Tivantinib (ARQ 197)

Catalog No.S2753

Tivantinib (ARQ 197) Chemical Structure

Molecular Weight(MW): 369.42

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

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2 Customer Reviews

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

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

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

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

Purity & Quality Control

Choose Selective c-Met Inhibitors

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 NXjCO3R5U2mwYYPlJIF{e2G7 NU\ETmp3hjFyIN88US=> MVvpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NV\tNllKOjB2OESwNVg>
HT29 MlzvT4lv[XOnIHHzd4F6 NGmzTmh,OTBizszN MXvpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M1;FUVIxPDh2MEG4
MDA-MB-231 NIO0VG9McW6jc3WgZZN{[Xl? NE\yUYJ,OTBizszN MYXpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NFvTeoczODR6NECxPC=>
NCI-H441 M1HCTWtqdmG|ZTDhd5NigQ>? NX;1VYU2hjFyIN88US=> NULT[pJQcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NWXpR3lQOjB2OESwNVg>
SK-MEL-28 MknhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYHKemJNOzNizszN NFfLS2lKSzVyPkOzJO69VQ>? NFPUXlUzODR6NECxPC=>
NCI-H661 M3\uT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFPZVYw{OyEQvF2= MkTjTWM2OD5|MzFOwG0> NFHTNHUzODR6NECxPC=>
NCI-H446 M13pTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4W2ZVM{KM7:TR?= NE\BTFRKSzVyPUeg{txO M1Lx[VIxPDh2MEG4
MDA-MB-231 M3rz[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXqzN{DPxE1? MmLlTWM2OD1yLkW1JO69VQ>? MkLTNlA1QDRyMUi=
DLD-1 M1HITGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLEN|Mh|ryP M{DJcWlEPTB;MD61N{DPxE1? MWKyNFQ5PDBzOB?=
A549 M37pOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYX3S25kOzNizszN NYm1WJdEUUN3ME2wMlU6KM7:TR?= MoDSNlA1QDRyMUi=
SK-OV-3 M3XLbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEDSRpc{OyEQvF2= Mn;jTWM2OD1yLk[2JO69VQ>? NYflV5BZOjB2OESwNVg>
NCI-H460 NUXidXluT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1myO|M{KM7:TR?= M4PyR2lEPTB;MD62JO69VQ>? NI[4VFUzODR6NECxPC=>
A375 NYPRN|R4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmXyN|Mh|ryP M3X5TWlEPTB;MD60NkDPxE1? M1\DfVIxPDh2MEG4
NCI-H441 M1ra[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYDmO4xpOzNizszN MlqxTWM2OD1yLkOg{txO MlXKNlA1QDRyMUi=
HT29 NGO1emVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml3qN|Mh|ryP MmDhTWM2OD1yLkS5JO69VQ>? MWeyNFQ5PDBzOB?=
MKN-45 NVnTXXVIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEjNbnU{OyEQvF2= MX\JR|UxRTBwNUig{txO NHzneYQzODR6NECxPC=>
HT29 NU\wXpB3SXCxcITvd4l{KGG|c3H5 M{j6bZ4yOCEQvF2= M{jNdpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MorvNlA1QDRyMUi=
MKN-45 M{C5b2Fxd3C2b4Ppd{Bie3OjeR?= NYnzZVJZhjFyIN88US=> Mn;Nd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw M2rzXVIxPDh2MEG4
MDA-MB-231 M{\W[GFxd3C2b4Ppd{Bie3OjeR?= NIjQS5d,OTBizszN M1TRXI1w\GW|dHz5JIlv\HWlZYOgZZBweHSxc3nzJIJ6KDN3JT6= MXiyNFQ5PDBzOB?=
MDA-MB-231/TGL MoXSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml72glExOCEQvF2= MVTHTVUxRTFwMjFOwG0> MoX4NlIxOjd4OUC=
1833/TGL NUPwOIpmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1\5ep4yODBizszN MkGzS2k2OD1|Lkeg{txO NWjnWpcyOjJyMke2PVA>
EBC1 M2rJRWN6fG:2b4jpZ:Kh[XO|YYm= MWD+NVAh|ryP M3T6SolvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= M1vRWVI{PTl6Mke2
SNU638 Ml3hR5l1d3SxeHnjxsBie3OjeR?= NIrUO3Z,OTBizszN NHvTeGVqdmirYnn0d{B1cGViY3XscEBoem:5dHiu Mnr5NlM2QTh{N{[=
A549 MV3DfZRwfG:6aXRCpIF{e2G7 NWDZW5VZhjFyIN88US=> MULuc5Qh[W[oZXP0 MlH6NlM2QTh{N{[=
H460 NELMSmxEgXSxdH;4bYPDqGG|c3H5 NF:5ZYJ,OTBizszN NHXBT2dvd3RiYX\m[YN1 M4nVeFI{PTl6Mke2
HCC827 NUTiZnZ2S3m2b4TvfIlkyqCjc4PhfS=> M4C5OJ4yOCEQvF2= MVPuc5Qh[W[oZXP0 MljqNlM2QTh{N{[=
A549 MX7GeY5kfGmxbjDhd5NigQ>? NG\lOY4yOCEQvF2= MlTp[Il{enWydIOgcYlkem:2dXL1cIU> MVeyN|U6QDJ5Nh?=
EBC1 Ml7CSpVv[3Srb36gZZN{[Xl? NVHOSmc4OTBizszN M1uxboRqe3K3cITzJI1q[3KxdIXieYxm MUCyN|U6QDJ5Nh?=
H460 M4DiNmZ2dmO2aX;uJIF{e2G7 MlfCNVAh|ryP Ml\WbY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? M1zDcFI2OzF|MEGw
K562/VCR M{njfWN6fG:2b4jpZ:Kh[XO|YYm= NInoeVd,OTBizszN NV;zZ3VLe2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 Mni0NlU{OTNyMUC=
CEM/VBL MnX6R5l1d3SxeHnjxsBie3OjeR?= MkHCglExKM7:TR?= MWDzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MoLLNlU{OTNyMUC=
U266 NUS4WG1NS3m2b4TvfIlkyqCjc4PhfS=> MoXBglMh|ryPwrC= NVnNcWtqUUN3ME2xMlEh|ryP MVSyOVgyODBzMx?=
OPM-2 M{nuOWN6fG:2b4jpZ:Kh[XO|YYm= MYn+N{DPxE4EoB?= M2PKU2lEPTB;MT64JO69VQ>? NInQZVkzPThzMECxNy=>
MM.1S M1XGOWN6fG:2b4jpZ:Kh[XO|YYm= NW\x[|M2hjNizszNxsA> MmjLTWM2OD1zLk[g{txO NWfUXJg4OjV6MUCwNVM>
MM.1R NX:xXlhbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWezJO69VcLi MYjpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= NEnGcFUzPThzMECxNy=>
RPMI-8226 M33mfWN6fG:2b4jpZ:Kh[XO|YYm= NFz2[4l,OyEQvF5CpC=> NHHISYpKSzVyPUCuPUDPxE1? MYiyOVgyODBzMx?=
ANBL-6 MYHDfZRwfG:6aXRCpIF{e2G7 NYfjWWVuOSEQvF5CpC=> M4n0SYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MV6yOVgyODBzMx?=
ANLB-6/V10R M{jjZ2N6fG:2b4jpZ:Kh[XO|YYm= M1yw[|Eh|ryPwrC= Mnn5bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= M1PzS|I2QDFyMEGz
KAS-6/1 MUTDfZRwfG:6aXRCpIF{e2G7 MVSxJO69VcLi NYXK[ow4cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MkDHNlU5OTByMUO=
KAS-6/V10R NGK2SJlEgXSxdH;4bYPDqGG|c3H5 NXn1e4xMOSEQvF5CpC=> M3mwc4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NHjKRmMzPThzMECxNy=>
KAS-6/R10R NV\jNXViS3m2b4TvfIlkyqCjc4PhfS=> NX;OWYFlOSEQvF5CpC=> MVjpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= M3TvZ|I2QDFyMEGz
8226/S MkTkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUizJO69VcLi M3vOTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> M13ZfFI2QDFyMEGz
8226/LR-5 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1zPc|Mh|ryPwrC= MUHpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= MWGyOVgyODBzMx?=
Huh7 MoDSR5l1d3SxeHnjxsBie3OjeR?= NEDWUHl,PC56IN88UeKh MW\EUXNQ M2rsWGlEPTB;OT65JI5O MojzNlYzPTl{NUC=
Hep3B NHXVUHVEgXSxdH;4bYPDqGG|c3H5 MkjLglQvQCEQvF5CpC=> NVfGWI1WTE2VTx?= M2\mXmlEPTB;NES4Mlchdk1? MYKyOlI2QTJ3MB?=
HepG2 Mmr2R5l1d3SxeHnjxsBie3OjeR?= NFXvZ4x,PC56IN88UeKh MX3EUXNQ NUH5OZFSUUN3ME2xN|kvPzdibl2= NFzFSGwzPjJ3OUK1NC=>
Chang Ml\kR5l1d3SxeHnjxsBie3OjeR?= MV3+OE45KM7:TdMg NYO4[|ZjTE2VTx?= MUDJR|UxRTR2OD63JI5O M1L3WlI3OjV7MkWw
Huh7 NIjsbZBHfW6ldHnvckBie3OjeR?= NFzVfIIyNjZizszNxsA> MlXNSG1UVw>? MYfjZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MV[yOlI2QTJ3MB?=
Hep3B NXfpU3N3TnWwY4Tpc44h[XO|YYm= MWexMlYh|ryPwrC= NGTHOHFFVVOR M2jrZYNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MX6yOlI2QTJ3MB?=
HepG2 M1juVmZ2dmO2aX;uJIF{e2G7 MoHpNU43KM7:TdMg NI\tOFJFVVOR NEHpZVhk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M1T0WFI3OjV7MkWw
Chang NWLRbJNyTnWwY4Tpc44h[XO|YYm= MWCxMlYh|ryPwrC= NI\HVYNFVVOR M1XTSoNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? Mn6zNlYzPTl{NUC=
MHCC97L MmPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXEglExKM7:TR?= MUHEUXNQ M4HoZWlEPTB;M{G1JI5O NXLFfWx{OjZ2NUi5OVM>
MHCC97H MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkD5glExKM7:TR?= NXeyO2dDTE2VTx?= M1HjdWlEPTB;M{[45qCKKG6P MWKyOlQ2QDl3Mx?=
Huh7 M1rQVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1fsZp4yOCEQvF2= Mn;BSG1UVw>? MonqTWM2OD1{NkWgcm0> Ml70NlY1PTh7NUO=
HepG2 M{PWPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWTk[Y1QhjFyIN88US=> NE\2[npFVVOR Mk\zTWM2OD1|OUKgcm0> MVqyOlQ2QDl3Mx?=
MHCC97L NGDsdXJHfW6ldHnvckBie3OjeR?= MV[xJO69VcLi M3TCeGROW09? MknObY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NH;jWJIzPjR3OEm1Ny=>
Huh7 M{XafWZ2dmO2aX;uJIF{e2G7 M{W4cVEh|ryPwrC= NWrQW4ZTTE2VTx?= MYHpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u M{m0eVI3PDV6OUWz
MHCC97L MYrBdI9xfG:|aYOgZZN{[Xl? NVLBZlFoOSEQvF5CpC=> NF:5e41FVVOR Moe5bY5lfWOnczDhdI9xfG:|aYO= MW[yOlQ2QDl3Mx?=
Huh7 MmS3RZBweHSxc3nzJIF{e2G7 NIDEepIyKM7:TdMg M3u0cGROW09? MWrpcoR2[2W|IHHwc5B1d3Orcx?= MlzMNlY1PTh7NUO=
C3H 10T1/2 mouse fibroblasts NEXoWnRMcW6jc3WgZZN{[Xl? NEP1UW0zPSEQvF2= M3\1d2ROW09? M1\sd5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MV6yNFU{PDN2NR?=
H23 NU\lRlIzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Moj4NlUh|ryP MVTEUXNQ MUfzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NFPES3YzODV|NEO0OS=>
WM35 M3TFV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1LLO|ExKM7:TR?= M2jXNGROW09? MkDwd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MYiyNFU{PDN2NR?=
NIH 3T3 NULUTldzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoHMNVAh|ryP NUfM[VEzTE2VTx?= NED0TW5ld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NXywXlhXOjB3M{SzOFU>
H838 MonXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3;1NVExKM7:TR?= M1;nc2ROW09? NXHaeHU{\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 M{[yUlIxPTN2M{S1
H1395 MlnBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVniWlQ4OTBizszN M3:wUWROW09? M2TiT4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MUOyNFU{PDN2NR?=
Quiescent S2 M3jvTGtqdmG|ZTDhd5NigQ>? NEG1V|k{OCEQvF2= M1fhXWROW09? MV7jc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? M{Dre|IyPTF6OUG1
PC3 NWT0NJhuSXCxcITvd4l{KGG|c3H5 NUPtS2ZLOjBizszN Mn3OSG1UVw>? MWPpcoR2[2W|IHHwc5B1d3Orcx?= M3PqV|IyPzB7MUOw
Du145 MVXBdI9xfG:|aYOgZZN{[Xl? NY\PRWVxOjBizszN MojHSG1UVw>? NXnCPJoycW6mdXPld{BieG:ydH;zbZM> NV;nVWF6OjF5MEmxN|A>
LNCaP MkG1RZBweHSxc3nzJIF{e2G7 NVPtco1uOjBizszN MmfBSG1UVw>? NEXXOXhqdmS3Y3XzJIFxd3C2b4Ppdy=> MWKyNVcxQTF|MB?=
LAPC-4 NIi2PFZCeG:ydH;zbZMh[XO|YYm= NFrMOIkzOCEQvF2= M33NOGROW09? NVnmW2Q5cW6mdXPld{BieG:ydH;zbZM> NUXpd4I2OjF5MEmxN|A>
LNCaP MVPGeY5kfGmxbjDhd5NigQ>? NWPhXFZiOjBizszN MV;EUXNQ NELDelNl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| MoPONlE4ODlzM{C=
LAPC-4 MXfGeY5kfGmxbjDhd5NigQ>? MYCyNEDPxE1? NW\3VnlmTE2VTx?= NWnuT4FT\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= NGrWVWczOTdyOUGzNC=>
Kasumi-1 NUPzTVRYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmT1glUxKM7:TR?= NY\DbG5STE2VTx?= M2DhPYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Mn7jNlM{QTB3M{[=
SKNO-1 M4PHNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoPCglUxKM7:TR?= MmPuSG1UVw>? MULpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M2qxOlI{OzlyNUO2
Kasumi-1 MkPZT4lv[XOnIHHzd4F6 NWe5OHFyhjFyIN88US=> M4XkbWROW09? M2LzeJJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> MmLJNlM{QTB3M{[=
SKNO-1 NFvldJVMcW6jc3WgZZN{[Xl? M4C2fp4yOCEQvF2= Mn7aSG1UVw>? NU[4UYJYemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z MnXONlM{QTB3M{[=
A549 MmT2SpVv[3Srb36gZZN{[Xl? NFXSSJUyOCEQvF2= MljySG1UVw>? NGP5OGpmdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm NWLRVYkzOjR5NE[1O|Q>
NRK-52E NV\k[mhWTnWwY4Tpc44h[XO|YYm= NXz0botoOTBizszN MY\EUXNQ MWPpcohq[mm2czDBcochUUlvaX7keYNm\CCVVFHUN{BvfWOuZXHyJJRz[W6|bH;jZZRqd25iYX7kJJRp\SCneIDy[ZN{cW:wIH;mJHRITi4QskGsJINwdGyjZ3XuJGlXKGGwZDDmbYJzd26nY4Tpci=> M3na[FI2ODh6MECy
PC12 NGfpTFBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV;+NVIvPSEQvF2= M2\GPWROW09? NHrRclhxemW4ZX70d{BVW0FvaX7keYNm\CCwZYXybZRmKG[xcn3heIlwdg>? NWmyUY5bOjVzMkizPFY>
HPMCs MlPuSpVv[3Srb36gZZN{[Xl? NWfYSIdXemW4ZYLz[ZMh\XCrdHjlcIlidCC2bzDt[ZNmdmOqeX3hcEB1emGwc3n0bY9vKG:oIHj1cYFvKHCncnn0c45m[WxibXXzc5Rp\WyrYXygZ4VtdHN? NVLvW5lZOjZyNEW3PFA>
A549 MW\GeY5kfGmxbjDhd5NigQ>? NIjORmZ,PTBizszN Mn[5SG1UVw>? M3WwSIFn\mWldIOgeIhmKH[rcnHsJIxq\mViY4njcIUh[W6mIHjvd5QhemW|cH;ud4U> MoPnNlY4OTF5NEi=
RAW264.7 MXPGeY5kfGmxbjDhd5NigQ>? NVTkdGU{hjNyIN88US=> MXjEUXNQ NGnjfolz\WS3Y3XzJJBzdy2rbn\sZY1u[XSxcomg[4Vv\SCneIDy[ZN{cW:w MW[yOlcyQDV6Nh?=
MEMM M1\vWmtqdmG|ZTDhd5NigQ>? NUHGcFM{OTViwsXN NH;ZbohFVVOR Mnvn[IVkemWjc3XzJIFk\XS7bHH0bY9vKG:oIHjpd5RwdmViSEO= M4P5TFI3QTJzNUC2
MEMM M3;uV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFntV4x,OjBiwsXN M1fmR2ROW09? MYXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NYjWNlZLOjZ7MkG1NFY>
MEMM M3HpT2Fxd3C2b4Ppd{Bie3OjeR?= M4Lje|E2KML3TR?= NXfaO3BETE2VTx?= NVTM[oY5cW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? MVmyOlkzOTVyNh?=
T47D NFPYclNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXOxNEDPxE1? MWPEUXNQ NHLjUJdKSzVyPUeyJI5O MV[xPFM5OTR2NB?=
ZR-75-1 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXvzN|ZCOTBizszN NVvqTmVQTE2VTx?= M1;xOWlEPTB;N{mgcm0> MXOxPFM5OTR2NB?=
BT474 M1WyWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXf4e4V6OTBizszN MYrEUXNQ M{j2TmlEPTB;OE[gcm0> MV:xPFM5OTR2NB?=
HCC1954 M2qzN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkXDNVAh|ryP MoPOSG1UVw>? NGfjZ3FKSzVyPUGxPUBvVQ>? NHfRdJUyQDN6MUS0OC=>
MDA-MB-453 NYTCeWtbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH7JXXEyOCEQvF2= Ml;lSG1UVw>? NGfJS|JKSzVyPUm3OUBvVQ>? NUfnSo1TOTh|OEG0OFQ>
MDA-MB-468 M3ftV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDGNVAh|ryP M{j6TmROW09? MXLJR|UxRTN{MEigcm0> MofoNVg{QDF2NES=
SkBr3 M2DlU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH7N[ZMyOCEQvF2= MXzEUXNQ NEPEU5NKSzVyPkGwMFAxOCCwTR?= M{jkOFE5OzhzNES0
MDA-MB-231 M{\4cGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXmxNEDPxE1? M4jlW2ROW09? MX\JR|UxRjFyLECwNEBvVQ>? NUHIO3JXOTh|OEG0OFQ>
HCT116 M3rpb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWqxNEDPxE1? NXznZZRNTE2VTx?= NFLBfnNKSzVyPUW4N|Yhdk1? NUjNT|ZTOTh|OEG0OFQ>
HT29 M4\kbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXK1W5VxOTBizszN NI\LcnRFVVOR MkfXTWM2OD5zMDywNFAhdk1? MYKxPFM5OTR2NB?=
HFF M3XTdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4f0flExKM7:TR?= NFXWV5BFVVOR NU\W[mZxUUN3ME23OlE2KG6P NUDKRZA4OTh|OEG0OFQ>
HN5 NVnVempUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mmn2NVAh|ryP MVXEUXNQ NEPse|BKSzVyPkGwMFAxOCCwTR?= MlPvNVg{QDF2NES=
786-0 NU\vS3duT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{\SNVExKM7:TR?= M37JNGROW09? M{LCR2lEPTB;NECwPUBvVQ>? NEjFS5QyQDN6MUS0OC=>
H157 NWL5dWtXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGXZTWkyOCEQvF2= NVT5cWpsTE2VTx?= MnnGTWM2OD1{NkSyJI5O M4XoZlE5OzhzNES0
NCI-H460 M4D4cWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NETtW2kyOCEQvF2= MUPEUXNQ M1T5UWlEPTB-Mjy1NFAhdk1? MVixPFM5OTR2NB?=
SKOV-3 NI\UXVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVnNV4ZVOTBizszN NVXvNnNtTE2VTx?= MVfJR|UxRTJzMk[gcm0> MlHTNVg{QDF2NES=
OVCAR-3 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWixNEDPxE1? Mn:5SG1UVw>? M{jLRWlEPTB;MkmxPEBvVQ>? M4LZZVE5OzhzNES0
BXPC3 M4DBSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1ftdVExKM7:TR?= NEDR[GhFVVOR NHvmZmlKSzVyPUOxOFEhdk1? M3rVc|E5OzhzNES0
MiaPaCa NIS3[lFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXHRdm1OOTBizszN MVvEUXNQ Mn;hTWM2OD13NEOzJI5O M3PTeFE5OzhzNES0
PANC-1 NITnd4tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUL3dJZ2OTBizszN M3fzemROW09? M4X0bmlEPTB;OE[4NUBvVQ>? NFeyfmIyQDN6MUS0OC=>
LNCaP NVHabVBRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4HrXFExKM7:TR?= M{\ZOWROW09? MkHJTWM2OD1zNEegcm0> NIDBR3AyQDN6MUS0OC=>
DU145 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmPUNVAh|ryP M{fNPGROW09? MkjtTWM2OD1|OEGyJI5O NYXn[ppxOTh|OEG0OFQ>
PC3 NXSzRm5QT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2HFbVExKM7:TR?= MXrEUXNQ NELaVG1KSzVyPkGwMFAxOCCwTR?= NV3LTW5rOTh|OEG0OFQ>
BT474 NYHmXJJrU2mwYYPlJIF{e2G7 NIPyfXAyOCEQvF2= NUj4S3lbTE2VTx?= MY\pcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kAyPjBibl2= MmXFNVg{QDF2NES=
786-0 NFrxVWZMcW6jc3WgZZN{[Xl? NGnPZY4yOCEQvF2= MWPEUXNQ M3nHd4lvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> NXXVNHA5OTh|OEG0OFQ>
LNCaP NX:xVYk4U2mwYYPlJIF{e2G7 NFzQeGgyOCEQvF2= MXjEUXNQ NF7YO5NqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2MzDuUS=> M2i4UVE5OzhzNES0
PC3 MoD6T4lv[XOnIHHzd4F6 NVzveHhvOTBizszN MXHEUXNQ M3TpZ4lvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR7IH7N NGnXUXUyQDN6MUS0OC=>
KARPAS-231 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV7aUJM3OTBizszN NEfW[I1FVVOR MlHBSWM2OD12MTDuUS=> MV2xPVA3PDd|MB?=
CCRFSB MoW5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnfwNVAh|ryP NXi5cHZ{TE2VTx?= NUHvU3ltTUN3ME2xOVUhdk1? MYSxPVA3PDd|MB?=
SUP B15 M4\xVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWKxNEDPxE1? MkPhSG1UVw>? M1i1Z2VEPTB;MUm3JI5O MYqxPVA3PDd|MB?=
SD-1 M2XXXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIGxVW8yOCEQvF2= M4LYXmROW09? NGHWV5ZGSzVyPUOyNEBvVQ>? MWGxPVA3PDd|MB?=
RS4;11 NYqyV2V[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVuxNEDPxE1? M13QUWROW09? MYnFR|UxRTZ3NDDuUS=> NUjUNlRbOTlyNkS3N|A>
MN-60 NGf6dHhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUixNEDPxE1? MXLEUXNQ NXnnbWs6TUN3ME2zOlAzKG6P M3nS[VE6ODZ2N{Ow
Tanoue NXn5U4Q4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HOO|ExKM7:TR?= MkHjSG1UVw>? MmT4SWM2OD12NUG3JI5O NEXkbpUyQTB4NEezNC=>
RCH-ACV MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1;xeFExKM7:TR?= MVPEUXNQ NILYOIRGSzVyPUG1NkBvVQ>? M1ztOFE6ODZ2N{Ow
SEM MnLLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4jpRVExKM7:TR?= M{TvXWROW09? Mn;oSWM2OD1{MEKgcm0> NGfJSFgyQTB4NEezNC=>
KASUMI-2 MljhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSxNEDPxE1? MnnYSG1UVw>? NIrEfWNGSzVyPUKyOUBvVQ>? MYOxPVA3PDd|MB?=
REH MkXzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NELXc|UyOCEQvF2= NWHtV416TE2VTx?= M1jwO2VEPTB;Mki4JI5O M3LqclE6ODZ2N{Ow
697 NIG1Z2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlzTNVAh|ryP M37nWWROW09? MYTFR|UxRTN|ODDuUS=> NFHLW2gyQTB4NEezNC=>
NALM-6 NWjRSHhLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVmxNEDPxE1? MXPEUXNQ MoHzSWM2OD12MkGgcm0> NInsOHAyQTB4NEezNC=>
MHH-CALL–3 Ml;vS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXTDRnVNOTBizszN MVXEUXNQ NIj2VmNGSzVyPUixNkBvVQ>? NGPmNWYyQTB4NEezNC=>
MHH-CALL–2 NYe1Wol4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1uzU|ExKM7:TR?= NILnfJFFVVOR M4rSXGVEPTB;MkGxOEBvVQ>? MkjyNVkxPjR5M{C=
J.GAMMA-1 MkDhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUWxNEDPxE1? MoTTSG1UVw>? M1jOdWVEPTB;NkWgcm0> NWH0WWFWOTlyNkS3N|A>
JR45.01 NH3ZT3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3[0NVExKM7:TR?= MnjiSG1UVw>? NET2Z2ZGSzVyPU[4JI5O MYexPVA3PDd|MB?=
A3 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3vrfVExKM7:TR?= NFLCPWNFVVOR MULFR|UxRTZ7IH7N NXzndolpOTlyNkS3N|A>
I 2.1 M{Llb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;NNoEyOCEQvF2= MYjEUXNQ NFf0d5VGSzVyPUezJI5O NV3qco5mOTlyNkS3N|A>
MOLT-3 Ml\WS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4S4bFExKM7:TR?= NInuO2RFVVOR NH\OSXFGSzVyPUe0JI5O NF3BfG0yQTB4NEezNC=>
P116 NEjWfW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXFb|RIOTBizszN MXPEUXNQ Mn36SWM2OD15ODDuUS=> M4f4NlE6ODZ2N{Ow
J.Cam1.6 MoHWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWKxNEDPxE1? NYPJcIk1TE2VTx?= NUPJdGNuTUN3ME23PUBvVQ>? NEnGV2cyQTB4NEezNC=>
I 9.2 MnXXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnHMNVAh|ryP MXHEUXNQ NEHSU3BGSzVyPUiwJI5O M1H6NVE6ODZ2N{Ow
LOUCY NXHLdXRwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV;KS3FbOTBizszN NGXjVmJFVVOR NH\iSYNGSzVyPUGxO{BvVQ>? NIjLclEyQTB4NEezNC=>
J.RT3-T3.5 NH7pToRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVzyS3ZjOTBizszN MW\EUXNQ NXTvV25nTUN3ME2xNlMhdk1? MXWxPVA3PDd|MB?=
800000 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3HGSVExKM7:TR?= NFTyRoRFVVOR MonBSWM2OD1zNkOgcm0> NWX3RpV3OTlyNkS3N|A>
Jurkat NH;JSnFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXexNEDPxE1? MnXPSG1UVw>? Mo\NSWM2OD1{MkWgcm0> MnvjNVkxPjR5M{C=
MOLT-4 MoK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUTLfG0yOTBizszN MXvEUXNQ M2fnfmVEPTB;MkOyJI5O NUHzUm9tOTlyNkS3N|A>
Molt-16 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEP0[oIyOCEQvF2= MoXVSG1UVw>? M4LkXWVEPTB;MkSxJI5O MlH5NVkxPjR5M{C=
CEM/C3 NU\NNmYxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPENVAh|ryP MmTZSG1UVw>? NEDmeohGSzVyPUK1O{BvVQ>? NVjSWlNKOTlyNkS3N|A>
CEM/C2 M3;1[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2XnOlExKM7:TR?= NFz1R45FVVOR MX7FR|UxRTJ5MTDuUS=> Mn3tNVkxPjR5M{C=
CCRFCEM NYHNfoptT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYSxNEDPxE1? M3LLVmROW09? MUHFR|UxRTN{NzDuUS=> Mmj6NVkxPjR5M{C=
CEM/C1 NGLvTVNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUjPZmZqOTBizszN MWLEUXNQ MXLFR|UxRTN6MjDuUS=> MmCyNVkxPjR5M{C=
SUPTI[VB] NWXNWpo{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojaNVAh|ryP M37aO2ROW09? MUDFR|UxRTZzOTDuUS=> MV:xPVA3PDd|MB?=
CCRF–HSB-2 NGKxNY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2HSbVExKM7:TR?= M1n1bGROW09? M{nWUWVEPTB;MkGxO{BvVQ>? M1XzW|E6ODZ2N{Ow
I 2.1 M4DnTWFxd3C2b4Ppd{Bie3OjeR?= MnvJNVAh|ryP MlXmSG1UVw>? MUnpcoR2[2W|IHHwc5B1d3Orcx?= MW[xPVA3PDd|MB?=
I 9.2 MVnBdI9xfG:|aYOgZZN{[Xl? MV2xNEDPxE1? MXrEUXNQ MmfMbY5lfWOnczDhdI9xfG:|aYO= Moe2NVkxPjR5M{C=
A3 MX;BdI9xfG:|aYOgZZN{[Xl? NFq5NXEyOCEQvF2= NFLFd|JFVVOR NWjzXmFVcW6mdXPld{BieG:ydH;zbZM> Mne5NVkxPjR5M{C=
RD NULLc4pvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVWxNEDPxE1? MlfCTWM2OD5zMDFOwG0> NIHtTGQzODd2ME[yNy=>
Rh41 NUnZd|FbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkPiNVAh|ryP NXnub5ZqUUN3ME2zN{45KG6P M4jtfVIxPzRyNkKz
Rh18 NGjJ[lBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH7sdXAyOCEQvF2= MlTmTWM2OD1|MEOgcm0> MnvnNlA4PDB4MkO=
Rh30 NYryWYxZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWKxNEDPxE1? MWHJR|UxRTRwOEGg{txO Mlv3NlA4PDB4MkO=
BT-12 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2HUe|ExKM7:TR?= M2HJNGlEPTB-MUCg{txO MWOyNFc1ODZ{Mx?=
CHLA-266 M{jwUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYLaT|JlOTBizszN MlzaTWM2OD1zLkKyJO69VQ>? MVWyNFc1ODZ{Mx?=
TC-71 NFe1R3BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mo[0NVAh|ryP NUXQSpBOUUN3ME2yMlUzKM7:TR?= MYKyNFc1ODZ{Mx?=
CHLA-9 MlH3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn7pNVAh|ryP MnizTWM2OD13OUGgcm0> M1S0RlIxPzRyNkKz
CHLA-10 MkHMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjYOVR4OTBizszN NYPRNJhCUUN3ME2xNFIhdk1? NXnJXpFJOjB5NEC2NlM>
CHLA-258 NYr0e4puT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYjKUI4{OTBizszN NEjO[mZKSzVyPUGuNFUh|ryP NIizUIgzODd2ME[yNy=>
GBM2 M3HqR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M374fFExKM7:TR?= Mof2TWM2OD17LkG1JO69VQ>? MXiyNFc1ODZ{Mx?=
NB-1643 NF3C[4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml7QNVAh|ryP MXrJR|UxRTVwNDFOwG0> M2Kxe|IxPzRyNkKz
NB-Ebc1 NVHOV2JpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYjBO5hJOTBizszN NYjWdVg4UUN3ME6xNEDPxE1? NUH5b45pOjB5NEC2NlM>
CHLA-90 NHvQPG9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVyxNEDPxE1? MYfJR|UxRjFyIN88US=> MYqyNFc1ODZ{Mx?=
CHLA-136 M1HaXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGf4NJIyOCEQvF2= M2f1cGlEPTB-MUCg{txO MknCNlA4PDB4MkO=
NALM-6 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M174cVExKM7:TR?= M3;zdGlEPTB;Mk[1JI5O NGDwWGgzODd2ME[yNy=>
COG-LL-317 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPRNVAh|ryP NUnnO3ZnUUN3ME22MlQ6KG6P NGrSRlQzODd2ME[yNy=>
RS4;11 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml2xNVAh|ryP MonTTWM2OD1zNEegcm0> NEjmVYEzODd2ME[yNy=>
MOLT-4 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX7DTJVDOTBizszN MkW5TWM2OD12MDDuUS=> NELpUHUzODd2ME[yNy=>
CCRF-CEM MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXyxNEDPxE1? M3vSfmlEPTB;Mk[4JI5O M1n2S|IxPzRyNkKz
Kasumi-1 NWfYPGV{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXPnOZVNOTBizszN NVm5fXhVUUN3ME2xNFchdk1? NYPiOohJOjB5NEC2NlM>
Karpas-299 NHXUS2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4DtZVExKM7:TR?= MlnaTWM2OD1{LkmzJO69VQ>? MkfONlA4PDB4MkO=
Ramos-RA1 NHzxVpJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUCxNEDPxE1? MUTJR|UxRTdwM{Wg{txO NFfhdW4zODd2ME[yNy=>
H1299 M4DD[WtqdmG|ZTDhd5NigQ>? M{TXZlExKM7:TR?= NILmToZqdmirYnn0d{BKU0KNRT3pcoR2[2WmIFHreEBC[3SrdnH0bY9v MnLuNlE6ODh4MU[=

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

Protocol

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

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01749384 Completed Solid Neoplasm National Cancer Institute (NCI) December 6 2012 Phase 1
NCT01755767 Completed Hepatocellular Carcinoma Daiichi Sankyo Inc.|ArQule December 27 2012 Phase 3
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 25 2011 Phase 1
NCT01654965 Completed Adult Solid Neoplasm National Cancer Institute (NCI) July 24 2012 Phase 1
NCT02608411 Terminated Carcinoma Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1

Tech Support

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

Handling Instructions

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID