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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NXrsOGh3U2mwYYPlJIF{e2G7 M2XNXp4yOCEQvF2= MWDpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NWfVcGNvOjB2OESwNVg>
HT29 NVX5SJJQU2mwYYPlJIF{e2G7 MVX+NVAh|ryP MV\pcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M{Hn[lIxPDh2MEG4
MDA-MB-231 NED2SZBMcW6jc3WgZZN{[Xl? MoTIglExKM7:TR?= MnW5bY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NIHaRmMzODR6NECxPC=>
NCI-H441 MkG5T4lv[XOnIHHzd4F6 M2XJS54yOCEQvF2= NVPzfoxycW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MknGNlA1QDRyMUi=
SK-MEL-28 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXPrNoRuOzNizszN MkT4TWM2OD5|MzFOwG0> MojBNlA1QDRyMUi=
NCI-H661 NF36R4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jvV|M{KM7:TR?= M{DpZmlEPTB-M{Og{txO NGXwWYQzODR6NECxPC=>
NCI-H446 NXz1ZXZwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWWzN{DPxE1? NF;n[2ZKSzVyPUeg{txO MUOyNFQ5PDBzOB?=
MDA-MB-231 MnPRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXOyeod2OzNizszN MoLkTWM2OD1yLkW1JO69VQ>? MoTPNlA1QDRyMUi=
DLD-1 NEPVbXVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX\HWo41OzNizszN MV3JR|UxRTBwNUOg{txO MlSyNlA1QDRyMUi=
A549 M2\XZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUP4VG04OzNizszN NWLpdJFHUUN3ME2wMlU6KM7:TR?= NYD4Oo5VOjB2OESwNVg>
SK-OV-3 M2CydWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkPyN|Mh|ryP MXvJR|UxRTBwNk[g{txO NITLR4czODR6NECxPC=>
NCI-H460 NW\5fXN1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXmzN{DPxE1? NGX3bo1KSzVyPUCuOkDPxE1? MX[yNFQ5PDBzOB?=
A375 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmPsN|Mh|ryP M2XkZ2lEPTB;MD60NkDPxE1? M1zOTlIxPDh2MEG4
NCI-H441 NHLNWWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXmzN{DPxE1? M4PqUGlEPTB;MD6zJO69VQ>? M37tdFIxPDh2MEG4
HT29 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHvOW2k{OyEQvF2= MljUTWM2OD1yLkS5JO69VQ>? M4f0O|IxPDh2MEG4
MKN-45 NIDxTXhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jXXVM{KM7:TR?= NXL2NIJVUUN3ME2wMlU5KM7:TR?= NI\VWJkzODR6NECxPC=>
HT29 NYTWRZZbSXCxcITvd4l{KGG|c3H5 NVTwboNuhjFyIN88US=> MkHXd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MYCyNFQ5PDBzOB?=
MKN-45 MVPBdI9xfG:|aYOgZZN{[Xl? NWe3XGJbhjFyIN88US=> M2XCUpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= MWSyNFQ5PDBzOB?=
MDA-MB-231 MWjBdI9xfG:|aYOgZZN{[Xl? M1vLeZ4yOCEQvF2= MWrtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw NVrCO2hUOjB2OESwNVg>
MDA-MB-231/TGL M4XMbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm\lglExOCEQvF2= MlTNS2k2OD1zLkKg{txO M1TNS|IzODJ5Nkmw
1833/TGL M1;TdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoW0glExOCEQvF2= M2PH[WdKPTB;Mz63JO69VQ>? M3vwU|IzODJ5Nkmw
EBC1 MoK1R5l1d3SxeHnjxsBie3OjeR?= MlzrglExKM7:TR?= NGiwbpFqdmirYnn0d{B1cGViY3XscEBoem:5dHiu NHvaOG4zOzV7OEK3Oi=>
SNU638 NYTYe|A1S3m2b4TvfIlkyqCjc4PhfS=> M3r5b54yOCEQvF2= M3HF[YlvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= Mo\sNlM2QTh{N{[=
A549 MkP5R5l1d3SxeHnjxsBie3OjeR?= MmLuglExKM7:TR?= Ml:yco91KGGoZnXjeC=> NH:xRo4zOzV7OEK3Oi=>
H460 NUPnSnM3S3m2b4TvfIlkyqCjc4PhfS=> MmfYglExKM7:TR?= M4\FcI5wfCCjZn\lZ5Q> M33LSVI{PTl6Mke2
HCC827 NIrvTGdEgXSxdH;4bYPDqGG|c3H5 NFvpTFJ,OTBizszN MVLuc5Qh[W[oZXP0 MXKyN|U6QDJ5Nh?=
A549 NH\kNIpHfW6ldHnvckBie3OjeR?= MWqxNEDPxE1? MVnkbZNzfXC2czDtbYNzd3S3YoXs[S=> MYqyN|U6QDJ5Nh?=
EBC1 NV;L[XlxTnWwY4Tpc44h[XO|YYm= MorKNVAh|ryP NEfPfphlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? Mnv6NlM2QTh{N{[=
H460 MVvGeY5kfGmxbjDhd5NigQ>? NE\WVo0yOCEQvF2= NITERldqdmirYnn0d{B1fWK3bHnuJJBwdHmvZYLpfoF1cW:w MkjGNlU{OTNyMUC=
K562/VCR MV\DfZRwfG:6aXRCpIF{e2G7 MoDGglExKM7:TR?= M2C0PZNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= MYiyOVMyOzBzMB?=
CEM/VBL MlvxR5l1d3SxeHnjxsBie3OjeR?= NF;ETGJ,OTBizszN NV3iSIdne2ixd4OgZ5l1d3SxeHnjJIFkfGm4aYT5 M{\FXFI2OzF|MEGw
U266 NIjwT5JEgXSxdH;4bYPDqGG|c3H5 MknsglMh|ryPwrC= MVjJR|UxRTFwMTFOwG0> MXGyOVgyODBzMx?=
OPM-2 MlGyR5l1d3SxeHnjxsBie3OjeR?= MU\+N{DPxE4EoB?= M13DfWlEPTB;MT64JO69VQ>? NXHMfWNXOjV6MUCwNVM>
MM.1S M3jEWmN6fG:2b4jpZ:Kh[XO|YYm= Ml;oglMh|ryPwrC= MWXJR|UxRTFwNjFOwG0> NXfLNWdIOjV6MUCwNVM>
MM.1R MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXPmPYVbOyEQvF5CpC=> MorobY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml MkHhNlU5OTByMUO=
RPMI-8226 MWLDfZRwfG:6aXRCpIF{e2G7 NF72eYV,OyEQvF5CpC=> NHXZO4RKSzVyPUCuPUDPxE1? MXmyOVgyODBzMx?=
ANBL-6 MoLvR5l1d3SxeHnjxsBie3OjeR?= M1rMbFEh|ryPwrC= MYjpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MoLYNlU5OTByMUO=
ANLB-6/V10R MlTpR5l1d3SxeHnjxsBie3OjeR?= MUKxJO69VcLi NYTBXZZXcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> Mlq4NlU5OTByMUO=
KAS-6/1 NWHBRXlUS3m2b4TvfIlkyqCjc4PhfS=> MV2xJO69VcLi NV;1elducW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> Mkn6NlU5OTByMUO=
KAS-6/V10R MX7DfZRwfG:6aXRCpIF{e2G7 NInU[ngyKM7:TdMg NFHtNIhqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MlTTNlU5OTByMUO=
KAS-6/R10R M2fmUGN6fG:2b4jpZ:Kh[XO|YYm= M2GxelEh|ryPwrC= NGX0TmFqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NXHYNoNSOjV6MUCwNVM>
8226/S M4TEbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4r0bVMh|ryPwrC= NYPlSVFxcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm NGPlZm8zPThzMECxNy=>
8226/LR-5 MlXqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSzJO69VcLi M3nyU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MoDENlU5OTByMUO=
Huh7 M{XnbGN6fG:2b4jpZ:Kh[XO|YYm= Mn;6glQvQCEQvF5CpC=> MkTsSG1UVw>? MmXtTWM2OD17Lkmgcm0> M1nLd|I3OjV7MkWw
Hep3B NEniVppEgXSxdH;4bYPDqGG|c3H5 NXzEbIZshjRwODFOwG3DqA>? M1rkXWROW09? NULCXGdTUUN3ME20OFgvPyCwTR?= M2j2UVI3OjV7MkWw
HepG2 NEi1SJpEgXSxdH;4bYPDqGG|c3H5 NXXUeXFwhjRwODFOwG3DqA>? MUTEUXNQ MlTqTWM2OD1zM{muO|chdk1? M1z6UFI3OjV7MkWw
Chang MmC0R5l1d3SxeHnjxsBie3OjeR?= MXP+OE45KM7:TdMg NYTIdlBsTE2VTx?= M4jSe2lEPTB;NES4Mlchdk1? NXnMWHAzOjZ{NUmyOVA>
Huh7 M3LhR2Z2dmO2aX;uJIF{e2G7 NYPWbHE5OS54IN88UeKh NH7NVpBFVVOR NY\zNFAz[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= NXPPclJWOjZ{NUmyOVA>
Hep3B M3u1UGZ2dmO2aX;uJIF{e2G7 MnvUNU43KM7:TdMg M{m5OmROW09? MW\jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 M3LSWFI3OjV7MkWw
HepG2 MUHGeY5kfGmxbjDhd5NigQ>? M3zEbVEvPiEQvF5CpC=> Mmj5SG1UVw>? MoTnZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NEH0O2wzPjJ3OUK1NC=>
Chang M2jPVmZ2dmO2aX;uJIF{e2G7 MYGxMlYh|ryPwrC= Ml7SSG1UVw>? MlX4Z4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M33xWFI3OjV7MkWw
MHCC97L NXWyfWdIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVv+NVAh|ryP MWHEUXNQ M1TIUmlEPTB;M{G1JI5O MorhNlY1PTh7NUO=
MHCC97H MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXLYcFNZhjFyIN88US=> M{npbmROW09? MlrCTWM2OD1|NklihKkhdk1? MlnxNlY1PTh7NUO=
Huh7 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHVglExKM7:TR?= NIG3c2tFVVOR NYD6UYRJUUN3ME2yOlUhdk1? NITq[mIzPjR3OEm1Ny=>
HepG2 M2juUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGXsO21,OTBizszN M{G1WWROW09? NEK5VlBKSzVyPUO5NkBvVQ>? NFy4WFMzPjR3OEm1Ny=>
MHCC97L MVLGeY5kfGmxbjDhd5NigQ>? NYXybWV7OSEQvF5CpC=> MmG4SG1UVw>? NW\SZ3dKcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? Mn7PNlY1PTh7NUO=
Huh7 M2f6VGZ2dmO2aX;uJIF{e2G7 NULlZ4dNOSEQvF5CpC=> MoTFSG1UVw>? MXPpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u NUPTb|hNOjZ2NUi5OVM>
MHCC97L MU\BdI9xfG:|aYOgZZN{[Xl? MUOxJO69VcLi NGXUc3NFVVOR NVXLc2JpcW6mdXPld{BieG:ydH;zbZM> MmLTNlY1PTh7NUO=
Huh7 MV;BdI9xfG:|aYOgZZN{[Xl? MX2xJO69VcLi NHzJcpNFVVOR M1HKNolv\HWlZYOgZZBweHSxc3nz MlzMNlY1PTh7NUO=
C3H 10T1/2 mouse fibroblasts NH\tPFVMcW6jc3WgZZN{[Xl? NFrjNnQzPSEQvF2= M2XaTmROW09? MmH3doVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> M1nM[FIxPTN2M{S1
H23 NYHhZnMyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnxNlUh|ryP MkfpSG1UVw>? NFvsOXV{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> Mm\SNlA2OzR|NEW=
WM35 NFfC[|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M13DUVExKM7:TR?= MYLEUXNQ NIW2UWt{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> MorhNlA2OzR|NEW=
NIH 3T3 M1PSR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWq2O|VGOTBizszN MYnEUXNQ M33P[4Rw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M3nEd|IxPTN2M{S1
H838 NV\Peo1uT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGLEVGcyOCEQvF2= MXnEUXNQ NIHWVHBld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> MmT1NlA2OzR|NEW=
H1395 NFfqSXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUK4OWxFOTBizszN NV\pSVJJTE2VTx?= MUjkc4V{KG6xdDDoZZZmKGFic3nncolncWOjboSgbY5pcWKrdH;yfUBm\m[nY4S= MmfPNlA2OzR|NEW=
Quiescent S2 MnzhT4lv[XOnIHHzd4F6 MX[zNEDPxE1? NHTzW5lFVVOR MX3jc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? NH[3cJYzOTVzOEmxOS=>
PC3 Mlj6RZBweHSxc3nzJIF{e2G7 NYXpelYzOjBizszN M1TmOWROW09? M3PIXolv\HWlZYOgZZBweHSxc3nz NH;KU|IzOTdyOUGzNC=>
Du145 M4TFWmFxd3C2b4Ppd{Bie3OjeR?= MUGyNEDPxE1? NGrH[4xFVVOR MoLRbY5lfWOnczDhdI9xfG:|aYO= MX6yNVcxQTF|MB?=
LNCaP M3T5N2Fxd3C2b4Ppd{Bie3OjeR?= MWWyNEDPxE1? Mn;1SG1UVw>? MXzpcoR2[2W|IHHwc5B1d3Orcx?= NYn1T2xYOjF5MEmxN|A>
LAPC-4 NW\h[pN7SXCxcITvd4l{KGG|c3H5 M3XRVFIxKM7:TR?= MUPEUXNQ NW\ad21IcW6mdXPld{BieG:ydH;zbZM> M3OxNFIyPzB7MUOw
LNCaP Mn;QSpVv[3Srb36gZZN{[Xl? M1XPTlIxKM7:TR?= MXzEUXNQ MlXk[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? M3SwbVIyPzB7MUOw
LAPC-4 NIroUFFHfW6ldHnvckBie3OjeR?= M1\L[lIxKM7:TR?= NYToTYZXTE2VTx?= MkH0[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? NEHOTmYzOTdyOUGzNC=>
Kasumi-1 MlvlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1rJeJ42OCEQvF2= NInpbHpFVVOR NVv0Onc2cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnraNlM{QTB3M{[=
SKNO-1 NFTrZZBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkK1glUxKM7:TR?= MoWwSG1UVw>? MWHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MWCyN|M6ODV|Nh?=
Kasumi-1 M4ewN2tqdmG|ZTDhd5NigQ>? MkC4glExKM7:TR?= NIfkO2dFVVOR NUTHOYVyemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z MYiyN|M6ODV|Nh?=
SKNO-1 MV\LbY5ie2ViYYPzZZk> NGnoOFN,OTBizszN NWfTVphwTE2VTx?= NWHMb|ZYemWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z M1HObVI{OzlyNUO2
A549 MlPHSpVv[3Srb36gZZN{[Xl? M1LIeVExKM7:TR?= NVjufWdCTE2VTx?= Morw[Y5p[W6lZYOgcYl1d3SrYzDjZZRie3S{b4Do[S=> MWCyOFc1PjV5NB?=
NRK-52E MYDGeY5kfGmxbjDhd5NigQ>? M3jPXFExKM7:TR?= MmnQSG1UVw>? NVrOVlQ{cW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgV3RCXDNiboXjcIVieiC2cnHud4xw[2G2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCWR1[t{tIyNCClb3zsZYdmdiCLVjDhcoQh\mmkcn;u[YN1cW5? M2LmPVI2ODh6MECy
PC12 MmXOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUD+NVIvPSEQvF2= MlK3SG1UVw>? MYHwdoV3\W62czDUV2EucW6mdXPl[EBv\XW{aYTlJIZwem2jdHnvci=> MmjGNlUyOjh|OE[=
HPMCs MkK1SpVv[3Srb36gZZN{[Xl? NV\DfFhzemW4ZYLz[ZMh\XCrdHjlcIlidCC2bzDt[ZNmdmOqeX3hcEB1emGwc3n0bY9vKG:oIHj1cYFvKHCncnn0c45m[WxibXXzc5Rp\WyrYXygZ4VtdHN? M2TjUFI3ODR3N{iw
A549 MmLzSpVv[3Srb36gZZN{[Xl? MWP+OVAh|ryP Mn3tSG1UVw>? MmDFZYZn\WO2czD0bIUhfmm{YXygcIln\SCleXPs[UBidmRiaH;zeEBz\XOyb37z[S=> MofhNlY4OTF5NEi=
RAW264.7 MUHGeY5kfGmxbjDhd5NigQ>? M37RSp4{OCEQvF2= MkLzSG1UVw>? NGDNRYpz\WS3Y3XzJJBzdy2rbn\sZY1u[XSxcomg[4Vv\SCneIDy[ZN{cW:w M2P5RlI3PzF6NUi2
MEMM MX3LbY5ie2ViYYPzZZk> NYH1SmN7OTViwsXN NEKwOohFVVOR M{DQXYRm[3KnYYPld{Bi[2W2eXzheIlwdiCxZjDobZN1d26nIFiz NUPh[m06OjZ7MkG1NFY>
MEMM M{i2fmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;3Wm5rhjJyINM1US=> NWeweVZMTE2VTx?= M3XXc4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NUT2eZlrOjZ7MkG1NFY>
MEMM NXLFZXF4SXCxcITvd4l{KGG|c3H5 NIPSNpQyPSEEtV2= NH7lNVdFVVOR Mlf3bY5lfWOnczD0bIUheHKnc3XuZ4Uhd2ZidHjlJIFxd3C2b4Ppd{Bxem:2ZXnuMEBkdGWjdnXkJGNie3Cjc3WtNy=> MV:yOlkzOTVyNh?=
T47D Mmq2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYrINIRtOTBizszN Mmf4SG1UVw>? MW\JR|UxRTd{IH7N MYCxPFM5OTR2NB?=
ZR-75-1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWDyU5Z7OTBizszN MWDEUXNQ M1LVU2lEPTB;N{mgcm0> NHnZfI8yQDN6MUS0OC=>
BT474 NYW5dG9pT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4j2cVExKM7:TR?= Mn\RSG1UVw>? MorHTWM2OD16NjDuUS=> NHfUPIYyQDN6MUS0OC=>
HCC1954 NF;zN3lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEm1bZYyOCEQvF2= MWXEUXNQ NWH4eJFTUUN3ME2xNVkhdk1? NXnPXXF6OTh|OEG0OFQ>
MDA-MB-453 NFfCXYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXuxNEDPxE1? M1jhfGROW09? M2n1b2lEPTB;OUe1JI5O M2X4VVE5OzhzNES0
MDA-MB-468 MmjHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmq1NVAh|ryP Mnu3SG1UVw>? MYPJR|UxRTN{MEigcm0> NIrkPHYyQDN6MUS0OC=>
SkBr3 NHHHNo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnTnNVAh|ryP M{TnV2ROW09? M4OzeGlEPTB-MUCsNFAxKG6P NVnXSWhVOTh|OEG0OFQ>
MDA-MB-231 M2Pjb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1L0UVExKM7:TR?= MlLxSG1UVw>? MmXoTWM2OD5zMDywNFAhdk1? MYWxPFM5OTR2NB?=
HCT116 M3zOOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYnVc21pOTBizszN NXHjUJFxTE2VTx?= MV3JR|UxRTV6M{[gcm0> MXSxPFM5OTR2NB?=
HT29 NIXwS5VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYm4c3M1OTBizszN MVTEUXNQ NGjtZmVKSzVyPkGwMFAxOCCwTR?= MUSxPFM5OTR2NB?=
HFF NYHu[Y1sT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUXpZ|EzOTBizszN M17CV2ROW09? MUTJR|UxRTd4MUWgcm0> MnTINVg{QDF2NES=
HN5 MmHSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWW0c2I1OTBizszN NFPV[HVFVVOR MkXmTWM2OD5zMDywNFAhdk1? M1:ybFE5OzhzNES0
786-0 Mny1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXrOWmhZOTBizszN MoLJSG1UVw>? NWTBRYZYUUN3ME20NFA6KG6P M3noSFE5OzhzNES0
H157 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWr0[nRpOTBizszN MkCySG1UVw>? NI[1W|lKSzVyPUK2OFIhdk1? NVnaW253OTh|OEG0OFQ>
NCI-H460 NEXrXlhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEKxVVEyOCEQvF2= M{n4TGROW09? NUD5Z3lwUUN3ME6yMFUxOCCwTR?= MYixPFM5OTR2NB?=
SKOV-3 NWCycohXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2nnTFExKM7:TR?= M1;uTWROW09? NI\K[IJKSzVyPUKxNlYhdk1? MkjiNVg{QDF2NES=
OVCAR-3 MoLHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1nOU|ExKM7:TR?= MX\EUXNQ MVXJR|UxRTJ7MUigcm0> MkHDNVg{QDF2NES=
BXPC3 NYDhSW4xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV7lem02OTBizszN M3rwT2ROW09? M1ztZmlEPTB;M{G0NUBvVQ>? M2e3b|E5OzhzNES0
MiaPaCa MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV3KcFQ5OTBizszN MUnEUXNQ NF7PTmxKSzVyPUW0N|Mhdk1? M4fRWFE5OzhzNES0
PANC-1 MnfGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHZR4kyOCEQvF2= MkLvSG1UVw>? NETIcGlKSzVyPUi2PFEhdk1? NVHDNHllOTh|OEG0OFQ>
LNCaP Ml7iS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYTHe4FbOTBizszN M13Cc2ROW09? NIj2bYhKSzVyPUG0O{BvVQ>? NVu3[G93OTh|OEG0OFQ>
DU145 MkTuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFX1NnkyOCEQvF2= NU\CZZlpTE2VTx?= NW\KflhvUUN3ME2zPFEzKG6P M4nyZlE5OzhzNES0
PC3 NYfIfpVLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUSxNEDPxE1? M4TaeGROW09? Mo\oTWM2OD5zMDywNFAhdk1? MV[xPFM5OTR2NB?=
BT474 M4TGVmtqdmG|ZTDhd5NigQ>? NH\2dFgyOCEQvF2= MVfEUXNQ Moq0bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTZyIH7N NIfKVZQyQDN6MUS0OC=>
786-0 M4H4UmtqdmG|ZTDhd5NigQ>? MmG5NVAh|ryP M3TINmROW09? Ml:2bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTVyIH7N M1rURVE5OzhzNES0
LNCaP MnnOT4lv[XOnIHHzd4F6 M1;VbVExKM7:TR?= NX32[JZETE2VTx?= NH3LR4tqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2MzDuUS=> M1y5Z|E5OzhzNES0
PC3 MUHLbY5ie2ViYYPzZZk> MYqxNEDPxE1? NWC0fJoxTE2VTx?= NVz4dFNUcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEmgcm0> NH3hT3YyQDN6MUS0OC=>
KARPAS-231 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NG\YdmsyOCEQvF2= M2rWc2ROW09? M3;ScWVEPTB;NEGgcm0> MUSxPVA3PDd|MB?=
CCRFSB NHXI[Y5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\UNVAh|ryP M3vRfGROW09? NWrjWpMyTUN3ME2xOVUhdk1? M4DHTFE6ODZ2N{Ow
SUP B15 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUfhbpozOTBizszN NILHPWRFVVOR NH7aUWFGSzVyPUG5O{BvVQ>? NF7GR4oyQTB4NEezNC=>
SD-1 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUSxNEDPxE1? NFvwdphFVVOR NHrKUpNGSzVyPUOyNEBvVQ>? NXnzSmo6OTlyNkS3N|A>
RS4;11 MoiwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo\QNVAh|ryP NGe2O2NFVVOR NEPBOZlGSzVyPU[1OEBvVQ>? MoKwNVkxPjR5M{C=
MN-60 MlmzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGe3UFYyOCEQvF2= MmnlSG1UVw>? MX3FR|UxRTN4MEKgcm0> NELK[XEyQTB4NEezNC=>
Tanoue M332dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoLxNVAh|ryP NWPTe3F6TE2VTx?= NHraUoNGSzVyPUS1NVchdk1? NYjRVlJ1OTlyNkS3N|A>
RCH-ACV MnjYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3q3OVExKM7:TR?= MonaSG1UVw>? MXHFR|UxRTF3MjDuUS=> NITVRpQyQTB4NEezNC=>
SEM NWnSeJRXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYixNEDPxE1? MX;EUXNQ NXTxXo1FTUN3ME2yNFIhdk1? NWjhdZZ6OTlyNkS3N|A>
KASUMI-2 NXrMZm1ST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH7GcnUyOCEQvF2= Mn;OSG1UVw>? NGTl[mJGSzVyPUKyOUBvVQ>? MlHkNVkxPjR5M{C=
REH MlzLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHrpTY4yOCEQvF2= NVX3e4NMTE2VTx?= MY\FR|UxRTJ6ODDuUS=> MXqxPVA3PDd|MB?=
697 NH7nUJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFn2[nUyOCEQvF2= Ml7WSG1UVw>? MYPFR|UxRTN|ODDuUS=> NGnZTowyQTB4NEezNC=>
NALM-6 M2HwXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1ryXVExKM7:TR?= Mo\zSG1UVw>? M1LPOWVEPTB;NEKxJI5O NIT1WI4yQTB4NEezNC=>
MHH-CALL–3 M1rt[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoXhNVAh|ryP M4jDNmROW09? NVjQXW5TTUN3ME24NVIhdk1? MUWxPVA3PDd|MB?=
MHH-CALL–2 NXy3V4VwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEHBeJQyOCEQvF2= NHvacllFVVOR NFTIdIVGSzVyPUKxNVQhdk1? NWHTVHc3OTlyNkS3N|A>
J.GAMMA-1 M1jmWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NETNZnMyOCEQvF2= M3vwcmROW09? NUT5UIJ4TUN3ME22OUBvVQ>? NWLGb5RzOTlyNkS3N|A>
JR45.01 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIrQ[IIyOCEQvF2= MnvBSG1UVw>? NUPWOm9GTUN3ME22PEBvVQ>? NF\aT5AyQTB4NEezNC=>
A3 M175UGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGPGRYkyOCEQvF2= MlXsSG1UVw>? MXjFR|UxRTZ7IH7N NY\3cnRNOTlyNkS3N|A>
I 2.1 M4DzUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4jHUFExKM7:TR?= NFL4[VBFVVOR M{DkdWVEPTB;N{Ogcm0> NI[3OIkyQTB4NEezNC=>
MOLT-3 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4HISVExKM7:TR?= NWjRdXhOTE2VTx?= NWD1WWtQTUN3ME23OEBvVQ>? MWOxPVA3PDd|MB?=
P116 NWPacIJ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3Hme|ExKM7:TR?= MorrSG1UVw>? NX\GRnl2TUN3ME23PEBvVQ>? MoX3NVkxPjR5M{C=
J.Cam1.6 M1HO[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUPqR2lDOTBizszN MV;EUXNQ NXXGPGJITUN3ME23PUBvVQ>? Ml7wNVkxPjR5M{C=
I 9.2 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXS5N2tPOTBizszN NFuxfJlFVVOR M1XhTmVEPTB;OECgcm0> Mkm0NVkxPjR5M{C=
LOUCY Ml7qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWmxNEDPxE1? MW\EUXNQ MofwSWM2OD1zMUegcm0> NH74[oYyQTB4NEezNC=>
J.RT3-T3.5 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYWxNEDPxE1? NEDPcY1FVVOR M1HUXWVEPTB;MUKzJI5O MVyxPVA3PDd|MB?=
800000 M2rHVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHHqWmIyOCEQvF2= NITQWmpFVVOR MorKSWM2OD1zNkOgcm0> NFryd3QyQTB4NEezNC=>
Jurkat NWr5b215T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnHWNVAh|ryP MW\EUXNQ NWTLdmF3TUN3ME2yNlUhdk1? NEHaO2wyQTB4NEezNC=>
MOLT-4 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NY\hcY5POTBizszN M1zCUmROW09? NVi5[JpWTUN3ME2yN|Ihdk1? MmrCNVkxPjR5M{C=
Molt-16 NGqyT|NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{jSdFExKM7:TR?= MkLFSG1UVw>? MULFR|UxRTJ2MTDuUS=> MVuxPVA3PDd|MB?=
CEM/C3 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1Pkd|ExKM7:TR?= NIXmc4lFVVOR M{LacWVEPTB;MkW3JI5O MnT3NVkxPjR5M{C=
CEM/C2 M2fCb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnnJNVAh|ryP MnjrSG1UVw>? NWTFZ3d[TUN3ME2yO|Ehdk1? MX:xPVA3PDd|MB?=
CCRFCEM MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mmf6NVAh|ryP NF;TdZJFVVOR NF;6OY5GSzVyPUOyO{BvVQ>? MXyxPVA3PDd|MB?=
CEM/C1 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGPzdXUyOCEQvF2= NV2zfZBKTE2VTx?= MWrFR|UxRTN6MjDuUS=> M4TmdFE6ODZ2N{Ow
SUPTI[VB] M1[wbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlGzNVAh|ryP MXjEUXNQ MX7FR|UxRTZzOTDuUS=> M2XHVFE6ODZ2N{Ow
CCRF–HSB-2 NEnte3ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPYb2EyOCEQvF2= MUTEUXNQ MlrhSWM2OD1{MUG3JI5O MXyxPVA3PDd|MB?=
I 2.1 NH[5UpJCeG:ydH;zbZMh[XO|YYm= M4r4clExKM7:TR?= NYjqOGY4TE2VTx?= M{W1W4lv\HWlZYOgZZBweHSxc3nz MVSxPVA3PDd|MB?=
I 9.2 M{Pk[GFxd3C2b4Ppd{Bie3OjeR?= M3fMWlExKM7:TR?= M2WyWWROW09? MmfWbY5lfWOnczDhdI9xfG:|aYO= MX2xPVA3PDd|MB?=
A3 NV;MRZVLSXCxcITvd4l{KGG|c3H5 NFz0NIkyOCEQvF2= NGXwVHJFVVOR NIr1WWJqdmS3Y3XzJIFxd3C2b4Ppdy=> M1vtfVE6ODZ2N{Ow
RD MlTVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV33XJdIOTBizszN NH25fXhKSzVyPkGwJO69VQ>? MkHVNlA4PDB4MkO=
Rh41 NESw[o5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFz2R5MyOCEQvF2= M{mwT2lEPTB;M{OuPEBvVQ>? MnqxNlA4PDB4MkO=
Rh18 Mn:5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUjlWHU{OTBizszN NWfUe5oxUUN3ME2zNFMhdk1? M3r3O|IxPzRyNkKz
Rh30 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVyxNEDPxE1? M3HtVGlEPTB;ND64NUDPxE1? M3nxPFIxPzRyNkKz
BT-12 MnHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFTHWJMyOCEQvF2= NXjHZVI2UUN3ME6xNEDPxE1? NGXEfGMzODd2ME[yNy=>
CHLA-266 NEHJdHdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUe1O3lzOTBizszN NHjNU4hKSzVyPUGuNlIh|ryP NHHoUpYzODd2ME[yNy=>
TC-71 NVjpOGJTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWS5ZlVxOTBizszN NEnvfG1KSzVyPUKuOVIh|ryP MUKyNFc1ODZ{Mx?=
CHLA-9 M4LzVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFe3N3MyOCEQvF2= MoHvTWM2OD13OUGgcm0> NF3TTXAzODd2ME[yNy=>
CHLA-10 NHPCTFVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnTJNVAh|ryP MoLQTWM2OD1zMEKgcm0> NU\ze5FROjB5NEC2NlM>
CHLA-258 Mlj4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVu0cnFOOTBizszN MornTWM2OD1zLkC1JO69VQ>? NHjCZmgzODd2ME[yNy=>
GBM2 NHnHSHhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mm[zNVAh|ryP NF;U[|VKSzVyPUmuNVUh|ryP NHzBNGgzODd2ME[yNy=>
NB-1643 NFPsdVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXjvTGg6OTBizszN NHy4[2ZKSzVyPUWuOEDPxE1? NV2xVmNYOjB5NEC2NlM>
NB-Ebc1 NHnicXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MojENVAh|ryP M4XMPGlEPTB-MUCg{txO M4HYV|IxPzRyNkKz
CHLA-90 MmK0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorFNVAh|ryP NX[2R|dRUUN3ME6xNEDPxE1? M4PMblIxPzRyNkKz
CHLA-136 NIHlXnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmTHNVAh|ryP M4rHemlEPTB-MUCg{txO NI\iVZUzODd2ME[yNy=>
NALM-6 NVTTfYk3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVGxNEDPxE1? MX;JR|UxRTJ4NTDuUS=> M3nsdFIxPzRyNkKz
COG-LL-317 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWSxNEDPxE1? NXzV[2Y5UUN3ME22MlQ6KG6P MmPMNlA4PDB4MkO=
RS4;11 NX\lXHk1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUixNEDPxE1? MVnJR|UxRTF2NzDuUS=> M3nhc|IxPzRyNkKz
MOLT-4 NHHi[4dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NY\INo4xOTBizszN M3nrW2lEPTB;NECgcm0> M2HqRVIxPzRyNkKz
CCRF-CEM NYX4b2NrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnH5NVAh|ryP M3\2WmlEPTB;Mk[4JI5O NW\JbnBKOjB5NEC2NlM>
Kasumi-1 MnP1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NU\pc25rOTBizszN NVn0Vox1UUN3ME2xNFchdk1? MVeyNFc1ODZ{Mx?=
Karpas-299 NYOybm9nT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYCxNEDPxE1? NFuwTVNKSzVyPUKuPVMh|ryP NVH0XlVMOjB5NEC2NlM>
Ramos-RA1 Mn3kS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHXFN3QyOCEQvF2= NUT3ZZFXUUN3ME23MlM2KM7:TR?= MViyNFc1ODZ{Mx?=
H1299 MUjLbY5ie2ViYYPzZZk> NH:wfnoyOCEQvF2= Ml20bY5pcWKrdIOgTWtDU0VvaX7keYNm\CCDa4SgRYN1cX[jdHnvci=> M3HPSVIyQTB6NkG2

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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
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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
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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
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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

Bio Calculators

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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 Company, Limited January 2014 Phase 3
NCT01892527 Active, not recruiting Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro, MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT01861301 Terminated Epithelioid Mesothelioma|Recurrent Malignant Mesothelioma|Sarcomatoid Mesothelioma|Stage II Pleural Mesothelioma|Stage III Pleural Mesothelioma|Stage IV Pleural Mesothelioma National Cancer Institute (NCI) January 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID