Tivantinib (ARQ 197)

Catalog No.S2753

Tivantinib (ARQ 197) Chemical Structure

Molecular Weight(MW): 369.42

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

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2 Customer Reviews

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

    Clin Cancer Res, 2017. Tivantinib (ARQ 197) purchased from Selleck.

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

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

Purity & Quality Control

Choose Selective c-Met Inhibitors

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 NHXxOFNMcW6jc3WgZZN{[Xl? M3i2SJ4yOCEQvF2= MVzpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MlTENlA1QDRyMUi=
HT29 M{DMNGtqdmG|ZTDhd5NigQ>? MXj+NVAh|ryP MV\pcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M3zMXVIxPDh2MEG4
MDA-MB-231 NGX1NI1McW6jc3WgZZN{[Xl? MXP+NVAh|ryP NYj1R21HcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NFWyZW0zODR6NECxPC=>
NCI-H441 NG\5S2RMcW6jc3WgZZN{[Xl? M1rzWZ4yOCEQvF2= M1XNN4lvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MWGyNFQ5PDBzOB?=
SK-MEL-28 NI\PWYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXizN{DPxE1? MYnJR|UxRjN|IN88US=> NG\HcI4zODR6NECxPC=>
NCI-H661 MoX1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3;TZ|M{KM7:TR?= MVHJR|UxRjN|IN88US=> NFX1O5czODR6NECxPC=>
NCI-H446 MmrHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2Xyd|M{KM7:TR?= MVvJR|UxRTdizszN M{fqd|IxPDh2MEG4
MDA-MB-231 NUi0bnVsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPzVGQ{OyEQvF2= NVHnfFk2UUN3ME2wMlU2KM7:TR?= Mn6wNlA1QDRyMUi=
DLD-1 NIDDU3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXPVOol1OzNizszN M4[0T2lEPTB;MD61N{DPxE1? NFnTUW8zODR6NECxPC=>
A549 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1ftcVM{KM7:TR?= NIDoSGNKSzVyPUCuOVkh|ryP M17jSVIxPDh2MEG4
SK-OV-3 NEnLSHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3m2VFM{KM7:TR?= MkX4TWM2OD1yLk[2JO69VQ>? MVuyNFQ5PDBzOB?=
NCI-H460 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVSzN{DPxE1? M1;IdGlEPTB;MD62JO69VQ>? MV:yNFQ5PDBzOB?=
A375 NEHNSodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVmzN{DPxE1? M1HnUGlEPTB;MD60NkDPxE1? M4fiU|IxPDh2MEG4
NCI-H441 M3z1cWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVq3c3F7OzNizszN NYn0PWExUUN3ME2wMlMh|ryP NELQXZgzODR6NECxPC=>
HT29 M1vYSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4jJeVM{KM7:TR?= NF\uZmZKSzVyPUCuOFkh|ryP MXiyNFQ5PDBzOB?=
MKN-45 NWD6RmhsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MknuN|Mh|ryP NHzzTmNKSzVyPUCuOVgh|ryP NI\UemEzODR6NECxPC=>
HT29 NYD0T4xZSXCxcITvd4l{KGG|c3H5 NXrnR4d4hjFyIN88US=> MoPid4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NWfHeJhWOjB2OESwNVg>
MKN-45 NETmdWJCeG:ydH;zbZMh[XO|YYm= Ml25glExKM7:TR?= NVX1XWVTe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NIHaOXYzODR6NECxPC=>
MDA-MB-231 MkHmRZBweHSxc3nzJIF{e2G7 MUT+NVAh|ryP MXrtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw Mo\0NlA1QDRyMUi=
MDA-MB-231/TGL NF;hNndIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkCzglExOCEQvF2= M2DVSWdKPTB;MT6yJO69VQ>? NXrhPHU{OjJyMke2PVA>
1833/TGL MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2\OR54yODBizszN MnfHS2k2OD1|Lkeg{txO Mmr3NlIxOjd4OUC=
EBC1 MXvDfZRwfG:6aXRCpIF{e2G7 MnfoglExKM7:TR?= M1vre4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NHn0R3AzOzV7OEK3Oi=>
SNU638 M3ThVmN6fG:2b4jpZ:Kh[XO|YYm= NXyzXlgyhjFyIN88US=> MUfpcohq[mm2czD0bIUh[2WubDDndo94fGhw MmnYNlM2QTh{N{[=
A549 M2HzXWN6fG:2b4jpZ:Kh[XO|YYm= MUD+NVAh|ryP M2jzV45wfCCjZn\lZ5Q> NFjkfHQzOzV7OEK3Oi=>
H460 M4\FcGN6fG:2b4jpZ:Kh[XO|YYm= M{PVUZ4yOCEQvF2= NHXNOnhvd3RiYX\m[YN1 MW[yN|U6QDJ5Nh?=
HCC827 NVTTUIEyS3m2b4TvfIlkyqCjc4PhfS=> Ml;rglExKM7:TR?= NVfqVXMxdm:2IHHm[oVkfA>? MnPJNlM2QTh{N{[=
A549 NXW3U4ZVTnWwY4Tpc44h[XO|YYm= MYCxNEDPxE1? MnnJ[Il{enWydIOgcYlkem:2dXL1cIU> MXGyN|U6QDJ5Nh?=
EBC1 Ml7vSpVv[3Srb36gZZN{[Xl? MWOxNEDPxE1? Mn;V[Il{enWydIOgcYlkem:2dXL1cIU> MnTaNlM2QTh{N{[=
H460 NFfJWpNHfW6ldHnvckBie3OjeR?= MU[xNEDPxE1? Mmq1bY5pcWKrdIOgeJVjfWyrbjDwc4x6dWW{aYrheIlwdg>? M2j4b|I2OzF|MEGw
K562/VCR MmHUR5l1d3SxeHnjxsBie3OjeR?= Mor1glExKM7:TR?= NUXpNlM6e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 MVyyOVMyOzBzMB?=
CEM/VBL NFW4NnpEgXSxdH;4bYPDqGG|c3H5 NEfRcmd,OTBizszN MoHRd4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 MVyyOVMyOzBzMB?=
U266 M2njSWN6fG:2b4jpZ:Kh[XO|YYm= M4PGdJ4{KM7:TdMg MVHJR|UxRTFwMTFOwG0> NV;PWlB2OjV6MUCwNVM>
OPM-2 Mn\IR5l1d3SxeHnjxsBie3OjeR?= M{XmdZ4{KM7:TdMg NXvkVFE1UUN3ME2xMlgh|ryP NHXVdHQzPThzMECxNy=>
MM.1S NULJZ4NES3m2b4TvfIlkyqCjc4PhfS=> NEnMdJB,OyEQvF5CpC=> Ml7yTWM2OD1zLk[g{txO M1uxe|I2QDFyMEGz
MM.1R NVXRN2M6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2ftV|Mh|ryPwrC= NX;4bmdscW6qaXLpeJMh[2WubDDndo94fGhiYomgOFkm MU[yOVgyODBzMx?=
RPMI-8226 M2HP[2N6fG:2b4jpZ:Kh[XO|YYm= M4O0UZ4{KM7:TdMg NEDHNYpKSzVyPUCuPUDPxE1? MlHtNlU5OTByMUO=
ANBL-6 M{nteGN6fG:2b4jpZ:Kh[XO|YYm= MV:xJO69VcLi M3yxUIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M4i5VVI2QDFyMEGz
ANLB-6/V10R M1\CeWN6fG:2b4jpZ:Kh[XO|YYm= MUmxJO69VcLi NGjTfJZqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NYO3[W9vOjV6MUCwNVM>
KAS-6/1 MlfDR5l1d3SxeHnjxsBie3OjeR?= NVTr[G9EOSEQvF5CpC=> NX\ETG86cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> M1TzV|I2QDFyMEGz
KAS-6/V10R NYjTcWNyS3m2b4TvfIlkyqCjc4PhfS=> NVn4R4h7OSEQvF5CpC=> NVXoeXk3cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NILETmIzPThzMECxNy=>
KAS-6/R10R MkHIR5l1d3SxeHnjxsBie3OjeR?= MWWxJO69VcLi MWjpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= M1PiflI2QDFyMEGz
8226/S MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXjqOph[OyEQvF5CpC=> MonHbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NFz6RlgzPThzMECxNy=>
8226/LR-5 NUnXUm1xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnhN{DPxE4EoB?= NIPjeWFqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> NVzQSHl[OjV6MUCwNVM>
Huh7 MXfDfZRwfG:6aXRCpIF{e2G7 MkT4glQvQCEQvF5CpC=> NGP3d3VFVVOR Mm\aTWM2OD17Lkmgcm0> MVGyOlI2QTJ3MB?=
Hep3B MUfDfZRwfG:6aXRCpIF{e2G7 MXP+OE45KM7:TdMg MnjQSG1UVw>? NG\3ZlFKSzVyPUS0PE44KG6P MUWyOlI2QTJ3MB?=
HepG2 M{\0WWN6fG:2b4jpZ:Kh[XO|YYm= M3;XOp41NjhizszNxsA> NFe3T4pFVVOR NHTuOndKSzVyPUGzPU44PyCwTR?= M4fDc|I3OjV7MkWw
Chang NI\tfGREgXSxdH;4bYPDqGG|c3H5 MmHkglQvQCEQvF5CpC=> M3zITmROW09? MU\JR|UxRTR2OD63JI5O MUWyOlI2QTJ3MB?=
Huh7 NEHwNVNHfW6ldHnvckBie3OjeR?= NUG2c5R[OS54IN88UeKh MUDEUXNQ M3PMWYNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M1XsPVI3OjV7MkWw
Hep3B NVvIW4F[TnWwY4Tpc44h[XO|YYm= MoLBNU43KM7:TdMg MVHEUXNQ Mnf6Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MUOyOlI2QTJ3MB?=
HepG2 MmHnSpVv[3Srb36gZZN{[Xl? NWrDTnpZOS54IN88UeKh MlrOSG1UVw>? MnHzZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M2HWbVI3OjV7MkWw
Chang M4DtdmZ2dmO2aX;uJIF{e2G7 Mn:3NU43KM7:TdMg NH3WeG1FVVOR MlHYZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NVfpXlA2OjZ{NUmyOVA>
MHCC97L M{faXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFv6U|Z,OTBizszN M3;BR2ROW09? NFWySlBKSzVyPUOxOUBvVQ>? MWSyOlQ2QDl3Mx?=
MHCC97H MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXHjSHpYhjFyIN88US=> NVLEXHI6TE2VTx?= NUnoflExUUN3ME2zOljjiIlibl2= MVOyOlQ2QDl3Mx?=
Huh7 MonIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUjSZ|M1hjFyIN88US=> NIPo[2RFVVOR NWjFUIZ{UUN3ME2yOlUhdk1? NGjRR4ozPjR3OEm1Ny=>
HepG2 M2n2ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NECzbXZ,OTBizszN MYTEUXNQ M131Z2lEPTB;M{myJI5O MWiyOlQ2QDl3Mx?=
MHCC97L M1nFZ2Z2dmO2aX;uJIF{e2G7 MXWxJO69VcLi MWDEUXNQ NGW0e3JqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v MUOyOlQ2QDl3Mx?=
Huh7 M1ztN2Z2dmO2aX;uJIF{e2G7 MlzuNUDPxE4EoB?= MkXwSG1UVw>? NFnmcZZqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v M{fpblI3PDV6OUWz
MHCC97L NHvCfWhCeG:ydH;zbZMh[XO|YYm= MmLONUDPxE4EoB?= M3XTXGROW09? NG\QNINqdmS3Y3XzJIFxd3C2b4Ppdy=> MluxNlY1PTh7NUO=
Huh7 MlXhRZBweHSxc3nzJIF{e2G7 NX[4OYR6OSEQvF5CpC=> NFn1[nJFVVOR MmfKbY5lfWOnczDhdI9xfG:|aYO= M{jRRlI3PDV6OUWz
C3H 10T1/2 mouse fibroblasts MoLxT4lv[XOnIHHzd4F6 NVKzbGZ5OjVizszN NEHUXpFFVVOR Mn7idoVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> Mli0NlA2OzR|NEW=
H23 NYHwWmpwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXmyOUDPxE1? MkjaSG1UVw>? NIrMdm9{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M4rvWVIxPTN2M{S1
WM35 Mo\XS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{HUT|ExKM7:TR?= NGnMVJFFVVOR Ml3Qd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NWDY[3FkOjB3M{SzOFU>
NIH 3T3 NUHDVGRDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYOxNEDPxE1? MmfYSG1UVw>? NXzzPXlH\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MknKNlA2OzR|NEW=
H838 M4rn[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX7iS|ZjOTBizszN NXjIZ4NLTE2VTx?= Mlry[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 Mmf3NlA2OzR|NEW=
H1395 MkTBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUHiPY5wOTBizszN NYfQWow6TE2VTx?= MV\kc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= MXqyNFU{PDN2NR?=
Quiescent S2 M3vwN2tqdmG|ZTDhd5NigQ>? M4jqVFMxKM7:TR?= NUTLdI06TE2VTx?= MYfjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? Mn3SNlE2OTh7MUW=
PC3 MX;BdI9xfG:|aYOgZZN{[Xl? Mnr1NlAh|ryP MUjEUXNQ NEHCZ2VqdmS3Y3XzJIFxd3C2b4Ppdy=> MXeyNVcxQTF|MB?=
Du145 NWPrdoRwSXCxcITvd4l{KGG|c3H5 NEfM[JozOCEQvF2= M3u0dGROW09? NYDhPFhkcW6mdXPld{BieG:ydH;zbZM> NFPYNYozOTdyOUGzNC=>
LNCaP NUKyUHZTSXCxcITvd4l{KGG|c3H5 MX2yNEDPxE1? Ml6ySG1UVw>? MlHObY5lfWOnczDhdI9xfG:|aYO= MV6yNVcxQTF|MB?=
LAPC-4 NEfPfpVCeG:ydH;zbZMh[XO|YYm= MVyyNEDPxE1? MU\EUXNQ MXnpcoR2[2W|IHHwc5B1d3Orcx?= NXjOdnBFOjF5MEmxN|A>
LNCaP NFvtSXBHfW6ldHnvckBie3OjeR?= NETFRoEzOCEQvF2= M2TyPWROW09? NYfYPZdy\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= M1ztfFIyPzB7MUOw
LAPC-4 M4jUUmZ2dmO2aX;uJIF{e2G7 MX6yNEDPxE1? MnvwSG1UVw>? NIKwfXdl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| M4DRO|IyPzB7MUOw
Kasumi-1 NYjmb|hiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWr+OVAh|ryP NGPCeHdFVVOR MlTXbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NYjTNpRJOjN|OUC1N|Y>
SKNO-1 NXy2enBOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVjSbVVbhjVyIN88US=> MnPJSG1UVw>? NXHLflRscW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MVeyN|M6ODV|Nh?=
Kasumi-1 NVz0eoJ1U2mwYYPlJIF{e2G7 MluzglExKM7:TR?= M1q2XWROW09? NFL2N5Zz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> NXfZRmJvOjN|OUC1N|Y>
SKNO-1 MXnLbY5ie2ViYYPzZZk> M4LFNJ4yOCEQvF2= MorESG1UVw>? NWDYbXg3emWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z Mn7MNlM{QTB3M{[=
A549 NVrGOmN4TnWwY4Tpc44h[XO|YYm= NX;DeoRnOTBizszN NYHJTYE1TE2VTx?= M1HLVYVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> MUmyOFc1PjV5NB?=
NRK-52E M13oe2Z2dmO2aX;uJIF{e2G7 M4\nV|ExKM7:TR?= NFzLeW1FVVOR MkLFbY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiU2TBWFMhdnWlbHXhdkB1emGwc3zvZ4F1cW:wIHHu[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEBkd2yuYXflckBKXiCjbnSg[oljem:wZXP0bY4> M4TIbVI2ODh6MECy
PC12 MkXOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYf3c5c5hjF{LkWg{txO MX3EUXNQ NHHTOXVxemW4ZX70d{BVW0FvaX7keYNm\CCwZYXybZRmKG[xcn3heIlwdg>? MnjzNlUyOjh|OE[=
HPMCs NGjKPWVHfW6ldHnvckBie3OjeR?= NEHL[XJz\X[ncoPld{BmeGm2aHXsbYFtKHSxIH3ld4Vv[2i7bXHsJJRz[W6|aYTpc44hd2ZiaIXtZY4heGW{aYTvcoVidCCvZYPveIhmdGmjbDDj[Yxtew>? NYDmR2tiOjZyNEW3PFA>
A549 M2PkXmZ2dmO2aX;uJIF{e2G7 MkHhglUxKM7:TR?= M3XLTWROW09? NHvuTFdi\m[nY4TzJJRp\SC4aYLhcEBtcW[nIHP5Z4xmKGGwZDDoc5N1KHKnc4DvcpNm MWSyOlcyOTd2OB?=
RAW264.7 MkXySpVv[3Srb36gZZN{[Xl? NGDIRY9,OzBizszN NFGwNWlFVVOR NV20e|ZtemWmdXPld{Bxem9vaX7mcIFudWG2b4L5JIdmdmViZYjwdoV{e2mxbh?= NUi1enN[OjZ5MUi1PFY>
MEMM MXLLbY5ie2ViYYPzZZk> MljiNVUhyrWP MkDVSG1UVw>? NYXtVFVI\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> NWftdndEOjZ7MkG1NFY>
MEMM MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1fYSp4zOCEEtV2= NYf2SZQ{TE2VTx?= M3fBbolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MWSyOlkzOTVyNh?=
MEMM NIPoU5VCeG:ydH;zbZMh[XO|YYm= Mlm5NVUhyrWP NEjTeIdFVVOR NHLKe5RqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ MWOyOlkzOTVyNh?=
T47D NXzXXYFiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHXZSYIyOCEQvF2= M2e5OWROW09? MYfJR|UxRTd{IH7N M4i5SlE5OzhzNES0
ZR-75-1 NFfJVGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NE\LcowyOCEQvF2= NHSyT2tFVVOR M3H6ZmlEPTB;N{mgcm0> NIHaVFIyQDN6MUS0OC=>
BT474 MmXyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4H4c|ExKM7:TR?= Mm\0SG1UVw>? NH;S[YdKSzVyPUi2JI5O MnX4NVg{QDF2NES=
HCC1954 M2TRWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHTiZYoyOCEQvF2= MlvqSG1UVw>? NV7Reo9ZUUN3ME2xNVkhdk1? Mmj1NVg{QDF2NES=
MDA-MB-453 Mn3FS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4P0ZVExKM7:TR?= MYrEUXNQ NXjmTGg2UUN3ME25O|Uhdk1? MoXuNVg{QDF2NES=
MDA-MB-468 MlXJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVqxNEDPxE1? M{HqSWROW09? NGXNdHdKSzVyPUOyNFghdk1? NHjsVXQyQDN6MUS0OC=>
SkBr3 MmTDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVWyd|djOTBizszN MUHEUXNQ M4HsRWlEPTB-MUCsNFAxKG6P NXjEcHJ1OTh|OEG0OFQ>
MDA-MB-231 NYLlWYFST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWS1SZJZOTBizszN MlLtSG1UVw>? NWfWTppzUUN3ME6xNEwxODBibl2= NIny[mwyQDN6MUS0OC=>
HCT116 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mmn2NVAh|ryP NGnNNpBFVVOR NEX1Z|hKSzVyPUW4N|Yhdk1? MlPXNVg{QDF2NES=
HT29 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkPnNVAh|ryP MVzEUXNQ MULJR|UxRjFyLECwNEBvVQ>? MUOxPFM5OTR2NB?=
HFF MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3zNUVExKM7:TR?= NYXiRWlXTE2VTx?= NEXKeHZKSzVyPUe2NVUhdk1? NHniV4oyQDN6MUS0OC=>
HN5 NGLyRpJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{W5eFExKM7:TR?= NWHhWo85TE2VTx?= NHe4Zm1KSzVyPkGwMFAxOCCwTR?= NUXGNXlwOTh|OEG0OFQ>
786-0 MkH0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXX2V3FiOTBizszN NEPibHFFVVOR NHzSNIxKSzVyPUSwNFkhdk1? M37oRlE5OzhzNES0
H157 MmnSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFjafJQyOCEQvF2= NVTtcJp2TE2VTx?= NELOVYxKSzVyPUK2OFIhdk1? NGLHeZEyQDN6MUS0OC=>
NCI-H460 MljJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlWyNVAh|ryP MYDEUXNQ MnnDTWM2OD5{LEWwNEBvVQ>? M3nucFE5OzhzNES0
SKOV-3 M1vw[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmC0NVAh|ryP Ml3oSG1UVw>? NWX4XG84UUN3ME2yNVI3KG6P MlXmNVg{QDF2NES=
OVCAR-3 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV2xNEDPxE1? NYnKSpFRTE2VTx?= Mk\sTWM2OD1{OUG4JI5O NYXqVW1mOTh|OEG0OFQ>
BXPC3 NEXwR3ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV6xNEDPxE1? NIfPUIJFVVOR NUfk[3RkUUN3ME2zNVQyKG6P NIfvZ28yQDN6MUS0OC=>
MiaPaCa MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHGxPVAyOCEQvF2= M2DUSWROW09? NF7NOmVKSzVyPUW0N|Mhdk1? NVPFOGlyOTh|OEG0OFQ>
PANC-1 MoHvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHPYS2YyOCEQvF2= NHnIV5hFVVOR MV3JR|UxRTh4OEGgcm0> NYDmXVF[OTh|OEG0OFQ>
LNCaP NVjYcndUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkflNVAh|ryP M{DEOGROW09? M3PEZWlEPTB;MUS3JI5O M3zBd|E5OzhzNES0
DU145 Ml20S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{S3V|ExKM7:TR?= MVTEUXNQ MoLBTWM2OD1|OEGyJI5O MnXUNVg{QDF2NES=
PC3 M3fQU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF:0fZcyOCEQvF2= NH;6SYhFVVOR NF\Bc5lKSzVyPkGwMFAxOCCwTR?= MorsNVg{QDF2NES=
BT474 MWXLbY5ie2ViYYPzZZk> MoLDNVAh|ryP M2jiXGROW09? MmTXbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTZyIH7N M1f0XlE5OzhzNES0
786-0 M2fUNmtqdmG|ZTDhd5NigQ>? MV6xNEDPxE1? MXfEUXNQ M17nO4lvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDF3MDDuUS=> NH\NcXEyQDN6MUS0OC=>
LNCaP MXnLbY5ie2ViYYPzZZk> MX:xNEDPxE1? M3zu[WROW09? NFy2fpRqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2MzDuUS=> MoPJNVg{QDF2NES=
PC3 M13TU2tqdmG|ZTDhd5NigQ>? MlPpNVAh|ryP NGjlb3NFVVOR MU\pcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1QSCwTR?= MmrZNVg{QDF2NES=
KARPAS-231 M2e0dGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYixNEDPxE1? M4XiXGROW09? MWTFR|UxRTRzIH7N MXKxPVA3PDd|MB?=
CCRFSB MoezS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSxNEDPxE1? Ml;2SG1UVw>? NUX5e5hCTUN3ME2xOVUhdk1? NUf5OmZmOTlyNkS3N|A>
SUP B15 NVvPOZZMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mom0NVAh|ryP NFmxTJFFVVOR NInmOJVGSzVyPUG5O{BvVQ>? NX;5bZBiOTlyNkS3N|A>
SD-1 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3\QeVExKM7:TR?= NYXvSWRPTE2VTx?= NHfYVFVGSzVyPUOyNEBvVQ>? MoHxNVkxPjR5M{C=
RS4;11 NHLWUJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmfKNVAh|ryP MW\EUXNQ NWrobVNDTUN3ME22OVQhdk1? MYexPVA3PDd|MB?=
MN-60 NYPhOGg3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoTSNVAh|ryP NX\jeoltTE2VTx?= NWPIeFdFTUN3ME2zOlAzKG6P MYCxPVA3PDd|MB?=
Tanoue NW[4N4dGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M33JWlExKM7:TR?= MULEUXNQ MoXvSWM2OD12NUG3JI5O MlHRNVkxPjR5M{C=
RCH-ACV NU[zbWx3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojNNVAh|ryP MVvEUXNQ NXrOWXlHTUN3ME2xOVIhdk1? NGn2bmUyQTB4NEezNC=>
SEM M2niZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWjlTJBbOTBizszN MkfnSG1UVw>? M4jBNmVEPTB;MkCyJI5O MW[xPVA3PDd|MB?=
KASUMI-2 NWLrOZBST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHvNTWEyOCEQvF2= MYrEUXNQ M4PxOGVEPTB;MkK1JI5O NFzJSpoyQTB4NEezNC=>
REH MkLSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPQNVAh|ryP MYfEUXNQ M4rvXmVEPTB;Mki4JI5O MWmxPVA3PDd|MB?=
697 NHL6WIdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH7YUlIyOCEQvF2= NVXm[lU3TE2VTx?= NXnnbndFTUN3ME2zN|ghdk1? M{fHUFE6ODZ2N{Ow
NALM-6 M4C2Zmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnPPNVAh|ryP MlraSG1UVw>? M1joTmVEPTB;NEKxJI5O MXmxPVA3PDd|MB?=
MHH-CALL–3 M3TKNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYmxNEDPxE1? MUPEUXNQ NHvJdVNGSzVyPUixNkBvVQ>? MnnFNVkxPjR5M{C=
MHH-CALL–2 NWjKdZhGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGO0O44yOCEQvF2= MV\EUXNQ MXzFR|UxRTJzMUSgcm0> MYCxPVA3PDd|MB?=
J.GAMMA-1 M1vpTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3z2U|ExKM7:TR?= NX6yUVdRTE2VTx?= MlXSSWM2OD14NTDuUS=> NXTxOGM6OTlyNkS3N|A>
JR45.01 M2L2eWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrDVFc{OTBizszN MXPEUXNQ M{DxfGVEPTB;Nkigcm0> Ml24NVkxPjR5M{C=
A3 M3jZUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUjFcJdXOTBizszN MXrEUXNQ MlTUSWM2OD14OTDuUS=> NETmfIEyQTB4NEezNC=>
I 2.1 NYC0Z|BlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXnGVWdyOTBizszN MknHSG1UVw>? NFnySHRGSzVyPUezJI5O NVrWc|UyOTlyNkS3N|A>
MOLT-3 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWKxNEDPxE1? MoCwSG1UVw>? NHXnfm1GSzVyPUe0JI5O MnHrNVkxPjR5M{C=
P116 NV;FWI1NT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4WzZlExKM7:TR?= MWfEUXNQ NGrldnNGSzVyPUe4JI5O MUixPVA3PDd|MB?=
J.Cam1.6 MoXwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDidZhROTBizszN MVrEUXNQ NV\YXGp6TUN3ME23PUBvVQ>? NE\GSoEyQTB4NEezNC=>
I 9.2 NYDMNZJCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWexNEDPxE1? M3vIdmROW09? M{\IV2VEPTB;OECgcm0> M4OyRVE6ODZ2N{Ow
LOUCY NFjDeolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2D4VFExKM7:TR?= MXvEUXNQ Mn61SWM2OD1zMUegcm0> MYOxPVA3PDd|MB?=
J.RT3-T3.5 NXfwflJCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo\wNVAh|ryP MkfxSG1UVw>? M{DhW2VEPTB;MUKzJI5O NHLqSI4yQTB4NEezNC=>
800000 M2LF[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHm5V2kyOCEQvF2= NWLSOmNxTE2VTx?= NF7FWpVGSzVyPUG2N{BvVQ>? MUGxPVA3PDd|MB?=
Jurkat NV;qdIRnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUexNEDPxE1? M{\MR2ROW09? MVTFR|UxRTJ{NTDuUS=> M1LWe|E6ODZ2N{Ow
MOLT-4 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHkNVAh|ryP NHz4VVlFVVOR NXrDbGE3TUN3ME2yN|Ihdk1? M4fHc|E6ODZ2N{Ow
Molt-16 NV64dmprT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVPYS5BoOTBizszN NFvBdYVFVVOR MX;FR|UxRTJ2MTDuUS=> MWmxPVA3PDd|MB?=
CEM/C3 MnPNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnzONVAh|ryP MoL4SG1UVw>? NYDueJdMTUN3ME2yOVchdk1? MVuxPVA3PDd|MB?=
CEM/C2 NEDvUG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGjBPGQyOCEQvF2= NUHFW2R7TE2VTx?= NEnIbG5GSzVyPUK3NUBvVQ>? MU[xPVA3PDd|MB?=
CCRFCEM Mo[1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWmxNEDPxE1? MXHEUXNQ MlvySWM2OD1|Mkegcm0> NEnOSHoyQTB4NEezNC=>
CEM/C1 M3fuWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF3rdpoyOCEQvF2= NF74THRFVVOR MlfBSWM2OD1|OEKgcm0> NF3SZpEyQTB4NEezNC=>
SUPTI[VB] NH;VT2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1LyeVExKM7:TR?= MX\EUXNQ M{O0NmVEPTB;NkG5JI5O NYDqOo8{OTlyNkS3N|A>
CCRF–HSB-2 NHfub41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWqxNEDPxE1? Mlq2SG1UVw>? NGnGSlZGSzVyPUKxNVchdk1? NXHUR4k1OTlyNkS3N|A>
I 2.1 MXvBdI9xfG:|aYOgZZN{[Xl? NH3HcmoyOCEQvF2= MkS1SG1UVw>? NXG5Tox4cW6mdXPld{BieG:ydH;zbZM> MofuNVkxPjR5M{C=
I 9.2 MU\BdI9xfG:|aYOgZZN{[Xl? MY[xNEDPxE1? M2C5RWROW09? Ml3QbY5lfWOnczDhdI9xfG:|aYO= M2n2NVE6ODZ2N{Ow
A3 NIjsc5hCeG:ydH;zbZMh[XO|YYm= Mn7vNVAh|ryP M2rvemROW09? NFrCNZBqdmS3Y3XzJIFxd3C2b4Ppdy=> MlXnNVkxPjR5M{C=
RD MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUmxNEDPxE1? MmDMTWM2OD5zMDFOwG0> MUOyNFc1ODZ{Mx?=
Rh41 Ml30S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVvoeY5SOTBizszN MWTJR|UxRTN|Lkigcm0> MlvtNlA4PDB4MkO=
Rh18 Mn7GS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIfPbWkyOCEQvF2= NUOxeGFOUUN3ME2zNFMhdk1? MoTKNlA4PDB4MkO=
Rh30 NEPPPYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4HjbVExKM7:TR?= NXnmbYlqUUN3ME20MlgyKM7:TR?= NHPzWWwzODd2ME[yNy=>
BT-12 NVe3ToFrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlrJNVAh|ryP MUnJR|UxRjFyIN88US=> NEKxOIIzODd2ME[yNy=>
CHLA-266 NHLlZpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkHvNVAh|ryP NHvjSHdKSzVyPUGuNlIh|ryP NYr6d2FvOjB5NEC2NlM>
TC-71 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF\XdWYyOCEQvF2= Ml3NTWM2OD1{LkWyJO69VQ>? MUCyNFc1ODZ{Mx?=
CHLA-9 M{Ptc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUnnVJF2OTBizszN NEnBW4NKSzVyPUW5NUBvVQ>? NX\ES5l4OjB5NEC2NlM>
CHLA-10 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1K3WVExKM7:TR?= MmrVTWM2OD1zMEKgcm0> M3n4b|IxPzRyNkKz
CHLA-258 Mn\sS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXT3bIRPOTBizszN NIH5VIhKSzVyPUGuNFUh|ryP NYDhUGM1OjB5NEC2NlM>
GBM2 Mom2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWixNEDPxE1? NGrHc2hKSzVyPUmuNVUh|ryP NISxRZIzODd2ME[yNy=>
NB-1643 M1rHNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1z4WFExKM7:TR?= NFv0U49KSzVyPUWuOEDPxE1? M1nxSlIxPzRyNkKz
NB-Ebc1 NH\oSZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnfoNVAh|ryP MkfETWM2OD5zMDFOwG0> NUj5N|JmOjB5NEC2NlM>
CHLA-90 NF;STVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MorXNVAh|ryP MXrJR|UxRjFyIN88US=> M1ryRVIxPzRyNkKz
CHLA-136 MkfWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmK5NVAh|ryP M1\FN2lEPTB-MUCg{txO M1rLXlIxPzRyNkKz
NALM-6 MnvIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVOxNEDPxE1? M3P2RWlEPTB;Mk[1JI5O MUOyNFc1ODZ{Mx?=
COG-LL-317 M2PXW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlLzNVAh|ryP M1L6XmlEPTB;Nj60PUBvVQ>? NWO1cGlFOjB5NEC2NlM>
RS4;11 M2njPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF:zblQyOCEQvF2= M2KzUWlEPTB;MUS3JI5O MoLzNlA4PDB4MkO=
MOLT-4 NHTTWHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGDkR3kyOCEQvF2= M4DseWlEPTB;NECgcm0> M4PTSFIxPzRyNkKz
CCRF-CEM MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXW3RlJsOTBizszN NXG1NJkyUUN3ME2yOlghdk1? M{SwXlIxPzRyNkKz
Kasumi-1 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIHjblgyOCEQvF2= MXnJR|UxRTFyNzDuUS=> MlPVNlA4PDB4MkO=
Karpas-299 NUTnUHdRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVHy[FU4OTBizszN M1;5U2lEPTB;Mj65N{DPxE1? NFnUSGMzODd2ME[yNy=>
Ramos-RA1 M1S1OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm[5NVAh|ryP MYHJR|UxRTdwM{Wg{txO MlPYNlA4PDB4MkO=
H1299 NVe0W|VKU2mwYYPlJIF{e2G7 MXKxNEDPxE1? MnHvbY5pcWKrdIOgTWtDU0VvaX7keYNm\CCDa4SgRYN1cX[jdHnvci=> MUiyNVkxQDZzNh?=

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

Protocol

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

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 24, 2011 Phase 1
NCT02608411 Recruiting Carcinoma, Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace, Inc. April 2014 Phase 1
NCT02029157 Recruiting Liver Cancer Kyowa Hakko Kirin Co., Ltd January 2014 Phase 3
NCT01892527 Active, not recruiting Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro, MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Active, not recruiting Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro, MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2

Tech Support

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID