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.

Size Price Stock Quantity  
USD 110 In stock
USD 470 In stock

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • 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

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MoH5T4lv[XOnIHHzd4F6 NIfOUGl,OTBizszN MWHpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MoPqNlA1QDRyMUi=
HT29 MmjYT4lv[XOnIHHzd4F6 MVT+NVAh|ryP NILSS2RqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz M4XOdVIxPDh2MEG4
MDA-MB-231 M{HBVmtqdmG|ZTDhd5NigQ>? M4\oOp4yOCEQvF2= Mn3NbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NIrPR2IzODR6NECxPC=>
NCI-H441 NWmyUVlNU2mwYYPlJIF{e2G7 NFPqfGp,OTBizszN NGi4W4FqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NVvqTGNjOjB2OESwNVg>
SK-MEL-28 NFm1TZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3HZdlM{KM7:TR?= NHLiOWNKSzVyPkOzJO69VQ>? MUmyNFQ5PDBzOB?=
NCI-H661 MnjvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYPYZmM3OzNizszN NU\SN5Z7UUN3ME6zN{DPxE1? NVm2T2ZZOjB2OESwNVg>
NCI-H446 NIryOGJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUCzN{DPxE1? M3L0[GlEPTB;NzFOwG0> NFPNc|IzODR6NECxPC=>
MDA-MB-231 Mm\MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXTkOZhKOzNizszN MUjJR|UxRTBwNUWg{txO MkfRNlA1QDRyMUi=
DLD-1 MkHOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVezN{DPxE1? MoD1TWM2OD1yLkWzJO69VQ>? M2\weVIxPDh2MEG4
A549 NYjacZhMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHK5WVU{OyEQvF2= NV;0eGd{UUN3ME2wMlU6KM7:TR?= M2XGVlIxPDh2MEG4
SK-OV-3 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXfGSIoyOzNizszN M1vEV2lEPTB;MD62OkDPxE1? NFTEdmczODR6NECxPC=>
NCI-H460 M2DrOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXizN{DPxE1? NU[4flRvUUN3ME2wMlYh|ryP M4jtVVIxPDh2MEG4
A375 M1jCV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHOxbG0{OyEQvF2= NIPOeo9KSzVyPUCuOFIh|ryP NIDON4UzODR6NECxPC=>
NCI-H441 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlnEN|Mh|ryP MoHlTWM2OD1yLkOg{txO NX;SfoRxOjB2OESwNVg>
HT29 NUmyWJVwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2LCfVM{KM7:TR?= NUT2dGwxUUN3ME2wMlQ6KM7:TR?= MkfENlA1QDRyMUi=
MKN-45 NIWycmFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYWzN{DPxE1? NXXaOYhVUUN3ME2wMlU5KM7:TR?= MmnmNlA1QDRyMUi=
HT29 NYnFT|NkSXCxcITvd4l{KGG|c3H5 M1nje54yOCEQvF2= MnW1d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NIHHW4EzODR6NECxPC=>
MKN-45 NInqe4lCeG:ydH;zbZMh[XO|YYm= MYH+NVAh|ryP NHSzNHh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|IHL5JFgxNTlyJT6= NFyzOmIzODR6NECxPC=>
MDA-MB-231 M3TIeWFxd3C2b4Ppd{Bie3OjeR?= MlGyglExKM7:TR?= M4[wS41w\GW|dHz5JIlv\HWlZYOgZZBweHSxc3nzJIJ6KDN3JT6= NIWzfWczODR6NECxPC=>
MDA-MB-231/TGL NFHtc4lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVr+NVAxKM7:TR?= MljWS2k2OD1zLkKg{txO NILKdJIzOjB{N{[5NC=>
1833/TGL MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1fZNZ4yODBizszN MVvHTVUxRTNwNzFOwG0> NHLmOHozOjB{N{[5NC=>
EBC1 M4TLWmN6fG:2b4jpZ:Kh[XO|YYm= M37xc54yOCEQvF2= M{G5XolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= M4LVXFI{PTl6Mke2
SNU638 NFzVT49EgXSxdH;4bYPDqGG|c3H5 NVHt[Yp6hjFyIN88US=> M4PVVIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NHHUfJozOzV7OEK3Oi=>
A549 NHTTN3hEgXSxdH;4bYPDqGG|c3H5 MXf+NVAh|ryP MYjuc5Qh[W[oZXP0 MojNNlM2QTh{N{[=
H460 NUTIPG5RS3m2b4TvfIlkyqCjc4PhfS=> NVzzTpdohjFyIN88US=> NUTmbpc6dm:2IHHm[oVkfA>? MYeyN|U6QDJ5Nh?=
HCC827 Ml70R5l1d3SxeHnjxsBie3OjeR?= MWf+NVAh|ryP M{HnVo5wfCCjZn\lZ5Q> MlrXNlM2QTh{N{[=
A549 MofxSpVv[3Srb36gZZN{[Xl? MknONVAh|ryP NFLTXHllcXO{dYD0d{BucWO{b4T1ZpVt\Q>? NVvPbHNGOjN3OUiyO|Y>
EBC1 MlTJSpVv[3Srb36gZZN{[Xl? MlfINVAh|ryP Mkf0[Il{enWydIOgcYlkem:2dXL1cIU> Mkn3NlM2QTh{N{[=
H460 M4HENGZ2dmO2aX;uJIF{e2G7 MVuxNEDPxE1? MYTpcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v MlXWNlU{OTNyMUC=
K562/VCR MkfKR5l1d3SxeHnjxsBie3OjeR?= MXT+NVAh|ryP M{fv[5Npd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= M4[4ZlI2OzF|MEGw
CEM/VBL MnzxR5l1d3SxeHnjxsBie3OjeR?= M1jRcJ4yOCEQvF2= MWLzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MmPJNlU{OTNyMUC=
U266 MWjDfZRwfG:6aXRCpIF{e2G7 Moe5glMh|ryPwrC= NHvJfoZKSzVyPUGuNUDPxE1? NVvaPI1xOjV6MUCwNVM>
OPM-2 NVvKclVuS3m2b4TvfIlkyqCjc4PhfS=> MXP+N{DPxE4EoB?= M{nVTmlEPTB;MT64JO69VQ>? Mn:1NlU5OTByMUO=
MM.1S MV7DfZRwfG:6aXRCpIF{e2G7 NVL4N4xDhjNizszNxsA> M4DrbWlEPTB;MT62JO69VQ>? NFLTOHozPThzMECxNy=>
MM.1R NHjHXZFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{fv[lMh|ryPwrC= NV\NW2lkcW6qaXLpeJMh[2WubDDndo94fGhiYomgOFkm MkSxNlU5OTByMUO=
RPMI-8226 NW\aU|RuS3m2b4TvfIlkyqCjc4PhfS=> NXrIemZnhjNizszNxsA> NX7DN25[UUN3ME2wMlkh|ryP MWmyOVgyODBzMx?=
ANBL-6 MUTDfZRwfG:6aXRCpIF{e2G7 NV7WZmluOSEQvF5CpC=> NXLycmVmcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NIDKUlAzPThzMECxNy=>
ANLB-6/V10R MnOzR5l1d3SxeHnjxsBie3OjeR?= NHG0c3kyKM7:TdMg NXLsUldjcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NUTweYtlOjV6MUCwNVM>
KAS-6/1 M2\6PWN6fG:2b4jpZ:Kh[XO|YYm= NGjYSVQyKM7:TdMg M2fMNolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NYPX[lBQOjV6MUCwNVM>
KAS-6/V10R M2PteGN6fG:2b4jpZ:Kh[XO|YYm= Mm\hNUDPxE4EoB?= NWfLcWR6cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NYDp[INKOjV6MUCwNVM>
KAS-6/R10R MoSyR5l1d3SxeHnjxsBie3OjeR?= M{Do[|Eh|ryPwrC= NWjwVXkycW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MnPFNlU5OTByMUO=
8226/S MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmPJN{DPxE4EoB?= MnHobY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl M1jTcVI2QDFyMEGz
8226/LR-5 NUfhRnRYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXPMSXlHOyEQvF5CpC=> NGHXeoRqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> MoLxNlU5OTByMUO=
Huh7 M3\NW2N6fG:2b4jpZ:Kh[XO|YYm= MUj+OE45KM7:TdMg NUjHVlQ3TE2VTx?= MXPJR|UxRTlwOTDuUS=> MmnHNlYzPTl{NUC=
Hep3B NH:4ZmdEgXSxdH;4bYPDqGG|c3H5 MWD+OE45KM7:TdMg M3Wzd2ROW09? MoHpTWM2OD12NEiuO{BvVQ>? MmLnNlYzPTl{NUC=
HepG2 MULDfZRwfG:6aXRCpIF{e2G7 NGflTFB,PC56IN88UeKh M17JZmROW09? NFzONXVKSzVyPUGzPU44PyCwTR?= MoD2NlYzPTl{NUC=
Chang MW\DfZRwfG:6aXRCpIF{e2G7 M1z0Xp41NjhizszNxsA> Mlj6SG1UVw>? MVzJR|UxRTR2OD63JI5O M3v4[lI3OjV7MkWw
Huh7 M2jHNGZ2dmO2aX;uJIF{e2G7 MmT1NU43KM7:TdMg NFXveoFFVVOR MonUZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MV2yOlI2QTJ3MB?=
Hep3B MorBSpVv[3Srb36gZZN{[Xl? NUDxeJpOOS54IN88UeKh NX\wbmozTE2VTx?= NVX2XXYz[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= MkDYNlYzPTl{NUC=
HepG2 M3foWmZ2dmO2aX;uJIF{e2G7 MnTwNU43KM7:TdMg MVTEUXNQ M{j4VINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M3\hZ|I3OjV7MkWw
Chang M1TFUmZ2dmO2aX;uJIF{e2G7 M3mw[lEvPiEQvF5CpC=> MVTEUXNQ M{PkRoNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MVyyOlI2QTJ3MB?=
MHCC97L NFHlfZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MomzglExKM7:TR?= NEnUdZBFVVOR NYLUWHhYUUN3ME2zNVUhdk1? NY\EOI5pOjZ2NUi5OVM>
MHCC97H MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUS2VlM5hjFyIN88US=> MYDEUXNQ M3\sU2lEPTB;M{[45qCKKG6P NXW0V492OjZ2NUi5OVM>
Huh7 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2XaXp4yOCEQvF2= NF35WXVFVVOR M2PuTWlEPTB;Mk[1JI5O MYCyOlQ2QDl3Mx?=
HepG2 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGm0fGZ,OTBizszN NXPCRoJtTE2VTx?= MULJR|UxRTN7MjDuUS=> M3rycVI3PDV6OUWz
MHCC97L MVTGeY5kfGmxbjDhd5NigQ>? MmHRNUDPxE4EoB?= MWnEUXNQ MlXnbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> M1\MV|I3PDV6OUWz
Huh7 NGO4WINHfW6ldHnvckBie3OjeR?= MnW4NUDPxE4EoB?= MlnuSG1UVw>? NVj5[2xLcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? M4XQWVI3PDV6OUWz
MHCC97L M3G3fGFxd3C2b4Ppd{Bie3OjeR?= M{\mdlEh|ryPwrC= NX3YU4k6TE2VTx?= MWLpcoR2[2W|IHHwc5B1d3Orcx?= Mn7uNlY1PTh7NUO=
Huh7 NIW4OXhCeG:ydH;zbZMh[XO|YYm= MXyxJO69VcLi MUPEUXNQ M4Lhc4lv\HWlZYOgZZBweHSxc3nz NH;Dd2gzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts M3KwZ2tqdmG|ZTDhd5NigQ>? NYmzbpd3OjVizszN NVTMTlJoTE2VTx?= NX3aXmR7emWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? MYeyNFU{PDN2NR?=
H23 Mo\jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnPrNlUh|ryP MVnEUXNQ MUnzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MVKyNFU{PDN2NR?=
WM35 Mmr2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\Gb|ExKM7:TR?= M{X2[mROW09? M{HNW5Nq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MVOyNFU{PDN2NR?=
NIH 3T3 NED1[phIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3W2XFExKM7:TR?= MWLEUXNQ NHPVbHBld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NVLsUnJGOjB3M{SzOFU>
H838 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHqNVAh|ryP MmrNSG1UVw>? Mnu4[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NGG5Z2UzODV|NEO0OS=>
H1395 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mkm4NVAh|ryP MYXEUXNQ MnnE[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 M3vD[|IxPTN2M{S1
Quiescent S2 NYe0ZmNHU2mwYYPlJIF{e2G7 NWL3fm92OzBizszN NH\sSpVFVVOR NYq2cYx{[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz NInBTGMzOTVzOEmxOS=>
PC3 NEW1V|ZCeG:ydH;zbZMh[XO|YYm= M1PBWFIxKM7:TR?= M3\NdGROW09? M1vZV4lv\HWlZYOgZZBweHSxc3nz NGiyOWczOTdyOUGzNC=>
Du145 M4jOd2Fxd3C2b4Ppd{Bie3OjeR?= MnnmNlAh|ryP M3\jUGROW09? MXvpcoR2[2W|IHHwc5B1d3Orcx?= NUjEW4NMOjF5MEmxN|A>
LNCaP NYfQfW1mSXCxcITvd4l{KGG|c3H5 M4LC[VIxKM7:TR?= MlTCSG1UVw>? MXjpcoR2[2W|IHHwc5B1d3Orcx?= MmjLNlE4ODlzM{C=
LAPC-4 M3Xxd2Fxd3C2b4Ppd{Bie3OjeR?= MYWyNEDPxE1? NYjKWm9iTE2VTx?= NUjYNmc{cW6mdXPld{BieG:ydH;zbZM> MnXWNlE4ODlzM{C=
LNCaP M4fJ[2Z2dmO2aX;uJIF{e2G7 M3LCWlIxKM7:TR?= MU\EUXNQ MkjT[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MWiyNVcxQTF|MB?=
LAPC-4 M1TCeGZ2dmO2aX;uJIF{e2G7 NUDUWpN{OjBizszN NE\YVY5FVVOR Ml7S[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? M37ZdVIyPzB7MUOw
Kasumi-1 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYr3eoRThjVyIN88US=> NX7nN4tVTE2VTx?= Ml7zbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NHftSoIzOzN7MEWzOi=>
SKNO-1 MkLvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGXIN|B,PTBizszN MnrOSG1UVw>? MV7pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MoC0NlM{QTB3M{[=
Kasumi-1 MWTLbY5ie2ViYYPzZZk> NGnOToR,OTBizszN NWDzN|cyTE2VTx?= MVny[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NUjYN3V4OjN|OUC1N|Y>
SKNO-1 NXjWTYJjU2mwYYPlJIF{e2G7 MYj+NVAh|ryP M4G1d2ROW09? Mo\4doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NFX2TpUzOzN7MEWzOi=>
A549 NVz4dpBpTnWwY4Tpc44h[XO|YYm= NEPEcVcyOCEQvF2= M1\LOWROW09? MVLlcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl NIPMZmszPDd2NkW3OC=>
NRK-52E Mn;mSpVv[3Srb36gZZN{[Xl? MVuxNEDPxE1? NHzXNoNFVVOR NEDkbGFqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDTWGFVOyCwdXPs[YFzKHS{YX7zcI9k[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKFSJRj5OtlEtKGOxbHzh[4VvKEmYIHHu[EBncWK{b37lZ5Rqdg>? M1GxfFI2ODh6MECy
PC12 MkO2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFjoTm9,OTJwNTFOwG0> NWDqNFAzTE2VTx?= Ml;ndJJmfmWwdIOgWHNCNWmwZIXj[YQhdmW3cnn0[UBnd3KvYYTpc44> M{nyTFI2OTJ6M{i2
HPMCs Mk\ZSpVv[3Srb36gZZN{[Xl? M2KxNJJmfmW{c3XzJIVxcXSqZXzpZYwhfG9ibXXz[Y5kcHmvYXygeJJidnOrdHnvckBw\iCqdX3hckBx\XKrdH;u[YFtKG2nc3;0bIVtcWGuIHPlcIx{ M4jMPFI3ODR3N{iw
A549 M1nVdWZ2dmO2aX;uJIF{e2G7 MUf+OVAh|ryP M1HvN2ROW09? NYLDTYxb[W[oZXP0d{B1cGVidnnyZYwhdGmoZTDjfYNt\SCjbnSgbI9{fCC{ZYPwc45{\Q>? NXjGb3B6OjZ5MUG3OFg>
RAW264.7 M4L2R2Z2dmO2aX;uJIF{e2G7 NYnURm0yhjNyIN88US=> M2SwV2ROW09? MVTy[YR2[2W|IIDyc{1qdm[uYX3tZZRwenliZ3Xu[UBmgHC{ZYPzbY9v M3TQfVI3PzF6NUi2
MEMM NHr2SmtMcW6jc3WgZZN{[Xl? NWTXTnVLOTViwsXN MX;EUXNQ NWe0OJRY\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> NX[3UWdtOjZ7MkG1NFY>
MEMM NVTv[mp3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYj+NlAhyrWP MY\EUXNQ M2m5bIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NHu5eWEzPjl{MUWwOi=>
MEMM NHG4cWpCeG:ydH;zbZMh[XO|YYm= NEjZdYIyPSEEtV2= MYnEUXNQ M4TZZolv\HWlZYOgeIhmKHC{ZYPlcoNmKG:oIITo[UBieG:ydH;zbZMheHKxdHXpckwh[2ynYY\l[EBE[XOyYYPlMVM> MmXONlY6OjF3ME[=
T47D NF60XGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1zYfVExKM7:TR?= M2\y[WROW09? MYLJR|UxRTd{IH7N NWq3d4RtOTh|OEG0OFQ>
ZR-75-1 NELkb3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVexNEDPxE1? NHy4VJpFVVOR M3[5[mlEPTB;N{mgcm0> NVHPO3h3OTh|OEG0OFQ>
BT474 M4DXe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NU\6dHlMOTBizszN MUXEUXNQ MXTJR|UxRTh4IH7N NGnCcHQyQDN6MUS0OC=>
HCC1954 NF7RWlhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYKxNEDPxE1? MUXEUXNQ MkHMTWM2OD1zMUmgcm0> Mmn3NVg{QDF2NES=
MDA-MB-453 M4H2[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVOxNEDPxE1? Mo\RSG1UVw>? M2HFXGlEPTB;OUe1JI5O Mn7JNVg{QDF2NES=
MDA-MB-468 M1:xZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHfhbVkyOCEQvF2= NX\0ZYhSTE2VTx?= NFHJNXNKSzVyPUOyNFghdk1? NIjCWoUyQDN6MUS0OC=>
SkBr3 NVL5bXdlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3r0d|ExKM7:TR?= NXrCS404TE2VTx?= M4HnNWlEPTB-MUCsNFAxKG6P NEjGZnMyQDN6MUS0OC=>
MDA-MB-231 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUWxNEDPxE1? NV\mXYpDTE2VTx?= Mkm1TWM2OD5zMDywNFAhdk1? MXqxPFM5OTR2NB?=
HCT116 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1ntRVExKM7:TR?= MoWwSG1UVw>? MUDJR|UxRTV6M{[gcm0> M4jNUFE5OzhzNES0
HT29 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NI\SV3QyOCEQvF2= M{K4VGROW09? NHq0THBKSzVyPkGwMFAxOCCwTR?= M3rBcVE5OzhzNES0
HFF NWjyUodHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn3QNVAh|ryP MoHLSG1UVw>? NUj3SVZHUUN3ME23OlE2KG6P NF;WXFYyQDN6MUS0OC=>
HN5 NYTWTlVJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MofVNVAh|ryP M3vYd2ROW09? MmrHTWM2OD5zMDywNFAhdk1? NHnaVIIyQDN6MUS0OC=>
786-0 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnGyNVAh|ryP MVHEUXNQ MVXJR|UxRTRyMEmgcm0> M{n5dFE5OzhzNES0
H157 NGHKWYtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1PYTlExKM7:TR?= MnTvSG1UVw>? NFru[G5KSzVyPUK2OFIhdk1? NWPYO3RQOTh|OEG0OFQ>
NCI-H460 NFzMUXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVLjO216OTBizszN Mm[0SG1UVw>? NHv1PJlKSzVyPkKsOVAxKG6P MVOxPFM5OTR2NB?=
SKOV-3 MlHuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXmxNEDPxE1? MkTESG1UVw>? MlPsTWM2OD1{MUK2JI5O M1\hR|E5OzhzNES0
OVCAR-3 NVTPVGNxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3;zO|ExKM7:TR?= MmjKSG1UVw>? NUm3UW9YUUN3ME2yPVE5KG6P NYPmUYNiOTh|OEG0OFQ>
BXPC3 NGX6bFdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEPKPG0yOCEQvF2= MYnEUXNQ M1zpUmlEPTB;M{G0NUBvVQ>? MVexPFM5OTR2NB?=
MiaPaCa M1nmW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M17lWlExKM7:TR?= M3LR[GROW09? MXPJR|UxRTV2M{Ogcm0> MUKxPFM5OTR2NB?=
PANC-1 NX3vbWxjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NESzfZoyOCEQvF2= M17mVmROW09? NI\3NJBKSzVyPUi2PFEhdk1? MoS0NVg{QDF2NES=
LNCaP Mo[zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHnKUZEyOCEQvF2= NFGzfXFFVVOR NG\ne4ZKSzVyPUG0O{BvVQ>? NF:0XXYyQDN6MUS0OC=>
DU145 NV61WlhlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHjheJgyOCEQvF2= MnjzSG1UVw>? MV3JR|UxRTN6MUKgcm0> MVOxPFM5OTR2NB?=
PC3 NXvpe|J2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoC4NVAh|ryP NF3ZNpdFVVOR MWLJR|UxRjFyLECwNEBvVQ>? MUOxPFM5OTR2NB?=
BT474 MWDLbY5ie2ViYYPzZZk> NWHUTpZ3OTBizszN NWPpR3VQTE2VTx?= NGrocnhqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNkCgcm0> NYPufIx[OTh|OEG0OFQ>
786-0 MoHmT4lv[XOnIHHzd4F6 MX:xNEDPxE1? MkjSSG1UVw>? NYjoT25vcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMUWwJI5O M4HVclE5OzhzNES0
LNCaP MYTLbY5ie2ViYYPzZZk> NW\aNolJOTBizszN MkDCSG1UVw>? M3LySYlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR|IH7N MnzENVg{QDF2NES=
PC3 NHS4[21McW6jc3WgZZN{[Xl? NUDEU3A3OTBizszN NHjLNZlFVVOR M1;sXIlvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR7IH7N NF3X[5IyQDN6MUS0OC=>
KARPAS-231 Mk\5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mkj2NVAh|ryP NXPHfZRzTE2VTx?= NUnUcpI1TUN3ME20NUBvVQ>? MoDqNVkxPjR5M{C=
CCRFSB MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLoemEyOCEQvF2= NVm3SpFzTE2VTx?= Mnv4SWM2OD1zNUWgcm0> Mn73NVkxPjR5M{C=
SUP B15 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHjBZpgyOCEQvF2= NGfyRWlFVVOR M3HlfGVEPTB;MUm3JI5O M4r2O|E6ODZ2N{Ow
SD-1 NHXLfpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXKxNEDPxE1? NWj4WpFrTE2VTx?= NGr0TnVGSzVyPUOyNEBvVQ>? MkmzNVkxPjR5M{C=
RS4;11 M2S5[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MU[xNEDPxE1? NF\Gd2dFVVOR MXXFR|UxRTZ3NDDuUS=> MoqxNVkxPjR5M{C=
MN-60 NF7aUWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWLYcXlkOTBizszN MY\EUXNQ M2fKV2VEPTB;M{[wNkBvVQ>? NIfFWZEyQTB4NEezNC=>
Tanoue NITSbZNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2nZeVExKM7:TR?= NVf2fG9pTE2VTx?= MXnFR|UxRTR3MUegcm0> MX6xPVA3PDd|MB?=
RCH-ACV NH;kWmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEHkPWwyOCEQvF2= NYHZ[5NiTE2VTx?= NXPoXVhTTUN3ME2xOVIhdk1? M1\zWlE6ODZ2N{Ow
SEM NYG5SIhTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX2xNEDPxE1? NWe3dmM5TE2VTx?= MkC3SWM2OD1{MEKgcm0> NH70eFYyQTB4NEezNC=>
KASUMI-2 MlnFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHnlVpYyOCEQvF2= MVXEUXNQ M2\LNGVEPTB;MkK1JI5O NWfu[lVlOTlyNkS3N|A>
REH Mn;qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGTiU3YyOCEQvF2= MWLEUXNQ NF30[phGSzVyPUK4PEBvVQ>? NWXoSWJzOTlyNkS3N|A>
697 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGDiOIwyOCEQvF2= M1j3fGROW09? NU[1ZpV6TUN3ME2zN|ghdk1? NYrnW5RZOTlyNkS3N|A>
NALM-6 M4H0OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYXJfFNROTBizszN MlnTSG1UVw>? MYrFR|UxRTR{MTDuUS=> NEfMRm0yQTB4NEezNC=>
MHH-CALL–3 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXqxNEDPxE1? NWnCeXdNTE2VTx?= MWLFR|UxRThzMjDuUS=> NVfNUolxOTlyNkS3N|A>
MHH-CALL–2 NYW2bnpIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnT5NVAh|ryP NXXC[GZZTE2VTx?= M2LCeGVEPTB;MkGxOEBvVQ>? M17TXFE6ODZ2N{Ow
J.GAMMA-1 NYrkXnk3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrTb29DOTBizszN MUDEUXNQ M3f0[WVEPTB;NkWgcm0> M1\kNlE6ODZ2N{Ow
JR45.01 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1fHWFExKM7:TR?= NVrVVoV{TE2VTx?= M{HWbGVEPTB;Nkigcm0> NYOzOFU5OTlyNkS3N|A>
A3 MorES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWnnPI5ZOTBizszN NUfLVmZ{TE2VTx?= MYTFR|UxRTZ7IH7N NVvlUXRFOTlyNkS3N|A>
I 2.1 MmHwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV3IRoc4OTBizszN NV:0fIROTE2VTx?= Mn\QSWM2OD15MzDuUS=> MYSxPVA3PDd|MB?=
MOLT-3 NXXkdJRsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmPkNVAh|ryP NXzKWVE6TE2VTx?= NHjKXW1GSzVyPUe0JI5O M4\zWFE6ODZ2N{Ow
P116 NVG0flRLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVexNEDPxE1? MlXRSG1UVw>? NXvhWYxITUN3ME23PEBvVQ>? MYOxPVA3PDd|MB?=
J.Cam1.6 Ml7aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEPq[JQyOCEQvF2= NXThSmc{TE2VTx?= NFiyc|BGSzVyPUe5JI5O NF7ETXEyQTB4NEezNC=>
I 9.2 NXG0W2E2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXOxNEDPxE1? NFP3SGRFVVOR M2rPPWVEPTB;OECgcm0> NVH2WWM2OTlyNkS3N|A>
LOUCY Mn65S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NICyfFIyOCEQvF2= NYK0eYFWTE2VTx?= MnXmSWM2OD1zMUegcm0> Mk[zNVkxPjR5M{C=
J.RT3-T3.5 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlGyNVAh|ryP MVjEUXNQ MVPFR|UxRTF{MzDuUS=> NVnjOnJ1OTlyNkS3N|A>
800000 NVvocXNLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWWxNEDPxE1? NI\B[ZVFVVOR NEL6UFBGSzVyPUG2N{BvVQ>? MWexPVA3PDd|MB?=
Jurkat NXHRWmNKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFH2bnAyOCEQvF2= NGPj[mNFVVOR MmDGSWM2OD1{MkWgcm0> MUGxPVA3PDd|MB?=
MOLT-4 NILUeHdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUWxNEDPxE1? MnT6SG1UVw>? MVHFR|UxRTJ|MjDuUS=> MVexPVA3PDd|MB?=
Molt-16 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXzO[GtHOTBizszN NGXKbGtFVVOR NY\6RlR1TUN3ME2yOFEhdk1? Mkf1NVkxPjR5M{C=
CEM/C3 M1vFeWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXKxNEDPxE1? NXjicVJvTE2VTx?= NIPa[5VGSzVyPUK1O{BvVQ>? NHHFO2IyQTB4NEezNC=>
CEM/C2 NYrtR2RrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHXDNWIyOCEQvF2= MmPBSG1UVw>? NYrm[|ZQTUN3ME2yO|Ehdk1? MWWxPVA3PDd|MB?=
CCRFCEM M3\qe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWGxNEDPxE1? NXjjT2Z5TE2VTx?= MlrvSWM2OD1|Mkegcm0> MmTmNVkxPjR5M{C=
CEM/C1 NUHmb3lnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG\lSHEyOCEQvF2= MmjWSG1UVw>? MXjFR|UxRTN6MjDuUS=> NXzITnJqOTlyNkS3N|A>
SUPTI[VB] MljQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXSxNEDPxE1? NHTKUoxFVVOR NIjNemJGSzVyPU[xPUBvVQ>? M1TXbVE6ODZ2N{Ow
CCRF–HSB-2 MlXxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVixNEDPxE1? NFj0NYRFVVOR NXLuNItYTUN3ME2yNVE4KG6P M4\w[|E6ODZ2N{Ow
I 2.1 MoKwRZBweHSxc3nzJIF{e2G7 M4jSOlExKM7:TR?= M3LVW2ROW09? MofkbY5lfWOnczDhdI9xfG:|aYO= MnmxNVkxPjR5M{C=
I 9.2 NUDWfJFQSXCxcITvd4l{KGG|c3H5 MmHRNVAh|ryP NXrTO2FITE2VTx?= NHS3VFBqdmS3Y3XzJIFxd3C2b4Ppdy=> M1nIOlE6ODZ2N{Ow
A3 M4TkOmFxd3C2b4Ppd{Bie3OjeR?= MVqxNEDPxE1? NWrL[5VJTE2VTx?= M1XoV4lv\HWlZYOgZZBweHSxc3nz NIjqTYcyQTB4NEezNC=>
RD M3rEbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3kNYpoOTBizszN NXzPWGZ2UUN3ME6xNEDPxE1? MXOyNFc1ODZ{Mx?=
Rh41 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH3oc4gyOCEQvF2= NWKyd5lPUUN3ME2zN{45KG6P NEL6SI0zODd2ME[yNy=>
Rh18 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlfJNVAh|ryP Ml\6TWM2OD1|MEOgcm0> NV21SIdNOjB5NEC2NlM>
Rh30 NFPiNYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\UNVAh|ryP NUX5d|hnUUN3ME20MlgyKM7:TR?= M1TPXVIxPzRyNkKz
BT-12 NHjpfGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGixTHQyOCEQvF2= MkLrTWM2OD5zMDFOwG0> NHn4OmwzODd2ME[yNy=>
CHLA-266 NY\pR5JRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zzc|ExKM7:TR?= NV\UVHkxUUN3ME2xMlIzKM7:TR?= MXSyNFc1ODZ{Mx?=
TC-71 NXTYTmhHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlXjNVAh|ryP NIq2dYtKSzVyPUKuOVIh|ryP NIHLPYEzODd2ME[yNy=>
CHLA-9 M37RTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWmxNEDPxE1? M2fiemlEPTB;NUmxJI5O M2LsNlIxPzRyNkKz
CHLA-10 M13DcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2rzXVExKM7:TR?= M2m5UmlEPTB;MUCyJI5O MYSyNFc1ODZ{Mx?=
CHLA-258 M13Tb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXW3[286OTBizszN MXPJR|UxRTFwMEWg{txO NYXzUpZVOjB5NEC2NlM>
GBM2 Mnf6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{D4elExKM7:TR?= NXy3OWRQUUN3ME25MlE2KM7:TR?= MlvENlA4PDB4MkO=
NB-1643 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn63NVAh|ryP Moq3TWM2OD13LkSg{txO MX6yNFc1ODZ{Mx?=
NB-Ebc1 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1;nUlExKM7:TR?= NX7O[GtxUUN3ME6xNEDPxE1? MonBNlA4PDB4MkO=
CHLA-90 NXjRS3NMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmPpNVAh|ryP NGD6[VZKSzVyPkGwJO69VQ>? M1TqNlIxPzRyNkKz
CHLA-136 NUjJSpJxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVPkRpF2OTBizszN NFLJPHRKSzVyPkGwJO69VQ>? MmDCNlA4PDB4MkO=
NALM-6 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUKxNEDPxE1? M3ztemlEPTB;Mk[1JI5O M2m0TVIxPzRyNkKz
COG-LL-317 MlLnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYmxNEDPxE1? M3:4NmlEPTB;Nj60PUBvVQ>? MYCyNFc1ODZ{Mx?=
RS4;11 M4LmXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFnY[|AyOCEQvF2= M2fadGlEPTB;MUS3JI5O NXn5TI42OjB5NEC2NlM>
MOLT-4 M2nUS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1XBNVExKM7:TR?= NGPNcmpKSzVyPUSwJI5O NVTtPJFmOjB5NEC2NlM>
CCRF-CEM M4S5[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX[xNEDPxE1? MorOTWM2OD1{Nkigcm0> NXq3TlFnOjB5NEC2NlM>
Kasumi-1 NH7aTXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEnreIcyOCEQvF2= M1jveGlEPTB;MUC3JI5O MWeyNFc1ODZ{Mx?=
Karpas-299 NXPNTIxXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zo[lExKM7:TR?= MmTKTWM2OD1{LkmzJO69VQ>? NX34Z|NvOjB5NEC2NlM>
Ramos-RA1 NFnJTFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NITy[3YyOCEQvF2= M3GzNGlEPTB;Nz6zOUDPxE1? MVyyNFc1ODZ{Mx?=
H1299 NY\VNYlsU2mwYYPlJIF{e2G7 MVixNEDPxE1? NIXybohqdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v NV\T[pRjOjF7MEi2NVY>

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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

Molarity Calculator

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

Related c-Met Products

Tags: buy Tivantinib (ARQ 197) | Tivantinib (ARQ 197) supplier | purchase Tivantinib (ARQ 197) | Tivantinib (ARQ 197) cost | Tivantinib (ARQ 197) manufacturer | order Tivantinib (ARQ 197) | Tivantinib (ARQ 197) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID