Tivantinib (ARQ 197)

製品コードS2753

Tivantinib (ARQ 197)化学構造

分子量(MW):369.42

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。

サイズ 価格(税別) 在庫  
JPY 18260.00 あり
JPY 78020.00 あり

カスタマーフィードバック(2)

  • 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. 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.

製品安全説明書

c-Met阻害剤の選択性比較

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。
特性 The first selective c-Met inhibitor to be advanced into human clinical trials.
ターゲット
c-Met [1]
(Cell-free assay)
0.355 μM(Ki)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 MkL3T4lv[XOnIHHzd4F6 MojnglExKM7:TR?= NH;RVnRqdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz NGrIbVczODR6NECxPC=>
HT29 MUXLbY5ie2ViYYPzZZk> NXK1cJhNhjFyIN88US=> NFrXUm1qdmirYnn0d{BkNU2ndDDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0h[y2PZYSgd4lodmGuaX7nJJBifGi5YYnz Mnn0NlA1QDRyMUi=
MDA-MB-231 M{DmXWtqdmG|ZTDhd5NigQ>? MYD+NVAh|ryP NV\3OG5HcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> NV\iWJdKOjB2OESwNVg>
NCI-H441 NUDleo5lU2mwYYPlJIF{e2G7 NWL1V4luhjFyIN88US=> MmfMbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= NFX0UXIzODR6NECxPC=>
SK-MEL-28 NVrSTVl[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoPMN|Mh|ryP MXvJR|UxRjN|IN88US=> NEfOXpgzODR6NECxPC=>
NCI-H661 MlTHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWL1fmFGOzNizszN MkP6TWM2OD5|MzFOwG0> NYDKUG93OjB2OESwNVg>
NCI-H446 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkP2N|Mh|ryP NU\nXZlZUUN3ME23JO69VQ>? M{DiN|IxPDh2MEG4
MDA-MB-231 M{jocGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnW4N|Mh|ryP NYnNW|BRUUN3ME2wMlU2KM7:TR?= NX\FZlJqOjB2OESwNVg>
DLD-1 M3OwVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NI[zZWw{OyEQvF2= MnjaTWM2OD1yLkWzJO69VQ>? M13CZlIxPDh2MEG4
A549 M{ThTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH3KNYQ{OyEQvF2= NXn1XY9pUUN3ME2wMlU6KM7:TR?= M2\lfFIxPDh2MEG4
SK-OV-3 NHnCfm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NE\xR5k{OyEQvF2= NEnTWGJKSzVyPUCuOlYh|ryP NEXnZYwzODR6NECxPC=>
NCI-H460 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2D6VFM{KM7:TR?= NInxPHlKSzVyPUCuOkDPxE1? M2Xue|IxPDh2MEG4
A375 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF\OS3Q{OyEQvF2= MUfJR|UxRTBwNEKg{txO M3myVVIxPDh2MEG4
NCI-H441 M1Pyd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIfqNJI{OyEQvF2= MVjJR|UxRTBwMzFOwG0> NXznd|FuOjB2OESwNVg>
HT29 NH\YbJpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH7nO3g{OyEQvF2= NX\hdmF4UUN3ME2wMlQ6KM7:TR?= M{jveFIxPDh2MEG4
MKN-45 NX25T2toT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVvkVXRHOzNizszN NYfyRVVoUUN3ME2wMlU5KM7:TR?= MlrKNlA1QDRyMUi=
HT29 NHHIbJZCeG:ydH;zbZMh[XO|YYm= M3zxR54yOCEQvF2= MXTzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? M4W1N|IxPDh2MEG4
MKN-45 NHrKN4RCeG:ydH;zbZMh[XO|YYm= NYnpUnVRhjFyIN88US=> MnS3d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5NqeyCkeTC4NE06OCVw NX7PZ5l2OjB2OESwNVg>
MDA-MB-231 MXTBdI9xfG:|aYOgZZN{[Xl? NF;nVlV,OTBizszN Mn22cY9l\XO2bImgbY5lfWOnczDhdI9xfG:|aYOgZpkhOzVnLh?= MXmyNFQ5PDBzOB?=
MDA-MB-231/TGL NUH5T|lkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1:1VZ4yODBizszN MV\HTVUxRTFwMjFOwG0> NUPpTnMyOjJyMke2PVA>
1833/TGL Ml2zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUP+NVAxKM7:TR?= MUHHTVUxRTNwNzFOwG0> M2DrU|IzODJ5Nkmw
EBC1 MojNR5l1d3SxeHnjxsBie3OjeR?= MWP+NVAh|ryP NXjwfo5WcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> M1LHeVI{PTl6Mke2
SNU638 NIHZboZEgXSxdH;4bYPDqGG|c3H5 NEXrRph,OTBizszN NYHkeI9xcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> NELafpgzOzV7OEK3Oi=>
A549 Moe5R5l1d3SxeHnjxsBie3OjeR?= M3Tqcp4yOCEQvF2= MWTuc5Qh[W[oZXP0 NYPocmplOjN3OUiyO|Y>
H460 NIq0NmdEgXSxdH;4bYPDqGG|c3H5 MlXrglExKM7:TR?= MVLuc5Qh[W[oZXP0 NFrhNXczOzV7OEK3Oi=>
HCC827 MYnDfZRwfG:6aXRCpIF{e2G7 MWj+NVAh|ryP NEK3O3lvd3RiYX\m[YN1 M{izfVI{PTl6Mke2
A549 M{j4c2Z2dmO2aX;uJIF{e2G7 NIriS3YyOCEQvF2= MnXo[Il{enWydIOgcYlkem:2dXL1cIU> NI\Td2gzOzV7OEK3Oi=>
EBC1 NGfRSmtHfW6ldHnvckBie3OjeR?= M4Gw[|ExKM7:TR?= MWnkbZNzfXC2czDtbYNzd3S3YoXs[S=> NWHHVGNtOjN3OUiyO|Y>
H460 NH2ydHpHfW6ldHnvckBie3OjeR?= M3yyb|ExKM7:TR?= MUHpcohq[mm2czD0eYJ2dGmwIIDvcJlu\XKrenH0bY9v MkX2NlU{OTNyMUC=
K562/VCR MUTDfZRwfG:6aXRCpIF{e2G7 M1K0Xp4yOCEQvF2= M1jNXJNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= MWiyOVMyOzBzMB?=
CEM/VBL NFjJVIJEgXSxdH;4bYPDqGG|c3H5 MVL+NVAh|ryP NFK3WmZ{cG:5czDjfZRwfG:6aXOgZYN1cX[rdIm= M4DNT|I2OzF|MEGw
U266 MmDpR5l1d3SxeHnjxsBie3OjeR?= NUXZb5NwhjNizszNxsA> Ml76TWM2OD1zLkGg{txO MWeyOVgyODBzMx?=
OPM-2 M1[1fWN6fG:2b4jpZ:Kh[XO|YYm= NUntT5BKhjNizszNxsA> M2jOXmlEPTB;MT64JO69VQ>? NGG2eYEzPThzMECxNy=>
MM.1S MUjDfZRwfG:6aXRCpIF{e2G7 MonXglMh|ryPwrC= NYnP[FBZUUN3ME2xMlYh|ryP NVLC[3hZOjV6MUCwNVM>
MM.1R MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWTmWlFnOyEQvF5CpC=> MYrpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB2OTW= M{XOd|I2QDFyMEGz
RPMI-8226 M374NWN6fG:2b4jpZ:Kh[XO|YYm= NYjWWJB1hjNizszNxsA> MlnQTWM2OD1yLkmg{txO MVOyOVgyODBzMx?=
ANBL-6 M3\VbmN6fG:2b4jpZ:Kh[XO|YYm= NITpUGgyKM7:TdMg MmK0bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MnraNlU5OTByMUO=
ANLB-6/V10R Ml\JR5l1d3SxeHnjxsBie3OjeR?= MkKxNUDPxE4EoB?= Mn;4bY5lfWOnczDj[YxtKGSnYYToJIJ6KG2xcnWgeIhidiB3MDW= MXiyOVgyODBzMx?=
KAS-6/1 MUTDfZRwfG:6aXRCpIF{e2G7 MWGxJO69VcLi M{LZWolv\HWlZYOgZ4VtdCCmZXH0bEBjgSCvb4LlJJRp[W5iNUCl M2XafFI2QDFyMEGz
KAS-6/V10R NVGzRpQ1S3m2b4TvfIlkyqCjc4PhfS=> M3na[lEh|ryPwrC= NYOxZpZxcW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> NFzXZlkzPThzMECxNy=>
KAS-6/R10R NETKUnlEgXSxdH;4bYPDqGG|c3H5 NFrqS5YyKM7:TdMg NG\ZSG9qdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> NV;W[5Y3OjV6MUCwNVM>
8226/S Ml22S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3jITFMh|ryPwrC= MVrpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= M3nudVI2QDFyMEGz
8226/LR-5 NHPiR5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2HHV|Mh|ryPwrC= MUPpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= NYXlUWZzOjV6MUCwNVM>
Huh7 NWDBb3k5S3m2b4TvfIlkyqCjc4PhfS=> NIrwbnp,PC56IN88UeKh NVn6TXZDTE2VTx?= MYjJR|UxRTlwOTDuUS=> MnfBNlYzPTl{NUC=
Hep3B NIfqVm1EgXSxdH;4bYPDqGG|c3H5 NX;hVVN2hjRwODFOwG3DqA>? M2XkVWROW09? NI\W[G1KSzVyPUS0PE44KG6P NWX4VW02OjZ{NUmyOVA>
HepG2 M3LmVmN6fG:2b4jpZ:Kh[XO|YYm= M1zDSZ41NjhizszNxsA> MWfEUXNQ M2XNSWlEPTB;MUO5Mlc4KG6P M37vW|I3OjV7MkWw
Chang NYHDbY0xS3m2b4TvfIlkyqCjc4PhfS=> Mn72glQvQCEQvF5CpC=> M{DiWmROW09? Ml\5TWM2OD12NEiuO{BvVQ>? NFHqSFEzPjJ3OUK1NC=>
Huh7 NGrOZXJHfW6ldHnvckBie3OjeR?= M1GxbFEvPiEQvF5CpC=> NGXqd4VFVVOR Ml3iZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NGnrNWUzPjJ3OUK1NC=>
Hep3B MVnGeY5kfGmxbjDhd5NigQ>? NVzYeFRiOS54IN88UeKh M13RRmROW09? MX\jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 NV\me5o2OjZ{NUmyOVA>
HepG2 MmTwSpVv[3Srb36gZZN{[Xl? NWrCTYE5OS54IN88UeKh MVLEUXNQ NWLYUHJR[2G3c3XzJIEhTzJxTTDj[YxtKGO7Y3zlJIFzemW|dB?= M{PuUVI3OjV7MkWw
Chang NFr0ZY9HfW6ldHnvckBie3OjeR?= NWDVWJVUOS54IN88UeKh NY\XN405TE2VTx?= M{O4fYNifXOnczDhJGczN01iY3XscEBkgWOuZTDhdpJme3R? MXmyOlI2QTJ3MB?=
MHCC97L MkDzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEHKV4l,OTBizszN M2e5dmROW09? NXzTWJlCUUN3ME2zNVUhdk1? MmK4NlY1PTh7NUO=
MHCC97H NFT5[HRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUT+NVAh|ryP NFOzOlJFVVOR M1rNPGlEPTB;M{[45qCKKG6P MUSyOlQ2QDl3Mx?=
Huh7 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmXJglExKM7:TR?= NV62eFl{TE2VTx?= M4\iV2lEPTB;Mk[1JI5O NXHK[lE6OjZ2NUi5OVM>
HepG2 NV7vVoZbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnL4glExKM7:TR?= NEWzfW9FVVOR MnjCTWM2OD1|OUKgcm0> MX[yOlQ2QDl3Mx?=
MHCC97L NH;LUpZHfW6ldHnvckBie3OjeR?= NHLvOooyKM7:TdMg MVLEUXNQ MXjpcoR2[2W|IH3pZ5JwfHWkdXzld{Bl\XCxbInt[ZJqgmG2aX;u M4TFfFI3PDV6OUWz
Huh7 NY\RN|hTTnWwY4Tpc44h[XO|YYm= M1fqRVEh|ryPwrC= M1PRfWROW09? NYXmb|VpcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NFrUUpIzPjR3OEm1Ny=>
MHCC97L MXvBdI9xfG:|aYOgZZN{[Xl? M3rvcVEh|ryPwrC= MWXEUXNQ Mo\IbY5lfWOnczDhdI9xfG:|aYO= NU[1e2hCOjZ2NUi5OVM>
Huh7 M4DDcWFxd3C2b4Ppd{Bie3OjeR?= M2n2PVEh|ryPwrC= NYWyeVZYTE2VTx?= NYK4epZrcW6mdXPld{BieG:ydH;zbZM> NVLnOndFOjZ2NUi5OVM>
C3H 10T1/2 mouse fibroblasts MUnLbY5ie2ViYYPzZZk> MnPPNlUh|ryP NEfBNpFFVVOR MlLJdoVlfWOnczDIbZN1d26nIFizJIFv\CCKNDDhZ4V1gWyjdHnvckBt\X[nbIRCpC=> M3;YWlIxPTN2M{S1
H23 MkH6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXmyOUDPxE1? NHqzOoFFVVOR NXnx[oR[e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MVWyNFU{PDN2NR?=
WM35 MlflS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU[xNEDPxE1? NYnlcIxOTE2VTx?= Ml7Td4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MUKyNFU{PDN2NR?=
NIH 3T3 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFnzOHoyOCEQvF2= NWnTZ41rTE2VTx?= Ml7O[I9meyCwb4SgbIF3\SCjIIPp[45q\mmlYX70JIlvcGmkaYTvdpkh\W[oZXP0 MUCyNFU{PDN2NR?=
H838 MkPOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1;lS|ExKM7:TR?= NX6yd3NVTE2VTx?= NFL1T3pld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> MVGyNFU{PDN2NR?=
H1395 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXexNEDPxE1? MVfEUXNQ M2XSfoRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> M4TVclIxPTN2M{S1
Quiescent S2 NWqyXJEyU2mwYYPlJIF{e2G7 MnyzN|Ah|ryP NULlUppSTE2VTx?= NIr4b4xkd22ybHX0[Yx6KGGkcn;nZZRmeyCWU1GtbY5lfWOnZDDofZBmemGlZYT5cIF1cW:wIH;mJGg{UzSvZUOgbIl{fG:wZYO= MWGyNVUyQDlzNR?=
PC3 NWLBN3VXSXCxcITvd4l{KGG|c3H5 NXW2d4FKOjBizszN Mo\3SG1UVw>? MV7pcoR2[2W|IHHwc5B1d3Orcx?= MXWyNVcxQTF|MB?=
Du145 Mn7nRZBweHSxc3nzJIF{e2G7 MlniNlAh|ryP M2PrdWROW09? NIjqNFhqdmS3Y3XzJIFxd3C2b4Ppdy=> MoKwNlE4ODlzM{C=
LNCaP MVnBdI9xfG:|aYOgZZN{[Xl? MVmyNEDPxE1? M32z[2ROW09? M17Edolv\HWlZYOgZZBweHSxc3nz NHnpcYUzOTdyOUGzNC=>
LAPC-4 MULBdI9xfG:|aYOgZZN{[Xl? NWjkcolOOjBizszN MmHSSG1UVw>? NFnUVXdqdmS3Y3XzJIFxd3C2b4Ppdy=> NVLJe3NpOjF5MEmxN|A>
LNCaP MnP4SpVv[3Srb36gZZN{[Xl? MY[yNEDPxE1? NILmOGtFVVOR NF[5XlRl\WO{ZXHz[ZMhWFODIIPlZ5JmfGmxbjDhcoQheDZ3IHX4dJJme3Orb36gcIV3\Wy| NYjyOmNKOjF5MEmxN|A>
LAPC-4 MmrqSpVv[3Srb36gZZN{[Xl? NVjmbGZtOjBizszN NV3JTmI2TE2VTx?= MVPk[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ MnfZNlE4ODlzM{C=
Kasumi-1 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHjtd5B,PTBizszN MXHEUXNQ NFPNPJFqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NF\o[m8zOzN7MEWzOi=>
SKNO-1 NXKwcVVIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHfEOmZ,PTBizszN NWjsNnl{TE2VTx?= MmHybY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MmnJNlM{QTB3M{[=
Kasumi-1 MYjLbY5ie2ViYYPzZZk> M{DRdJ4yOCEQvF2= NWfXelZsTE2VTx?= MnrXdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y MlHlNlM{QTB3M{[=
SKNO-1 NUHKOWJUU2mwYYPlJIF{e2G7 Mo\BglExKM7:TR?= MWHEUXNQ NXztWmd[emWmdXPld{BmgHC{ZYPzbY9vKG:oIHHj[ZR6dGG2ZXSgbIl{fG:wZTDIN{zDqGNva3n0xsBidmUEoHLjcE0z NYnz[otIOjN|OUC1N|Y>
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Karpas-299 MmnUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUiyO3FWOTBizszN NGfuN2lKSzVyPUKuPVMh|ryP NE\lblYzODd2ME[yNy=>
Ramos-RA1 M2LZS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;JNVIyOCEQvF2= NFTCTnRKSzVyPUeuN|Uh|ryP M2C0e|IxPzRyNkKz
H1299 MWLLbY5ie2ViYYPzZZk> MknHNVAh|ryP NWXUXHZUcW6qaXLpeJMhUUuES1WtbY5lfWOnZDDBb5QhSWO2aY\heIlwdg>? NUHoOYNMOjF7MEi2NVY>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
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c-Met SDS-PAGE in vitro kinase assay:

Recombinant c-Met protein (100 ng) is preincubated with increasing concentrations of ARQ-197 for 30 minutes at room temperature. Following preincubation, 100 μM of poly-Glu-Tyr substrate and various concentrations of ATP containing 5 μCi of [γ-32P]ATP are added to the reaction mixture. The reaction is incubated for 5 minutes at room temperature and then stopped by the addition of 5 μL of SDS-polyacrylamide gel, reducing sample buffer. The samples are then loaded onto a 7.5% acrylamide gel and SDS-PAGE is performed. The phosphorylated poly-Glu-Tyr substrates are ultimately visualized by autoradiography. c-Met activity is quantified by densitometry.
細胞試験: [1]
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  • 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.
    (参考用のみ)
動物試験:[1]
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  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 73 mg/mL (197.6 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 369.42
化学式

C23H19N3O2

CAS No. 905854-02-6
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01468922 Completed Sarcoma|Stomach Neoplasms|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 24, 2011 Phase 1
NCT02608411 Recruiting Carcinoma, Small Cell Istituto Oncologico Veneto IRCCS October 2015 Phase 2
NCT02150733 Completed Hepatic Impairment|Solid Tumor|Cancer Daiichi Sankyo Inc.|Medpace, Inc. April 2014 Phase 1
NCT02029157 Recruiting Liver Cancer Kyowa Hakko Kirin Co., Ltd January 2014 Phase 3
NCT01892527 Active, not recruiting Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro, MD|Istituto Clinico Humanitas March 2013 Phase 2
NCT02049060 Active, not recruiting Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro, MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2

技術サポート

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。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

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

  • 回答:

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

c-Met信号経路図

c-Met Inhibitors with Unique Features

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