTBizszN NF:1WFl{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M2HiOlI2OzF|MEGw
U266 NXf5U2xqS3m2b4TvfIlkyqCjc4PhfS=> M1\GR54{KM7:TdMg M13EeGlEPTB;MT6xJO69VQ>? NH62fWQzPThzMECxNy=>
OPM-2 MY\DfZRwfG:6aXRCpIF{e2G7 NImzcmV,OyEQvF5CpC=> MkLRTWM2OD1zLkig{txO MX[yOVgyODBzMx?=
MM.1S NGXDSZBEgXSxdH;4bYPDqGG|c3H5 MkjRglMh|ryPwrC= MmXKTWM2OD1zLk[g{txO MnvQNlU5OTByMUO=
MM.1R NIrDTFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlzRN{DPxE4EoB?= MUHpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= MlXzNlU5OTByMUO=
RPMI-8226 MVfDfZRwfG:6aXRCpIF{e2G7 NXrSSnRHhjNizszNxsA> M4PLR2lEPTB;MD65JO69VQ>? M{LZOVI2QDFyMEGz
ANBL-6 MYDDfZRwfG:6aXRCpIF{e2G7 NY\nbW52OSEQvF5CpC=> MXfpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NIjlbI4zPThzMECxNy=>
ANLB-6/V10R MnHpR5l1d3SxeHnjxsBie3OjeR?= M2TMXVEh|ryPwrC= MkjVbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= M2TaUVI2QDFyMEGz
KAS-6/1 Ml33R5l1d3SxeHnjxsBie3OjeR?= MY[xJO69VcLi MkfjbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= Mmr5NlU5OTByMUO=
KAS-6/V10R MoLLR5l1d3SxeHnjxsBie3OjeR?= MUmxJO69VcLi M{nVS4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NWjDSZpxOjV6MUCwNVM>
KAS-6/R10R NV\oPHlUS3m2b4TvfIlkyqCjc4PhfS=> NIDzN2IyKM7:TdMg Mlu5bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NEHXR2EzPThzMECxNy=>
8226/S MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1XweVMh|ryPwrC= MVfpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NF;Ne|EzPThzMECxNy=>
8226/LR-5 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHWyZ5k{KM7:TdMg MlzHbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NFGzVIUzPThzMECxNy=>
Huh7 NYLiN2MyS3m2b4TvfIlkyqCjc4PhfS=> Mk\HglQvQCEQvF5CpC=> NGPGc|FFVVOR NX72T4s1UUN3ME25Mlkhdk1? MkfaNlYzPTl{NUC=
Hep3B NIL6dGlEgXSxdH;4bYPDqGG|c3H5 M4XZfJ41NjhizszNxsA> M2LUO2ROW09? MnjjTWM2OD12NEiuO{BvVQ>? M17BZVI3OjV7MkWw
HepG2 MoTvR5l1d3SxeHnjxsBie3OjeR?= M2DZWp41NjhizszNxsA> NEXDVVZFVVOR MlvsTWM2OD1zM{muO|chdk1? MmDxNlYzPTl{NUC=
Chang M{fZ[mN6fG:2b4jpZ:Kh[XO|YYm= NV\UdWxqhjRwODFOwG3DqA>? MY\EUXNQ MX3JR|UxRTR2OD63JI5O NGLFVnYzPjJ3OUK1NC=>
Huh7 MUnGeY5kfGmxbjDhd5NigQ>? NXnkfJhQOS54IN88UeKh MlP4SG1UVw>? MmXWZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NYjV[pNSOjZ{NUmyOVA>
Hep3B MnXOSpVv[3Srb36gZZN{[Xl? M3uwR|EvPiEQvF5CpC=> NYD2eXV[TE2VTx?= M2HP[YNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NVXOW|NKOjZ{NUmyOVA>
HepG2 MlrCSpVv[3Srb36gZZN{[Xl? NUjhT2xXOS54IN88UeKh MoDVSG1UVw>? NIPJRYxk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NWfvNYF3OjZ{NUmyOVA>
Chang MoS3SpVv[3Srb36gZZN{[Xl? MYSxMlYh|ryPwrC= MkOySG1UVw>? MXHjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MWeyOlI2QTJ3MB?=
MHCC97L NVzIRY1bT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUf5O5JyhjFyIN88US=> NFTFPVBFVVOR M37OU2lEPTB;M{G1JI5O MVWyOlQ2QDl3Mx?=
MHCC97H M2TnTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4PE[p4yOCEQvF2= NXHHfXRNTE2VTx?= NHjZbXBKSzVyPUO2PQKBkSCwTR?= M{PqSFI3PDV6OUWz
Huh7 M1\QN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2DoVp4yOCEQvF2= NETQeXNFVVOR MnLETWM2OD1{NkWgcm0> M3LXN|I3PDV6OUWz
HepG2 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4WwWZ4yOCEQvF2= MkTOSG1UVw>? MVfJR|UxRTN7MjDuUS=> MkTlNlY1PTh7NUO=
MHCC97L NYfqfodpTnWwY4Tpc44h[XO|YYm= NGmweGEyKM7:TdMg NX2ybIZqTE2VTx?= NWe5SlJKcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NI\ZdokzPjR3OEm1Ny=>
Huh7 NX\x[ndHTnWwY4Tpc44h[XO|YYm= NY\xeYtROSEQvF5CpC=> NXTLd49STE2VTx?= M4D6[Ilv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NXTsUnVZOjZ2NUi5OVM>
MHCC97L MUHBdI9xfG:|aYOgZZN{[Xl? MWGxJO69VcLi NG[5TGFFVVOR NIfJZ4RqdmS3Y3XzJIFxd3C2b4Ppdy=> MWKyOlQ2QDl3Mx?=
Huh7 MnPYRZBweHSxc3nzJIF{e2G7 NYHUbHRxOSEQvF5CpC=> Ml\lSG1UVw>? MWPpcoR2[2W|IHHwc5B1d3Orcx?= MYGyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts NIf5TXFMcW6jc3WgZZN{[Xl? NXPIO29zOjVizszN MluxSG1UVw>? M{jVR5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> M3KwdFIxPTN2M{S1
H23 NXrLeFdFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1LQOVI2KM7:TR?= NIOyZoNFVVOR MV;zbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= M3qybVIxPTN2M{S1
WM35 NIjHNY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVj3T2p[OTBizszN MXXEUXNQ M1\Wc5Nq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu M2GxUFIxPTN2M{S1
NIH 3T3 NHjIRXlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnnkNVAh|ryP NWr1c2x1TE2VTx?= NEfoUmpld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NIP4OoYzODV|NEO0OS=>
H838 NHq0XY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXWxNEDPxE1? M4SxUmROW09? NYPKWXl4\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NHrybIkzODV|NEO0OS=>
H1395 M{nHOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIH4b4QyOCEQvF2= NHzT[5hFVVOR NGPldWZld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NFnwNnQzODV|NEO0OS=>
Quiescent S2 M3vmdGtqdmG|ZTDhd5NigQ>? NWPsdlRTOzBizszN M4PvOGROW09? MXrjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? NHPwZnUzOTVzOEmxOS=>
PC3 MUXBdI9xfG:|aYOgZZN{[Xl? M3jj[VIxKM7:TR?= MVjEUXNQ M2q0Nolv\HWlZYOgZZBweHSxc3nz MViyNVcxQTF|MB?=
Du145 NWn0e4FuSXCxcITvd4l{KGG|c3H5 NV7xbHBUOjBizszN MkWwSG1UVw>? MkPNbY5lfWOnczDhdI9xfG:|aYO= NHe2SG8zOTdyOUGzNC=>
LNCaP MV7BdI9xfG:|aYOgZZN{[Xl? MoHHNlAh|ryP NVTMfGpyTE2VTx?= M376OYlv\HWlZYOgZZBweHSxc3nz NUTUOopIOjF5MEmxN|A>
LAPC-4 MljORZBweHSxc3nzJIF{e2G7 MkTZNlAh|ryP MmHkSG1UVw>? MY\pcoR2[2W|IHHwc5B1d3Orcx?= MYiyNVcxQTF|MB?=
LNCaP MnjaSpVv[3Srb36gZZN{[Xl? NXj0N41ZOjBizszN M2Lpe2ROW09? M3rrN4Rm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? MUeyNVcxQTF|MB?=
LAPC-4 MXvGeY5kfGmxbjDhd5NigQ>? NIrkPVMzOCEQvF2= NWXMS2VOTE2VTx?= NHnGN2xl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| MljaNlE4ODlzM{C=
Kasumi-1 MoL6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmDmglUxKM7:TR?= MlPsSG1UVw>? NGHSeJBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M1LZPVI{OzlyNUO2
SKNO-1 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2q5[J42OCEQvF2= NXLaeHpnTE2VTx?= M1fKTYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Ml71NlM{QTB3M{[=
Kasumi-1 MnP1T4lv[XOnIHHzd4F6 NVPjTWZ3hjFyIN88US=> NWnqenJDTE2VTx?= MXTy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NFH0PZEzOzN7MEWzOi=>
SKNO-1 MV;LbY5ie2ViYYPzZZk> MoDYglExKM7:TR?= NIrGbI9FVVOR NIL3SWxz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MVKyN|M6ODV|Nh?=
A549 MoPlSpVv[3Srb36gZZN{[Xl? NY\QZm84OTBizszN MoPlSG1UVw>? M{iwdIVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> NEDROVczPDd2NkW3OC=>
NRK-52E Mm\uSpVv[3Srb36gZZN{[Xl? M2PYTlExKM7:TR?= NWXNXYI2TE2VTx?= M3ntSYlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv M{\mb|I2ODh6MECy
PC12 NEPV[YNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2G0XJ4yOi53IN88US=> NXLOXGFCTE2VTx?= MX;wdoV3\W62czDUV2EucW6mdXPl[EBv\XW{aYTlJIZwem2jdHnvci=> MlrTNlUyOjh|OE[=
HPMCs NI\lZ|lHfW6ldHnvckBie3OjeR?= MljWdoV3\XK|ZYOg[ZBqfGinbHnhcEB1dyCvZYPlcoNpgW2jbDD0doFve2m2aX;uJI9nKGi3bXHuJJBmemm2b37lZYwhdWW|b4To[Yxq[WxiY3XscJM> NFznV24zPjB2NUe4NC=>
A549 NGXzcWRHfW6ldHnvckBie3OjeR?= NY\nO49QhjVyIN88US=> NFTQTVhFVVOR NWjWRY14[W[oZXP0d{B1cGVidnnyZYwhdGmoZTDjfYNt\SCjbnSgbI9{fCC{ZYPwc45{\Q>? MkjoNlY4OTF5NEi=
RAW264.7 NGm3SnNHfW6ldHnvckBie3OjeR?= MlvOglMxKM7:TR?= MYDEUXNQ NWPWZm5MemWmdXPld{Bxem9vaX7mcIFudWG2b4L5JIdmdmViZYjwdoV{e2mxbh?= M3no[|I3PzF6NUi2
MEMM NF6wcGRMcW6jc3WgZZN{[Xl? NFfZZpgyPSEEtV2= NVrvVmZMTE2VTx?= NXvWRm1P\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> MXeyOlkzOTVyNh?=
MEMM NXvzVIpTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4H4Rp4zOCEEtV2= MkPGSG1UVw>? NFfqV3dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MWCyOlkzOTVyNh?=
MEMM M3jyT2Fxd3C2b4Ppd{Bie3OjeR?= M3L4NFE2KML3TR?= NU\DVHJZTE2VTx?= MXHpcoR2[2W|IITo[UBxemW|ZX7j[UBw\iC2aHWgZZBweHSxc3nzJJBzd3SnaX6sJINt\WG4ZXSgR4F{eGG|ZT2z MWmyOlkzOTVyNh?=
T47D M{LBfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYPZepdsOTBizszN MUDEUXNQ NFTqPY5KSzVyPUeyJI5O MWCxPFM5OTR2NB?=
ZR-75-1 NGD2[5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mo\SNVAh|ryP M{XHRWROW09? Mk\xTWM2OD15OTDuUS=> NHXtWogyQDN6MUS0OC=>
BT474 NIqzR3NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVyxNEDPxE1? MlTMSG1UVw>? MVHJR|UxRTh4IH7N NGLvSHoyQDN6MUS0OC=>
HCC1954 NF;5TZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmTzNVAh|ryP NYPiVoROTE2VTx?= NEH4fZFKSzVyPUGxPUBvVQ>? MXqxPFM5OTR2NB?=
MDA-MB-453 NFzNbFhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH7vU2UyOCEQvF2= NGLP[GdFVVOR NIrjeJJKSzVyPUm3OUBvVQ>? MX6xPFM5OTR2NB?=
MDA-MB-468 M2P4PGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUixNEDPxE1? MULEUXNQ NH;XTZJKSzVyPUOyNFghdk1? M{fwdFE5OzhzNES0
SkBr3 MkTCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVvvZVMxOTBizszN M3vO[2ROW09? MWPJR|UxRjFyLECwNEBvVQ>? NF24e3YyQDN6MUS0OC=>
MDA-MB-231 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX6xNEDPxE1? NEjmNo9FVVOR Mme0TWM2OD5zMDywNFAhdk1? M3;CXFE5OzhzNES0
HCT116 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlTENVAh|ryP M1[5VmROW09? NFG0XZlKSzVyPUW4N|Yhdk1? NFTtT3kyQDN6MUS0OC=>
HT29 Ml\yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2LVV|ExKM7:TR?= M2DDfGROW09? MUXJR|UxRjFyLECwNEBvVQ>? M13lTFE5OzhzNES0
HFF M13zfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH\OS48yOCEQvF2= NF\HeWVFVVOR MXHJR|UxRTd4MUWgcm0> NUPtNms3OTh|OEG0OFQ>
HN5 M2jRUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXWxNEDPxE1? M33sPGROW09? M{HD[2lEPTB-MUCsNFAxKG6P MoDENVg{QDF2NES=
786-0 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MojzNVAh|ryP MYjEUXNQ M1Gwc2lEPTB;NECwPUBvVQ>? M3;HcVE5OzhzNES0
H157 NH3DWG9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2no[|ExKM7:TR?= NWqzd3pLTE2VTx?= M3TUeGlEPTB;Mk[0NkBvVQ>? NYjoXXM2OTh|OEG0OFQ>
NCI-H460 NYXW[G14T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3\We|ExKM7:TR?= NUfSfGFmTE2VTx?= NGXPWWNKSzVyPkKsOVAxKG6P MkfFNVg{QDF2NES=
SKOV-3 M{j0eWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHTNVoYyOCEQvF2= MWTEUXNQ M1WzXGlEPTB;MkGyOkBvVQ>? MoDRNVg{QDF2NES=
OVCAR-3 NGHOb5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVGxNEDPxE1? NEK0[opFVVOR MWLJR|UxRTJ7MUigcm0> MV:xPFM5OTR2NB?=
BXPC3 NHPlNWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MofuNVAh|ryP NUDiNnhjTE2VTx?= Mn\HTWM2OD1|MUSxJI5O NES0S40yQDN6MUS0OC=>
MiaPaCa M37EdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW[xNEDPxE1? NHXCOWhFVVOR Mn3oTWM2OD13NEOzJI5O NFS2NnIyQDN6MUS0OC=>
PANC-1 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWrlc49[OTBizszN M2nUO2ROW09? MWfJR|UxRTh4OEGgcm0> M3G5blE5OzhzNES0
LNCaP MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFLPXmEyOCEQvF2= M3jQeWROW09? Mm\kTWM2OD1zNEegcm0> MnrKNVg{QDF2NES=
DU145 Mkn0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1Xke|ExKM7:TR?= NYDkRmJNTE2VTx?= M2TyV2lEPTB;M{ixNkBvVQ>? MmX4NVg{QDF2NES=
PC3 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWKxNEDPxE1? NF\6O4ZFVVOR MmfpTWM2OD5zMDywNFAhdk1? M2rJWFE5OzhzNES0
BT474 MX3LbY5ie2ViYYPzZZk> NI\LZmcyOCEQvF2= MV;EUXNQ M2\GRYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF4MDDuUS=> M{T6flE5OzhzNES0
786-0 NFP4bZJMcW6jc3WgZZN{[Xl? MVuxNEDPxE1? M2HBOmROW09? MlvZbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTVyIH7N MYGxPFM5OTR2NB?=
LNCaP MWLLbY5ie2ViYYPzZZk> MlW3NVAh|ryP NWjUR3J4TE2VTx?= MV3pcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1OyCwTR?= NUmzS3h4OTh|OEG0OFQ>
PC3 MUHLbY5ie2ViYYPzZZk> M1LZPVExKM7:TR?= NYL5cWJ7TE2VTx?= MWTpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1QSCwTR?= MVuxPFM5OTR2NB?=
KARPAS-231 NUTlVXR1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnvONVAh|ryP M2LwSWROW09? MmrZSWM2OD12MTDuUS=> MmT2NVkxPjR5M{C=
CCRFSB NEjPdppIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXexNEDPxE1? MlvUSG1UVw>? M2O5N2VEPTB;MUW1JI5O MofMNVkxPjR5M{C=
SUP B15 NV7a[HBRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEWyNFEyOCEQvF2= M17CV2ROW09? MV;FR|UxRTF7NzDuUS=> MnLFNVkxPjR5M{C=
SD-1 Mn3TS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFy5dHMyOCEQvF2= NHf4TYVFVVOR NG\jUplGSzVyPUOyNEBvVQ>? MmPpNVkxPjR5M{C=
RS4;11 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MojzNVAh|ryP NGLPblJFVVOR NHuydGRGSzVyPU[1OEBvVQ>? NHjRbVkyQTB4NEezNC=>
MN-60 NH;zXIRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWixNEDPxE1? NUTUbJhuTE2VTx?= NU\Bb5JyTUN3ME2zOlAzKG6P NUjqUoExOTlyNkS3N|A>
Tanoue MmnES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml\wNVAh|ryP M1PGTGROW09? MnHFSWM2OD12NUG3JI5O NXHpU2pMOTlyNkS3N|A>
RCH-ACV MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEGydHkyOCEQvF2= NXjpPWQ6TE2VTx?= NXHZcoxZTUN3ME2xOVIhdk1? NF:1bYUyQTB4NEezNC=>
SEM MoD0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUOxNEDPxE1? MUfEUXNQ MoDTSWM2OD1{MEKgcm0> MojDNVkxPjR5M{C=
KASUMI-2 NVv3fZp{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3i4SlExKM7:TR?= NUf2bWRxTE2VTx?= NXXEdphJTUN3ME2yNlUhdk1? Ml\vNVkxPjR5M{C=
REH NYTMRZI{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWTvRZRXOTBizszN MVfEUXNQ M3HGSGVEPTB;Mki4JI5O Ml\BNVkxPjR5M{C=
697 NWrGT|l2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVL2N5d1OTBizszN MYDEUXNQ NEDUOWtGSzVyPUOzPEBvVQ>? M2ruZVE6ODZ2N{Ow
NALM-6 MmLkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2rDOlExKM7:TR?= M1nZOWROW09? NUKxN5VMTUN3ME20NlEhdk1? M2q0eVE6ODZ2N{Ow
MHH-CALL–3 M3nSWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3f6[VExKM7:TR?= MVzEUXNQ NGHIZY9GSzVyPUixNkBvVQ>? NGXlPJkyQTB4NEezNC=>
MHH-CALL–2 NWLnV|ZRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmruNVAh|ryP MmfaSG1UVw>? M1jic2VEPTB;MkGxOEBvVQ>? M2Pv[FE6ODZ2N{Ow
J.GAMMA-1 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEX1ZZQyOCEQvF2= Ml;MSG1UVw>? MYDFR|UxRTZ3IH7N MmHENVkxPjR5M{C=
JR45.01 M2DJ[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV7RVpJZOTBizszN MXzEUXNQ MVLFR|UxRTZ6IH7N NYry[GNpOTlyNkS3N|A>
A3 M2TPc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlKwNVAh|ryP NWrzSoZ4TE2VTx?= MYHFR|UxRTZ7IH7N MoH4NVkxPjR5M{C=
I 2.1 M2jYVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIPVcJMyOCEQvF2= MWPEUXNQ MYDFR|UxRTd|IH7N NUfqOlNEOTlyNkS3N|A>
MOLT-3 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmrtNVAh|ryP Ml75SG1UVw>? MUTFR|UxRTd2IH7N MV2xPVA3PDd|MB?=
P116 M1nzcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2nJWVExKM7:TR?= M2nrdmROW09? MnzISWM2OD15ODDuUS=> M4rSTVE6ODZ2N{Ow
J.Cam1.6 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXqxNEDPxE1? M2rIVWROW09? M4\MPGVEPTB;N{mgcm0> MnHvNVkxPjR5M{C=
I 9.2 NYrEWIU4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUTEN4pFOTBizszN NUS1bXZYTE2VTx?= M{LNdmVEPTB;OECgcm0> M4O3XVE6ODZ2N{Ow
LOUCY M37De2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGrFencyOCEQvF2= Mln1SG1UVw>? NYi4VZRtTUN3ME2xNVchdk1? M4\NelE6ODZ2N{Ow
J.RT3-T3.5 NIXZcmhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlviNVAh|ryP M2CxV2ROW09? NVTscpN{TUN3ME2xNlMhdk1? M{LMZVE6ODZ2N{Ow
800000 NVzOd4NHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPtVWwyOCEQvF2= M{fZcWROW09? NW\0N2lGTUN3ME2xOlMhdk1? NEjOdHMyQTB4NEezNC=>
Jurkat M1zSS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2ezOVExKM7:TR?= NHjXOZRFVVOR MYTFR|UxRTJ{NTDuUS=> M4TWXFE6ODZ2N{Ow
MOLT-4 MofLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkHGNVAh|ryP NYjobJF6TE2VTx?= MmXjSWM2OD1{M{Kgcm0> MmDXNVkxPjR5M{C=
Molt-16 Mn7ES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmm1NVAh|ryP MV\EUXNQ NUjmV3lKTUN3ME2yOFEhdk1? NXzRWZhIOTlyNkS3N|A>
CEM/C3 MnrnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGD2eVcyOCEQvF2= M3vQSGROW09? MVLFR|UxRTJ3NzDuUS=> NV;mXWZFOTlyNkS3N|A>
CEM/C2 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUTmbIc3OTBizszN NF31UohFVVOR NFvZeXdGSzVyPUK3NUBvVQ>? MoDYNVkxPjR5M{C=
CCRFCEM NIGzcI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYWxNEDPxE1? NIDTZppFVVOR MUjFR|UxRTN{NzDuUS=> NWDNUW0{OTlyNkS3N|A>
CEM/C1 MmXyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\zWVExKM7:TR?= NYrjRYQ{TE2VTx?= MXHFR|UxRTN6MjDuUS=> NG\BfIIyQTB4NEezNC=>
SUPTI[VB] MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MU[xNEDPxE1? NHzPRYFFVVOR M3POcGVEPTB;NkG5JI5O MkW1NVkxPjR5M{C=
CCRF–HSB-2 NWDmbJJVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHW4SnAyOCEQvF2= NVrDOlF4TE2VTx?= Mn\qSWM2OD1{MUG3JI5O NWTkOJVEOTlyNkS3N|A>
I 2.1 MmjlRZBweHSxc3nzJIF{e2G7 MmfvNVAh|ryP M2TKcGROW09? MmqybY5lfWOnczDhdI9xfG:|aYO= M{Czd|E6ODZ2N{Ow
I 9.2 MW\BdI9xfG:|aYOgZZN{[Xl? NVO2VWR3OTBizszN M3jmN2ROW09? MUjpcoR2[2W|IHHwc5B1d3Orcx?= MUixPVA3PDd|MB?=
A3 M3TlWWFxd3C2b4Ppd{Bie3OjeR?= M{O2W|ExKM7:TR?= M{DIbWROW09? Mnq1bY5lfWOnczDhdI9xfG:|aYO= M1TwUVE6ODZ2N{Ow
RD MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPZb|kyOCEQvF2= NU\pPZVDUUN3ME6xNEDPxE1? MlT5NlA4PDB4MkO=
Rh41 NGfwSodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnHUNVAh|ryP NXGyN45NUUN3ME2zN{45KG6P MX2yNFc1ODZ{Mx?=
Rh18 NYrJTJk2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1LuZ|ExKM7:TR?= NV;KRXJrUUN3ME2zNFMhdk1? MXeyNFc1ODZ{Mx?=
Rh30 MnPoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYexNEDPxE1? M1vYOWlEPTB;ND64NUDPxE1? MYSyNFc1ODZ{Mx?=
BT-12 NUHKR2VnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUWxNEDPxE1? MWTJR|UxRjFyIN88US=> MYmyNFc1ODZ{Mx?=
CHLA-266 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFLIfG4yOCEQvF2= NUPGR5pqUUN3ME2xMlIzKM7:TR?= M{S1WVIxPzRyNkKz
TC-71 NGXtdY9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4LsdVExKM7:TR?= M{XpWmlEPTB;Mj61NkDPxE1? NEPMSnkzODd2ME[yNy=>
CHLA-9 NHf4bJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGj4[G8yOCEQvF2= NX;UO4dKUUN3ME21PVEhdk1? NHzNSYEzODd2ME[yNy=>
CHLA-10 M4H5XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmnUNVAh|ryP Mn7KTWM2OD1zMEKgcm0> NIDBVHIzODd2ME[yNy=>
CHLA-258 MnHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGHVTWQyOCEQvF2= MnP1TWM2OD1zLkC1JO69VQ>? MXeyNFc1ODZ{Mx?=
GBM2 Ml2yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFrFUWgyOCEQvF2= MV;JR|UxRTlwMUWg{txO MWeyNFc1ODZ{Mx?=
NB-1643 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWP1cWE4OTBizszN NUf4fnJUUUN3ME21MlQh|ryP MUeyNFc1ODZ{Mx?=
NB-Ebc1 M4\VPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHLhXJUyOCEQvF2= NYL5fGVNUUN3ME6xNEDPxE1? MWOyNFc1ODZ{Mx?=
CHLA-90 NUnjZlg{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX[xNEDPxE1? NVHoWlIxUUN3ME6xNEDPxE1? NVPwcpJpOjB5NEC2NlM>
CHLA-136 M2HYcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;OSJZTOTBizszN MUfJR|UxRjFyIN88US=> MV:yNFc1ODZ{Mx?=
NALM-6 NXS5Zm5mT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVLESlBUOTBizszN MV\JR|UxRTJ4NTDuUS=> NHPBeJkzODd2ME[yNy=>
COG-LL-317 NWjZbVZZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWKxNEDPxE1? MmjXTWM2OD14LkS5JI5O NGrqbWkzODd2ME[yNy=>
RS4;11 NVi3PG1RT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkjkNVAh|ryP NX6ydFQ5UUN3ME2xOFchdk1? NFLFdpozODd2ME[yNy=>
MOLT-4 M2LleGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFn1TWQyOCEQvF2= MVzJR|UxRTRyIH7N NETrcnQzODd2ME[yNy=>
CCRF-CEM NWS0XZFrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2K3UFExKM7:TR?= MljDTWM2OD1{Nkigcm0> M4jOSVIxPzRyNkKz
Kasumi-1 NVrKd|lWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojHNVAh|ryP M{\Se2lEPTB;MUC3JI5O M1fVRlIxPzRyNkKz
Karpas-299 MkXkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{PXTVExKM7:TR?= NUTVS5g5UUN3ME2yMlk{KM7:TR?= NUHkS4ZFOjB5NEC2NlM>
Ramos-RA1 MnK4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWqxNEDPxE1? M{nP[2lEPTB;Nz6zOUDPxE1? MV[yNFc1ODZ{Mx?=
H1299 NVTnOGQ3U2mwYYPlJIF{e2G7 NHLXTHoyOCEQvF2= MVPpcohq[mm2czDJT2JMTS2rbnT1Z4VlKEGtdDDBZ5RqfmG2aX;u MXKyNVkxQDZzNh?=

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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
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 24, 2011 Phase 1
NCT02608411 Recruiting Carcinoma, Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace, Inc. April 2014 Phase 1
NCT02029157 Recruiting Liver Cancer Kyowa Hakko Kirin Co., Ltd January 2014 Phase 3
NCT01892527 Active, not recruiting Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro, MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Active, not recruiting Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro, MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2

Tech Support

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

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