Tivantinib (ARQ 197)

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

価格 在庫  
USD 138 あり
USD 592 あり

Tivantinib (ARQ 197) 化学構造
分子量: 369.42

高品質保証

カスタマーフィードバック(1)

MSDS

製品説明

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

製品の説明

生物活性

製品説明 Tivantinib (ARQ 197)は初めの非ATP競争性的なc-Met阻害剤で、無細胞実験でKi値が0.355 μMです。Tivantinib (ARQ 197)はRonに作用する活性が殆どなくて、EGFR、InsR、PDGFRαとFGFR1/4を抑制する作用がありません。臨床3期。
ターゲット c-Met
IC50 0.355 μM (Ki) [1]
In vitro試験 ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549, DBTRG and NCI-H441 cells with IC50 of 0.38, 0.45, 0.29 μM. Treatment with ARQ-197 results in a decrease in phosphorylation of the MAPK signaling cascade and prevention of invasion and migration. In addition, ectopic expression of c-Met in NCI-H661, a cell line having no endogenous expression of c-Met, causes it to acquire an invasive phenotype that is also suppressed by ARQ-197. Although the addition of increasing concentrations of ARQ-197 does not significantly affect the Km of ATP, exposure of c-Met to 0.5 μM ARQ-197 decreased the Vmax of c-Met by approximately 3-fold. The ability of ARQ-197 to decrease the Vmax without affecting the Km of ATP confirmed that ARQ-197 inhibits c-Met through a non–ATP-competitive mechanism and may therefore account for its high degree of kinase selectivity. ARQ-197 prevents human recombinant c-Met with a calculated inhibitory constant Ki of approximately 355 nM. Although the highest concentration of ATP used is 200 μM, the potency of ARQ-197 against c-Met is not reduced by using concentrations of ATP up to 1 mM. ARQ-197 blocks c-Met phosphorylation and downstream c-Met signaling pathways. ARQ-197 suppresses constitutive and ligand-mediated c-Met autophosphorylation and, by extension, c-Met activity, in turn leading to the inhibition of downstream c-Met effectors. ARQ-197 induction of caspase-dependent apoptosis is increased in c-Met–expressing human cancer cells including HT29, MKN-45, and MDA-MB-231 cells.[1][2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MNK-45 NXTQUWpZU2mwYYPlJIF{e2G7 Mlm1glExKM7:TR?= MnnMbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NEnNTGYzODR6NECxPC=>
HT29 NGfvVo5McW6jc3WgZZN{[Xl? M4XLeZ4yOCEQvF2= NWHJ[|c1cW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MkfSNlA1QDRyMUi=
MDA-MB-231 NFHMbGtMcW6jc3WgZZN{[Xl? MkTYglExKM7:TR?= MVjpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| M{\uXFIxPDh2MEG4
NCI-H441 MmKzT4lv[XOnIHHzd4F6 MYX+NVAh|ryP MofhbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NY[wVFVqOjB2OESwNVg>
SK-MEL-28 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYGzN{DPxE1? NWnoW5FlUUN3ME6zN{DPxE1? MkfBNlA1QDRyMUi=
NCI-H661 NHzi[21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV[zN{DPxE1? M4jQVWlEPTB-M{Og{txO M4nOXlIxPDh2MEG4
NCI-H446 NYT6Xnk5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXWzN{DPxE1? NHPWSYlKSzVyPUeg{txO MmjMNlA1QDRyMUi=
MDA-MB-231 M3\wfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MonhN|Mh|ryP MUnJR|UxRTBwNUWg{txO NFThWoYzODR6NECxPC=>
DLD-1 M1O4TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3jm[lM{KM7:TR?= MkHaTWM2OD1yLkWzJO69VQ>? MYGyNFQ5PDBzOB?=
A549 NHrNN2FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVizN{DPxE1? NUf2e5hiUUN3ME2wMlU6KM7:TR?= NIXv[VAzODR6NECxPC=>
SK-OV-3 MkLOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\Ldmk{OyEQvF2= M4n2fGlEPTB;MD62OkDPxE1? Mon0NlA1QDRyMUi=
NCI-H460 NWLjPWZwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEXJNWc{OyEQvF2= M2fSV2lEPTB;MD62JO69VQ>? NIHXfZozODR6NECxPC=>
A375 NInxdFhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4Wwe|M{KM7:TR?= NV7aWnVWUUN3ME2wMlQzKM7:TR?= NU\PWVFQOjB2OESwNVg>
NCI-H441 NGrlboVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1LaRVM{KM7:TR?= NULNO|k3UUN3ME2wMlMh|ryP M3jnbVIxPDh2MEG4
HT29 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3HEOlM{KM7:TR?= NFv2[HlKSzVyPUCuOFkh|ryP Ml24NlA1QDRyMUi=
MKN-45 NFTYT4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHjsbI8{OyEQvF2= NU\XW2J6UUN3ME2wMlU5KM7:TR?= NUPOXWxZOjB2OESwNVg>
HT29 Mlv6RZBweHSxc3nzJIF{e2G7 MoTHglExKM7:TR?= MkH5d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NFy0PIUzODR6NECxPC=>
MKN-45 NH36fHVCeG:ydH;zbZMh[XO|YYm= NULRW5M3hjFyIN88US=> Mln5d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw MXmyNFQ5PDBzOB?=
MDA-MB-231 MYfBdI9xfG:|aYOgZZN{[Xl? MorNglExKM7:TR?= MXHtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw M1PjVVIxPDh2MEG4
MDA-MB-231/TGL MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVPkfY5ZhjFyMDFOwG0> MUDHTVUxRTFwMjFOwG0> M3TSXVIzODJ5Nkmw
1833/TGL NV\JZXZUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXT+NVAxKM7:TR?= MUjHTVUxRTNwNzFOwG0> NFfsWZozOjB{N{[5NC=>
EBC1 M2judmN6fG:2b4jpZ:Kh[XO|YYm= NVrUWpJLhjFyIN88US=> M{jQO4lvcGmkaYTzJJRp\SClZXzsJIdzd3e2aD6= NV\qb2NjOjN3OUiyO|Y>
SNU638 MlLRR5l1d3SxeHnjxsBie3OjeR?= M2fHSZ4yOCEQvF2= NV21[Gl{cW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> M1:wVlI{PTl6Mke2
A549 Mnf2R5l1d3SxeHnjxsBie3OjeR?= NGDs[VB,OTBizszN NELHOY5vd3RiYX\m[YN1 M4nBWVI{PTl6Mke2
H460 M4r0VGN6fG:2b4jpZ:Kh[XO|YYm= MkHqglExKM7:TR?= MkLQco91KGGoZnXjeC=> NGjRNJAzOzV7OEK3Oi=>
HCC827 NFHaO4VEgXSxdH;4bYPDqGG|c3H5 MV7+NVAh|ryP M{Pye45wfCCjZn\lZ5Q> MVmyN|U6QDJ5Nh?=
A549 NVrJTZhsTnWwY4Tpc44h[XO|YYm= MorsNVAh|ryP NHLiXJRlcXO{dYD0d{BucWO{b4T1ZpVt\Q>? NGfGd48zOzV7OEK3Oi=>
EBC1 MnjwSpVv[3Srb36gZZN{[Xl? NHTyRVYyOCEQvF2= NXv4N|Q4\Gm|coXweJMhdWmlcn;0eYJ2dGV? NFS4OmwzOzV7OEK3Oi=>
H460 MmjCSpVv[3Srb36gZZN{[Xl? M3TyeFExKM7:TR?= NWrWSIducW6qaXLpeJMhfHWkdXzpckBxd2y7bXXybZpifGmxbh?= NHHDUHYzPTNzM{CxNC=>
K562/VCR MYHDfZRwfG:6aXRCpIF{e2G7 MYn+NVAh|ryP M2[2Z5Npd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= NV3Bc2tnOjV|MUOwNVA>
CEM/VBL NWDmVIdGS3m2b4TvfIlkyqCjc4PhfS=> NWfveJc{hjFyIN88US=> MWjzbI94eyCleYTveI95cWNiYXP0bZZqfHl? M3:3d|I2OzF|MEGw
U266 NHv4VYJEgXSxdH;4bYPDqGG|c3H5 MUT+N{DPxE4EoB?= NFvCfHlKSzVyPUGuNUDPxE1? MlvzNlU5OTByMUO=
OPM-2 MoDFR5l1d3SxeHnjxsBie3OjeR?= Mn:0glMh|ryPwrC= NXqwdXI2UUN3ME2xMlgh|ryP MlnPNlU5OTByMUO=
MM.1S NVHHdFM6S3m2b4TvfIlkyqCjc4PhfS=> NXnKPIZ4hjNizszNxsA> NEPUc25KSzVyPUGuOkDPxE1? MlXQNlU5OTByMUO=
MM.1R NHK3UGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1[wPFMh|ryPwrC= NFHHUXRqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> MXSyOVgyODBzMx?=
RPMI-8226 M1TWPWN6fG:2b4jpZ:Kh[XO|YYm= MnKzglMh|ryPwrC= MX7JR|UxRTBwOTFOwG0> MlrRNlU5OTByMUO=
ANBL-6 NUjFSJRGS3m2b4TvfIlkyqCjc4PhfS=> MnrGNUDPxE4EoB?= M4HHSYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NYXEWJNbOjV6MUCwNVM>
ANLB-6/V10R M1\Be2N6fG:2b4jpZ:Kh[XO|YYm= M1TZd|Eh|ryPwrC= MXPpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= NXzuXIo3OjV6MUCwNVM>
KAS-6/1 NFS5XmZEgXSxdH;4bYPDqGG|c3H5 Mlm0NUDPxE4EoB?= M12yXYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl MViyOVgyODBzMx?=
KAS-6/V10R MoXCR5l1d3SxeHnjxsBie3OjeR?= NFHsNGYyKM7:TdMg M2nQeYlv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NFT3foMzPThzMECxNy=>
KAS-6/R10R NUTZN3pqS3m2b4TvfIlkyqCjc4PhfS=> M3PTW|Eh|ryPwrC= M2H2Wolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl NEnkfnczPThzMECxNy=>
8226/S MkPlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NG[1[mg{KM7:TdMg MoDxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[nliNUSl NGCzSHczPThzMECxNy=>
8226/LR-5 NGLXeHdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV2zJO69VcLi NVHmUFNRcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm NVn0Zm9SOjV6MUCwNVM>
Huh7 M2K1cGN6fG:2b4jpZ:Kh[XO|YYm= NUixeopuhjRwODFOwG3DqA>? MX;EUXNQ MkSyTWM2OD17Lkmgcm0> M3u0eVI3OjV7MkWw
Hep3B MoDNR5l1d3SxeHnjxsBie3OjeR?= NXjtXY9zhjRwODFOwG3DqA>? NHW0XGFFVVOR MWPJR|UxRTR2OD63JI5O MmTHNlYzPTl{NUC=
HepG2 Ml3aR5l1d3SxeHnjxsBie3OjeR?= M3[4T541NjhizszNxsA> M{D3PGROW09? M2jhOmlEPTB;MUO5Mlc4KG6P MVeyOlI2QTJ3MB?=
Chang NFPaemxEgXSxdH;4bYPDqGG|c3H5 NG\a[3F,PC56IN88UeKh NEHMeWVFVVOR NILNOFNKSzVyPUS0PE44KG6P NF3VOVEzPjJ3OUK1NC=>
Huh7 NFrsXWpHfW6ldHnvckBie3OjeR?= MkHPNU43KM7:TdMg MVTEUXNQ M4HoO4NifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? M3zMc|I3OjV7MkWw
Hep3B NFLoPVlHfW6ldHnvckBie3OjeR?= NF7K[IkyNjZizszNxsA> NXHsRW0{TE2VTx?= MonhZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? MYWyOlI2QTJ3MB?=
HepG2 M1f3bGZ2dmO2aX;uJIF{e2G7 MWSxMlYh|ryPwrC= MY\EUXNQ NV7XW4hL[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= NIPy[4UzPjJ3OUK1NC=>
Chang MlnjSpVv[3Srb36gZZN{[Xl? Mli2NU43KM7:TdMg NFvXPW9FVVOR MlHDZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M4\EdVI3OjV7MkWw
MHCC97L MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVf+NVAh|ryP M3rHeWROW09? NYfR[|FpUUN3ME2zNVUhdk1? MVyyOlQ2QDl3Mx?=
MHCC97H MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlTWglExKM7:TR?= M3r4VmROW09? NEXsUplKSzVyPUO2PQKBkSCwTR?= M3HFTVI3PDV6OUWz
Huh7 MnjxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXH+NVAh|ryP NFfSV2RFVVOR MYnJR|UxRTJ4NTDuUS=> M1\HTlI3PDV6OUWz
HepG2 NGrmTWNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoDPglExKM7:TR?= NH\QXGtFVVOR NGj4bIRKSzVyPUO5NkBvVQ>? NUHHSmZ7OjZ2NUi5OVM>
MHCC97L M4SxeGZ2dmO2aX;uJIF{e2G7 MkTENUDPxE4EoB?= NFrwWJVFVVOR MUjpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u M{HRN|I3PDV6OUWz
Huh7 M2jodmZ2dmO2aX;uJIF{e2G7 M{H6T|Eh|ryPwrC= M1TXSGROW09? M4ntPYlv\HWlZYOgcYlkem:2dXL1cIV{KGSncH;sfY1memm8YYTpc44> NHrrNIYzPjR3OEm1Ny=>
MHCC97L M1LCTGFxd3C2b4Ppd{Bie3OjeR?= NFvnUY4yKM7:TdMg NEjLZ25FVVOR Ml3abY5lfWOnczDhdI9xfG:|aYO= M1fnNlI3PDV6OUWz
Huh7 NHHuSVVCeG:ydH;zbZMh[XO|YYm= MUWxJO69VcLi M4\SVWROW09? MonxbY5lfWOnczDhdI9xfG:|aYO= MVSyOlQ2QDl3Mx?=
C3H 10T1/2 mouse fibroblasts NFX5N3lMcW6jc3WgZZN{[Xl? MWGyOUDPxE1? NXTXeGhkTE2VTx?= MnvpdoVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> MVOyNFU{PDN2NR?=
H23 NUHETnQ1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYWyOUDPxE1? NV35eXgyTE2VTx?= NWrnWW84e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NUTF[ZR6OjB3M{SzOFU>
WM35 Ml3QS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYTZVpVUOTBizszN Mk\GSG1UVw>? NH2wSIh{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M3i3RlIxPTN2M{S1
NIH 3T3 MnPXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3TkO|ExKM7:TR?= MkTUSG1UVw>? NETJSFVld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> NVHHUYo6OjB3M{SzOFU>
H838 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3zYfFExKM7:TR?= MXTEUXNQ Mnvt[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MlzvNlA2OzR|NEW=
H1395 M1vPSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVOxNEDPxE1? MoPrSG1UVw>? NV:0Omtj\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 M2jVUVIxPTN2M{S1
Quiescent S2 MYrLbY5ie2ViYYPzZZk> M2HzcFMxKM7:TR?= M4jYbGROW09? MYfjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? NVPaToNQOjF3MUi5NVU>
PC3 M1vKOGFxd3C2b4Ppd{Bie3OjeR?= MnXMNlAh|ryP MWTEUXNQ MkDFbY5lfWOnczDhdI9xfG:|aYO= MVWyNVcxQTF|MB?=
Du145 MXrBdI9xfG:|aYOgZZN{[Xl? MlzRNlAh|ryP MYLEUXNQ M3LxTolv\HWlZYOgZZBweHSxc3nz NELNTHkzOTdyOUGzNC=>
LNCaP MoD2RZBweHSxc3nzJIF{e2G7 Ml;kNlAh|ryP M4fNe2ROW09? M2KyWolv\HWlZYOgZZBweHSxc3nz MoPNNlE4ODlzM{C=
LAPC-4 NVe1c3B2SXCxcITvd4l{KGG|c3H5 NH7UboozOCEQvF2= NGDuVIVFVVOR MoPVbY5lfWOnczDhdI9xfG:|aYO= NIHjOGIzOTdyOUGzNC=>
LNCaP MnnQSpVv[3Srb36gZZN{[Xl? NUKy[XRUOjBizszN MX\EUXNQ M1PPcYRm[3KnYYPld{BRW0Fic3XjdoV1cW:wIHHu[EBxPjViZYjwdoV{e2mxbjDs[ZZmdHN? NGTFepEzOTdyOUGzNC=>
LAPC-4 NHTTfW9HfW6ldHnvckBie3OjeR?= MVuyNEDPxE1? NYPuUlZQTE2VTx?= MXvk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ NXPrVIo3OjF5MEmxN|A>
Kasumi-1 M3fEb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIXz[2J,PTBizszN NGjyWG1FVVOR M1jLeolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Mo[2NlM{QTB3M{[=
SKNO-1 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVj+OVAh|ryP MYnEUXNQ NH7hZmNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NUS0cZZmOjN|OUC1N|Y>
Kasumi-1 M3S4c2tqdmG|ZTDhd5NigQ>? MkjiglExKM7:TR?= MVXEUXNQ MXjy[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= MVeyN|M6ODV|Nh?=
SKNO-1 NE\EVZlMcW6jc3WgZZN{[Xl? MYX+NVAh|ryP NGjL[lNFVVOR MX7y[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= NYPKOZlvOjN|OUC1N|Y>
A549 NFX6colHfW6ldHnvckBie3OjeR?= NWfhW5FDOTBizszN MWLEUXNQ M3HYRoVvcGGwY3XzJI1qfG:2aXOgZ4F1[XO2cn;wbIU> M1ftblI1PzR4NUe0
NRK-52E MkXNSpVv[3Srb36gZZN{[Xl? Ml;MNVAh|ryP NFvieYhFVVOR M4\RZolvcGmkaYTzJGFv\yCLST3pcoR2[2WmIGPURXQ{KG63Y3zlZZIhfHKjboPsc4NifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhXEeILd8yNUwh[2:ubHHn[Y4hUVZiYX7kJIZq[nKxbnXjeIlv MWSyOVA5QDByMh?=
PC12 M3TBeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHnZU29,OTJwNTFOwG0> NETyeHhFVVOR NUnxd5Q1eHKndnXueJMhXFODLXnu[JVk\WRibnX1dol1\SCob4LtZZRqd25? NG\iOXIzPTF{OEO4Oi=>
HPMCs MoPoSpVv[3Srb36gZZN{[Xl? NGL4[Y9z\X[ncoPld{BmeGm2aHXsbYFtKHSxIH3ld4Vv[2i7bXHsJJRz[W6|aYTpc44hd2ZiaIXtZY4heGW{aYTvcoVidCCvZYPveIhmdGmjbDDj[Yxtew>? NYT4OJY6OjZyNEW3PFA>
A549 M2XrbGZ2dmO2aX;uJIF{e2G7 MWH+OVAh|ryP MV;EUXNQ NF\Vbm5i\m[nY4TzJJRp\SC4aYLhcEBtcW[nIHP5Z4xmKGGwZDDoc5N1KHKnc4DvcpNm MkS2NlY4OTF5NEi=
RAW264.7 NGTX[WtHfW6ldHnvckBie3OjeR?= MUH+N|Ah|ryP M3\1cmROW09? M1zVUJJm\HWlZYOgdJJwNWmwZnzhcY1ifG:{eTDn[Y5mKGW6cILld5Nqd25? MlK5NlY4OTh3OE[=
MEMM M2q0eGtqdmG|ZTDhd5NigQ>? MWWxOUDDvU1? M2DZPGROW09? M2DxeoRm[3KnYYPld{Bi[2W2eXzheIlwdiCxZjDobZN1d26nIFiz MnnkNlY6OjF3ME[=
MEMM NXTI[2dJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnnpglIxKML3TR?= NUK0co5DTE2VTx?= M1PwT4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NILGTJIzPjl{MUWwOi=>
MEMM MYXBdI9xfG:|aYOgZZN{[Xl? NWj5U5FkOTViwsXN NYrFZZNFTE2VTx?= NHP1UXZqdmS3Y3XzJJRp\SCycnXz[Y5k\SCxZjD0bIUh[XCxcITvd4l{KHC{b4TlbY4tKGOuZXH2[YQhS2G|cHHz[U0{ MXOyOlkzOTVyNh?=
T47D MkXoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvmUo8yOCEQvF2= NEnrWZRFVVOR NFHqPXdKSzVyPUeyJI5O NH;CdG0yQDN6MUS0OC=>
ZR-75-1 NEDZeFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV[xNEDPxE1? NH3pfJJFVVOR MULJR|UxRTd7IH7N NFzj[oQyQDN6MUS0OC=>
BT474 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2TnZlExKM7:TR?= M3vM[WROW09? NGO1V3NKSzVyPUi2JI5O NYnN[YtVOTh|OEG0OFQ>
HCC1954 M{PQdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLZNVAh|ryP NYq0eJRlTE2VTx?= MVTJR|UxRTFzOTDuUS=> MkDPNVg{QDF2NES=
MDA-MB-453 Mo[3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoXyNVAh|ryP NV7QR|ZMTE2VTx?= M4LOU2lEPTB;OUe1JI5O M1zEW|E5OzhzNES0
MDA-MB-468 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmfBNVAh|ryP MnnkSG1UVw>? NFvTeWVKSzVyPUOyNFghdk1? NEfue5EyQDN6MUS0OC=>
SkBr3 M13GZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE\LbIkyOCEQvF2= NYjmU5piTE2VTx?= NVrZVmVPUUN3ME6xNEwxODBibl2= MlHwNVg{QDF2NES=
MDA-MB-231 MnroS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYmxNEDPxE1? MVrEUXNQ MWrJR|UxRjFyLECwNEBvVQ>? MWqxPFM5OTR2NB?=
HCT116 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGC5c28yOCEQvF2= NYrDc3hZTE2VTx?= NX\RZpU1UUN3ME21PFM3KG6P MmD0NVg{QDF2NES=
HT29 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mnn3NVAh|ryP MlLhSG1UVw>? Mlu0TWM2OD5zMDywNFAhdk1? NFfHOXkyQDN6MUS0OC=>
HFF NYX6XIJGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF3qfmUyOCEQvF2= NXHWPY1lTE2VTx?= NH;sS2ZKSzVyPUe2NVUhdk1? MkXhNVg{QDF2NES=
HN5 NUnobpp2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUWxNEDPxE1? Mn7xSG1UVw>? NFTac3hKSzVyPkGwMFAxOCCwTR?= M3vsfVE5OzhzNES0
786-0 NW\TU2xJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoXYNVAh|ryP NYC1R2p1TE2VTx?= M4XWdWlEPTB;NECwPUBvVQ>? MkTJNVg{QDF2NES=
H157 NWLYRVFnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIXlSIwyOCEQvF2= MYjEUXNQ MV3JR|UxRTJ4NEKgcm0> Mkj2NVg{QDF2NES=
NCI-H460 NFKyc2FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnvfm9UOTBizszN NGXHe|NFVVOR MX7JR|UxRjJuNUCwJI5O M4DhZVE5OzhzNES0
SKOV-3 M4fPV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUCxNEDPxE1? MnP6SG1UVw>? NE\GOmFKSzVyPUKxNlYhdk1? MWexPFM5OTR2NB?=
OVCAR-3 NFjaWWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1jsR|ExKM7:TR?= NGPJTpNFVVOR MVfJR|UxRTJ7MUigcm0> NWezZ5JHOTh|OEG0OFQ>
BXPC3 MoXVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWSxNEDPxE1? MYHEUXNQ NFX3UpVKSzVyPUOxOFEhdk1? MWSxPFM5OTR2NB?=
MiaPaCa M1TjO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUmxNEDPxE1? MnfnSG1UVw>? M3;XO2lEPTB;NUSzN{BvVQ>? NUHzXpFvOTh|OEG0OFQ>
PANC-1 M4WzNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWSxNEDPxE1? MUTEUXNQ M4jZVmlEPTB;OE[4NUBvVQ>? MoezNVg{QDF2NES=
LNCaP MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkLVNVAh|ryP MmnGSG1UVw>? Ml7sTWM2OD1zNEegcm0> NIXzeoYyQDN6MUS0OC=>
DU145 MorRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1jRNFExKM7:TR?= M1G4emROW09? MVTJR|UxRTN6MUKgcm0> NVrLdpk2OTh|OEG0OFQ>
PC3 NYPYcYVXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1jqTVExKM7:TR?= NWfUS5FFTE2VTx?= MYjJR|UxRjFyLECwNEBvVQ>? MnPLNVg{QDF2NES=
BT474 NEnxNpdMcW6jc3WgZZN{[Xl? NGG2WWIyOCEQvF2= NEjpXXVFVVOR NWjHUZI5cW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiMU[wJI5O MYexPFM5OTR2NB?=
786-0 MoK3T4lv[XOnIHHzd4F6 NITGUm0yOCEQvF2= MUHEUXNQ MoX5bY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhOTVyIH7N NUPLTJQ6OTh|OEG0OFQ>
LNCaP NIjqSmJMcW6jc3WgZZN{[Xl? NV;FcoNbOTBizszN NH3TSmNFVVOR NV3SUJVYcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEOgcm0> MYWxPFM5OTR2NB?=
PC3 MmnpT4lv[XOnIHHzd4F6 M{XTW|ExKM7:TR?= MVTEUXNQ NVLhenpvcW6qaXLpeJMheEeVS{ROtkB4cXSqIFnDOVAhd2ZiNEmgcm0> MVmxPFM5OTR2NB?=
KARPAS-231 M{fWcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mk\rNVAh|ryP M2\OSWROW09? MYjFR|UxRTRzIH7N MYWxPVA3PDd|MB?=
CCRFSB M{TlS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlT5NVAh|ryP MXTEUXNQ MUXFR|UxRTF3NTDuUS=> NHX4fIcyQTB4NEezNC=>
SUP B15 M4f0PGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4G2dFExKM7:TR?= MXXEUXNQ NWOwR4JKTUN3ME2xPVchdk1? NUHXNINOOTlyNkS3N|A>
SD-1 NX3ySYdKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWDjOFVLOTBizszN NVHVbW5MTE2VTx?= Mn[5SWM2OD1|MkCgcm0> NW\KNXpuOTlyNkS3N|A>
RS4;11 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mk\VNVAh|ryP NHPod5JFVVOR MUfFR|UxRTZ3NDDuUS=> M4\iclE6ODZ2N{Ow
MN-60 NFiy[3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1i5SVExKM7:TR?= M1XjbWROW09? NYTUdplSTUN3ME2zOlAzKG6P NGHhUmwyQTB4NEezNC=>
Tanoue MmPmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NInCdGcyOCEQvF2= MVfEUXNQ NFztPFVGSzVyPUS1NVchdk1? MWCxPVA3PDd|MB?=
RCH-ACV NGr5V41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUOxNEDPxE1? Ml;jSG1UVw>? MV7FR|UxRTF3MjDuUS=> MUCxPVA3PDd|MB?=
SEM MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1WzdFExKM7:TR?= M4nBdWROW09? M1KwXWVEPTB;MkCyJI5O M2HiXVE6ODZ2N{Ow
KASUMI-2 MnL4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4fTTVExKM7:TR?= NEDvXWJFVVOR NHzJSmZGSzVyPUKyOUBvVQ>? NHfxXJYyQTB4NEezNC=>
REH Mk\DS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXfWUHFbOTBizszN MnTESG1UVw>? M{j6cmVEPTB;Mki4JI5O MnzkNVkxPjR5M{C=
697 NGfWSJhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH3DbXMyOCEQvF2= NXO3T2hkTE2VTx?= MkXlSWM2OD1|M{igcm0> M2fxUFE6ODZ2N{Ow
NALM-6 NX6zenBQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkO5NVAh|ryP MlLxSG1UVw>? NUjidGF5TUN3ME20NlEhdk1? Mlf1NVkxPjR5M{C=
MHH-CALL–3 M4DYVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWOxNEDPxE1? M3u0cGROW09? NFj0PVNGSzVyPUixNkBvVQ>? M4TRVFE6ODZ2N{Ow
MHH-CALL–2 M3juOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX[xNEDPxE1? M4W5V2ROW09? NHSySXhGSzVyPUKxNVQhdk1? M{fXNVE6ODZ2N{Ow
J.GAMMA-1 M2nBUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVmxNEDPxE1? M37EVmROW09? M3PaTmVEPTB;NkWgcm0> MUGxPVA3PDd|MB?=
JR45.01 MofXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoXhNVAh|ryP M{fXNGROW09? MUPFR|UxRTZ6IH7N MnnINVkxPjR5M{C=
A3 NH;NWY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVGxNEDPxE1? NX;H[XJ[TE2VTx?= NGfKXXhGSzVyPU[5JI5O Mn\vNVkxPjR5M{C=
I 2.1 Mn;ES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEHlfnoyOCEQvF2= NUTZ[WdWTE2VTx?= MX3FR|UxRTd|IH7N M2G3[|E6ODZ2N{Ow
MOLT-3 M2LyNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnPVNVAh|ryP MUXEUXNQ MnHqSWM2OD15NDDuUS=> NXrjW4lPOTlyNkS3N|A>
P116 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3LHOlExKM7:TR?= NVu0TWVCTE2VTx?= MVPFR|UxRTd6IH7N MornNVkxPjR5M{C=
J.Cam1.6 NX[2cYdST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXvMSGdDOTBizszN M4rs[WROW09? MortSWM2OD15OTDuUS=> Ml7jNVkxPjR5M{C=
I 9.2 MmSzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYXmcYE6OTBizszN MWrEUXNQ M{flbmVEPTB;OECgcm0> MlvsNVkxPjR5M{C=
LOUCY MorlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4XsclExKM7:TR?= NVHNcW5CTE2VTx?= NWXPT5RsTUN3ME2xNVchdk1? M2X3XVE6ODZ2N{Ow
J.RT3-T3.5 MnnTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUKxNEDPxE1? NET1[FJFVVOR NXvkb|VLTUN3ME2xNlMhdk1? NYrs[YpEOTlyNkS3N|A>
800000 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUGyNpVMOTBizszN Ml23SG1UVw>? NG\0bZRGSzVyPUG2N{BvVQ>? M{fh[|E6ODZ2N{Ow
Jurkat MnrBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWHhfnk1OTBizszN NHfFS|ZFVVOR M{i0UGVEPTB;MkK1JI5O M2DRflE6ODZ2N{Ow
MOLT-4 M4nvRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWWxNEDPxE1? NWHTSINiTE2VTx?= NWfneFZUTUN3ME2yN|Ihdk1? M{Ht[lE6ODZ2N{Ow
Molt-16 NF7qW3dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MU[xNEDPxE1? NFH5bWVFVVOR NFPyVZhGSzVyPUK0NUBvVQ>? NHTzUocyQTB4NEezNC=>
CEM/C3 NWPNZ45oT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmjBNVAh|ryP NEjQPIZFVVOR MUHFR|UxRTJ3NzDuUS=> NHHrcpoyQTB4NEezNC=>
CEM/C2 NYTNSHhwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIPXVpkyOCEQvF2= M1HCSmROW09? NELXXYlGSzVyPUK3NUBvVQ>? NW\4elVNOTlyNkS3N|A>
CCRFCEM NHnmXI1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1;KelExKM7:TR?= M1PmXGROW09? NGnFPZNGSzVyPUOyO{BvVQ>? MXSxPVA3PDd|MB?=
CEM/C1 NH\mfGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXWxNEDPxE1? MoLNSG1UVw>? M3XuVmVEPTB;M{iyJI5O M3jxfFE6ODZ2N{Ow
SUPTI[VB] NWjSNYJyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnfINVAh|ryP M2jOVGROW09? NYnoeXQ4TUN3ME22NVkhdk1? MVixPVA3PDd|MB?=
CCRF–HSB-2 Mn3YS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlXHNVAh|ryP NVW5UHlmTE2VTx?= MUfFR|UxRTJzMUegcm0> M1HWO|E6ODZ2N{Ow
I 2.1 MV7BdI9xfG:|aYOgZZN{[Xl? MoP2NVAh|ryP MnHySG1UVw>? MlfqbY5lfWOnczDhdI9xfG:|aYO= NH\idmkyQTB4NEezNC=>
I 9.2 NYHBeIt3SXCxcITvd4l{KGG|c3H5 NVHxT41MOTBizszN NWLoWnNFTE2VTx?= NYH4ZXFvcW6mdXPld{BieG:ydH;zbZM> NYLNV4R5OTlyNkS3N|A>
A3 MnPyRZBweHSxc3nzJIF{e2G7 MnXKNVAh|ryP MVfEUXNQ MmnmbY5lfWOnczDhdI9xfG:|aYO= NGDjcWYyQTB4NEezNC=>
RD NYe5dlNIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NY\BfYdbOTBizszN MWDJR|UxRjFyIN88US=> M1\Kd|IxPzRyNkKz
Rh41 MlvCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXewcYE5OTBizszN M1P0WmlEPTB;M{OuPEBvVQ>? NFi4eIQzODd2ME[yNy=>
Rh18 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Moj5NVAh|ryP NEnxOI5KSzVyPUOwN{BvVQ>? MoLtNlA4PDB4MkO=
Rh30 M1y2fWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV3rfYZuOTBizszN NUC3OW15UUN3ME20MlgyKM7:TR?= NYPBT4oxOjB5NEC2NlM>
BT-12 NGrkVZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmmzNVAh|ryP MXvJR|UxRjFyIN88US=> NXq5[opFOjB5NEC2NlM>
CHLA-266 MmnXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPONVAh|ryP NFTsXnhKSzVyPUGuNlIh|ryP MYWyNFc1ODZ{Mx?=
TC-71 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn3INVAh|ryP M3TQeGlEPTB;Mj61NkDPxE1? M1\K[VIxPzRyNkKz
CHLA-9 M{nOUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4TIeFExKM7:TR?= MnjWTWM2OD13OUGgcm0> NU\UflY6OjB5NEC2NlM>
CHLA-10 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4HROlExKM7:TR?= NV3MTVJKUUN3ME2xNFIhdk1? M4nBS|IxPzRyNkKz
CHLA-258 NX\LSYZwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLsVY1WOTBizszN NXTUUFlKUUN3ME2xMlA2KM7:TR?= NX;I[|h[OjB5NEC2NlM>
GBM2 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\jVFExKM7:TR?= M4PxS2lEPTB;OT6xOUDPxE1? M37IXlIxPzRyNkKz
NB-1643 NFni[45Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3fuelExKM7:TR?= MmmwTWM2OD13LkSg{txO Ml3yNlA4PDB4MkO=
NB-Ebc1 NEnkUmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXm2Oo5JOTBizszN NVrWdJluUUN3ME6xNEDPxE1? NFPHXo0zODd2ME[yNy=>
CHLA-90 NUPQ[oVsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWLHS5dLOTBizszN MlrhTWM2OD5zMDFOwG0> MVSyNFc1ODZ{Mx?=
CHLA-136 MmrRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVGxNEDPxE1? MXvJR|UxRjFyIN88US=> NFXWWGYzODd2ME[yNy=>
NALM-6 MoS1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MonWNVAh|ryP NYHq[oRkUUN3ME2yOlUhdk1? MkDENlA4PDB4MkO=
COG-LL-317 NWL2WphOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;jVHMyOCEQvF2= MnXJTWM2OD14LkS5JI5O NHnhd2szODd2ME[yNy=>
RS4;11 Mo\LS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2rQSlExKM7:TR?= NGHy[2tKSzVyPUG0O{BvVQ>? MmSzNlA4PDB4MkO=
MOLT-4 MljrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3:3OlExKM7:TR?= MULJR|UxRTRyIH7N M3\nRVIxPzRyNkKz
CCRF-CEM NX76fJg2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NITqNIMyOCEQvF2= NYHMSZVMUUN3ME2yOlghdk1? MXGyNFc1ODZ{Mx?=
Kasumi-1 NVmwdpEzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWixNEDPxE1? MUfJR|UxRTFyNzDuUS=> Mo\3NlA4PDB4MkO=
Karpas-299 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MW[xNEDPxE1? NITm[5NKSzVyPUKuPVMh|ryP M4\MelIxPzRyNkKz
Ramos-RA1 NIWyNJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYe3RphkOTBizszN NHj1OFVKSzVyPUeuN|Uh|ryP M3PIOlIxPzRyNkKz
H1299 NYq5cXpMU2mwYYPlJIF{e2G7 MYKxNEDPxE1? M4\LUIlvcGmkaYTzJGlMSkuHLXnu[JVk\WRiQXv0JGFkfGm4YYTpc44> M2nxWVIyQTB6NkG2

... Click to View More Cell Line Experimental Data

In vivo試験 All three xenograft models treated with ARQ-197 display reductions in tumor growth: 66% in the HT29 model, 45% in the MKN-45 model, and 79% in the MDA-MB-231 model. In these xenograft studies, no significant body weight changes following oral administration of ARQ-197 at 200 mg/kg are observed. Pharmacodynamically, the phosphorylation of c-Met in human colon xenograft tumors (HT29) is strongly inhibited by ARQ-197, as assessed by a dramatic reduction of c-Met autophosphorylation 24 hours after a single oral dose of 200 mg/kg of ARQ-197. This same dosage in mice exhibits that tumor xenografts are exposed to sustained plasma levels of ARQ-197, consistent with the observed pharmacodynamic inhibition of c-Met phosphorylation and inhibition of proliferation of c-Met harboring cancer cell lines. Plasma levels of ARQ-197 10 hours after dosing are determined to be 1.3 μM, more than 3-fold above the biochemical inhibitory constant of ARQ-197 for c-Met. Therefore, ARQ-197 is able to suppress its target in vivo in the xenografted human tumor tissue. In conclusion, ARQ-197 inhibits the growth of c-Met-dependent xenografted human tumors.[1]
臨床試験 ARQ 197 plus erlotinib is currently in Phase III study in subjects with locally advanced or metastatic non-squamous, non-small cell lung cancer who have received 1 or 2 prior systemic anti-cancer therapies.
特集 The first selective c-Met inhibitor to be advanced into human clinical trials.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

c-Met SDS-PAGE in vitro kinase assay Recombinant c-Met protein (100 ng) is preincubated with increasing concentrations of ARQ-197 for 30 minutes at room temperature. Following preincubation, 100 μM of poly-Glu-Tyr substrate and various concentrations of ATP containing 5 μCi of [γ-32P]ATP are added to the reaction mixture. The reaction is incubated for 5 minutes at room temperature and then stopped by the addition of 5 μL of SDS-polyacrylamide gel, reducing sample buffer. The samples are then loaded onto a 7.5% acrylamide gel and SDS-PAGE is performed. The phosphorylated poly-Glu-Tyr substrates are ultimately visualized by autoradiography. c-Met activity is quantified by densitometry.

細胞アッセイ: [1]

細胞株 T29, MKN-45 and MDA-MB-231 cells
濃度 0.03-10 μM
反応時間 24, 32, and 48 hours
実験の流れ HT29, MKN-45, and MDA-MB-231 cells are seeded in black 96-well plates at 5 × 103 cells per well overnight in a medium with 10% FBS. The next day, cells are treated with increasing concentrations of ARQ-197 (0.03-10 μM) for 24, 32, and 48 hours at 37 °C. After ARQ-197 treatment, the drug-containing medium is removed and cells are incubated for at least 10 minutes in a labeling solution (10 mM HEPES, 140 mM NaCl, and 6 mM CaCl2) containing 2 μg/mL Hoescht 33342 (blue channel), 500-times diluted Annexin V-FITC (green channel), and 1 μg/mL propidium iodide (red channel). High-content image acquisition and analysis are carried out. The program is set to take four images per well. The exposure time is set at 16.7 ms/10% gain, 500 ms/35% gain, and 300 ms/30% gain for the 4,6-diamidino-2-phenylindole, FITC, and rhodamine channels, respectively. Images are processed and the numbers of positive cells for each channel and each condition are determined. In addition, HT29 cells are treated with increasing concentrations of ARQ-197 for 32 hours in the absence or the presence of 25, 50, and 100 μM ZvAD-FMK (irreversible general caspase inhibitor), and the same procedures are undertaken. All experiments are done in triplicate. To determine whether the apoptotic effect is due to c-Met inhibition, the effect of ARQ-197 when glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and c-Met are knocked down using siRNA is investigated. HT29, MKN-45, and MDA-MB-231 cells are transfected with a nontargeted control siRNA, a gapgh-targeted control siRNA, or a met-targeted siRNA. After 3 days, c-Met, GAPDH, and β-actin expression levels are determined using specific antibodies. To determine if the effect is caspase dependent, HT29, MKN-45, and MDA-MB-231 cells are transfected with a met-targeted siRNA for 2 days and incubated in the absence or the presence of increasing concentrations of ZvAD-FMK for 1 additional day. A nontargeted siRNA and a gapgh-targeted siRNA (siRNA GAPDH) are also transfected in parallel, as controls. Cells are then stained with Annexin V-FITC and propidium iodide, and the percentage of apoptotic cells is determined.

動物実験: [1]

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

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

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

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

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

参考

化学情報

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

C23H19N3O2

CAS No. 905854-02-6
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 73 mg/mL (197.6 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (3R,4R)-3-(2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione

文献中の引用 (4)

Frequently Asked Questions

  • Question 1
    Are there any other solutions (apart from DMSO) I can dissolve S2753 for in vivo experiment?

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

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related c-Met 阻害剤

  • NPS-1034は一種の二重Met/Axl阻害剤で、IC50値が48 nMと10.3 nMです。

  • Erlotinib

    Erlotinibは一種のEGFR阻害剤で、このIC50値が2 nMです。Erlotinibは、EGFRに対する敏感性は人間c-Src或いはv-Abに対する敏感性より1000倍以上が高くなります。

  • R428 (BGB324)

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.

  • Crizotinib (PF-02341066)

    Crizotinib (PF-02341066)は一種の有効なc-MetとALK阻害剤で、細胞試験でIC50値が11 nMと24 nMです。

  • Foretinib (GSK1363089)

    Foretinib (GSK1363089)は一種のATP競争性的なHGFRとVEGFRの阻害剤です。Foretinib (GSK1363089)はMetとKDRに作用する効果が一番強くて、無細胞試験でこのIC50が0.4 nM と 0.9 nMに分かれますが、Ron、Flt-1/3/4、Kit、PDGFRα/βとTie-2に作用する効果が少し弱くて、FGFR1とEGFRに抑制活性を殆ど表しません。臨床2期。

  • Capmatinib (INCB28060)

    Capmatinib (INCB28060)は一種の新たで、ATP競争性的なc-MET阻害剤で、無細胞実験でIC50値が0.13 nMです。Capmatinib (INCB28060)はRONβ、EGFRとHER-3に活性を表しません。臨床1期。

    Features:Inactive against RONβ, another member of the c-MET RTK family, as well as EGFR and HER-3 (members of the EGFR RTK family).

  • PHA-665752

    PHA-665752は一種の有効で、選択性的で、ATP競争性的なc-Met阻害剤で、無細胞実験でIC50値が9 nMです。PHA-665752はc-Metに作用する選択性はRTKsとSTKsに作用する選択性より50倍以上が高くなります。

  • BMS-777607

    BMS-777607は一種のMet関連の阻害剤で、無細胞実験でc-Met、Axl、RonとTyro3に作用する時のIC50値が3.9 nM、1.1 nM、1.8 nMと4.3 nMにそれぞれ分かれることです。BMS-777607は、Met関連ターゲットに作用する選択性はLck、VEGFR-2とTrkA/Bに作用する選択性より40倍が高くなって、他の受容体と非受容体のキナーゼに作用する選択性より500倍が高くなります。臨床 1/2期。

    Features:A potent inhibitor of the Met family, and >40-fold selectivity vs. Lck, VEGFR2, and TrkA/B and >500-fold selective vs. other receptor and non-receptor kinases.

最近チェックしたアイテム

Tags: Tivantinib (ARQ 197)を買う | Tivantinib (ARQ 197)供給者 | Tivantinib (ARQ 197)を購入する | Tivantinib (ARQ 197)費用 | Tivantinib (ARQ 197)生産者 | オーダーTivantinib (ARQ 197) | Tivantinib (ARQ 197)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ