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.

Size Price Stock Quantity  
USD 110 In stock
USD 470 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 7 Publications

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 NGTSb4tMcW6jc3WgZZN{[Xl? MWj+NVAh|ryP MmTGbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MmDvNlA1QDRyMUi=
HT29 NFPhdmxMcW6jc3WgZZN{[Xl? NWjubFBlhjFyIN88US=> M1PqWIlvcGmkaYTzJIMuVWW2IIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUBkNU2ndDDzbYdv[WyrbnegdIF1cHejeYO= NWPPZmZwOjB2OESwNVg>
MDA-MB-231 MkX5T4lv[XOnIHHzd4F6 NHLkOpF,OTBizszN NWCxcm9ScW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> M3SzO|IxPDh2MEG4
NCI-H441 MXXLbY5ie2ViYYPzZZk> MXP+NVAh|ryP MmLrbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NF3JPYwzODR6NECxPC=>
SK-MEL-28 M323[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1K5[VM{KM7:TR?= Mme3TWM2OD5|MzFOwG0> MXWyNFQ5PDBzOB?=
NCI-H661 M{T6N2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXmzN{DPxE1? NVvjTVJwUUN3ME6zN{DPxE1? MmXDNlA1QDRyMUi=
NCI-H446 M1Pifmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGflTm0{OyEQvF2= NEnETFNKSzVyPUeg{txO NHi3bpczODR6NECxPC=>
MDA-MB-231 M4nlSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYOzN{DPxE1? NH\sfWNKSzVyPUCuOVUh|ryP MVOyNFQ5PDBzOB?=
DLD-1 M36wR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX6zN{DPxE1? M1OyTWlEPTB;MD61N{DPxE1? MonuNlA1QDRyMUi=
A549 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlzuN|Mh|ryP Mn7VTWM2OD1yLkW5JO69VQ>? MkPvNlA1QDRyMUi=
SK-OV-3 NVzqcJF2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVn2eGRnOzNizszN NHzNSWZKSzVyPUCuOlYh|ryP MlLINlA1QDRyMUi=
NCI-H460 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmPSN|Mh|ryP M3PNTGlEPTB;MD62JO69VQ>? MXGyNFQ5PDBzOB?=
A375 MknWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1raOFM{KM7:TR?= M2GzVGlEPTB;MD60NkDPxE1? M36xZVIxPDh2MEG4
NCI-H441 M3HQWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M13heVM{KM7:TR?= MmfJTWM2OD1yLkOg{txO NV7LRZVlOjB2OESwNVg>
HT29 NFK1OmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkPRN|Mh|ryP Mnf6TWM2OD1yLkS5JO69VQ>? MXeyNFQ5PDBzOB?=
MKN-45 NVK1S3JtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUWzN{DPxE1? NX\2[o9YUUN3ME2wMlU5KM7:TR?= M3[ybVIxPDh2MEG4
HT29 MUHBdI9xfG:|aYOgZZN{[Xl? MY\+NVAh|ryP NUjzT5V4e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3OrczDifUA5OC17MDWu NFuwRYYzODR6NECxPC=>
MKN-45 NVHjdW5GSXCxcITvd4l{KGG|c3H5 M2riUJ4yOCEQvF2= MnXwd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NV:yXnI4OjB2OESwNVg>
MDA-MB-231 MnXvRZBweHSxc3nzJIF{e2G7 MV;+NVAh|ryP MWntc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw MXWyNFQ5PDBzOB?=
MDA-MB-231/TGL MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYTXeIozhjFyMDFOwG0> NVXGcHdJT0l3ME2xMlIh|ryP NYm2UJM3OjJyMke2PVA>
1833/TGL NF3JTFJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWXuV4J2hjFyMDFOwG0> MnL2S2k2OD1|Lkeg{txO NWPGRpBDOjJyMke2PVA>
EBC1 NIT2e2tEgXSxdH;4bYPDqGG|c3H5 M3y1fp4yOCEQvF2= NVfSVpVYcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> NGrlSWozOzV7OEK3Oi=>
SNU638 NFm5NmdEgXSxdH;4bYPDqGG|c3H5 M1;JXJ4yOCEQvF2= NEW2UXlqdmirYnn0d{B1cGViY3XscEBoem:5dHiu MXeyN|U6QDJ5Nh?=
A549 NGK5c4tEgXSxdH;4bYPDqGG|c3H5 M{eyUZ4yOCEQvF2= NVf1cFhodm:2IHHm[oVkfA>? MWGyN|U6QDJ5Nh?=
H460 NYDSW4E3S3m2b4TvfIlkyqCjc4PhfS=> M1zRW54yOCEQvF2= NVvTUGlCdm:2IHHm[oVkfA>? M17kVFI{PTl6Mke2
HCC827 MmfrR5l1d3SxeHnjxsBie3OjeR?= NGPsTXZ,OTBizszN Mn\uco91KGGoZnXjeC=> NV65SXF1OjN3OUiyO|Y>
A549 NETUeWVHfW6ldHnvckBie3OjeR?= NY\FS2dNOTBizszN MUHkbZNzfXC2czDtbYNzd3S3YoXs[S=> MlrhNlM2QTh{N{[=
EBC1 MVrGeY5kfGmxbjDhd5NigQ>? MX:xNEDPxE1? NET4UG9lcXO{dYD0d{BucWO{b4T1ZpVt\Q>? NIXzdoIzOzV7OEK3Oi=>
H460 NGTlPGZHfW6ldHnvckBie3OjeR?= MnLBNVAh|ryP MWDpcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v MmTuNlU{OTNyMUC=
K562/VCR NWmwd5JpS3m2b4TvfIlkyqCjc4PhfS=> MW\+NVAh|ryP NH\5SGh{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= MUSyOVMyOzBzMB?=
CEM/VBL NGfhUHpEgXSxdH;4bYPDqGG|c3H5 M4q3V54yOCEQvF2= MXXzbI94eyCleYTveI95cWNiYXP0bZZqfHl? MkXWNlU{OTNyMUC=
U266 MVnDfZRwfG:6aXRCpIF{e2G7 MXr+N{DPxE4EoB?= NY\EU25UUUN3ME2xMlEh|ryP MWGyOVgyODBzMx?=
OPM-2 NHzzfHREgXSxdH;4bYPDqGG|c3H5 MXf+N{DPxE4EoB?= MWPJR|UxRTFwODFOwG0> MXmyOVgyODBzMx?=
MM.1S MnX6R5l1d3SxeHnjxsBie3OjeR?= MojTglMh|ryPwrC= NUHOOlNQUUN3ME2xMlYh|ryP NXfhRogyOjV6MUCwNVM>
MM.1R MkfSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWqzJO69VcLi MmPWbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNEml NFTGblIzPThzMECxNy=>
RPMI-8226 MnLwR5l1d3SxeHnjxsBie3OjeR?= NGj6T2t,OyEQvF5CpC=> NUKxe5Q2UUN3ME2wMlkh|ryP MWOyOVgyODBzMx?=
ANBL-6 M2XTTmN6fG:2b4jpZ:Kh[XO|YYm= MUixJO69VcLi MXTpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NGfVUnIzPThzMECxNy=>
ANLB-6/V10R M4DpVGN6fG:2b4jpZ:Kh[XO|YYm= NGfkOHQyKM7:TdMg M4Xrfolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NXS3[GpuOjV6MUCwNVM>
KAS-6/1 NG[0fIdEgXSxdH;4bYPDqGG|c3H5 MYCxJO69VcLi MXvpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= M3\PbFI2QDFyMEGz
KAS-6/V10R NVfCe3R6S3m2b4TvfIlkyqCjc4PhfS=> NHvk[nEyKM7:TdMg M1rrOYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MUiyOVgyODBzMx?=
KAS-6/R10R NYi1[25jS3m2b4TvfIlkyqCjc4PhfS=> MXWxJO69VcLi NUDBUJJVcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> MUCyOVgyODBzMx?=
8226/S Mlv5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnfqN{DPxE4EoB?= MoXrbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl MkDPNlU5OTByMUO=
8226/LR-5 NV\BRmo3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HGVlMh|ryPwrC= M4T5XIlvcGmkaYTzJINmdGxiZ4Lve5RpKGK7IEW0KS=> MnTYNlU5OTByMUO=
Huh7 NXHEO2EyS3m2b4TvfIlkyqCjc4PhfS=> NFT2b|h,PC56IN88UeKh M1nTcWROW09? NFq0TYdKSzVyPUmuPUBvVQ>? M{DPOVI3OjV7MkWw
Hep3B NGj6XYNEgXSxdH;4bYPDqGG|c3H5 NG\QNXh,PC56IN88UeKh M{fWe2ROW09? M{HzNWlEPTB;NES4Mlchdk1? MlrjNlYzPTl{NUC=
HepG2 NHrLTFZEgXSxdH;4bYPDqGG|c3H5 MmHRglQvQCEQvF5CpC=> MVfEUXNQ MUPJR|UxRTF|OT63O{BvVQ>? M2XmblI3OjV7MkWw
Chang M1PWRmN6fG:2b4jpZ:Kh[XO|YYm= NH3pNWZ,PC56IN88UeKh Mk\XSG1UVw>? NUDNV4l2UUN3ME20OFgvPyCwTR?= MoD0NlYzPTl{NUC=
Huh7 M37YWGZ2dmO2aX;uJIF{e2G7 M1jzUVEvPiEQvF5CpC=> M4jGbmROW09? NGHxTGdk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MofFNlYzPTl{NUC=
Hep3B NWXQdJlWTnWwY4Tpc44h[XO|YYm= NFTyelgyNjZizszNxsA> NW\JfnB3TE2VTx?= NYrj[npG[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= Mn\wNlYzPTl{NUC=
HepG2 MYDGeY5kfGmxbjDhd5NigQ>? MYOxMlYh|ryPwrC= MX;EUXNQ NGrlWVZk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 NYDNO3I3OjZ{NUmyOVA>
Chang NFjGUXJHfW6ldHnvckBie3OjeR?= MlfZNU43KM7:TdMg NEH5[oxFVVOR NFn6[ppk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 MmrGNlYzPTl{NUC=
MHCC97L MoLYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHOzbG1,OTBizszN NETLTlBFVVOR NG\5eHVKSzVyPUOxOUBvVQ>? M{\hOFI3PDV6OUWz
MHCC97H MmfSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH[0S5R,OTBizszN MX\EUXNQ NInyOFBKSzVyPUO2PQKBkSCwTR?= NYTK[JNxOjZ2NUi5OVM>
Huh7 NEn1[HZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlrXglExKM7:TR?= MWrEUXNQ MoizTWM2OD1{NkWgcm0> MWKyOlQ2QDl3Mx?=
HepG2 NH7H[IhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkTwglExKM7:TR?= NH3iZ2lFVVOR Ml;jTWM2OD1|OUKgcm0> MVOyOlQ2QDl3Mx?=
MHCC97L M3y5NmZ2dmO2aX;uJIF{e2G7 NV3PZZdGOSEQvF5CpC=> M13oXWROW09? NX75UJZ3cW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NGe3PHUzPjR3OEm1Ny=>
Huh7 NIfuVHVHfW6ldHnvckBie3OjeR?= MmrkNUDPxE4EoB?= MlTISG1UVw>? Mn7xbY5lfWOnczDtbYNzd3S3YoXs[ZMh\GWyb3z5cYVzcXqjdHnvci=> NFfjV5AzPjR3OEm1Ny=>
MHCC97L M4frS2Fxd3C2b4Ppd{Bie3OjeR?= M2XJNlEh|ryPwrC= NX:zZ2hRTE2VTx?= M3PFfYlv\HWlZYOgZZBweHSxc3nz NVr2c4NQOjZ2NUi5OVM>
Huh7 M3j6e2Fxd3C2b4Ppd{Bie3OjeR?= NHLNNmsyKM7:TdMg NXrpTXhFTE2VTx?= MlrGbY5lfWOnczDhdI9xfG:|aYO= MoH5NlY1PTh7NUO=
C3H 10T1/2 mouse fibroblasts M{H0dGtqdmG|ZTDhd5NigQ>? MUeyOUDPxE1? MlLBSG1UVw>? M{D1V5Jm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> MWWyNFU{PDN2NR?=
H23 M3XOXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3XiVVI2KM7:TR?= NInMdmZFVVOR NFvSN|Z{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M3jBO|IxPTN2M{S1
WM35 NFjhO4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWqxNEDPxE1? M3zmRmROW09? MV;zbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= Mo[yNlA2OzR|NEW=
NIH 3T3 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXxNVAh|ryP MkXCSG1UVw>? M1TNSYRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> MkjVNlA2OzR|NEW=
H838 M4izWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXmxNEDPxE1? MWPEUXNQ Mn;D[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 NHjZcHEzODV|NEO0OS=>
H1395 MlrES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{XTb|ExKM7:TR?= NEn1XXNFVVOR NEfF[ZNld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> MVOyNFU{PDN2NR?=
Quiescent S2 Ml3lT4lv[XOnIHHzd4F6 Mo\iN|Ah|ryP NYnkfGlQTE2VTx?= NVPmUFQ3[2:vcHzleIVtgSCjYoLv[4F1\XNiVGPBMYlv\HWlZXSgbJlx\XKjY3X0fYxifGmxbjDv[kBJO0t2bXWzJIhqe3SxbnXz MmPTNlE2OTh7MUW=
PC3 MX7BdI9xfG:|aYOgZZN{[Xl? Mn7HNlAh|ryP MUXEUXNQ NFTRUXpqdmS3Y3XzJIFxd3C2b4Ppdy=> NILEV3AzOTdyOUGzNC=>
Du145 NGrRU5NCeG:ydH;zbZMh[XO|YYm= M3fyWVIxKM7:TR?= NU\mUllZTE2VTx?= NGnET2FqdmS3Y3XzJIFxd3C2b4Ppdy=> NYXI[IVzOjF5MEmxN|A>
LNCaP MWfBdI9xfG:|aYOgZZN{[Xl? NEPZTI8zOCEQvF2= NFPiWmJFVVOR NIrQOYtqdmS3Y3XzJIFxd3C2b4Ppdy=> NFnIV4QzOTdyOUGzNC=>
LAPC-4 MnfURZBweHSxc3nzJIF{e2G7 NH35e20zOCEQvF2= NHvk[4xFVVOR M{\XWolv\HWlZYOgZZBweHSxc3nz NFXUVlgzOTdyOUGzNC=>
LNCaP Mn;4SpVv[3Srb36gZZN{[Xl? M2LSU|IxKM7:TR?= MoXqSG1UVw>? M1LQ[4Rm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? M1HyeVIyPzB7MUOw
LAPC-4 NWnnSHJ1TnWwY4Tpc44h[XO|YYm= MXSyNEDPxE1? NXnQR4oxTE2VTx?= MkHi[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MUWyNVcxQTF|MB?=
Kasumi-1 M3jROGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlvlglUxKM7:TR?= MXjEUXNQ NHvaWnBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NVHyWVc6OjN|OUC1N|Y>
SKNO-1 NFvWUXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{fTWp42OCEQvF2= NXfYRZY{TE2VTx?= NWLnbmdscW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHe5XWIzOzN7MEWzOi=>
Kasumi-1 M3XVUGtqdmG|ZTDhd5NigQ>? M3rXZZ4yOCEQvF2= NYnEWnFmTE2VTx?= NHm0ToVz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> M4HJZVI{OzlyNUO2
SKNO-1 MUTLbY5ie2ViYYPzZZk> MXn+NVAh|ryP NELmOmNFVVOR NIDkS4Vz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiYXPleJlt[XSnZDDobZN1d26nIFizMOKh[y2taYVCpIFv\MLiYnPsMVI> NFiyU5IzOzN7MEWzOi=>
A549 NWDiS2dZTnWwY4Tpc44h[XO|YYm= NV76VIc1OTBizszN NVLsU442TE2VTx?= MX;lcohidmOnczDtbZRwfGmlIHPheIF{fHKxcHjl NWn0NJRSOjR5NE[1O|Q>
NRK-52E NYXa[pVVTnWwY4Tpc44h[XO|YYm= M2XlVFExKM7:TR?= NYf3UW4{TE2VTx?= MUPpcohq[mm2czDBcochUUlvaX7keYNm\CCVVFHUN{BvfWOuZXHyJJRz[W6|bH;jZZRqd25iYX7kJJRp\SCneIDy[ZN{cW:wIH;mJHRITi4QskGsJINwdGyjZ3XuJGlXKGGwZDDmbYJzd26nY4Tpci=> M{DvOlI2ODh6MECy
PC12 NYO1V3hqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYTqOWhrhjF{LkWg{txO Mn3uSG1UVw>? NUDCVXN7eHKndnXueJMhXFODLXnu[JVk\WRibnX1dol1\SCob4LtZZRqd25? MlLwNlUyOjh|OE[=
HPMCs NGrwXJpHfW6ldHnvckBie3OjeR?= M1rKcZJmfmW{c3XzJIVxcXSqZXzpZYwhfG9ibXXz[Y5kcHmvYXygeJJidnOrdHnvckBw\iCqdX3hckBx\XKrdH;u[YFtKG2nc3;0bIVtcWGuIHPlcIx{ MVOyOlA1PTd6MB?=
A549 M1jY[GZ2dmO2aX;uJIF{e2G7 NX3MeXB7hjVyIN88US=> NHW4O5lFVVOR NI\SVHZi\m[nY4TzJJRp\SC4aYLhcEBtcW[nIHP5Z4xmKGGwZDDoc5N1KHKnc4DvcpNm M1m5TFI3PzFzN{S4
RAW264.7 NEnaU2xHfW6ldHnvckBie3OjeR?= MWn+N|Ah|ryP MkDiSG1UVw>? MorXdoVlfWOnczDwdo8ucW6obHHtcYF1d3K7IHflcoUh\XiycnXzd4lwdg>? MY[yOlcyQDV6Nh?=
MEMM MlH1T4lv[XOnIHHzd4F6 Mk\SNVUhyrWP MojESG1UVw>? MYPk[YNz\WG|ZYOgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SCKMx?= MXKyOlkzOTVyNh?=
MEMM MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NW\ZWnRshjJyINM1US=> Ml;JSG1UVw>? M1\CXIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NXPJRXB5OjZ7MkG1NFY>
MEMM MkfURZBweHSxc3nzJIF{e2G7 MnTLNVUhyrWP M4HYO2ROW09? NYrl[5JGcW6mdXPld{B1cGVicILld4Vv[2Vib3[geIhmKGGyb4D0c5NqeyCycn;0[YlvNCClbHXheoVlKEOjc4Dhd4UuOw>? NHLHdlEzPjl{MUWwOi=>
T47D NXv0ZoZQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4H0W|ExKM7:TR?= NE\LU4pFVVOR M1LwSWlEPTB;N{Kgcm0> MUSxPFM5OTR2NB?=
ZR-75-1 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlnHNVAh|ryP MlfYSG1UVw>? MXvJR|UxRTd7IH7N M2G1UlE5OzhzNES0
BT474 M4DKXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnPrNVAh|ryP NVH5Z2c4TE2VTx?= M1jxUmlEPTB;OE[gcm0> NYfyVIFnOTh|OEG0OFQ>
HCC1954 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M13h[lExKM7:TR?= NUDHPYNSTE2VTx?= NIHtbIFKSzVyPUGxPUBvVQ>? NUi5NYplOTh|OEG0OFQ>
MDA-MB-453 NUS1fZhVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGDzSIMyOCEQvF2= MmjqSG1UVw>? MoDuTWM2OD17N{Wgcm0> M{PNVlE5OzhzNES0
MDA-MB-468 NGiweoFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYn5XHV6OTBizszN M3HG[mROW09? MljLTWM2OD1|MkC4JI5O M2K3bFE5OzhzNES0
SkBr3 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYnnS3luOTBizszN MXTEUXNQ MYrJR|UxRjFyLECwNEBvVQ>? NF;ae4QyQDN6MUS0OC=>
MDA-MB-231 NHL1T5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVKxNEDPxE1? MVfEUXNQ NUjwcHkzUUN3ME6xNEwxODBibl2= MmPhNVg{QDF2NES=
HCT116 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2q2cVExKM7:TR?= MmLxSG1UVw>? M2CyWmlEPTB;NUizOkBvVQ>? MnzuNVg{QDF2NES=
HT29 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkfONVAh|ryP NIPrR5ZFVVOR NIjDcGdKSzVyPkGwMFAxOCCwTR?= Mnu5NVg{QDF2NES=
HFF NHrKUG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWrI[HhiOTBizszN MYDEUXNQ NEDXT3RKSzVyPUe2NVUhdk1? MknBNVg{QDF2NES=
HN5 NXXUN49wT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoG2NVAh|ryP NGnZc|RFVVOR MnmyTWM2OD5zMDywNFAhdk1? NXXobIVjOTh|OEG0OFQ>
786-0 NXzS[VV[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVqxNEDPxE1? MWPEUXNQ M3HiemlEPTB;NECwPUBvVQ>? M4jiSFE5OzhzNES0
H157 NFf1WWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3TjVFExKM7:TR?= MULEUXNQ M1\4N2lEPTB;Mk[0NkBvVQ>? NY\Nb5k{OTh|OEG0OFQ>
NCI-H460 NUe5N3U3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2GydVExKM7:TR?= M1:xdGROW09? NWPWV2x5UUN3ME6yMFUxOCCwTR?= NU\ibYhsOTh|OEG0OFQ>
SKOV-3 M1rpTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFjROlMyOCEQvF2= NILMSZBFVVOR M3XiZmlEPTB;MkGyOkBvVQ>? NGG0bG0yQDN6MUS0OC=>
OVCAR-3 NYfDd29ZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2DBeFExKM7:TR?= MWTEUXNQ M3ewWWlEPTB;MkmxPEBvVQ>? Mor3NVg{QDF2NES=
BXPC3 NXOxN4M2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX\3dJdsOTBizszN MWLEUXNQ NVXZdHF6UUN3ME2zNVQyKG6P NYXnNIxKOTh|OEG0OFQ>
MiaPaCa M3HZeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NELvNFgyOCEQvF2= NUS2WFlETE2VTx?= M{PtTmlEPTB;NUSzN{BvVQ>? NUOydXBPOTh|OEG0OFQ>
PANC-1 M1uxVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUKxNEDPxE1? MnSwSG1UVw>? NYK4ToRSUUN3ME24OlgyKG6P MkPTNVg{QDF2NES=
LNCaP MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmS5NVAh|ryP MYrEUXNQ NXPtTItHUUN3ME2xOFchdk1? MYqxPFM5OTR2NB?=
DU145 NF3zXmpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVGxNEDPxE1? M4n1fWROW09? NY\ZVGhkUUN3ME2zPFEzKG6P NWP5bIx5OTh|OEG0OFQ>
PC3 Mke3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmK5NVAh|ryP MoPXSG1UVw>? NYizTFl1UUN3ME6xNEwxODBibl2= MVGxPFM5OTR2NB?=
BT474 NHuyRZhMcW6jc3WgZZN{[Xl? Ml7vNVAh|ryP NInZd5BFVVOR NVrBd4xOcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMU[wJI5O MmrWNVg{QDF2NES=
786-0 NGTOcZFMcW6jc3WgZZN{[Xl? Mo\DNVAh|ryP NX\ySmN{TE2VTx?= NUDUVmNscW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMUWwJI5O MX[xPFM5OTR2NB?=
LNCaP MVrLbY5ie2ViYYPzZZk> MV[xNEDPxE1? Mki4SG1UVw>? NUHWNoZ6cW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEOgcm0> M3rHSVE5OzhzNES0
PC3 NFH6N2JMcW6jc3WgZZN{[Xl? NHv2Z3gyOCEQvF2= MnPUSG1UVw>? NF;MTZpqdmirYnn0d{BxT1ONM98yJJdqfGhiSVO1NEBw\iB2OTDuUS=> M{XYclE5OzhzNES0
KARPAS-231 NX3meWYxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYCxNEDPxE1? NHnuTndFVVOR NEi5XmZGSzVyPUSxJI5O NUXqWo1NOTlyNkS3N|A>
CCRFSB M3nkOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4XaeVExKM7:TR?= NUPydGZmTE2VTx?= MUHFR|UxRTF3NTDuUS=> MmTUNVkxPjR5M{C=
SUP B15 NWjuU4E4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2L0[|ExKM7:TR?= M{G1PWROW09? MlfSSWM2OD1zOUegcm0> MXyxPVA3PDd|MB?=
SD-1 M3K2S2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEi4[GYyOCEQvF2= MoTISG1UVw>? NHLpTW1GSzVyPUOyNEBvVQ>? MnLpNVkxPjR5M{C=
RS4;11 NW\PNHF4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2f5W|ExKM7:TR?= NF;JXZNFVVOR NVq1WXE4TUN3ME22OVQhdk1? NIfp[5oyQTB4NEezNC=>
MN-60 NFW2eWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYmxNEDPxE1? MYjEUXNQ M{XBOGVEPTB;M{[wNkBvVQ>? M{\5NVE6ODZ2N{Ow
Tanoue NXzVbnh6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4r1SlExKM7:TR?= NGX2W3dFVVOR NXflO4lQTUN3ME20OVE4KG6P NHLBPJIyQTB4NEezNC=>
RCH-ACV MmHiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVO0R2RjOTBizszN NIDxPFZFVVOR M3HwZ2VEPTB;MUWyJI5O MnPsNVkxPjR5M{C=
SEM M2HF[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmnCNVAh|ryP NVOzfWhpTE2VTx?= NGDYZlNGSzVyPUKwNkBvVQ>? Ml3UNVkxPjR5M{C=
KASUMI-2 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF7CdYIyOCEQvF2= MlTLSG1UVw>? MkC3SWM2OD1{MkWgcm0> MWKxPVA3PDd|MB?=
REH NUnQRmVxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mmr4NVAh|ryP NI\XW3FFVVOR MYnFR|UxRTJ6ODDuUS=> M3z6NVE6ODZ2N{Ow
697 NX61TVhpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW[xNEDPxE1? MVTEUXNQ MYPFR|UxRTN|ODDuUS=> MXmxPVA3PDd|MB?=
NALM-6 M3LUUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlniNVAh|ryP NX7Fd2Z6TE2VTx?= MYTFR|UxRTR{MTDuUS=> NIf0R2IyQTB4NEezNC=>
MHH-CALL–3 M1rm[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{nRUlExKM7:TR?= MULEUXNQ Mnn6SWM2OD16MUKgcm0> MV:xPVA3PDd|MB?=
MHH-CALL–2 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoKzNVAh|ryP MknNSG1UVw>? NIrtfJZGSzVyPUKxNVQhdk1? MkfVNVkxPjR5M{C=
J.GAMMA-1 MkLqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{XkUFExKM7:TR?= MW\EUXNQ MV;FR|UxRTZ3IH7N NXfuV4duOTlyNkS3N|A>
JR45.01 NWPBWnQ6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXixNEDPxE1? M3;BSmROW09? MmnESWM2OD14ODDuUS=> M{f4OVE6ODZ2N{Ow
A3 NVj2OJBvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{jjU|ExKM7:TR?= MX7EUXNQ MXfFR|UxRTZ7IH7N NY\uOXROOTlyNkS3N|A>
I 2.1 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\mOlExKM7:TR?= MV\EUXNQ NXjkNok4TUN3ME23N{BvVQ>? NXPubZFvOTlyNkS3N|A>
MOLT-3 NHfORZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3zpO|ExKM7:TR?= M{LrW2ROW09? MnL6SWM2OD15NDDuUS=> MkTpNVkxPjR5M{C=
P116 NWXJboM6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml:zNVAh|ryP M3\5VGROW09? M{PaO2VEPTB;N{igcm0> NGfQUpoyQTB4NEezNC=>
J.Cam1.6 M{TBPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmDXNVAh|ryP M1y2emROW09? MXjFR|UxRTd7IH7N NFq2O2MyQTB4NEezNC=>
I 9.2 NWfQO3I4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2HRNVExKM7:TR?= MYLEUXNQ NEDBNJNGSzVyPUiwJI5O NHjJPG4yQTB4NEezNC=>
LOUCY NYTVblJ6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV6xNEDPxE1? M2LZNGROW09? MVjFR|UxRTFzNzDuUS=> MmrnNVkxPjR5M{C=
J.RT3-T3.5 NGDFfVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NULnW2p4OTBizszN M1;tfmROW09? M1SwW2VEPTB;MUKzJI5O M3L0TVE6ODZ2N{Ow
800000 NEDmV45Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jE[FExKM7:TR?= MkfuSG1UVw>? NHXye|JGSzVyPUG2N{BvVQ>? MYqxPVA3PDd|MB?=
Jurkat MlrlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUT2fZNKOTBizszN NUi4c|lWTE2VTx?= NEj4ZnVGSzVyPUKyOUBvVQ>? MmC5NVkxPjR5M{C=
MOLT-4 NV63fZBXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW[xNEDPxE1? Mn[2SG1UVw>? NXrXToxXTUN3ME2yN|Ihdk1? NXPxfHZZOTlyNkS3N|A>
Molt-16 MoDpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoPqNVAh|ryP MX\EUXNQ MYfFR|UxRTJ2MTDuUS=> M2ryeVE6ODZ2N{Ow
CEM/C3 NG\kXZZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlLrNVAh|ryP NWn4OWlpTE2VTx?= MVXFR|UxRTJ3NzDuUS=> M2W5c|E6ODZ2N{Ow
CEM/C2 M3TKc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGS4dmkyOCEQvF2= NXTKTGxRTE2VTx?= NFTE[otGSzVyPUK3NUBvVQ>? NFfyfXkyQTB4NEezNC=>
CCRFCEM MojWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX[xNEDPxE1? NV\UZWk{TE2VTx?= MlrESWM2OD1|Mkegcm0> M1fLZVE6ODZ2N{Ow
CEM/C1 MmfJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVmxNEDPxE1? M{S1fGROW09? M4f3[mVEPTB;M{iyJI5O NUjue|A1OTlyNkS3N|A>
SUPTI[VB] Ml7RS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1S5PVExKM7:TR?= NUHZVFUxTE2VTx?= NEP0OZJGSzVyPU[xPUBvVQ>? MUGxPVA3PDd|MB?=
CCRF–HSB-2 M1:1dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4Hx[VExKM7:TR?= MVzEUXNQ M37oUGVEPTB;MkGxO{BvVQ>? MkPwNVkxPjR5M{C=
I 2.1 MWTBdI9xfG:|aYOgZZN{[Xl? NH2zOVUyOCEQvF2= MojUSG1UVw>? M3fPc4lv\HWlZYOgZZBweHSxc3nz M2q0WlE6ODZ2N{Ow
I 9.2 NEnFcZBCeG:ydH;zbZMh[XO|YYm= M1LZUlExKM7:TR?= M2L1d2ROW09? NIH2U4tqdmS3Y3XzJIFxd3C2b4Ppdy=> M2jWeVE6ODZ2N{Ow
A3 MY\BdI9xfG:|aYOgZZN{[Xl? MYmxNEDPxE1? MYTEUXNQ MmDDbY5lfWOnczDhdI9xfG:|aYO= MWqxPVA3PDd|MB?=
RD NVnsSW5HT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFzRUHIyOCEQvF2= MWjJR|UxRjFyIN88US=> NWKyVHZNOjB5NEC2NlM>
Rh41 Mn\oS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvkZ3oyOCEQvF2= MUDJR|UxRTN|Lkigcm0> M{G2V|IxPzRyNkKz
Rh18 NH3sS3BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4TT[|ExKM7:TR?= MWDJR|UxRTNyMzDuUS=> M4jBU|IxPzRyNkKz
Rh30 NILNXmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MU[xNEDPxE1? MVvJR|UxRTRwOEGg{txO NHP1V2czODd2ME[yNy=>
BT-12 NHTxZVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFToPFcyOCEQvF2= NFfYOldKSzVyPkGwJO69VQ>? M2\NeVIxPzRyNkKz
CHLA-266 M1\1bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M161VFExKM7:TR?= M1XrdGlEPTB;MT6yNkDPxE1? NVvweYVmOjB5NEC2NlM>
TC-71 MmTrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXexNEDPxE1? M{XBZmlEPTB;Mj61NkDPxE1? NFO0c3YzODd2ME[yNy=>
CHLA-9 M1yweWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLiNVAh|ryP Ml[wTWM2OD13OUGgcm0> NXPRPJM2OjB5NEC2NlM>
CHLA-10 M3HoR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV2xNEDPxE1? Mni4TWM2OD1zMEKgcm0> MkXGNlA4PDB4MkO=
CHLA-258 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn7WNVAh|ryP MVjJR|UxRTFwMEWg{txO NEXqVI0zODd2ME[yNy=>
GBM2 NVXsbXFMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mk\aNVAh|ryP MULJR|UxRTlwMUWg{txO NVHxR2IyOjB5NEC2NlM>
NB-1643 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{i1bVExKM7:TR?= MULJR|UxRTVwNDFOwG0> M2PxblIxPzRyNkKz
NB-Ebc1 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIP2WmoyOCEQvF2= NVjBW25xUUN3ME6xNEDPxE1? NWnKSGdxOjB5NEC2NlM>
CHLA-90 NXG3UZZsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M33FRlExKM7:TR?= MVjJR|UxRjFyIN88US=> M2XaO|IxPzRyNkKz
CHLA-136 MnHyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnrnNVAh|ryP NVfIWZRUUUN3ME6xNEDPxE1? NYLQZpEyOjB5NEC2NlM>
NALM-6 MoPpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWjySVkxOTBizszN NI[3NpRKSzVyPUK2OUBvVQ>? M3PsUFIxPzRyNkKz
COG-LL-317 M1jIRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGK4RZgyOCEQvF2= MYDJR|UxRTZwNEmgcm0> NFPMdIozODd2ME[yNy=>
RS4;11 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUOxNEDPxE1? MmHWTWM2OD1zNEegcm0> MnHvNlA4PDB4MkO=
MOLT-4 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEf2XGgyOCEQvF2= NWLqW4tzUUN3ME20NEBvVQ>? MXqyNFc1ODZ{Mx?=
CCRF-CEM M37uUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{HJNlExKM7:TR?= MojxTWM2OD1{Nkigcm0> MoC1NlA4PDB4MkO=
Kasumi-1 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{P2elExKM7:TR?= M{\PSmlEPTB;MUC3JI5O Mm\LNlA4PDB4MkO=
Karpas-299 M2P5[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnG1NVAh|ryP M1f0bWlEPTB;Mj65N{DPxE1? M1vhRVIxPzRyNkKz
Ramos-RA1 NY[yN4RST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUOxNEDPxE1? NYj4UmVvUUN3ME23MlM2KM7:TR?= NY\qT4xHOjB5NEC2NlM>
H1299 MYTLbY5ie2ViYYPzZZk> M4j6[lExKM7:TR?= NYHLUIRmcW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? MX6yNVkxQDZzNh?=

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02150733 Completed Drug: Tivantinib Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace Inc. April 2014 Phase 1
NCT01892527 Unknown status Drug: Tivantinib (ARQ197) Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Unknown status Drug: Tivantinib 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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

  • Answer:

    S2753 Tivantinib (ARQ 197) can be dissolved in 1% methylcellulose at15 mg/ml as a suspension.

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

Related c-Met Products

Tags: buy Tivantinib (ARQ 197) | Tivantinib (ARQ 197) supplier | purchase Tivantinib (ARQ 197) | Tivantinib (ARQ 197) cost | Tivantinib (ARQ 197) manufacturer | order Tivantinib (ARQ 197) | Tivantinib (ARQ 197) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID