Tivantinib (ARQ 197)

Tivantinib (ARQ 197)は初めの非ATP競争性的なc-Met阻害剤で、無細胞実験でKi値が0.355 μMです。Tivantinib (ARQ 197)はRonに作用する活性が殆どなくて、EGFR、InsR、PDGFRαとFGFR1/4を抑制する作用がありません。臨床3期。

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Tivantinib (ARQ 197) 化学構造
分子量: 369.42

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製品説明

  • Compare c-Met Inhibitors
    c-Met製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 Tivantinib (ARQ 197)は初めの非ATP競争性的なc-Met阻害剤で、無細胞実験でKi値が0.355 μMです。Tivantinib (ARQ 197)はRonに作用する活性が殆どなくて、EGFR、InsR、PDGFRαとFGFR1/4を抑制する作用がありません。臨床3期。
ターゲット c-Met
IC50 0.355 μM (Ki) [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MNK-45 MYHLbY5ie2ViYYPzZZk> NEXi[Jp,OTBizszN M{\GPIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= M2\V[FIxPDh2MEG4
HT29 Mo\ET4lv[XOnIHHzd4F6 MYT+NVAh|ryP NVnWSYNzcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MYKyNFQ5PDBzOB?=
MDA-MB-231 NY\D[VFKU2mwYYPlJIF{e2G7 MmrQglExKM7:TR?= NICwXJpqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NHW4UGUzODR6NECxPC=>
NCI-H441 MnHyT4lv[XOnIHHzd4F6 MVL+NVAh|ryP MnuwbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NYq4S2FoOjB2OESwNVg>
SK-MEL-28 Mmj0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU[zN{DPxE1? NFfFfJJKSzVyPkOzJO69VQ>? NHP0NmMzODR6NECxPC=>
NCI-H661 NWGxOIE5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlTrN|Mh|ryP NYfwSWFoUUN3ME6zN{DPxE1? NETWdHMzODR6NECxPC=>
NCI-H446 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV:zN{DPxE1? M4SxZmlEPTB;NzFOwG0> M2\XWlIxPDh2MEG4
MDA-MB-231 M4jHTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUf3XmRVOzNizszN NVTyOZNQUUN3ME2wMlU2KM7:TR?= M4jjU|IxPDh2MEG4
DLD-1 NXrvfpZvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlO4N|Mh|ryP MnTtTWM2OD1yLkWzJO69VQ>? Mn[yNlA1QDRyMUi=
A549 M4LoSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFHJRpE{OyEQvF2= NGXGUIdKSzVyPUCuOVkh|ryP MkLrNlA1QDRyMUi=
SK-OV-3 NGGxS5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFP3[nI{OyEQvF2= M1u0eGlEPTB;MD62OkDPxE1? NH\ZcJIzODR6NECxPC=>
NCI-H460 Ml7IS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVLYZZZPOzNizszN MX3JR|UxRTBwNjFOwG0> NU\KSGZmOjB2OESwNVg>
A375 MmjwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXf4PXZHOzNizszN M13PbGlEPTB;MD60NkDPxE1? M{DJ[VIxPDh2MEG4
NCI-H441 M1i3NGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXeyZpk5OzNizszN NV;ybWtUUUN3ME2wMlMh|ryP M1PvSFIxPDh2MEG4
HT29 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXL4eGQ3OzNizszN MmPKTWM2OD1yLkS5JO69VQ>? MkTCNlA1QDRyMUi=
MKN-45 NFvKVIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M37odlM{KM7:TR?= NX70TIZ3UUN3ME2wMlU5KM7:TR?= MU[yNFQ5PDBzOB?=
HT29 MUHBdI9xfG:|aYOgZZN{[Xl? NUnYW3dMhjFyIN88US=> NVzMPVJEe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NVnTVXQ5OjB2OESwNVg>
MKN-45 NEXi[phCeG:ydH;zbZMh[XO|YYm= M1P0c54yOCEQvF2= NYHz[o4ye2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu Mk\YNlA1QDRyMUi=
MDA-MB-231 NFHwWJpCeG:ydH;zbZMh[XO|YYm= NE[0S3p,OTBizszN NW[xc4htdW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> MVWyNFQ5PDBzOB?=
MDA-MB-231/TGL NV62OoZNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NW[wRogzhjFyMDFOwG0> MULHTVUxRTFwMjFOwG0> MXWyNlAzPzZ7MB?=
1833/TGL NIr6SnNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFnXNVB,OTByIN88US=> Ml\TS2k2OD1|Lkeg{txO NIXDXGIzOjB{N{[5NC=>
EBC1 MXrDfZRwfG:6aXRCpIF{e2G7 NH7SNXp,OTBizszN M4P1OIlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NEDkSoozOzV7OEK3Oi=>
SNU638 NIDOb5hEgXSxdH;4bYPDqGG|c3H5 NITH[W5,OTBizszN NHW1emxqdmirYnn0d{B1cGViY3XscEBoem:5dHiu M2DDblI{PTl6Mke2
A549 MWHDfZRwfG:6aXRCpIF{e2G7 M1fmWp4yOCEQvF2= NE\wSHhvd3RiYX\m[YN1 MUmyN|U6QDJ5Nh?=
H460 M{Ozd2N6fG:2b4jpZ:Kh[XO|YYm= MlnSglExKM7:TR?= MnvJco91KGGoZnXjeC=> MYCyN|U6QDJ5Nh?=
HCC827 MUfDfZRwfG:6aXRCpIF{e2G7 MYP+NVAh|ryP NXvJN21Hdm:2IHHm[oVkfA>? MWmyN|U6QDJ5Nh?=
A549 NVSzZWI{TnWwY4Tpc44h[XO|YYm= NWPaVlV{OTBizszN NFXXc4tlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? MU[yN|U6QDJ5Nh?=
EBC1 MYnGeY5kfGmxbjDhd5NigQ>? MonxNVAh|ryP NUDUcnhx\Gm|coXweJMhdWmlcn;0eYJ2dGV? MW[yN|U6QDJ5Nh?=
H460 MljkSpVv[3Srb36gZZN{[Xl? MUGxNEDPxE1? NHvjXYRqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w NES0NmozPTNzM{CxNC=>
K562/VCR MXvDfZRwfG:6aXRCpIF{e2G7 NYfwN457hjFyIN88US=> NWnsWo1ve2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NVPpb2s1OjV|MUOwNVA>
CEM/VBL M1PsfmN6fG:2b4jpZ:Kh[XO|YYm= MmrUglExKM7:TR?= NVnUOFI1e2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 NIr6U4ozPTNzM{CxNC=>
U266 Mo\rR5l1d3SxeHnjxsBie3OjeR?= NG\XRoV,OyEQvF5CpC=> NWjTeJRDUUN3ME2xMlEh|ryP NGLlVnIzPThzMECxNy=>
OPM-2 NWnjeYd1S3m2b4TvfIlkyqCjc4PhfS=> NWKwTHFKhjNizszNxsA> NGG4eGlKSzVyPUGuPEDPxE1? NXT5UYZIOjV6MUCwNVM>
MM.1S MnK3R5l1d3SxeHnjxsBie3OjeR?= MnLzglMh|ryPwrC= MmnsTWM2OD1zLk[g{txO MXOyOVgyODBzMx?=
MM.1R MkHhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH7I[VA{KM7:TdMg NUPVWpFxcW6qaXLpeJMh[2WubDDndo94fGhiYomgOFkm NHPpSlQzPThzMECxNy=>
RPMI-8226 NIjmZZREgXSxdH;4bYPDqGG|c3H5 NWizVmVohjNizszNxsA> M1TmS2lEPTB;MD65JO69VQ>? MXKyOVgyODBzMx?=
ANBL-6 MnvDR5l1d3SxeHnjxsBie3OjeR?= MYexJO69VcLi NVvibWNkcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NWDZdYFmOjV6MUCwNVM>
ANLB-6/V10R NE\tNpFEgXSxdH;4bYPDqGG|c3H5 MWixJO69VcLi MlX5bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MoHlNlU5OTByMUO=
KAS-6/1 Mo\UR5l1d3SxeHnjxsBie3OjeR?= MlfTNUDPxE4EoB?= MmLMbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= NGTaR40zPThzMECxNy=>
KAS-6/V10R MXfDfZRwfG:6aXRCpIF{e2G7 M2W3flEh|ryPwrC= NV3SOGVDcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MYqyOVgyODBzMx?=
KAS-6/R10R M4fqPWN6fG:2b4jpZ:Kh[XO|YYm= M{PG[lEh|ryPwrC= MlrjbY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MXKyOVgyODBzMx?=
8226/S NF\4bZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MY[zJO69VcLi NUXJXW1GcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm M4q1PFI2QDFyMEGz
8226/LR-5 M2Hx[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWHDOoVOOyEQvF5CpC=> M3nXXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> M1T6elI2QDFyMEGz
Huh7 NXf6NW1JS3m2b4TvfIlkyqCjc4PhfS=> NUG5TopVhjRwODFOwG3DqA>? NGm5So1FVVOR MkXvTWM2OD17Lkmgcm0> NGDlc2QzPjJ3OUK1NC=>
Hep3B MkLiR5l1d3SxeHnjxsBie3OjeR?= NXLQeGV6hjRwODFOwG3DqA>? MkHpSG1UVw>? MoTjTWM2OD12NEiuO{BvVQ>? MojVNlYzPTl{NUC=
HepG2 Ml;5R5l1d3SxeHnjxsBie3OjeR?= MVv+OE45KM7:TdMg Mm[ySG1UVw>? MWDJR|UxRTF|OT63O{BvVQ>? NEPj[5ozPjJ3OUK1NC=>
Chang NXjpZ3FrS3m2b4TvfIlkyqCjc4PhfS=> NIniU4F,PC56IN88UeKh NVzzenhsTE2VTx?= Mmm4TWM2OD12NEiuO{BvVQ>? M4LXWVI3OjV7MkWw
Huh7 NV75dGJjTnWwY4Tpc44h[XO|YYm= MknPNU43KM7:TdMg NHKzUFhFVVOR MX;jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M4ToW|I3OjV7MkWw
Hep3B NIrpco9HfW6ldHnvckBie3OjeR?= MnPQNU43KM7:TdMg NECwcINFVVOR NEH3XFFk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M2rBRlI3OjV7MkWw
HepG2 M4XyZ2Z2dmO2aX;uJIF{e2G7 Ml7XNU43KM7:TdMg Ml72SG1UVw>? NEP1eolk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NITY[|kzPjJ3OUK1NC=>
Chang MnfxSpVv[3Srb36gZZN{[Xl? NEPR[W4yNjZizszNxsA> Mlr3SG1UVw>? NGnoSoxk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NGLVcXozPjJ3OUK1NC=>
MHCC97L NGHmXohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2L5SJ4yOCEQvF2= MVfEUXNQ NHT4e5VKSzVyPUOxOUBvVQ>? NGfkbIkzPjR3OEm1Ny=>
MHCC97H NHHKUGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1HU[Z4yOCEQvF2= NXu1fGFvTE2VTx?= NHP1TJdKSzVyPUO2PQKBkSCwTR?= MVKyOlQ2QDl3Mx?=
Huh7 NYfWT3loT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zz[54yOCEQvF2= NXPLTFVVTE2VTx?= NVS5WZpOUUN3ME2yOlUhdk1? NXnXcmZnOjZ2NUi5OVM>
HepG2 M4Prbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmX1glExKM7:TR?= MYfEUXNQ NVL3TGdpUUN3ME2zPVIhdk1? MmrHNlY1PTh7NUO=
MHCC97L M2XscWZ2dmO2aX;uJIF{e2G7 NYjxSFFZOSEQvF5CpC=> MlPhSG1UVw>? NIm4WYtqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v NH;IVGczPjR3OEm1Ny=>
Huh7 NGDhdFhHfW6ldHnvckBie3OjeR?= MWmxJO69VcLi MVjEUXNQ NGXjXpBqdmS3Y3XzJI1q[3KxdIXieYxmeyCmZYDvcJlu\XKrenH0bY9v M4HudVI3PDV6OUWz
MHCC97L M17RW2Fxd3C2b4Ppd{Bie3OjeR?= M4XO[lEh|ryPwrC= MXPEUXNQ MVfpcoR2[2W|IHHwc5B1d3Orcx?= MUWyOlQ2QDl3Mx?=
Huh7 NFXKRVBCeG:ydH;zbZMh[XO|YYm= M1nkTVEh|ryPwrC= NIPMVHlFVVOR MnvxbY5lfWOnczDhdI9xfG:|aYO= MkXHNlY1PTh7NUO=
C3H 10T1/2 mouse fibroblasts NVTiS2NqU2mwYYPlJIF{e2G7 MUmyOUDPxE1? NGDUXZFFVVOR M2qxZZJm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> Ml3GNlA2OzR|NEW=
H23 NEDzVIhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIrEd4YzPSEQvF2= M{fRV2ROW09? NVrPUG1He2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MXyyNFU{PDN2NR?=
WM35 NH[zdmxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWOwNlNZOTBizszN MYXEUXNQ NYjIT4s3e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MoXDNlA2OzR|NEW=
NIH 3T3 M2\XZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXexNEDPxE1? NInyenBFVVOR NVThZZh6\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NHLm[JgzODV|NEO0OS=>
H838 NV3UeXhmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHXWPJQyOCEQvF2= NHK3UJZFVVOR NGXhTplld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> M2\QeVIxPTN2M{S1
H1395 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLnN|AyOCEQvF2= MYDEUXNQ NXHte2Jb\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 MYWyNFU{PDN2NR?=
Quiescent S2 MUXLbY5ie2ViYYPzZZk> Mn:wN|Ah|ryP MmDYSG1UVw>? M3u0RYNwdXCuZYTlcJkh[WK{b3fheIV{KFSVQT3pcoR2[2WmIHj5dIVz[WOndInsZZRqd25ib3[gTFNMPG2nMzDobZN1d26ncx?= Ml7zNlE2OTh7MUW=
PC3 Ml\nRZBweHSxc3nzJIF{e2G7 MXeyNEDPxE1? NFnHWGFFVVOR NWiwUI5JcW6mdXPld{BieG:ydH;zbZM> M1nESlIyPzB7MUOw
Du145 NI\nSHNCeG:ydH;zbZMh[XO|YYm= M2\6O|IxKM7:TR?= NXrnZ2hKTE2VTx?= NI\wNYhqdmS3Y3XzJIFxd3C2b4Ppdy=> MkjXNlE4ODlzM{C=
LNCaP MVzBdI9xfG:|aYOgZZN{[Xl? MVuyNEDPxE1? NHLscpJFVVOR MYjpcoR2[2W|IHHwc5B1d3Orcx?= MUKyNVcxQTF|MB?=
LAPC-4 M1z5UWFxd3C2b4Ppd{Bie3OjeR?= NF\zS4IzOCEQvF2= MkXRSG1UVw>? MnLFbY5lfWOnczDhdI9xfG:|aYO= M1X2dlIyPzB7MUOw
LNCaP MWfGeY5kfGmxbjDhd5NigQ>? MnLwNlAh|ryP M2La[2ROW09? MoPk[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NGDXd2QzOTdyOUGzNC=>
LAPC-4 M1[2dmZ2dmO2aX;uJIF{e2G7 MmrzNlAh|ryP MofUSG1UVw>? Mke5[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NWPCPFdQOjF5MEmxN|A>
Kasumi-1 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYLoUlFOhjVyIN88US=> M4XDSmROW09? Mk\xbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MVqyN|M6ODV|Nh?=
SKNO-1 M3PlUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUXvSolvhjVyIN88US=> MknDSG1UVw>? MXfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MXGyN|M6ODV|Nh?=
Kasumi-1 M{XF[GtqdmG|ZTDhd5NigQ>? NU\NfXZ4hjFyIN88US=> NVjFfpZZTE2VTx?= Mo\LdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NIf1WlMzOzN7MEWzOi=>
SKNO-1 M4r4SGtqdmG|ZTDhd5NigQ>? NGD6XYp,OTBizszN NWDTS3VzTE2VTx?= M{K2XJJm\HWlZYOg[ZhxemW|c3nvckBw\iCjY3X0fYxifGWmIHjpd5RwdmViSEOsxsBkNWurdNMgZY5lyqCkY3ytNi=> M4m2PFI{OzlyNUO2
A549 NIfGN3FHfW6ldHnvckBie3OjeR?= NEj5TVAyOCEQvF2= Mn21SG1UVw>? M3vqeYVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> M{X4eFI1PzR4NUe0
NRK-52E Mk[1SpVv[3Srb36gZZN{[Xl? NH;PZ|QyOCEQvF2= NVjJNpZlTE2VTx?= MoLwbY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiU2TBWFMhdnWlbHXhdkB1emGwc3zvZ4F1cW:wIHHu[EB1cGViZYjwdoV{e2mxbjDv[kBVT0ZvzsKxMEBkd2yuYXflckBKXiCjbnSg[oljem:wZXP0bY4> MY[yOVA5QDByMh?=
PC12 M3S0R2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYH+NVIvPSEQvF2= M121cGROW09? M{TxUJBz\X[nboTzJHRUSS2rbnT1Z4VlKG6ndYLpeIUh\m:{bXH0bY9v M170V|I2OTJ6M{i2
HPMCs NIDEbFBHfW6ldHnvckBie3OjeR?= NX3Cc4tzemW4ZYLz[ZMh\XCrdHjlcIlidCC2bzDt[ZNmdmOqeX3hcEB1emGwc3n0bY9vKG:oIHj1cYFvKHCncnn0c45m[WxibXXzc5Rp\WyrYXygZ4VtdHN? MV:yOlA1PTd6MB?=
A549 NE[3VpNHfW6ldHnvckBie3OjeR?= M4fydp42OCEQvF2= NWSzSVNoTE2VTx?= MknOZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> MVmyOlcyOTd2OB?=
RAW264.7 NH;p[G9HfW6ldHnvckBie3OjeR?= MljjglMxKM7:TR?= NGfqeVNFVVOR NXHKR29vemWmdXPld{Bxem9vaX7mcIFudWG2b4L5JIdmdmViZYjwdoV{e2mxbh?= NELtNoQzPjdzOEW4Oi=>
MEMM MmjrT4lv[XOnIHHzd4F6 NWLNXVlMOTViwsXN NXTIT3lSTE2VTx?= NIHyeoJl\WO{ZXHz[ZMh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINy=> NXzRNpd2OjZ7MkG1NFY>
MEMM MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVX0dnZvhjJyINM1US=> MmHFSG1UVw>? MYfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MWqyOlkzOTVyNh?=
MEMM NXrvUI5oSXCxcITvd4l{KGG|c3H5 MXOxOUDDvU1? NHXCZWxFVVOR NGe1eFFqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ NITJUJQzPjl{MUWwOi=>
T47D M4nCT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{ixW|ExKM7:TR?= MXPEUXNQ NV65co9oUUN3ME23NkBvVQ>? M4PzdlE5OzhzNES0
ZR-75-1 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGjBUZoyOCEQvF2= M3HyZmROW09? M3;KUGlEPTB;N{mgcm0> NEPUOZEyQDN6MUS0OC=>
BT474 MlL5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVPIOGJ6OTBizszN MnrwSG1UVw>? M3Xi[mlEPTB;OE[gcm0> NF7welYyQDN6MUS0OC=>
HCC1954 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{T4UVExKM7:TR?= NYDJbYlTTE2VTx?= MnnrTWM2OD1zMUmgcm0> MVuxPFM5OTR2NB?=
MDA-MB-453 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWmxNEDPxE1? MkjrSG1UVw>? NWHhT5JGUUN3ME25O|Uhdk1? NFu0O2QyQDN6MUS0OC=>
MDA-MB-468 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3jOR|ExKM7:TR?= NIDpNYtFVVOR MUDJR|UxRTN{MEigcm0> MVOxPFM5OTR2NB?=
SkBr3 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkTvNVAh|ryP Ml;LSG1UVw>? NWfVOXpSUUN3ME6xNEwxODBibl2= NFHpbpAyQDN6MUS0OC=>
MDA-MB-231 NF;TfY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{\1T|ExKM7:TR?= MVzEUXNQ M3fOTmlEPTB-MUCsNFAxKG6P M1rkcFE5OzhzNES0
HCT116 NFH5ZlNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXXKcY9XOTBizszN M{n5V2ROW09? MUnJR|UxRTV6M{[gcm0> M4jCcVE5OzhzNES0
HT29 M3vwVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIHLVIoyOCEQvF2= NVHL[FdSTE2VTx?= NHf4dIpKSzVyPkGwMFAxOCCwTR?= NFrtfoUyQDN6MUS0OC=>
HFF MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MW[xNEDPxE1? MX;EUXNQ NWPvfoNYUUN3ME23OlE2KG6P MYixPFM5OTR2NB?=
HN5 NFjYeHhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2H3TFExKM7:TR?= M4jxSWROW09? MWXJR|UxRjFyLECwNEBvVQ>? NYPCblY1OTh|OEG0OFQ>
786-0 MmqxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1rLfFExKM7:TR?= MnTOSG1UVw>? M3vqd2lEPTB;NECwPUBvVQ>? MWCxPFM5OTR2NB?=
H157 NH3MeIhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2H4ZlExKM7:TR?= M3rxbmROW09? MWjJR|UxRTJ4NEKgcm0> NGS0R4wyQDN6MUS0OC=>
NCI-H460 M2raeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn62NVAh|ryP MlfYSG1UVw>? MXLJR|UxRjJuNUCwJI5O M{KxblE5OzhzNES0
SKOV-3 NUfpd|RRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUnnVGNzOTBizszN MXfEUXNQ NVO3SHFtUUN3ME2yNVI3KG6P MkLJNVg{QDF2NES=
OVCAR-3 NXvnSol2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGnrSmUyOCEQvF2= M4DiTmROW09? M2q5bGlEPTB;MkmxPEBvVQ>? M3HNdFE5OzhzNES0
BXPC3 NUPJT|VXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFriXlgyOCEQvF2= MmrDSG1UVw>? MYTJR|UxRTNzNEGgcm0> NVK4VHdFOTh|OEG0OFQ>
MiaPaCa MoPLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{S5eVExKM7:TR?= MVnEUXNQ NWTrNlE4UUN3ME21OFM{KG6P M2Lq[lE5OzhzNES0
PANC-1 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUnDdpBNOTBizszN MniwSG1UVw>? NHv4bZdKSzVyPUi2PFEhdk1? NYnudHBsOTh|OEG0OFQ>
LNCaP NVPTU|c{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG[xR4IyOCEQvF2= NU[2PIg3TE2VTx?= M{XSW2lEPTB;MUS3JI5O NIrzXlQyQDN6MUS0OC=>
DU145 NEe5NYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3P4PVExKM7:TR?= NVyxNoR7TE2VTx?= NX23NVRUUUN3ME2zPFEzKG6P NGXU[4YyQDN6MUS0OC=>
PC3 NWTsOII{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIjiUW4yOCEQvF2= NWCwVVBKTE2VTx?= MmH5TWM2OD5zMDywNFAhdk1? MUCxPFM5OTR2NB?=
BT474 M{HGS2tqdmG|ZTDhd5NigQ>? MXSxNEDPxE1? M4fKNGROW09? MXXpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kAyPjBibl2= NYLMOnhLOTh|OEG0OFQ>
786-0 NVPLOVRLU2mwYYPlJIF{e2G7 M4nXclExKM7:TR?= MWTEUXNQ NUe2TXlNcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMUWwJI5O NYrBbY5OOTh|OEG0OFQ>
LNCaP NVzse3dyU2mwYYPlJIF{e2G7 MnvtNVAh|ryP MmjHSG1UVw>? M2LtfolvcGmkaYTzJJBIW0t|zsKge4l1cCCLQ{WwJI9nKDR|IH7N MlW1NVg{QDF2NES=
PC3 M{fGTmtqdmG|ZTDhd5NigQ>? NH7FcnIyOCEQvF2= M3v6WWROW09? NEfyTYJqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2OTDuUS=> MW[xPFM5OTR2NB?=
KARPAS-231 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4O1e|ExKM7:TR?= NWLmcXZITE2VTx?= NFz0UI5GSzVyPUSxJI5O M4W5UlE6ODZ2N{Ow
CCRFSB MnPWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml3XNVAh|ryP M4G3XGROW09? NUTlOW9tTUN3ME2xOVUhdk1? NGjYcooyQTB4NEezNC=>
SUP B15 M2D4emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW[xNEDPxE1? MlrWSG1UVw>? NFXWVlZGSzVyPUG5O{BvVQ>? M1;lclE6ODZ2N{Ow
SD-1 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHjKbpAyOCEQvF2= MVPEUXNQ MULFR|UxRTN{MDDuUS=> NU[5fm9TOTlyNkS3N|A>
RS4;11 NUSzOlZzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYWxNEDPxE1? MkT3SG1UVw>? NUjQTnJQTUN3ME22OVQhdk1? MUSxPVA3PDd|MB?=
MN-60 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUP5[VFEOTBizszN MnTMSG1UVw>? NYD5RmxmTUN3ME2zOlAzKG6P NYG2TnJZOTlyNkS3N|A>
Tanoue MorkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWexNEDPxE1? NFTJ[5dFVVOR MUPFR|UxRTR3MUegcm0> MlroNVkxPjR5M{C=
RCH-ACV MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1vUbFExKM7:TR?= M{nRdGROW09? M1fpU2VEPTB;MUWyJI5O MlPDNVkxPjR5M{C=
SEM NEXHXI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUGxNEDPxE1? MV;EUXNQ MmX3SWM2OD1{MEKgcm0> MYOxPVA3PDd|MB?=
KASUMI-2 Mn\hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlnwNVAh|ryP MUnEUXNQ NYnhTI1NTUN3ME2yNlUhdk1? NVO3ZXBFOTlyNkS3N|A>
REH MmXBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEPnOmcyOCEQvF2= NEP0V5lFVVOR MUfFR|UxRTJ6ODDuUS=> NGTnenUyQTB4NEezNC=>
697 MkDIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHTxVYQyOCEQvF2= MVfEUXNQ M{fWRWVEPTB;M{O4JI5O MYWxPVA3PDd|MB?=
NALM-6 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXr2d4JPOTBizszN MVLEUXNQ MXzFR|UxRTR{MTDuUS=> NIrhbVEyQTB4NEezNC=>
MHH-CALL–3 M1vPcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2XMXlExKM7:TR?= NYXBToU{TE2VTx?= MoPkSWM2OD16MUKgcm0> MkHwNVkxPjR5M{C=
MHH-CALL–2 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWmxNEDPxE1? MnvoSG1UVw>? Mn;TSWM2OD1{MUG0JI5O MnHTNVkxPjR5M{C=
J.GAMMA-1 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXDNVAh|ryP MWPEUXNQ M4DJXmVEPTB;NkWgcm0> NFHE[ZAyQTB4NEezNC=>
JR45.01 M4Hvdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUWxNEDPxE1? NI\WbGhFVVOR M4XaXmVEPTB;Nkigcm0> NX76NHliOTlyNkS3N|A>
A3 M{H5V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\X[2kyOCEQvF2= MVnEUXNQ MUPFR|UxRTZ7IH7N MUOxPVA3PDd|MB?=
I 2.1 NF7pPGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXuxNEDPxE1? M{PqTGROW09? MmTzSWM2OD15MzDuUS=> MXSxPVA3PDd|MB?=
MOLT-3 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFLPbJUyOCEQvF2= M4j5fmROW09? NXLEW2R3TUN3ME23OEBvVQ>? NE\iNoEyQTB4NEezNC=>
P116 NXHSb4tiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3f1TFExKM7:TR?= NHfpZ2FFVVOR NGfoeWZGSzVyPUe4JI5O MYmxPVA3PDd|MB?=
J.Cam1.6 Mof5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjvelRROTBizszN MWHEUXNQ MYrFR|UxRTd7IH7N M3jZelE6ODZ2N{Ow
I 9.2 M3TpNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXWxNEDPxE1? M{PSSmROW09? NIP3cnJGSzVyPUiwJI5O MlX5NVkxPjR5M{C=
LOUCY MmPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUmxNEDPxE1? MYfEUXNQ MkDaSWM2OD1zMUegcm0> MVixPVA3PDd|MB?=
J.RT3-T3.5 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnHZNVAh|ryP MlH4SG1UVw>? M1i1fWVEPTB;MUKzJI5O MoXENVkxPjR5M{C=
800000 MkXCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NW\pcWhjOTBizszN NYqzbHdETE2VTx?= NUXzVo9tTUN3ME2xOlMhdk1? NXXEUHdvOTlyNkS3N|A>
Jurkat NVHZcXB[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3PZdlExKM7:TR?= NVjJPHVmTE2VTx?= NUnqTmtzTUN3ME2yNlUhdk1? MknLNVkxPjR5M{C=
MOLT-4 Mni3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX;zcHNjOTBizszN NGDnN|ZFVVOR MUjFR|UxRTJ|MjDuUS=> MUGxPVA3PDd|MB?=
Molt-16 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXKxNEDPxE1? NUi0T3BOTE2VTx?= MWjFR|UxRTJ2MTDuUS=> M3zFelE6ODZ2N{Ow
CEM/C3 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVX5UIVpOTBizszN MnrGSG1UVw>? NVnKd2RETUN3ME2yOVchdk1? MUmxPVA3PDd|MB?=
CEM/C2 NHjkVmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnnuNVAh|ryP NVmze|V[TE2VTx?= MmfHSWM2OD1{N{Ggcm0> NF7CeGUyQTB4NEezNC=>
CCRFCEM MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUOxNEDPxE1? NV\ad5FCTE2VTx?= M4n5O2VEPTB;M{K3JI5O NVzSO3pzOTlyNkS3N|A>
CEM/C1 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYr3OIpyOTBizszN M{LVfmROW09? NEXqXlFGSzVyPUO4NkBvVQ>? MoW4NVkxPjR5M{C=
SUPTI[VB] M{HUZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYKxNEDPxE1? NF;lOJpFVVOR M3PES2VEPTB;NkG5JI5O NF;Fd4IyQTB4NEezNC=>
CCRF–HSB-2 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2joUFExKM7:TR?= M{K4NmROW09? NV;aUWJ5TUN3ME2yNVE4KG6P NULw[YF2OTlyNkS3N|A>
I 2.1 Mo\HRZBweHSxc3nzJIF{e2G7 MXWxNEDPxE1? M2DpZ2ROW09? MXjpcoR2[2W|IHHwc5B1d3Orcx?= Ml7ENVkxPjR5M{C=
I 9.2 NX34c|RMSXCxcITvd4l{KGG|c3H5 MXexNEDPxE1? M{i4dGROW09? NUHDZmcxcW6mdXPld{BieG:ydH;zbZM> MYexPVA3PDd|MB?=
A3 Mor6RZBweHSxc3nzJIF{e2G7 MVKxNEDPxE1? NED1OlJFVVOR MW\pcoR2[2W|IHHwc5B1d3Orcx?= MmPJNVkxPjR5M{C=
RD MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHvW[GcyOCEQvF2= MmHBTWM2OD5zMDFOwG0> MY[yNFc1ODZ{Mx?=
Rh41 NYXjXZVWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1nVNVExKM7:TR?= NV7vWldoUUN3ME2zN{45KG6P MV2yNFc1ODZ{Mx?=
Rh18 NUDNOG5xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1T3elExKM7:TR?= M2nibGlEPTB;M{CzJI5O MXOyNFc1ODZ{Mx?=
Rh30 MmHDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmq5NVAh|ryP NXvmfIFLUUN3ME20MlgyKM7:TR?= MYmyNFc1ODZ{Mx?=
BT-12 M2DibGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXyxNEDPxE1? NUTKbGFxUUN3ME6xNEDPxE1? M3PxWFIxPzRyNkKz
CHLA-266 NF\FfVJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV;UR41bOTBizszN NX\VSWNNUUN3ME2xMlIzKM7:TR?= NWTJS4lYOjB5NEC2NlM>
TC-71 M4Trc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoPXNVAh|ryP MlPOTWM2OD1{LkWyJO69VQ>? M3fseVIxPzRyNkKz
CHLA-9 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUTqXGlPOTBizszN MXrJR|UxRTV7MTDuUS=> NIHXT2kzODd2ME[yNy=>
CHLA-10 NVLaelBwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn\iNVAh|ryP M{S3UmlEPTB;MUCyJI5O MmSyNlA4PDB4MkO=
CHLA-258 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M17ab|ExKM7:TR?= NEjxRVhKSzVyPUGuNFUh|ryP NXTVfFNpOjB5NEC2NlM>
GBM2 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV\nOXo3OTBizszN MWHJR|UxRTlwMUWg{txO MkO0NlA4PDB4MkO=
NB-1643 NEfqNI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3zvXlExKM7:TR?= M1PMXGlEPTB;NT60JO69VQ>? MnzmNlA4PDB4MkO=
NB-Ebc1 Mk\nS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn\NNVAh|ryP MYTJR|UxRjFyIN88US=> MX6yNFc1ODZ{Mx?=
CHLA-90 MnvwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW[xNEDPxE1? M12zVmlEPTB-MUCg{txO NFXKco0zODd2ME[yNy=>
CHLA-136 M1zJVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX6xNEDPxE1? MVrJR|UxRjFyIN88US=> NYHOUFZQOjB5NEC2NlM>
NALM-6 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUKxNEDPxE1? MmHjTWM2OD1{NkWgcm0> NGOx[WEzODd2ME[yNy=>
COG-LL-317 MnXvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFnKfIsyOCEQvF2= NHLub5VKSzVyPU[uOFkhdk1? M3HoS|IxPzRyNkKz
RS4;11 NHTHVVZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGnSOZEyOCEQvF2= M{DJRmlEPTB;MUS3JI5O NFHMSmMzODd2ME[yNy=>
MOLT-4 NFjxV4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnNdJNTOTBizszN NV7pOZpwUUN3ME20NEBvVQ>? M3TFOlIxPzRyNkKz
CCRF-CEM NXS0PG1wT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFnvU|gyOCEQvF2= MlLqTWM2OD1{Nkigcm0> NVnzU4NkOjB5NEC2NlM>
Kasumi-1 NVy2PYhCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYWxNEDPxE1? M3y3RmlEPTB;MUC3JI5O NVjrRWx7OjB5NEC2NlM>
Karpas-299 NWS0WJY6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkTXNVAh|ryP NGjrVmFKSzVyPUKuPVMh|ryP MkPiNlA4PDB4MkO=
Ramos-RA1 NWHXeVJVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHLtcIEyOCEQvF2= M2raRmlEPTB;Nz6zOUDPxE1? M1;oSVIxPzRyNkKz
H1299 MYjLbY5ie2ViYYPzZZk> NHHleYgyOCEQvF2= M2LTbYlvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> NEjlcoQzOTlyOE[xOi=>

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In vivo試験 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]
臨床試験 ARQ 197 plus erlotinib is currently in Phase III study in subjects with locally advanced or metastatic non-squamous, non-small cell lung cancer who have received 1 or 2 prior systemic anti-cancer therapies.
特集 The first selective c-Met inhibitor to be advanced into human clinical trials.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

細胞株 T29, MKN-45 and MDA-MB-231 cells
濃度 0.03-10 μM
反応時間 24, 32, and 48 hours
実験の流れ 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.

動物実験: [1]

動物モデル Female athymic nude mice bearing HT29, MKN-45, or MDA-MB-231 tumor xenografts
製剤 In polyethylene glycol 400/20% Vitamin E tocopheryl polyethylene glycol succinate (60:40) 30 mg/mL
投薬量 200 mg/kg
投与方法 Orally administered

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Tivantinib (ARQ 197) SDF
分子量 369.42
化学式

C23H19N3O2

CAS No. 905854-02-6
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (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.
化学名 (3R,4R)-3-(2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione

文献中の引用 (4)

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.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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