Tivantinib (ARQ 197)

Catalog No.S2753

Tivantinib (ARQ 197) Chemical Structure

Molecular Weight(MW): 369.42

Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.

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Cited by 5 Publications

2 Customer Reviews

  • Effect of tivantinib on the mitotic index was compared with the antimitotic drugs paclitaxel and vinblastine after overnight treatment of the HLE cell line with two different concentrations of each drug

    Clin Cancer Res, 2017, 23(15):4364-4375. Tivantinib (ARQ 197) purchased from Selleck.

    H513 cells were treated with ARQ 197, GDC-0980, NVP-BEZ235 alone and in combination for 48 h. Cell lysates were prepared and immunoblotted for total PARP, cleaved PARP, cyclin D1 and actin as a loading control.

    PLoS One, 2014, 9(9): e105919. Tivantinib (ARQ 197) purchased from Selleck.

Purity & Quality Control

Choose Selective c-Met Inhibitors

Biological Activity

Description Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.
Features The first selective c-Met inhibitor to be advanced into human clinical trials.
Targets
c-Met [1]
(Cell-free assay)
0.355 μM(Ki)
In vitro

ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549, DBTRG and NCI-H441 cells with IC50 of 0.38, 0.45, 0.29 μM. Treatment with ARQ-197 results in a decrease in phosphorylation of the MAPK signaling cascade and prevention of invasion and migration. In addition, ectopic expression of c-Met in NCI-H661, a cell line having no endogenous expression of c-Met, causes it to acquire an invasive phenotype that is also suppressed by ARQ-197. Although the addition of increasing concentrations of ARQ-197 does not significantly affect the Km of ATP, exposure of c-Met to 0.5 μM ARQ-197 decreased the Vmax of c-Met by approximately 3-fold. The ability of ARQ-197 to decrease the Vmax without affecting the Km of ATP confirmed that ARQ-197 inhibits c-Met through a non–ATP-competitive mechanism and may therefore account for its high degree of kinase selectivity. ARQ-197 prevents human recombinant c-Met with a calculated inhibitory constant Ki of approximately 355 nM. Although the highest concentration of ATP used is 200 μM, the potency of ARQ-197 against c-Met is not reduced by using concentrations of ATP up to 1 mM. ARQ-197 blocks c-Met phosphorylation and downstream c-Met signaling pathways. ARQ-197 suppresses constitutive and ligand-mediated c-Met autophosphorylation and, by extension, c-Met activity, in turn leading to the inhibition of downstream c-Met effectors. ARQ-197 induction of caspase-dependent apoptosis is increased in c-Met–expressing human cancer cells including HT29, MKN-45, and MDA-MB-231 cells.[1][2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 MoLVT4lv[XOnIHHzd4F6 MmTFglExKM7:TR?= NH61[Y1qdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz M33oXVIxPDh2MEG4
HT29 NEfBU2tMcW6jc3WgZZN{[Xl? NY\jTlV5hjFyIN88US=> MX3pcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NFTiRZkzODR6NECxPC=>
MDA-MB-231 MmXOT4lv[XOnIHHzd4F6 MV\+NVAh|ryP NFi2ZmhqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MojrNlA1QDRyMUi=
NCI-H441 NWLYO2tiU2mwYYPlJIF{e2G7 M37rO54yOCEQvF2= NIK2XndqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz M3vycFIxPDh2MEG4
SK-MEL-28 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mne5N|Mh|ryP NVrQdJVTUUN3ME6zN{DPxE1? M2fZbFIxPDh2MEG4
NCI-H661 NYrpOmI4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MknnN|Mh|ryP MnL2TWM2OD5|MzFOwG0> NXr2eG9lOjB2OESwNVg>
NCI-H446 NF\pV5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH3HU|A{OyEQvF2= MWnJR|UxRTdizszN MojsNlA1QDRyMUi=
MDA-MB-231 NEHLcIVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVqzN{DPxE1? MnHpTWM2OD1yLkW1JO69VQ>? M37rPVIxPDh2MEG4
DLD-1 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLtUHQ{OyEQvF2= MnnwTWM2OD1yLkWzJO69VQ>? MnjxNlA1QDRyMUi=
A549 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmT5N|Mh|ryP NWnjPHlFUUN3ME2wMlU6KM7:TR?= NHLsTYIzODR6NECxPC=>
SK-OV-3 NEjOVIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXtZ4ZVOzNizszN M1vLWWlEPTB;MD62OkDPxE1? NEnZOHYzODR6NECxPC=>
NCI-H460 M2\pZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUGzN{DPxE1? MmH6TWM2OD1yLk[g{txO M13vdVIxPDh2MEG4
A375 NUjLXJpvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWSzN{DPxE1? NH7kZoVKSzVyPUCuOFIh|ryP NVuzVGdoOjB2OESwNVg>
NCI-H441 NF3ETWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmfVN|Mh|ryP NHTpNY5KSzVyPUCuN{DPxE1? M{PMfFIxPDh2MEG4
HT29 M3T2VWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVfadpZVOzNizszN NXTZeIw4UUN3ME2wMlQ6KM7:TR?= M17YNlIxPDh2MEG4
MKN-45 MkHpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmTUN|Mh|ryP M{TYdmlEPTB;MD61PEDPxE1? NVnHOpJlOjB2OESwNVg>
HT29 NGfhfGVCeG:ydH;zbZMh[XO|YYm= NXXsWYNGhjFyIN88US=> MmCwd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NVvnb5B7OjB2OESwNVg>
MKN-45 MYnBdI9xfG:|aYOgZZN{[Xl? NGnZZ3F,OTBizszN M4DuS5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MlHYNlA1QDRyMUi=
MDA-MB-231 NYr1WW5nSXCxcITvd4l{KGG|c3H5 MkC5glExKM7:TR?= NXjGeYlLdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> NUT1eGN3OjB2OESwNVg>
MDA-MB-231/TGL NXHVVIpyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYnsWYszhjFyMDFOwG0> NEn0O4ZIUTVyPUGuNkDPxE1? MnjoNlIxOjd4OUC=
1833/TGL MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF;E[Wl,OTByIN88US=> NUH0NItDT0l3ME2zMlch|ryP M2D1VlIzODJ5Nkmw
EBC1 NFLQ[VdEgXSxdH;4bYPDqGG|c3H5 NF75bId,OTBizszN NFvvU5VqdmirYnn0d{B1cGViY3XscEBoem:5dHiu NUDsTVJNOjN3OUiyO|Y>
SNU638 NGDt[5FEgXSxdH;4bYPDqGG|c3H5 MX7+NVAh|ryP M4G3TIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NGfmOW0zOzV7OEK3Oi=>
A549 MXfDfZRwfG:6aXRCpIF{e2G7 MVz+NVAh|ryP NEDW[4Nvd3RiYX\m[YN1 MYKyN|U6QDJ5Nh?=
H460 M2\qXGN6fG:2b4jpZ:Kh[XO|YYm= MmPqglExKM7:TR?= NFnlbFJvd3RiYX\m[YN1 MVuyN|U6QDJ5Nh?=
HCC827 NWOyPGFFS3m2b4TvfIlkyqCjc4PhfS=> MUX+NVAh|ryP Mm\Uco91KGGoZnXjeC=> NIC0S3kzOzV7OEK3Oi=>
A549 MV\GeY5kfGmxbjDhd5NigQ>? MVOxNEDPxE1? NX7ITVN4\Gm|coXweJMhdWmlcn;0eYJ2dGV? MlPpNlM2QTh{N{[=
EBC1 M4C4TmZ2dmO2aX;uJIF{e2G7 NIPCWFAyOCEQvF2= MV;kbZNzfXC2czDtbYNzd3S3YoXs[S=> M4HI[VI{PTl6Mke2
H460 NFTnOmhHfW6ldHnvckBie3OjeR?= NXrVZ2pHOTBizszN MlrPbY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? NXe0XJFvOjV|MUOwNVA>
K562/VCR NFn0RnVEgXSxdH;4bYPDqGG|c3H5 NGe5N5h,OTBizszN MUDzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NH;iTmMzPTNzM{CxNC=>
CEM/VBL NXv6WW04S3m2b4TvfIlkyqCjc4PhfS=> M3;nTp4yOCEQvF2= NX\UcYZne2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NHHhXmQzPTNzM{CxNC=>
U266 NGP6TG1EgXSxdH;4bYPDqGG|c3H5 NXHLN2JNhjNizszNxsA> NES5flBKSzVyPUGuNUDPxE1? NH;1VZUzPThzMECxNy=>
OPM-2 MXnDfZRwfG:6aXRCpIF{e2G7 NEnwdmN,OyEQvF5CpC=> M1vK[WlEPTB;MT64JO69VQ>? MnLrNlU5OTByMUO=
MM.1S NG\TRpJEgXSxdH;4bYPDqGG|c3H5 NVfWT2dVhjNizszNxsA> M2nW[GlEPTB;MT62JO69VQ>? M3\OfVI2QDFyMEGz
MM.1R M1;QOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIH1cmo{KM7:TdMg NGn4OpNqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> NVHyVoJEOjV6MUCwNVM>
RPMI-8226 MVLDfZRwfG:6aXRCpIF{e2G7 MXr+N{DPxE4EoB?= Mor3TWM2OD1yLkmg{txO NWDnOWFyOjV6MUCwNVM>
ANBL-6 NF\NV2FEgXSxdH;4bYPDqGG|c3H5 MVSxJO69VcLi MWrpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MmTyNlU5OTByMUO=
ANLB-6/V10R NIq3cGpEgXSxdH;4bYPDqGG|c3H5 MXexJO69VcLi MknMbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NFLHR2EzPThzMECxNy=>
KAS-6/1 NIPSTWhEgXSxdH;4bYPDqGG|c3H5 Mny2NUDPxE4EoB?= M1LSbIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MViyOVgyODBzMx?=
KAS-6/V10R NUK5PFc1S3m2b4TvfIlkyqCjc4PhfS=> MVyxJO69VcLi NYraTmZ4cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MU[yOVgyODBzMx?=
KAS-6/R10R M1r2bWN6fG:2b4jpZ:Kh[XO|YYm= MnHWNUDPxE4EoB?= M{fabIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MWCyOVgyODBzMx?=
8226/S MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3\zW|Mh|ryPwrC= Mlr3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NXzsTHRoOjV6MUCwNVM>
8226/LR-5 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LU[lMh|ryPwrC= MnnSbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl MWWyOVgyODBzMx?=
Huh7 NIPzU4VEgXSxdH;4bYPDqGG|c3H5 NX\VS5MzhjRwODFOwG3DqA>? NVfTVllITE2VTx?= NH3FO4RKSzVyPUmuPUBvVQ>? Mn60NlYzPTl{NUC=
Hep3B MkO3R5l1d3SxeHnjxsBie3OjeR?= MUn+OE45KM7:TdMg NUnyNlJ7TE2VTx?= Mmm3TWM2OD12NEiuO{BvVQ>? MlHDNlYzPTl{NUC=
HepG2 NUD0[GxGS3m2b4TvfIlkyqCjc4PhfS=> NWnrW5lRhjRwODFOwG3DqA>? M4HSS2ROW09? MkjxTWM2OD1zM{muO|chdk1? NXqyUXJsOjZ{NUmyOVA>
Chang M37Z[WN6fG:2b4jpZ:Kh[XO|YYm= NWXCN4dmhjRwODFOwG3DqA>? Mmi5SG1UVw>? Mly4TWM2OD12NEiuO{BvVQ>? MX2yOlI2QTJ3MB?=
Huh7 MmroSpVv[3Srb36gZZN{[Xl? MVixMlYh|ryPwrC= MkXYSG1UVw>? NYj6TodW[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= NID0TGMzPjJ3OUK1NC=>
Hep3B M322ZmZ2dmO2aX;uJIF{e2G7 NV7OcnJ5OS54IN88UeKh NFXTcHFFVVOR MkLHZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Mkj0NlYzPTl{NUC=
HepG2 NFm3SphHfW6ldHnvckBie3OjeR?= M{\DclEvPiEQvF5CpC=> MW\EUXNQ M3j2NINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MVmyOlI2QTJ3MB?=
Chang MoroSpVv[3Srb36gZZN{[Xl? Mmj4NU43KM7:TdMg NET5SVFFVVOR NFf3ZoVk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MVGyOlI2QTJ3MB?=
MHCC97L MnLlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mne0glExKM7:TR?= MX;EUXNQ M4nUdmlEPTB;M{G1JI5O NWC1V|V2OjZ2NUi5OVM>
MHCC97H NYPTRnBPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUDZeFVqhjFyIN88US=> NYDWcI5pTE2VTx?= M4TDTWlEPTB;M{[45qCKKG6P NEPlSIQzPjR3OEm1Ny=>
Huh7 M4rXXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;YSZp,OTBizszN M{C0WmROW09? NIj6PGRKSzVyPUK2OUBvVQ>? NIrYUXgzPjR3OEm1Ny=>
HepG2 Mnj0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFnCSVB,OTBizszN MX;EUXNQ MmnTTWM2OD1|OUKgcm0> NF\ve|YzPjR3OEm1Ny=>
MHCC97L MYTGeY5kfGmxbjDhd5NigQ>? MmLXNUDPxE4EoB?= NVmyWFFHTE2VTx?= M1jnOYlv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> M{HHS|I3PDV6OUWz
Huh7 NH;iPZNHfW6ldHnvckBie3OjeR?= NYLqPVdLOSEQvF5CpC=> NWrvfFd6TE2VTx?= NFPVRmRqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MXWyOlQ2QDl3Mx?=
MHCC97L MnHkRZBweHSxc3nzJIF{e2G7 MVmxJO69VcLi MkW0SG1UVw>? NG\QV5ZqdmS3Y3XzJIFxd3C2b4Ppdy=> MmLnNlY1PTh7NUO=
Huh7 M1fyfWFxd3C2b4Ppd{Bie3OjeR?= NU\M[m9kOSEQvF5CpC=> MUPEUXNQ NFfa[VJqdmS3Y3XzJIFxd3C2b4Ppdy=> NYTq[3NLOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts NYPFRllLU2mwYYPlJIF{e2G7 M{T6[VI2KM7:TR?= NGT4VW1FVVOR Mk\TdoVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> M4HiNVIxPTN2M{S1
H23 MmPaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEDCUJkzPSEQvF2= NF6wWoxFVVOR MkTid4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MVmyNFU{PDN2NR?=
WM35 NXr0O2JLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVzPdWVIOTBizszN M3PZWGROW09? NXLxRXJ5e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> M2ixTlIxPTN2M{S1
NIH 3T3 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX;j[ldHOTBizszN M3jO[WROW09? MXrkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= NXPlTodzOjB3M{SzOFU>
H838 M4DoPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFLlWm0yOCEQvF2= MnfjSG1UVw>? M4HQbYRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NV7pVFdXOjB3M{SzOFU>
H1395 MmiwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUGxNEDPxE1? NHvjSJpFVVOR MnXP[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NGP1UIgzODV|NEO0OS=>
Quiescent S2 M4TmNWtqdmG|ZTDhd5NigQ>? MVWzNEDPxE1? M2XRTGROW09? NGHiOmhkd22ybHX0[Yx6KGGkcn;nZZRmeyCWU1GtbY5lfWOnZDDofZBmemGlZYT5cIF1cW:wIH;mJGg{UzSvZUOgbIl{fG:wZYO= M2H4NVIyPTF6OUG1
PC3 MYTBdI9xfG:|aYOgZZN{[Xl? MWiyNEDPxE1? NFzvTGJFVVOR NFToSmdqdmS3Y3XzJIFxd3C2b4Ppdy=> NVzQTpZrOjF5MEmxN|A>
Du145 MoPsRZBweHSxc3nzJIF{e2G7 MoPENlAh|ryP MofRSG1UVw>? M1rQdolv\HWlZYOgZZBweHSxc3nz MonSNlE4ODlzM{C=
LNCaP MXfBdI9xfG:|aYOgZZN{[Xl? NXW4Z5JzOjBizszN MUHEUXNQ MkfBbY5lfWOnczDhdI9xfG:|aYO= NYn2NWNOOjF5MEmxN|A>
LAPC-4 NF3mUI5CeG:ydH;zbZMh[XO|YYm= M17INlIxKM7:TR?= MmCwSG1UVw>? NH;KS3FqdmS3Y3XzJIFxd3C2b4Ppdy=> NFzQ[HczOTdyOUGzNC=>
LNCaP NXT1RWdsTnWwY4Tpc44h[XO|YYm= NUf3b5hOOjBizszN MoT5SG1UVw>? NEixbpFl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NXu5XINpOjF5MEmxN|A>
LAPC-4 M1jXVGZ2dmO2aX;uJIF{e2G7 NHuwSGwzOCEQvF2= Moe0SG1UVw>? M2\4eoRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? M3zQeVIyPzB7MUOw
Kasumi-1 NYPi[VVOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEL2fZR,PTBizszN M33SbGROW09? M{TvbIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NYTzSVdyOjN|OUC1N|Y>
SKNO-1 NEC1OGxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4L2cp42OCEQvF2= Ml7uSG1UVw>? M{j6cYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MlX5NlM{QTB3M{[=
Kasumi-1 NE\vRVlMcW6jc3WgZZN{[Xl? NFLsO|R,OTBizszN MnTqSG1UVw>? M2K2bZJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> NX7ibFlNOjN|OUC1N|Y>
SKNO-1 M4PlXmtqdmG|ZTDhd5NigQ>? MkPPglExKM7:TR?= MkDwSG1UVw>? NXu3cWNiemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NXTVS4RIOjN|OUC1N|Y>
A549 M3P1OWZ2dmO2aX;uJIF{e2G7 NXX3TY9ROTBizszN NX[zeYNbTE2VTx?= M{W0R4VvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> M1;1V|I1PzR4NUe0
NRK-52E M{LDRWZ2dmO2aX;uJIF{e2G7 MUCxNEDPxE1? NYPQ[Hh7TE2VTx?= M1;hd4lvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv M1TMeVI2ODh6MECy
PC12 M2jSWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2Hafp4yOi53IN88US=> MXHEUXNQ MXPwdoV3\W62czDUV2EucW6mdXPl[EBv\XW{aYTlJIZwem2jdHnvci=> Mn;zNlUyOjh|OE[=
HPMCs M3fBR2Z2dmO2aX;uJIF{e2G7 MXLy[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> MVuyOlA1PTd6MB?=
A549 MYXGeY5kfGmxbjDhd5NigQ>? MlnSglUxKM7:TR?= NX3S[HVKTE2VTx?= MX\h[oZm[3S|IITo[UB3cXKjbDDsbYZmKGO7Y3zlJIFv\CCqb4P0JJJme3CxboPl NGH2TFUzPjdzMUe0PC=>
RAW264.7 NWDJfXJ3TnWwY4Tpc44h[XO|YYm= NGj1SW5,OzBizszN MoLmSG1UVw>? NV;RRpduemWmdXPld{Bxem9vaX7mcIFudWG2b4L5JIdmdmViZYjwdoV{e2mxbh?= Mm\wNlY4OTh3OE[=
MEMM NXLFZot{U2mwYYPlJIF{e2G7 NHPkPGsyPSEEtV2= MYDEUXNQ MVrk[YNz\WG|ZYOgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SCKMx?= MUSyOlkzOTVyNh?=
MEMM MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlPWglIxKML3TR?= NWDaO5M4TE2VTx?= NUfwOVM6cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NWHkPVdoOjZ7MkG1NFY>
MEMM M325UWFxd3C2b4Ppd{Bie3OjeR?= M4r1[VE2KML3TR?= NG\aPXpFVVOR M4q4O4lv\HWlZYOgeIhmKHC{ZYPlcoNmKG:oIITo[UBieG:ydH;zbZMheHKxdHXpckwh[2ynYY\l[EBE[XOyYYPlMVM> NVfYV214OjZ7MkG1NFY>
T47D NFjSRpJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYqxNEDPxE1? NXi5bolETE2VTx?= MYDJR|UxRTd{IH7N NXfjeIVlOTh|OEG0OFQ>
ZR-75-1 NWC1ZldIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MY[xNEDPxE1? MnvwSG1UVw>? MnntTWM2OD15OTDuUS=> MUGxPFM5OTR2NB?=
BT474 NGrGfXhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mnf4NVAh|ryP M33qdWROW09? M1noeWlEPTB;OE[gcm0> NXLuZVFJOTh|OEG0OFQ>
HCC1954 Moj3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX7Pb25bOTBizszN NYHjOoFPTE2VTx?= NHmwWGVKSzVyPUGxPUBvVQ>? M1i5c|E5OzhzNES0
MDA-MB-453 NIrVV2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmGxNVAh|ryP NXPkSmk4TE2VTx?= MmLMTWM2OD17N{Wgcm0> NVS1ZZlkOTh|OEG0OFQ>
MDA-MB-468 NV7wc3ZIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXqxNEDPxE1? NWLse5FXTE2VTx?= NHrrbnFKSzVyPUOyNFghdk1? MXixPFM5OTR2NB?=
SkBr3 MnzSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGfqOosyOCEQvF2= MnHlSG1UVw>? MXTJR|UxRjFyLECwNEBvVQ>? MnLnNVg{QDF2NES=
MDA-MB-231 NH30Xm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnrlNVAh|ryP MWPEUXNQ Mn3aTWM2OD5zMDywNFAhdk1? M4TqdFE5OzhzNES0
HCT116 MoXKS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\kfVExKM7:TR?= NGm2cHVFVVOR NWjBV|V3UUN3ME21PFM3KG6P M3XpdFE5OzhzNES0
HT29 M3TJVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkTaNVAh|ryP NFq5WGRFVVOR MX3JR|UxRjFyLECwNEBvVQ>? MmT2NVg{QDF2NES=
HFF NEXLTo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn\sNVAh|ryP NHnqRWxFVVOR NVHjWno6UUN3ME23OlE2KG6P NGCy[pYyQDN6MUS0OC=>
HN5 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV:xNEDPxE1? MkTqSG1UVw>? NFvIVlFKSzVyPkGwMFAxOCCwTR?= MWqxPFM5OTR2NB?=
786-0 NFrCfI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1\VZ|ExKM7:TR?= NXvqdJBETE2VTx?= NFm0PVBKSzVyPUSwNFkhdk1? NETn[3IyQDN6MUS0OC=>
H157 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVOxNEDPxE1? NH;PPIZFVVOR Mm\qTWM2OD1{NkSyJI5O NVTzSpE5OTh|OEG0OFQ>
NCI-H460 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWjme4tkOTBizszN MYLEUXNQ NFnwTY1KSzVyPkKsOVAxKG6P NGDmWocyQDN6MUS0OC=>
SKOV-3 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2LmVFExKM7:TR?= NXK0XpBXTE2VTx?= M1LJSGlEPTB;MkGyOkBvVQ>? MVuxPFM5OTR2NB?=
OVCAR-3 M1PhWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUOxNEDPxE1? MX3EUXNQ NXvnVmtTUUN3ME2yPVE5KG6P NFGw[ZUyQDN6MUS0OC=>
BXPC3 NFjFcI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlfYNVAh|ryP Ml7jSG1UVw>? M13QemlEPTB;M{G0NUBvVQ>? NEjzNGwyQDN6MUS0OC=>
MiaPaCa Mom5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkDHNVAh|ryP MlfuSG1UVw>? M2XyPGlEPTB;NUSzN{BvVQ>? MkfZNVg{QDF2NES=
PANC-1 NVvQVGY1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXuxNEDPxE1? M1LleWROW09? M1XhbmlEPTB;OE[4NUBvVQ>? NUC1WZRLOTh|OEG0OFQ>
LNCaP M1fPdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYfpfm44OTBizszN MkDESG1UVw>? NXLqS5BIUUN3ME2xOFchdk1? MoHXNVg{QDF2NES=
DU145 NX3ifXVjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHXMdVIyOCEQvF2= MYDEUXNQ MYfJR|UxRTN6MUKgcm0> M4L5dlE5OzhzNES0
PC3 NHLFdXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGGyNWQyOCEQvF2= MWjEUXNQ M3HydWlEPTB-MUCsNFAxKG6P M2DFflE5OzhzNES0
BT474 MnzWT4lv[XOnIHHzd4F6 MkTZNVAh|ryP MWLEUXNQ MmW5bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTZyIH7N MoL2NVg{QDF2NES=
786-0 NFntWFVMcW6jc3WgZZN{[Xl? MkjmNVAh|ryP NEfwO4ZFVVOR M4\QfolvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> NHS3TVYyQDN6MUS0OC=>
LNCaP M4nOdmtqdmG|ZTDhd5NigQ>? NXvGVZo1OTBizszN MmrtSG1UVw>? M3rDXolvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR|IH7N MmLuNVg{QDF2NES=
PC3 MkfIT4lv[XOnIHHzd4F6 M3;3TlExKM7:TR?= NIn0S4hFVVOR MojWbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDlibl2= Mn[xNVg{QDF2NES=
KARPAS-231 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV7YWnU5OTBizszN NH;FeHhFVVOR NF7l[oRGSzVyPUSxJI5O NIGxR3UyQTB4NEezNC=>
CCRFSB NVrQSoJ{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3LyXVExKM7:TR?= MkjGSG1UVw>? NF;0e4VGSzVyPUG1OUBvVQ>? M4G2N|E6ODZ2N{Ow
SUP B15 NFPwNpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGW0WZkyOCEQvF2= M4XEUmROW09? MlnySWM2OD1zOUegcm0> MnvBNVkxPjR5M{C=
SD-1 NIHVXnlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGfVcGcyOCEQvF2= NEDOfIpFVVOR NYHxW2RCTUN3ME2zNlAhdk1? MXqxPVA3PDd|MB?=
RS4;11 MkS1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjqO3JLOTBizszN NEf4foNFVVOR MoXMSWM2OD14NUSgcm0> M4C1dFE6ODZ2N{Ow
MN-60 NXzWOXIzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYmxNEDPxE1? M2jlc2ROW09? NEn5e3FGSzVyPUO2NFIhdk1? NHnoOJoyQTB4NEezNC=>
Tanoue M3\ae2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX\TR|V[OTBizszN MXjEUXNQ MWjFR|UxRTR3MUegcm0> MVOxPVA3PDd|MB?=
RCH-ACV MmewS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWKxNEDPxE1? NXPrSZc5TE2VTx?= M3W4dmVEPTB;MUWyJI5O M4ixV|E6ODZ2N{Ow
SEM M3nSUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlT1NVAh|ryP MnLkSG1UVw>? NGP1eIJGSzVyPUKwNkBvVQ>? M2THOVE6ODZ2N{Ow
KASUMI-2 M1;pOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NETC[nYyOCEQvF2= NWTQeo8yTE2VTx?= NVTpRVc1TUN3ME2yNlUhdk1? MkL3NVkxPjR5M{C=
REH NEDzZlVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M170eFExKM7:TR?= M2exXWROW09? NWnUbFdOTUN3ME2yPFghdk1? NXT0TIQ2OTlyNkS3N|A>
697 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUWxNEDPxE1? NW\S[IM3TE2VTx?= M{nIR2VEPTB;M{O4JI5O M1faVVE6ODZ2N{Ow
NALM-6 Mnq5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX2yRYtbOTBizszN NEj2OY1FVVOR MlG0SWM2OD12MkGgcm0> NIDkZWYyQTB4NEezNC=>
MHH-CALL–3 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH\JNlEyOCEQvF2= Mn7HSG1UVw>? MWDFR|UxRThzMjDuUS=> M2PDS|E6ODZ2N{Ow
MHH-CALL–2 NULMPYRoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1PmPFExKM7:TR?= NGqxeHZFVVOR MlXXSWM2OD1{MUG0JI5O MX:xPVA3PDd|MB?=
J.GAMMA-1 M2HEO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\BXJQyOCEQvF2= MnrNSG1UVw>? MV3FR|UxRTZ3IH7N NVjhbXg6OTlyNkS3N|A>
JR45.01 MoDLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUmxNEDPxE1? NIjmZ2FFVVOR NWHESI5RTUN3ME22PEBvVQ>? NFjqd|IyQTB4NEezNC=>
A3 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3PO[FExKM7:TR?= NXPPU3FWTE2VTx?= NHXwRmpGSzVyPU[5JI5O NUfjcJVuOTlyNkS3N|A>
I 2.1 NFfWSWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETwWlEyOCEQvF2= NUOwb|ZCTE2VTx?= NWnwUHdNTUN3ME23N{BvVQ>? NYHYUINPOTlyNkS3N|A>
MOLT-3 M2HZbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGTjZWcyOCEQvF2= MWTEUXNQ NIj0NIVGSzVyPUe0JI5O MkXaNVkxPjR5M{C=
P116 MorJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2fxNFExKM7:TR?= NVrKNJR3TE2VTx?= M4fzUmVEPTB;N{igcm0> NGTZb2oyQTB4NEezNC=>
J.Cam1.6 NUXPRlFjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHraVWoyOCEQvF2= MVLEUXNQ NWG2PXdDTUN3ME23PUBvVQ>? MY[xPVA3PDd|MB?=
I 9.2 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV2xNEDPxE1? M{ewfmROW09? Mn:zSWM2OD16MDDuUS=> M1\yPVE6ODZ2N{Ow
LOUCY NHHiOWxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnXrNVAh|ryP MYXEUXNQ NH7oOGNGSzVyPUGxO{BvVQ>? NYnvTWdzOTlyNkS3N|A>
J.RT3-T3.5 Mk\SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnHLNVAh|ryP M1rqfmROW09? M2LlSGVEPTB;MUKzJI5O MXixPVA3PDd|MB?=
800000 M4jvXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmK4NVAh|ryP M2PxN2ROW09? NHfyVXVGSzVyPUG2N{BvVQ>? Ml\pNVkxPjR5M{C=
Jurkat MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHixV2syOCEQvF2= NGDjeWpFVVOR M1XUVGVEPTB;MkK1JI5O NHXhS|IyQTB4NEezNC=>
MOLT-4 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1\EcVExKM7:TR?= NH6wdJNFVVOR NU\Gc5NtTUN3ME2yN|Ihdk1? MlnJNVkxPjR5M{C=
Molt-16 NVnDWY4xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF7JXJMyOCEQvF2= NEPke4JFVVOR NYfCbVJRTUN3ME2yOFEhdk1? NY\oZZNLOTlyNkS3N|A>
CEM/C3 MoTnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnewNVAh|ryP NYPuclJRTE2VTx?= MUPFR|UxRTJ3NzDuUS=> MXmxPVA3PDd|MB?=
CEM/C2 M3TjZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXTo[oJzOTBizszN Mk\GSG1UVw>? NYX2d3FMTUN3ME2yO|Ehdk1? NHn0PFAyQTB4NEezNC=>
CCRFCEM NYXOW4xDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NU\0U5FlOTBizszN MXrEUXNQ MmjySWM2OD1|Mkegcm0> NY\Mc3ZIOTlyNkS3N|A>
CEM/C1 NYfnZZd7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFjlS3IyOCEQvF2= NH7Id2JFVVOR MXXFR|UxRTN6MjDuUS=> Mo\oNVkxPjR5M{C=
SUPTI[VB] NYO3NFB1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUHTPGxpOTBizszN MkXTSG1UVw>? NVPMTVRqTUN3ME22NVkhdk1? MlezNVkxPjR5M{C=
CCRF–HSB-2 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{TkcFExKM7:TR?= Mm\sSG1UVw>? MnPwSWM2OD1{MUG3JI5O NIT2XHAyQTB4NEezNC=>
I 2.1 NH;rXnJCeG:ydH;zbZMh[XO|YYm= MY[xNEDPxE1? NV;aboJtTE2VTx?= NHnONZhqdmS3Y3XzJIFxd3C2b4Ppdy=> MnTtNVkxPjR5M{C=
I 9.2 NF\BO3hCeG:ydH;zbZMh[XO|YYm= NILXdXEyOCEQvF2= Mo\ySG1UVw>? MXHpcoR2[2W|IHHwc5B1d3Orcx?= M3j5bVE6ODZ2N{Ow
A3 NW\xWHVnSXCxcITvd4l{KGG|c3H5 MlO2NVAh|ryP MULEUXNQ M1LyOYlv\HWlZYOgZZBweHSxc3nz M2PReVE6ODZ2N{Ow
RD Mo\JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWexNEDPxE1? NY\JXlYxUUN3ME6xNEDPxE1? Mn7DNlA4PDB4MkO=
Rh41 NGLDcYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUG3e5BJOTBizszN MUPJR|UxRTN|Lkigcm0> MYSyNFc1ODZ{Mx?=
Rh18 M4DDRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1iwZlExKM7:TR?= MnyxTWM2OD1|MEOgcm0> MlXGNlA4PDB4MkO=
Rh30 M33oVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUPWOYZNOTBizszN NWjOUI5iUUN3ME20MlgyKM7:TR?= NYPBfm1POjB5NEC2NlM>
BT-12 NYTTb3RZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYLNToVwOTBizszN MmDVTWM2OD5zMDFOwG0> MlW0NlA4PDB4MkO=
CHLA-266 NEW5fohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYexNEDPxE1? NG\jVmxKSzVyPUGuNlIh|ryP M4rPNFIxPzRyNkKz
TC-71 NWrTdYYyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHPh[3EyOCEQvF2= NW[5SmxMUUN3ME2yMlUzKM7:TR?= MVeyNFc1ODZ{Mx?=
CHLA-9 NYP0e2dkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4TESlExKM7:TR?= NWmxdpdGUUN3ME21PVEhdk1? MlGzNlA4PDB4MkO=
CHLA-10 NITKXlFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnr[HFzOTBizszN MVzJR|UxRTFyMjDuUS=> MYmyNFc1ODZ{Mx?=
CHLA-258 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXTsfIJoOTBizszN MXPJR|UxRTFwMEWg{txO MWKyNFc1ODZ{Mx?=
GBM2 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF\ONpkyOCEQvF2= MXLJR|UxRTlwMUWg{txO NF\1WlMzODd2ME[yNy=>
NB-1643 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlTTNVAh|ryP NHvmZoZKSzVyPUWuOEDPxE1? MXqyNFc1ODZ{Mx?=
NB-Ebc1 MkTtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWWydZA1OTBizszN NX32fHZ1UUN3ME6xNEDPxE1? NFP0dYUzODd2ME[yNy=>
CHLA-90 M1OyfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkL1NVAh|ryP MVvJR|UxRjFyIN88US=> M4niSVIxPzRyNkKz
CHLA-136 NInuZ|lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUSxNEDPxE1? Mn3STWM2OD5zMDFOwG0> NGHhfmkzODd2ME[yNy=>
NALM-6 NGP6V|hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NESyb2QyOCEQvF2= NYHiRoVUUUN3ME2yOlUhdk1? NYTQb4NFOjB5NEC2NlM>
COG-LL-317 M2HKSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFGxU5kyOCEQvF2= MmHPTWM2OD14LkS5JI5O MVeyNFc1ODZ{Mx?=
RS4;11 M4\aRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF;lW3IyOCEQvF2= Mn7zTWM2OD1zNEegcm0> MXiyNFc1ODZ{Mx?=
MOLT-4 NXLRXIdMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXW0cpdSOTBizszN MlLqTWM2OD12MDDuUS=> NIq4dJczODd2ME[yNy=>
CCRF-CEM M{L5SWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLyNVAh|ryP NFTz[pJKSzVyPUK2PEBvVQ>? MWGyNFc1ODZ{Mx?=
Kasumi-1 NEe1SoJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NELFc3kyOCEQvF2= M1\hdmlEPTB;MUC3JI5O Mmn5NlA4PDB4MkO=
Karpas-299 NF\USGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2fTNFExKM7:TR?= NXLESm11UUN3ME2yMlk{KM7:TR?= M1WzfFIxPzRyNkKz
Ramos-RA1 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mor2NVAh|ryP NWrzXWZyUUN3ME23MlM2KM7:TR?= MU[yNFc1ODZ{Mx?=
H1299 NFrmRmJMcW6jc3WgZZN{[Xl? NH7wWXMyOCEQvF2= MVzpcohq[mm2czDJT2JMTS2rbnT1Z4VlKEGtdDDBZ5RqfmG2aX;u NWLKb4xZOjF7MEi2NVY>

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In vivo All three xenograft models treated with ARQ-197 display reductions in tumor growth: 66% in the HT29 model, 45% in the MKN-45 model, and 79% in the MDA-MB-231 model. In these xenograft studies, no significant body weight changes following oral administration of ARQ-197 at 200 mg/kg are observed. Pharmacodynamically, the phosphorylation of c-Met in human colon xenograft tumors (HT29) is strongly inhibited by ARQ-197, as assessed by a dramatic reduction of c-Met autophosphorylation 24 hours after a single oral dose of 200 mg/kg of ARQ-197. This same dosage in mice exhibits that tumor xenografts are exposed to sustained plasma levels of ARQ-197, consistent with the observed pharmacodynamic inhibition of c-Met phosphorylation and inhibition of proliferation of c-Met harboring cancer cell lines. Plasma levels of ARQ-197 10 hours after dosing are determined to be 1.3 μM, more than 3-fold above the biochemical inhibitory constant of ARQ-197 for c-Met. Therefore, ARQ-197 is able to suppress its target in vivo in the xenografted human tumor tissue. In conclusion, ARQ-197 inhibits the growth of c-Met-dependent xenografted human tumors.[1]

Protocol

Kinase Assay:[1]
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c-Met SDS-PAGE in vitro kinase assay:

Recombinant c-Met protein (100 ng) is preincubated with increasing concentrations of ARQ-197 for 30 minutes at room temperature. Following preincubation, 100 μM of poly-Glu-Tyr substrate and various concentrations of ATP containing 5 μCi of [γ-32P]ATP are added to the reaction mixture. The reaction is incubated for 5 minutes at room temperature and then stopped by the addition of 5 μL of SDS-polyacrylamide gel, reducing sample buffer. The samples are then loaded onto a 7.5% acrylamide gel and SDS-PAGE is performed. The phosphorylated poly-Glu-Tyr substrates are ultimately visualized by autoradiography. c-Met activity is quantified by densitometry.
Cell Research:[1]
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  • Cell lines: T29, MKN-45 and MDA-MB-231 cells
  • Concentrations: 0.03-10 μM
  • Incubation Time: 24, 32, and 48 hours
  • Method: HT29, MKN-45, and MDA-MB-231 cells are seeded in black 96-well plates at 5 × 103 cells per well overnight in a medium with 10% FBS. The next day, cells are treated with increasing concentrations of ARQ-197 (0.03-10 μM) for 24, 32, and 48 hours at 37 °C. After ARQ-197 treatment, the drug-containing medium is removed and cells are incubated for at least 10 minutes in a labeling solution (10 mM HEPES, 140 mM NaCl, and 6 mM CaCl2) containing 2 μg/mL Hoescht 33342 (blue channel), 500-times diluted Annexin V-FITC (green channel), and 1 μg/mL propidium iodide (red channel). High-content image acquisition and analysis are carried out. The program is set to take four images per well. The exposure time is set at 16.7 ms/10% gain, 500 ms/35% gain, and 300 ms/30% gain for the 4,6-diamidino-2-phenylindole, FITC, and rhodamine channels, respectively. Images are processed and the numbers of positive cells for each channel and each condition are determined. In addition, HT29 cells are treated with increasing concentrations of ARQ-197 for 32 hours in the absence or the presence of 25, 50, and 100 μM ZvAD-FMK (irreversible general caspase inhibitor), and the same procedures are undertaken. All experiments are done in triplicate. To determine whether the apoptotic effect is due to c-Met inhibition, the effect of ARQ-197 when glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and c-Met are knocked down using siRNA is investigated. HT29, MKN-45, and MDA-MB-231 cells are transfected with a nontargeted control siRNA, a gapgh-targeted control siRNA, or a met-targeted siRNA. After 3 days, c-Met, GAPDH, and β-actin expression levels are determined using specific antibodies. To determine if the effect is caspase dependent, HT29, MKN-45, and MDA-MB-231 cells are transfected with a met-targeted siRNA for 2 days and incubated in the absence or the presence of increasing concentrations of ZvAD-FMK for 1 additional day. A nontargeted siRNA and a gapgh-targeted siRNA (siRNA GAPDH) are also transfected in parallel, as controls. Cells are then stained with Annexin V-FITC and propidium iodide, and the percentage of apoptotic cells is determined.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
  • Formulation: In polyethylene glycol 400/20% Vitamin E tocopheryl polyethylene glycol succinate (60:40) 30 mg/mL
  • Dosages: 200 mg/kg
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (197.6 mM)
Water Insoluble
Ethanol Insoluble

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

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02608411 Terminated Carcinoma Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02608411 Terminated Carcinoma Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3
NCT02029157 Completed Liver Cancer Kyowa Hakko Kirin Co. Ltd January 2014 Phase 3

Tech Support

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

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

  • Answer:

    S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID