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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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

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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 NVvZXIU5U2mwYYPlJIF{e2G7 NGjVWnp,OTBizszN NHuwO5lqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz MmT1NlA1QDRyMUi=
HT29 MVrLbY5ie2ViYYPzZZk> MmPDglExKM7:TR?= Ml7IbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MoPjNlA1QDRyMUi=
MDA-MB-231 MWnLbY5ie2ViYYPzZZk> NXnybItThjFyIN88US=> NWrjeVRVcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NXrO[HAxOjB2OESwNVg>
NCI-H441 MXLLbY5ie2ViYYPzZZk> M{fqSZ4yOCEQvF2= M4D1PIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NF3PSWEzODR6NECxPC=>
SK-MEL-28 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlLpN|Mh|ryP M{XyZ2lEPTB-M{Og{txO NUK4bHN2OjB2OESwNVg>
NCI-H661 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWHmW3N{OzNizszN NVzQdXFUUUN3ME6zN{DPxE1? NHnnNmkzODR6NECxPC=>
NCI-H446 MoXMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3fWZ|M{KM7:TR?= MV3JR|UxRTdizszN MWmyNFQ5PDBzOB?=
MDA-MB-231 NH;wfJhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGe3O2Y{OyEQvF2= M2H5fWlEPTB;MD61OUDPxE1? NIH2T44zODR6NECxPC=>
DLD-1 NHHPWINIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWDkU3JOOzNizszN M1HRb2lEPTB;MD61N{DPxE1? NVLq[YhIOjB2OESwNVg>
A549 NECx[GdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXfBd29nOzNizszN NWPo[WJpUUN3ME2wMlU6KM7:TR?= NGnyfoczODR6NECxPC=>
SK-OV-3 NFLLdmpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWH2[JVFOzNizszN M2fVS2lEPTB;MD62OkDPxE1? MYGyNFQ5PDBzOB?=
NCI-H460 NVXaWYFtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2G3U|M{KM7:TR?= NG\KbI1KSzVyPUCuOkDPxE1? NFzSZowzODR6NECxPC=>
A375 M2XyNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3juPFM{KM7:TR?= NVzUO2N5UUN3ME2wMlQzKM7:TR?= M2nCRVIxPDh2MEG4
NCI-H441 NHOwVWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWCzN{DPxE1? MWLJR|UxRTBwMzFOwG0> MV2yNFQ5PDBzOB?=
HT29 MoDBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1LsUlM{KM7:TR?= MWrJR|UxRTBwNEmg{txO MYSyNFQ5PDBzOB?=
MKN-45 NIDhNZdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn61N|Mh|ryP Ml3YTWM2OD1yLkW4JO69VQ>? NXzL[5B6OjB2OESwNVg>
HT29 NEPLN41CeG:ydH;zbZMh[XO|YYm= MmTkglExKM7:TR?= MXPzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NIrRc|IzODR6NECxPC=>
MKN-45 MYjBdI9xfG:|aYOgZZN{[Xl? MW\+NVAh|ryP MV\zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? NV7zZWZwOjB2OESwNVg>
MDA-MB-231 M{TubGFxd3C2b4Ppd{Bie3OjeR?= NWfEfm86hjFyIN88US=> NVL5RphKdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> NFHEeZczODR6NECxPC=>
MDA-MB-231/TGL M4XHdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWTXe2xuhjFyMDFOwG0> NWDs[2V7T0l3ME2xMlIh|ryP MWmyNlAzPzZ7MB?=
1833/TGL NFj5RVBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWr+NVAxKM7:TR?= NXK5SHBZT0l3ME2zMlch|ryP M1XBS|IzODJ5Nkmw
EBC1 NYjqUVNnS3m2b4TvfIlkyqCjc4PhfS=> NXq4[5RshjFyIN88US=> MWDpcohq[mm2czD0bIUh[2WubDDndo94fGhw MXOyN|U6QDJ5Nh?=
SNU638 NVPPS4tnS3m2b4TvfIlkyqCjc4PhfS=> NEG5d5N,OTBizszN Mo[wbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqLh?= MU[yN|U6QDJ5Nh?=
A549 M1vlWmN6fG:2b4jpZ:Kh[XO|YYm= MmnKglExKM7:TR?= NYm3do1sdm:2IHHm[oVkfA>? MorjNlM2QTh{N{[=
H460 MkPrR5l1d3SxeHnjxsBie3OjeR?= MYT+NVAh|ryP NYC3eoltdm:2IHHm[oVkfA>? NIf2eVAzOzV7OEK3Oi=>
HCC827 NEXaTZBEgXSxdH;4bYPDqGG|c3H5 MVf+NVAh|ryP MWXuc5Qh[W[oZXP0 NGXQZ4szOzV7OEK3Oi=>
A549 NFXMd3JHfW6ldHnvckBie3OjeR?= M{XUPVExKM7:TR?= MnLC[Il{enWydIOgcYlkem:2dXL1cIU> NYTVcFBIOjN3OUiyO|Y>
EBC1 MojpSpVv[3Srb36gZZN{[Xl? MWOxNEDPxE1? M4H2Z4Rqe3K3cITzJI1q[3KxdIXieYxm MUmyN|U6QDJ5Nh?=
H460 NFLvTHNHfW6ldHnvckBie3OjeR?= M17RdVExKM7:TR?= MnLPbY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? NXi4dJNFOjV|MUOwNVA>
K562/VCR M1jlPGN6fG:2b4jpZ:Kh[XO|YYm= MWT+NVAh|ryP M4HLe5Npd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= NWn1UohmOjV|MUOwNVA>
CEM/VBL M3PxNGN6fG:2b4jpZ:Kh[XO|YYm= MnjpglExKM7:TR?= Ml3qd4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 NXPPc4tIOjV|MUOwNVA>
U266 MoLCR5l1d3SxeHnjxsBie3OjeR?= M4exPJ4{KM7:TdMg MnLMTWM2OD1zLkGg{txO MVyyOVgyODBzMx?=
OPM-2 NXzT[JBqS3m2b4TvfIlkyqCjc4PhfS=> MWr+N{DPxE4EoB?= NFf0VGpKSzVyPUGuPEDPxE1? M2DmXVI2QDFyMEGz
MM.1S MYXDfZRwfG:6aXRCpIF{e2G7 NYLsZlZNhjNizszNxsA> M2\QdGlEPTB;MT62JO69VQ>? NUDSNHFOOjV6MUCwNVM>
MM.1R NGe5UWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4fSS|Mh|ryPwrC= MlTIbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml M4\RflI2QDFyMEGz
RPMI-8226 MnTkR5l1d3SxeHnjxsBie3OjeR?= MnLKglMh|ryPwrC= M2XDUmlEPTB;MD65JO69VQ>? MXqyOVgyODBzMx?=
ANBL-6 MXnDfZRwfG:6aXRCpIF{e2G7 M3viXVEh|ryPwrC= NEnle3hqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NEDy[pgzPThzMECxNy=>
ANLB-6/V10R MWnDfZRwfG:6aXRCpIF{e2G7 NWfIfY54OSEQvF5CpC=> NXrG[Wx2cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NWTIUIltOjV6MUCwNVM>
KAS-6/1 NHjHemZEgXSxdH;4bYPDqGG|c3H5 NHmw[osyKM7:TdMg NFrpUZZqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NVnE[I1pOjV6MUCwNVM>
KAS-6/V10R MU\DfZRwfG:6aXRCpIF{e2G7 MYOxJO69VcLi MWfpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MmG2NlU5OTByMUO=
KAS-6/R10R NHX0dHZEgXSxdH;4bYPDqGG|c3H5 Mk\FNUDPxE4EoB?= M{P2TIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NWW0fo1rOjV6MUCwNVM>
8226/S MkHvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYWzJO69VcLi MnHwbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl Mmf6NlU5OTByMUO=
8226/LR-5 Mlr6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVSzJO69VcLi MXrpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= MYWyOVgyODBzMx?=
Huh7 NXPjfVk2S3m2b4TvfIlkyqCjc4PhfS=> NV7ZZ4E1hjRwODFOwG3DqA>? NHnHWJhFVVOR MXnJR|UxRTlwOTDuUS=> NYLhbopsOjZ{NUmyOVA>
Hep3B NHrDWHlEgXSxdH;4bYPDqGG|c3H5 M1H6fJ41NjhizszNxsA> MUTEUXNQ M{fMeGlEPTB;NES4Mlchdk1? MoDKNlYzPTl{NUC=
HepG2 NX3q[W1NS3m2b4TvfIlkyqCjc4PhfS=> Mk\QglQvQCEQvF5CpC=> MkG0SG1UVw>? NY\WVml6UUN3ME2xN|kvPzdibl2= M3HKVlI3OjV7MkWw
Chang M13IeWN6fG:2b4jpZ:Kh[XO|YYm= MVL+OE45KM7:TdMg NUXrTotQTE2VTx?= M3W5[WlEPTB;NES4Mlchdk1? M1vJdlI3OjV7MkWw
Huh7 M{[yeWZ2dmO2aX;uJIF{e2G7 MkHRNU43KM7:TdMg M2\IUGROW09? Mn;pZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NYLTU4VJOjZ{NUmyOVA>
Hep3B NF7lTFBHfW6ldHnvckBie3OjeR?= M2\pbFEvPiEQvF5CpC=> M2rJ[WROW09? MlH1Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? Mmi2NlYzPTl{NUC=
HepG2 NXn3V5VrTnWwY4Tpc44h[XO|YYm= Mn7RNU43KM7:TdMg NHzQRldFVVOR M2TBd4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NGr2SJMzPjJ3OUK1NC=>
Chang MlizSpVv[3Srb36gZZN{[Xl? M2HzSlEvPiEQvF5CpC=> Mn20SG1UVw>? MV7jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NWrONpRiOjZ{NUmyOVA>
MHCC97L MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILpe2F,OTBizszN NGDGSnRFVVOR MV;JR|UxRTNzNTDuUS=> NIT4b5czPjR3OEm1Ny=>
MHCC97H Ml\RS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoLIglExKM7:TR?= M3LyOWROW09? NI[2fI5KSzVyPUO2PQKBkSCwTR?= MmG3NlY1PTh7NUO=
Huh7 MkD0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\qe54yOCEQvF2= NWXPWZhGTE2VTx?= MXPJR|UxRTJ4NTDuUS=> NE\YPJAzPjR3OEm1Ny=>
HepG2 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVr+NVAh|ryP MnnJSG1UVw>? MnzJTWM2OD1|OUKgcm0> NVf1eGh6OjZ2NUi5OVM>
MHCC97L MnjXSpVv[3Srb36gZZN{[Xl? MnjWNUDPxE4EoB?= NXroUolITE2VTx?= NWTYbXlQcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NHTJSXMzPjR3OEm1Ny=>
Huh7 MmTSSpVv[3Srb36gZZN{[Xl? MVmxJO69VcLi NGnvR5VFVVOR NVjqc5dMcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NGmyRWEzPjR3OEm1Ny=>
MHCC97L NHjlVlRCeG:ydH;zbZMh[XO|YYm= NIrEUYoyKM7:TdMg MoDJSG1UVw>? Mn;3bY5lfWOnczDhdI9xfG:|aYO= MUGyOlQ2QDl3Mx?=
Huh7 MXXBdI9xfG:|aYOgZZN{[Xl? MUKxJO69VcLi NIrFbIRFVVOR Mo\FbY5lfWOnczDhdI9xfG:|aYO= NHzBW2YzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts NXXyNlNpU2mwYYPlJIF{e2G7 Moq0NlUh|ryP M1jySGROW09? MV3y[YR2[2W|IFjpd5RwdmViSEOgZY5lKEh2IHHj[ZR6dGG2aX;uJIxmfmWuc9Mg NYn0R5k{OjB3M{SzOFU>
H23 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVX5Z3F1OjVizszN M3[1d2ROW09? NXPTRXFWe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> M1rrTVIxPTN2M{S1
WM35 MnSxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkLJNVAh|ryP MUjEUXNQ MnHod4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= Mn61NlA2OzR|NEW=
NIH 3T3 MoXkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoHJNVAh|ryP NGrQUYtFVVOR M2DhUIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NGCxU4QzODV|NEO0OS=>
H838 M2\u[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUCxNEDPxE1? NF76cYpFVVOR NVPXblc2\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MYSyNFU{PDN2NR?=
H1395 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXPze3g2OTBizszN NX36UWtkTE2VTx?= MoPh[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NEe4bHYzODV|NEO0OS=>
Quiescent S2 NX;sbJptU2mwYYPlJIF{e2G7 NH31bo0{OCEQvF2= M4nZemROW09? MoXzZ49ueGyndHXsfUBi[nKxZ3H0[ZMhXFODLXnu[JVk\WRiaInw[ZJi[2W2eXzheIlwdiCxZjDIN2s1dWV|IHjpd5RwdmW| NGDwdJczOTVzOEmxOS=>
PC3 NILGd4lCeG:ydH;zbZMh[XO|YYm= MnzwNlAh|ryP Mki4SG1UVw>? MX7pcoR2[2W|IHHwc5B1d3Orcx?= NWHRUWN1OjF5MEmxN|A>
Du145 MkXvRZBweHSxc3nzJIF{e2G7 M1f4eFIxKM7:TR?= MmfqSG1UVw>? MoL2bY5lfWOnczDhdI9xfG:|aYO= MkniNlE4ODlzM{C=
LNCaP MWLBdI9xfG:|aYOgZZN{[Xl? M3;oOlIxKM7:TR?= M{fqSGROW09? MojnbY5lfWOnczDhdI9xfG:|aYO= MnnaNlE4ODlzM{C=
LAPC-4 NYfRPVh[SXCxcITvd4l{KGG|c3H5 NV\aXml3OjBizszN NVy3T4tuTE2VTx?= MlznbY5lfWOnczDhdI9xfG:|aYO= MWeyNVcxQTF|MB?=
LNCaP Mn2xSpVv[3Srb36gZZN{[Xl? NHzY[ZQzOCEQvF2= MYjEUXNQ M{jkOIRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? MVeyNVcxQTF|MB?=
LAPC-4 NUD5[m5KTnWwY4Tpc44h[XO|YYm= MUKyNEDPxE1? MWDEUXNQ NGr3OWhl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NV7BXYZTOjF5MEmxN|A>
Kasumi-1 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVH+OVAh|ryP MmXoSG1UVw>? NUm2eHhCcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NH3YOYczOzN7MEWzOi=>
SKNO-1 NI\ORZFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlPuglUxKM7:TR?= NXP3cYVrTE2VTx?= NVTjbmhWcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NFPpWXIzOzN7MEWzOi=>
Kasumi-1 MW\LbY5ie2ViYYPzZZk> NX;zTZRohjFyIN88US=> MoDXSG1UVw>? NHHsR41z\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> MoHNNlM{QTB3M{[=
SKNO-1 M4rLWWtqdmG|ZTDhd5NigQ>? NVXjfJFQhjFyIN88US=> NX\UfmpQTE2VTx?= MnXhdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NXPNcm95OjN|OUC1N|Y>
A549 NWjzSHhoTnWwY4Tpc44h[XO|YYm= M1\xd|ExKM7:TR?= MX;EUXNQ MnPG[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> M4HBbVI1PzR4NUe0
NRK-52E MkfuSpVv[3Srb36gZZN{[Xl? MXixNEDPxE1? MX\EUXNQ NHfyO3dqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDTWGFVOyCwdXPs[YFzKHS{YX7zcI9k[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKFSJRj5OtlEtKGOxbHzh[4VvKEmYIHHu[EBncWK{b37lZ5Rqdg>? MorINlUxQDhyMEK=
PC12 NIKyVodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoroglEzNjVizszN NGG5SXhFVVOR MX3wdoV3\W62czDUV2EucW6mdXPl[EBv\XW{aYTlJIZwem2jdHnvci=> NGOwT5UzPTF{OEO4Oi=>
HPMCs NUjOR4JITnWwY4Tpc44h[XO|YYm= MoDvdoV3\XK|ZYOg[ZBqfGinbHnhcEB1dyCvZYPlcoNpgW2jbDD0doFve2m2aX;uJI9nKGi3bXHuJJBmemm2b37lZYwhdWW|b4To[Yxq[WxiY3XscJM> NVTicJBIOjZyNEW3PFA>
A549 MmfOSpVv[3Srb36gZZN{[Xl? MnTvglUxKM7:TR?= M{f2bWROW09? NGHEVZFi\m[nY4TzJJRp\SC4aYLhcEBtcW[nIHP5Z4xmKGGwZDDoc5N1KHKnc4DvcpNm NFrldI8zPjdzMUe0PC=>
RAW264.7 MkLLSpVv[3Srb36gZZN{[Xl? MWD+N|Ah|ryP MmLRSG1UVw>? NG\oRlFz\WS3Y3XzJJBzdy2rbn\sZY1u[XSxcomg[4Vv\SCneIDy[ZN{cW:w MoS2NlY4OTh3OE[=
MEMM NVHsSnpzU2mwYYPlJIF{e2G7 NYDTdJMzOTViwsXN MYHEUXNQ M{nMU4Rm[3KnYYPld{Bi[2W2eXzheIlwdiCxZjDobZN1d26nIFiz MUmyOlkzOTVyNh?=
MEMM NVvYOoR7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2nrT54zOCEEtV2= MYrEUXNQ M4i3fYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NYTleolMOjZ7MkG1NFY>
MEMM Mmm1RZBweHSxc3nzJIF{e2G7 MlTiNVUhyrWP M4LsZ2ROW09? M{jNVolv\HWlZYOgeIhmKHC{ZYPlcoNmKG:oIITo[UBieG:ydH;zbZMheHKxdHXpckwh[2ynYY\l[EBE[XOyYYPlMVM> M3POc|I3QTJzNUC2
T47D MkW1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWWxNEDPxE1? MY\EUXNQ NH\nfmNKSzVyPUeyJI5O M1\0PFE5OzhzNES0
ZR-75-1 NFLsUWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUfpeZdROTBizszN NVj1[2xYTE2VTx?= MV\JR|UxRTd7IH7N M{\CPFE5OzhzNES0
BT474 M1TQXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmjBNVAh|ryP MYLEUXNQ MV3JR|UxRTh4IH7N MUGxPFM5OTR2NB?=
HCC1954 MnrHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFHaO4syOCEQvF2= NH:2U5NFVVOR NXHY[GJwUUN3ME2xNVkhdk1? NWrv[Y5HOTh|OEG0OFQ>
MDA-MB-453 NHnTWVhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGW4NVYyOCEQvF2= NV:5OZhQTE2VTx?= NYjHZo9PUUN3ME25O|Uhdk1? Mni1NVg{QDF2NES=
MDA-MB-468 M3LiUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{L2PVExKM7:TR?= MYHEUXNQ M3rLWGlEPTB;M{KwPEBvVQ>? M12w[VE5OzhzNES0
SkBr3 MkH4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmXQNVAh|ryP MnrmSG1UVw>? MnnzTWM2OD5zMDywNFAhdk1? M2P3RVE5OzhzNES0
MDA-MB-231 NHvXbWtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGrSWHgyOCEQvF2= NHnZTopFVVOR MlTWTWM2OD5zMDywNFAhdk1? NVfMVZJJOTh|OEG0OFQ>
HCT116 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHXJTWoyOCEQvF2= NVP5[YR3TE2VTx?= MWHJR|UxRTV6M{[gcm0> M3z6b|E5OzhzNES0
HT29 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkXKNVAh|ryP NIjm[2hFVVOR NFfaNINKSzVyPkGwMFAxOCCwTR?= MkPMNVg{QDF2NES=
HFF M3yyRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYr5OZJTOTBizszN MUjEUXNQ M3vYfmlEPTB;N{[xOUBvVQ>? NXrIc|VqOTh|OEG0OFQ>
HN5 NIj4cFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEjwT|gyOCEQvF2= NHrLUo1FVVOR MVrJR|UxRjFyLECwNEBvVQ>? M4fGRVE5OzhzNES0
786-0 NULZWlZnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHzVb3UyOCEQvF2= MkjmSG1UVw>? NWHpTXVMUUN3ME20NFA6KG6P MWSxPFM5OTR2NB?=
H157 M3jlTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF\UNoUyOCEQvF2= NWHVO3NlTE2VTx?= M{DqVWlEPTB;Mk[0NkBvVQ>? MVmxPFM5OTR2NB?=
NCI-H460 NYrQOmhyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYKxNEDPxE1? MYXEUXNQ M2\ESmlEPTB-Mjy1NFAhdk1? NXiyWnQ5OTh|OEG0OFQ>
SKOV-3 MnXzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVP0Z3J{OTBizszN MUDEUXNQ MX\JR|UxRTJzMk[gcm0> NV7N[WpHOTh|OEG0OFQ>
OVCAR-3 MkXWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3WycFExKM7:TR?= MnXsSG1UVw>? M4XnbWlEPTB;MkmxPEBvVQ>? M1exOVE5OzhzNES0
BXPC3 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mkj2NVAh|ryP NF;GTJVFVVOR MmH1TWM2OD1|MUSxJI5O MVGxPFM5OTR2NB?=
MiaPaCa M2DTUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWGxNEDPxE1? MoXISG1UVw>? NIjhb3hKSzVyPUW0N|Mhdk1? MXmxPFM5OTR2NB?=
PANC-1 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHTWXpoyOCEQvF2= MXXEUXNQ NHf5XGpKSzVyPUi2PFEhdk1? MUGxPFM5OTR2NB?=
LNCaP NGPXcIlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4DtU|ExKM7:TR?= M{jOc2ROW09? MkDiTWM2OD1zNEegcm0> M2[0S|E5OzhzNES0
DU145 M4nONGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW[4dY1{OTBizszN NHvOPWVFVVOR MV\JR|UxRTN6MUKgcm0> M123b|E5OzhzNES0
PC3 NYnYdnNrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlLINVAh|ryP MYfEUXNQ M2HDTWlEPTB-MUCsNFAxKG6P NV3NXYVzOTh|OEG0OFQ>
BT474 NVHBd|hQU2mwYYPlJIF{e2G7 Mn;VNVAh|ryP MmS5SG1UVw>? NU\3XIh{cW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMU[wJI5O M1LCWFE5OzhzNES0
786-0 NWj5[IZ5U2mwYYPlJIF{e2G7 M3nKTlExKM7:TR?= MmTWSG1UVw>? M{TLcolvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> MmjuNVg{QDF2NES=
LNCaP MWfLbY5ie2ViYYPzZZk> NGDtXpYyOCEQvF2= MV\EUXNQ M1rPVolvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR|IH7N MnLkNVg{QDF2NES=
PC3 MorHT4lv[XOnIHHzd4F6 NWnoZWd3OTBizszN MWjEUXNQ NIXu[JdqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2OTDuUS=> M3LKXlE5OzhzNES0
KARPAS-231 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFXLb4cyOCEQvF2= M1n6emROW09? NVfJOXlCTUN3ME20NUBvVQ>? MkH5NVkxPjR5M{C=
CCRFSB NULYV3F6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUHvXmlWOTBizszN MoLDSG1UVw>? Mn;vSWM2OD1zNUWgcm0> M3K4TFE6ODZ2N{Ow
SUP B15 M3nUfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnfVNVAh|ryP M1rxXmROW09? MlPESWM2OD1zOUegcm0> M{jpZlE6ODZ2N{Ow
SD-1 NV3VTHJHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYLVOWFUOTBizszN MmC4SG1UVw>? NGfsc41GSzVyPUOyNEBvVQ>? Mn7BNVkxPjR5M{C=
RS4;11 MlrCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MljENVAh|ryP M2TxVGROW09? M2flVmVEPTB;NkW0JI5O NVe0e5RWOTlyNkS3N|A>
MN-60 NITkOmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVHoRmlQOTBizszN NInMU45FVVOR MoPlSWM2OD1|NkCyJI5O MVyxPVA3PDd|MB?=
Tanoue NVLvWGtXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1O1WVExKM7:TR?= MYnEUXNQ NYT3WINvTUN3ME20OVE4KG6P NEnMc|QyQTB4NEezNC=>
RCH-ACV MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1\NflExKM7:TR?= NH\0d2lFVVOR NFi3VGxGSzVyPUG1NkBvVQ>? M1;xS|E6ODZ2N{Ow
SEM NUGwVItZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlvINVAh|ryP MnzYSG1UVw>? MkDvSWM2OD1{MEKgcm0> M{XTZlE6ODZ2N{Ow
KASUMI-2 M1PyRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYH0UnlzOTBizszN MVLEUXNQ NEnKSmhGSzVyPUKyOUBvVQ>? M{Hz[VE6ODZ2N{Ow
REH M2HaO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWDDcHV3OTBizszN M4rYZmROW09? NX3hSJhZTUN3ME2yPFghdk1? MXqxPVA3PDd|MB?=
697 Mn;VS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH71[20yOCEQvF2= NF;uPW9FVVOR MmX0SWM2OD1|M{igcm0> M3HWSVE6ODZ2N{Ow
NALM-6 MoPZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFLHcW0yOCEQvF2= NHrpZlRFVVOR MVzFR|UxRTR{MTDuUS=> MXGxPVA3PDd|MB?=
MHH-CALL–3 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MofBNVAh|ryP NWfpUpNrTE2VTx?= M1fiemVEPTB;OEGyJI5O NHPEOIUyQTB4NEezNC=>
MHH-CALL–2 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXSxNEDPxE1? Mn7iSG1UVw>? MYLFR|UxRTJzMUSgcm0> NWSxbpFWOTlyNkS3N|A>
J.GAMMA-1 M4XibWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX2xNEDPxE1? MV;EUXNQ MnzxSWM2OD14NTDuUS=> NHvLeWoyQTB4NEezNC=>
JR45.01 NX62fWdXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYWxNEDPxE1? NFvzNZZFVVOR NHTiT3dGSzVyPU[4JI5O NFLPXIgyQTB4NEezNC=>
A3 M1\LS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWmxNEDPxE1? M1ix[2ROW09? MXHFR|UxRTZ7IH7N M1vKXVE6ODZ2N{Ow
I 2.1 M2Xkfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVSxNEDPxE1? NWXyXJYzTE2VTx?= MlnTSWM2OD15MzDuUS=> M1PzdlE6ODZ2N{Ow
MOLT-3 NHLqV29Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLBeXp5OTBizszN M17jWGROW09? NFHMN29GSzVyPUe0JI5O NEK1b4IyQTB4NEezNC=>
P116 MoPLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYf5OHo6OTBizszN MVnEUXNQ M4\zTmVEPTB;N{igcm0> MlPVNVkxPjR5M{C=
J.Cam1.6 M{TIR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFy0NFYyOCEQvF2= MojySG1UVw>? M4n0T2VEPTB;N{mgcm0> MYKxPVA3PDd|MB?=
I 9.2 M3r1dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFS0bYQyOCEQvF2= NYfZZVBTTE2VTx?= MWPFR|UxRThyIH7N M3n1e|E6ODZ2N{Ow
LOUCY M{TUbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV[xNEDPxE1? NIDXU4pFVVOR Ml3PSWM2OD1zMUegcm0> MoLzNVkxPjR5M{C=
J.RT3-T3.5 NY\WflZnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVvhZ5lvOTBizszN MlX6SG1UVw>? NFG2[mdGSzVyPUGyN{BvVQ>? NV3UeHBpOTlyNkS3N|A>
800000 NUTDXWFZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVnjdmdOOTBizszN NX70NGc3TE2VTx?= NGfCR3RGSzVyPUG2N{BvVQ>? NUPuSG1bOTlyNkS3N|A>
Jurkat NFPDXW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoP1NVAh|ryP M1zNdmROW09? Mn;uSWM2OD1{MkWgcm0> MmfaNVkxPjR5M{C=
MOLT-4 M3e4d2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoTmNVAh|ryP MVrEUXNQ NIjaWGNGSzVyPUKzNkBvVQ>? NXXFcYx6OTlyNkS3N|A>
Molt-16 NXu4blNST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFW3RYgyOCEQvF2= MWLEUXNQ M2fBTGVEPTB;MkSxJI5O MVSxPVA3PDd|MB?=
CEM/C3 M1zaSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mlu5NVAh|ryP NUPaUnlZTE2VTx?= NHztV3BGSzVyPUK1O{BvVQ>? M1nMZVE6ODZ2N{Ow
CEM/C2 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnH0NVAh|ryP NV;mOVVKTE2VTx?= M2TFRWVEPTB;MkexJI5O M{DtS|E6ODZ2N{Ow
CCRFCEM NWC5dW91T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{XC[|ExKM7:TR?= MmjtSG1UVw>? NIrrVmFGSzVyPUOyO{BvVQ>? NWXCS|I{OTlyNkS3N|A>
CEM/C1 NHTSWopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEXHZWwyOCEQvF2= MXTEUXNQ MYDFR|UxRTN6MjDuUS=> NGXpe48yQTB4NEezNC=>
SUPTI[VB] Ml:3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjVUnREOTBizszN NIO5SIZFVVOR M1PZeWVEPTB;NkG5JI5O NXPhRmJxOTlyNkS3N|A>
CCRF–HSB-2 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoTpNVAh|ryP NFfB[WpFVVOR NW\KPW13TUN3ME2yNVE4KG6P MoLlNVkxPjR5M{C=
I 2.1 MmXJRZBweHSxc3nzJIF{e2G7 MnfVNVAh|ryP Mof4SG1UVw>? MXzpcoR2[2W|IHHwc5B1d3Orcx?= MlewNVkxPjR5M{C=
I 9.2 NFrZc3hCeG:ydH;zbZMh[XO|YYm= NITmdZIyOCEQvF2= MVvEUXNQ MlXybY5lfWOnczDhdI9xfG:|aYO= MVGxPVA3PDd|MB?=
A3 Ml;RRZBweHSxc3nzJIF{e2G7 MXexNEDPxE1? M3S2cGROW09? MmHabY5lfWOnczDhdI9xfG:|aYO= NIHsNnUyQTB4NEezNC=>
RD MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1y3UFExKM7:TR?= M4mzPGlEPTB-MUCg{txO MmP1NlA4PDB4MkO=
Rh41 NWfzdHl2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{LFZlExKM7:TR?= NEKycnJKSzVyPUOzMlghdk1? M2n4dFIxPzRyNkKz
Rh18 M1jwdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{ewbFExKM7:TR?= NVTBPGZiUUN3ME2zNFMhdk1? MUCyNFc1ODZ{Mx?=
Rh30 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3zpc|ExKM7:TR?= NEXnN2dKSzVyPUSuPFEh|ryP NXfneo1VOjB5NEC2NlM>
BT-12 NVzLcHpmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF3G[FUyOCEQvF2= MoLqTWM2OD5zMDFOwG0> M{S1R|IxPzRyNkKz
CHLA-266 MoPYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1TGSlExKM7:TR?= NEPWclNKSzVyPUGuNlIh|ryP M{L5VVIxPzRyNkKz
TC-71 MkK4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NULnPItDOTBizszN Mn7GTWM2OD1{LkWyJO69VQ>? MlHtNlA4PDB4MkO=
CHLA-9 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn3xNVAh|ryP NULzW5d2UUN3ME21PVEhdk1? M1e2[lIxPzRyNkKz
CHLA-10 Ml3qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorhNVAh|ryP NFvIOFFKSzVyPUGwNkBvVQ>? MY[yNFc1ODZ{Mx?=
CHLA-258 NWi1[FlZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFfSOWsyOCEQvF2= NUPFbIx7UUN3ME2xMlA2KM7:TR?= MVuyNFc1ODZ{Mx?=
GBM2 NYjocHZlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWixNEDPxE1? MWLJR|UxRTlwMUWg{txO NGrY[mkzODd2ME[yNy=>
NB-1643 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2X4RVExKM7:TR?= M3jCTGlEPTB;NT60JO69VQ>? MVSyNFc1ODZ{Mx?=
NB-Ebc1 NUXwSoRwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkfYNVAh|ryP M3\3e2lEPTB-MUCg{txO M1HVWVIxPzRyNkKz
CHLA-90 M3rHbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFX4XlYyOCEQvF2= NED1TmVKSzVyPkGwJO69VQ>? NHOyO|czODd2ME[yNy=>
CHLA-136 Mn33S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXGxNEDPxE1? M3jYWWlEPTB-MUCg{txO MXiyNFc1ODZ{Mx?=
NALM-6 NHj0Z|ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV2xNEDPxE1? M{e5[2lEPTB;Mk[1JI5O NWfkXnd6OjB5NEC2NlM>
COG-LL-317 NYrvN3NkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUGxNEDPxE1? M4D4UWlEPTB;Nj60PUBvVQ>? NIPuNmIzODd2ME[yNy=>
RS4;11 NXT6UnRST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWSxNEDPxE1? MWHJR|UxRTF2NzDuUS=> NE\zSFkzODd2ME[yNy=>
MOLT-4 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYn5W2VJOTBizszN MWjJR|UxRTRyIH7N MWiyNFc1ODZ{Mx?=
CCRF-CEM M2\iZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWCxNEDPxE1? M{\RT2lEPTB;Mk[4JI5O M2nyWVIxPzRyNkKz
Kasumi-1 NVTDW3l3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4n1fFExKM7:TR?= MV;JR|UxRTFyNzDuUS=> M3r4VFIxPzRyNkKz
Karpas-299 NUmzTWg2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYixNEDPxE1? NELKZZdKSzVyPUKuPVMh|ryP NGflUIczODd2ME[yNy=>
Ramos-RA1 MoDNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVixNEDPxE1? M37OU2lEPTB;Nz6zOUDPxE1? M2PIN|IxPzRyNkKz
H1299 NVTRc5UxU2mwYYPlJIF{e2G7 Ml7INVAh|ryP NGXPNZZqdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v NGPGXoozOTlyOE[xOi=>

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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 <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

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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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID