Tivantinib (ARQ 197)

For research use only.

Catalog No.S2753

29 publications

Tivantinib (ARQ 197) Chemical Structure

CAS No. 905854-02-6

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. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. Phase 3.

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

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

Selleck's Tivantinib (ARQ 197) has been cited by 29 publications

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. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. 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 MVXLbY5ie2ViYYPzZZk> MYD+NVAh|ryP MXTpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NYLlOGJQOjB2OESwNVg>
HT29 M4fLOWtqdmG|ZTDhd5NigQ>? NEfMdFZ,OTBizszN MoHmbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MmPPNlA1QDRyMUi=
MDA-MB-231 NGO3ZWlMcW6jc3WgZZN{[Xl? MoLyglExKM7:TR?= M4PmSYlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= M{LyUFIxPDh2MEG4
NCI-H441 MmC3T4lv[XOnIHHzd4F6 NFe1bnl,OTBizszN NXf1NHBNcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MlXQNlA1QDRyMUi=
SK-MEL-28 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1\5e|M{KM7:TR?= MV7JR|UxRjN|IN88US=> MYGyNFQ5PDBzOB?=
NCI-H661 M4XGSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVWzN{DPxE1? MX;JR|UxRjN|IN88US=> M4XxOVIxPDh2MEG4
NCI-H446 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{jaeVM{KM7:TR?= NX7MUZRDUUN3ME23JO69VQ>? NIrIN3UzODR6NECxPC=>
MDA-MB-231 NX\ZNZhDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnnQN|Mh|ryP MoDnTWM2OD1yLkW1JO69VQ>? MmC1NlA1QDRyMUi=
DLD-1 NWTnZWxkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGHhOnQ{OyEQvF2= NUL6OZNxUUN3ME2wMlU{KM7:TR?= NWnaV2tMOjB2OESwNVg>
A549 NFTRNYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NG\Pb44{OyEQvF2= NET0cmVKSzVyPUCuOVkh|ryP NV3UWHplOjB2OESwNVg>
SK-OV-3 M{PNfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkfkN|Mh|ryP MVrJR|UxRTBwNk[g{txO NF72cXEzODR6NECxPC=>
NCI-H460 MkfBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFHFdmk{OyEQvF2= MWXJR|UxRTBwNjFOwG0> NUGwfo52OjB2OESwNVg>
A375 NIHyfYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGHTRoU{OyEQvF2= NWHJUVdzUUN3ME2wMlQzKM7:TR?= NXWzfI9zOjB2OESwNVg>
NCI-H441 M{f2WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3\zOlM{KM7:TR?= NVPEW403UUN3ME2wMlMh|ryP NHf0cYwzODR6NECxPC=>
HT29 MorxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUizN{DPxE1? MkfjTWM2OD1yLkS5JO69VQ>? MXKyNFQ5PDBzOB?=
MKN-45 NGC5PY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4\lR|M{KM7:TR?= MVPJR|UxRTBwNUig{txO NWDneWNLOjB2OESwNVg>
HT29 MoPoRZBweHSxc3nzJIF{e2G7 Mm\nglExKM7:TR?= MlLYd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MnHkNlA1QDRyMUi=
MKN-45 NGex[ZRCeG:ydH;zbZMh[XO|YYm= MWH+NVAh|ryP MWjzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? MYGyNFQ5PDBzOB?=
MDA-MB-231 NIHUe3BCeG:ydH;zbZMh[XO|YYm= NFjIcJl,OTBizszN NI\RUGpud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu NWfkUVF2OjB2OESwNVg>
MDA-MB-231/TGL NV;S[VVwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlr4glExOCEQvF2= M3GwdmdKPTB;MT6yJO69VQ>? NE[0XGkzOjB{N{[5NC=>
1833/TGL NEnhbnhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnPHglExOCEQvF2= MYfHTVUxRTNwNzFOwG0> MUSyNlAzPzZ7MB?=
EBC1 M1rGd2N6fG:2b4jpZ:Kh[XO|YYm= MXX+NVAh|ryP MW\pcohq[mm2czD0bIUh[2WubDDndo94fGhw MmHENlM2QTh{N{[=
SNU638 NYSzXXJRS3m2b4TvfIlkyqCjc4PhfS=> NVLy[FNqhjFyIN88US=> NHnqUYhqdmirYnn0d{B1cGViY3XscEBoem:5dHiu NX7oc3JyOjN3OUiyO|Y>
A549 NF7lS3dEgXSxdH;4bYPDqGG|c3H5 M4TZU54yOCEQvF2= M3rOdY5wfCCjZn\lZ5Q> MUGyN|U6QDJ5Nh?=
H460 MmTlR5l1d3SxeHnjxsBie3OjeR?= NFPSRXp,OTBizszN MkToco91KGGoZnXjeC=> NUPobWV1OjN3OUiyO|Y>
HCC827 NFjvOmhEgXSxdH;4bYPDqGG|c3H5 MVT+NVAh|ryP M3;Db45wfCCjZn\lZ5Q> MW[yN|U6QDJ5Nh?=
A549 NVP3OG5nTnWwY4Tpc44h[XO|YYm= NXvj[pRTOTBizszN NGq4SZFlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? MXqyN|U6QDJ5Nh?=
EBC1 MYLGeY5kfGmxbjDhd5NigQ>? NEPjVlIyOCEQvF2= Ml3s[Il{enWydIOgcYlkem:2dXL1cIU> MVSyN|U6QDJ5Nh?=
H460 NX30dm5kTnWwY4Tpc44h[XO|YYm= NWiyWnZ3OTBizszN NFzEbJVqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w M3L0V|I2OzF|MEGw
K562/VCR NX7Y[nhQS3m2b4TvfIlkyqCjc4PhfS=> MoWxglExKM7:TR?= M2fHOJNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= M1P1[|I2OzF|MEGw
CEM/VBL M4frZWN6fG:2b4jpZ:Kh[XO|YYm= MUn+NVAh|ryP NUfPXoFFe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NFPxS5czPTNzM{CxNC=>
U266 MWXDfZRwfG:6aXRCpIF{e2G7 MVf+N{DPxE4EoB?= MXLJR|UxRTFwMTFOwG0> MUiyOVgyODBzMx?=
OPM-2 MlrlR5l1d3SxeHnjxsBie3OjeR?= MlnBglMh|ryPwrC= M4fTRWlEPTB;MT64JO69VQ>? NFnPOFczPThzMECxNy=>
MM.1S MW\DfZRwfG:6aXRCpIF{e2G7 NIKwOYx,OyEQvF5CpC=> Mnj2TWM2OD1zLk[g{txO MViyOVgyODBzMx?=
MM.1R M4r5ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXfWXJI3OyEQvF5CpC=> NIP4OZNqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> MkTwNlU5OTByMUO=
RPMI-8226 NFv3UpVEgXSxdH;4bYPDqGG|c3H5 NFTmOm9,OyEQvF5CpC=> M1fIVmlEPTB;MD65JO69VQ>? NUnEPY5qOjV6MUCwNVM>
ANBL-6 M1rxfWN6fG:2b4jpZ:Kh[XO|YYm= MoPoNUDPxE4EoB?= MY\pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= Mn3SNlU5OTByMUO=
ANLB-6/V10R NHLBUXJEgXSxdH;4bYPDqGG|c3H5 NX;qbFQ{OSEQvF5CpC=> NXfOcXY4cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MkLtNlU5OTByMUO=
KAS-6/1 M{i1WGN6fG:2b4jpZ:Kh[XO|YYm= MX6xJO69VcLi NVz5NoJncW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NXTjXmhpOjV6MUCwNVM>
KAS-6/V10R M1TwdWN6fG:2b4jpZ:Kh[XO|YYm= Ml:3NUDPxE4EoB?= NUnu[IRzcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M4THTVI2QDFyMEGz
KAS-6/R10R M3HHR2N6fG:2b4jpZ:Kh[XO|YYm= NGqwfGUyKM7:TdMg MWnpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NW\neIQxOjV6MUCwNVM>
8226/S M4Xhfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmTZN{DPxE4EoB?= Mlf3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl M{jVWVI2QDFyMEGz
8226/LR-5 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4T2WlMh|ryPwrC= MVTpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NHX0[FczPThzMECxNy=>
Huh7 MVnDfZRwfG:6aXRCpIF{e2G7 NELQSIV,PC56IN88UeKh MkOwSG1UVw>? MX7JR|UxRTlwOTDuUS=> NEW0V2EzPjJ3OUK1NC=>
Hep3B M1TqUGN6fG:2b4jpZ:Kh[XO|YYm= M{L5VZ41NjhizszNxsA> M2OwUGROW09? NXe5eYdVUUN3ME20OFgvPyCwTR?= M2PlXVI3OjV7MkWw
HepG2 NFL4cXFEgXSxdH;4bYPDqGG|c3H5 NX7T[4QxhjRwODFOwG3DqA>? Mnv3SG1UVw>? NHzoUHVKSzVyPUGzPU44PyCwTR?= M2fld|I3OjV7MkWw
Chang NGHY[XFEgXSxdH;4bYPDqGG|c3H5 MVn+OE45KM7:TdMg MoXNSG1UVw>? NEXTOIZKSzVyPUS0PE44KG6P NUjpT3dIOjZ{NUmyOVA>
Huh7 MonWSpVv[3Srb36gZZN{[Xl? Ml;BNU43KM7:TdMg NV;mT3VNTE2VTx?= NUXmRYQ1[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M1rpXVI3OjV7MkWw
Hep3B MYfGeY5kfGmxbjDhd5NigQ>? NFjNPVIyNjZizszNxsA> NEPTT4FFVVOR M{TGTYNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? NYW1dplyOjZ{NUmyOVA>
HepG2 MnvFSpVv[3Srb36gZZN{[Xl? MVixMlYh|ryPwrC= NHL0VXdFVVOR NFzXd4Fk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MWGyOlI2QTJ3MB?=
Chang Mme4SpVv[3Srb36gZZN{[Xl? M3fDWlEvPiEQvF5CpC=> NHLJWIxFVVOR M164N4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MVyyOlI2QTJ3MB?=
MHCC97L M3LIU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2TmU54yOCEQvF2= MlfmSG1UVw>? M4GzR2lEPTB;M{G1JI5O NFHjbJgzPjR3OEm1Ny=>
MHCC97H M2DYSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLTglExKM7:TR?= M4LkRmROW09? MkLGTWM2OD1|NklihKkhdk1? MWKyOlQ2QDl3Mx?=
Huh7 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml3hglExKM7:TR?= NYrwbZBLTE2VTx?= NILlR|RKSzVyPUK2OUBvVQ>? M1O1b|I3PDV6OUWz
HepG2 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NITTWIt,OTBizszN MknoSG1UVw>? MUDJR|UxRTN7MjDuUS=> MXiyOlQ2QDl3Mx?=
MHCC97L Mlr6SpVv[3Srb36gZZN{[Xl? MUSxJO69VcLi MmTwSG1UVw>? M4fC[Ilv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NWTOTIoyOjZ2NUi5OVM>
Huh7 MWPGeY5kfGmxbjDhd5NigQ>? NV6yfFdUOSEQvF5CpC=> M1PFN2ROW09? MoXGbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> M1nhelI3PDV6OUWz
MHCC97L NYPlVpViSXCxcITvd4l{KGG|c3H5 M4nCZlEh|ryPwrC= MYTEUXNQ MWLpcoR2[2W|IHHwc5B1d3Orcx?= M4jp[FI3PDV6OUWz
Huh7 NVLCepJLSXCxcITvd4l{KGG|c3H5 NYXNZoh1OSEQvF5CpC=> MYPEUXNQ MXzpcoR2[2W|IHHwc5B1d3Orcx?= NGXabWozPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts MVvLbY5ie2ViYYPzZZk> NFnKeI8zPSEQvF2= MW\EUXNQ M4[5cJJm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MW[yNFU{PDN2NR?=
H23 MmXOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2W1ZVI2KM7:TR?= M3vzWWROW09? Mojwd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MnrXNlA2OzR|NEW=
WM35 MoHIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF:zc4oyOCEQvF2= NYSxcpUxTE2VTx?= NIroV29{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NYi2ZnFJOjB3M{SzOFU>
NIH 3T3 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFT4cVQyOCEQvF2= NIH2WoJFVVOR Mlzj[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MmHQNlA2OzR|NEW=
H838 M4T1bmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn32NVAh|ryP NILkXnBFVVOR NVi0eoxb\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MWSyNFU{PDN2NR?=
H1395 MlSyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmL2NVAh|ryP NYHj[4NZTE2VTx?= NUH2dI1s\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NYXmZoR3OjB3M{SzOFU>
Quiescent S2 M{WzTWtqdmG|ZTDhd5NigQ>? M2rhW|MxKM7:TR?= MXjEUXNQ MVfjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? M{LMUVIyPTF6OUG1
PC3 NUXQfJFXSXCxcITvd4l{KGG|c3H5 M2HsV|IxKM7:TR?= M{fJU2ROW09? MUTpcoR2[2W|IHHwc5B1d3Orcx?= NGDRRVUzOTdyOUGzNC=>
Du145 NIDYOW9CeG:ydH;zbZMh[XO|YYm= NXK5To5OOjBizszN NX3vN|llTE2VTx?= MX;pcoR2[2W|IHHwc5B1d3Orcx?= M{LVSVIyPzB7MUOw
LNCaP NFvlN4NCeG:ydH;zbZMh[XO|YYm= NGrGNZAzOCEQvF2= NWLXeZBvTE2VTx?= M2PpUolv\HWlZYOgZZBweHSxc3nz M2\6XFIyPzB7MUOw
LAPC-4 M4XJfWFxd3C2b4Ppd{Bie3OjeR?= NHfVRYozOCEQvF2= Mn\GSG1UVw>? NFHUdY9qdmS3Y3XzJIFxd3C2b4Ppdy=> MoXONlE4ODlzM{C=
LNCaP M3Hlc2Z2dmO2aX;uJIF{e2G7 NGLkbZczOCEQvF2= NYjKcWllTE2VTx?= NUDhXWpp\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= NWDkZVFFOjF5MEmxN|A>
LAPC-4 M136VmZ2dmO2aX;uJIF{e2G7 MW[yNEDPxE1? NIfmSmVFVVOR MmP0[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MoPaNlE4ODlzM{C=
Kasumi-1 NH;LVo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnH1glUxKM7:TR?= MnvUSG1UVw>? Ml3hbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MmqyNlM{QTB3M{[=
SKNO-1 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3LiRZ42OCEQvF2= M1PnR2ROW09? NV7wcGRHcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NEj6U3kzOzN7MEWzOi=>
Kasumi-1 MoDhT4lv[XOnIHHzd4F6 NVTGe49KhjFyIN88US=> MVjEUXNQ MnnwdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NGrJcVczOzN7MEWzOi=>
SKNO-1 NHjYT49McW6jc3WgZZN{[Xl? MmizglExKM7:TR?= NGLTeGxFVVOR Mln1doVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y Mmn3NlM{QTB3M{[=
A549 M2DVeGZ2dmO2aX;uJIF{e2G7 MlS2NVAh|ryP M2fOe2ROW09? MlX3[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> NIDjcowzPDd2NkW3OC=>
NRK-52E MofTSpVv[3Srb36gZZN{[Xl? MVmxNEDPxE1? Ml34SG1UVw>? M1jIO4lvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv M3rJPFI2ODh6MECy
PC12 MlvtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFfHfVd,OTJwNTFOwG0> MlHxSG1UVw>? NH\WXnBxemW4ZX70d{BVW0FvaX7keYNm\CCwZYXybZRmKG[xcn3heIlwdg>? MVqyOVEzQDN6Nh?=
HPMCs M2ntcWZ2dmO2aX;uJIF{e2G7 NGnMdYRz\X[ncoPld{BmeGm2aHXsbYFtKHSxIH3ld4Vv[2i7bXHsJJRz[W6|aYTpc44hd2ZiaIXtZY4heGW{aYTvcoVidCCvZYPveIhmdGmjbDDj[Yxtew>? NULBOXJ3OjZyNEW3PFA>
A549 Mnq3SpVv[3Srb36gZZN{[Xl? MWD+OVAh|ryP M13ubmROW09? MVrh[oZm[3S|IITo[UB3cXKjbDDsbYZmKGO7Y3zlJIFv\CCqb4P0JJJme3CxboPl NXq0XllDOjZ5MUG3OFg>
RAW264.7 M2rwcWZ2dmO2aX;uJIF{e2G7 M3n0OJ4{OCEQvF2= NX2x[4VXTE2VTx?= MYry[YR2[2W|IIDyc{1qdm[uYX3tZZRwenliZ3Xu[UBmgHC{ZYPzbY9v MWqyOlcyQDV6Nh?=
MEMM NUnvTm92U2mwYYPlJIF{e2G7 NGL0SGoyPSEEtV2= MlTqSG1UVw>? NVLVN3p{\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> NE[yPXozPjl{MUWwOi=>
MEMM MmPCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn\hglIxKML3TR?= M4jSTmROW09? M{jxfIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M4XkVFI3QTJzNUC2
MEMM NV\CSXg4SXCxcITvd4l{KGG|c3H5 NGGwfGgyPSEEtV2= MXPEUXNQ NWHze4llcW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? NFXLS5UzPjl{MUWwOi=>
T47D NXfXZWRxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGT4O|kyOCEQvF2= NX3LUW1QTE2VTx?= M1;CTWlEPTB;N{Kgcm0> MljNNVg{QDF2NES=
ZR-75-1 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmTYNVAh|ryP NVnSeoo4TE2VTx?= MlTwTWM2OD15OTDuUS=> MWKxPFM5OTR2NB?=
BT474 NHTXemRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVyxNEDPxE1? MYDEUXNQ Mof2TWM2OD16NjDuUS=> MYGxPFM5OTR2NB?=
HCC1954 NX;nUJVwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2f3cVExKM7:TR?= M{LjfmROW09? MYnJR|UxRTFzOTDuUS=> NV6wdGd7OTh|OEG0OFQ>
MDA-MB-453 NXf5SGV{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVGxNEDPxE1? MmrjSG1UVw>? NHGxXI9KSzVyPUm3OUBvVQ>? Mlj6NVg{QDF2NES=
MDA-MB-468 NVLibJJqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWexNEDPxE1? M13LVmROW09? NULmOolHUUN3ME2zNlA5KG6P NFrPfZoyQDN6MUS0OC=>
SkBr3 NE\MTm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2XWO|ExKM7:TR?= NXyxRoZ4TE2VTx?= MWrJR|UxRjFyLECwNEBvVQ>? M4fCflE5OzhzNES0
MDA-MB-231 MnXGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoP4NVAh|ryP MXrEUXNQ NIX1UItKSzVyPkGwMFAxOCCwTR?= MlvNNVg{QDF2NES=
HCT116 M1HGOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3HVXFExKM7:TR?= M1nENWROW09? M4i1XGlEPTB;NUizOkBvVQ>? MYixPFM5OTR2NB?=
HT29 NX7ZSlE5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWX6Z4p2OTBizszN NED3R|BFVVOR MXjJR|UxRjFyLECwNEBvVQ>? Moq2NVg{QDF2NES=
HFF NIPaZoFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHT5RYgyOCEQvF2= NFnVOHNFVVOR NIXBPW9KSzVyPUe2NVUhdk1? MVmxPFM5OTR2NB?=
HN5 NGD0WpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGjjOXIyOCEQvF2= NYTMOVlPTE2VTx?= MXzJR|UxRjFyLECwNEBvVQ>? NVXiUVhEOTh|OEG0OFQ>
786-0 M1HrPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmfINVAh|ryP NX20bGVtTE2VTx?= M3jyVGlEPTB;NECwPUBvVQ>? MmLDNVg{QDF2NES=
H157 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVHtWHVrOTBizszN M4LCWGROW09? M1PWZWlEPTB;Mk[0NkBvVQ>? NFLDbnQyQDN6MUS0OC=>
NCI-H460 MojhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlnONVAh|ryP MVnEUXNQ NVrBZ4tjUUN3ME6yMFUxOCCwTR?= MWWxPFM5OTR2NB?=
SKOV-3 M1XVNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmjCNVAh|ryP NWjxT3dDTE2VTx?= M3LDTmlEPTB;MkGyOkBvVQ>? M3qy[VE5OzhzNES0
OVCAR-3 MnnQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFKzTY0yOCEQvF2= M{P3UmROW09? MUTJR|UxRTJ7MUigcm0> M2LYeFE5OzhzNES0
BXPC3 NYf0cnpkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnnSNVAh|ryP NF\KemVFVVOR MUfJR|UxRTNzNEGgcm0> NX24[lZsOTh|OEG0OFQ>
MiaPaCa NXvySmZUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWKxNEDPxE1? MVvEUXNQ NVm5W5NJUUN3ME21OFM{KG6P NETpZWYyQDN6MUS0OC=>
PANC-1 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYKxNEDPxE1? MXnEUXNQ MmHZTWM2OD16NkixJI5O MoL1NVg{QDF2NES=
LNCaP M3H1Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVqyXXhLOTBizszN MW\EUXNQ NUHvdXRJUUN3ME2xOFchdk1? Mm\2NVg{QDF2NES=
DU145 NWLOOoNyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmK0NVAh|ryP NIe4d5lFVVOR MYXJR|UxRTN6MUKgcm0> MXGxPFM5OTR2NB?=
PC3 NXLO[phoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV:xNEDPxE1? MoLzSG1UVw>? NGT6VINKSzVyPkGwMFAxOCCwTR?= M3jPWFE5OzhzNES0
BT474 MlfmT4lv[XOnIHHzd4F6 Mo[0NVAh|ryP NETHb|BFVVOR MoDzbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTZyIH7N MonjNVg{QDF2NES=
786-0 NUDDdVJRU2mwYYPlJIF{e2G7 Mk\NNVAh|ryP MW\EUXNQ MmXWbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTVyIH7N NWHzc2N5OTh|OEG0OFQ>
LNCaP M3S3V2tqdmG|ZTDhd5NigQ>? M3LmWlExKM7:TR?= MkPjSG1UVw>? MmKzbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDNibl2= M2P2cVE5OzhzNES0
PC3 NYXrSGJuU2mwYYPlJIF{e2G7 MkLZNVAh|ryP M{LyUGROW09? MnL1bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDlibl2= NGn3d2syQDN6MUS0OC=>
KARPAS-231 NFXHWHhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4fS[VExKM7:TR?= NIXETllFVVOR NFzoSlRGSzVyPUSxJI5O M2rPVlE6ODZ2N{Ow
CCRFSB M1zIWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYWxNEDPxE1? NGnablhFVVOR NFLiXpFGSzVyPUG1OUBvVQ>? MWSxPVA3PDd|MB?=
SUP B15 MkSxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo\JNVAh|ryP M4P3b2ROW09? M4jGfmVEPTB;MUm3JI5O M3HSeVE6ODZ2N{Ow
SD-1 NUHxNVMzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX2xNEDPxE1? M{ftbGROW09? M1S2UGVEPTB;M{KwJI5O NXX5O3Z5OTlyNkS3N|A>
RS4;11 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MonaNVAh|ryP M2\RWGROW09? NG\PVXVGSzVyPU[1OEBvVQ>? NHPCWHUyQTB4NEezNC=>
MN-60 NX;ifIJ2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mkj1NVAh|ryP NGXJN5dFVVOR MUTFR|UxRTN4MEKgcm0> NYfzUXhqOTlyNkS3N|A>
Tanoue MlPPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{T4fFExKM7:TR?= NHrZRpBFVVOR M2HmUmVEPTB;NEWxO{BvVQ>? NVrzT5VrOTlyNkS3N|A>
RCH-ACV NXLaSXZJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYGxNEDPxE1? M2PiW2ROW09? MkLoSWM2OD1zNUKgcm0> MYSxPVA3PDd|MB?=
SEM M{T4emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2XCNFExKM7:TR?= MVLEUXNQ MY\FR|UxRTJyMjDuUS=> M12z[lE6ODZ2N{Ow
KASUMI-2 NFzSU3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfLRlVnOTBizszN NVnac4R2TE2VTx?= NGq4eHNGSzVyPUKyOUBvVQ>? M3fkUlE6ODZ2N{Ow
REH MknsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1[ydVExKM7:TR?= Ml7ISG1UVw>? MmLzSWM2OD1{OEigcm0> M3f2[FE6ODZ2N{Ow
697 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4m4XlExKM7:TR?= Mn;tSG1UVw>? NYXmSGxSTUN3ME2zN|ghdk1? M2jGbFE6ODZ2N{Ow
NALM-6 NYf5WmYzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn;PNVAh|ryP NUO2NmpZTE2VTx?= MYDFR|UxRTR{MTDuUS=> NInYXm0yQTB4NEezNC=>
MHH-CALL–3 M37CSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGDzWHMyOCEQvF2= Mkm5SG1UVw>? Mn3qSWM2OD16MUKgcm0> MWqxPVA3PDd|MB?=
MHH-CALL–2 NGjob2FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVmxNEDPxE1? MmHkSG1UVw>? MkjNSWM2OD1{MUG0JI5O NVexT3gyOTlyNkS3N|A>
J.GAMMA-1 Mom0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWmxNEDPxE1? MXnEUXNQ M4TTb2VEPTB;NkWgcm0> NYH5OFd6OTlyNkS3N|A>
JR45.01 MnfxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGL5cHkyOCEQvF2= M1joVWROW09? MUXFR|UxRTZ6IH7N NXLVNHpHOTlyNkS3N|A>
A3 MlW1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoPENVAh|ryP MVXEUXNQ NYH2O2QyTUN3ME22PUBvVQ>? MYCxPVA3PDd|MB?=
I 2.1 M37ld2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlPUNVAh|ryP NVi2NJc2TE2VTx?= NVnyTVlZTUN3ME23N{BvVQ>? MnjjNVkxPjR5M{C=
MOLT-3 MmSzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXexNEDPxE1? MkfLSG1UVw>? NV\JfIlETUN3ME23OEBvVQ>? NUPMTGVLOTlyNkS3N|A>
P116 NXHpbHA{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfoNVAh|ryP NHy1fGZFVVOR M4TYU2VEPTB;N{igcm0> MXOxPVA3PDd|MB?=
J.Cam1.6 M4TBUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUixNEDPxE1? NXXpdI51TE2VTx?= M1fwdWVEPTB;N{mgcm0> MVuxPVA3PDd|MB?=
I 9.2 NI\lW2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2DI[VExKM7:TR?= NFvaSYRFVVOR MWLFR|UxRThyIH7N MUexPVA3PDd|MB?=
LOUCY MoDFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLj[2FtOTBizszN NEnPN4lFVVOR MmP6SWM2OD1zMUegcm0> NGTSe4oyQTB4NEezNC=>
J.RT3-T3.5 M3LjU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1XUXVExKM7:TR?= MoTmSG1UVw>? MnnnSWM2OD1zMkOgcm0> NHrYXI4yQTB4NEezNC=>
800000 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGf0UZMyOCEQvF2= M4XHOmROW09? NFS2TWFGSzVyPUG2N{BvVQ>? NFnyV2kyQTB4NEezNC=>
Jurkat NIfmbZBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFjF[I0yOCEQvF2= MYHEUXNQ MYTFR|UxRTJ{NTDuUS=> NE\IfWkyQTB4NEezNC=>
MOLT-4 NILVcWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWOxNEDPxE1? MWDEUXNQ M2HsPWVEPTB;MkOyJI5O MVqxPVA3PDd|MB?=
Molt-16 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFji[G0yOCEQvF2= NIi2bW1FVVOR MUPFR|UxRTJ2MTDuUS=> NIm1R|QyQTB4NEezNC=>
CEM/C3 M3j4fmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3vrWFExKM7:TR?= MYTEUXNQ NYHrNoFTTUN3ME2yOVchdk1? NFi0O4cyQTB4NEezNC=>
CEM/C2 MnnBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NG\qRlAyOCEQvF2= NILN[mlFVVOR M3y3W2VEPTB;MkexJI5O MmHnNVkxPjR5M{C=
CCRFCEM NX;idJhRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml;VNVAh|ryP NIDuSYlFVVOR M{G1bGVEPTB;M{K3JI5O NFzlZXQyQTB4NEezNC=>
CEM/C1 M1HueGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn3mNVAh|ryP MXHEUXNQ MVTFR|UxRTN6MjDuUS=> MVmxPVA3PDd|MB?=
SUPTI[VB] MoHBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLpco9zOTBizszN MVTEUXNQ MYTFR|UxRTZzOTDuUS=> NXnHUFViOTlyNkS3N|A>
CCRF–HSB-2 Ml76S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\i[FExKM7:TR?= Ml;OSG1UVw>? NFzXXndGSzVyPUKxNVchdk1? MljtNVkxPjR5M{C=
I 2.1 NU\BT4RDSXCxcITvd4l{KGG|c3H5 M2\3VlExKM7:TR?= M2PHOWROW09? M1vlc4lv\HWlZYOgZZBweHSxc3nz NFzRZo0yQTB4NEezNC=>
I 9.2 MVjBdI9xfG:|aYOgZZN{[Xl? MofsNVAh|ryP NXPmOnZlTE2VTx?= M1fyd4lv\HWlZYOgZZBweHSxc3nz M4HobFE6ODZ2N{Ow
A3 MYnBdI9xfG:|aYOgZZN{[Xl? MmLvNVAh|ryP NGXEbmtFVVOR M3XGSYlv\HWlZYOgZZBweHSxc3nz Ml62NVkxPjR5M{C=
RD NFfLTWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnjzNVAh|ryP M4m4WGlEPTB-MUCg{txO NEDKblYzODd2ME[yNy=>
Rh41 NUTxcY0yT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWKxNEDPxE1? NIDKVJRKSzVyPUOzMlghdk1? MorvNlA4PDB4MkO=
Rh18 NEHWNo1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M13NRlExKM7:TR?= NFPYW5ZKSzVyPUOwN{BvVQ>? NI\4fXgzODd2ME[yNy=>
Rh30 NULrNpNET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmO1NVAh|ryP NHjYeJhKSzVyPUSuPFEh|ryP M{fRSVIxPzRyNkKz
BT-12 NGrKeXZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{fHWlExKM7:TR?= NVfyZZhrUUN3ME6xNEDPxE1? NV;FNmNuOjB5NEC2NlM>
CHLA-266 M1vFcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;DS3kyOCEQvF2= MoXpTWM2OD1zLkKyJO69VQ>? M1HQPFIxPzRyNkKz
TC-71 M3nJT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH7jU3QyOCEQvF2= NF:zNldKSzVyPUKuOVIh|ryP MUCyNFc1ODZ{Mx?=
CHLA-9 NEjXbIJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX:xNEDPxE1? NIW3dG5KSzVyPUW5NUBvVQ>? MUWyNFc1ODZ{Mx?=
CHLA-10 Mm\wS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYDBfJREOTBizszN M1zXWmlEPTB;MUCyJI5O MWOyNFc1ODZ{Mx?=
CHLA-258 NVT4eItVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUjRd2dyOTBizszN MmHyTWM2OD1zLkC1JO69VQ>? NEHFPWgzODd2ME[yNy=>
GBM2 MkfQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHf1NJgyOCEQvF2= M2HrTmlEPTB;OT6xOUDPxE1? NV7icZNtOjB5NEC2NlM>
NB-1643 NUX3[IRtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo[1NVAh|ryP M4\hemlEPTB;NT60JO69VQ>? M1TyUlIxPzRyNkKz
NB-Ebc1 NXLmOlBzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3\KT|ExKM7:TR?= NFSwU5pKSzVyPkGwJO69VQ>? NITjV|MzODd2ME[yNy=>
CHLA-90 NHvPNlJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWfrNmZUOTBizszN NGTNc4tKSzVyPkGwJO69VQ>? NYT5dpg2OjB5NEC2NlM>
CHLA-136 NVTqVYlHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEXsdJgyOCEQvF2= MnO4TWM2OD5zMDFOwG0> M2mzUFIxPzRyNkKz
NALM-6 M{HxXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{jieVExKM7:TR?= NVTLS4pEUUN3ME2yOlUhdk1? MVGyNFc1ODZ{Mx?=
COG-LL-317 MkjBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7DTm4yOTBizszN NXjxW4dNUUN3ME22MlQ6KG6P MorZNlA4PDB4MkO=
RS4;11 MorYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSxNEDPxE1? NFTXSVhKSzVyPUG0O{BvVQ>? Moi2NlA4PDB4MkO=
MOLT-4 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGTmWG8yOCEQvF2= NXTIO2VZUUN3ME20NEBvVQ>? NGTsUYczODd2ME[yNy=>
CCRF-CEM NYTsRoR3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoPuNVAh|ryP NYTuXY9iUUN3ME2yOlghdk1? NF3kcWQzODd2ME[yNy=>
Kasumi-1 MmPUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{\ueVExKM7:TR?= MVLJR|UxRTFyNzDuUS=> MmfaNlA4PDB4MkO=
Karpas-299 NFOxTVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWTleXJ4OTBizszN NH;YVJdKSzVyPUKuPVMh|ryP Mof6NlA4PDB4MkO=
Ramos-RA1 NIfBPGtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4qzVlExKM7:TR?= NEezbpBKSzVyPUeuN|Uh|ryP M17BU|IxPzRyNkKz
H1299 M1S2OmtqdmG|ZTDhd5NigQ>? NFnBeJUyOCEQvF2= NELyWpJqdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v MlTGNlE6ODh4MU[=

... Click to View More Cell Line Experimental Data

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

PubMed: 23022995     


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

23022995
Growth inhibition assay
Cell viability; 

PubMed: 23598276     


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

23598276
In vivo All three xenograft models treated with ARQ-197 display reductions in tumor growth: 66% in the HT29 model, 45% in the MKN-45 model, and 79% in the MDA-MB-231 model. In these xenograft studies, no significant body weight changes following oral administration of ARQ-197 at 200 mg/kg are observed. Pharmacodynamically, the phosphorylation of c-Met in human colon xenograft tumors (HT29) is strongly inhibited by ARQ-197, as assessed by a dramatic reduction of c-Met autophosphorylation 24 hours after a single oral dose of 200 mg/kg of ARQ-197. This same dosage in mice exhibits that tumor xenografts are exposed to sustained plasma levels of ARQ-197, consistent with the observed pharmacodynamic inhibition of c-Met phosphorylation and inhibition of proliferation of c-Met harboring cancer cell lines. Plasma levels of ARQ-197 10 hours after dosing are determined to be 1.3 μM, more than 3-fold above the biochemical inhibitory constant of ARQ-197 for c-Met. Therefore, ARQ-197 is able to suppress its target in vivo in the xenografted human tumor tissue. In conclusion, ARQ-197 inhibits the growth of c-Met-dependent xenografted human tumors.[1]

Protocol

Kinase Assay:[1]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
  • Dosages: 200 mg/kg
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

CAS No. 905854-02-6
Storage powder
in solvent
Synonyms N/A
Smiles C1CC2=C3C(=CC=C2)C(=CN3C1)C4C(C(=O)NC4=O)C5=CNC6=CC=CC=C65

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02150733 Completed Drug: Tivantinib Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT01892527 Unknown status Drug: Tivantinib (ARQ197) Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Unknown status Drug: Tivantinib Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2
NCT01755767 Completed Drug: Tivantinib|Drug: Placebo Hepatocellular Carcinoma Daiichi Sankyo Inc.|ArQule December 27 2012 Phase 3

Tech Support

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

Handling Instructions

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

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

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

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