TAE684 (NVP-TAE684) 化学構造
分子量: 614.2

高品質保証

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Quality Control & MSDS

製品説明

  • Compare ALK Inhibitors
    ALK製品生物活性の比較
  • 研究分野
  • TAE684 (NVP-TAE684)のメカニズム

製品の説明

生物活性

製品説明 TAE684 (NVP-TAE684)は、3nMのIC50による強力で選択的なALKキナーゼ阻害剤です。
ターゲット ALK
IC50 3 nM [1]
In vitro試験 TAE684 does not exhibit significant cross-reactivity against other kinases. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for TAE684. TAE684 treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines. [1] TAE684 markedly overcomes Crizotinib-resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis.[2] Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SCC-3 NFfGUVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rhOWlEPTB;MD6wNFAxPjB|IN88US=> NGS3b4lUSU6JRWK=
SF539 NVrzVI9OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwMECwOVY1KM7:TR?= M4DIRXNCVkeHUh?=
DEL M1LTN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnDNW4xUUN3ME2wMlAxODl{NzFOwG0> NWfZOnQzW0GQR1XS
NB1 NVH2SVhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j3NWlEPTB;MD6wNFE3OiEQvF2= NG\PVXBUSU6JRWK=
SR MmLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ftRWlEPTB;MD6wNFI4PyEQvF2= MW\TRW5ITVJ?
KARPAS-299 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwMEKzPFQh|ryP NIDjd4pUSU6JRWK=
MHH-CALL-2 NGjNfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33P[GlEPTB;MD6wNlk2OiEQvF2= NUn6WG5IW0GQR1XS
SU-DHL-1 NUXLb|R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\CNGlEPTB;MD6wOFg3PSEQvF2= MWrTRW5ITVJ?
A4-Fuk NFX3VnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;B[mlEPTB;MD6wOVU3PSEQvF2= M1e4bHNCVkeHUh?=
EW-1 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD2TWM2OD1yLkGwNlU3KM7:TR?= MnLCV2FPT0WU
NOS-1 NHGzPYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMUCyPVQh|ryP MU\TRW5ITVJ?
EW-16 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PHWGlEPTB;MD6xNFU3QCEQvF2= Mn7wV2FPT0WU
TE-11 M2DpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCyTpRKSzVyPUCuNVYxQTZizszN NInFR4ZUSU6JRWK=
SW982 NWLSWYRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwMU[0O|gh|ryP MXfTRW5ITVJ?
LAN-6 MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ThOGlEPTB;MD6xO|Q1OyEQvF2= M4jpR3NCVkeHUh?=
MZ1-PC M1\5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3JTWM2OD1yLkG3PFM2KM7:TR?= M{LZNnNCVkeHUh?=
KS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTVWFhbUUN3ME2wMlE6OzR|IN88US=> M1myVXNCVkeHUh?=
PSN1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DaSmlEPTB;MD6xPVY{OSEQvF2= NIe3T2hUSU6JRWK=
LC-2-ad MnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7KcFJKSzVyPUCuNVk3QTJizszN M4L2OXNCVkeHUh?=
COLO-320-HSR MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTsW2ttUUN3ME2wMlE6Pzd4IN88US=> NVrk[HRHW0GQR1XS
OPM-2 MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwMkK2Olkh|ryP NGfyeXFUSU6JRWK=
SK-NEP-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLHO5JKSzVyPUCuNlM2OjRizszN NY\tZpVYW0GQR1XS
ALL-PO MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwMkS1NlQh|ryP M{iweXNCVkeHUh?=
CMK M4fNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjLTWM2OD1yLkK1OVMh|ryP NXvoUW1YW0GQR1XS
NCI-H1648 MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPNeIdKSzVyPUCuNlc5PTVizszN MmHtV2FPT0WU
SIG-M5 MlvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjCfmlKSzVyPUCuNlkyPTlizszN M1X5SXNCVkeHUh?=
TGBC24TKB NEPEempIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT2bmYxUUN3ME2wMlMxOjF6IN88US=> NVzvO5o2W0GQR1XS
DOHH-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT0TIJ3UUN3ME2wMlMyOjB2IN88US=> NFXCOWRUSU6JRWK=
NB69 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXNZXJKSzVyPUCuN|E4QDdizszN NUXhdllOW0GQR1XS
MFH-ino NFPscmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrkeXA1UUN3ME2wMlMzPTJ|IN88US=> M{joOHNCVkeHUh?=
KP-N-RT-BM-1 NXjrR2I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1WyZWlEPTB;MD6zN|EzOyEQvF2= MYrTRW5ITVJ?
MONO-MAC-6 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwM{OyPVEh|ryP NVLBd|lWW0GQR1XS
ATN-1 NF7xZoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXxNJBPUUN3ME2wMlM{OzB|IN88US=> M4XKO3NCVkeHUh?=
NTERA-S-cl-D1 NITtSFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3ETWM2OD1yLkOzN|k3KM7:TR?= NYTafXAzW0GQR1XS
L-540 NUT4T|hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrXTWM2OD1yLkO2PVg5KM7:TR?= MnP4V2FPT0WU
GB-1 M1\YOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LFWWlEPTB;MD6zPFg3PyEQvF2= MlPDV2FPT0WU
MV-4-11 NHnsZpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7yTWM2OD1yLkO5OFQ3KM7:TR?= NE\VVYlUSU6JRWK=
KG-1 NEnse4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXEdZZKSzVyPUCuN|k2PjFizszN MnPSV2FPT0WU
OVCAR-4 NWjwOohMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXRSWZKSzVyPUCuOFA2PjlizszN MYjTRW5ITVJ?
NEC8 M4jZTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Pr[WlEPTB;MD60NVI6OiEQvF2= MnmxV2FPT0WU
SK-MM-2 MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwNEG2NFkh|ryP Ml;lV2FPT0WU
TE-8 M4rp[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4G5WWlEPTB;MD60Nlg5KM7:TR?= NHj4[nFUSU6JRWK=
697 Ml3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;5NmdKSzVyPUCuOFMzOTVizszN NVjEXop[W0GQR1XS
NB14 M2j6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGryN2tKSzVyPUCuOFM5OjZizszN MWXTRW5ITVJ?
GDM-1 NUHaUVBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHoSGlKSzVyPUCuOFcyOTZizszN NUXJOFY1W0GQR1XS
HUTU-80 NH7JRlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInC[|dKSzVyPUCuOFc{PzVizszN MWLTRW5ITVJ?
HL-60 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;CcotkUUN3ME2wMlQ5OTR{IN88US=> MmLEV2FPT0WU
OCI-AML2 M3zMfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDO[pNUUUN3ME2wMlQ5OzJ6IN88US=> NXXjZnA4W0GQR1XS
ML-2 M1HiSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwNEmwN|Eh|ryP NWW4fI0{W0GQR1XS
ES4 NX7JeIFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDWZnVKSzVyPUCuOFkyODlizszN MkHrV2FPT0WU
NCI-H747 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHYd3hkUUN3ME2wMlQ6QDlizszN MoPiV2FPT0WU
RL95-2 M4XqUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;FRWlEPTB;MD61NFEyOiEQvF2= MVzTRW5ITVJ?
TE-15 NVXLNnBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK1N4dKSzVyPUCuOVEyOjRizszN NIS5NHlUSU6JRWK=
TE-12 NEDyOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DuT2lEPTB;MD61N|M1QSEQvF2= NUSyOYNXW0GQR1XS
LB1047-RCC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rFUmlEPTB;MD61OFU1QSEQvF2= NYj1PG9EW0GQR1XS
LB831-BLC M1O5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjHOXVyUUN3ME2wMlU2ODJ|IN88US=> NXvZcnhbW0GQR1XS
NCI-H1355 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjqTWM2OD1yLkW1NVg1KM7:TR?= M{KzO3NCVkeHUh?=
CTV-1 M37kfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwNUW2NlQh|ryP NYLjVmQ{W0GQR1XS
RXF393 NVXRR5c6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjKb4lKSzVyPUCuOVU4QTRizszN NGD6e3pUSU6JRWK=
SW872 NHvS[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwNU[3NlQh|ryP MnrFV2FPT0WU
MPP-89 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf3TWM2OD1yLkW3PFg1KM7:TR?= MVfTRW5ITVJ?
RPMI-8226 M4LFc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYX5NotMUUN3ME2wMlY{PTJ4IN88US=> MnvOV2FPT0WU
LS-1034 NGHtfYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwNkO1PEDPxE1? NWHwUodpW0GQR1XS
SJSA-1 MlrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[xPFhKSzVyPUCuOlM4OjVizszN MWfTRW5ITVJ?
HOP-62 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvJcJVKSzVyPUCuOlUxOzNizszN MUPTRW5ITVJ?
KGN NXG2WnBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwNk[xOlgh|ryP M3K1N3NCVkeHUh?=
D-336MG NFq2NFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\RTWM2OD1yLk[2NVY6KM7:TR?= NVrLcotmW0GQR1XS
LS-411N NVHMWIVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DO[mlEPTB;MD62O|Q3OiEQvF2= Mn71V2FPT0WU
TE-1 NWXiT5FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjyTWM2OD1yLk[5NFc1KM7:TR?= MkXBV2FPT0WU
LB996-RCC NHLpOIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\nTWM2OD1yLk[5N|g6KM7:TR?= NXS0V3FYW0GQR1XS
TE-10 M2Kyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\hdmlEPTB;MD63NVQ6PiEQvF2= MmLMV2FPT0WU
NCI-SNU-16 MoLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjjTWM2OD1yLkeyOlY1KM7:TR?= M1\OZ3NCVkeHUh?=
ES8 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUCx[2NRUUN3ME2wMlc1QTd3IN88US=> MVrTRW5ITVJ?
COLO-800 NHOydVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\LbYtJUUN3ME2wMlc3Pjl3IN88US=> MmXsV2FPT0WU
ES6 MkLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzLfndKSzVyPUCuO|c2PTlizszN MVfTRW5ITVJ?
L-363 NWL6VopXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwOEKzO|Uh|ryP NEDPSIhUSU6JRWK=
NMC-G1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1voTmlEPTB;MD64N|I{OyEQvF2= Mk\KV2FPT0WU
LU-134-A NGTSd2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrPPWlqUUN3ME2wMlg{QTF{IN88US=> M3P0cHNCVkeHUh?=
SF268 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwOESwOFIh|ryP NFH5bIxUSU6JRWK=
KARPAS-45 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjvXlQ3UUN3ME2wMlg1OjZ|IN88US=> NFfuT|FUSU6JRWK=
TGW MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHMWGJxUUN3ME2wMlg2QDZ|IN88US=> NGHXSoJUSU6JRWK=
CHP-126 M{PnSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\ETWM2OD1yLki1PVU4KM7:TR?= MnLoV2FPT0WU
MOLT-16 M2HBUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwOEe1PFkh|ryP MYjTRW5ITVJ?
LB771-HNC MnP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\UeFZbUUN3ME2wMlg6PzV5IN88US=> M4PEcHNCVkeHUh?=
NALM-6 NGfpRZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLlTWM2OD1yLkmwO|M6KM7:TR?= NXvPd4dSW0GQR1XS
GCIY MnTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrIWoZzUUN3ME2wMlk2PTJ4IN88US=> M2LkZ3NCVkeHUh?=
IST-MES1 NFrub|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOxdZpRUUN3ME2wMlk5QDJ2IN88US=> NGO0N4pUSU6JRWK=
LB2241-RCC NYDMXldpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTBwOUi4OEDPxE1? MXHTRW5ITVJ?
BL-70 NH;NcXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzQZZVKSzVyPUCuPVk2OzVizszN M4rrVXNCVkeHUh?=
NB17 M1j2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rrd2lEPTB;MT6wNFY{QSEQvF2= M1XoUXNCVkeHUh?=
LXF-289 M1vwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r0cWlEPTB;MT6wN|A4PiEQvF2= MkDTV2FPT0WU
TK10 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDQTWM2OD1zLkC1NFY{KM7:TR?= MULTRW5ITVJ?
K5 NHX1e49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j5RmlEPTB;MT6wOlI4PCEQvF2= NUnyWXk6W0GQR1XS
NCI-H716 NVXoZmNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwMEeyOVkh|ryP NUTscmJ5W0GQR1XS
HCE-T NFTF[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fMdWlEPTB;MT6wPFgyQSEQvF2= NGDPUZhUSU6JRWK=
GI-1 NUH6dZhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzVelRCUUN3ME2xMlA6Pzl6IN88US=> MlPNV2FPT0WU
KARPAS-422 NH7wTWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\XTWM2OD1zLkGwNFIzKM7:TR?= NXfWXo9{W0GQR1XS
TE-9 NVXD[4FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrjNWJKSzVyPUGuNVE{OjhizszN M1izTHNCVkeHUh?=
SF126 NWfhXndNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXmxUJdpUUN3ME2xMlEyPTZ6IN88US=> M1jpSXNCVkeHUh?=
BB30-HNC NF7NSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zxOmlEPTB;MT6xN|EyOiEQvF2= NXmy[lZMW0GQR1XS
NCI-H1304 NUP1S4NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LmUGlEPTB;MT6xN|M{QCEQvF2= Mn;xV2FPT0WU
HEL MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;I[4JFUUN3ME2xMlE1QDl3IN88US=> NFrpd4hUSU6JRWK=
HAL-01 M{e3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwMUWyPFMh|ryP MWLTRW5ITVJ?
SK-LMS-1 Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLXTWM2OD1zLkG1PVc1KM7:TR?= NH6wcJFUSU6JRWK=
SW954 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnLOmNKSzVyPUGuNVk2PjdizszN NYfxUXRHW0GQR1XS
D-283MED M2XFOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7Jbpc6UUN3ME2xMlIzOzd7IN88US=> NGWx[2tUSU6JRWK=
NCI-H1882 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX6wdHl{UUN3ME2xMlI{QDlizszN MkDpV2FPT0WU
GI-ME-N NXuycFdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFwMkWyNFgh|ryP MlfQV2FPT0WU
SK-PN-DW M4DEPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjITWM2OD1zLkK2N|Q5KM7:TR?= M{iwNHNCVkeHUh?=
C2BBe1 NWqzbFlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLBTWM2OD1zLkK5NVE4KM7:TR?= MWPTRW5ITVJ?
A704 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm2fXFqUUN3ME2xMlMzPjh7IN88US=> NIW0V41USU6JRWK=
KALS-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTFwM{SwPEDPxE1? M{HtWHNCVkeHUh?=
ETK-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwM{S0PFkh|ryP NGX4TGZUSU6JRWK=
LB647-SCLC NF3xfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFwM{S5PFYh|ryP MYrTRW5ITVJ?
OCUB-M MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XNOmlEPTB;MT6zOlE1OyEQvF2= M3;SRXNCVkeHUh?=
NCI-H720 M4n1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PBbWlEPTB;MT6zOlM4QCEQvF2= NIKzOFdUSU6JRWK=
NB13 M1Ljdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFwM{eyPVMh|ryP MYfTRW5ITVJ?
GR-ST Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\DTWM2OD1zLkO4O|U4KM7:TR?= NHT2N3lUSU6JRWK=
DU-4475 MkTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD0TWM2OD1zLkS1PFU{KM7:TR?= MWPTRW5ITVJ?
HCC2157 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFwNE[2OVkh|ryP MmDFV2FPT0WU
RKO M2XuPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVji[VlyUUN3ME2xMlQ6QTJ{IN88US=> NIjHcJVUSU6JRWK=
LS-123 M{Xv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTFwNUG1PVQh|ryP MXzTRW5ITVJ?
NCI-H69 NH62WplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTFwNUW4NVEh|ryP MULTRW5ITVJ?
SW962 M4m4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XH[WlEPTB;MT61OlE{KM7:TR?= MVTTRW5ITVJ?
PF-382 Ml;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLWTWM2OD1zLkW2PVYh|ryP MnfFV2FPT0WU
A101D MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvkcW1SUUN3ME2xMlU4OTF|IN88US=> NFTMVXRUSU6JRWK=
NB10 M{\6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPuTWM2OD1zLkW3N|kzKM7:TR?= M4DoUHNCVkeHUh?=
NB5 Mm[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwNUi0O|Yh|ryP MYPTRW5ITVJ?
HCE-4 MmH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHvPFhbUUN3ME2xMlYxQDVizszN NVPRb3plW0GQR1XS
HT-144 M2jFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP1coVVUUN3ME2xMlY{OTlizszN MlXkV2FPT0WU
NCI-H524 NGrG[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;PXFZKSzVyPUGuOlQ{ODdizszN MnHQV2FPT0WU
NKM-1 NVnWc3FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjnTWM2OD1zLk[4OlYh|ryP NEHkbXNUSU6JRWK=
KURAMOCHI NUPvPZdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXJTWM2OD1zLk[5OVc{KM7:TR?= M33vSnNCVkeHUh?=
NCI-H187 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHL5WmlKSzVyPUGuO|AxOzZizszN NHzF[ppUSU6JRWK=
U-266 NYrBO3dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPTTWM2OD1zLkezPFQzKM7:TR?= NGLxeFhUSU6JRWK=
BL-41 Mkf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLETWM2OD1zLke2NlczKM7:TR?= NFjvZlNUSU6JRWK=
SK-N-DZ NEDZdHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;yR|NuUUN3ME2xMlc5OzB7IN88US=> NULoVYpbW0GQR1XS
Daudi MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fZVGlEPTB;MT63PFk3PyEQvF2= MYnTRW5ITVJ?
CPC-N MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnyTmRKSzVyPUGuPFUxQTZizszN MkjtV2FPT0WU
EM-2 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof2TWM2OD1zLki1NUDPxE1? NFS3XGNUSU6JRWK=
HCC1187 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PRfGlEPTB;MT64OlI1OSEQvF2= MUjTRW5ITVJ?
LP-1 NGjuVWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwOEexOFMh|ryP MVnTRW5ITVJ?
CAS-1 NX;3SodiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[3XJZKSzVyPUGuPVgzQTlizszN NFS5dWxUSU6JRWK=
NB7 M2PsV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJwMEC1OVUh|ryP M3zmR3NCVkeHUh?=
VA-ES-BJ Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIq5dmJKSzVyPUKuNFE2OTNizszN NHTYWmFUSU6JRWK=
SNU-C2B MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHQfmpKSzVyPUKuNFM{PTFizszN NXTQNXlvW0GQR1XS
LOXIMVI NXv4PIVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fmW2lEPTB;Mj6wOlc5PiEQvF2= NVS2eGFYW0GQR1XS
NCI-H1581 NYnuWGsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO3PHRKSzVyPUKuNVE2PTlizszN M2XTcHNCVkeHUh?=
IST-SL2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTJwMUK0OFUh|ryP MlnaV2FPT0WU
NOMO-1 Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDmXWdKSzVyPUKuNVc3QDNizszN MoXwV2FPT0WU
TE-6 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13zbGlEPTB;Mj6xPVA2KM7:TR?= NWr4[|RLW0GQR1XS
NCI-H526 M{\VVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP1PFVJUUN3ME2yMlE6OTRzIN88US=> NYTsc3dZW0GQR1XS
MSTO-211H NWHHbY5NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJwMkCwOFEh|ryP MlfCV2FPT0WU
LS-513 NHvWSotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJwMkKyOlkh|ryP NIracYxUSU6JRWK=
NCI-SNU-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJwM{OyOVYh|ryP M2nuVXNCVkeHUh?=
BB65-RCC NWTSTXc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\3TWM2OD1{LkO3OFk{KM7:TR?= NXPhWIp2W0GQR1XS
GT3TKB MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknRTWM2OD1{LkO5PVczKM7:TR?= NEjiT25USU6JRWK=
OS-RC-2 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJwNEKzOFEh|ryP MmHoV2FPT0WU
NCI-H2126 NIrkco9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3WUFhKSzVyPUKuOFM3PzRizszN Mor1V2FPT0WU
SK-UT-1 M1fLN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJwNEe0Olch|ryP M{XnfXNCVkeHUh?=
DMS-114 M4nTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr5UW5IUUN3ME2yMlYyPTJ2IN88US=> NYqwbWplW0GQR1XS
ONS-76 Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3LcGU2UUN3ME2yMlY{PjRzIN88US=> M1PSVnNCVkeHUh?=
8-MG-BA M4\3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3yTWM2OD1{Lk[1OFE1KM7:TR?= Mn7qV2FPT0WU
BOKU MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jPb2lEPTB;Mj63Nlc3PCEQvF2= NYLSZo5tW0GQR1XS
LAMA-84 M2frT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDaTWM2OD1{Lke5PVEzKM7:TR?= MnPzV2FPT0WU
ES1 NH\3bWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJwOEG4NFQh|ryP MUPTRW5ITVJ?
NCI-H1395 NIDZOXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTJwOEKwNVIh|ryP MYDTRW5ITVJ?
A388 NFL6eW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTjWmg{UUN3ME2yMlk3OTdizszN MWLTRW5ITVJ?
NCCIT MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfGbXhpUUN3ME2zMlA5QDZ{IN88US=> MXfTRW5ITVJ?
HD-MY-Z NEXYRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTNwMUOyNFMh|ryP NVPacVJtW0GQR1XS
NCI-H510A NV;FdG15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfXTWM2OD1|LkG4PVQ{KM7:TR?= NWTuOWg4W0GQR1XS
NCI-N87 NHTOTlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;ZTWM2OD1|LkKwNFIh|ryP MW\TRW5ITVJ?
SCLC-21H NYS5Zms{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzkTmNOUUN3ME2zMlI3QDV7IN88US=> Mn\6V2FPT0WU
SH-4 MoHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTNwMki3PVch|ryP NFzPd2hUSU6JRWK=
QIMR-WIL MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH34bVlKSzVyPUOuN|I5PDlizszN M1XQSHNCVkeHUh?=
KM12 M2TTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LGZWlEPTB;Mz6zN|U1PCEQvF2= MVrTRW5ITVJ?
ST486 NYSwWYdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LvWGlEPTB;Mz61N|g5OyEQvF2= Mn;PV2FPT0WU
HC-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLXOmpKSzVyPUOuOlIxOjhizszN M2PMb3NCVkeHUh?=
BV-173 M1\4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTNwNkSwPFgh|ryP MWnTRW5ITVJ?
EW-24 NH3CPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNwNk[0N|Qh|ryP NVTUfnVkW0GQR1XS
LU-65 MlzmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTNwNki3NUDPxE1? NXeyV3VFW0GQR1XS
ECC4 M4XzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDISVZUUUN3ME2zMlc4PTZizszN NFqxWYdUSU6JRWK=
ARH-77 NHziNlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnNW2FKSzVyPUSuNVExPjdizszN NXryS2RPW0GQR1XS
BC-3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnZSWxIUUN3ME20MlE{ODZ6IN88US=> MYnTRW5ITVJ?
SNB75 MojKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTRwMk[xPUDPxE1? MkHkV2FPT0WU
MEG-01 NFK5[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPKNWNKSzVyPUSuNlc1OTlizszN MknFV2FPT0WU
NCI-H1417 NV;VZY83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\pSmdKSzVyPUSuNlg1PDNizszN NHzLS5hUSU6JRWK=
MDA-MB-134-VI MmHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\rcHk{UUN3ME20MlMxPjBzIN88US=> NEO4fIdUSU6JRWK=
Becker MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTRwNEezN|Yh|ryP MYnTRW5ITVJ?
DMS-153 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonZTWM2OD12Lk[2OFc2KM7:TR?= M1viTXNCVkeHUh?=
TGBC1TKB M{i3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{SwUmlEPTB;ND62PFUyPSEQvF2= M{PJfHNCVkeHUh?=
EW-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;HOIRKSzVyPUSuO|YzPDhizszN NXfpbYhTW0GQR1XS
KE-37 NFrVclVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTRwOE[xPVYh|ryP MWTTRW5ITVJ?
NCI-H23 M3jiemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7IdWhKSzVyPUSuPFczOjdizszN NIjGbmpUSU6JRWK=
MC116 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfPTWM2OD12Lkm0NVI3KM7:TR?= M{PaVXNCVkeHUh?=
NH-12 NGTOfpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n3cGlEPTB;ND65OlQ{QSEQvF2= M1rBPHNCVkeHUh?=
CTB-1 NYjWR4p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLzXpRQUUN3ME20Mlk4PzJzIN88US=> MlHGV2FPT0WU
KM-H2 M{jDc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTVwMEWzNlMh|ryP M4nJS3NCVkeHUh?=
MOLT-4 NXjrPGxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTVwMUG4N{DPxE1? NYDyfmVbW0GQR1XS
NCI-H2141 NWfWd21XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTVwMUSyOlgh|ryP NIrFZ2ZUSU6JRWK=
EB-3 M3jWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTVwMUe1NFQh|ryP NHfLNXRUSU6JRWK=
NCI-H1522 NELENmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HlUWlEPTB;NT6yOlMzOiEQvF2= MYPTRW5ITVJ?
MRK-nu-1 MnfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTVwNEO2N|Mh|ryP MWLTRW5ITVJ?
no-11 NVTRPY4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjWbWN1UUN3ME21MlQ4ODh5IN88US=> MV7TRW5ITVJ?
CESS NIrIfGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLRcopKSzVyPUWuOVgxOzRizszN MkXBV2FPT0WU
KMOE-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi1TWM2OD13LkW4OlU6KM7:TR?= NFviPWdUSU6JRWK=
REH M17GNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHmeHNKSzVyPU[uNlU3OThizszN NHfKdYFUSU6JRWK=
KU812 NYjMS5VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jDZWlEPTB;Nj60Nlc6OSEQvF2= MXLTRW5ITVJ?
SK-N-FI NF7odJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTZwNkC2O|Qh|ryP MUXTRW5ITVJ?
MMAC-SF NVm1O4RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTdwME[0PVIh|ryP NVzkUXIyW0GQR1XS
RCC10RGB NHHYTZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF35dG5KSzVyPUeuNlI6PzdizszN M17RTXNCVkeHUh?=
NCI-H322M MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rnTmlEPTB;Nz6zN|M{PSEQvF2= NELQW|RUSU6JRWK=
NB6 M33iTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTdwNUS4PVkh|ryP NYPKOZBVW0GQR1XS
MN-60 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTdwNkmyNVUh|ryP MXrTRW5ITVJ?
NCI-H1092 NF;0T29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn5XGJbUUN3ME24MlAyPzN2IN88US=> NHPkOIZUSU6JRWK=
EKVX MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWwTWM2OD16LkS3NFY3KM7:TR?= M{fDSnNCVkeHUh?=
D-263MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXrWYNCUUN3ME24MlU2Ozl4IN88US=> MV\TRW5ITVJ?
NCI-H209 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRThwNkSwNFYh|ryP NU\vTFFmW0GQR1XS
IST-SL1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRThwOEm4PVIh|ryP MomzV2FPT0WU
ACN NWTlTVJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTlwMUmxOVch|ryP NX[zVJlRW0GQR1XS
MHH-PREB-1 MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3GWIdKSzVyPUmuNlEzOTlizszN M1LBRnNCVkeHUh?=
EW-11 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTlwNkWzPVYh|ryP MYfTRW5ITVJ?
KASUMI-1 M4PQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEK2U3VKSzVyPUmuO|g4PyEQvF2= M4fv[XNCVkeHUh?=
KINGS-1 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfRc4FKSzVyPUGwMlI{PDdizszN NXi1UVR1W0GQR1XS
EVSA-T M2nU[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT5Zo93UUN3ME2xNE4{OTl{IN88US=> MlPlV2FPT0WU
DSH1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[2T2lEPTB;MUCuN|k4OiEQvF2= MXrTRW5ITVJ?
COLO-824 NFfZenZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHOXoFEUUN3ME2xNE45PjZ7IN88US=> NX;QXZlpW0GQR1XS
K052 NITBVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nwOmlEPTB;MUCuPVMzOiEQvF2= M13VWHNCVkeHUh?=
SK-MEL-2 NEn5e2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrTTWM2OD1zMD65PVM6KM7:TR?= MWPTRW5ITVJ?

... Click to View More Cell Line Experimental Data

In vivo試験 After 4 weeks of treatment with TAE684 at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. TAE684 treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression. [1] TAE684 also shows impressive antitumor activity against H3122 CR xenograft tumors. [2] Furthermore, treatment with TAE684 improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q, whereas Crizotinib has little effect on either phenotype. [3]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

In vitro Enzyme Assays. All in vitro enzyme assays are done at Upstate Biotechnology with the exception of InsR and IGF-1R. To determine the IC50 of TAE684 against InsR and IGF-1R a homogeneous time-resolved fluorescence assay is performed. ATP (10 mM) and 20 mg/ml biotinylated PolyEY (Glu, Tyr 4:1) are combined with 50 nL of serial dilutions of TAE684 (10-500 nM) and 4 ng of InsR enzyme in the presence of the kinase reaction buffer (20 mM Tris譎Cl, pH 7.5/10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA). Assays are incubated for 1 hour at ambient temperature. Reactions are terminated by adding 10 mL of the detection solution containing 50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/mL Eu3+ cryptate-labeled anti-phosphotyrosine antibody Mab PT66-K, and 5 mg/mL Streptavidin-XLent. The reaction is incubated for half an hour, and fluorescence signals are read on Analyst GT.

細胞アッセイ: [1]

細胞株 Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, Bcr-Abl, or TEL-kinase fusion constructs.
濃度 1 nM-10 μM
反応時間 2–3 days
実験の流れ Cells are seeded in 384-well plates (2.5×104 cells per well) and incubated with serial dilutions of TAE684 or DMSO for 2–3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.

動物実験: [1]

動物モデル Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice.
製剤 Resuspended in 10% 1-methyl-2-pyrrolidinone/90% polyethylene glycol 300 solution
投薬量 1, 3, and 10 mg/kg
投与方法 Once daily by oral gavage for 3 weeks

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 TAE684 (NVP-TAE684) SDF
分子量 614.2
化学式

C30H40ClN7O3S

CAS No. 761439-42-3
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 3 mg/mL (4.88 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol, pH 4 10 mg/mL
* <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 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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