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 MUfLbY5ie2ViYYPzZZk> NYHMUWNHhjFyIN88US=> NWT2c45VcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MV2yNFQ5PDBzOB?=
HT29 M3i2NGtqdmG|ZTDhd5NigQ>? M4PMPZ4yOCEQvF2= NUT6bnAzcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NILSeoIzODR6NECxPC=>
MDA-MB-231 NVnMeoczU2mwYYPlJIF{e2G7 M1i1SJ4yOCEQvF2= NFqzVZpqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MnHRNlA1QDRyMUi=
NCI-H441 MlrsT4lv[XOnIHHzd4F6 NVvxUVNRhjFyIN88US=> NICwVHVqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz M{fFb|IxPDh2MEG4
SK-MEL-28 MnzQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWnsOFlDOzNizszN NFLXT3dKSzVyPkOzJO69VQ>? NIPkSJozODR6NECxPC=>
NCI-H661 MoW0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIHqRlc{OyEQvF2= MX7JR|UxRjN|IN88US=> MlHvNlA1QDRyMUi=
NCI-H446 NV;WeYRrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{PRUFM{KM7:TR?= M4fUVWlEPTB;NzFOwG0> MUeyNFQ5PDBzOB?=
MDA-MB-231 Ml7uS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1;sclM{KM7:TR?= Mni0TWM2OD1yLkW1JO69VQ>? MVeyNFQ5PDBzOB?=
DLD-1 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWKzN{DPxE1? NUX2VIlkUUN3ME2wMlU{KM7:TR?= MViyNFQ5PDBzOB?=
A549 NXiyO45VT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEjjR3c{OyEQvF2= MUfJR|UxRTBwNUmg{txO M{HnT|IxPDh2MEG4
SK-OV-3 MmjaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmnVN|Mh|ryP NWXmS4xQUUN3ME2wMlY3KM7:TR?= Mn\XNlA1QDRyMUi=
NCI-H460 M3;lUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3IUoZnOzNizszN MkC1TWM2OD1yLk[g{txO NH7UXY8zODR6NECxPC=>
A375 NXLu[WhHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWezN{DPxE1? MWjJR|UxRTBwNEKg{txO M{S2WlIxPDh2MEG4
NCI-H441 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIS1dII{OyEQvF2= NFzzZ5NKSzVyPUCuN{DPxE1? NEm3NHYzODR6NECxPC=>
HT29 NVLyfplZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXL5OXRzOzNizszN NETEPYZKSzVyPUCuOFkh|ryP NEXYUI0zODR6NECxPC=>
MKN-45 M33qZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV:zN{DPxE1? NUTsWodMUUN3ME2wMlU5KM7:TR?= MnLINlA1QDRyMUi=
HT29 NYHQenBJSXCxcITvd4l{KGG|c3H5 MU\+NVAh|ryP MoGyd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NH[3d20zODR6NECxPC=>
MKN-45 MULBdI9xfG:|aYOgZZN{[Xl? M2C1bZ4yOCEQvF2= NFrXSIx{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= M4LNU|IxPDh2MEG4
MDA-MB-231 NFq5ZY9CeG:ydH;zbZMh[XO|YYm= MnvOglExKM7:TR?= NID4fnpud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu M{fIN|IxPDh2MEG4
MDA-MB-231/TGL M1PzOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M13JZp4yODBizszN MW\HTVUxRTFwMjFOwG0> NFS2eWYzOjB{N{[5NC=>
1833/TGL MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEOyVlZ,OTByIN88US=> NF\xOYNIUTVyPUOuO{DPxE1? NUSzc|VEOjJyMke2PVA>
EBC1 M1LLO2N6fG:2b4jpZ:Kh[XO|YYm= MWT+NVAh|ryP NF7rTXlqdmirYnn0d{B1cGViY3XscEBoem:5dHiu MX[yN|U6QDJ5Nh?=
SNU638 MWHDfZRwfG:6aXRCpIF{e2G7 MYH+NVAh|ryP NFHncldqdmirYnn0d{B1cGViY3XscEBoem:5dHiu MoLRNlM2QTh{N{[=
A549 M3TtXWN6fG:2b4jpZ:Kh[XO|YYm= NILYO3Z,OTBizszN MXfuc5Qh[W[oZXP0 NX\oW5g6OjN3OUiyO|Y>
H460 M4DCWmN6fG:2b4jpZ:Kh[XO|YYm= NFXIZ4p,OTBizszN NGDO[Y9vd3RiYX\m[YN1 MXeyN|U6QDJ5Nh?=
HCC827 NIrDSolEgXSxdH;4bYPDqGG|c3H5 NVvqSWRKhjFyIN88US=> MW\uc5Qh[W[oZXP0 NH:3TXozOzV7OEK3Oi=>
A549 Mo\LSpVv[3Srb36gZZN{[Xl? NH;6UGMyOCEQvF2= Mk\B[Il{enWydIOgcYlkem:2dXL1cIU> M2fsVVI{PTl6Mke2
EBC1 M3\USGZ2dmO2aX;uJIF{e2G7 M4TrV|ExKM7:TR?= M2nYTYRqe3K3cITzJI1q[3KxdIXieYxm MViyN|U6QDJ5Nh?=
H460 NWfPUmY1TnWwY4Tpc44h[XO|YYm= NEHEOoYyOCEQvF2= NHfrZVJqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w NV31U5ZtOjV|MUOwNVA>
K562/VCR M4jqPGN6fG:2b4jpZ:Kh[XO|YYm= M1;BRZ4yOCEQvF2= M37hNJNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= MYmyOVMyOzBzMB?=
CEM/VBL NETIeXZEgXSxdH;4bYPDqGG|c3H5 NWrEeHFChjFyIN88US=> NGXvO2J{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M1q0dVI2OzF|MEGw
U266 MV3DfZRwfG:6aXRCpIF{e2G7 NGDrPJR,OyEQvF5CpC=> MVLJR|UxRTFwMTFOwG0> M{nlT|I2QDFyMEGz
OPM-2 M{K2dmN6fG:2b4jpZ:Kh[XO|YYm= NH;3UG1,OyEQvF5CpC=> Mm[4TWM2OD1zLkig{txO NIfQcVAzPThzMECxNy=>
MM.1S NGjzTJJEgXSxdH;4bYPDqGG|c3H5 NFnC[I9,OyEQvF5CpC=> NHe2dWRKSzVyPUGuOkDPxE1? NXX2Nm01OjV6MUCwNVM>
MM.1R MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX:zJO69VcLi NFLxboJqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> MoK4NlU5OTByMUO=
RPMI-8226 MoD1R5l1d3SxeHnjxsBie3OjeR?= MYP+N{DPxE4EoB?= M{HZZmlEPTB;MD65JO69VQ>? NI\U[YEzPThzMECxNy=>
ANBL-6 NW\5Z3hoS3m2b4TvfIlkyqCjc4PhfS=> NYriZ2dmOSEQvF5CpC=> NH7CNZlqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NWrLd5BFOjV6MUCwNVM>
ANLB-6/V10R MmP3R5l1d3SxeHnjxsBie3OjeR?= NEjTPIEyKM7:TdMg M3fJUIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MmLNNlU5OTByMUO=
KAS-6/1 NWHxdJdsS3m2b4TvfIlkyqCjc4PhfS=> NVfRZVZtOSEQvF5CpC=> NYDFOpR7cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NI\KW2QzPThzMECxNy=>
KAS-6/V10R MlzrR5l1d3SxeHnjxsBie3OjeR?= MnTwNUDPxE4EoB?= M{\1Z4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MmnkNlU5OTByMUO=
KAS-6/R10R NYfLV|FwS3m2b4TvfIlkyqCjc4PhfS=> NUXhfZZNOSEQvF5CpC=> MULpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MX2yOVgyODBzMx?=
8226/S MofsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGLDNpI{KM7:TdMg MX3pcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= MWGyOVgyODBzMx?=
8226/LR-5 MnrXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWO3S|huOyEQvF5CpC=> MkT4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NYHyTYlsOjV6MUCwNVM>
Huh7 MnzJR5l1d3SxeHnjxsBie3OjeR?= M{fJZ541NjhizszNxsA> M{XxUGROW09? M362NGlEPTB;OT65JI5O MkPVNlYzPTl{NUC=
Hep3B MljhR5l1d3SxeHnjxsBie3OjeR?= MVf+OE45KM7:TdMg NEPtNXpFVVOR M3LsSGlEPTB;NES4Mlchdk1? NGTabGwzPjJ3OUK1NC=>
HepG2 NWfaS3hTS3m2b4TvfIlkyqCjc4PhfS=> MUP+OE45KM7:TdMg NGrBSHhFVVOR MW\JR|UxRTF|OT63O{BvVQ>? MlXRNlYzPTl{NUC=
Chang MUDDfZRwfG:6aXRCpIF{e2G7 NELOZ5Z,PC56IN88UeKh NUi1V2FETE2VTx?= NHmxWGdKSzVyPUS0PE44KG6P MmLxNlYzPTl{NUC=
Huh7 MXTGeY5kfGmxbjDhd5NigQ>? NVzJbHFWOS54IN88UeKh NUDpdZd3TE2VTx?= M3\EZ4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MUWyOlI2QTJ3MB?=
Hep3B MVXGeY5kfGmxbjDhd5NigQ>? NInX[nIyNjZizszNxsA> MYXEUXNQ MUjjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NUf5XWhXOjZ{NUmyOVA>
HepG2 NH7QPZBHfW6ldHnvckBie3OjeR?= M{n6cFEvPiEQvF5CpC=> NGjrU2JFVVOR NHS5T4Nk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MmLQNlYzPTl{NUC=
Chang MkG4SpVv[3Srb36gZZN{[Xl? NEi3NmUyNjZizszNxsA> M4rveWROW09? MmrZZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MlP5NlYzPTl{NUC=
MHCC97L M2nMfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2G1XZ4yOCEQvF2= MmXmSG1UVw>? NHXQZmtKSzVyPUOxOUBvVQ>? Mof6NlY1PTh7NUO=
MHCC97H NHqxdY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVy4bok3hjFyIN88US=> M{mzT2ROW09? MmHaTWM2OD1|NklihKkhdk1? MWOyOlQ2QDl3Mx?=
Huh7 M{PWNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2n3Np4yOCEQvF2= M3nafGROW09? NWLXdYNOUUN3ME2yOlUhdk1? Mn3NNlY1PTh7NUO=
HepG2 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGTR[W5,OTBizszN NH32S|NFVVOR NEHwWmlKSzVyPUO5NkBvVQ>? NGLwUZYzPjR3OEm1Ny=>
MHCC97L NVTKN4IxTnWwY4Tpc44h[XO|YYm= NYD4RnM6OSEQvF5CpC=> MUHEUXNQ NGKyUmtqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v M2n6SlI3PDV6OUWz
Huh7 MVrGeY5kfGmxbjDhd5NigQ>? Mmj6NUDPxE4EoB?= NFPwcYJFVVOR Ml63bY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NGiwbWMzPjR3OEm1Ny=>
MHCC97L M3fTe2Fxd3C2b4Ppd{Bie3OjeR?= M1HMSFEh|ryPwrC= M3O0fGROW09? NETiVlVqdmS3Y3XzJIFxd3C2b4Ppdy=> MmfWNlY1PTh7NUO=
Huh7 NXzhc|BMSXCxcITvd4l{KGG|c3H5 NFvicVkyKM7:TdMg M4TPPGROW09? NFrwRWtqdmS3Y3XzJIFxd3C2b4Ppdy=> MV6yOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts M{XTfGtqdmG|ZTDhd5NigQ>? NGf3R4QzPSEQvF2= MmjNSG1UVw>? NX\Me3NnemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? MmH1NlA2OzR|NEW=
H23 Ml;TS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEHFW4QzPSEQvF2= MnXMSG1UVw>? NVvaSJBye2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> M2e5PVIxPTN2M{S1
WM35 NXjaelc4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1TKSVExKM7:TR?= NYfyc5ZSTE2VTx?= MoPtd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MmrqNlA2OzR|NEW=
NIH 3T3 NYnydWMzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVHxN297OTBizszN NUXyT454TE2VTx?= MWjkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= Mm\2NlA2OzR|NEW=
H838 Mmm1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mof1NVAh|ryP MmPYSG1UVw>? MUPkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= M1W5OVIxPTN2M{S1
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Quiescent S2 M1TGTmtqdmG|ZTDhd5NigQ>? NH\x[Xo{OCEQvF2= MXHEUXNQ MWHjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? MWCyNVUyQDlzNR?=
PC3 NUjMe49nSXCxcITvd4l{KGG|c3H5 M4DvRVIxKM7:TR?= MY\EUXNQ M{TsNolv\HWlZYOgZZBweHSxc3nz MlPLNlE4ODlzM{C=
Du145 MWfBdI9xfG:|aYOgZZN{[Xl? NWnoN3hGOjBizszN MYTEUXNQ NX;vTYJucW6mdXPld{BieG:ydH;zbZM> NUTOe4VtOjF5MEmxN|A>
LNCaP MX\BdI9xfG:|aYOgZZN{[Xl? NXHUPHlsOjBizszN MUPEUXNQ MlvSbY5lfWOnczDhdI9xfG:|aYO= MVSyNVcxQTF|MB?=
LAPC-4 NYXRRpI5SXCxcITvd4l{KGG|c3H5 M4q2ZlIxKM7:TR?= NYHENVVmTE2VTx?= NV\SOW8zcW6mdXPld{BieG:ydH;zbZM> MmDXNlE4ODlzM{C=
LNCaP NX\NO5hLTnWwY4Tpc44h[XO|YYm= M1f2SFIxKM7:TR?= MnH1SG1UVw>? NHX2fpNl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| MlvjNlE4ODlzM{C=
LAPC-4 MXLGeY5kfGmxbjDhd5NigQ>? MYWyNEDPxE1? M3v6fmROW09? NEPQPZJl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| M2e3XFIyPzB7MUOw
Kasumi-1 MnfpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUL+OVAh|ryP M2OzOmROW09? MmPDbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MorHNlM{QTB3M{[=
SKNO-1 M{jsOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlrKglUxKM7:TR?= M1i3TmROW09? Ml\GbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NGXMXngzOzN7MEWzOi=>
Kasumi-1 MXzLbY5ie2ViYYPzZZk> NIe5S3J,OTBizszN MYjEUXNQ NUn3Omd1emWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z MmXTNlM{QTB3M{[=
SKNO-1 MmHTT4lv[XOnIHHzd4F6 NWnNWWFVhjFyIN88US=> M2PGe2ROW09? M2rjO5Jm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> NGe4[4EzOzN7MEWzOi=>
A549 MUDGeY5kfGmxbjDhd5NigQ>? M17Xe|ExKM7:TR?= NFvKW41FVVOR MX7lcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl MkS1NlQ4PDZ3N{S=
NRK-52E M{TlZ2Z2dmO2aX;uJIF{e2G7 NUPXWoxMOTBizszN Ml;3SG1UVw>? MX7pcohq[mm2czDBcochUUlvaX7keYNm\CCVVFHUN{BvfWOuZXHyJJRz[W6|bH;jZZRqd25iYX7kJJRp\SCneIDy[ZN{cW:wIH;mJHRITi4QskGsJINwdGyjZ3XuJGlXKGGwZDDmbYJzd26nY4Tpci=> MkD6NlUxQDhyMEK=
PC12 M3zvd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUDNVlB4hjF{LkWg{txO NEDNZ41FVVOR MkfGdJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> NV;LN4JFOjVzMkizPFY>
HPMCs NETDOJBHfW6ldHnvckBie3OjeR?= MUny[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> MmjTNlYxPDV5OEC=
A549 NYjxVGVUTnWwY4Tpc44h[XO|YYm= MnzGglUxKM7:TR?= M3LU[WROW09? Mn3DZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> NWDwT5ZHOjZ5MUG3OFg>
RAW264.7 M3O1ZmZ2dmO2aX;uJIF{e2G7 NH3VcnN,OzBizszN Mm\KSG1UVw>? MkTGdoVlfWOnczDwdo8ucW6obHHtcYF1d3K7IHflcoUh\XiycnXzd4lwdg>? MmTiNlY4OTh3OE[=
MEMM M2TlTWtqdmG|ZTDhd5NigQ>? M3rpSFE2KML3TR?= M3HTXmROW09? Mn\m[IVkemWjc3XzJIFk\XS7bHH0bY9vKG:oIHjpd5RwdmViSEO= M2r4OlI3QTJzNUC2
MEMM M{\SNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NID5PXJ,OjBiwsXN M4fkbmROW09? MX7pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M37XSVI3QTJzNUC2
MEMM Ml[zRZBweHSxc3nzJIF{e2G7 NUjzS3FYOTViwsXN NFHlU|RFVVOR Mo\0bY5lfWOnczD0bIUheHKnc3XuZ4Uhd2ZidHjlJIFxd3C2b4Ppd{Bxem:2ZXnuMEBkdGWjdnXkJGNie3Cjc3WtNy=> NIfQSFAzPjl{MUWwOi=>
T47D NHPaWFJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXexNEDPxE1? MnW0SG1UVw>? MVrJR|UxRTd{IH7N Ml;zNVg{QDF2NES=
ZR-75-1 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWm3fGlwOTBizszN MUTEUXNQ M2fkRWlEPTB;N{mgcm0> MmHJNVg{QDF2NES=
BT474 Mn;jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXrzdIVVOTBizszN MoXLSG1UVw>? M3\DO2lEPTB;OE[gcm0> NGTPOYYyQDN6MUS0OC=>
HCC1954 NX3oRXJLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojSNVAh|ryP M1vMZ2ROW09? M{Xr[WlEPTB;MUG5JI5O NXL0bnVWOTh|OEG0OFQ>
MDA-MB-453 NHzlUpVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoTtNVAh|ryP M4Kw[GROW09? MWLJR|UxRTl5NTDuUS=> Ml\UNVg{QDF2NES=
MDA-MB-468 NYXqRVJNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mmm0NVAh|ryP M3n3WWROW09? NGL6PFRKSzVyPUOyNFghdk1? M1rtdVE5OzhzNES0
SkBr3 MkPvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEPXcmUyOCEQvF2= Mn;4SG1UVw>? NHvpVoFKSzVyPkGwMFAxOCCwTR?= MYexPFM5OTR2NB?=
MDA-MB-231 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mle4NVAh|ryP M2\KR2ROW09? MnW3TWM2OD5zMDywNFAhdk1? M2O4V|E5OzhzNES0
HCT116 MoHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGXzdIQyOCEQvF2= M4fOfmROW09? NVmzXXRHUUN3ME21PFM3KG6P M4DsbFE5OzhzNES0
HT29 M{TkeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2nsWFExKM7:TR?= MnfISG1UVw>? MXzJR|UxRjFyLECwNEBvVQ>? MnLpNVg{QDF2NES=
HFF NUWxO4JCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3;2WVExKM7:TR?= NH;sUlRFVVOR MXPJR|UxRTd4MUWgcm0> MlS1NVg{QDF2NES=
HN5 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHKyTJYyOCEQvF2= MoDhSG1UVw>? MVvJR|UxRjFyLECwNEBvVQ>? MYKxPFM5OTR2NB?=
786-0 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M37KXFExKM7:TR?= M1jmd2ROW09? MWTJR|UxRTRyMEmgcm0> MkTPNVg{QDF2NES=
H157 NH3qUYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoqzNVAh|ryP MmHoSG1UVw>? NGnnNZdKSzVyPUK2OFIhdk1? NI\1OFcyQDN6MUS0OC=>
NCI-H460 MkT6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUXoUJZ4OTBizszN NH\HbYdFVVOR MoO3TWM2OD5{LEWwNEBvVQ>? M{H0NFE5OzhzNES0
SKOV-3 M3HjZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4jGOVExKM7:TR?= MYnEUXNQ NXy5NG5TUUN3ME2yNVI3KG6P Mmq2NVg{QDF2NES=
OVCAR-3 NG\rRW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX62W4VDOTBizszN NWfNUYNzTE2VTx?= NF6ybXVKSzVyPUK5NVghdk1? Mn\5NVg{QDF2NES=
BXPC3 NGnEVmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWOxNEDPxE1? MULEUXNQ NIH5bW5KSzVyPUOxOFEhdk1? NYr6Z3FYOTh|OEG0OFQ>
MiaPaCa NVvBc5lnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NE\KWYMyOCEQvF2= M4HTZmROW09? M1XaZWlEPTB;NUSzN{BvVQ>? M2[2bVE5OzhzNES0
PANC-1 NVfEU4RuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlHRNVAh|ryP MkjUSG1UVw>? NIric3JKSzVyPUi2PFEhdk1? MmGxNVg{QDF2NES=
LNCaP MoTJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NI\MOJcyOCEQvF2= MW\EUXNQ MlHJTWM2OD1zNEegcm0> MkHRNVg{QDF2NES=
DU145 NITCeolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2jVTFExKM7:TR?= MUHEUXNQ MnP4TWM2OD1|OEGyJI5O NVvxS5ZIOTh|OEG0OFQ>
PC3 M{\XXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mnz3NVAh|ryP NXG2cXMzTE2VTx?= Mn3GTWM2OD5zMDywNFAhdk1? NYHW[3VbOTh|OEG0OFQ>
BT474 MlnPT4lv[XOnIHHzd4F6 MmTkNVAh|ryP NGHvTYNFVVOR NIL2SJNqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNkCgcm0> NXzTe3B{OTh|OEG0OFQ>
786-0 NVj0bXlmU2mwYYPlJIF{e2G7 NELiVZUyOCEQvF2= MWTEUXNQ NIDzZ3dqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNUCgcm0> Ml;0NVg{QDF2NES=
LNCaP MXzLbY5ie2ViYYPzZZk> MV2xNEDPxE1? NVG2bnF4TE2VTx?= NFzWTlZqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2MzDuUS=> M2jMblE5OzhzNES0
PC3 NYjP[2dmU2mwYYPlJIF{e2G7 NYHrOnB4OTBizszN NXrGRmZ3TE2VTx?= MnS2bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDlibl2= NW\tUYdYOTh|OEG0OFQ>
KARPAS-231 NIrudYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkjMNVAh|ryP NWDie4pJTE2VTx?= MU\FR|UxRTRzIH7N NV3iTGtGOTlyNkS3N|A>
CCRFSB NYOxNYpZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWLyVoZSOTBizszN M3\LZWROW09? NFnuS2dGSzVyPUG1OUBvVQ>? MUOxPVA3PDd|MB?=
SUP B15 Ml;hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX[xNEDPxE1? M2PONWROW09? MlTPSWM2OD1zOUegcm0> Mlm0NVkxPjR5M{C=
SD-1 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVSxNEDPxE1? M{PWfWROW09? MV;FR|UxRTN{MDDuUS=> MUSxPVA3PDd|MB?=
RS4;11 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3rNTFExKM7:TR?= NHnsUoFFVVOR MYnFR|UxRTZ3NDDuUS=> MUmxPVA3PDd|MB?=
MN-60 M3PTSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2C1SlExKM7:TR?= MkLHSG1UVw>? NHvlfIZGSzVyPUO2NFIhdk1? NYPUTYdDOTlyNkS3N|A>
Tanoue MlS4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{CzblExKM7:TR?= NXjPWFB3TE2VTx?= MYfFR|UxRTR3MUegcm0> MXqxPVA3PDd|MB?=
RCH-ACV NXnqNJUzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGDB[2UyOCEQvF2= MUfEUXNQ NEHnb5JGSzVyPUG1NkBvVQ>? NXjkTXU2OTlyNkS3N|A>
SEM NV7QPFd4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zPXFExKM7:TR?= NFzUWHZFVVOR NF\lNolGSzVyPUKwNkBvVQ>? MXOxPVA3PDd|MB?=
KASUMI-2 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXWxNEDPxE1? MlnPSG1UVw>? MU\FR|UxRTJ{NTDuUS=> MXuxPVA3PDd|MB?=
REH MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn3oNVAh|ryP NWrwbmZ7TE2VTx?= NYqwWmJ7TUN3ME2yPFghdk1? M2DPVVE6ODZ2N{Ow
697 NX\xcVdtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkXrNVAh|ryP MYXEUXNQ M3v6TmVEPTB;M{O4JI5O MnzZNVkxPjR5M{C=
NALM-6 NYHVVIFpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M37KdFExKM7:TR?= Ml:xSG1UVw>? M4f1NWVEPTB;NEKxJI5O NXS1O5V{OTlyNkS3N|A>
MHH-CALL–3 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXTNVAh|ryP NFn1UIpFVVOR Ml[0SWM2OD16MUKgcm0> MkT3NVkxPjR5M{C=
MHH-CALL–2 M{\ucWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkDaNVAh|ryP NH\0TXdFVVOR NXz0THc5TUN3ME2yNVE1KG6P M2LUblE6ODZ2N{Ow
J.GAMMA-1 MoTJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUCxNEDPxE1? NW\ESpk2TE2VTx?= MYnFR|UxRTZ3IH7N Mo\sNVkxPjR5M{C=
JR45.01 NITRdYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXyxNEDPxE1? M{TmPGROW09? M4TTU2VEPTB;Nkigcm0> NYL3bGI5OTlyNkS3N|A>
A3 MoPXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEDqO20yOCEQvF2= NHjDXY9FVVOR NX71U|c1TUN3ME22PUBvVQ>? NEHvXXUyQTB4NEezNC=>
I 2.1 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVqxNEDPxE1? Ml62SG1UVw>? NHW4Z3RGSzVyPUezJI5O M2jLdVE6ODZ2N{Ow
MOLT-3 NWnCXFh6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFHhdYoyOCEQvF2= MnznSG1UVw>? MkLlSWM2OD15NDDuUS=> Mn7VNVkxPjR5M{C=
P116 Mn2yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4LmNlExKM7:TR?= NGXEbYpFVVOR NFPMbIFGSzVyPUe4JI5O MW[xPVA3PDd|MB?=
J.Cam1.6 M1fEdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUD5c2h5OTBizszN NVPwV3A1TE2VTx?= MmO4SWM2OD15OTDuUS=> NVXvd29{OTlyNkS3N|A>
I 9.2 M3WzbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIPoSGcyOCEQvF2= MXLEUXNQ MVjFR|UxRThyIH7N MVqxPVA3PDd|MB?=
LOUCY M1X4S2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NULvdoV7OTBizszN MYPEUXNQ MVvFR|UxRTFzNzDuUS=> NFqwVGIyQTB4NEezNC=>
J.RT3-T3.5 NVTtUZJQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWOxNEDPxE1? MWDEUXNQ MUHFR|UxRTF{MzDuUS=> MYCxPVA3PDd|MB?=
800000 NV\CSoRJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HYNlExKM7:TR?= MXzEUXNQ M1rGc2VEPTB;MU[zJI5O Mm\UNVkxPjR5M{C=
Jurkat MmPCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1XZe|ExKM7:TR?= M4\FRWROW09? NHy0dGZGSzVyPUKyOUBvVQ>? MnjlNVkxPjR5M{C=
MOLT-4 MlfBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUOxNEDPxE1? NGrSXoFFVVOR M1\oTGVEPTB;MkOyJI5O NE\peHkyQTB4NEezNC=>
Molt-16 M{nKXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmDrNVAh|ryP NF3OOJNFVVOR MnfwSWM2OD1{NEGgcm0> NVzF[FEyOTlyNkS3N|A>
CEM/C3 M2PJdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHn2VmUyOCEQvF2= M1XhWWROW09? NXe2fJRkTUN3ME2yOVchdk1? MUCxPVA3PDd|MB?=
CEM/C2 MoHTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWjXeFdlOTBizszN NFHGcWxFVVOR M1rYcWVEPTB;MkexJI5O MnvFNVkxPjR5M{C=
CCRFCEM NIDlRXhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUmxNEDPxE1? NHrMbnBFVVOR NEG5U|JGSzVyPUOyO{BvVQ>? NUPiblNCOTlyNkS3N|A>
CEM/C1 NFjQWJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWWxNEDPxE1? M{\QeGROW09? M1PUT2VEPTB;M{iyJI5O NEnFcVYyQTB4NEezNC=>
SUPTI[VB] MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFjQTIwyOCEQvF2= NX7CSnpUTE2VTx?= M2X1XGVEPTB;NkG5JI5O M4nQW|E6ODZ2N{Ow
CCRF–HSB-2 NV\scYV3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWr5co9[OTBizszN M2[1cGROW09? NVT1UYxITUN3ME2yNVE4KG6P NFrudnEyQTB4NEezNC=>
I 2.1 MnP5RZBweHSxc3nzJIF{e2G7 MluwNVAh|ryP MYjEUXNQ M3fTNIlv\HWlZYOgZZBweHSxc3nz NYTYSZdpOTlyNkS3N|A>
I 9.2 NWDyOZBmSXCxcITvd4l{KGG|c3H5 M1iwflExKM7:TR?= M4GyS2ROW09? NWDS[W1bcW6mdXPld{BieG:ydH;zbZM> NIrRZosyQTB4NEezNC=>
A3 MVTBdI9xfG:|aYOgZZN{[Xl? NVXSS3VHOTBizszN MY\EUXNQ M1m1eYlv\HWlZYOgZZBweHSxc3nz MUmxPVA3PDd|MB?=
RD MoDRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4D4cVExKM7:TR?= MWDJR|UxRjFyIN88US=> MmPONlA4PDB4MkO=
Rh41 M1u3OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWjTR|F[OTBizszN NXf3b5huUUN3ME2zN{45KG6P M3;oOlIxPzRyNkKz
Rh18 M{[0WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnfBNVAh|ryP MV3JR|UxRTNyMzDuUS=> NU[5O4l3OjB5NEC2NlM>
Rh30 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1TldFExKM7:TR?= NWrhfpFoUUN3ME20MlgyKM7:TR?= NYTscnBkOjB5NEC2NlM>
BT-12 NFH6WYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVrhUZl2OTBizszN M4L5SmlEPTB-MUCg{txO NEK2[mgzODd2ME[yNy=>
CHLA-266 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NW\JZnhNOTBizszN NYK4VnF6UUN3ME2xMlIzKM7:TR?= MWCyNFc1ODZ{Mx?=
TC-71 NWDzXZB3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;vZlgyOCEQvF2= MmrHTWM2OD1{LkWyJO69VQ>? MWOyNFc1ODZ{Mx?=
CHLA-9 NXSze4dqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkLrNVAh|ryP M1XhV2lEPTB;NUmxJI5O NUnZO4twOjB5NEC2NlM>
CHLA-10 NEK3XoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXSxNEDPxE1? MnTMTWM2OD1zMEKgcm0> NYTzU4lEOjB5NEC2NlM>
CHLA-258 MnLHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7oZ4lNOTBizszN MkHqTWM2OD1zLkC1JO69VQ>? NHPuRXIzODd2ME[yNy=>
GBM2 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUC5NXhYOTBizszN NVLRVnVRUUN3ME25MlE2KM7:TR?= NYntNZRnOjB5NEC2NlM>
NB-1643 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4jIUlExKM7:TR?= MofWTWM2OD13LkSg{txO NXvxcppDOjB5NEC2NlM>
NB-Ebc1 NEHpVYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGLX[XoyOCEQvF2= MknzTWM2OD5zMDFOwG0> NVnDfoxQOjB5NEC2NlM>
CHLA-90 Mln2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{jkR|ExKM7:TR?= MYfJR|UxRjFyIN88US=> Mn76NlA4PDB4MkO=
CHLA-136 Mle0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NE\IZ|UyOCEQvF2= MYDJR|UxRjFyIN88US=> NXPCdnd5OjB5NEC2NlM>
NALM-6 NILIRlZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXWxNEDPxE1? MXLJR|UxRTJ4NTDuUS=> NX;C[|BYOjB5NEC2NlM>
COG-LL-317 NX3WXFU{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NITGd4MyOCEQvF2= MV;JR|UxRTZwNEmgcm0> NFfkdXMzODd2ME[yNy=>
RS4;11 M37qe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrxNVAh|ryP NGjOR3FKSzVyPUG0O{BvVQ>? NXHlVo5DOjB5NEC2NlM>
MOLT-4 MnLzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX:xNEDPxE1? MXzJR|UxRTRyIH7N MXmyNFc1ODZ{Mx?=
CCRF-CEM M1T5dWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NILsd3MyOCEQvF2= M{HwRmlEPTB;Mk[4JI5O MViyNFc1ODZ{Mx?=
Kasumi-1 M4H0Xmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYOwZYp[OTBizszN MnizTWM2OD1zMEegcm0> NUD2WmhiOjB5NEC2NlM>
Karpas-299 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MorJNVAh|ryP M2LjXGlEPTB;Mj65N{DPxE1? NGi1OZAzODd2ME[yNy=>
Ramos-RA1 NUDsenZCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4\BZVExKM7:TR?= NWm5fFBRUUN3ME23MlM2KM7:TR?= Ml;PNlA4PDB4MkO=
H1299 NHTBd2JMcW6jc3WgZZN{[Xl? MkDSNVAh|ryP M3ji[olvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> NFvW[2EzOTlyOE[xOi=>

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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
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
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3
NCT01892527 Unknown status 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
NCT01861301 Terminated Epithelioid Mesothelioma|Recurrent Malignant Mesothelioma|Sarcomatoid Mesothelioma|Stage II Pleural Mesothelioma|Stage III Pleural Mesothelioma|Stage IV Pleural Mesothelioma National Cancer Institute (NCI) January 2013 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

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID