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. 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 MX\LbY5ie2ViYYPzZZk> MU\+NVAh|ryP NV7NW3U5cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NFHLXJIzODR6NECxPC=>
HT29 MmqxT4lv[XOnIHHzd4F6 NX;hOoZjhjFyIN88US=> MYjpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MWWyNFQ5PDBzOB?=
MDA-MB-231 M4DRbmtqdmG|ZTDhd5NigQ>? NV;k[GpJhjFyIN88US=> NEfnXIpqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NW\NRpB4OjB2OESwNVg>
NCI-H441 MnW5T4lv[XOnIHHzd4F6 NGK2V4d,OTBizszN NHj3V|BqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MUeyNFQ5PDBzOB?=
SK-MEL-28 M4XUSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFPLdXo{OyEQvF2= MYXJR|UxRjN|IN88US=> M1HLVVIxPDh2MEG4
NCI-H661 Mn7JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVzhWZJpOzNizszN MU\JR|UxRjN|IN88US=> MVmyNFQ5PDBzOB?=
NCI-H446 NVLxNJhmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoK2N|Mh|ryP MofjTWM2OD15IN88US=> MWWyNFQ5PDBzOB?=
MDA-MB-231 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGTIfVc{OyEQvF2= NUPwbJBYUUN3ME2wMlU2KM7:TR?= MVqyNFQ5PDBzOB?=
DLD-1 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWWzN{DPxE1? NXLKWo8xUUN3ME2wMlU{KM7:TR?= NW\aTXlnOjB2OESwNVg>
A549 NHy0blRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1LWVVM{KM7:TR?= MV\JR|UxRTBwNUmg{txO MVGyNFQ5PDBzOB?=
SK-OV-3 NEXkcHpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFuxWmE{OyEQvF2= MUjJR|UxRTBwNk[g{txO MljwNlA1QDRyMUi=
NCI-H460 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH\t[WY{OyEQvF2= M3m5cWlEPTB;MD62JO69VQ>? NVXLeZFtOjB2OESwNVg>
A375 M1nTe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWH1R3lyOzNizszN MVfJR|UxRTBwNEKg{txO MVGyNFQ5PDBzOB?=
NCI-H441 NUfJZoZjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEn3NG4{OyEQvF2= MXHJR|UxRTBwMzFOwG0> MUGyNFQ5PDBzOB?=
HT29 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXhN|Mh|ryP NHfxUVRKSzVyPUCuOFkh|ryP NUHLe3I6OjB2OESwNVg>
MKN-45 Mo\zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVThcZNyOzNizszN MVHJR|UxRTBwNUig{txO M4HOV|IxPDh2MEG4
HT29 NI\OfJRCeG:ydH;zbZMh[XO|YYm= M3\nO54yOCEQvF2= NFfyTI5{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= M4TrNFIxPDh2MEG4
MKN-45 M4jRfmFxd3C2b4Ppd{Bie3OjeR?= MXn+NVAh|ryP MnPld4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NIHrelIzODR6NECxPC=>
MDA-MB-231 NE\UbWJCeG:ydH;zbZMh[XO|YYm= Ml65glExKM7:TR?= MlrVcY9l\XO2bImgbY5lfWOnczDhdI9xfG:|aYOgZpkhOzVnLh?= MYWyNFQ5PDBzOB?=
MDA-MB-231/TGL NGP4Z2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M33ETZ4yODBizszN NVHxeYFMT0l3ME2xMlIh|ryP MYGyNlAzPzZ7MB?=
1833/TGL MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXSx[VNRhjFyMDFOwG0> MljlS2k2OD1|Lkeg{txO NUn3RnE6OjJyMke2PVA>
EBC1 MVPDfZRwfG:6aXRCpIF{e2G7 NWnQR2Q{hjFyIN88US=> M2TqUolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= MUWyN|U6QDJ5Nh?=
SNU638 MkDPR5l1d3SxeHnjxsBie3OjeR?= MUH+NVAh|ryP M2jYZYlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= MnrHNlM2QTh{N{[=
A549 MoDnR5l1d3SxeHnjxsBie3OjeR?= NHLOPHZ,OTBizszN M{D6OY5wfCCjZn\lZ5Q> MVKyN|U6QDJ5Nh?=
H460 MXXDfZRwfG:6aXRCpIF{e2G7 NUPmfnBLhjFyIN88US=> MUnuc5Qh[W[oZXP0 NFvWNJAzOzV7OEK3Oi=>
HCC827 NELxS4dEgXSxdH;4bYPDqGG|c3H5 M2P2VZ4yOCEQvF2= MWjuc5Qh[W[oZXP0 M2XXflI{PTl6Mke2
A549 NXLqdlQ{TnWwY4Tpc44h[XO|YYm= M{HS[|ExKM7:TR?= MU\kbZNzfXC2czDtbYNzd3S3YoXs[S=> M1zXS|I{PTl6Mke2
EBC1 M3rzcmZ2dmO2aX;uJIF{e2G7 NWT0[ZlZOTBizszN M4PSdIRqe3K3cITzJI1q[3KxdIXieYxm MmDWNlM2QTh{N{[=
H460 MV7GeY5kfGmxbjDhd5NigQ>? MlHMNVAh|ryP MX;pcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v NFz3OHUzPTNzM{CxNC=>
K562/VCR NUjxeoxrS3m2b4TvfIlkyqCjc4PhfS=> MUP+NVAh|ryP NEWw[It{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= NX\RSYxWOjV|MUOwNVA>
CEM/VBL MYLDfZRwfG:6aXRCpIF{e2G7 MoTtglExKM7:TR?= MYTzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MX2yOVMyOzBzMB?=
U266 NFTJPGVEgXSxdH;4bYPDqGG|c3H5 M2XFS54{KM7:TdMg M3j4XmlEPTB;MT6xJO69VQ>? NETvXo0zPThzMECxNy=>
OPM-2 NVXRb3huS3m2b4TvfIlkyqCjc4PhfS=> NGP1[JB,OyEQvF5CpC=> MlnKTWM2OD1zLkig{txO MXKyOVgyODBzMx?=
MM.1S NV;6OXpyS3m2b4TvfIlkyqCjc4PhfS=> M2TGXJ4{KM7:TdMg NFrQWWNKSzVyPUGuOkDPxE1? NF3ncHgzPThzMECxNy=>
MM.1R MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mk\nN{DPxE4EoB?= MVnpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= M4roSFI2QDFyMEGz
RPMI-8226 MnLiR5l1d3SxeHnjxsBie3OjeR?= MmfnglMh|ryPwrC= NFLuRpNKSzVyPUCuPUDPxE1? NGGzbmwzPThzMECxNy=>
ANBL-6 NUOwTGlGS3m2b4TvfIlkyqCjc4PhfS=> MXexJO69VcLi NEnMboFqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MlezNlU5OTByMUO=
ANLB-6/V10R M3nxeWN6fG:2b4jpZ:Kh[XO|YYm= NFLHbHkyKM7:TdMg NHfiPYlqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MnG0NlU5OTByMUO=
KAS-6/1 MVXDfZRwfG:6aXRCpIF{e2G7 M2PH[FEh|ryPwrC= NYG5em9RcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NYT4NnNTOjV6MUCwNVM>
KAS-6/V10R NVvveWV7S3m2b4TvfIlkyqCjc4PhfS=> MmDCNUDPxE4EoB?= NH3qcHZqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NH\IWGszPThzMECxNy=>
KAS-6/R10R NFewRYZEgXSxdH;4bYPDqGG|c3H5 NWXrU4pCOSEQvF5CpC=> MlTRbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MmrtNlU5OTByMUO=
8226/S NVLJS5ZkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmmzN{DPxE4EoB?= M{LmN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MmD5NlU5OTByMUO=
8226/LR-5 NHvnRnZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4PJN|Mh|ryPwrC= MlHJbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl MknSNlU5OTByMUO=
Huh7 NXPsXZB[S3m2b4TvfIlkyqCjc4PhfS=> MVP+OE45KM7:TdMg MofYSG1UVw>? NHLVZYFKSzVyPUmuPUBvVQ>? M1vpVVI3OjV7MkWw
Hep3B NEDyUllEgXSxdH;4bYPDqGG|c3H5 NIjEVYF,PC56IN88UeKh MVfEUXNQ M4DxPWlEPTB;NES4Mlchdk1? MUGyOlI2QTJ3MB?=
HepG2 MWnDfZRwfG:6aXRCpIF{e2G7 MWX+OE45KM7:TdMg M1fFN2ROW09? NX\vc4VCUUN3ME2xN|kvPzdibl2= NV;BcYFROjZ{NUmyOVA>
Chang NYXhS|M4S3m2b4TvfIlkyqCjc4PhfS=> NYf6Sm5KhjRwODFOwG3DqA>? NXH6c3lmTE2VTx?= MnzJTWM2OD12NEiuO{BvVQ>? MYeyOlI2QTJ3MB?=
Huh7 NFLCUmZHfW6ldHnvckBie3OjeR?= M3;FSlEvPiEQvF5CpC=> NF7OTIpFVVOR NHTPU|Jk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NU\jNoJLOjZ{NUmyOVA>
Hep3B M13IOWZ2dmO2aX;uJIF{e2G7 M1fudVEvPiEQvF5CpC=> M3HlXWROW09? M13wbYNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? Ml3oNlYzPTl{NUC=
HepG2 MlnaSpVv[3Srb36gZZN{[Xl? M3zoW|EvPiEQvF5CpC=> MoOzSG1UVw>? MXTjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M3W1dlI3OjV7MkWw
Chang Mom0SpVv[3Srb36gZZN{[Xl? NF3r[3EyNjZizszNxsA> NEXze3BFVVOR MoC2Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MoXnNlYzPTl{NUC=
MHCC97L NX3mT3p5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWLjNFFqhjFyIN88US=> NETNXZhFVVOR NWHteJpOUUN3ME2zNVUhdk1? MVyyOlQ2QDl3Mx?=
MHCC97H NHTXUmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnwdWxShjFyIN88US=> M164S2ROW09? MYTJR|UxRTN4OPMAjUBvVQ>? Mo\SNlY1PTh7NUO=
Huh7 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIPEcml,OTBizszN M1:zT2ROW09? NEnXeodKSzVyPUK2OUBvVQ>? NWPhUVJnOjZ2NUi5OVM>
HepG2 NIXnWYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MljIglExKM7:TR?= NYXZ[oJ6TE2VTx?= MkLITWM2OD1|OUKgcm0> NFTnelczPjR3OEm1Ny=>
MHCC97L NHzsU3VHfW6ldHnvckBie3OjeR?= NXn3[IpQOSEQvF5CpC=> NV7iZ4p[TE2VTx?= M3rWUYlv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NFXjT2UzPjR3OEm1Ny=>
Huh7 NXO0O|hMTnWwY4Tpc44h[XO|YYm= M2LqeVEh|ryPwrC= MVTEUXNQ MXLpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u MkXINlY1PTh7NUO=
MHCC97L NVO4Z2tvSXCxcITvd4l{KGG|c3H5 M4X0d|Eh|ryPwrC= MWDEUXNQ NFSyN5pqdmS3Y3XzJIFxd3C2b4Ppdy=> NWHsXplJOjZ2NUi5OVM>
Huh7 MULBdI9xfG:|aYOgZZN{[Xl? MoP5NUDPxE4EoB?= M4jC[GROW09? M33BXolv\HWlZYOgZZBweHSxc3nz NIq4SYwzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts M{HH[mtqdmG|ZTDhd5NigQ>? M1\hOFI2KM7:TR?= M33qemROW09? NX;nbJBYemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? NY\6RXB6OjB3M{SzOFU>
H23 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUjleoJMOjVizszN M3nBW2ROW09? MVPzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NFrmZ2QzODV|NEO0OS=>
WM35 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVuxNEDPxE1? MkjZSG1UVw>? NInrfIV{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M3XOZVIxPTN2M{S1
NIH 3T3 NVHiclBmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlfVNVAh|ryP Mnr5SG1UVw>? MlnJ[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MonyNlA2OzR|NEW=
H838 NG\KdIpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmLINVAh|ryP NGnDbWlFVVOR MmfK[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 Mlz1NlA2OzR|NEW=
H1395 NYLzU2ZLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUKxNEDPxE1? NVjU[3lxTE2VTx?= NV\lNWhY\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NIn4c4QzODV|NEO0OS=>
Quiescent S2 NFrHRZFMcW6jc3WgZZN{[Xl? NUPKbZhXOzBizszN NGrLU3ZFVVOR NInneWpkd22ybHX0[Yx6KGGkcn;nZZRmeyCWU1GtbY5lfWOnZDDofZBmemGlZYT5cIF1cW:wIH;mJGg{UzSvZUOgbIl{fG:wZYO= M17GNFIyPTF6OUG1
PC3 MYjBdI9xfG:|aYOgZZN{[Xl? NWToZpRpOjBizszN M4TkSmROW09? MXnpcoR2[2W|IHHwc5B1d3Orcx?= MUiyNVcxQTF|MB?=
Du145 NEn6XXlCeG:ydH;zbZMh[XO|YYm= NFrLWIgzOCEQvF2= MoXiSG1UVw>? MWLpcoR2[2W|IHHwc5B1d3Orcx?= NFzxfokzOTdyOUGzNC=>
LNCaP M4f4TGFxd3C2b4Ppd{Bie3OjeR?= MlztNlAh|ryP NF;6XmhFVVOR Mn;XbY5lfWOnczDhdI9xfG:|aYO= NYrrUYZXOjF5MEmxN|A>
LAPC-4 MlLiRZBweHSxc3nzJIF{e2G7 NFX1PI8zOCEQvF2= MXPEUXNQ M3W0folv\HWlZYOgZZBweHSxc3nz NYHkNJFwOjF5MEmxN|A>
LNCaP M1faeGZ2dmO2aX;uJIF{e2G7 M{XJ[|IxKM7:TR?= MWrEUXNQ NW[4XXBN\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= NX\yc5V6OjF5MEmxN|A>
LAPC-4 NV\MW2FOTnWwY4Tpc44h[XO|YYm= NGKwS|czOCEQvF2= M2Xp[WROW09? NYXaPFI1\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= NWW5TXc4OjF5MEmxN|A>
Kasumi-1 M3HGZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkPXglUxKM7:TR?= MnLvSG1UVw>? NU\vXlNwcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MmHMNlM{QTB3M{[=
SKNO-1 NVrv[IVQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3S3ZZ42OCEQvF2= MonWSG1UVw>? M13x[IlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M2j5NlI{OzlyNUO2
Kasumi-1 NUnodIxvU2mwYYPlJIF{e2G7 MX\+NVAh|ryP MnfHSG1UVw>? MnTTdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NEXR[WMzOzN7MEWzOi=>
SKNO-1 M1\qW2tqdmG|ZTDhd5NigQ>? NXTKb2d[hjFyIN88US=> Ml7WSG1UVw>? M1PuTJJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> MYmyN|M6ODV|Nh?=
A549 M1;ycGZ2dmO2aX;uJIF{e2G7 M3nvSlExKM7:TR?= NWPO[2xjTE2VTx?= NUf1OHZ[\W6qYX7j[ZMhdWm2b4TpZ{Bk[XSjc4Tyc5Bp\Q>? NFn2TlMzPDd2NkW3OC=>
NRK-52E M{LQU2Z2dmO2aX;uJIF{e2G7 M1q0eFExKM7:TR?= MnvySG1UVw>? MUPpcohq[mm2czDBcochUUlvaX7keYNm\CCVVFHUN{BvfWOuZXHyJJRz[W6|bH;jZZRqd25iYX7kJJRp\SCneIDy[ZN{cW:wIH;mJHRITi4QskGsJINwdGyjZ3XuJGlXKGGwZDDmbYJzd26nY4Tpci=> MljINlUxQDhyMEK=
PC12 MnX0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkjaglEzNjVizszN NEDpPJpFVVOR M2DDXpBz\X[nboTzJHRUSS2rbnT1Z4VlKG6ndYLpeIUh\m:{bXH0bY9v MkGzNlUyOjh|OE[=
HPMCs NEL2OoRHfW6ldHnvckBie3OjeR?= M3zCO5JmfmW{c3XzJIVxcXSqZXzpZYwhfG9ibXXz[Y5kcHmvYXygeJJidnOrdHnvckBw\iCqdX3hckBx\XKrdH;u[YFtKG2nc3;0bIVtcWGuIHPlcIx{ MmDlNlYxPDV5OEC=
A549 MWjGeY5kfGmxbjDhd5NigQ>? MV7+OVAh|ryP MkfiSG1UVw>? Ml;MZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> NYjScJA4OjZ5MUG3OFg>
RAW264.7 NV\TOVdzTnWwY4Tpc44h[XO|YYm= NUnTOGFkhjNyIN88US=> MmPCSG1UVw>? Mly4doVlfWOnczDwdo8ucW6obHHtcYF1d3K7IHflcoUh\XiycnXzd4lwdg>? M{XN[VI3PzF6NUi2
MEMM NVfFSlAyU2mwYYPlJIF{e2G7 MmPpNVUhyrWP NUDQe2I{TE2VTx?= M3P6fIRm[3KnYYPld{Bi[2W2eXzheIlwdiCxZjDobZN1d26nIFiz M1HWXFI3QTJzNUC2
MEMM NWTVV5NNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoD1glIxKML3TR?= NF3BfYJFVVOR NUfpb4tCcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MoPSNlY6OjF3ME[=
MEMM M4\0e2Fxd3C2b4Ppd{Bie3OjeR?= NH7sN44yPSEEtV2= Ml3rSG1UVw>? NXfzN4JWcW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? MmHHNlY6OjF3ME[=
T47D MmLIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnL4NVAh|ryP MlK5SG1UVw>? NGfVSHpKSzVyPUeyJI5O MXOxPFM5OTR2NB?=
ZR-75-1 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnKzNVAh|ryP NFXGN5pFVVOR MkD1TWM2OD15OTDuUS=> MoPNNVg{QDF2NES=
BT474 NXHJbIZnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV3UfXJkOTBizszN M{jmeGROW09? M{j5SmlEPTB;OE[gcm0> M4LybFE5OzhzNES0
HCC1954 MkXNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX3lc4pUOTBizszN M37BPGROW09? M3HLN2lEPTB;MUG5JI5O NHLNfI4yQDN6MUS0OC=>
MDA-MB-453 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MW[xNEDPxE1? NFfm[oFFVVOR NYrmRVVUUUN3ME25O|Uhdk1? NXjhRZE4OTh|OEG0OFQ>
MDA-MB-468 NFLmWXhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NG\IPZQyOCEQvF2= NIm3c|FFVVOR MmiyTWM2OD1|MkC4JI5O MXixPFM5OTR2NB?=
SkBr3 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4[2b|ExKM7:TR?= M{Wwc2ROW09? M1jmeWlEPTB-MUCsNFAxKG6P M2iycFE5OzhzNES0
MDA-MB-231 NEXTTJFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVGxNEDPxE1? NVX0cplJTE2VTx?= M3f6O2lEPTB-MUCsNFAxKG6P MoHRNVg{QDF2NES=
HCT116 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2\Eb|ExKM7:TR?= NYjDcHV4TE2VTx?= NUPlcmhmUUN3ME21PFM3KG6P MnzWNVg{QDF2NES=
HT29 NYjpWYxyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M12yeVExKM7:TR?= M{PVN2ROW09? NH3CSFRKSzVyPkGwMFAxOCCwTR?= NITkb2MyQDN6MUS0OC=>
HFF MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2L3cVExKM7:TR?= MUTEUXNQ MXPJR|UxRTd4MUWgcm0> NV;hWHhKOTh|OEG0OFQ>
HN5 NI\sS|VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWGxNEDPxE1? NILj[HBFVVOR NH\qc4JKSzVyPkGwMFAxOCCwTR?= MmLiNVg{QDF2NES=
786-0 M17RWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVmxNEDPxE1? M1LPUWROW09? M3rJRWlEPTB;NECwPUBvVQ>? M3zBSlE5OzhzNES0
H157 M{DZT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW[xNEDPxE1? M{Lpb2ROW09? M{C4[GlEPTB;Mk[0NkBvVQ>? M4H2XFE5OzhzNES0
NCI-H460 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2G0OFExKM7:TR?= Ml3TSG1UVw>? NInLVodKSzVyPkKsOVAxKG6P MlK1NVg{QDF2NES=
SKOV-3 NEfzSI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUOxNEDPxE1? M2jxbGROW09? MoXOTWM2OD1{MUK2JI5O MWOxPFM5OTR2NB?=
OVCAR-3 NF71O4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUKxNEDPxE1? MUnEUXNQ MXLJR|UxRTJ7MUigcm0> NIrp[2cyQDN6MUS0OC=>
BXPC3 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHGNVAh|ryP NV:0OZdFTE2VTx?= MnXjTWM2OD1|MUSxJI5O NGTDOI8yQDN6MUS0OC=>
MiaPaCa M4L2b2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4S3[VExKM7:TR?= M4TXVGROW09? Mm\2TWM2OD13NEOzJI5O MoLXNVg{QDF2NES=
PANC-1 NFu0WYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmjKNVAh|ryP M3\mdmROW09? NEfhT2FKSzVyPUi2PFEhdk1? NGrJb2MyQDN6MUS0OC=>
LNCaP NIezTmpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVqxNEDPxE1? NEHMcVlFVVOR MYTJR|UxRTF2NzDuUS=> MX2xPFM5OTR2NB?=
DU145 Ml;NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHP2fpcyOCEQvF2= MVPEUXNQ M1njRWlEPTB;M{ixNkBvVQ>? NYixXopTOTh|OEG0OFQ>
PC3 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2HLXVExKM7:TR?= NHrPZnBFVVOR MmHITWM2OD5zMDywNFAhdk1? MWmxPFM5OTR2NB?=
BT474 NIrWbHNMcW6jc3WgZZN{[Xl? MmC1NVAh|ryP M1n5U2ROW09? M323ZolvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF4MDDuUS=> MYWxPFM5OTR2NB?=
786-0 NEGwT4hMcW6jc3WgZZN{[Xl? M1LkNVExKM7:TR?= NHr4e|RFVVOR MXvpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kAyPTBibl2= NEe1O2syQDN6MUS0OC=>
LNCaP MmXpT4lv[XOnIHHzd4F6 NUnuenE6OTBizszN NIm5WolFVVOR MVfpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1OyCwTR?= NX\USGlROTh|OEG0OFQ>
PC3 M4LyT2tqdmG|ZTDhd5NigQ>? MXixNEDPxE1? MWjEUXNQ MUDpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1QSCwTR?= NXezPWZ4OTh|OEG0OFQ>
KARPAS-231 NH\QXJFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXWxNEDPxE1? Mmm0SG1UVw>? NHvPNGRGSzVyPUSxJI5O MU[xPVA3PDd|MB?=
CCRFSB NIm3VFhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYHZe2hzOTBizszN MlXWSG1UVw>? NXHpfnVITUN3ME2xOVUhdk1? M2q4blE6ODZ2N{Ow
SUP B15 NHPFSIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF:4OGwyOCEQvF2= MYrEUXNQ MWjFR|UxRTF7NzDuUS=> NV32NXJKOTlyNkS3N|A>
SD-1 NIntWmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV6xNEDPxE1? M4HuVmROW09? M2OyWWVEPTB;M{KwJI5O MYWxPVA3PDd|MB?=
RS4;11 NF\TNpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVW2dlZ5OTBizszN NUHmOW5zTE2VTx?= NIPDRYZGSzVyPU[1OEBvVQ>? MVmxPVA3PDd|MB?=
MN-60 NVfzTHVKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1P2fVExKM7:TR?= M2GxfmROW09? MVHFR|UxRTN4MEKgcm0> MXuxPVA3PDd|MB?=
Tanoue NF7IfoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUOxNEDPxE1? MmruSG1UVw>? MX3FR|UxRTR3MUegcm0> MnTYNVkxPjR5M{C=
RCH-ACV Ml3qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYiz[YNFOTBizszN Mor6SG1UVw>? MoHFSWM2OD1zNUKgcm0> NGTKeIcyQTB4NEezNC=>
SEM NFfKWWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3nQSFExKM7:TR?= NUezNXZZTE2VTx?= M4nLNGVEPTB;MkCyJI5O NUn6SHc{OTlyNkS3N|A>
KASUMI-2 MmLTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWHQXG5zOTBizszN MX\EUXNQ M4LSNGVEPTB;MkK1JI5O NUXHeZk4OTlyNkS3N|A>
REH MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWSxNEDPxE1? MVnEUXNQ NHXaSJZGSzVyPUK4PEBvVQ>? MlfaNVkxPjR5M{C=
697 NW\5fY45T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXzq[|RVOTBizszN NWf6PHlRTE2VTx?= NHexTFNGSzVyPUOzPEBvVQ>? MlPSNVkxPjR5M{C=
NALM-6 M1;MTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGn6N28yOCEQvF2= NELFTppFVVOR MVjFR|UxRTR{MTDuUS=> MYqxPVA3PDd|MB?=
MHH-CALL–3 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWGxNEDPxE1? MWrEUXNQ MoTsSWM2OD16MUKgcm0> MWmxPVA3PDd|MB?=
MHH-CALL–2 NUe2NHE{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVTxOVhvOTBizszN MWDEUXNQ M3TTZmVEPTB;MkGxOEBvVQ>? M1zxd|E6ODZ2N{Ow
J.GAMMA-1 NHjGN5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\RNVAh|ryP NVHVPHJvTE2VTx?= MWnFR|UxRTZ3IH7N NEPiRoUyQTB4NEezNC=>
JR45.01 M3roZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXTnZ3l3OTBizszN MYHEUXNQ MonRSWM2OD14ODDuUS=> NUjESVZyOTlyNkS3N|A>
A3 Mmq5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4jvb|ExKM7:TR?= MkHySG1UVw>? M3TrTWVEPTB;Nkmgcm0> MV2xPVA3PDd|MB?=
I 2.1 MlGzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUiwfVF5OTBizszN MkDvSG1UVw>? MYHFR|UxRTd|IH7N NHjDTFMyQTB4NEezNC=>
MOLT-3 M1XjPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYWxNEDPxE1? Mme5SG1UVw>? NYT6ZW9bTUN3ME23OEBvVQ>? NFPHSWwyQTB4NEezNC=>
P116 NXPLU4l3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGTxXZYyOCEQvF2= MUfEUXNQ NHvIdWZGSzVyPUe4JI5O NICwZnkyQTB4NEezNC=>
J.Cam1.6 M{K2O2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlXaNVAh|ryP MX;EUXNQ NYjtcZM5TUN3ME23PUBvVQ>? MkO1NVkxPjR5M{C=
I 9.2 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEXaZYwyOCEQvF2= NXLqW4VzTE2VTx?= M1ToW2VEPTB;OECgcm0> MVKxPVA3PDd|MB?=
LOUCY M4THNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlLDNVAh|ryP M4rnTWROW09? NXjFSWtbTUN3ME2xNVchdk1? Ml72NVkxPjR5M{C=
J.RT3-T3.5 NUe1fZg2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXmxNEDPxE1? M{C1XWROW09? MofuSWM2OD1zMkOgcm0> NYjqUJNtOTlyNkS3N|A>
800000 MmDoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{PUblExKM7:TR?= M{\4cGROW09? MkDuSWM2OD1zNkOgcm0> NUm5bG96OTlyNkS3N|A>
Jurkat Ml3aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYHt[2VLOTBizszN NV2xZo9NTE2VTx?= M37NfWVEPTB;MkK1JI5O MnL5NVkxPjR5M{C=
MOLT-4 NXfBNnA3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3jpclExKM7:TR?= NVv6SVZXTE2VTx?= MXjFR|UxRTJ|MjDuUS=> NF\CVlUyQTB4NEezNC=>
Molt-16 MlfhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUWxNEDPxE1? M17zT2ROW09? MVLFR|UxRTJ2MTDuUS=> Ml;INVkxPjR5M{C=
CEM/C3 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYP5O|RMOTBizszN MYHEUXNQ M2TWZmVEPTB;MkW3JI5O NYiyV|h3OTlyNkS3N|A>
CEM/C2 M{THeWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoTjNVAh|ryP NFXne4lFVVOR MXfFR|UxRTJ5MTDuUS=> NXH6UYE5OTlyNkS3N|A>
CCRFCEM NIK1WolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml3sNVAh|ryP NUCzfGFLTE2VTx?= NVjGTXFSTUN3ME2zNlchdk1? NV\oVHNuOTlyNkS3N|A>
CEM/C1 NH7wV25Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlziNVAh|ryP NVPrO3hRTE2VTx?= M1jxSWVEPTB;M{iyJI5O NIPXXJAyQTB4NEezNC=>
SUPTI[VB] M{jzTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHG4ZZkyOCEQvF2= Mlu4SG1UVw>? MUTFR|UxRTZzOTDuUS=> NXXOXpBSOTlyNkS3N|A>
CCRF–HSB-2 M4jXN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3zIRVExKM7:TR?= M2K1bGROW09? NHPSN2ZGSzVyPUKxNVchdk1? NUT4SlR5OTlyNkS3N|A>
I 2.1 M3S4XWFxd3C2b4Ppd{Bie3OjeR?= MmPmNVAh|ryP NYPuNGJMTE2VTx?= NH;qdWNqdmS3Y3XzJIFxd3C2b4Ppdy=> NWfoW4xzOTlyNkS3N|A>
I 9.2 MljqRZBweHSxc3nzJIF{e2G7 NH7meXAyOCEQvF2= NHLsZ5VFVVOR NYGxNG9[cW6mdXPld{BieG:ydH;zbZM> NF\CTJMyQTB4NEezNC=>
A3 MmPuRZBweHSxc3nzJIF{e2G7 MlLrNVAh|ryP MnPtSG1UVw>? M37jOYlv\HWlZYOgZZBweHSxc3nz MnXaNVkxPjR5M{C=
RD NXjjOGdHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV:xNEDPxE1? NUntVoRDUUN3ME6xNEDPxE1? NFr6TmQzODd2ME[yNy=>
Rh41 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoPJNVAh|ryP MnrVTWM2OD1|Mz64JI5O Mm\1NlA4PDB4MkO=
Rh18 NEjjXmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGf4WoQyOCEQvF2= NFzmUmxKSzVyPUOwN{BvVQ>? NIHV[XUzODd2ME[yNy=>
Rh30 NXvIR3d1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHTCXGoyOCEQvF2= MVXJR|UxRTRwOEGg{txO NHTBNo0zODd2ME[yNy=>
BT-12 NXjydmlHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYGxNEDPxE1? NFzTVlhKSzVyPkGwJO69VQ>? MVyyNFc1ODZ{Mx?=
CHLA-266 MkjQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mnj3NVAh|ryP MnXZTWM2OD1zLkKyJO69VQ>? M3;3WFIxPzRyNkKz
TC-71 NIHIOlFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWmxNEDPxE1? NVm3NYp6UUN3ME2yMlUzKM7:TR?= NXTDTW1UOjB5NEC2NlM>
CHLA-9 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH3ZPIUyOCEQvF2= NXXl[XRwUUN3ME21PVEhdk1? NEHGSXozODd2ME[yNy=>
CHLA-10 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MY[xNEDPxE1? M33WcGlEPTB;MUCyJI5O MYeyNFc1ODZ{Mx?=
CHLA-258 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkLzNVAh|ryP M3;s[2lEPTB;MT6wOUDPxE1? MWeyNFc1ODZ{Mx?=
GBM2 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWOxNEDPxE1? Mmj1TWM2OD17LkG1JO69VQ>? M3;FVFIxPzRyNkKz
NB-1643 NWLSSYpFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3vSWlExKM7:TR?= NWixZWlsUUN3ME21MlQh|ryP MXmyNFc1ODZ{Mx?=
NB-Ebc1 NHm2R5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1nTdVExKM7:TR?= M3;mb2lEPTB-MUCg{txO MlP5NlA4PDB4MkO=
CHLA-90 MnHGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXGxNEDPxE1? NUnVSIc3UUN3ME6xNEDPxE1? MVmyNFc1ODZ{Mx?=
CHLA-136 NYKxOoFET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWPIO21sOTBizszN MkD3TWM2OD5zMDFOwG0> NVfJUmVROjB5NEC2NlM>
NALM-6 NV2wb2g4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV[xNEDPxE1? NEPCXYNKSzVyPUK2OUBvVQ>? NIPpXWczODd2ME[yNy=>
COG-LL-317 MlXNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEXPdWYyOCEQvF2= M3rCbGlEPTB;Nj60PUBvVQ>? NFT4WI0zODd2ME[yNy=>
RS4;11 NXXnXHNCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWqxNEDPxE1? NUfUXGZnUUN3ME2xOFchdk1? M{eyW|IxPzRyNkKz
MOLT-4 NF\ZSmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnfRNVAh|ryP MkPzTWM2OD12MDDuUS=> NV3EdnFCOjB5NEC2NlM>
CCRF-CEM NV3wNmF5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4PxfVExKM7:TR?= MojpTWM2OD1{Nkigcm0> MYWyNFc1ODZ{Mx?=
Kasumi-1 NEXjeJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXOw[5NbOTBizszN NIHxO4JKSzVyPUGwO{BvVQ>? MoXVNlA4PDB4MkO=
Karpas-299 MmjYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4fFZVExKM7:TR?= MVPJR|UxRTJwOUOg{txO NHHMTpAzODd2ME[yNy=>
Ramos-RA1 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYexNEDPxE1? MXPJR|UxRTdwM{Wg{txO MYmyNFc1ODZ{Mx?=
H1299 Mm\ET4lv[XOnIHHzd4F6 M1nTflExKM7:TR?= MoDqbY5pcWKrdIOgTWtDU0VvaX7keYNm\CCDa4SgRYN1cX[jdHnvci=> M2LUclIyQTB6NkG2

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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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

CAS No. 905854-02-6
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID