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 Mk\5T4lv[XOnIHHzd4F6 MWL+NVAh|ryP NFzC[4NqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MnTqNlA1QDRyMUi=
HT29 NVvB[ZE6U2mwYYPlJIF{e2G7 M13QVJ4yOCEQvF2= NYq4UGxPcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NVvzb3NWOjB2OESwNVg>
MDA-MB-231 NV7ucW1xU2mwYYPlJIF{e2G7 MY\+NVAh|ryP NEDlNG5qdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NGrGc|kzODR6NECxPC=>
NCI-H441 NFPCNVRMcW6jc3WgZZN{[Xl? NVuyZXM5hjFyIN88US=> MlXIbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MnXMNlA1QDRyMUi=
SK-MEL-28 NEHIXXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3rDSlM{KM7:TR?= M2DvNmlEPTB-M{Og{txO M3znWlIxPDh2MEG4
NCI-H661 NFnEeW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3PDTlM{KM7:TR?= MlK2TWM2OD5|MzFOwG0> M3jKe|IxPDh2MEG4
NCI-H446 M1\MZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGjjSGU{OyEQvF2= MUTJR|UxRTdizszN MWSyNFQ5PDBzOB?=
MDA-MB-231 Moe1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml3NN|Mh|ryP NEe1VotKSzVyPUCuOVUh|ryP NYGzR49DOjB2OESwNVg>
DLD-1 NH60VWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVizN{DPxE1? M2XkNmlEPTB;MD61N{DPxE1? NFj5eXMzODR6NECxPC=>
A549 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWHxe2JzOzNizszN NYXJfldbUUN3ME2wMlU6KM7:TR?= MXSyNFQ5PDBzOB?=
SK-OV-3 NYTSSnlMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3\rWlM{KM7:TR?= NW\rZmU2UUN3ME2wMlY3KM7:TR?= M2fTbFIxPDh2MEG4
NCI-H460 NIm3NG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{HZOVM{KM7:TR?= M1XsWGlEPTB;MD62JO69VQ>? MUeyNFQ5PDBzOB?=
A375 M2mx[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUnGNYVtOzNizszN NXL4VpA3UUN3ME2wMlQzKM7:TR?= Mn\rNlA1QDRyMUi=
NCI-H441 Mn60S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4j1cVM{KM7:TR?= NVvQO4xbUUN3ME2wMlMh|ryP NGnlVYIzODR6NECxPC=>
HT29 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn\YN|Mh|ryP MnrkTWM2OD1yLkS5JO69VQ>? NEnvTJgzODR6NECxPC=>
MKN-45 NWnU[WpWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVfVVIZFOzNizszN NYmze2FSUUN3ME2wMlU5KM7:TR?= M4DSW|IxPDh2MEG4
HT29 MmfpRZBweHSxc3nzJIF{e2G7 NXq5cIZuhjFyIN88US=> NHXUW5d{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= MkXKNlA1QDRyMUi=
MKN-45 MXrBdI9xfG:|aYOgZZN{[Xl? MlPHglExKM7:TR?= MmrPd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw M{nib|IxPDh2MEG4
MDA-MB-231 NXHKcIh2SXCxcITvd4l{KGG|c3H5 NYr5[odShjFyIN88US=> NV22U5lWdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> NVXFRW1COjB2OESwNVg>
MDA-MB-231/TGL M2XqTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX[3Z3E2hjFyMDFOwG0> M2PC[GdKPTB;MT6yJO69VQ>? M2qxb|IzODJ5Nkmw
1833/TGL MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1zzT54yODBizszN NF3UNW1IUTVyPUOuO{DPxE1? Mn7qNlIxOjd4OUC=
EBC1 MUXDfZRwfG:6aXRCpIF{e2G7 MWj+NVAh|ryP NH\uNHpqdmirYnn0d{B1cGViY3XscEBoem:5dHiu M3HlOlI{PTl6Mke2
SNU638 NHXzRnhEgXSxdH;4bYPDqGG|c3H5 NYjTVXdEhjFyIN88US=> NEfNUI5qdmirYnn0d{B1cGViY3XscEBoem:5dHiu MkHKNlM2QTh{N{[=
A549 NIHsTZZEgXSxdH;4bYPDqGG|c3H5 NUPFbVFQhjFyIN88US=> M3rYOI5wfCCjZn\lZ5Q> MXuyN|U6QDJ5Nh?=
H460 NUnP[INiS3m2b4TvfIlkyqCjc4PhfS=> NH7Vd29,OTBizszN NUfrdWJqdm:2IHHm[oVkfA>? NVnIVVAzOjN3OUiyO|Y>
HCC827 Ml\RR5l1d3SxeHnjxsBie3OjeR?= NUe0U4N3hjFyIN88US=> MnPlco91KGGoZnXjeC=> M2iyV|I{PTl6Mke2
A549 MYrGeY5kfGmxbjDhd5NigQ>? Ml\CNVAh|ryP MVnkbZNzfXC2czDtbYNzd3S3YoXs[S=> MVGyN|U6QDJ5Nh?=
EBC1 NH36V3JHfW6ldHnvckBie3OjeR?= NGGyO3gyOCEQvF2= MlfJ[Il{enWydIOgcYlkem:2dXL1cIU> NHjZSFczOzV7OEK3Oi=>
H460 NEjOTFdHfW6ldHnvckBie3OjeR?= NHuxUHgyOCEQvF2= NFjHd3VqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w NGK1RpgzPTNzM{CxNC=>
K562/VCR NFH0UGdEgXSxdH;4bYPDqGG|c3H5 NFzWOox,OTBizszN MmnPd4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 MVuyOVMyOzBzMB?=
CEM/VBL NV\pUlJmS3m2b4TvfIlkyqCjc4PhfS=> MnXDglExKM7:TR?= NVrLd4pue2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 M1jlN|I2OzF|MEGw
U266 MWfDfZRwfG:6aXRCpIF{e2G7 NHHYbGl,OyEQvF5CpC=> MnGxTWM2OD1zLkGg{txO NE\wZ4gzPThzMECxNy=>
OPM-2 NHLIUW1EgXSxdH;4bYPDqGG|c3H5 NHXnRnl,OyEQvF5CpC=> MV7JR|UxRTFwODFOwG0> M1vZbFI2QDFyMEGz
MM.1S MnPBR5l1d3SxeHnjxsBie3OjeR?= NILZVVR,OyEQvF5CpC=> MoK3TWM2OD1zLk[g{txO NYTl[oVVOjV6MUCwNVM>
MM.1R NXz0[WRwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUPLd|dSOyEQvF5CpC=> NVvCNXhVcW6qaXLpeJMh[2WubDDndo94fGhiYomgOFkm NGrncmwzPThzMECxNy=>
RPMI-8226 MnzHR5l1d3SxeHnjxsBie3OjeR?= NUnLNZhXhjNizszNxsA> NH:yRZlKSzVyPUCuPUDPxE1? M3vqRVI2QDFyMEGz
ANBL-6 NXi4NpNrS3m2b4TvfIlkyqCjc4PhfS=> MmjqNUDPxE4EoB?= NYr5RpBScW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MX[yOVgyODBzMx?=
ANLB-6/V10R MYHDfZRwfG:6aXRCpIF{e2G7 NUf6fVR{OSEQvF5CpC=> NV3NZo54cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M4\MblI2QDFyMEGz
KAS-6/1 M1Wy[GN6fG:2b4jpZ:Kh[XO|YYm= NV3ibod5OSEQvF5CpC=> NEHMO45qdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MkXaNlU5OTByMUO=
KAS-6/V10R M{nPRWN6fG:2b4jpZ:Kh[XO|YYm= M4\1eVEh|ryPwrC= MVjpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NXnSVVFkOjV6MUCwNVM>
KAS-6/R10R MYPDfZRwfG:6aXRCpIF{e2G7 M37PfFEh|ryPwrC= MVzpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= Ml\RNlU5OTByMUO=
8226/S NVXN[25vT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFvtRVM{KM7:TdMg MmHubY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NXXucWNPOjV6MUCwNVM>
8226/LR-5 NVrHXYQ{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV72PW9HOyEQvF5CpC=> M2nncIlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> NXnnR41ZOjV6MUCwNVM>
Huh7 MYrDfZRwfG:6aXRCpIF{e2G7 M{jLUJ41NjhizszNxsA> MoTPSG1UVw>? NVSwfZZRUUN3ME25Mlkhdk1? MXOyOlI2QTJ3MB?=
Hep3B MXPDfZRwfG:6aXRCpIF{e2G7 MVv+OE45KM7:TdMg M{jDRmROW09? NFmxUmRKSzVyPUS0PE44KG6P NXuzUGROOjZ{NUmyOVA>
HepG2 M2HoOWN6fG:2b4jpZ:Kh[XO|YYm= M2jafJ41NjhizszNxsA> MVjEUXNQ MVXJR|UxRTF|OT63O{BvVQ>? MUeyOlI2QTJ3MB?=
Chang M{n3dWN6fG:2b4jpZ:Kh[XO|YYm= NIDDXYt,PC56IN88UeKh MVfEUXNQ MlTMTWM2OD12NEiuO{BvVQ>? MkH5NlYzPTl{NUC=
Huh7 MVTGeY5kfGmxbjDhd5NigQ>? MYixMlYh|ryPwrC= NUKx[|JTTE2VTx?= NYXw[2Zn[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M33x[VI3OjV7MkWw
Hep3B NHjZVWFHfW6ldHnvckBie3OjeR?= NFvjbVYyNjZizszNxsA> MYDEUXNQ NFPrSYVk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M134bFI3OjV7MkWw
HepG2 MmToSpVv[3Srb36gZZN{[Xl? MYCxMlYh|ryPwrC= NVrCdYxjTE2VTx?= NXzZcIZt[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M1\JbVI3OjV7MkWw
Chang M1LY[2Z2dmO2aX;uJIF{e2G7 M1vo[lEvPiEQvF5CpC=> M2L0d2ROW09? M2PWd4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NELxXYczPjJ3OUK1NC=>
MHCC97L NGnST2VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHLCUWJ,OTBizszN NHz0XYNFVVOR MXHJR|UxRTNzNTDuUS=> MV:yOlQ2QDl3Mx?=
MHCC97H NGH0eZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1u5b54yOCEQvF2= NInlc|hFVVOR Mof1TWM2OD1|NklihKkhdk1? NYnDVXBuOjZ2NUi5OVM>
Huh7 M3f6OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3rXep4yOCEQvF2= MYDEUXNQ NVv3cll5UUN3ME2yOlUhdk1? NXPyWGgzOjZ2NUi5OVM>
HepG2 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M165fp4yOCEQvF2= NF;p[mVFVVOR M4iy[mlEPTB;M{myJI5O NIHjeZMzPjR3OEm1Ny=>
MHCC97L MWjGeY5kfGmxbjDhd5NigQ>? M2rLcVEh|ryPwrC= M3ezcmROW09? NWi2cYdjcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NGjGbFUzPjR3OEm1Ny=>
Huh7 MVLGeY5kfGmxbjDhd5NigQ>? Ml\aNUDPxE4EoB?= NWLEZ|lKTE2VTx?= MoPqbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NF34U3MzPjR3OEm1Ny=>
MHCC97L M2iwUWFxd3C2b4Ppd{Bie3OjeR?= NFzmN5cyKM7:TdMg NHrLb5lFVVOR NWnONJVFcW6mdXPld{BieG:ydH;zbZM> MUKyOlQ2QDl3Mx?=
Huh7 NGXsUmpCeG:ydH;zbZMh[XO|YYm= MoDWNUDPxE4EoB?= NUXrfJRqTE2VTx?= MXrpcoR2[2W|IHHwc5B1d3Orcx?= NHnKRZUzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts MYrLbY5ie2ViYYPzZZk> NUfOeHljOjVizszN M1:wc2ROW09? M2jCcJJm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MWOyNFU{PDN2NR?=
H23 MnPhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1ixNVI2KM7:TR?= Ml;RSG1UVw>? MmDUd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NV7LT2t5OjB3M{SzOFU>
WM35 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXKxNEDPxE1? M1\SSmROW09? NELUU5p{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> MVSyNFU{PDN2NR?=
NIH 3T3 MoLmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIG1UmYyOCEQvF2= NVjPe3pITE2VTx?= NH3JO3Bld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NYD5TXplOjB3M{SzOFU>
H838 NEfDS3RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYPQR4pjOTBizszN NXPDOoFsTE2VTx?= M3\qSoRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MYCyNFU{PDN2NR?=
H1395 NH3GNWtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWqxNEDPxE1? MWHEUXNQ NW\XbXd2\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NEn3RZozODV|NEO0OS=>
Quiescent S2 MYTLbY5ie2ViYYPzZZk> NVr5UndQOzBizszN MlO4SG1UVw>? MlHZZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| M1XnV|IyPTF6OUG1
PC3 MYTBdI9xfG:|aYOgZZN{[Xl? NFHaeI4zOCEQvF2= M3[wdmROW09? MXjpcoR2[2W|IHHwc5B1d3Orcx?= NEKxOYUzOTdyOUGzNC=>
Du145 MWHBdI9xfG:|aYOgZZN{[Xl? MV6yNEDPxE1? M3GxTmROW09? MXrpcoR2[2W|IHHwc5B1d3Orcx?= NFW1VVYzOTdyOUGzNC=>
LNCaP MWHBdI9xfG:|aYOgZZN{[Xl? MmTBNlAh|ryP MnXOSG1UVw>? MmLXbY5lfWOnczDhdI9xfG:|aYO= NHrQbnQzOTdyOUGzNC=>
LAPC-4 NWSycHdGSXCxcITvd4l{KGG|c3H5 NIK2OWozOCEQvF2= MWfEUXNQ MUHpcoR2[2W|IHHwc5B1d3Orcx?= NF;pZ|kzOTdyOUGzNC=>
LNCaP NGrWSGpHfW6ldHnvckBie3OjeR?= NGPPPW0zOCEQvF2= M1f6PWROW09? NEfIRoJl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NHTOe3czOTdyOUGzNC=>
LAPC-4 NWjlcI9oTnWwY4Tpc44h[XO|YYm= M13UUVIxKM7:TR?= NHe5O2tFVVOR MnrS[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MmfkNlE4ODlzM{C=
Kasumi-1 NFTzVpJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3XKWp42OCEQvF2= NIO4eYpFVVOR M{HLbolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NG\KXo8zOzN7MEWzOi=>
SKNO-1 NInaVW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\IglUxKM7:TR?= NWXuNVlMTE2VTx?= NX7WTJRUcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4ruXFI{OzlyNUO2
Kasumi-1 M1jRWWtqdmG|ZTDhd5NigQ>? NFz3UmZ,OTBizszN MYXEUXNQ M3zUd5Jm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> NEOz[WMzOzN7MEWzOi=>
SKNO-1 NYTUW3ZOU2mwYYPlJIF{e2G7 NF;YOY9,OTBizszN NX3ZXmIxTE2VTx?= NWHXSVQxemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NEfpZ3ozOzN7MEWzOi=>
A549 Mn;tSpVv[3Srb36gZZN{[Xl? M3LENlExKM7:TR?= M{nQR2ROW09? M4LEbYVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> NGrvRXAzPDd2NkW3OC=>
NRK-52E MYLGeY5kfGmxbjDhd5NigQ>? M4rsN|ExKM7:TR?= M4TvWWROW09? MULpcohq[mm2czDBcochUUlvaX7keYNm\CCVVFHUN{BvfWOuZXHyJJRz[W6|bH;jZZRqd25iYX7kJJRp\SCneIDy[ZN{cW:wIH;mJHRITi4QskGsJINwdGyjZ3XuJGlXKGGwZDDmbYJzd26nY4Tpci=> NXj6d|VHOjVyOEiwNFI>
PC12 M1nnOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnjDglEzNjVizszN NXHocld7TE2VTx?= MnmzdJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> NHHvcmkzPTF{OEO4Oi=>
HPMCs NXTxPG5mTnWwY4Tpc44h[XO|YYm= MUHy[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> NUjUb3VnOjZyNEW3PFA>
A549 NX;oZmx3TnWwY4Tpc44h[XO|YYm= MVT+OVAh|ryP M{fsemROW09? MmjPZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> MXSyOlcyOTd2OB?=
RAW264.7 MmTSSpVv[3Srb36gZZN{[Xl? NFzqe3V,OzBizszN MmPOSG1UVw>? M2GzfpJm\HWlZYOgdJJwNWmwZnzhcY1ifG:{eTDn[Y5mKGW6cILld5Nqd25? MkHXNlY4OTh3OE[=
MEMM M4XEVmtqdmG|ZTDhd5NigQ>? M1Xa[VE2KML3TR?= NXXHSIhJTE2VTx?= NWPRV3dn\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> NWm1NW4zOjZ7MkG1NFY>
MEMM NGTscoFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUH+NlAhyrWP M13VTWROW09? NWLNO|BKcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4CwW|I3QTJzNUC2
MEMM NHnsfZRCeG:ydH;zbZMh[XO|YYm= NVW3bXJ2OTViwsXN NH7vN3ZFVVOR NULhUpE2cW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? M1vDZ|I3QTJzNUC2
T47D NWfwfZpsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFPIUJEyOCEQvF2= NXXEOJd7TE2VTx?= MYTJR|UxRTd{IH7N MUGxPFM5OTR2NB?=
ZR-75-1 NUS3[lh7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIL1bXcyOCEQvF2= NV[2eZRlTE2VTx?= MoPiTWM2OD15OTDuUS=> MlPrNVg{QDF2NES=
BT474 NWGyb4hnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUHXR4JiOTBizszN NX;4ZnI{TE2VTx?= NH7ONm5KSzVyPUi2JI5O M2qyV|E5OzhzNES0
HCC1954 MkjNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;ad5EyOCEQvF2= NGrmfIpFVVOR MWPJR|UxRTFzOTDuUS=> NGHGSocyQDN6MUS0OC=>
MDA-MB-453 NHPXcndIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVKxNEDPxE1? MlvtSG1UVw>? NUPaW5Q6UUN3ME25O|Uhdk1? MonUNVg{QDF2NES=
MDA-MB-468 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFzIcnUyOCEQvF2= NWTpVIF2TE2VTx?= NFHQWphKSzVyPUOyNFghdk1? M4PmdlE5OzhzNES0
SkBr3 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFTafVEyOCEQvF2= M1XNd2ROW09? M2GxVmlEPTB-MUCsNFAxKG6P NF7DO2cyQDN6MUS0OC=>
MDA-MB-231 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1nQcVExKM7:TR?= MUnEUXNQ NWDFN2xvUUN3ME6xNEwxODBibl2= NXjoPYdQOTh|OEG0OFQ>
HCT116 M3XVNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF7QNGMyOCEQvF2= NXTheYptTE2VTx?= NH73epBKSzVyPUW4N|Yhdk1? NH7aTosyQDN6MUS0OC=>
HT29 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWexNEDPxE1? Mn7jSG1UVw>? M3X3OmlEPTB-MUCsNFAxKG6P MWCxPFM5OTR2NB?=
HFF MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUKxNEDPxE1? MYnEUXNQ MX3JR|UxRTd4MUWgcm0> NFf4coUyQDN6MUS0OC=>
HN5 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4fHVFExKM7:TR?= NHWzSVRFVVOR NW\VNWJCUUN3ME6xNEwxODBibl2= MlTkNVg{QDF2NES=
786-0 MmW5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGHzcJUyOCEQvF2= NE\SPHVFVVOR M4G2TWlEPTB;NECwPUBvVQ>? MYOxPFM5OTR2NB?=
H157 NE\JOZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2rQN|ExKM7:TR?= NX7uPWcxTE2VTx?= NWPpR|E6UUN3ME2yOlQzKG6P MXWxPFM5OTR2NB?=
NCI-H460 MkfkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWCxNEDPxE1? NFfGWmZFVVOR NVfhcGw2UUN3ME6yMFUxOCCwTR?= M1T4NVE5OzhzNES0
SKOV-3 MnvHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVrBWXNZOTBizszN NUX6WpRrTE2VTx?= NV3rT2FyUUN3ME2yNVI3KG6P NWDmSZFyOTh|OEG0OFQ>
OVCAR-3 NWjMZmljT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlXPNVAh|ryP NFXRc25FVVOR Mo\PTWM2OD1{OUG4JI5O NUjnfZRkOTh|OEG0OFQ>
BXPC3 NEHWNXhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWfQdJBnOTBizszN M3HaemROW09? NVf6SVUxUUN3ME2zNVQyKG6P NFrue3EyQDN6MUS0OC=>
MiaPaCa MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVSxNEDPxE1? MX3EUXNQ Moq0TWM2OD13NEOzJI5O M{m4SlE5OzhzNES0
PANC-1 Mn[1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUPaR|BPOTBizszN NHrC[|NFVVOR M2jpemlEPTB;OE[4NUBvVQ>? NEC4VJEyQDN6MUS0OC=>
LNCaP MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXBNVAh|ryP MXPEUXNQ NEH6XVJKSzVyPUG0O{BvVQ>? M2jCO|E5OzhzNES0
DU145 MoDFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlzmNVAh|ryP NXyyW2VrTE2VTx?= MmXJTWM2OD1|OEGyJI5O Mm[0NVg{QDF2NES=
PC3 M17PcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVmxNEDPxE1? MV;EUXNQ M4DnW2lEPTB-MUCsNFAxKG6P M4f6dlE5OzhzNES0
BT474 NXL1SGlnU2mwYYPlJIF{e2G7 NEDWPVgyOCEQvF2= Mn6xSG1UVw>? MmTCbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTZyIH7N MmfLNVg{QDF2NES=
786-0 Ml;VT4lv[XOnIHHzd4F6 NEjOfoYyOCEQvF2= M2DTb2ROW09? NULieGdzcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMUWwJI5O NXXEfXpZOTh|OEG0OFQ>
LNCaP M3eyS2tqdmG|ZTDhd5NigQ>? MmTzNVAh|ryP M3TLUmROW09? Moi1bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDNibl2= NWH6WoI4OTh|OEG0OFQ>
PC3 MYPLbY5ie2ViYYPzZZk> M2qwS|ExKM7:TR?= NE\x[JNFVVOR MWDpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1QSCwTR?= NHz2cIQyQDN6MUS0OC=>
KARPAS-231 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkjmNVAh|ryP M33uN2ROW09? MlKySWM2OD12MTDuUS=> NYK1d2R5OTlyNkS3N|A>
CCRFSB M3L5fWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYSxNEDPxE1? MnHwSG1UVw>? MVzFR|UxRTF3NTDuUS=> NIXGZWkyQTB4NEezNC=>
SUP B15 M3yzfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml\6NVAh|ryP M2e1fGROW09? MkO3SWM2OD1zOUegcm0> NIP4[XUyQTB4NEezNC=>
SD-1 MnHJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmn2NVAh|ryP M2j4fmROW09? Ml;nSWM2OD1|MkCgcm0> MoDVNVkxPjR5M{C=
RS4;11 M2TjZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUmxNEDPxE1? NVH2dGZuTE2VTx?= NXfrNpVnTUN3ME22OVQhdk1? MU[xPVA3PDd|MB?=
MN-60 NXvVb4FHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUexNEDPxE1? NEf4b2pFVVOR M2rxemVEPTB;M{[wNkBvVQ>? MkC3NVkxPjR5M{C=
Tanoue MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M13hc|ExKM7:TR?= MlTVSG1UVw>? MV7FR|UxRTR3MUegcm0> Ml:yNVkxPjR5M{C=
RCH-ACV NWTkS3p[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3rCUFExKM7:TR?= NGjpeXpFVVOR NFLVT|dGSzVyPUG1NkBvVQ>? M1HwNFE6ODZ2N{Ow
SEM MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHPBVYkyOCEQvF2= MVTEUXNQ NGPUOlhGSzVyPUKwNkBvVQ>? M1i5[FE6ODZ2N{Ow
KASUMI-2 MoOwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX\SV45tOTBizszN NFPRb41FVVOR NHnYOmpGSzVyPUKyOUBvVQ>? NGPxNpcyQTB4NEezNC=>
REH NH72eHNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\jNVAh|ryP MXTEUXNQ NV\XXpVLTUN3ME2yPFghdk1? NHrnN2QyQTB4NEezNC=>
697 M4rQOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmnFNVAh|ryP NX3UcmhoTE2VTx?= MUXFR|UxRTN|ODDuUS=> Ml;VNVkxPjR5M{C=
NALM-6 NHn2SpBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlPRNVAh|ryP Mlu3SG1UVw>? NX\YW|RmTUN3ME20NlEhdk1? NHrwPWcyQTB4NEezNC=>
MHH-CALL–3 NH3HfWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4TwWlExKM7:TR?= MlrTSG1UVw>? Ml\hSWM2OD16MUKgcm0> MlHmNVkxPjR5M{C=
MHH-CALL–2 MmjCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFjKdIUyOCEQvF2= NVTaUnNPTE2VTx?= Mnj0SWM2OD1{MUG0JI5O MX6xPVA3PDd|MB?=
J.GAMMA-1 NF\tN2NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEPwZY0yOCEQvF2= MkTOSG1UVw>? NWm1RopQTUN3ME22OUBvVQ>? NHTUbWkyQTB4NEezNC=>
JR45.01 MmPJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnnyNVAh|ryP MWrEUXNQ M1u1[2VEPTB;Nkigcm0> MkXYNVkxPjR5M{C=
A3 NYT6c|N2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYCxNEDPxE1? NH3uW4RFVVOR NYfOS2tPTUN3ME22PUBvVQ>? M1:0RlE6ODZ2N{Ow
I 2.1 NWfoTpV2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX6xNEDPxE1? NWSycoFYTE2VTx?= NFn4UYFGSzVyPUezJI5O MWixPVA3PDd|MB?=
MOLT-3 NFnwZ|VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGrWWnMyOCEQvF2= MVnEUXNQ MoHqSWM2OD15NDDuUS=> Mlm4NVkxPjR5M{C=
P116 M2LjUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M37Ee|ExKM7:TR?= MUTEUXNQ NXraV4h6TUN3ME23PEBvVQ>? M2nhNlE6ODZ2N{Ow
J.Cam1.6 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYDMeWZ[OTBizszN NHjBfmpFVVOR Mm[2SWM2OD15OTDuUS=> NYm0U4UxOTlyNkS3N|A>
I 9.2 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXqxNEDPxE1? MYPEUXNQ M2LVb2VEPTB;OECgcm0> NIfvTWEyQTB4NEezNC=>
LOUCY M1KzbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVOxNEDPxE1? MmDMSG1UVw>? M3zKd2VEPTB;MUG3JI5O M4e5PVE6ODZ2N{Ow
J.RT3-T3.5 NE\LOGlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3[5fFExKM7:TR?= M4\jfmROW09? M4fscWVEPTB;MUKzJI5O MnjNNVkxPjR5M{C=
800000 NV;n[ZFvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml;oNVAh|ryP M2jKU2ROW09? NFy0UXBGSzVyPUG2N{BvVQ>? MXOxPVA3PDd|MB?=
Jurkat NVH0WZdpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnjaNVAh|ryP NFvyflhFVVOR M3e5PGVEPTB;MkK1JI5O MYKxPVA3PDd|MB?=
MOLT-4 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIfYN3YyOCEQvF2= NFnqOoFFVVOR NXWyTHZqTUN3ME2yN|Ihdk1? M4juUlE6ODZ2N{Ow
Molt-16 M2\Zfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M13ncFExKM7:TR?= M1XEXWROW09? MUXFR|UxRTJ2MTDuUS=> M2foWVE6ODZ2N{Ow
CEM/C3 M3y5SGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUnJcW9MOTBizszN NID6eG9FVVOR MUjFR|UxRTJ3NzDuUS=> M{DYXlE6ODZ2N{Ow
CEM/C2 MlnLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYCxNEDPxE1? NYH1e4lKTE2VTx?= MUnFR|UxRTJ5MTDuUS=> NUHrU|FrOTlyNkS3N|A>
CCRFCEM MnHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVnoTIJYOTBizszN NI[0boxFVVOR NHzpR2FGSzVyPUOyO{BvVQ>? M{fwNFE6ODZ2N{Ow
CEM/C1 M3exfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4nZUlExKM7:TR?= MWPEUXNQ NVflS2R5TUN3ME2zPFIhdk1? Mo\6NVkxPjR5M{C=
SUPTI[VB] NYD5eIFqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYSxNEDPxE1? NIHzbWtFVVOR MW\FR|UxRTZzOTDuUS=> NFXV[VUyQTB4NEezNC=>
CCRF–HSB-2 Mn31S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHLuVnEyOCEQvF2= NHXkVIpFVVOR NXi5[Ic6TUN3ME2yNVE4KG6P MXuxPVA3PDd|MB?=
I 2.1 NXn2N2xlSXCxcITvd4l{KGG|c3H5 NVjkXZlTOTBizszN M4nMbGROW09? MmDCbY5lfWOnczDhdI9xfG:|aYO= Moq3NVkxPjR5M{C=
I 9.2 MUfBdI9xfG:|aYOgZZN{[Xl? MUixNEDPxE1? MmLZSG1UVw>? NVjISmtUcW6mdXPld{BieG:ydH;zbZM> NHHvN|cyQTB4NEezNC=>
A3 M4rqN2Fxd3C2b4Ppd{Bie3OjeR?= MoXvNVAh|ryP NYDiVFBbTE2VTx?= Mk[zbY5lfWOnczDhdI9xfG:|aYO= MlT5NVkxPjR5M{C=
RD NELBU2JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVnMe|lrOTBizszN M3n6UWlEPTB-MUCg{txO MoXSNlA4PDB4MkO=
Rh41 M3u0[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWXYTWY6OTBizszN NXPKb4hGUUN3ME2zN{45KG6P NEXvZmUzODd2ME[yNy=>
Rh18 MnPYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUCxNEDPxE1? M37HTWlEPTB;M{CzJI5O MnjkNlA4PDB4MkO=
Rh30 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUWxNEDPxE1? M{P1fWlEPTB;ND64NUDPxE1? Mn72NlA4PDB4MkO=
BT-12 M{nZOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVOxNEDPxE1? NHvBb4JKSzVyPkGwJO69VQ>? NX3meZpKOjB5NEC2NlM>
CHLA-266 NEn0PHpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mlj3NVAh|ryP MULJR|UxRTFwMkKg{txO NIrlO44zODd2ME[yNy=>
TC-71 M13zbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUDYSIZyOTBizszN Ml3jTWM2OD1{LkWyJO69VQ>? NYfKcpBWOjB5NEC2NlM>
CHLA-9 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX:xNEDPxE1? NHrqUnRKSzVyPUW5NUBvVQ>? MlzINlA4PDB4MkO=
CHLA-10 M3r1Wmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXexNEDPxE1? MnnOTWM2OD1zMEKgcm0> NImzcXEzODd2ME[yNy=>
CHLA-258 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXUNVAh|ryP M3:0cmlEPTB;MT6wOUDPxE1? NFPuO3ozODd2ME[yNy=>
GBM2 NXXpcIQ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkPlNVAh|ryP MlTsTWM2OD17LkG1JO69VQ>? NX7s[JZGOjB5NEC2NlM>
NB-1643 NIHhfHJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkDYNVAh|ryP NYr0UlBwUUN3ME21MlQh|ryP MW[yNFc1ODZ{Mx?=
NB-Ebc1 NF7vZ3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIXYc5EyOCEQvF2= NXT4enBbUUN3ME6xNEDPxE1? NIH1T|YzODd2ME[yNy=>
CHLA-90 MnPrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGfHc2IyOCEQvF2= NXjhWnY3UUN3ME6xNEDPxE1? MWOyNFc1ODZ{Mx?=
CHLA-136 NHTRToJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVLacWZ1OTBizszN Mlj3TWM2OD5zMDFOwG0> M2XMO|IxPzRyNkKz
NALM-6 NGTNOmFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWCwVoR5OTBizszN MkX2TWM2OD1{NkWgcm0> NGrM[WYzODd2ME[yNy=>
COG-LL-317 Mo[5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX2xNEDPxE1? Ml;XTWM2OD14LkS5JI5O M2HQNlIxPzRyNkKz
RS4;11 NUXzNW9jT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWDEVlRGOTBizszN NVizXnd7UUN3ME2xOFchdk1? MkPGNlA4PDB4MkO=
MOLT-4 M{DLbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVjOZnJLOTBizszN M1fmVWlEPTB;NECgcm0> MojnNlA4PDB4MkO=
CCRF-CEM NGXPV5hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnnRNVAh|ryP MorhTWM2OD1{Nkigcm0> NIO1b4MzODd2ME[yNy=>
Kasumi-1 NWribHkyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX:xNEDPxE1? MW\JR|UxRTFyNzDuUS=> NFK5UZQzODd2ME[yNy=>
Karpas-299 NFrQXo1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MW[xNEDPxE1? NWHnNWNvUUN3ME2yMlk{KM7:TR?= MV6yNFc1ODZ{Mx?=
Ramos-RA1 NWXJXXFOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXPK[mdSOTBizszN NWDLR3JrUUN3ME23MlM2KM7:TR?= MnrkNlA4PDB4MkO=
H1299 NF7UWppMcW6jc3WgZZN{[Xl? MnizNVAh|ryP Mnv0bY5pcWKrdIOgTWtDU0VvaX7keYNm\CCDa4SgRYN1cX[jdHnvci=> MWCyNVkxQDZzNh?=

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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
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.

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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