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 NF3PbXVMcW6jc3WgZZN{[Xl? M1PYfp4yOCEQvF2= NHnwTVBqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MmHNNlA1QDRyMUi=
HT29 Ml\0T4lv[XOnIHHzd4F6 MX7+NVAh|ryP NESwcVlqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MlnTNlA1QDRyMUi=
MDA-MB-231 MkHzT4lv[XOnIHHzd4F6 MYX+NVAh|ryP M1PBcolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MojLNlA1QDRyMUi=
NCI-H441 NUG4S482U2mwYYPlJIF{e2G7 MnPjglExKM7:TR?= Ml\UbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NEXBN4IzODR6NECxPC=>
SK-MEL-28 NEO0XJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnfKN|Mh|ryP NXvONoJRUUN3ME6zN{DPxE1? NGnId2ozODR6NECxPC=>
NCI-H661 M1nVPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYfKUGJ3OzNizszN MYXJR|UxRjN|IN88US=> NWi2eHVtOjB2OESwNVg>
NCI-H446 NIH2PFVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4j4O|M{KM7:TR?= MYfJR|UxRTdizszN M3:3SFIxPDh2MEG4
MDA-MB-231 NYDTNZFzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYOzN{DPxE1? NIrDcXZKSzVyPUCuOVUh|ryP M{nsOFIxPDh2MEG4
DLD-1 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXGzN{DPxE1? NH3yTY5KSzVyPUCuOVMh|ryP MUmyNFQ5PDBzOB?=
A549 NIDjepdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXtVFJmOzNizszN MVTJR|UxRTBwNUmg{txO NYPuPVhEOjB2OESwNVg>
SK-OV-3 MnTGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NULSW3NvOzNizszN Mom1TWM2OD1yLk[2JO69VQ>? MoTnNlA1QDRyMUi=
NCI-H460 NYfDUWtCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmT2N|Mh|ryP NEHnV5dKSzVyPUCuOkDPxE1? MVuyNFQ5PDBzOB?=
A375 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlTFN|Mh|ryP MkixTWM2OD1yLkSyJO69VQ>? MWeyNFQ5PDBzOB?=
NCI-H441 M{i0XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2fRRlM{KM7:TR?= NF3PVJFKSzVyPUCuN{DPxE1? NXH4U5JZOjB2OESwNVg>
HT29 M2TYO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{jXU|M{KM7:TR?= NVfGTXlKUUN3ME2wMlQ6KM7:TR?= Mk\sNlA1QDRyMUi=
MKN-45 M2HPWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVKzN{DPxE1? NYDoWY14UUN3ME2wMlU5KM7:TR?= MWiyNFQ5PDBzOB?=
HT29 M1zzOGFxd3C2b4Ppd{Bie3OjeR?= M3nHPJ4yOCEQvF2= MUXzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NXvlemJGOjB2OESwNVg>
MKN-45 M1f2VmFxd3C2b4Ppd{Bie3OjeR?= MWH+NVAh|ryP MWLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? MW[yNFQ5PDBzOB?=
MDA-MB-231 M1r4U2Fxd3C2b4Ppd{Bie3OjeR?= NGmw[4d,OTBizszN MX;tc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw NVjwd5VGOjB2OESwNVg>
MDA-MB-231/TGL M130T2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4G0XJ4yODBizszN M2T6SmdKPTB;MT6yJO69VQ>? M1P5bVIzODJ5Nkmw
1833/TGL NFe2T4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlT5glExOCEQvF2= M3LDb2dKPTB;Mz63JO69VQ>? NWLi[Zc3OjJyMke2PVA>
EBC1 M{XmfWN6fG:2b4jpZ:Kh[XO|YYm= NEnDb4Z,OTBizszN NY\pSJRXcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> NGmzRpEzOzV7OEK3Oi=>
SNU638 MYfDfZRwfG:6aXRCpIF{e2G7 Mnu1glExKM7:TR?= M1e2bIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NF72foczOzV7OEK3Oi=>
A549 MX;DfZRwfG:6aXRCpIF{e2G7 Mn:yglExKM7:TR?= M1XKTY5wfCCjZn\lZ5Q> NWDW[odrOjN3OUiyO|Y>
H460 M2faWGN6fG:2b4jpZ:Kh[XO|YYm= MVX+NVAh|ryP MYDuc5Qh[W[oZXP0 NWn5ZpY5OjN3OUiyO|Y>
HCC827 NXnzPWNuS3m2b4TvfIlkyqCjc4PhfS=> MoXmglExKM7:TR?= MoLDco91KGGoZnXjeC=> NFywNpMzOzV7OEK3Oi=>
A549 NX7YTWdjTnWwY4Tpc44h[XO|YYm= MmrqNVAh|ryP NGGxOZllcXO{dYD0d{BucWO{b4T1ZpVt\Q>? NIjEPGgzOzV7OEK3Oi=>
EBC1 NFOxcIhHfW6ldHnvckBie3OjeR?= Mlr1NVAh|ryP NXzjOml[\Gm|coXweJMhdWmlcn;0eYJ2dGV? MWOyN|U6QDJ5Nh?=
H460 M1\XemZ2dmO2aX;uJIF{e2G7 M2\XdFExKM7:TR?= NGfTeHVqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w NI[xbI8zPTNzM{CxNC=>
K562/VCR MmTQR5l1d3SxeHnjxsBie3OjeR?= NULZfG5MhjFyIN88US=> MWPzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MUCyOVMyOzBzMB?=
CEM/VBL MVHDfZRwfG:6aXRCpIF{e2G7 NHnRT|J,OTBizszN NX\tVVBNe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 M2PSSVI2OzF|MEGw
U266 MUDDfZRwfG:6aXRCpIF{e2G7 NHvSRYl,OyEQvF5CpC=> M3\HN2lEPTB;MT6xJO69VQ>? M2rGSVI2QDFyMEGz
OPM-2 MVLDfZRwfG:6aXRCpIF{e2G7 M3v5NJ4{KM7:TdMg NID3VHZKSzVyPUGuPEDPxE1? MkDnNlU5OTByMUO=
MM.1S M4HJdGN6fG:2b4jpZ:Kh[XO|YYm= M2q5bZ4{KM7:TdMg MnjvTWM2OD1zLk[g{txO M17HfFI2QDFyMEGz
MM.1R NIO3UlhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{TIWFMh|ryPwrC= NYnFSVdGcW6qaXLpeJMh[2WubDDndo94fGhiYomgOFkm MXyyOVgyODBzMx?=
RPMI-8226 NYTmS3RMS3m2b4TvfIlkyqCjc4PhfS=> Mo\1glMh|ryPwrC= MYPJR|UxRTBwOTFOwG0> M4ezc|I2QDFyMEGz
ANBL-6 NFXuVVNEgXSxdH;4bYPDqGG|c3H5 NGrNTHMyKM7:TdMg M{jOVYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NYLzc5h4OjV6MUCwNVM>
ANLB-6/V10R MlnwR5l1d3SxeHnjxsBie3OjeR?= NV31VFZpOSEQvF5CpC=> MUXpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NFHqeGQzPThzMECxNy=>
KAS-6/1 NEXIbnpEgXSxdH;4bYPDqGG|c3H5 NX3RPFhCOSEQvF5CpC=> M4TENYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M2nkN|I2QDFyMEGz
KAS-6/V10R Mn7JR5l1d3SxeHnjxsBie3OjeR?= NGX0dVAyKM7:TdMg Mo\EbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NYnZPYJiOjV6MUCwNVM>
KAS-6/R10R NVfofG4xS3m2b4TvfIlkyqCjc4PhfS=> MnXuNUDPxE4EoB?= M2fJcolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MU[yOVgyODBzMx?=
8226/S NEjU[nlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3LxOFMh|ryPwrC= MmjFbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl MY[yOVgyODBzMx?=
8226/LR-5 MmHLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MonIN{DPxE4EoB?= NXHtOYlLcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm M4f4NFI2QDFyMEGz
Huh7 MWXDfZRwfG:6aXRCpIF{e2G7 NEXzZlZ,PC56IN88UeKh M13zV2ROW09? M1f4O2lEPTB;OT65JI5O MYGyOlI2QTJ3MB?=
Hep3B NXe2eZZPS3m2b4TvfIlkyqCjc4PhfS=> MlTtglQvQCEQvF5CpC=> M2r6eWROW09? MWTJR|UxRTR2OD63JI5O NULae4h7OjZ{NUmyOVA>
HepG2 NYnlN3I2S3m2b4TvfIlkyqCjc4PhfS=> M2Cw[541NjhizszNxsA> NVP3VZpQTE2VTx?= MY\JR|UxRTF|OT63O{BvVQ>? MkHjNlYzPTl{NUC=
Chang MVjDfZRwfG:6aXRCpIF{e2G7 NYnQUmNuhjRwODFOwG3DqA>? MmfTSG1UVw>? Mo\TTWM2OD12NEiuO{BvVQ>? MWGyOlI2QTJ3MB?=
Huh7 NX7vVoRZTnWwY4Tpc44h[XO|YYm= MXKxMlYh|ryPwrC= NVq5dIJwTE2VTx?= NIfnRY5k[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MlrHNlYzPTl{NUC=
Hep3B NYLidHBkTnWwY4Tpc44h[XO|YYm= M1TudlEvPiEQvF5CpC=> MW\EUXNQ Mlz2Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M1q5NFI3OjV7MkWw
HepG2 Mn3BSpVv[3Srb36gZZN{[Xl? NYrLTXdpOS54IN88UeKh NXv2OJp{TE2VTx?= MVPjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MlT3NlYzPTl{NUC=
Chang NIHOdotHfW6ldHnvckBie3OjeR?= MljKNU43KM7:TdMg NWjr[FFETE2VTx?= Mle2Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MYWyOlI2QTJ3MB?=
MHCC97L M2njcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTHb45RhjFyIN88US=> MlTiSG1UVw>? M3[5W2lEPTB;M{G1JI5O MX[yOlQ2QDl3Mx?=
MHCC97H M{PaZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1jaVp4yOCEQvF2= M1q3VWROW09? MoPtTWM2OD1|NklihKkhdk1? NGi2ZnIzPjR3OEm1Ny=>
Huh7 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGrD[nV,OTBizszN Mn7TSG1UVw>? MXvJR|UxRTJ4NTDuUS=> NVPq[Jg1OjZ2NUi5OVM>
HepG2 NWLoSmZkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmW3glExKM7:TR?= NUW0R3F2TE2VTx?= NEn2So5KSzVyPUO5NkBvVQ>? M{OwXVI3PDV6OUWz
MHCC97L M17JfGZ2dmO2aX;uJIF{e2G7 MUSxJO69VcLi NFSzV5JFVVOR M4rZ[Ilv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> M3izPVI3PDV6OUWz
Huh7 NWnDPYYzTnWwY4Tpc44h[XO|YYm= MlezNUDPxE4EoB?= NVf1cWlyTE2VTx?= MnfobY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NHXqRXQzPjR3OEm1Ny=>
MHCC97L NIDnUZVCeG:ydH;zbZMh[XO|YYm= M3W3PFEh|ryPwrC= M{\YU2ROW09? NHzrUlBqdmS3Y3XzJIFxd3C2b4Ppdy=> NHv4bGIzPjR3OEm1Ny=>
Huh7 NHTpfHJCeG:ydH;zbZMh[XO|YYm= MYqxJO69VcLi NWHYXYwyTE2VTx?= MXvpcoR2[2W|IHHwc5B1d3Orcx?= NHS2T|IzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts M1jn[mtqdmG|ZTDhd5NigQ>? MYGyOUDPxE1? M1fxNmROW09? NHTSfZRz\WS3Y3XzJGhqe3SxbnWgTFMh[W6mIFi0JIFk\XS7bHH0bY9vKGyndnXsd:Kh NFO4NW0zODV|NEO0OS=>
H23 M1XIXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYfUUppLOjVizszN M2XMXWROW09? NFn3S29{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NYD6elJEOjB3M{SzOFU>
WM35 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mk\kNVAh|ryP NFnEfJNFVVOR NYTqbZRKe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NIjxfnIzODV|NEO0OS=>
NIH 3T3 M4jLXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1vJe|ExKM7:TR?= NF\yVHNFVVOR M2jEb4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NFWzVlMzODV|NEO0OS=>
H838 NGLsfmpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVWxNEDPxE1? MnriSG1UVw>? NVnjdYlH\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 M4HPZ|IxPTN2M{S1
H1395 Mo\jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFSzSmkyOCEQvF2= Mlv2SG1UVw>? Ml7G[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NYfCcG85OjB3M{SzOFU>
Quiescent S2 Mny5T4lv[XOnIHHzd4F6 NU\aS5BMOzBizszN NVjKb4RDTE2VTx?= NX\ESFd1[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz MlHPNlE2OTh7MUW=
PC3 MnfyRZBweHSxc3nzJIF{e2G7 Ml;zNlAh|ryP MkTjSG1UVw>? NHfqUIFqdmS3Y3XzJIFxd3C2b4Ppdy=> M{nrcFIyPzB7MUOw
Du145 NH3Zc4pCeG:ydH;zbZMh[XO|YYm= MlvXNlAh|ryP MlnhSG1UVw>? NXnCWZNzcW6mdXPld{BieG:ydH;zbZM> Ml:1NlE4ODlzM{C=
LNCaP MmnYRZBweHSxc3nzJIF{e2G7 NHX3W5YzOCEQvF2= NIfyN3FFVVOR M{P3dYlv\HWlZYOgZZBweHSxc3nz NXnre4lpOjF5MEmxN|A>
LAPC-4 M1jKemFxd3C2b4Ppd{Bie3OjeR?= NWO5Tm5COjBizszN M4\PXmROW09? M2f5dIlv\HWlZYOgZZBweHSxc3nz M37xUVIyPzB7MUOw
LNCaP M{WyV2Z2dmO2aX;uJIF{e2G7 MYmyNEDPxE1? MXrEUXNQ Mnf2[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MnfLNlE4ODlzM{C=
LAPC-4 NVnjRnNYTnWwY4Tpc44h[XO|YYm= MkHQNlAh|ryP NV3YdXRkTE2VTx?= MkTE[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? M3HmVVIyPzB7MUOw
Kasumi-1 MknwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWD+OVAh|ryP NH62dYxFVVOR M1jVSIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M13Z[|I{OzlyNUO2
SKNO-1 NF\vW4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkTLglUxKM7:TR?= NXv4flc3TE2VTx?= NXPiXY1ScW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M2\xWlI{OzlyNUO2
Kasumi-1 MWHLbY5ie2ViYYPzZZk> M4\VNZ4yOCEQvF2= NE\KNoVFVVOR NIfBTWVz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MoHlNlM{QTB3M{[=
SKNO-1 NID0UJNMcW6jc3WgZZN{[Xl? NUnvWVBzhjFyIN88US=> Mn\LSG1UVw>? NGHoXopz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> M3XsOFI{OzlyNUO2
A549 NH[1UpNHfW6ldHnvckBie3OjeR?= MYmxNEDPxE1? MlrpSG1UVw>? MUnlcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl M1HNflI1PzR4NUe0
NRK-52E NYLke2xNTnWwY4Tpc44h[XO|YYm= MVmxNEDPxE1? MlK4SG1UVw>? NVjr[VZjcW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgV3RCXDNiboXjcIVieiC2cnHud4xw[2G2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCWR1[t{tIyNCClb3zsZYdmdiCLVjDhcoQh\mmkcn;u[YN1cW5? MmC1NlUxQDhyMEK=
PC12 NXfv[IduT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXH+NVIvPSEQvF2= M2rDOGROW09? NVjSW2pueHKndnXueJMhXFODLXnu[JVk\WRibnX1dol1\SCob4LtZZRqd25? M2LUb|I2OTJ6M{i2
HPMCs NYnKV4hPTnWwY4Tpc44h[XO|YYm= NHPjWWpz\X[ncoPld{BmeGm2aHXsbYFtKHSxIH3ld4Vv[2i7bXHsJJRz[W6|aYTpc44hd2ZiaIXtZY4heGW{aYTvcoVidCCvZYPveIhmdGmjbDDj[Yxtew>? M3XFcVI3ODR3N{iw
A549 MkXDSpVv[3Srb36gZZN{[Xl? MYf+OVAh|ryP NHHNfGRFVVOR MoTTZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> M2TVRVI3PzFzN{S4
RAW264.7 MVLGeY5kfGmxbjDhd5NigQ>? MlTPglMxKM7:TR?= M{HGOGROW09? NUjxR3ZGemWmdXPld{Bxem9vaX7mcIFudWG2b4L5JIdmdmViZYjwdoV{e2mxbh?= NGnneXIzPjdzOEW4Oi=>
MEMM MonsT4lv[XOnIHHzd4F6 M4\4XlE2KML3TR?= NYHYUYxoTE2VTx?= MXPk[YNz\WG|ZYOgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SCKMx?= M1nJOVI3QTJzNUC2
MEMM NV\KTXp3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnK4glIxKML3TR?= NUnXUW8{TE2VTx?= M4rYcYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NW\POmFOOjZ7MkG1NFY>
MEMM NVvVemV[SXCxcITvd4l{KGG|c3H5 MkjINVUhyrWP Mn7USG1UVw>? NETaRWFqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ M2DnfVI3QTJzNUC2
T47D M1\iXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVnIc25JOTBizszN Mme3SG1UVw>? MXXJR|UxRTd{IH7N M373SlE5OzhzNES0
ZR-75-1 NGXXb3ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFO3e|YyOCEQvF2= NGrkZmZFVVOR MlXtTWM2OD15OTDuUS=> NWPzeJA4OTh|OEG0OFQ>
BT474 M3LCO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MonONVAh|ryP NYHL[nA4TE2VTx?= M{Lve2lEPTB;OE[gcm0> MWWxPFM5OTR2NB?=
HCC1954 NWLEfHVTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{S0RlExKM7:TR?= NUXKdmQ3TE2VTx?= NUDnVVB6UUN3ME2xNVkhdk1? M4\JcFE5OzhzNES0
MDA-MB-453 NFf5e|BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHPNfGoyOCEQvF2= MY\EUXNQ NXf5fJRTUUN3ME25O|Uhdk1? NVHKV|JCOTh|OEG0OFQ>
MDA-MB-468 NVTld|F3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zFTFExKM7:TR?= NHjtTVRFVVOR NV:5O483UUN3ME2zNlA5KG6P MlzlNVg{QDF2NES=
SkBr3 MmT5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mm\hNVAh|ryP NH:2XpdFVVOR M{jCSWlEPTB-MUCsNFAxKG6P M17xR|E5OzhzNES0
MDA-MB-231 MkT2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NILwemsyOCEQvF2= NYHx[FhlTE2VTx?= NUfxSnRsUUN3ME6xNEwxODBibl2= MoCxNVg{QDF2NES=
HCT116 MoXQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYTIcpRwOTBizszN M{DsWWROW09? NYjvVFg5UUN3ME21PFM3KG6P M3vKTlE5OzhzNES0
HT29 MnfIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVTRSpF4OTBizszN MUjEUXNQ M135[GlEPTB-MUCsNFAxKG6P M1LhUlE5OzhzNES0
HFF NFSy[4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmLZNVAh|ryP M4\iXGROW09? MVTJR|UxRTd4MUWgcm0> Mk\uNVg{QDF2NES=
HN5 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV\vfWVlOTBizszN Mk\YSG1UVw>? Mnr1TWM2OD5zMDywNFAhdk1? MnfTNVg{QDF2NES=
786-0 NFuwO4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX6xNEDPxE1? MXrEUXNQ MYHJR|UxRTRyMEmgcm0> M1jaTFE5OzhzNES0
H157 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYDMR|UyOTBizszN NXTUVphFTE2VTx?= MkP0TWM2OD1{NkSyJI5O NF7EW5oyQDN6MUS0OC=>
NCI-H460 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYXCXppSOTBizszN Ml3WSG1UVw>? MnK1TWM2OD5{LEWwNEBvVQ>? MVGxPFM5OTR2NB?=
SKOV-3 NYPTRo1XT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4fTU|ExKM7:TR?= MXnEUXNQ MUTJR|UxRTJzMk[gcm0> M1;MN|E5OzhzNES0
OVCAR-3 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NI\NTVUyOCEQvF2= NYLKZmRpTE2VTx?= NIm1VJFKSzVyPUK5NVghdk1? MnLVNVg{QDF2NES=
BXPC3 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NI\TbFkyOCEQvF2= NX3PfFFKTE2VTx?= M1HKZWlEPTB;M{G0NUBvVQ>? NFfITGIyQDN6MUS0OC=>
MiaPaCa NHS5b5FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX6xNEDPxE1? MYrEUXNQ NUezbGJ5UUN3ME21OFM{KG6P M2D1b|E5OzhzNES0
PANC-1 NW\QTWY{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYnhS5BjOTBizszN MUnEUXNQ MXXJR|UxRTh4OEGgcm0> MmThNVg{QDF2NES=
LNCaP MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVWxNEDPxE1? NVXjeItJTE2VTx?= Mo\FTWM2OD1zNEegcm0> NYjjcpZVOTh|OEG0OFQ>
DU145 NFj6NIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4XtXVExKM7:TR?= M4P3TGROW09? Mm[0TWM2OD1|OEGyJI5O NHXSSJAyQDN6MUS0OC=>
PC3 MkeyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXS4PJY6OTBizszN M3nId2ROW09? M3G3VGlEPTB-MUCsNFAxKG6P MXGxPFM5OTR2NB?=
BT474 NFXo[pZMcW6jc3WgZZN{[Xl? NFW5XI8yOCEQvF2= NH3rRVJFVVOR NG\vVJJqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNkCgcm0> NHKwNWcyQDN6MUS0OC=>
786-0 MWHLbY5ie2ViYYPzZZk> M1TwcFExKM7:TR?= NGPp[GFFVVOR NUfOZo1[cW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMUWwJI5O MmjLNVg{QDF2NES=
LNCaP NWTQdmI1U2mwYYPlJIF{e2G7 Mmf4NVAh|ryP MlHBSG1UVw>? M3LMNYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR|IH7N NXjINXFQOTh|OEG0OFQ>
PC3 MmjMT4lv[XOnIHHzd4F6 Ml;lNVAh|ryP MWjEUXNQ NVTrU|FRcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEmgcm0> MWSxPFM5OTR2NB?=
KARPAS-231 NXzsOnNMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWSxNEDPxE1? M1X1e2ROW09? MX3FR|UxRTRzIH7N NYKyeodLOTlyNkS3N|A>
CCRFSB Mo\PS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIfrN5QyOCEQvF2= MlzNSG1UVw>? M1\tU2VEPTB;MUW1JI5O MV2xPVA3PDd|MB?=
SUP B15 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3jkSFExKM7:TR?= MXXEUXNQ MkflSWM2OD1zOUegcm0> NX[1Vnd7OTlyNkS3N|A>
SD-1 M2m0XWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVzXVHU1OTBizszN M{f0S2ROW09? MmjpSWM2OD1|MkCgcm0> NF[4TVIyQTB4NEezNC=>
RS4;11 NH35NHFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3juelExKM7:TR?= NIP1XoxFVVOR NHPGb4tGSzVyPU[1OEBvVQ>? MnjINVkxPjR5M{C=
MN-60 NHr0OYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVXJUIo1OTBizszN MlPkSG1UVw>? M3nPNmVEPTB;M{[wNkBvVQ>? NXnrSHhnOTlyNkS3N|A>
Tanoue MmT6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYD0NopDOTBizszN NVTrSo1FTE2VTx?= M33WV2VEPTB;NEWxO{BvVQ>? M1uxNlE6ODZ2N{Ow
RCH-ACV M{nRbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4jjT|ExKM7:TR?= MYDEUXNQ MX7FR|UxRTF3MjDuUS=> NHHBUVEyQTB4NEezNC=>
SEM NFvOb5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1n1UVExKM7:TR?= NHe0PJBFVVOR NUPtcJB2TUN3ME2yNFIhdk1? M4LyeFE6ODZ2N{Ow
KASUMI-2 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LJcFExKM7:TR?= MnLSSG1UVw>? NIHp[ZVGSzVyPUKyOUBvVQ>? NU\zRpF7OTlyNkS3N|A>
REH MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3vUcVExKM7:TR?= M4XFXmROW09? NETrenZGSzVyPUK4PEBvVQ>? NUf3S|RxOTlyNkS3N|A>
697 NWjqSWJzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3raRVExKM7:TR?= NG\GSnNFVVOR NIXHUGdGSzVyPUOzPEBvVQ>? M3;lV|E6ODZ2N{Ow
NALM-6 NHnqSJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXyxNEDPxE1? NXLMOG1vTE2VTx?= MlvjSWM2OD12MkGgcm0> NITNd2wyQTB4NEezNC=>
MHH-CALL–3 NWW1XolxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWWxNEDPxE1? NVfvV2ozTE2VTx?= M{XNUmVEPTB;OEGyJI5O M1rKeVE6ODZ2N{Ow
MHH-CALL–2 MofES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWGxNEDPxE1? NFK1dlFFVVOR NFfsdYJGSzVyPUKxNVQhdk1? MmXzNVkxPjR5M{C=
J.GAMMA-1 MlvjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLvPXg6OTBizszN NVrxeVRnTE2VTx?= M2PKc2VEPTB;NkWgcm0> M4XQNFE6ODZ2N{Ow
JR45.01 NUPod401T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2XFeFExKM7:TR?= NWnSdIhuTE2VTx?= Mk\oSWM2OD14ODDuUS=> NGfXXGMyQTB4NEezNC=>
A3 MmL5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\SfocyOCEQvF2= NUXPfGpYTE2VTx?= NX3oU3R6TUN3ME22PUBvVQ>? MmLqNVkxPjR5M{C=
I 2.1 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXyxNEDPxE1? MVLEUXNQ M2Lv[WVEPTB;N{Ogcm0> NXXvS3I5OTlyNkS3N|A>
MOLT-3 MmPtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYG3bGw6OTBizszN M1fv[GROW09? M2nmZWVEPTB;N{Sgcm0> NFm4ZYIyQTB4NEezNC=>
P116 NUH5[ox2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmjrNVAh|ryP M4WxVWROW09? NGDN[mZGSzVyPUe4JI5O MoXaNVkxPjR5M{C=
J.Cam1.6 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUCxNEDPxE1? NF3ucZVFVVOR M{KwbGVEPTB;N{mgcm0> MWCxPVA3PDd|MB?=
I 9.2 NVHlTo1lT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn;YNVAh|ryP M4fs[WROW09? NH;aWFVGSzVyPUiwJI5O Mo\1NVkxPjR5M{C=
LOUCY MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWCxNEDPxE1? MYXEUXNQ MYPFR|UxRTFzNzDuUS=> MWOxPVA3PDd|MB?=
J.RT3-T3.5 M2jKZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGLWTXAyOCEQvF2= MUTEUXNQ NFLmbYtGSzVyPUGyN{BvVQ>? MVyxPVA3PDd|MB?=
800000 MoXvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGjkdIoyOCEQvF2= NHW4dmRFVVOR NV7KOoNJTUN3ME2xOlMhdk1? MlHKNVkxPjR5M{C=
Jurkat NYPTNXNxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEDQb|IyOCEQvF2= MlW1SG1UVw>? Mo[zSWM2OD1{MkWgcm0> M4O5SlE6ODZ2N{Ow
MOLT-4 MoflS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEfFSJkyOCEQvF2= NU\iTm1rTE2VTx?= MVTFR|UxRTJ|MjDuUS=> MX:xPVA3PDd|MB?=
Molt-16 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4j1RlExKM7:TR?= NVn1eJhQTE2VTx?= M2nteGVEPTB;MkSxJI5O NVHxO4R6OTlyNkS3N|A>
CEM/C3 M1jle2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTWRY9lOTBizszN NGW0VWFFVVOR MnviSWM2OD1{NUegcm0> MXixPVA3PDd|MB?=
CEM/C2 NV7ScppDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF7hfI0yOCEQvF2= NHK0RmNFVVOR MkXBSWM2OD1{N{Ggcm0> MnnuNVkxPjR5M{C=
CCRFCEM M1qzV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUjIXmZkOTBizszN M1HRbmROW09? MULFR|UxRTN{NzDuUS=> MWKxPVA3PDd|MB?=
CEM/C1 Mlv0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\2PXIyOCEQvF2= NIP0NoVFVVOR NWLJ[m55TUN3ME2zPFIhdk1? M{nSflE6ODZ2N{Ow
SUPTI[VB] MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXGxNEDPxE1? M3TrN2ROW09? MUDFR|UxRTZzOTDuUS=> M{LWeVE6ODZ2N{Ow
CCRF–HSB-2 NYqwXm5GT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MY[xNEDPxE1? M2Hu[2ROW09? MVrFR|UxRTJzMUegcm0> MUmxPVA3PDd|MB?=
I 2.1 NGHtc2tCeG:ydH;zbZMh[XO|YYm= NH;HdJAyOCEQvF2= M4TCbmROW09? M3qwNYlv\HWlZYOgZZBweHSxc3nz NWPU[ZJnOTlyNkS3N|A>
I 9.2 NUDOPXBQSXCxcITvd4l{KGG|c3H5 M37aWlExKM7:TR?= NHXFcoJFVVOR MVjpcoR2[2W|IHHwc5B1d3Orcx?= MmTuNVkxPjR5M{C=
A3 MlL4RZBweHSxc3nzJIF{e2G7 NI\ueJkyOCEQvF2= Mm[1SG1UVw>? M1L3Nolv\HWlZYOgZZBweHSxc3nz NV[wNo5TOTlyNkS3N|A>
RD MoH1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1nQTlExKM7:TR?= MWHJR|UxRjFyIN88US=> MXuyNFc1ODZ{Mx?=
Rh41 NH;OTW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXexNEDPxE1? MYLJR|UxRTN|Lkigcm0> MWiyNFc1ODZ{Mx?=
Rh18 NGLyNm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mk\TNVAh|ryP MnfaTWM2OD1|MEOgcm0> Mn;lNlA4PDB4MkO=
Rh30 NUnGOHNQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYfnNJlnOTBizszN NVLKdGk4UUN3ME20MlgyKM7:TR?= Ml;0NlA4PDB4MkO=
BT-12 M3:xUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHfadXYyOCEQvF2= M{WzbGlEPTB-MUCg{txO M4TGcVIxPzRyNkKz
CHLA-266 NYXJVVJ2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVyyT|FJOTBizszN MnXvTWM2OD1zLkKyJO69VQ>? MVyyNFc1ODZ{Mx?=
TC-71 MnXIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVGxNEDPxE1? MnPRTWM2OD1{LkWyJO69VQ>? M3\RflIxPzRyNkKz
CHLA-9 NX3OOoE2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFja[VkyOCEQvF2= NFPLfHJKSzVyPUW5NUBvVQ>? NI\MN4UzODd2ME[yNy=>
CHLA-10 Mn:yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3vjc|ExKM7:TR?= M1G4NGlEPTB;MUCyJI5O NUjqRoR[OjB5NEC2NlM>
CHLA-258 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3m1c|ExKM7:TR?= MWXJR|UxRTFwMEWg{txO M1PJOFIxPzRyNkKz
GBM2 NI\McmdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXniSlBIOTBizszN MVfJR|UxRTlwMUWg{txO M{DjbVIxPzRyNkKz
NB-1643 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXrZZ|FQOTBizszN MUfJR|UxRTVwNDFOwG0> NHjoU5czODd2ME[yNy=>
NB-Ebc1 MkDlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1rOd|ExKM7:TR?= NWjacmQyUUN3ME6xNEDPxE1? NWLZO|RFOjB5NEC2NlM>
CHLA-90 NGPReoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{jpd|ExKM7:TR?= NFrNbI9KSzVyPkGwJO69VQ>? MVeyNFc1ODZ{Mx?=
CHLA-136 MmLNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoPQNVAh|ryP M2XEbWlEPTB-MUCg{txO M{P1cFIxPzRyNkKz
NALM-6 NF2zOFBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXneopDOTBizszN MYXJR|UxRTJ4NTDuUS=> NH7oXG8zODd2ME[yNy=>
COG-LL-317 NGDsZ5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV6xNEDPxE1? M1j2bWlEPTB;Nj60PUBvVQ>? MYCyNFc1ODZ{Mx?=
RS4;11 MknxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4G5WlExKM7:TR?= MkfGTWM2OD1zNEegcm0> MVKyNFc1ODZ{Mx?=
MOLT-4 M3\sPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGTMOmcyOCEQvF2= M4TVTmlEPTB;NECgcm0> NWTkc2dXOjB5NEC2NlM>
CCRF-CEM M1zjfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2\pPVExKM7:TR?= MmjDTWM2OD1{Nkigcm0> Mn7BNlA4PDB4MkO=
Kasumi-1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3m0VlExKM7:TR?= MmHGTWM2OD1zMEegcm0> NYHMN4Z{OjB5NEC2NlM>
Karpas-299 MkXLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX2xNEDPxE1? NVL6eGhUUUN3ME2yMlk{KM7:TR?= MmfxNlA4PDB4MkO=
Ramos-RA1 NUO3bm5JT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHHq[HgyOCEQvF2= MYjJR|UxRTdwM{Wg{txO M2fLc|IxPzRyNkKz
H1299 NUTSPXNkU2mwYYPlJIF{e2G7 MWmxNEDPxE1? M2rDSIlvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> NYC2R2x4OjF7MEi2NVY>

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID