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 NIXXOHRMcW6jc3WgZZN{[Xl? NI\sdHh,OTBizszN MVXpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MYOyNFQ5PDBzOB?=
HT29 MUnLbY5ie2ViYYPzZZk> MnzhglExKM7:TR?= NY\OPXc6cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MmnsNlA1QDRyMUi=
MDA-MB-231 M1rlfGtqdmG|ZTDhd5NigQ>? MVz+NVAh|ryP MkPhbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MVuyNFQ5PDBzOB?=
NCI-H441 MlvVT4lv[XOnIHHzd4F6 NVPS[4xChjFyIN88US=> MlLkbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= M4PibFIxPDh2MEG4
SK-MEL-28 MoTuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkHKN|Mh|ryP MWHJR|UxRjN|IN88US=> MknrNlA1QDRyMUi=
NCI-H661 MlvZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUD3dZZCOzNizszN M3rkTmlEPTB-M{Og{txO MYmyNFQ5PDBzOB?=
NCI-H446 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWXoOZFbOzNizszN NWjYUHdXUUN3ME23JO69VQ>? NGnkWG8zODR6NECxPC=>
MDA-MB-231 NIi4SY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3PpSlM{KM7:TR?= MWPJR|UxRTBwNUWg{txO M133NFIxPDh2MEG4
DLD-1 M3ntXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3;JOVM{KM7:TR?= NGfubIRKSzVyPUCuOVMh|ryP Ml\kNlA1QDRyMUi=
A549 M4fOWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVK2[lZ7OzNizszN Mo\TTWM2OD1yLkW5JO69VQ>? M3[5RlIxPDh2MEG4
SK-OV-3 NY\LT5pOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NES5dnE{OyEQvF2= NFPZWG9KSzVyPUCuOlYh|ryP MoCzNlA1QDRyMUi=
NCI-H460 NWnobnI4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGD3Tpo{OyEQvF2= MmXyTWM2OD1yLk[g{txO NIr0Um8zODR6NECxPC=>
A375 M3K1e2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnzmN|Mh|ryP NGfDXmtKSzVyPUCuOFIh|ryP NVXrdIozOjB2OESwNVg>
NCI-H441 NHzXZ3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX[zN{DPxE1? MXLJR|UxRTBwMzFOwG0> M1f0TlIxPDh2MEG4
HT29 Mn75S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXHh[oxTOzNizszN MlPXTWM2OD1yLkS5JO69VQ>? MVKyNFQ5PDBzOB?=
MKN-45 NFnMcoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGjxUYE{OyEQvF2= NX6yR5V{UUN3ME2wMlU5KM7:TR?= MoTyNlA1QDRyMUi=
HT29 M3fJZ2Fxd3C2b4Ppd{Bie3OjeR?= NFHJepV,OTBizszN MWDzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? MXGyNFQ5PDBzOB?=
MKN-45 M3mxZmFxd3C2b4Ppd{Bie3OjeR?= MlLDglExKM7:TR?= NWrJUppLe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NGK3RWozODR6NECxPC=>
MDA-MB-231 NUjSNW5bSXCxcITvd4l{KGG|c3H5 MWD+NVAh|ryP NWnBeYFldW:mZYP0cJkhcW6mdXPld{BieG:ydH;zbZMh[nliM{WlMi=> MljONlA1QDRyMUi=
MDA-MB-231/TGL MnX3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYT+NVAxKM7:TR?= MXrHTVUxRTFwMjFOwG0> NUT0RXNHOjJyMke2PVA>
1833/TGL NH:yTnFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4rzcJ4yODBizszN M3ntWmdKPTB;Mz63JO69VQ>? MnnkNlIxOjd4OUC=
EBC1 NF;2UJVEgXSxdH;4bYPDqGG|c3H5 NEOwWIV,OTBizszN NWPQWJptcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> M1TlSlI{PTl6Mke2
SNU638 MkDLR5l1d3SxeHnjxsBie3OjeR?= NXq3[Xh6hjFyIN88US=> MWnpcohq[mm2czD0bIUh[2WubDDndo94fGhw MnjQNlM2QTh{N{[=
A549 NXnsVJlwS3m2b4TvfIlkyqCjc4PhfS=> MV3+NVAh|ryP M4jiS45wfCCjZn\lZ5Q> NXLRfWpnOjN3OUiyO|Y>
H460 NETwboREgXSxdH;4bYPDqGG|c3H5 M4DhXJ4yOCEQvF2= M3v6Wo5wfCCjZn\lZ5Q> MVGyN|U6QDJ5Nh?=
HCC827 MW\DfZRwfG:6aXRCpIF{e2G7 MmTzglExKM7:TR?= MkHxco91KGGoZnXjeC=> MWSyN|U6QDJ5Nh?=
A549 NGO0Z3RHfW6ldHnvckBie3OjeR?= NEP6V3AyOCEQvF2= Mn\H[Il{enWydIOgcYlkem:2dXL1cIU> NHP4dlIzOzV7OEK3Oi=>
EBC1 MYrGeY5kfGmxbjDhd5NigQ>? NELOOZAyOCEQvF2= MV\kbZNzfXC2czDtbYNzd3S3YoXs[S=> NEXTeoYzOzV7OEK3Oi=>
H460 NUPPbIlHTnWwY4Tpc44h[XO|YYm= NX\4Z2hwOTBizszN M{W3SIlvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? NFnySoszPTNzM{CxNC=>
K562/VCR Mn:1R5l1d3SxeHnjxsBie3OjeR?= MX;+NVAh|ryP NF\Gfnd{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M4HUPFI2OzF|MEGw
CEM/VBL NXXQWIF[S3m2b4TvfIlkyqCjc4PhfS=> NHvBeY9,OTBizszN M1S1OZNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= Ml;YNlU{OTNyMUC=
U266 NFrHNYhEgXSxdH;4bYPDqGG|c3H5 NHG4RlN,OyEQvF5CpC=> NXK0fVU3UUN3ME2xMlEh|ryP MnnxNlU5OTByMUO=
OPM-2 MV;DfZRwfG:6aXRCpIF{e2G7 NHn5Vpl,OyEQvF5CpC=> NYL6bWFvUUN3ME2xMlgh|ryP M1y4TVI2QDFyMEGz
MM.1S NF\6e2ZEgXSxdH;4bYPDqGG|c3H5 NGnNZop,OyEQvF5CpC=> NEHYTmVKSzVyPUGuOkDPxE1? NHvOZYYzPThzMECxNy=>
MM.1R NIX4VI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn3rN{DPxE4EoB?= M3i2NIlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IES5KS=> NX3J[HkyOjV6MUCwNVM>
RPMI-8226 MoG0R5l1d3SxeHnjxsBie3OjeR?= M2DhTJ4{KM7:TdMg NUnwVlA6UUN3ME2wMlkh|ryP MVyyOVgyODBzMx?=
ANBL-6 MVHDfZRwfG:6aXRCpIF{e2G7 NWPmUGNmOSEQvF5CpC=> MVPpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NVLqNpdkOjV6MUCwNVM>
ANLB-6/V10R MlLLR5l1d3SxeHnjxsBie3OjeR?= MlnDNUDPxE4EoB?= NGnkb3hqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NHLnTpgzPThzMECxNy=>
KAS-6/1 MnGxR5l1d3SxeHnjxsBie3OjeR?= Mn7ZNUDPxE4EoB?= NX7uO4EycW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NFf1c2ozPThzMECxNy=>
KAS-6/V10R M1zBO2N6fG:2b4jpZ:Kh[XO|YYm= NWHqOVlxOSEQvF5CpC=> NFrwWWJqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MXeyOVgyODBzMx?=
KAS-6/R10R MnzVR5l1d3SxeHnjxsBie3OjeR?= M3HSOVEh|ryPwrC= M4Lue4lv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M4DiOVI2QDFyMEGz
8226/S M2\6dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWXGPZl1OyEQvF5CpC=> MV3pcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NUf5T2JmOjV6MUCwNVM>
8226/LR-5 NHPidGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVXLTpd{OyEQvF5CpC=> NG\5cmVqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC1OEU> MoO2NlU5OTByMUO=
Huh7 M2nwSWN6fG:2b4jpZ:Kh[XO|YYm= Ml\OglQvQCEQvF5CpC=> M1ToRmROW09? MXrJR|UxRTlwOTDuUS=> NESxdpAzPjJ3OUK1NC=>
Hep3B MlXiR5l1d3SxeHnjxsBie3OjeR?= NX7Z[ot2hjRwODFOwG3DqA>? NGHyb5JFVVOR Mn;5TWM2OD12NEiuO{BvVQ>? MWKyOlI2QTJ3MB?=
HepG2 MVrDfZRwfG:6aXRCpIF{e2G7 M4HJTZ41NjhizszNxsA> MWLEUXNQ MWfJR|UxRTF|OT63O{BvVQ>? MV6yOlI2QTJ3MB?=
Chang NIKwOIVEgXSxdH;4bYPDqGG|c3H5 M{TreZ41NjhizszNxsA> M1jKZWROW09? NGXkWXhKSzVyPUS0PE44KG6P NFHsSVkzPjJ3OUK1NC=>
Huh7 M{W0T2Z2dmO2aX;uJIF{e2G7 MXuxMlYh|ryPwrC= M125RWROW09? NVLrTFBD[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= NGnIbG8zPjJ3OUK1NC=>
Hep3B MX\GeY5kfGmxbjDhd5NigQ>? NFf4UogyNjZizszNxsA> NXvp[|NiTE2VTx?= NInwc5hk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MViyOlI2QTJ3MB?=
HepG2 Ml;KSpVv[3Srb36gZZN{[Xl? NGDRbIUyNjZizszNxsA> NUnGeXFnTE2VTx?= M{jVOINifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MWSyOlI2QTJ3MB?=
Chang NH7nNmVHfW6ldHnvckBie3OjeR?= NV;qWI11OS54IN88UeKh M3rqPWROW09? MmriZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MVuyOlI2QTJ3MB?=
MHCC97L MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXxglExKM7:TR?= MVfEUXNQ MWfJR|UxRTNzNTDuUS=> M2LpUVI3PDV6OUWz
MHCC97H M1nlc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;3NGJ,OTBizszN MnywSG1UVw>? MojtTWM2OD1|NklihKkhdk1? NYLU[HR[OjZ2NUi5OVM>
Huh7 NHTYV4VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnS0glExKM7:TR?= MmT3SG1UVw>? M1PJNWlEPTB;Mk[1JI5O MX[yOlQ2QDl3Mx?=
HepG2 NWO3fVBNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1;DWJ4yOCEQvF2= M1XOSWROW09? NHjQdnhKSzVyPUO5NkBvVQ>? MlrSNlY1PTh7NUO=
MHCC97L M{PDS2Z2dmO2aX;uJIF{e2G7 NVr2cYtjOSEQvF5CpC=> MWnEUXNQ M2Ts[olv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NUHPcJlpOjZ2NUi5OVM>
Huh7 NGrDdZVHfW6ldHnvckBie3OjeR?= MlTMNUDPxE4EoB?= NHnIXGxFVVOR M4i4folv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> MUiyOlQ2QDl3Mx?=
MHCC97L NWTRTIJ2SXCxcITvd4l{KGG|c3H5 NUT6dWxPOSEQvF5CpC=> M3jZNGROW09? MVvpcoR2[2W|IHHwc5B1d3Orcx?= MkmyNlY1PTh7NUO=
Huh7 Mn7jRZBweHSxc3nzJIF{e2G7 NGLvVYIyKM7:TdMg M4T2WmROW09? MW\pcoR2[2W|IHHwc5B1d3Orcx?= M4Gzc|I3PDV6OUWz
C3H 10T1/2 mouse fibroblasts MYLLbY5ie2ViYYPzZZk> MkjVNlUh|ryP MV\EUXNQ MknXdoVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> NGXHTWQzODV|NEO0OS=>
H23 M4fl[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV7ZRpdGOjVizszN M37PTGROW09? NIPne|F{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> MXyyNFU{PDN2NR?=
WM35 NG\PTotIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnLUNVAh|ryP MnjRSG1UVw>? MX7zbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MX6yNFU{PDN2NR?=
NIH 3T3 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmLGNVAh|ryP NXm0eYN[TE2VTx?= MmC1[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MoTuNlA2OzR|NEW=
H838 Mk\nS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXKxNEDPxE1? MX3EUXNQ MYDkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= NVTENYNmOjB3M{SzOFU>
H1395 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPVSHkyOCEQvF2= NUX2[5J5TE2VTx?= MlTI[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NVr3NHc{OjB3M{SzOFU>
Quiescent S2 Mo\kT4lv[XOnIHHzd4F6 NWDO[VI1OzBizszN NYPHVZVuTE2VTx?= NVzJWnZG[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz MnPDNlE2OTh7MUW=
PC3 MYXBdI9xfG:|aYOgZZN{[Xl? M1fzcVIxKM7:TR?= MlzRSG1UVw>? NUXROHhncW6mdXPld{BieG:ydH;zbZM> M2LJfVIyPzB7MUOw
Du145 NULIelZlSXCxcITvd4l{KGG|c3H5 NVrPRmZiOjBizszN MYLEUXNQ MmXmbY5lfWOnczDhdI9xfG:|aYO= NXHLRlBxOjF5MEmxN|A>
LNCaP NYXVeoFZSXCxcITvd4l{KGG|c3H5 NETGcWYzOCEQvF2= NFn0fJFFVVOR NVv0UnRmcW6mdXPld{BieG:ydH;zbZM> NWrs[Y0{OjF5MEmxN|A>
LAPC-4 MkHKRZBweHSxc3nzJIF{e2G7 NI\YfVczOCEQvF2= NWXXO5c2TE2VTx?= M1PIfIlv\HWlZYOgZZBweHSxc3nz NVHWO2lWOjF5MEmxN|A>
LNCaP M{i2NmZ2dmO2aX;uJIF{e2G7 NGW2dFEzOCEQvF2= MnLZSG1UVw>? NFTQZ5Fl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| Mmr6NlE4ODlzM{C=
LAPC-4 MXrGeY5kfGmxbjDhd5NigQ>? M4PS[FIxKM7:TR?= MUTEUXNQ Mkey[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? M1fvcVIyPzB7MUOw
Kasumi-1 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEeyU3Z,PTBizszN MnnOSG1UVw>? NGnnWXhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MnPnNlM{QTB3M{[=
SKNO-1 Ml\hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1T2[p42OCEQvF2= M1e2emROW09? NETwWoNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NEHuToIzOzN7MEWzOi=>
Kasumi-1 MlfkT4lv[XOnIHHzd4F6 NI[zSJF,OTBizszN MUnEUXNQ MXjy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NWXRN4FsOjN|OUC1N|Y>
SKNO-1 MXfLbY5ie2ViYYPzZZk> MX;+NVAh|ryP NFXEUHdFVVOR NWTzW2p[emWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NXvLeWhZOjN|OUC1N|Y>
A549 NH7lU5NHfW6ldHnvckBie3OjeR?= MYexNEDPxE1? MW\EUXNQ NWm1cYpC\W6qYX7j[ZMhdWm2b4TpZ{Bk[XSjc4Tyc5Bp\Q>? M3[0fVI1PzR4NUe0
NRK-52E NHTBcmtHfW6ldHnvckBie3OjeR?= M2LsVlExKM7:TR?= MWrEUXNQ NHfnVoNqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDTWGFVOyCwdXPs[YFzKHS{YX7zcI9k[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKFSJRj5OtlEtKGOxbHzh[4VvKEmYIHHu[EBncWK{b37lZ5Rqdg>? Mln1NlUxQDhyMEK=
PC12 MkHzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW\+NVIvPSEQvF2= NVvuUJQ2TE2VTx?= NVzkZW5KeHKndnXueJMhXFODLXnu[JVk\WRibnX1dol1\SCob4LtZZRqd25? MnHrNlUyOjh|OE[=
HPMCs NVnMVGVGTnWwY4Tpc44h[XO|YYm= NHTMNJZz\X[ncoPld{BmeGm2aHXsbYFtKHSxIH3ld4Vv[2i7bXHsJJRz[W6|aYTpc44hd2ZiaIXtZY4heGW{aYTvcoVidCCvZYPveIhmdGmjbDDj[Yxtew>? NEfOc|EzPjB2NUe4NC=>
A549 MnToSpVv[3Srb36gZZN{[Xl? NXiwd2QzhjVyIN88US=> M4CwUWROW09? NE\DcIdi\m[nY4TzJJRp\SC4aYLhcEBtcW[nIHP5Z4xmKGGwZDDoc5N1KHKnc4DvcpNm M4fwNFI3PzFzN{S4
RAW264.7 MYTGeY5kfGmxbjDhd5NigQ>? NEP5OVN,OzBizszN M2XRVmROW09? NGjJeFJz\WS3Y3XzJJBzdy2rbn\sZY1u[XSxcomg[4Vv\SCneIDy[ZN{cW:w Moi1NlY4OTh3OE[=
MEMM M{PqUWtqdmG|ZTDhd5NigQ>? NEnJN|YyPSEEtV2= Mm\rSG1UVw>? NViw[I5y\GWlcnXhd4V{KGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFM> M1HzRlI3QTJzNUC2
MEMM NEnpXHdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2eydJ4zOCEEtV2= NYrxSlVVTE2VTx?= MkLNbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MXeyOlkzOTVyNh?=
MEMM M3PVPWFxd3C2b4Ppd{Bie3OjeR?= M2ft[|E2KML3TR?= NGX2R5pFVVOR M1SzeYlv\HWlZYOgeIhmKHC{ZYPlcoNmKG:oIITo[UBieG:ydH;zbZMheHKxdHXpckwh[2ynYY\l[EBE[XOyYYPlMVM> M4DB[VI3QTJzNUC2
T47D M2C5bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYf6V29SOTBizszN MnS1SG1UVw>? MVvJR|UxRTd{IH7N NWnUU4Q1OTh|OEG0OFQ>
ZR-75-1 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILtXlUyOCEQvF2= NW\vUWQ6TE2VTx?= NVu2ZVJNUUN3ME23PUBvVQ>? M3vhelE5OzhzNES0
BT474 Mn3xS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXy0bYw1OTBizszN M4TuNGROW09? NWjNNHRyUUN3ME24OkBvVQ>? NF;KVGcyQDN6MUS0OC=>
HCC1954 NF7sSmpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnPONVAh|ryP NVv5THpGTE2VTx?= MVjJR|UxRTFzOTDuUS=> NIT2UIEyQDN6MUS0OC=>
MDA-MB-453 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX\3XWEzOTBizszN MWrEUXNQ Mn\JTWM2OD17N{Wgcm0> NHHNUo4yQDN6MUS0OC=>
MDA-MB-468 M1j2V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV:weXV3OTBizszN M4i0eGROW09? MkP0TWM2OD1|MkC4JI5O M2jmfFE5OzhzNES0
SkBr3 NHvKWJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4TjN|ExKM7:TR?= MlO4SG1UVw>? MXHJR|UxRjFyLECwNEBvVQ>? NXvwR|M2OTh|OEG0OFQ>
MDA-MB-231 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUDQcnhUOTBizszN MWrEUXNQ MUfJR|UxRjFyLECwNEBvVQ>? NFHCbZAyQDN6MUS0OC=>
HCT116 NYHNSlJZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkjMNVAh|ryP MWnEUXNQ MljHTWM2OD13OEO2JI5O NX3UWGI{OTh|OEG0OFQ>
HT29 Ml\0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1OxRVExKM7:TR?= MmG1SG1UVw>? NH\mOYxKSzVyPkGwMFAxOCCwTR?= M2mweFE5OzhzNES0
HFF NGDtXm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXTScnFJOTBizszN NX;DVI9xTE2VTx?= MnqyTWM2OD15NkG1JI5O NX6zTnJqOTh|OEG0OFQ>
HN5 NV3USXRNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWWxNEDPxE1? MVPEUXNQ MYnJR|UxRjFyLECwNEBvVQ>? M3rPTlE5OzhzNES0
786-0 MlnhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{jsOlExKM7:TR?= MX7EUXNQ MX3JR|UxRTRyMEmgcm0> NI\FZVQyQDN6MUS0OC=>
H157 NY\LbpJLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4nrflExKM7:TR?= NVvtO2FqTE2VTx?= MYTJR|UxRTJ4NEKgcm0> NUnNNIhwOTh|OEG0OFQ>
NCI-H460 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mo\ENVAh|ryP NVW5TJI1TE2VTx?= MkO0TWM2OD5{LEWwNEBvVQ>? MWixPFM5OTR2NB?=
SKOV-3 NYfm[5FMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXuxNEDPxE1? NX[zW2l7TE2VTx?= NYroeJg6UUN3ME2yNVI3KG6P NYjEdHBmOTh|OEG0OFQ>
OVCAR-3 Ml;WS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkPkNVAh|ryP MYjEUXNQ M2PNNmlEPTB;MkmxPEBvVQ>? M4LtblE5OzhzNES0
BXPC3 M{jlS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXTQRog2OTBizszN NHLKS5pFVVOR NFrFV2xKSzVyPUOxOFEhdk1? NHG4bJoyQDN6MUS0OC=>
MiaPaCa NYXpd2h5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWLXb5B2OTBizszN NHHTPVdFVVOR NUXvXmdwUUN3ME21OFM{KG6P NEe4dFMyQDN6MUS0OC=>
PANC-1 NXrxe3lFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHrpdZcyOCEQvF2= MljaSG1UVw>? NUTp[ZZMUUN3ME24OlgyKG6P NUW3S4wzOTh|OEG0OFQ>
LNCaP NVm0Vpo2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYW4WZBsOTBizszN M3\ZbGROW09? M2jZVWlEPTB;MUS3JI5O MVexPFM5OTR2NB?=
DU145 M{PnOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVnxW4lqOTBizszN MVPEUXNQ NHvhZXJKSzVyPUO4NVIhdk1? MUOxPFM5OTR2NB?=
PC3 NVTSR3BIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlf5NVAh|ryP M4DKdWROW09? Mn7DTWM2OD5zMDywNFAhdk1? NHvmVZoyQDN6MUS0OC=>
BT474 NVX3S3I1U2mwYYPlJIF{e2G7 MkjvNVAh|ryP MV7EUXNQ NXfDbGd2cW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMU[wJI5O NXHMOmxqOTh|OEG0OFQ>
786-0 M3rJVmtqdmG|ZTDhd5NigQ>? M{j3W|ExKM7:TR?= MorMSG1UVw>? NHu2cGVqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iBzNUCgcm0> NWnlSIhKOTh|OEG0OFQ>
LNCaP NXrXcVJyU2mwYYPlJIF{e2G7 MXWxNEDPxE1? NXi4VWZoTE2VTx?= MVHpcohq[mm2czDwS3NMO87{IIfpeIghUUN3MDDv[kA1OyCwTR?= MUexPFM5OTR2NB?=
PC3 NIS5b4ZMcW6jc3WgZZN{[Xl? NWHQNW9nOTBizszN NWDuZZBlTE2VTx?= MljibY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDlibl2= MWCxPFM5OTR2NB?=
KARPAS-231 NH\FXmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1XlR|ExKM7:TR?= NWrifVl4TE2VTx?= M4XyVWVEPTB;NEGgcm0> M4TFeFE6ODZ2N{Ow
CCRFSB Mn[3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXzhTZp5OTBizszN NVXm[|c1TE2VTx?= NXX3bmh2TUN3ME2xOVUhdk1? MXGxPVA3PDd|MB?=
SUP B15 Ml3NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmTmNVAh|ryP M1PGWGROW09? M{fZ[WVEPTB;MUm3JI5O NF\zdZcyQTB4NEezNC=>
SD-1 MljUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGLIXVYyOCEQvF2= M4HDXmROW09? MVnFR|UxRTN{MDDuUS=> NVfPPJNkOTlyNkS3N|A>
RS4;11 NUm2WXR1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVK5NGdQOTBizszN NIfsRpVFVVOR NUHIbWZRTUN3ME22OVQhdk1? M2L1cFE6ODZ2N{Ow
MN-60 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVuxNEDPxE1? NH\NPJJFVVOR MWnFR|UxRTN4MEKgcm0> M372UFE6ODZ2N{Ow
Tanoue MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYOxNEDPxE1? MYfEUXNQ NVT1fmNzTUN3ME20OVE4KG6P NWPUbYFXOTlyNkS3N|A>
RCH-ACV NHf1V2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mnn1NVAh|ryP Mnf3SG1UVw>? MkPPSWM2OD1zNUKgcm0> M1fnSVE6ODZ2N{Ow
SEM MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NInZVWUyOCEQvF2= M{HqSGROW09? NHX5R5FGSzVyPUKwNkBvVQ>? NIrrUIIyQTB4NEezNC=>
KASUMI-2 MoLlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmXtNVAh|ryP MmrISG1UVw>? NUfyZ|RSTUN3ME2yNlUhdk1? M3:z[|E6ODZ2N{Ow
REH NUe4e2xNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn;4NVAh|ryP NHTkRZJFVVOR M{TJfmVEPTB;Mki4JI5O MUexPVA3PDd|MB?=
697 NH7VRpFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUHXbYd2OTBizszN MXvEUXNQ NGDwSXNGSzVyPUOzPEBvVQ>? M3fqZlE6ODZ2N{Ow
NALM-6 NEHaT3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVzld4dlOTBizszN NYPxUVJPTE2VTx?= NIfrOGdGSzVyPUSyNUBvVQ>? NIL0NWUyQTB4NEezNC=>
MHH-CALL–3 MlnOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIL1cZoyOCEQvF2= NGLLPYxFVVOR MYjFR|UxRThzMjDuUS=> M3jMXVE6ODZ2N{Ow
MHH-CALL–2 NH;X[Y9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXXaNY5pOTBizszN NI\wTo9FVVOR Mln5SWM2OD1{MUG0JI5O MWCxPVA3PDd|MB?=
J.GAMMA-1 M{izcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVr6cWxEOTBizszN MYrEUXNQ NGnGbGRGSzVyPU[1JI5O MW[xPVA3PDd|MB?=
JR45.01 NXzJTYxNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3PPO|ExKM7:TR?= M{DTUWROW09? NGnuPFlGSzVyPU[4JI5O NG\rWG4yQTB4NEezNC=>
A3 M3[5Wmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWDPN2V4OTBizszN NFzYelFFVVOR M165R2VEPTB;Nkmgcm0> MYWxPVA3PDd|MB?=
I 2.1 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF;scIkyOCEQvF2= MWXEUXNQ NHvjVG1GSzVyPUezJI5O M1;DXVE6ODZ2N{Ow
MOLT-3 NHL4dJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1nvdVExKM7:TR?= MX7EUXNQ MWLFR|UxRTd2IH7N NVHnd2lTOTlyNkS3N|A>
P116 MlzYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmK2NVAh|ryP M4\aN2ROW09? NHHJXGJGSzVyPUe4JI5O M17NZlE6ODZ2N{Ow
J.Cam1.6 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1nxSFExKM7:TR?= MlnlSG1UVw>? MUnFR|UxRTd7IH7N MVyxPVA3PDd|MB?=
I 9.2 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYqxNEDPxE1? MVfEUXNQ NH:wNHZGSzVyPUiwJI5O NXPyN4R3OTlyNkS3N|A>
LOUCY NVnQS3ZoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHfoZ|MyOCEQvF2= NEDhZ4FFVVOR M3;0emVEPTB;MUG3JI5O MnHkNVkxPjR5M{C=
J.RT3-T3.5 MojRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{OxeVExKM7:TR?= MlfmSG1UVw>? MUDFR|UxRTF{MzDuUS=> MVuxPVA3PDd|MB?=
800000 M2Xjb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1TZdVExKM7:TR?= M3LCNWROW09? MVHFR|UxRTF4MzDuUS=> NH\6W|kyQTB4NEezNC=>
Jurkat M4HOSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW[xNEDPxE1? M1HyNmROW09? M{f3c2VEPTB;MkK1JI5O MVyxPVA3PDd|MB?=
MOLT-4 MorvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWP3cGM5OTBizszN NEPRcotFVVOR NIKydJdGSzVyPUKzNkBvVQ>? NH:4VVkyQTB4NEezNC=>
Molt-16 M3n5SWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVi1NoJZOTBizszN NHrk[G9FVVOR M2W3e2VEPTB;MkSxJI5O MUKxPVA3PDd|MB?=
CEM/C3 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVKxNEDPxE1? Mo\0SG1UVw>? NHG5[FZGSzVyPUK1O{BvVQ>? NFm5WpIyQTB4NEezNC=>
CEM/C2 NVXSSplmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4jUVFExKM7:TR?= M3HmbWROW09? M4fjOmVEPTB;MkexJI5O NGjsVlcyQTB4NEezNC=>
CCRFCEM NWLYVldwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIPYS5YyOCEQvF2= M4jRd2ROW09? NV\aUZZTTUN3ME2zNlchdk1? M3:1O|E6ODZ2N{Ow
CEM/C1 M4HhSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mmr0NVAh|ryP M1HUfWROW09? M1fVVGVEPTB;M{iyJI5O M17X[FE6ODZ2N{Ow
SUPTI[VB] NIPmcXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MljmNVAh|ryP MojlSG1UVw>? MlLDSWM2OD14MUmgcm0> M3TWRVE6ODZ2N{Ow
CCRF–HSB-2 NE\6So9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXuxNEDPxE1? M2GwV2ROW09? NF7WXWdGSzVyPUKxNVchdk1? M3zMN|E6ODZ2N{Ow
I 2.1 Ml;JRZBweHSxc3nzJIF{e2G7 NHTvbZgyOCEQvF2= NUj0bXdjTE2VTx?= NFPlSpNqdmS3Y3XzJIFxd3C2b4Ppdy=> NYTHUYlkOTlyNkS3N|A>
I 9.2 M{G1Z2Fxd3C2b4Ppd{Bie3OjeR?= NX7MT29COTBizszN MkjZSG1UVw>? MmDtbY5lfWOnczDhdI9xfG:|aYO= M4HIW|E6ODZ2N{Ow
A3 Ml;BRZBweHSxc3nzJIF{e2G7 MmnqNVAh|ryP NUfYSHVMTE2VTx?= Ml;wbY5lfWOnczDhdI9xfG:|aYO= M{D1VFE6ODZ2N{Ow
RD MmfoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkLQNVAh|ryP MVvJR|UxRjFyIN88US=> NFTD[VgzODd2ME[yNy=>
Rh41 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFXRVJcyOCEQvF2= NWHNTGRyUUN3ME2zN{45KG6P MX:yNFc1ODZ{Mx?=
Rh18 M{HTWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUGxNEDPxE1? MX3JR|UxRTNyMzDuUS=> Ml3hNlA4PDB4MkO=
Rh30 MmHlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVy2XnNDOTBizszN NW[zdJBJUUN3ME20MlgyKM7:TR?= MX:yNFc1ODZ{Mx?=
BT-12 NGPs[HJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYmxNEDPxE1? NET5WYdKSzVyPkGwJO69VQ>? Ml3lNlA4PDB4MkO=
CHLA-266 MnjrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUf6[mdmOTBizszN M{LUZmlEPTB;MT6yNkDPxE1? NGG3d4IzODd2ME[yNy=>
TC-71 MorYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIj2bm8yOCEQvF2= NV;re5lmUUN3ME2yMlUzKM7:TR?= MYiyNFc1ODZ{Mx?=
CHLA-9 MlOzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnrPNVAh|ryP M1jrWmlEPTB;NUmxJI5O M3q3UVIxPzRyNkKz
CHLA-10 NEjieHRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGHaT44yOCEQvF2= MUPJR|UxRTFyMjDuUS=> M2XjXFIxPzRyNkKz
CHLA-258 NEn2cnlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUGxNEDPxE1? Mmf4TWM2OD1zLkC1JO69VQ>? M3jTU|IxPzRyNkKz
GBM2 NXW2WI41T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXqxNEDPxE1? MWLJR|UxRTlwMUWg{txO NWfRT4ZkOjB5NEC2NlM>
NB-1643 M1ziVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2K2UFExKM7:TR?= NW\LTnJpUUN3ME21MlQh|ryP MXmyNFc1ODZ{Mx?=
NB-Ebc1 M1;zOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1LHZ|ExKM7:TR?= NGjoTHZKSzVyPkGwJO69VQ>? MVmyNFc1ODZ{Mx?=
CHLA-90 NXHVVohST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXOxNEDPxE1? M1vOemlEPTB-MUCg{txO MXSyNFc1ODZ{Mx?=
CHLA-136 NED1NmRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYDQR4xqOTBizszN MlTrTWM2OD5zMDFOwG0> NXjGU5h6OjB5NEC2NlM>
NALM-6 M1nv[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn\5NVAh|ryP Ml3rTWM2OD1{NkWgcm0> NVrhVo93OjB5NEC2NlM>
COG-LL-317 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFHiS3EyOCEQvF2= Mni0TWM2OD14LkS5JI5O NWDCempqOjB5NEC2NlM>
RS4;11 M4DGNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoHVNVAh|ryP MXTJR|UxRTF2NzDuUS=> MWCyNFc1ODZ{Mx?=
MOLT-4 NFPIWmlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mkm5NVAh|ryP M3j1XGlEPTB;NECgcm0> M1HmR|IxPzRyNkKz
CCRF-CEM MnOxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXqxNEDPxE1? NVvaXmoyUUN3ME2yOlghdk1? MUmyNFc1ODZ{Mx?=
Kasumi-1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWmxNEDPxE1? NFqySIRKSzVyPUGwO{BvVQ>? MVeyNFc1ODZ{Mx?=
Karpas-299 M1LsWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUO5eoFOOTBizszN M17wZmlEPTB;Mj65N{DPxE1? NGXpZmozODd2ME[yNy=>
Ramos-RA1 NHq0U21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXmxNEDPxE1? MXTJR|UxRTdwM{Wg{txO MnW1NlA4PDB4MkO=
H1299 MXHLbY5ie2ViYYPzZZk> MoHCNVAh|ryP NVnJfW42cW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? NFm1Zm8zOTlyOE[xOi=>

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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
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.

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID