Tivantinib (ARQ 197)

Catalog No.S2753

Tivantinib (ARQ 197) Chemical Structure

Molecular Weight(MW): 369.42

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

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1 Customer Review

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

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

Purity & Quality Control

Choose Selective c-Met Inhibitors

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 M2CxdWtqdmG|ZTDhd5NigQ>? NHvVfFJ,OTBizszN M13BWolvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= M2LlN|IxPDh2MEG4
HT29 NV3yU3F6U2mwYYPlJIF{e2G7 MnPwglExKM7:TR?= MnXIbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MYiyNFQ5PDBzOB?=
MDA-MB-231 MmX5T4lv[XOnIHHzd4F6 M{jXZZ4yOCEQvF2= M3rse4lvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= MnPwNlA1QDRyMUi=
NCI-H441 NEfXTm1McW6jc3WgZZN{[Xl? NE[yb5d,OTBizszN NXOwfXJlcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MVqyNFQ5PDBzOB?=
SK-MEL-28 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWCzN{DPxE1? NXrBVIJ{UUN3ME6zN{DPxE1? MV:yNFQ5PDBzOB?=
NCI-H661 NXPLeZhYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1i0TFM{KM7:TR?= MXvJR|UxRjN|IN88US=> NWrLfldOOjB2OESwNVg>
NCI-H446 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUWzN{DPxE1? MonQTWM2OD15IN88US=> NUfnTnYzOjB2OESwNVg>
MDA-MB-231 NV7LWZo6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWnZbJd{OzNizszN MoKyTWM2OD1yLkW1JO69VQ>? NHf0V4czODR6NECxPC=>
DLD-1 NIr4T5lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX[zN{DPxE1? NIDM[FhKSzVyPUCuOVMh|ryP NGTvfo0zODR6NECxPC=>
A549 Moe5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVmzN{DPxE1? MnPoTWM2OD1yLkW5JO69VQ>? M2nT[|IxPDh2MEG4
SK-OV-3 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGnHW4Q{OyEQvF2= MkjuTWM2OD1yLk[2JO69VQ>? MWKyNFQ5PDBzOB?=
NCI-H460 MknvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnT4N|Mh|ryP M2fZfGlEPTB;MD62JO69VQ>? MXSyNFQ5PDBzOB?=
A375 NXTWbHFJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIrxUXk{OyEQvF2= M3vVOGlEPTB;MD60NkDPxE1? MUGyNFQ5PDBzOB?=
NCI-H441 M{jZXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV6zN{DPxE1? NWDQfnI4UUN3ME2wMlMh|ryP NUDm[HplOjB2OESwNVg>
HT29 NY[4fWljT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoTpN|Mh|ryP MofSTWM2OD1yLkS5JO69VQ>? NYjlSpFoOjB2OESwNVg>
MKN-45 M{PqXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{joeFM{KM7:TR?= NHjP[FhKSzVyPUCuOVgh|ryP M1LGZVIxPDh2MEG4
HT29 M2W4OWFxd3C2b4Ppd{Bie3OjeR?= NEXTPZZ,OTBizszN NYjSVGVwe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NGjYZ3gzODR6NECxPC=>
MKN-45 NUnmV2l3SXCxcITvd4l{KGG|c3H5 MVX+NVAh|ryP NYfH[VZue2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu M4LFc|IxPDh2MEG4
MDA-MB-231 M4HnXmFxd3C2b4Ppd{Bie3OjeR?= MWX+NVAh|ryP NEPpc45ud2Snc4TsfUBqdmS3Y3XzJIFxd3C2b4Ppd{BjgSB|NTWu MYqyNFQ5PDBzOB?=
MDA-MB-231/TGL NVryVph3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWrHOY5EhjFyMDFOwG0> NIrkTIhIUTVyPUGuNkDPxE1? NGW1OoQzOjB{N{[5NC=>
1833/TGL MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXu4dHJJhjFyMDFOwG0> M4nJNmdKPTB;Mz63JO69VQ>? NGnLW48zOjB{N{[5NC=>
EBC1 NFrpUWhEgXSxdH;4bYPDqGG|c3H5 M{Lid54yOCEQvF2= NHL6ZVBqdmirYnn0d{B1cGViY3XscEBoem:5dHiu M3TwbFI{PTl6Mke2
SNU638 NIDHVllEgXSxdH;4bYPDqGG|c3H5 NFfvdZh,OTBizszN NFu5WVVqdmirYnn0d{B1cGViY3XscEBoem:5dHiu MnvXNlM2QTh{N{[=
A549 M4nqW2N6fG:2b4jpZ:Kh[XO|YYm= NYjCU29zhjFyIN88US=> NWTNWYg3dm:2IHHm[oVkfA>? M{nPdFI{PTl6Mke2
H460 NIPqPFJEgXSxdH;4bYPDqGG|c3H5 NGHzRXl,OTBizszN Mo\oco91KGGoZnXjeC=> NETWS4QzOzV7OEK3Oi=>
HCC827 NYTpc2dFS3m2b4TvfIlkyqCjc4PhfS=> MVz+NVAh|ryP NUnWVW1Wdm:2IHHm[oVkfA>? NFXVRVAzOzV7OEK3Oi=>
A549 NH\VblRHfW6ldHnvckBie3OjeR?= NF;RcZEyOCEQvF2= M4H2R4Rqe3K3cITzJI1q[3KxdIXieYxm MoPSNlM2QTh{N{[=
EBC1 NYPJdYR7TnWwY4Tpc44h[XO|YYm= NFL2eokyOCEQvF2= M4XybIRqe3K3cITzJI1q[3KxdIXieYxm NHHlcm4zOzV7OEK3Oi=>
H460 MUXGeY5kfGmxbjDhd5NigQ>? NUH0TYp2OTBizszN NX:wUHM3cW6qaXLpeJMhfHWkdXzpckBxd2y7bXXybZpifGmxbh?= NGHNVnMzPTNzM{CxNC=>
K562/VCR MXjDfZRwfG:6aXRCpIF{e2G7 MV;+NVAh|ryP MVvzbI94eyCleYTveI95cWNiYXP0bZZqfHl? NV3tTnlGOjV|MUOwNVA>
CEM/VBL MYfDfZRwfG:6aXRCpIF{e2G7 M1;aZZ4yOCEQvF2= NXLoO|F{e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 Mk\HNlU{OTNyMUC=
U266 MULDfZRwfG:6aXRCpIF{e2G7 MnezglMh|ryPwrC= M2HUcGlEPTB;MT6xJO69VQ>? NXvqRm8xOjV6MUCwNVM>
OPM-2 M2fROmN6fG:2b4jpZ:Kh[XO|YYm= NX7OWnQyhjNizszNxsA> NXrYRYs5UUN3ME2xMlgh|ryP M{\IXFI2QDFyMEGz
MM.1S MXrDfZRwfG:6aXRCpIF{e2G7 M3fDVp4{KM7:TdMg MmT4TWM2OD1zLk[g{txO NF\JW4czPThzMECxNy=>
MM.1R MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFv4XYw{KM7:TdMg M{T4eolvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> NUPk[JlUOjV6MUCwNVM>
RPMI-8226 NYnKWYNDS3m2b4TvfIlkyqCjc4PhfS=> MXf+N{DPxE4EoB?= M1jCU2lEPTB;MD65JO69VQ>? MnizNlU5OTByMUO=
ANBL-6 Mn\MR5l1d3SxeHnjxsBie3OjeR?= MXGxJO69VcLi Ml;UbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MnXoNlU5OTByMUO=
ANLB-6/V10R NE\3SmpEgXSxdH;4bYPDqGG|c3H5 MlnPNUDPxE4EoB?= MV7pcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MUKyOVgyODBzMx?=
KAS-6/1 NHXmSnREgXSxdH;4bYPDqGG|c3H5 MnPvNUDPxE4EoB?= MlXZbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MkXJNlU5OTByMUO=
KAS-6/V10R MVzDfZRwfG:6aXRCpIF{e2G7 NEfGe40yKM7:TdMg M{DCVIlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NXPsUFV{OjV6MUCwNVM>
KAS-6/R10R MWfDfZRwfG:6aXRCpIF{e2G7 MXqxJO69VcLi NFTH[5dqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NFrtdI0zPThzMECxNy=>
8226/S MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MorhN{DPxE4EoB?= NF\BNFZqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> NWi0OVlyOjV6MUCwNVM>
8226/LR-5 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX2zJO69VcLi MVnpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= M2joT|I2QDFyMEGz
Huh7 MorrR5l1d3SxeHnjxsBie3OjeR?= M2\yPZ41NjhizszNxsA> MmHmSG1UVw>? MXTJR|UxRTlwOTDuUS=> NFruc3czPjJ3OUK1NC=>
Hep3B NVz5cFc6S3m2b4TvfIlkyqCjc4PhfS=> M37VSZ41NjhizszNxsA> MojVSG1UVw>? MW\JR|UxRTR2OD63JI5O MoG1NlYzPTl{NUC=
HepG2 M2S1PGN6fG:2b4jpZ:Kh[XO|YYm= MXz+OE45KM7:TdMg M3K1T2ROW09? MlrtTWM2OD1zM{muO|chdk1? NGXvNlgzPjJ3OUK1NC=>
Chang M2i4XGN6fG:2b4jpZ:Kh[XO|YYm= MWX+OE45KM7:TdMg MX3EUXNQ M2ixSWlEPTB;NES4Mlchdk1? NIfxV2gzPjJ3OUK1NC=>
Huh7 MXjGeY5kfGmxbjDhd5NigQ>? NGPuWGoyNjZizszNxsA> MkDJSG1UVw>? MV7jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MUiyOlI2QTJ3MB?=
Hep3B NVjXO5h4TnWwY4Tpc44h[XO|YYm= NF;Jc|AyNjZizszNxsA> NH20NlhFVVOR NULmdYE6[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= NW\mPJVVOjZ{NUmyOVA>
HepG2 MlS3SpVv[3Srb36gZZN{[Xl? NXLPbG5DOS54IN88UeKh MY\EUXNQ Ml7GZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NUC5TGVvOjZ{NUmyOVA>
Chang MmfOSpVv[3Srb36gZZN{[Xl? NUTsVGk3OS54IN88UeKh MlG3SG1UVw>? MkXEZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NV21TZVzOjZ{NUmyOVA>
MHCC97L M3zJdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEGxV5R,OTBizszN MnTLSG1UVw>? NVGzNYZDUUN3ME2zNVUhdk1? MX[yOlQ2QDl3Mx?=
MHCC97H NYPqNmhiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXTqPWtUhjFyIN88US=> MlnwSG1UVw>? M2rJVGlEPTB;M{[45qCKKG6P NVjzdFFQOjZ2NUi5OVM>
Huh7 M3XkTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV;Xb4pmhjFyIN88US=> MXzEUXNQ MnTOTWM2OD1{NkWgcm0> Mlr2NlY1PTh7NUO=
HepG2 M1P6fGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYPCeIRWhjFyIN88US=> NF;TZ|NFVVOR NGPwZ3RKSzVyPUO5NkBvVQ>? MkXENlY1PTh7NUO=
MHCC97L NH\sfmNHfW6ldHnvckBie3OjeR?= M4XacFEh|ryPwrC= NEixc5FFVVOR Mn63bY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NIjTbnkzPjR3OEm1Ny=>
Huh7 MV3GeY5kfGmxbjDhd5NigQ>? M{TuU|Eh|ryPwrC= MX\EUXNQ MkTLbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> M4iwe|I3PDV6OUWz
MHCC97L NWLreHYzSXCxcITvd4l{KGG|c3H5 NUWxdnBxOSEQvF5CpC=> NH7uc|ZFVVOR NVvwUohicW6mdXPld{BieG:ydH;zbZM> MYiyOlQ2QDl3Mx?=
Huh7 NFrZeGhCeG:ydH;zbZMh[XO|YYm= NYqxem06OSEQvF5CpC=> MkTkSG1UVw>? MlHzbY5lfWOnczDhdI9xfG:|aYO= NGnTW5MzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts MknsT4lv[XOnIHHzd4F6 NXnu[5VNOjVizszN M{TFTWROW09? NYjLc2pCemWmdXPld{BJcXO2b37lJGg{KGGwZDDIOEBi[2W2eXzheIlwdiCuZY\lcJPDqA>? Mmf0NlA2OzR|NEW=
H23 NWDMSmg5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGDZXZIzPSEQvF2= MoDRSG1UVw>? M4HabJNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NWTpRVFjOjB3M{SzOFU>
WM35 NFnlSnRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlS2NVAh|ryP NFraeZRFVVOR MkDBd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MkXKNlA2OzR|NEW=
NIH 3T3 NV3jUpRxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4PJOlExKM7:TR?= NWrtbYM3TE2VTx?= M3W2XIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MYGyNFU{PDN2NR?=
H838 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkT3NVAh|ryP NYnIZpNoTE2VTx?= M4rFWIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M4TtelIxPTN2M{S1
H1395 NXz0NlF2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1HLeVExKM7:TR?= NWL6fIFwTE2VTx?= NUHpdops\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NIP5[5gzODV|NEO0OS=>
Quiescent S2 NYX1coFmU2mwYYPlJIF{e2G7 MXGzNEDPxE1? NXvTVJZXTE2VTx?= NFPNOI1kd22ybHX0[Yx6KGGkcn;nZZRmeyCWU1GtbY5lfWOnZDDofZBmemGlZYT5cIF1cW:wIH;mJGg{UzSvZUOgbIl{fG:wZYO= M3rDTFIyPTF6OUG1
PC3 MWnBdI9xfG:|aYOgZZN{[Xl? MVSyNEDPxE1? MYfEUXNQ M{m3NYlv\HWlZYOgZZBweHSxc3nz M4D5bVIyPzB7MUOw
Du145 MY\BdI9xfG:|aYOgZZN{[Xl? M{n3W|IxKM7:TR?= NITQ[VFFVVOR NXvHemR[cW6mdXPld{BieG:ydH;zbZM> NWDiW3B7OjF5MEmxN|A>
LNCaP NGj3TnhCeG:ydH;zbZMh[XO|YYm= M361RlIxKM7:TR?= NUfi[5E6TE2VTx?= MoftbY5lfWOnczDhdI9xfG:|aYO= MU[yNVcxQTF|MB?=
LAPC-4 Mni0RZBweHSxc3nzJIF{e2G7 NXyzZpdFOjBizszN NHvmWWNFVVOR NHjRS2tqdmS3Y3XzJIFxd3C2b4Ppdy=> M{nlU|IyPzB7MUOw
LNCaP NGjnUFVHfW6ldHnvckBie3OjeR?= MYSyNEDPxE1? Mn6zSG1UVw>? MWTk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ M1i0cFIyPzB7MUOw
LAPC-4 MnXDSpVv[3Srb36gZZN{[Xl? NFW4O5czOCEQvF2= NIfLeYxFVVOR NU\5PVNK\GWlcnXhd4V{KFCVQTDz[YNz\XSrb36gZY5lKHB4NTDlfJBz\XO|aX;uJIxmfmWucx?= M2LGVVIyPzB7MUOw
Kasumi-1 M1rJSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkfjglUxKM7:TR?= MXrEUXNQ NGXzPGRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NIW3Z|AzOzN7MEWzOi=>
SKNO-1 MmT0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\lcFN,PTBizszN M{PuWGROW09? M17VTYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NVzBfGdPOjN|OUC1N|Y>
Kasumi-1 M2iye2tqdmG|ZTDhd5NigQ>? M3LGWp4yOCEQvF2= M2XqNWROW09? M4exZZJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> NI[0NG8zOzN7MEWzOi=>
SKNO-1 NULKPJVCU2mwYYPlJIF{e2G7 MmLwglExKM7:TR?= MkTtSG1UVw>? MXry[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= MUeyN|M6ODV|Nh?=
A549 NYLGO2V{TnWwY4Tpc44h[XO|YYm= MYixNEDPxE1? MWPEUXNQ NWnwV|ZG\W6qYX7j[ZMhdWm2b4TpZ{Bk[XSjc4Tyc5Bp\Q>? M4fLW|I1PzR4NUe0
NRK-52E MXXGeY5kfGmxbjDhd5NigQ>? NUjL[5dzOTBizszN MUHEUXNQ MnvlbY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiU2TBWFMhdnWlbHXhdkB1emGwc3zvZ4F1cW:wIHHu[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEBkd2yuYXflckBKXiCjbnSg[oljem:wZXP0bY4> MUOyOVA5QDByMh?=
PC12 M4fsfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYj3UXB2hjF{LkWg{txO NELaOWZFVVOR NF7BXYVxemW4ZX70d{BVW0FvaX7keYNm\CCwZYXybZRmKG[xcn3heIlwdg>? NXfJVolxOjVzMkizPFY>
HPMCs NVvxNJdGTnWwY4Tpc44h[XO|YYm= MYTy[ZZmenOnczDldIl1cGWuaXHsJJRwKG2nc3XuZ4h6dWGuIITyZY5{cXSrb36gc4YhcHWvYX6gdIVzcXSxbnXhcEBu\XOxdHjlcIlidCClZXzsdy=> M{XFO|I3ODR3N{iw
A549 M2fZfmZ2dmO2aX;uJIF{e2G7 MX\+OVAh|ryP NHPFW5lFVVOR MlPUZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> NVLSblV7OjZ5MUG3OFg>
RAW264.7 MmLBSpVv[3Srb36gZZN{[Xl? MWX+N|Ah|ryP NVPOZXV{TE2VTx?= Moq5doVlfWOnczDwdo8ucW6obHHtcYF1d3K7IHflcoUh\XiycnXzd4lwdg>? MXmyOlcyQDV6Nh?=
MEMM MV3LbY5ie2ViYYPzZZk> Ml7CNVUhyrWP M17XOWROW09? MVXk[YNz\WG|ZYOgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SCKMx?= MX6yOlkzOTVyNh?=
MEMM M3vuWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWX+NlAhyrWP NUmxbnhYTE2VTx?= NHXi[G1qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NF;XXpAzPjl{MUWwOi=>
MEMM NX71bo1iSXCxcITvd4l{KGG|c3H5 NXnJN5h6OTViwsXN NUPxWJRbTE2VTx?= NFzUUXJqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ M4i3OVI3QTJzNUC2
T47D NV;TcpZ6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUixNEDPxE1? M3LxWGROW09? MWnJR|UxRTd{IH7N Mo\RNVg{QDF2NES=
ZR-75-1 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWWxNEDPxE1? M4HBfmROW09? NEC0e41KSzVyPUe5JI5O NHrhNIIyQDN6MUS0OC=>
BT474 NEnQOIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M332c|ExKM7:TR?= M1W0S2ROW09? NWnlfHAyUUN3ME24OkBvVQ>? MVKxPFM5OTR2NB?=
HCC1954 M4PpS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4f6cVExKM7:TR?= NU\D[VIzTE2VTx?= MYHJR|UxRTFzOTDuUS=> MlPVNVg{QDF2NES=
MDA-MB-453 NFe4T3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFm0e2syOCEQvF2= MlfqSG1UVw>? NV\XUXNnUUN3ME25O|Uhdk1? MnTZNVg{QDF2NES=
MDA-MB-468 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4O3NVExKM7:TR?= NVLqfJFzTE2VTx?= MX\JR|UxRTN{MEigcm0> NYDVfG1OOTh|OEG0OFQ>
SkBr3 NWfNNnNsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnLONVAh|ryP MkjESG1UVw>? M2TiWGlEPTB-MUCsNFAxKG6P MmjSNVg{QDF2NES=
MDA-MB-231 Mmm4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1vp[lExKM7:TR?= M2H6cWROW09? MVPJR|UxRjFyLECwNEBvVQ>? MUGxPFM5OTR2NB?=
HCT116 NX[4SW8zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3m3S|ExKM7:TR?= MUjEUXNQ NHf6VZlKSzVyPUW4N|Yhdk1? MnHFNVg{QDF2NES=
HT29 NFrZWoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWixNEDPxE1? MWTEUXNQ MV;JR|UxRjFyLECwNEBvVQ>? NYPqWlBROTh|OEG0OFQ>
HFF NUTEUoFGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NY\JXmE{OTBizszN MkXOSG1UVw>? NIXo[ZlKSzVyPUe2NVUhdk1? M3HBVlE5OzhzNES0
HN5 NU\tdmNtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfSNVAh|ryP MkXmSG1UVw>? MYTJR|UxRjFyLECwNEBvVQ>? MWWxPFM5OTR2NB?=
786-0 MlPnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV6xNEDPxE1? MmjNSG1UVw>? NIixWY1KSzVyPUSwNFkhdk1? NWPLVYVNOTh|OEG0OFQ>
H157 NVzLfG1iT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHH2XWMyOCEQvF2= NFW3eHNFVVOR M{TwfGlEPTB;Mk[0NkBvVQ>? M1Tx[lE5OzhzNES0
NCI-H460 NF[5cY9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFTXZ2gyOCEQvF2= NWfIXnRbTE2VTx?= MnnRTWM2OD5{LEWwNEBvVQ>? MkjQNVg{QDF2NES=
SKOV-3 NUiy[2pwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWWxNEDPxE1? NV7KWmZ[TE2VTx?= MU\JR|UxRTJzMk[gcm0> MlLRNVg{QDF2NES=
OVCAR-3 NVHXenUxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX:xNEDPxE1? NGO2UmpFVVOR NX;jeotwUUN3ME2yPVE5KG6P NX7tdmZ2OTh|OEG0OFQ>
BXPC3 MorOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYGxNEDPxE1? NVHWdG1kTE2VTx?= M4jDcmlEPTB;M{G0NUBvVQ>? NYDCWmdpOTh|OEG0OFQ>
MiaPaCa MoexS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVfCN4x[OTBizszN MXnEUXNQ MlLhTWM2OD13NEOzJI5O MofCNVg{QDF2NES=
PANC-1 MnfPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml7SNVAh|ryP NYXLRmFvTE2VTx?= MVvJR|UxRTh4OEGgcm0> NXfoPFRvOTh|OEG0OFQ>
LNCaP NWTTO3JyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGjjcXcyOCEQvF2= NVnXSIpiTE2VTx?= NYLsNpZ3UUN3ME2xOFchdk1? MVSxPFM5OTR2NB?=
DU145 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWrCfGxbOTBizszN M1HFbWROW09? NEjKWIxKSzVyPUO4NVIhdk1? M2f4V|E5OzhzNES0
PC3 NFjjTJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX6xNEDPxE1? NG\POYdFVVOR MkOzTWM2OD5zMDywNFAhdk1? NX\vWFN6OTh|OEG0OFQ>
BT474 NGDJ[ZBMcW6jc3WgZZN{[Xl? MmWyNVAh|ryP NGPxWplFVVOR MoLibY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTZyIH7N NH6xWm4yQDN6MUS0OC=>
786-0 MUTLbY5ie2ViYYPzZZk> NWfIPJRyOTBizszN M3XoOmROW09? NIjvPVlqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNUCgcm0> NWDa[HZjOTh|OEG0OFQ>
LNCaP NWn2[VJJU2mwYYPlJIF{e2G7 M3ToT|ExKM7:TR?= MoPBSG1UVw>? MVPpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1OyCwTR?= MXuxPFM5OTR2NB?=
PC3 M1jWfWtqdmG|ZTDhd5NigQ>? MXmxNEDPxE1? NX7idIJTTE2VTx?= NGLrOGJqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2OTDuUS=> MlzNNVg{QDF2NES=
KARPAS-231 MmXqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{LhdlExKM7:TR?= NIn4W29FVVOR NH3hOZhGSzVyPUSxJI5O M2[wNlE6ODZ2N{Ow
CCRFSB MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEjkXGQyOCEQvF2= M4ryd2ROW09? NGGwXWVGSzVyPUG1OUBvVQ>? NHzEOY8yQTB4NEezNC=>
SUP B15 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXe0O3ptOTBizszN M2P0OWROW09? M13v[mVEPTB;MUm3JI5O NVGwO4lvOTlyNkS3N|A>
SD-1 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3rpXVExKM7:TR?= MnLFSG1UVw>? NETBOJVGSzVyPUOyNEBvVQ>? MVixPVA3PDd|MB?=
RS4;11 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkS1NVAh|ryP NF7seoVFVVOR MVnFR|UxRTZ3NDDuUS=> NHvPN2syQTB4NEezNC=>
MN-60 NV:5dWV6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2\n[|ExKM7:TR?= M3Hnb2ROW09? MUPFR|UxRTN4MEKgcm0> NVrFOHA3OTlyNkS3N|A>
Tanoue M4W0c2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVfXWnRUOTBizszN MljpSG1UVw>? NYP3V|JDTUN3ME20OVE4KG6P NX\CS|ZVOTlyNkS3N|A>
RCH-ACV NFTuNHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4\nTFExKM7:TR?= MkHoSG1UVw>? MXzFR|UxRTF3MjDuUS=> MU[xPVA3PDd|MB?=
SEM NUj3UFRTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVvMUHo3OTBizszN M4PpU2ROW09? NXfyUmhOTUN3ME2yNFIhdk1? NV3FZ2tXOTlyNkS3N|A>
KASUMI-2 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWixNEDPxE1? M4rLS2ROW09? MWPFR|UxRTJ{NTDuUS=> NGHVRpYyQTB4NEezNC=>
REH NVPsT2FvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVexNEDPxE1? NF;GT|BFVVOR NX[1VHBqTUN3ME2yPFghdk1? Mmi0NVkxPjR5M{C=
697 MkC1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M37nO|ExKM7:TR?= M2TXWGROW09? MYDFR|UxRTN|ODDuUS=> NEmzSnQyQTB4NEezNC=>
NALM-6 M{PEWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3jKclExKM7:TR?= NGruWlZFVVOR MoL3SWM2OD12MkGgcm0> NWjKR5JxOTlyNkS3N|A>
MHH-CALL–3 NEfkO3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mm[1NVAh|ryP NGHhOYhFVVOR NEjBemZGSzVyPUixNkBvVQ>? MnPINVkxPjR5M{C=
MHH-CALL–2 NYHUPItxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXK5WJRbOTBizszN NV\FcVh5TE2VTx?= NEf3NHBGSzVyPUKxNVQhdk1? NWjiRmUzOTlyNkS3N|A>
J.GAMMA-1 MljOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoTRNVAh|ryP NEHXc29FVVOR MnTvSWM2OD14NTDuUS=> M{LZVFE6ODZ2N{Ow
JR45.01 MmW5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkTYNVAh|ryP NYfxbIhlTE2VTx?= NGqzR4FGSzVyPU[4JI5O M3O3VFE6ODZ2N{Ow
A3 NX3MdWFYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHO2Z4UyOCEQvF2= Ml\RSG1UVw>? MYXFR|UxRTZ7IH7N M3TFNFE6ODZ2N{Ow
I 2.1 M3r5[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2PKclExKM7:TR?= MXvEUXNQ MkTNSWM2OD15MzDuUS=> MYexPVA3PDd|MB?=
MOLT-3 M33HOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHjITnkyOCEQvF2= NWO4UXFCTE2VTx?= MmfhSWM2OD15NDDuUS=> Mli4NVkxPjR5M{C=
P116 M3vDTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV\tT5B4OTBizszN NFPiWXNFVVOR NWD3NmQ5TUN3ME23PEBvVQ>? MWWxPVA3PDd|MB?=
J.Cam1.6 MnfGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUixNEDPxE1? M2PEUWROW09? NVPpUHJnTUN3ME23PUBvVQ>? M13sUVE6ODZ2N{Ow
I 9.2 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGXn[JcyOCEQvF2= NIi0Wm1FVVOR MXXFR|UxRThyIH7N M{OyUVE6ODZ2N{Ow
LOUCY MoXmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3fi[FExKM7:TR?= NHrPfm9FVVOR NUjzdXBLTUN3ME2xNVchdk1? MmTmNVkxPjR5M{C=
J.RT3-T3.5 Ml[5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXXNVAh|ryP MYnEUXNQ MWHFR|UxRTF{MzDuUS=> NFm1ZnQyQTB4NEezNC=>
800000 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXH4XJp5OTBizszN MnO0SG1UVw>? NIi3UnVGSzVyPUG2N{BvVQ>? MYKxPVA3PDd|MB?=
Jurkat NF\FdZBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3PhdVExKM7:TR?= M122TmROW09? NF7kSpdGSzVyPUKyOUBvVQ>? MYqxPVA3PDd|MB?=
MOLT-4 NEP4[3dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFHzXpgyOCEQvF2= M{fXc2ROW09? MYHFR|UxRTJ|MjDuUS=> NYf5VGlqOTlyNkS3N|A>
Molt-16 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\UWlExKM7:TR?= MlHtSG1UVw>? MnHuSWM2OD1{NEGgcm0> M1qyZlE6ODZ2N{Ow
CEM/C3 M{LjRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYrZXmU{OTBizszN NXyzcmFKTE2VTx?= NInjd3hGSzVyPUK1O{BvVQ>? M1\GSlE6ODZ2N{Ow
CEM/C2 M2XoSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEflZnYyOCEQvF2= Ml62SG1UVw>? MnKxSWM2OD1{N{Ggcm0> MlzFNVkxPjR5M{C=
CCRFCEM MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFq2[|QyOCEQvF2= MYPEUXNQ NYniUnZHTUN3ME2zNlchdk1? MmTMNVkxPjR5M{C=
CEM/C1 NF7HOnNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1zVOFExKM7:TR?= MlS4SG1UVw>? NXrrW3dwTUN3ME2zPFIhdk1? MkjLNVkxPjR5M{C=
SUPTI[VB] MkS0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUjhS|JDOTBizszN NFfJWmVFVVOR NVzBOoZ6TUN3ME22NVkhdk1? NF7mT2oyQTB4NEezNC=>
CCRF–HSB-2 M3PIOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;ZclIyOTBizszN Mle2SG1UVw>? MkflSWM2OD1{MUG3JI5O MXWxPVA3PDd|MB?=
I 2.1 NXP6SHd2SXCxcITvd4l{KGG|c3H5 NFHOOWQyOCEQvF2= M{noVmROW09? M2K0colv\HWlZYOgZZBweHSxc3nz NIHSN5IyQTB4NEezNC=>
I 9.2 M4nlXmFxd3C2b4Ppd{Bie3OjeR?= M{fiTlExKM7:TR?= NHHSRm5FVVOR MlLQbY5lfWOnczDhdI9xfG:|aYO= MmHINVkxPjR5M{C=
A3 MYHBdI9xfG:|aYOgZZN{[Xl? NXrYfGcyOTBizszN MYXEUXNQ NE\1[ZZqdmS3Y3XzJIFxd3C2b4Ppdy=> NGjKeG8yQTB4NEezNC=>
RD MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYmxNEDPxE1? NVj6T|k6UUN3ME6xNEDPxE1? NYDxRVkyOjB5NEC2NlM>
Rh41 NFO5cWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXWxNEDPxE1? MV\JR|UxRTN|Lkigcm0> MXSyNFc1ODZ{Mx?=
Rh18 NHzWXWdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlzhNVAh|ryP NFmxOWdKSzVyPUOwN{BvVQ>? NUfTc4ZmOjB5NEC2NlM>
Rh30 NFrl[WJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2XWUFExKM7:TR?= NX\PZVJyUUN3ME20MlgyKM7:TR?= M3Hr[VIxPzRyNkKz
BT-12 MoDJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mk[2NVAh|ryP MYTJR|UxRjFyIN88US=> NGHzVmszODd2ME[yNy=>
CHLA-266 NGe0bZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFP4NVgyOCEQvF2= NHLmWVdKSzVyPUGuNlIh|ryP NILRflIzODd2ME[yNy=>
TC-71 NXnUNoJOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2X5NFExKM7:TR?= NFvUR2JKSzVyPUKuOVIh|ryP M{\EeVIxPzRyNkKz
CHLA-9 M4XjdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml7jNVAh|ryP MVTJR|UxRTV7MTDuUS=> MkKzNlA4PDB4MkO=
CHLA-10 M4LkWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV;wW2dyOTBizszN NHHjdZNKSzVyPUGwNkBvVQ>? MYCyNFc1ODZ{Mx?=
CHLA-258 MlXGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHP0UJQyOCEQvF2= M2riV2lEPTB;MT6wOUDPxE1? MVSyNFc1ODZ{Mx?=
GBM2 NYjubmprT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFrPXVUyOCEQvF2= M1TTWmlEPTB;OT6xOUDPxE1? NW[yUYp5OjB5NEC2NlM>
NB-1643 NXvrZYRRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{jaV|ExKM7:TR?= MXHJR|UxRTVwNDFOwG0> NIDmRZczODd2ME[yNy=>
NB-Ebc1 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYTGfoV4OTBizszN NWj1cVN2UUN3ME6xNEDPxE1? MoLoNlA4PDB4MkO=
CHLA-90 M2j3emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVLFXnYyOTBizszN NWPFVmNRUUN3ME6xNEDPxE1? NFrkVWozODd2ME[yNy=>
CHLA-136 MonGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M37nRVExKM7:TR?= MlT5TWM2OD5zMDFOwG0> M{[xcFIxPzRyNkKz
NALM-6 NH[yZ2NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2XFV|ExKM7:TR?= MYDJR|UxRTJ4NTDuUS=> MnnVNlA4PDB4MkO=
COG-LL-317 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXyxNEDPxE1? NX3Jbnp1UUN3ME22MlQ6KG6P M4KxcVIxPzRyNkKz
RS4;11 M4XFUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NULBZ3h{OTBizszN MYLJR|UxRTF2NzDuUS=> MorXNlA4PDB4MkO=
MOLT-4 MomxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFfq[2IyOCEQvF2= NWnqc2VjUUN3ME20NEBvVQ>? M2PyblIxPzRyNkKz
CCRF-CEM MlrkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml7lNVAh|ryP M3nXV2lEPTB;Mk[4JI5O M2HUelIxPzRyNkKz
Kasumi-1 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mor3NVAh|ryP NH7lSphKSzVyPUGwO{BvVQ>? MWqyNFc1ODZ{Mx?=
Karpas-299 NYDHO41NT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUKxNEDPxE1? MULJR|UxRTJwOUOg{txO Ml;1NlA4PDB4MkO=
Ramos-RA1 NGnqOHNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFvSb4EyOCEQvF2= NFrrT|hKSzVyPUeuN|Uh|ryP Mne2NlA4PDB4MkO=
H1299 NVK0TFc4U2mwYYPlJIF{e2G7 NIHNSlAyOCEQvF2= NWfDXYxCcW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? NV7mTphHOjF7MEi2NVY>

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

Protocol

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

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

Solubility (25°C)

In vitro DMSO 73 mg/mL (197.6 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

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

Chemical Information

Molecular Weight 369.42
Formula

C23H19N3O2

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

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Clinical Trial Information

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID