Tivantinib (ARQ 197)

For research use only. Not for use in humans.

目录号:S2753

Tivantinib (ARQ 197) Chemical Structure

CAS No. 905854-02-6

Tivantinib (ARQ 197) 是第一个非ATP竞争性的c-Met抑制剂,在无细胞试验中Ki为0.355 μM,对Ron几乎没有作用活性,对EGFR,InsR,PDGFRα和FGFR1/4没有抑制作用。Tivantinib (ARQ 197) 可诱导G2/M期细胞阻滞和凋亡。Phase 3。

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客户使用Selleck生产的Tivantinib (ARQ 197)发表文献35篇:

产品安全说明书

c-Met抑制剂选择性比较

生物活性

产品描述 Tivantinib (ARQ 197) 是第一个非ATP竞争性的c-Met抑制剂,在无细胞试验中Ki为0.355 μM,对Ron几乎没有作用活性,对EGFR,InsR,PDGFRα和FGFR1/4没有抑制作用。Tivantinib (ARQ 197) 可诱导G2/M期细胞阻滞和凋亡。Phase 3。
特性 ARQ-197是第一个应用到晚期人类临床试验的c-Met选择性抑制剂。
靶点
c-Met [1]
(Cell-free assay)
0.355 μM(Ki)
体外研究

ARQ-197抑制HGF/c-met诱导的细胞反应。ARQ-197具有抗肿瘤活性,抑制A549, DBTRG和NCI-H441细胞增殖,IC50分别为0.38, 0.45, 0.29 μM。用ARQ-197处理,导致MAPK信号级联放大磷酸化降低,且阻断入侵和迁移。此外,没有内源性c-Met表达的NCI-H661细胞中c-Met异常表达,形成一种入侵表现型,也被ARQ-197抑制。加入浓度不断增加的ARQ-197不会明显影响ATP的Km值,但是用0.5 μM ARQ-197处理c-Met,则降低c-Met的Vmax值,降低3倍。ARQ-197降低Vmax而不影响ATP的Km值说明ARQ-197抑制c-Met是非ATP竞争抑制,也说明ARQ-197具有高度激酶选择性。ARQ-197抑制人类重组c-Met,具有恒定的Ki值,为355 nM。虽然使用过的ATP最高浓度为200 μM, 但是当ATP浓度为1 mM时,ARQ-197抑制c-Met效果不会降低。ARQ-197抑制c-Met磷酸化,且阻断下游c-Met信号通路。ARQ-197阻断组成型和配体调节的c-Met自磷酸化,通过增强c-Met活性, 反过来抑制下游c-Met效应器。ARQ-197作用于表达c-Met的人类癌细胞包括HT29, MKN-45, 和MDA-MB-231细胞,诱导caspase依赖的凋亡。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MNK-45 Mmq2T4lv[XOnIHHzd4F6 MoLOglExKM7:TR?= MnrGbY5pcWKrdIOgZ{1O\XRicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJIMuVWW2IIPp[45idGmwZzDwZZRpf2G7cx?= MXmyNFQ5PDBzOB?=
HT29 M2fZUWtqdmG|ZTDhd5NigQ>? Mn:4glExKM7:TR?= MXHpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| NGKzUFkzODR6NECxPC=>
MDA-MB-231 NXLDTFY3U2mwYYPlJIF{e2G7 M{m0eZ4yOCEQvF2= MWLpcohq[mm2czDjMW1mfCCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gZ{1O\XRic3nncoFtcW6pIIDheIh4[Xm| MlywNlA1QDRyMUi=
NCI-H441 MXLLbY5ie2ViYYPzZZk> Ml3sglExKM7:TR?= NW\vdGRKcW6qaXLpeJMh[y2PZYSgdIhwe3Cqb4L5cIF1cW:wIHHu[EBld3ewc4Ty[YFuKGNvTXX0JJNq\26jbHnu[{Bx[XSqd3H5dy=> MWOyNFQ5PDBzOB?=
SK-MEL-28 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGXk[m4{OyEQvF2= NH;Rc4FKSzVyPkOzJO69VQ>? NIfUN3IzODR6NECxPC=>
NCI-H661 Mn7LS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHzVoc{OyEQvF2= MUHJR|UxRjN|IN88US=> MUSyNFQ5PDBzOB?=
NCI-H446 NGmxcoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkfXN|Mh|ryP NFzVV|JKSzVyPUeg{txO NVn0WGZkOjB2OESwNVg>
MDA-MB-231 NHrV[|lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWm3e4ljOzNizszN Mo\GTWM2OD1yLkW1JO69VQ>? NGPzOI4zODR6NECxPC=>
DLD-1 M1GxTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV24S4JOOzNizszN NGTzVFRKSzVyPUCuOVMh|ryP M3;jclIxPDh2MEG4
A549 Ml3BS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVuzN{DPxE1? NGmweHVKSzVyPUCuOVkh|ryP NESzU4kzODR6NECxPC=>
SK-OV-3 M2Tadmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NILKcWY{OyEQvF2= MX;JR|UxRTBwNk[g{txO NV\HclJOOjB2OESwNVg>
NCI-H460 NXXUZ|FmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojFN|Mh|ryP MYHJR|UxRTBwNjFOwG0> MnHhNlA1QDRyMUi=
A375 NFPjN4lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NELSfYQ{OyEQvF2= NUfEcJBpUUN3ME2wMlQzKM7:TR?= MYKyNFQ5PDBzOB?=
NCI-H441 MmrhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGD3NVc{OyEQvF2= M1e2e2lEPTB;MD6zJO69VQ>? NF3EUWczODR6NECxPC=>
HT29 NHjPTlVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MknHN|Mh|ryP NGniW2VKSzVyPUCuOFkh|ryP M4LqV|IxPDh2MEG4
MKN-45 M3zCOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlHRN|Mh|ryP MX\JR|UxRTBwNUig{txO MnqzNlA1QDRyMUi=
HT29 M2PjVWFxd3C2b4Ppd{Bie3OjeR?= M{PuPJ4yOCEQvF2= M3zoT5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXNiYomgPFAuQTBnLh?= M2LkXFIxPDh2MEG4
MKN-45 NYHacnB[SXCxcITvd4l{KGG|c3H5 MlTYglExKM7:TR?= MYLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{KGK7IEiwMVkxLS5? MXmyNFQ5PDBzOB?=
MDA-MB-231 MlL6RZBweHSxc3nzJIF{e2G7 NUnEUmNQhjFyIN88US=> MVHtc4Rme3SueTDpcoR2[2W|IHHwc5B1d3OrczDifUA{PSVw MW[yNFQ5PDBzOB?=
MDA-MB-231/TGL Mn;pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIrndXN,OTByIN88US=> NFP2UZBIUTVyPUGuNkDPxE1? NV\BXnVUOjJyMke2PVA>
1833/TGL NWfXcYk5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{DOUp4yODBizszN NH;vcVRIUTVyPUOuO{DPxE1? M3S5blIzODJ5Nkmw
EBC1 NILMNmlEgXSxdH;4bYPDqGG|c3H5 MWj+NVAh|ryP NUmydJB3cW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> MoHDNlM2QTh{N{[=
SNU638 MVPDfZRwfG:6aXRCpIF{e2G7 NXn0UnhVhjFyIN88US=> NUnDV4FwcW6qaXLpeJMhfGinIHPlcIwh\3Kxd4ToMi=> MVGyN|U6QDJ5Nh?=
A549 NWTHU|Z1S3m2b4TvfIlkyqCjc4PhfS=> NUe5O|VZhjFyIN88US=> M{H6eY5wfCCjZn\lZ5Q> MX2yN|U6QDJ5Nh?=
H460 Mm\iR5l1d3SxeHnjxsBie3OjeR?= NInC[Jh,OTBizszN NYHCSoVKdm:2IHHm[oVkfA>? MkLHNlM2QTh{N{[=
HCC827 MX7DfZRwfG:6aXRCpIF{e2G7 MkjXglExKM7:TR?= MWjuc5Qh[W[oZXP0 MYmyN|U6QDJ5Nh?=
A549 MnfaSpVv[3Srb36gZZN{[Xl? MkK1NVAh|ryP MmnU[Il{enWydIOgcYlkem:2dXL1cIU> M2O1N|I{PTl6Mke2
EBC1 M3vaemZ2dmO2aX;uJIF{e2G7 MX[xNEDPxE1? MlGz[Il{enWydIOgcYlkem:2dXL1cIU> M4fzNVI{PTl6Mke2
H460 NX7Hc5k{TnWwY4Tpc44h[XO|YYm= NYf5RY9POTBizszN M1;xNIlvcGmkaYTzJJR2[nWuaX6gdI9tgW2ncnn6ZZRqd25? MVKyOVMyOzBzMB?=
K562/VCR Ml;pR5l1d3SxeHnjxsBie3OjeR?= MVr+NVAh|ryP Mkf4d4hwf3NiY4n0c5RwgGmlIHHjeIl3cXS7 NH3SO5gzPTNzM{CxNC=>
CEM/VBL NFHiR4dEgXSxdH;4bYPDqGG|c3H5 MnLkglExKM7:TR?= M3f4WpNpd3e|IHP5eI91d3irYzDhZ5Rqfmm2eR?= MWiyOVMyOzBzMB?=
U266 MojDR5l1d3SxeHnjxsBie3OjeR?= MWH+N{DPxE4EoB?= NFrxWphKSzVyPUGuNUDPxE1? MorhNlU5OTByMUO=
OPM-2 NFLlSmVEgXSxdH;4bYPDqGG|c3H5 M4X5Up4{KM7:TdMg MYjJR|UxRTFwODFOwG0> MXWyOVgyODBzMx?=
MM.1S NXXsTmJGS3m2b4TvfIlkyqCjc4PhfS=> NITw[nZ,OyEQvF5CpC=> MoTmTWM2OD1zLk[g{txO NH7oVIwzPThzMECxNy=>
MM.1R NG\r[3RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{nmeFMh|ryPwrC= NIfZWopqdmirYnn0d{Bk\WyuIHfyc5d1cCCkeTC0PUU> NGP0OWUzPThzMECxNy=>
RPMI-8226 MnP2R5l1d3SxeHnjxsBie3OjeR?= NYDjOmVQhjNizszNxsA> NETaW45KSzVyPUCuPUDPxE1? Mle4NlU5OTByMUO=
ANBL-6 MnHGR5l1d3SxeHnjxsBie3OjeR?= M3r1WFEh|ryPwrC= NFHBPIVqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MmLINlU5OTByMUO=
ANLB-6/V10R MXrDfZRwfG:6aXRCpIF{e2G7 M3zk[|Eh|ryPwrC= MWPpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= M3vTS|I2QDFyMEGz
KAS-6/1 NXXM[2VMS3m2b4TvfIlkyqCjc4PhfS=> NEfzdYIyKM7:TdMg NF3jfYlqdmS3Y3XzJINmdGxiZHXheIgh[nlibX;y[UB1cGGwIEWwKS=> MV[yOVgyODBzMx?=
KAS-6/V10R MVTDfZRwfG:6aXRCpIF{e2G7 M3TrR|Eh|ryPwrC= MWrpcoR2[2W|IHPlcIwh\GWjdHigZpkhdW:{ZTD0bIFvKDVyJR?= MWSyOVgyODBzMx?=
KAS-6/R10R NYXHToZMS3m2b4TvfIlkyqCjc4PhfS=> M2HLdFEh|ryPwrC= NV7teoE5cW6mdXPld{Bk\WyuIHTlZZRpKGK7IH3vdoUhfGijbjC1NEU> Mn3ZNlU5OTByMUO=
8226/S M4Hydmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUCzJO69VcLi NY\hclJFcW6qaXLpeJMh[2WubDDndo94fGhiYomgOVQm MV6yOVgyODBzMx?=
8226/LR-5 MoDFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVqzJO69VcLi MVXpcohq[mm2czDj[YxtKGe{b4f0bEBjgSB3NDW= M2rYNlI2QDFyMEGz
Huh7 MknwR5l1d3SxeHnjxsBie3OjeR?= M3m4NZ41NjhizszNxsA> NVXXbYpITE2VTx?= MXrJR|UxRTlwOTDuUS=> NXKx[olOOjZ{NUmyOVA>
Hep3B M{nRWmN6fG:2b4jpZ:Kh[XO|YYm= M2m4TZ41NjhizszNxsA> NXf5W4d3TE2VTx?= M4DJ[2lEPTB;NES4Mlchdk1? NUnVXoo1OjZ{NUmyOVA>
HepG2 NEnwbYZEgXSxdH;4bYPDqGG|c3H5 MmXjglQvQCEQvF5CpC=> NV7GVHZpTE2VTx?= NYL3UlhrUUN3ME2xN|kvPzdibl2= NFjrW|YzPjJ3OUK1NC=>
Chang MXnDfZRwfG:6aXRCpIF{e2G7 MlWwglQvQCEQvF5CpC=> NEfkWohFVVOR NXq3To9EUUN3ME20OFgvPyCwTR?= Mn7wNlYzPTl{NUC=
Huh7 NGXpT41HfW6ldHnvckBie3OjeR?= NU\iOXh[OS54IN88UeKh M4LxU2ROW09? MnLvZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? NYH4ZmlyOjZ{NUmyOVA>
Hep3B NV32XVRnTnWwY4Tpc44h[XO|YYm= MnG5NU43KM7:TdMg M3vvfmROW09? NEDPcXFk[XW|ZYOgZUBIOi:PIHPlcIwh[3mlbHWgZZJz\XO2 M4HjblI3OjV7MkWw
HepG2 NGPSPI1HfW6ldHnvckBie3OjeR?= MorNNU43KM7:TdMg M374dGROW09? MV3jZZV{\XNiYTDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1 MYmyOlI2QTJ3MB?=
Chang MYHGeY5kfGmxbjDhd5NigQ>? MY[xMlYh|ryPwrC= MYXEUXNQ MnXnZ4F2e2W|IHGgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M4jnTlI3OjV7MkWw
MHCC97L M2DkVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3\YOp4yOCEQvF2= M2XjXWROW09? NHHG[ZJKSzVyPUOxOUBvVQ>? MYqyOlQ2QDl3Mx?=
MHCC97H NF7wbZdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVn2[Ik{hjFyIN88US=> M{TwOWROW09? Mm[zTWM2OD1|NklihKkhdk1? MnTuNlY1PTh7NUO=
Huh7 MnXQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXL+NVAh|ryP M3;Ob2ROW09? M1ewS2lEPTB;Mk[1JI5O NXe0dFVuOjZ2NUi5OVM>
HepG2 MlK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV:4dWFwhjFyIN88US=> NWDDU2hiTE2VTx?= M32wT2lEPTB;M{myJI5O M2HBS|I3PDV6OUWz
MHCC97L M3fFWWZ2dmO2aX;uJIF{e2G7 NUjUemd5OSEQvF5CpC=> MoizSG1UVw>? NXzLWms1cW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? NYnQUVY6OjZ2NUi5OVM>
Huh7 Mm\3SpVv[3Srb36gZZN{[Xl? MX2xJO69VcLi NG\4PWNFVVOR NXH6SmprcW6mdXPld{BucWO{b4T1ZpVt\XNiZHXwc4x6dWW{aYrheIlwdg>? MnKzNlY1PTh7NUO=
MHCC97L NYnGT2ZwSXCxcITvd4l{KGG|c3H5 NGfybHYyKM7:TdMg M3LSSGROW09? MVrpcoR2[2W|IHHwc5B1d3Orcx?= M4rwWVI3PDV6OUWz
Huh7 NV\4TFdPSXCxcITvd4l{KGG|c3H5 NVj2eHoyOSEQvF5CpC=> M4\HfmROW09? MYrpcoR2[2W|IHHwc5B1d3Orcx?= NILzXWgzPjR3OEm1Ny=>
C3H 10T1/2 mouse fibroblasts MkTST4lv[XOnIHHzd4F6 NYTFW2x2OjVizszN NYHLcXhQTE2VTx?= M1q1dZJm\HWlZYOgTIl{fG:wZTDIN{BidmRiSESgZYNmfHmuYYTpc44hdGW4ZXzzxsA> NXLqWXl3OjB3M{SzOFU>
H23 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWCyOUDPxE1? MXPEUXNQ MnTod4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= Mn\0NlA2OzR|NEW=
WM35 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3TYNlExKM7:TR?= MkDKSG1UVw>? MnzRd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NVrOPJFDOjB3M{SzOFU>
NIH 3T3 NVHpWIo6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml7oNVAh|ryP NGP0XJVFVVOR NEHZVIlld2W|IH7veEBp[X[nIHGgd4lodmmoaXPhcpQhcW6qaXLpeI9zgSCnZn\lZ5Q> MU[yNFU{PDN2NR?=
H838 NUPmXWlbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGP5XVUyOCEQvF2= NFPyfXpFVVOR M1X1dIRw\XNibn;0JIhifmViYTDzbYdvcW[rY3HueEBqdmirYnn0c5J6KGWoZnXjeC=> NYHGd403OjB3M{SzOFU>
H1395 NWjrW4p7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH:4dYwyOCEQvF2= NUfDTHU5TE2VTx?= NXewbJNO\G:nczDuc5QhcGG4ZTDhJJNq\26rZnnjZY51KGmwaHnibZRwenliZX\m[YN1 NWn5XVFrOjB3M{SzOFU>
Quiescent S2 NWi4dlFnU2mwYYPlJIF{e2G7 M3TCTFMxKM7:TR?= NEj3dnhFVVOR MXnjc41xdGW2ZXz5JIFjem:pYYTld{BVW0FvaX7keYNm\CCqeYDldoFk\XS7bHH0bY9vKG:oIFizT|Ru\TNiaHnzeI9v\XN? NXnZZolnOjF3MUi5NVU>
PC3 MWDBdI9xfG:|aYOgZZN{[Xl? NHfpWlYzOCEQvF2= M2XofmROW09? M4jNN4lv\HWlZYOgZZBweHSxc3nz NH;XbHYzOTdyOUGzNC=>
Du145 MW\BdI9xfG:|aYOgZZN{[Xl? MUmyNEDPxE1? MWTEUXNQ NGPrfW5qdmS3Y3XzJIFxd3C2b4Ppdy=> MVeyNVcxQTF|MB?=
LNCaP NYHtN4VbSXCxcITvd4l{KGG|c3H5 NUHXeFdFOjBizszN M4frZmROW09? MVLpcoR2[2W|IHHwc5B1d3Orcx?= MYKyNVcxQTF|MB?=
LAPC-4 MkHURZBweHSxc3nzJIF{e2G7 NF:wbVIzOCEQvF2= NU\QWFRZTE2VTx?= MYPpcoR2[2W|IHHwc5B1d3Orcx?= NVXJOmx6OjF5MEmxN|A>
LNCaP NHvrT2JHfW6ldHnvckBie3OjeR?= NEHpZWYzOCEQvF2= NG\ObpNFVVOR MX\k[YNz\WG|ZYOgVHNCKHOnY4LleIlwdiCjbnSgdFY2KGW6cILld5Nqd25ibHX2[Yx{ NUDOTmJ3OjF5MEmxN|A>
LAPC-4 NW\RNplQTnWwY4Tpc44h[XO|YYm= MlnRNlAh|ryP M1;PcmROW09? Morp[IVkemWjc3XzJHBUSSC|ZXPy[ZRqd25iYX7kJJA3PSCneIDy[ZN{cW:wIHzleoVtew>? MX:yNVcxQTF|MB?=
Kasumi-1 MlL3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYP+OVAh|ryP NG\Ze45FVVOR NYfjW4xDcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MlnRNlM{QTB3M{[=
SKNO-1 NIX1VlRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NU\uRox1hjVyIN88US=> NHvvVWFFVVOR Mkn3bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MV[yN|M6ODV|Nh?=
Kasumi-1 MWfLbY5ie2ViYYPzZZk> MVr+NVAh|ryP NWjIPZdLTE2VTx?= MYry[YR2[2W|IHX4dJJme3Orb36gc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|LNMgZ{1scXUEoHHu[OKh[mOuLUK= Mnm4NlM{QTB3M{[=
SKNO-1 NYDNTmh1U2mwYYPlJIF{e2G7 NX7iW5J[hjFyIN88US=> NWK1T|lCTE2VTx?= MmjSdoVlfWOnczDlfJBz\XO|aX;uJI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMz|CpIMuc2m2wrDhcoTDqGKlbD2y NYHkV2NDOjN|OUC1N|Y>
A549 NF;hXodHfW6ldHnvckBie3OjeR?= MmTENVAh|ryP NIrZ[IFFVVOR NEfFTZJmdmijbnPld{BucXSxdHnjJINifGG|dILvdIhm M2HJfVI1PzR4NUe0
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PC3 NWjJdmJrU2mwYYPlJIF{e2G7 MmfVNVAh|ryP NHrlOWdFVVOR MoXTbY5pcWKrdIOgdGdUUzQQsjD3bZRpKEmFNUCgc4YhPDlibl2= NHzIR|AyQDN6MUS0OC=>
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SUP B15 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoXiNVAh|ryP MnnBSG1UVw>? MnTVSWM2OD1zOUegcm0> Ml6yNVkxPjR5M{C=
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RS4;11 Mk\NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH;POIQyOCEQvF2= MYrEUXNQ MX\FR|UxRTZ3NDDuUS=> MmmzNVkxPjR5M{C=
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NALM-6 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NE[0XlMyOCEQvF2= NW[0SVBpTE2VTx?= MmTXSWM2OD12MkGgcm0> NXPxXYdkOTlyNkS3N|A>
MHH-CALL–3 M1Hrb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlvBNVAh|ryP NVnFZ2lUTE2VTx?= NHvNdVBGSzVyPUixNkBvVQ>? MmfnNVkxPjR5M{C=
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Molt-16 M2rOWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTsd4RGOTBizszN M4\wPGROW09? NH3rZ|NGSzVyPUK0NUBvVQ>? MVqxPVA3PDd|MB?=
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CCRFCEM NV\1VWU1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MorzNVAh|ryP NGfJdZBFVVOR NH65SoFGSzVyPUOyO{BvVQ>? MUexPVA3PDd|MB?=
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RD NF\vbY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYXKXHlCOTBizszN MWXJR|UxRjFyIN88US=> MWqyNFc1ODZ{Mx?=
Rh41 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3f1b|ExKM7:TR?= NGXNPJJKSzVyPUOzMlghdk1? M3jXVlIxPzRyNkKz
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BT-12 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkDDNVAh|ryP MkfLTWM2OD5zMDFOwG0> M2LjWVIxPzRyNkKz
CHLA-266 NILQXXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2fIWVExKM7:TR?= M3H1bGlEPTB;MT6yNkDPxE1? NYfoNZdNOjB5NEC2NlM>
TC-71 NH\VT5FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX2xNEDPxE1? M2DI[GlEPTB;Mj61NkDPxE1? M2\he|IxPzRyNkKz
CHLA-9 Mlv2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWOxNEDPxE1? MkHKTWM2OD13OUGgcm0> MoDDNlA4PDB4MkO=
CHLA-10 M4fuOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NET0ZoUyOCEQvF2= NIH5V2hKSzVyPUGwNkBvVQ>? M1TPVFIxPzRyNkKz
CHLA-258 NHnPU2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mmq4NVAh|ryP NYLoOIdUUUN3ME2xMlA2KM7:TR?= NEm4cW8zODd2ME[yNy=>
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NB-1643 NWPINmNHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M37WRVExKM7:TR?= M2m4NGlEPTB;NT60JO69VQ>? NF\BdJozODd2ME[yNy=>
NB-Ebc1 M3;OSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkDrNVAh|ryP MUfJR|UxRjFyIN88US=> M2j2dlIxPzRyNkKz
CHLA-90 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3GyZVExKM7:TR?= MX7JR|UxRjFyIN88US=> NIG4RXIzODd2ME[yNy=>
CHLA-136 M4TqV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M33iWlExKM7:TR?= NGXVfFZKSzVyPkGwJO69VQ>? MYKyNFc1ODZ{Mx?=
NALM-6 NYDCcpA{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M13JSVExKM7:TR?= MWHJR|UxRTJ4NTDuUS=> Mlf3NlA4PDB4MkO=
COG-LL-317 Ml\lS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGXhZWsyOCEQvF2= MYLJR|UxRTZwNEmgcm0> M{XyVFIxPzRyNkKz
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MOLT-4 MniwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkPDNVAh|ryP M3jRVWlEPTB;NECgcm0> NFrob3YzODd2ME[yNy=>
CCRF-CEM NF[wcJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXWxNEDPxE1? NYD5XmhMUUN3ME2yOlghdk1? MlTJNlA4PDB4MkO=
Kasumi-1 MoLMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWmxNEDPxE1? MlfCTWM2OD1zMEegcm0> NWDlR5dGOjB5NEC2NlM>
Karpas-299 NITWV4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoTUNVAh|ryP MoPJTWM2OD1{LkmzJO69VQ>? MoS5NlA4PDB4MkO=
Ramos-RA1 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnTZNVAh|ryP NH21W2ZKSzVyPUeuN|Uh|ryP MmjkNlA4PDB4MkO=
H1299 NVnXT4JOU2mwYYPlJIF{e2G7 M2LuPVExKM7:TR?= MVPpcohq[mm2czDJT2JMTS2rbnT1Z4VlKEGtdDDBZ5RqfmG2aX;u NGrYfI4zOTlyOE[xOi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cMET / p-cMET / p-AKT / p-ERK / p-rpS6 ; 

PubMed: 23022995     


A498 and 769P cell lines were treated with increasing concentrations of ARQ 197 for 24 h. Total c-Met expression remained relatively stable with drug treatment. Phosphorylated c-Met expression was highest in control (untreated cells) and was blocked with increasing concentrations of ARQ 197. Downstream changes in the c-Met pathway were seen predominantly in phosphorylated AKT, while decreased phosphorylated ERK1/2 and phosphorylated rpS6 (P70S6Kinase) occurred at higher c-Met inhibitor concentrations.

23022995
Growth inhibition assay
Cell viability; 

PubMed: 23598276     


Cells were treated with the increasing concentrations of tivantinib for 72 hr. Viable cells were assessed by CellTiter-Glo assay and were graphed relative to untreated cells. Experiments were carried out in sextuplet. The average values and SDs are shown. 

23598276
体内研究 ARQ-197处理 HT29,MKN-45,和MDA-MB-231三种移植瘤模型,肿瘤生长率分别降低66%,45%,和79%。ARQ-197按200 mg/kg剂量口服给药这三种移植瘤模型,显示体重都没有明显改变。药效学方面,ARQ-197作用于人类结肠移植瘤HT29,强抑制c-Met的磷酸化, ARQ-197按200 mg/kg剂量单独口服给药24小时后,c-Met自磷酸化强烈下降。总之,ARQ-197抑制人类c-Met依赖的移植瘤生长。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外c-Met SDS-PAGE 激酶试验:

100 ng重组c-Met蛋白和浓度不断增高ARQ-197在室温下预温育30分钟。随后,100 μM 聚Glu-Tyr底物和含5 μCi[γ-32P]ATP的不同浓度ATP加到反应混合物中。反应在室温下进行5分钟,然后加入5 μL SDS-聚丙烯酰胺胶,降低样本缓冲液。上样到7.5%丙烯酰胺胶上,进行SDS-PAGE。通过放射自显影观察到磷酸化的聚Glu-Tyr底物。通过光密度法测定c-Met活性。
细胞实验:[1]
- 合并
  • Cell lines: T29, MKN-45和MDA-MB-231细胞
  • Concentrations: 0.03-10 μM
  • Incubation Time: 24, 32,和48细胞
  • Method: HT29,MKN-45,和MDA-MB-231细胞按每孔5×103个接种在96孔板上,孔中有含10% FBS的培养基,在黑暗中过夜处理。第二天,用浓度不断增长的ARQ-197 (0.03-10 μM)在37oC下处理细胞24,32,和48 小时。ARQ-197处理后,移除培养基,细胞在含2 μg/mL Hoescht 33342的标签溶液(10 mM HEPES, 140 mM NaCl,和6 mM CaCl2)中温育至少10分钟, 用Annexin V-FITC(稀释500倍)和1 μg/mL碘化丙锭染色。进行高含量的图像采集和分析,每孔获取四个图像。 4,6-二脒基-2-苯基吲哚, FITC, 和罗丹明通道分别在16.7 ms/10%, 500 ms/35% ,和300 ms/30% 进行处理。处理图像,测定每组通道和每种情况下的阳性细胞数。此外,在有或者没有25,50,和100 μM ZvAD-FMK存在条件下,HT29细胞用浓度不断增加的ARQ-197处理32小时。所有实验重复进行三次。测定抑制c-Met是否导致细胞凋亡,当使用siRNA分解磷酸甘油醛脱氢酶(GAPDH)和c-Met时ARQ-197的作用效果。HT29, MKN-45,和MDA-MB-231细胞转染无靶点对照 siRNA, GAPDH靶点对照siRNA, 或met靶点siRNA。3天后,使用特点抗体测定c-Met, GAPDH, 和 β-actin表达水平。为了测定caspase依赖是否影响,HT29, MKN-45, 和MDA-MB-231细胞转染 met靶点 siRNA,进行2天。然后在有或没有浓度不断增高的ZvAD-FMK存在下再温育1天。无靶点siRNA和GAPDH siRNA也转染,作为对照。然后用Annexin V-FITC和碘化丙锭进行细胞染色,测定凋亡细胞百分数。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带HT29,MKN-45,或MDA-MB-231移植瘤的无胸腺裸鼠
  • Dosages: 200 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

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

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 369.42
化学式

C23H19N3O2

CAS号 905854-02-6
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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 Completed Drug: Tivantinib Malignant Pleural Mesothelioma|Nonsquamous Nonsmall Cell Neoplasm of Lung Armando Santoro MD|Istituto Clinico Humanitas January 2013 Phase 1|Phase 2
NCT01755767 Completed Drug: Tivantinib|Drug: Placebo Hepatocellular Carcinoma Daiichi Sankyo Inc.|ArQule Inc. (a wholly owned subsidiary of Merck Sharp and Dohme a subsidiary of Merck & Co. Inc.) December 27 2012 Phase 3

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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.

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c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID