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 8 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 M2HWZWtqdmG|ZTDhd5NigQ>? MoW0glExKM7:TR?= NGDqeFJqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MmDKNlA1QDRyMUi=
HT29 MnXPT4lv[XOnIHHzd4F6 M4OxdZ4yOCEQvF2= NYLkNndwcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MWOyNFQ5PDBzOB?=
MDA-MB-231 M2\ES2tqdmG|ZTDhd5NigQ>? M37qfJ4yOCEQvF2= NIL1[4pqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NWHQWox7OjB2OESwNVg>
NCI-H441 MXXLbY5ie2ViYYPzZZk> MmjEglExKM7:TR?= MlLtbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= M{X2TFIxPDh2MEG4
SK-MEL-28 M1uwZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEPMRZM{OyEQvF2= M3XRVmlEPTB-M{Og{txO M3nFOlIxPDh2MEG4
NCI-H661 NXPKNGV5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfWN|Mh|ryP NU[3coVTUUN3ME6zN{DPxE1? NX3OOFdrOjB2OESwNVg>
NCI-H446 M3GwVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXuzN{DPxE1? NIe5WJFKSzVyPUeg{txO Ml3NNlA1QDRyMUi=
MDA-MB-231 NGjQVGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYnoW2MxOzNizszN M{HBTWlEPTB;MD61OUDPxE1? NXTJflZ2OjB2OESwNVg>
DLD-1 MkCzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4P2XFM{KM7:TR?= MnT2TWM2OD1yLkWzJO69VQ>? M3;ROlIxPDh2MEG4
A549 M3LodGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXSzN{DPxE1? NHnoNodKSzVyPUCuOVkh|ryP NWHjS2U4OjB2OESwNVg>
SK-OV-3 NX7z[o5UT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIHScYs{OyEQvF2= NYrLZYp1UUN3ME2wMlY3KM7:TR?= Mom4NlA1QDRyMUi=
NCI-H460 NXz6XmtyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWX6RpJVOzNizszN Mmf3TWM2OD1yLk[g{txO M{L6TlIxPDh2MEG4
A375 MmXzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1fqT|M{KM7:TR?= M{DRfWlEPTB;MD60NkDPxE1? MljMNlA1QDRyMUi=
NCI-H441 M1mxcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVKzN{DPxE1? M2HyWGlEPTB;MD6zJO69VQ>? MmrBNlA1QDRyMUi=
HT29 NVqxOGF1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX6zN{DPxE1? M2D1U2lEPTB;MD60PUDPxE1? NVHxZmNmOjB2OESwNVg>
MKN-45 NFrPSmFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2TnXlM{KM7:TR?= MXnJR|UxRTBwNUig{txO NE\LOHMzODR6NECxPC=>
HT29 Mn65RZBweHSxc3nzJIF{e2G7 M4Lkd54yOCEQvF2= M1PRfpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MnjTNlA1QDRyMUi=
MKN-45 Mn7lRZBweHSxc3nzJIF{e2G7 MljKglExKM7:TR?= MoLSd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NXjKO3lsOjB2OESwNVg>
MDA-MB-231 MX7BdI9xfG:|aYOgZZN{[Xl? NUHFWY1XhjFyIN88US=> MXTtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw NF;6UWQzODR6NECxPC=>
MDA-MB-231/TGL M2TxV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVjXTHBthjFyMDFOwG0> M{XKVGdKPTB;MT6yJO69VQ>? MkXDNlIxOjd4OUC=
1833/TGL NHWyT|BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGLqXWV,OTByIN88US=> NUD0VnJVT0l3ME2zMlch|ryP NX\ObnQ{OjJyMke2PVA>
EBC1 NHLhNHlEgXSxdH;4bYPDqGG|c3H5 NIf6WVl,OTBizszN MkeybY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= M{LSelI{PTl6Mke2
SNU638 NI\M[pZEgXSxdH;4bYPDqGG|c3H5 NHvlOJV,OTBizszN MVTpcohq[mm2czD0bIUh[2WubDDndo94fGhw M3joUFI{PTl6Mke2
A549 NIqwWnJEgXSxdH;4bYPDqGG|c3H5 NW\jbZZlhjFyIN88US=> NH3VdmZvd3RiYX\m[YN1 Mkn0NlM2QTh{N{[=
H460 NUH5dolYS3m2b4TvfIlkyqCjc4PhfS=> NIC5[Xh,OTBizszN MV7uc5Qh[W[oZXP0 MlTrNlM2QTh{N{[=
HCC827 MlHLR5l1d3SxeHnjxsBie3OjeR?= NXT3W4VXhjFyIN88US=> NHXrZXVvd3RiYX\m[YN1 NYW5do44OjN3OUiyO|Y>
A549 NWrYU4NITnWwY4Tpc44h[XO|YYm= MoDXNVAh|ryP NH:1eIhlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? Mnf1NlM2QTh{N{[=
EBC1 NHW0OIxHfW6ldHnvckBie3OjeR?= NH3IdlAyOCEQvF2= M1exVoRqe3K3cITzJI1q[3KxdIXieYxm NG\lVZQzOzV7OEK3Oi=>
H460 MWrGeY5kfGmxbjDhd5NigQ>? MnmwNVAh|ryP MnTUbY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? NHjvb3IzPTNzM{CxNC=>
K562/VCR NWm4bm42S3m2b4TvfIlkyqCjc4PhfS=> MYH+NVAh|ryP NHfweo1{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= MWiyOVMyOzBzMB?=
CEM/VBL M2nxNGN6fG:2b4jpZ:Kh[XO|YYm= MXL+NVAh|ryP M{jkPZNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= NFLnV4czPTNzM{CxNC=>
U266 NFriPXhEgXSxdH;4bYPDqGG|c3H5 NFq0bYZ,OyEQvF5CpC=> M1XNS2lEPTB;MT6xJO69VQ>? M3rVZlI2QDFyMEGz
OPM-2 NUTKV41YS3m2b4TvfIlkyqCjc4PhfS=> NXrnPHdthjNizszNxsA> NHe2OFVKSzVyPUGuPEDPxE1? MXyyOVgyODBzMx?=
MM.1S NFfyUVFEgXSxdH;4bYPDqGG|c3H5 NHj2WZp,OyEQvF5CpC=> NXWwUZNiUUN3ME2xMlYh|ryP MX6yOVgyODBzMx?=
MM.1R MlnpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYfFUoF3OyEQvF5CpC=> M1;2RYlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> MonENlU5OTByMUO=
RPMI-8226 M1zWTWN6fG:2b4jpZ:Kh[XO|YYm= M1[2[p4{KM7:TdMg MlvCTWM2OD1yLkmg{txO NIHtNIMzPThzMECxNy=>
ANBL-6 M32ycmN6fG:2b4jpZ:Kh[XO|YYm= NFrq[IwyKM7:TdMg Mmr1bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NX\XcY9jOjV6MUCwNVM>
ANLB-6/V10R M3T6ZWN6fG:2b4jpZ:Kh[XO|YYm= Mn7GNUDPxE4EoB?= NEfnZ29qdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NH\JcmYzPThzMECxNy=>
KAS-6/1 M1yxd2N6fG:2b4jpZ:Kh[XO|YYm= NX;2[mpUOSEQvF5CpC=> MlPrbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NHHjS4szPThzMECxNy=>
KAS-6/V10R MlS0R5l1d3SxeHnjxsBie3OjeR?= NVL5Uo5FOSEQvF5CpC=> NIHuXohqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NHPkcFgzPThzMECxNy=>
KAS-6/R10R NGfyTZhEgXSxdH;4bYPDqGG|c3H5 NHjNV|kyKM7:TdMg NHq3W|BqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NYnuTI5oOjV6MUCwNVM>
8226/S M4XB[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWX3eIJ7OyEQvF5CpC=> MknVbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NU[0Om83OjV6MUCwNVM>
8226/LR-5 NIPQb2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVKzJO69VcLi NHHtNYtqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> MmrxNlU5OTByMUO=
Huh7 M1PoOmN6fG:2b4jpZ:Kh[XO|YYm= MlfwglQvQCEQvF5CpC=> NWL1N21wTE2VTx?= MXvJR|UxRTlwOTDuUS=> NX3JUlNJOjZ{NUmyOVA>
Hep3B MmDQR5l1d3SxeHnjxsBie3OjeR?= NEHxRmV,PC56IN88UeKh MVXEUXNQ M2TIUmlEPTB;NES4Mlchdk1? M{PFOVI3OjV7MkWw
HepG2 NGfDV5dEgXSxdH;4bYPDqGG|c3H5 M1jpWp41NjhizszNxsA> MXjEUXNQ NFPJV|NKSzVyPUGzPU44PyCwTR?= M{jhc|I3OjV7MkWw
Chang NGTiW2ZEgXSxdH;4bYPDqGG|c3H5 MUn+OE45KM7:TdMg M3e4emROW09? NH:zTolKSzVyPUS0PE44KG6P MWqyOlI2QTJ3MB?=
Huh7 M1\KS2Z2dmO2aX;uJIF{e2G7 MnXVNU43KM7:TdMg MlfWSG1UVw>? NIO2WXZk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NIfJSo0zPjJ3OUK1NC=>
Hep3B MlzkSpVv[3Srb36gZZN{[Xl? NYW1em05OS54IN88UeKh M2jvb2ROW09? NHTKNVRk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MkDjNlYzPTl{NUC=
HepG2 NXnwNFZKTnWwY4Tpc44h[XO|YYm= MWCxMlYh|ryPwrC= NEDFVmdFVVOR NFHFTnBk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M3fCO|I3OjV7MkWw
Chang MYXGeY5kfGmxbjDhd5NigQ>? Mnz0NU43KM7:TdMg NFi0ZY5FVVOR MU\jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NGTT[WMzPjJ3OUK1NC=>
MHCC97L NFnYc4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1PWUZ4yOCEQvF2= NI\ZSXBFVVOR MX\JR|UxRTNzNTDuUS=> M3jlSlI3PDV6OUWz
MHCC97H M{HrfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M17vS54yOCEQvF2= NWDlTW1ZTE2VTx?= MYnJR|UxRTN4OPMAjUBvVQ>? NEjvbJozPjR3OEm1Ny=>
Huh7 Mnj2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVH+NVAh|ryP NHH6dlNFVVOR NFPrTpJKSzVyPUK2OUBvVQ>? NU\sNmliOjZ2NUi5OVM>
HepG2 MnTqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlX5glExKM7:TR?= MUXEUXNQ NH23OHNKSzVyPUO5NkBvVQ>? MkLONlY1PTh7NUO=
MHCC97L NIDSU25HfW6ldHnvckBie3OjeR?= NXfSZWEyOSEQvF5CpC=> Mnu2SG1UVw>? MmjCbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NH;mZnozPjR3OEm1Ny=>
Huh7 M4XpbGZ2dmO2aX;uJIF{e2G7 MUmxJO69VcLi M4PJbmROW09? MYfpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u M4HyVlI3PDV6OUWz
MHCC97L Mn70RZBweHSxc3nzJIF{e2G7 M{LNZVEh|ryPwrC= NIHUXnhFVVOR MWTpcoR2[2W|IHHwc5B1d3Orcx?= MX6yOlQ2QDl3Mx?=
Huh7 MXvBdI9xfG:|aYOgZZN{[Xl? NEDGOZYyKM7:TdMg NWe0NY83TE2VTx?= M2fCUIlv\HWlZYOgZZBweHSxc3nz M4jRWVI3PDV6OUWz
C3H 10T1/2 mouse fibroblasts NX\RdpJoU2mwYYPlJIF{e2G7 NXfVOZNlOjVizszN NH\OUYNFVVOR NGG0NoRz\WS3Y3XzJGhqe3SxbnWgTFMh[W6mIFi0JIFk\XS7bHH0bY9vKGyndnXsd:Kh M4jiUlIxPTN2M{S1
H23 MmD2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWO4bI9[OjVizszN Ml25SG1UVw>? MoHLd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= M132fFIxPTN2M{S1
WM35 M4jDWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn3QNVAh|ryP Ml\ESG1UVw>? NXLyPGYze2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MUGyNFU{PDN2NR?=
NIH 3T3 M2nFWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHPwcWEyOCEQvF2= NHPWW5NFVVOR Ml;G[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MoTsNlA2OzR|NEW=
H838 M1LYXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4fSTVExKM7:TR?= M3WyNmROW09? M2DLe4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M1nUb|IxPTN2M{S1
H1395 M4fiZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3ObowzOTBizszN M1X4cmROW09? NH7n[YNld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> M3S4SlIxPTN2M{S1
Quiescent S2 MYPLbY5ie2ViYYPzZZk> NVLCTmlLOzBizszN NXOwdmRVTE2VTx?= NYPTRmRN[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz MUSyNVUyQDlzNR?=
PC3 NGWzXIFCeG:ydH;zbZMh[XO|YYm= M4e3UFIxKM7:TR?= M4W0dmROW09? MYPpcoR2[2W|IHHwc5B1d3Orcx?= NXu4e2hUOjF5MEmxN|A>
Du145 M4PkN2Fxd3C2b4Ppd{Bie3OjeR?= MUeyNEDPxE1? NH6zeHBFVVOR MnHubY5lfWOnczDhdI9xfG:|aYO= MlTJNlE4ODlzM{C=
LNCaP MnXtRZBweHSxc3nzJIF{e2G7 NWS0VJR6OjBizszN NF\rcWxFVVOR MVzpcoR2[2W|IHHwc5B1d3Orcx?= M1rKb|IyPzB7MUOw
LAPC-4 M1;xPWFxd3C2b4Ppd{Bie3OjeR?= MojxNlAh|ryP NYfMeZpCTE2VTx?= MVXpcoR2[2W|IHHwc5B1d3Orcx?= NHHVbnozOTdyOUGzNC=>
LNCaP MmnuSpVv[3Srb36gZZN{[Xl? MUGyNEDPxE1? M1\VcmROW09? MV7k[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ M{noW|IyPzB7MUOw
LAPC-4 MXrGeY5kfGmxbjDhd5NigQ>? NVjMZ2lKOjBizszN NEHuNW1FVVOR MlLk[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? Mnn6NlE4ODlzM{C=
Kasumi-1 NHjiWFRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M160c542OCEQvF2= NHyyPYxFVVOR NWOzZoREcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHXIWmgzOzN7MEWzOi=>
SKNO-1 MkO3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4nmNp42OCEQvF2= MWjEUXNQ NYDnO4xJcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4LMXVI{OzlyNUO2
Kasumi-1 M1fVTmtqdmG|ZTDhd5NigQ>? NV3K[Jo6hjFyIN88US=> M33ZU2ROW09? MVTy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= MXmyN|M6ODV|Nh?=
SKNO-1 NG[z[HFMcW6jc3WgZZN{[Xl? MmHVglExKM7:TR?= NGLsUVRFVVOR MXjy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= MUGyN|M6ODV|Nh?=
A549 MWDGeY5kfGmxbjDhd5NigQ>? MWGxNEDPxE1? MkTySG1UVw>? NF;3WWNmdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm MX2yOFc1PjV5NB?=
NRK-52E M16wWGZ2dmO2aX;uJIF{e2G7 Mm\yNVAh|ryP M2fuPWROW09? NV:0OYRncW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgV3RCXDNiboXjcIVieiC2cnHud4xw[2G2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCWR1[t{tIyNCClb3zsZYdmdiCLVjDhcoQh\mmkcn;u[YN1cW5? NIjQZm8zPTB6OECwNi=>
PC12 NWXBT5RwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmH6glEzNjVizszN NH25[mxFVVOR MnrldJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> NV7tSYZPOjVzMkizPFY>
HPMCs M1K3N2Z2dmO2aX;uJIF{e2G7 MkexdoV3\XK|ZYOg[ZBqfGinbHnhcEB1dyCvZYPlcoNpgW2jbDD0doFve2m2aX;uJI9nKGi3bXHuJJBmemm2b37lZYwhdWW|b4To[Yxq[WxiY3XscJM> MkHXNlYxPDV5OEC=
A549 M33ScmZ2dmO2aX;uJIF{e2G7 MW\+OVAh|ryP MVPEUXNQ NIDvdlFi\m[nY4TzJJRp\SC4aYLhcEBtcW[nIHP5Z4xmKGGwZDDoc5N1KHKnc4DvcpNm NUDzT3NlOjZ5MUG3OFg>
RAW264.7 NGPLOmxHfW6ldHnvckBie3OjeR?= Mly4glMxKM7:TR?= M{Xoe2ROW09? MYHy[YR2[2W|IIDyc{1qdm[uYX3tZZRwenliZ3Xu[UBmgHC{ZYPzbY9v M3nHOFI3PzF6NUi2
MEMM MWrLbY5ie2ViYYPzZZk> MWKxOUDDvU1? MlzzSG1UVw>? NYLDV3BG\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> NGLSbpQzPjl{MUWwOi=>
MEMM M4m1dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2f6WJ4zOCEEtV2= M2\QS2ROW09? MnWwbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MX6yOlkzOTVyNh?=
MEMM MVvBdI9xfG:|aYOgZZN{[Xl? M{K5N|E2KML3TR?= NIflPFRFVVOR NW\XbYJVcW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? NXfVfpF2OjZ7MkG1NFY>
T47D MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3vYW|ExKM7:TR?= M1\tVmROW09? M1TaZ2lEPTB;N{Kgcm0> NWq0Wll5OTh|OEG0OFQ>
ZR-75-1 M1O1XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGD4WmIyOCEQvF2= M4XUU2ROW09? MXvJR|UxRTd7IH7N NXfpWpA2OTh|OEG0OFQ>
BT474 M2PrfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4\TbFExKM7:TR?= NYDF[o9ZTE2VTx?= MX\JR|UxRTh4IH7N NV;5UIp{OTh|OEG0OFQ>
HCC1954 NX61Vm55T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXn4WmhkOTBizszN NISycIJFVVOR NEXa[XBKSzVyPUGxPUBvVQ>? NFvV[5UyQDN6MUS0OC=>
MDA-MB-453 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn;2NVAh|ryP NH;0T2dFVVOR NFrldI1KSzVyPUm3OUBvVQ>? MnXGNVg{QDF2NES=
MDA-MB-468 M{LMNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2XwV|ExKM7:TR?= MnzuSG1UVw>? MnXDTWM2OD1|MkC4JI5O NGm3O|UyQDN6MUS0OC=>
SkBr3 NE\2dJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4LmTVExKM7:TR?= MkDnSG1UVw>? M1HOVGlEPTB-MUCsNFAxKG6P Mo[0NVg{QDF2NES=
MDA-MB-231 NX[yWHM{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEXzTZEyOCEQvF2= M{DHTmROW09? MlLuTWM2OD5zMDywNFAhdk1? MlfvNVg{QDF2NES=
HCT116 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXP5eJNbOTBizszN NXXuOItETE2VTx?= MY\JR|UxRTV6M{[gcm0> NIDkPFkyQDN6MUS0OC=>
HT29 Mn;MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFTxWHYyOCEQvF2= MVXEUXNQ M3zYcWlEPTB-MUCsNFAxKG6P M1vTOlE5OzhzNES0
HFF NH6wZ25Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NULPdXhkOTBizszN MVTEUXNQ M4XEcmlEPTB;N{[xOUBvVQ>? M3vCZlE5OzhzNES0
HN5 M3jKVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVmxNEDPxE1? M{LlZmROW09? MYPJR|UxRjFyLECwNEBvVQ>? M{HuVVE5OzhzNES0
786-0 NH7YU4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUfpR5M3OTBizszN M{fMOGROW09? NXXwXJZJUUN3ME20NFA6KG6P M365SFE5OzhzNES0
H157 NHvQR4VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3zIe|ExKM7:TR?= M1zMZ2ROW09? NVHifmZUUUN3ME2yOlQzKG6P NH;pW5MyQDN6MUS0OC=>
NCI-H460 NWHFWoI5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW[xNEDPxE1? MXnEUXNQ Mk\NTWM2OD5{LEWwNEBvVQ>? M2rl[FE5OzhzNES0
SKOV-3 NWjjRVZST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4n6OFExKM7:TR?= NH3kTotFVVOR NEezVnFKSzVyPUKxNlYhdk1? MWqxPFM5OTR2NB?=
OVCAR-3 NInjfW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVuxNEDPxE1? M1P5emROW09? M1LjOmlEPTB;MkmxPEBvVQ>? NFixSXYyQDN6MUS0OC=>
BXPC3 M{jnfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2LHOVExKM7:TR?= M{DFdmROW09? NEHWO5JKSzVyPUOxOFEhdk1? MXexPFM5OTR2NB?=
MiaPaCa MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWexNEDPxE1? NFHpTplFVVOR M1LuOGlEPTB;NUSzN{BvVQ>? Mnu4NVg{QDF2NES=
PANC-1 NWDsdYxNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYmxNEDPxE1? MYjEUXNQ MVLJR|UxRTh4OEGgcm0> MWmxPFM5OTR2NB?=
LNCaP NInqfm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn:4NVAh|ryP NUnIZ21UTE2VTx?= NXrOcllQUUN3ME2xOFchdk1? MYKxPFM5OTR2NB?=
DU145 M2j1WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3L3ZlExKM7:TR?= Mli2SG1UVw>? MnzuTWM2OD1|OEGyJI5O M{TF[FE5OzhzNES0
PC3 M3TBXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmPjNVAh|ryP MWnEUXNQ NVTr[25SUUN3ME6xNEwxODBibl2= M2TjbFE5OzhzNES0
BT474 MXTLbY5ie2ViYYPzZZk> MmnGNVAh|ryP NGKxU|lFVVOR MWnpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kAyPjBibl2= NHPaXIsyQDN6MUS0OC=>
786-0 MnHYT4lv[XOnIHHzd4F6 M{L0UFExKM7:TR?= MonRSG1UVw>? MVrpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kAyPTBibl2= MV[xPFM5OTR2NB?=
LNCaP M4S2UmtqdmG|ZTDhd5NigQ>? NY[4ZnBGOTBizszN M4XxcWROW09? MmTObY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDNibl2= NWnpOWJROTh|OEG0OFQ>
PC3 M{HQemtqdmG|ZTDhd5NigQ>? M1Lh[FExKM7:TR?= MX\EUXNQ NV23OmRucW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEmgcm0> MXexPFM5OTR2NB?=
KARPAS-231 NYDrTlRpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH7re2IyOCEQvF2= NHTseo1FVVOR NUn2UZNSTUN3ME20NUBvVQ>? NYHYWXo6OTlyNkS3N|A>
CCRFSB MmXNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{XXT|ExKM7:TR?= NXTBepI5TE2VTx?= NFTBZlNGSzVyPUG1OUBvVQ>? M2\jdlE6ODZ2N{Ow
SUP B15 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPPZmwyOCEQvF2= MUfEUXNQ MVXFR|UxRTF7NzDuUS=> NGjMSocyQTB4NEezNC=>
SD-1 NYnye3FZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HTd|ExKM7:TR?= NIHVfIpFVVOR Mk\ySWM2OD1|MkCgcm0> NWnxVnhuOTlyNkS3N|A>
RS4;11 NGjiWGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mmj6NVAh|ryP NFzzcHlFVVOR M4P5SmVEPTB;NkW0JI5O MUexPVA3PDd|MB?=
MN-60 MlrzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4j1elExKM7:TR?= NGm2XW9FVVOR M{L6cGVEPTB;M{[wNkBvVQ>? MU[xPVA3PDd|MB?=
Tanoue M{[wVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1L2bVExKM7:TR?= MX3EUXNQ MkjvSWM2OD12NUG3JI5O MorLNVkxPjR5M{C=
RCH-ACV MkLkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1i5ZVExKM7:TR?= MXjEUXNQ NH3VUYNGSzVyPUG1NkBvVQ>? NGqzXlYyQTB4NEezNC=>
SEM M3jVe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX6xNEDPxE1? MWjEUXNQ NVTQOJpyTUN3ME2yNFIhdk1? NFfERZUyQTB4NEezNC=>
KASUMI-2 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlzZNVAh|ryP MoD3SG1UVw>? NGLBdW5GSzVyPUKyOUBvVQ>? NXXNcJZ{OTlyNkS3N|A>
REH M2jBUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUHuWlROOTBizszN MX\EUXNQ MYnFR|UxRTJ6ODDuUS=> NVLWblFGOTlyNkS3N|A>
697 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVyxNEDPxE1? MoHrSG1UVw>? M4XDNGVEPTB;M{O4JI5O Moj5NVkxPjR5M{C=
NALM-6 NEDKOo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rvVlExKM7:TR?= MWLEUXNQ MoO4SWM2OD12MkGgcm0> NUnQcWxJOTlyNkS3N|A>
MHH-CALL–3 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2PpblExKM7:TR?= MorBSG1UVw>? MVLFR|UxRThzMjDuUS=> MofaNVkxPjR5M{C=
MHH-CALL–2 M1LPV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEDyVowyOCEQvF2= M3;KZWROW09? MYPFR|UxRTJzMUSgcm0> NVvHR2VwOTlyNkS3N|A>
J.GAMMA-1 Mkm2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MonkNVAh|ryP NFm2PGpFVVOR MXTFR|UxRTZ3IH7N M4HUc|E6ODZ2N{Ow
JR45.01 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXWxNEDPxE1? MmrZSG1UVw>? NFLI[ZdGSzVyPU[4JI5O MkHENVkxPjR5M{C=
A3 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLJTJc4OTBizszN MmnaSG1UVw>? MYfFR|UxRTZ7IH7N MXmxPVA3PDd|MB?=
I 2.1 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV[xNEDPxE1? MoDHSG1UVw>? NXqzN|dFTUN3ME23N{BvVQ>? NIXu[o0yQTB4NEezNC=>
MOLT-3 M2PDdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGfG[3gyOCEQvF2= M33rbGROW09? M3PNfGVEPTB;N{Sgcm0> Mn;pNVkxPjR5M{C=
P116 M2[xV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUSxNEDPxE1? NIf3fllFVVOR M2DHOmVEPTB;N{igcm0> M3S0SFE6ODZ2N{Ow
J.Cam1.6 NH7HO41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGnRcnYyOCEQvF2= M{HwOWROW09? MoDUSWM2OD15OTDuUS=> M1XwT|E6ODZ2N{Ow
I 9.2 MkPES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVOxNEDPxE1? MX;EUXNQ NIL0UFRGSzVyPUiwJI5O MnrYNVkxPjR5M{C=
LOUCY NUezN3ZjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NULZXmdQOTBizszN MnjzSG1UVw>? NF\icWNGSzVyPUGxO{BvVQ>? MmjzNVkxPjR5M{C=
J.RT3-T3.5 MkX5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3z1PVExKM7:TR?= M3TQcWROW09? MYHFR|UxRTF{MzDuUS=> NYr6fJVsOTlyNkS3N|A>
800000 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHoW|J2OTBizszN NXnPeVdVTE2VTx?= MV;FR|UxRTF4MzDuUS=> NX\Q[Xl[OTlyNkS3N|A>
Jurkat M2LldGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYixNEDPxE1? MnTmSG1UVw>? M1HMcGVEPTB;MkK1JI5O NI\odI8yQTB4NEezNC=>
MOLT-4 MlrJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIfmXm0yOCEQvF2= MYLEUXNQ MV3FR|UxRTJ|MjDuUS=> MW[xPVA3PDd|MB?=
Molt-16 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYDTRVIxOTBizszN M2D4V2ROW09? MmrLSWM2OD1{NEGgcm0> Mle4NVkxPjR5M{C=
CEM/C3 M1;u[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{XOPFExKM7:TR?= MoHDSG1UVw>? NH\ieXZGSzVyPUK1O{BvVQ>? NVvBSXQ3OTlyNkS3N|A>
CEM/C2 M1HmXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1jrVFExKM7:TR?= NVPxe3RUTE2VTx?= MmW3SWM2OD1{N{Ggcm0> MUKxPVA3PDd|MB?=
CCRFCEM M3HhbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1v3Z|ExKM7:TR?= MVrEUXNQ NYTFW5BVTUN3ME2zNlchdk1? M{XXW|E6ODZ2N{Ow
CEM/C1 M3rZN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXq2T|g4OTBizszN MmLySG1UVw>? M1r5VGVEPTB;M{iyJI5O NYTDVW97OTlyNkS3N|A>
SUPTI[VB] M3rTZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWexNEDPxE1? NY\K[HpNTE2VTx?= Ml\ISWM2OD14MUmgcm0> M4e3Z|E6ODZ2N{Ow
CCRF–HSB-2 M3vyNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXP4Smp[OTBizszN NITXS5dFVVOR M3zZW2VEPTB;MkGxO{BvVQ>? NWTwT4VEOTlyNkS3N|A>
I 2.1 MYrBdI9xfG:|aYOgZZN{[Xl? M3LYcFExKM7:TR?= NWnjTmxbTE2VTx?= M4fNN4lv\HWlZYOgZZBweHSxc3nz MlfDNVkxPjR5M{C=
I 9.2 Mn7iRZBweHSxc3nzJIF{e2G7 Mnf1NVAh|ryP MYDEUXNQ NGTzR3RqdmS3Y3XzJIFxd3C2b4Ppdy=> M1PjUlE6ODZ2N{Ow
A3 Mo\oRZBweHSxc3nzJIF{e2G7 Mo\jNVAh|ryP NYju[mJCTE2VTx?= MkjHbY5lfWOnczDhdI9xfG:|aYO= MYexPVA3PDd|MB?=
RD NEnX[WlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnXvNVAh|ryP M1Tx[2lEPTB-MUCg{txO M3;3NlIxPzRyNkKz
Rh41 MmH6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYWxNEDPxE1? MWjJR|UxRTN|Lkigcm0> MknRNlA4PDB4MkO=
Rh18 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{LXfVExKM7:TR?= M3\KVGlEPTB;M{CzJI5O NEXoTlkzODd2ME[yNy=>
Rh30 NYnYTW9YT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVXQbGc5OTBizszN NWXVO4JJUUN3ME20MlgyKM7:TR?= MWOyNFc1ODZ{Mx?=
BT-12 M{LlV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWWxNEDPxE1? Mom2TWM2OD5zMDFOwG0> NXvKO5IyOjB5NEC2NlM>
CHLA-266 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1PlV|ExKM7:TR?= MUjJR|UxRTFwMkKg{txO MknxNlA4PDB4MkO=
TC-71 Mlj1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXfQXGkzOTBizszN MV;JR|UxRTJwNUKg{txO MVqyNFc1ODZ{Mx?=
CHLA-9 NVXmd3I2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2XXUlExKM7:TR?= Mki1TWM2OD13OUGgcm0> NEHJTm0zODd2ME[yNy=>
CHLA-10 NES5O2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF;xZoUyOCEQvF2= MXfJR|UxRTFyMjDuUS=> M2XnfVIxPzRyNkKz
CHLA-258 NEO3RlhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVWxNEDPxE1? NGDRPJNKSzVyPUGuNFUh|ryP MkLPNlA4PDB4MkO=
GBM2 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF2wZnAyOCEQvF2= NUfIOYZ4UUN3ME25MlE2KM7:TR?= NHm5N3MzODd2ME[yNy=>
NB-1643 M2\YdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFTONJoyOCEQvF2= NFPPdG5KSzVyPUWuOEDPxE1? NFHL[XMzODd2ME[yNy=>
NB-Ebc1 NIT5RYpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHrTS4cyOCEQvF2= MkjsTWM2OD5zMDFOwG0> NY[2UpFbOjB5NEC2NlM>
CHLA-90 NHToVGxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYOxNEDPxE1? NEPZU4tKSzVyPkGwJO69VQ>? NF7ZcnkzODd2ME[yNy=>
CHLA-136 NEfXPYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVj0Wok1OTBizszN MV\JR|UxRjFyIN88US=> MnHLNlA4PDB4MkO=
NALM-6 MnnQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVexNEDPxE1? MXrJR|UxRTJ4NTDuUS=> M2jRVVIxPzRyNkKz
COG-LL-317 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1W3T|ExKM7:TR?= MXfJR|UxRTZwNEmgcm0> NHvMPZIzODd2ME[yNy=>
RS4;11 NIPiXHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFXrb48yOCEQvF2= MUHJR|UxRTF2NzDuUS=> NX\XXnk{OjB5NEC2NlM>
MOLT-4 NIXKN4lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoHCNVAh|ryP MnT4TWM2OD12MDDuUS=> NHX4XYEzODd2ME[yNy=>
CCRF-CEM NGnKZpFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXvwSHd5OTBizszN NYLXSlA1UUN3ME2yOlghdk1? NV;wVYdCOjB5NEC2NlM>
Kasumi-1 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFe2NXIyOCEQvF2= M12xOmlEPTB;MUC3JI5O NWLlN5h4OjB5NEC2NlM>
Karpas-299 NYmzbotxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHPkelEyOCEQvF2= NYrrWoE3UUN3ME2yMlk{KM7:TR?= NGrZUGczODd2ME[yNy=>
Ramos-RA1 M4jsU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NELQOXAyOCEQvF2= M3fqT2lEPTB;Nz6zOUDPxE1? M17G[VIxPzRyNkKz
H1299 MV;LbY5ie2ViYYPzZZk> MlPQNVAh|ryP NH3ZN45qdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v Mn3jNlE6ODh4MU[=

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Assay
Methods Test Index PMID
Western blot
cMET / p-cMET / p-AKT / p-ERK / p-rpS6 ; 

PubMed: 23022995     


A498 and 769P cell lines were treated with increasing concentrations of ARQ 197 for 24 h. Total c-Met expression remained relatively stable with drug treatment. Phosphorylated c-Met expression was highest in control (untreated cells) and was blocked with increasing concentrations of ARQ 197. Downstream changes in the c-Met pathway were seen predominantly in phosphorylated AKT, while decreased phosphorylated ERK1/2 and phosphorylated rpS6 (P70S6Kinase) occurred at higher c-Met inhibitor concentrations.

23022995
Growth inhibition assay
Cell viability; 

PubMed: 23598276     


Cells were treated with the increasing concentrations of tivantinib for 72 hr. Viable cells were assessed by CellTiter-Glo assay and were graphed relative to untreated cells. Experiments were carried out in sextuplet. The average values and SDs are shown. 

23598276
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

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02150733 Completed Drug: Tivantinib Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT01892527 Unknown status Drug: Tivantinib (ARQ197) Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Unknown status Drug: Tivantinib Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2

Tech Support

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

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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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