TAE684 (NVP-TAE684) 化学構造
分子量: 614.2

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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 NWXwTXZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjmUZRKSzVyPUCuNFAxODZyMzFOwG0> NWjHeFBTW0GQR1XS
SF539 NFewU3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm2bWtRUUN3ME2wMlAxODV4NDFOwG0> Ml;lV2FPT0WU
DEL MmHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jUTWlEPTB;MD6wNFA6OjdizszN M1TpXHNCVkeHUh?=
NB1 NHfXU3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMECxOlIh|ryP MkX5V2FPT0WU
SR NIXhb4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7JSmgzUUN3ME2wMlAxOjd5IN88US=> MoPNV2FPT0WU
KARPAS-299 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LJU2lEPTB;MD6wNlM5PCEQvF2= NFP3fIFUSU6JRWK=
MHH-CALL-2 NUPQe4VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwMEK5OVIh|ryP MnntV2FPT0WU
SU-DHL-1 M{njV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTBwMES4OlUh|ryP NUnYSG5uW0GQR1XS
A4-Fuk NHTrUXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG2UWhrUUN3ME2wMlA2PTZ3IN88US=> NGnJZWJUSU6JRWK=
EW-1 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXaTXRKSzVyPUCuNVAzPTZizszN NV;DeGZ1W0GQR1XS
NOS-1 NFTFS45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnPTWM2OD1yLkGwNlk1KM7:TR?= M2K2[HNCVkeHUh?=
EW-16 NH[2XVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj6fYdsUUN3ME2wMlExPTZ6IN88US=> MWXTRW5ITVJ?
TE-11 M3jJcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1znSGlEPTB;MD6xOlA6PiEQvF2= NXfWSGdJW0GQR1XS
SW982 NGC1XWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwMU[0O|gh|ryP NETz[3hUSU6JRWK=
LAN-6 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTQTWM2OD1yLkG3OFQ{KM7:TR?= M16wTHNCVkeHUh?=
MZ1-PC MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M163bmlEPTB;MD6xO|g{PSEQvF2= MVnTRW5ITVJ?
KS-1 MorSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnK5TWM2OD1yLkG5N|Q{KM7:TR?= NVfPcHd[W0GQR1XS
PSN1 NE\lV49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2mwZmlEPTB;MD6xPVY{OSEQvF2= NUDOT3RTW0GQR1XS
LC-2-ad Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLXUW5KSzVyPUCuNVk3QTJizszN MmXxV2FPT0WU
COLO-320-HSR M{j3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nkXmlEPTB;MD6xPVc4PiEQvF2= NWL1dXVzW0GQR1XS
OPM-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2CwN2lEPTB;MD6yNlY3QSEQvF2= MWnTRW5ITVJ?
SK-NEP-1 NYWzWZI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMkO1NlQh|ryP MmDOV2FPT0WU
ALL-PO M1XkeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIr6ZnJKSzVyPUCuNlQ2OjRizszN NETHVXhUSU6JRWK=
CMK MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHsV21OUUN3ME2wMlI2PTNizszN MXvTRW5ITVJ?
NCI-H1648 NI\TWYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMke4OVUh|ryP NIf3OZhUSU6JRWK=
SIG-M5 M3zmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIi2[HVKSzVyPUCuNlkyPTlizszN MnG3V2FPT0WU
TGBC24TKB M1TUUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPL[nRKSzVyPUCuN|AzOThizszN MljNV2FPT0WU
DOHH-2 NEK2fI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2niS2lEPTB;MD6zNVIxPCEQvF2= NYHDcJBNW0GQR1XS
NB69 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fyNmlEPTB;MD6zNVc5PyEQvF2= NHjrUXBUSU6JRWK=
MFH-ino NFrUdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PSTWlEPTB;MD6zNlUzOyEQvF2= M3K1ZXNCVkeHUh?=
KP-N-RT-BM-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELjOZJKSzVyPUCuN|MyOjNizszN M3\oOXNCVkeHUh?=
MONO-MAC-6 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDuTWM2OD1yLkOzNlkyKM7:TR?= NYnue2MxW0GQR1XS
ATN-1 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXUUINKSzVyPUCuN|M{ODNizszN MXvTRW5ITVJ?
NTERA-S-cl-D1 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnpTWM2OD1yLkOzN|k3KM7:TR?= NFPR[oxUSU6JRWK=
L-540 M1[yRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTBT2l5UUN3ME2wMlM3QTh6IN88US=> M2nDSHNCVkeHUh?=
GB-1 M4\yT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX72eXVXUUN3ME2wMlM5QDZ5IN88US=> M{TFXXNCVkeHUh?=
MV-4-11 MnzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPFTmpZUUN3ME2wMlM6PDR4IN88US=> NWLrTGo5W0GQR1XS
KG-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwM{m1OlEh|ryP NH;JfWZUSU6JRWK=
OVCAR-4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTyTWM2OD1yLkSwOVY6KM7:TR?= NInJU4hUSU6JRWK=
NEC8 M1rLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\1eGQ5UUN3ME2wMlQyOjl{IN88US=> MlTzV2FPT0WU
SK-MM-2 M{G3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzQPGhpUUN3ME2wMlQyPjB7IN88US=> M1;lZnNCVkeHUh?=
TE-8 NWm1dIgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[1VXpyUUN3ME2wMlQzQDhizszN NIW2fmxUSU6JRWK=
697 MlT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLjTWM2OD1yLkSzNlE2KM7:TR?= MnvQV2FPT0WU
NB14 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwNEO4NlYh|ryP NFXnUlBUSU6JRWK=
GDM-1 M4fGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfZTWM2OD1yLkS3NVE3KM7:TR?= NHz0d3dUSU6JRWK=
HUTU-80 MoPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jPV2lEPTB;MD60O|M4PSEQvF2= MVXTRW5ITVJ?
HL-60 M372[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\hXlhKSzVyPUCuOFgyPDJizszN MkDSV2FPT0WU
OCI-AML2 M1PVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PQ[mlEPTB;MD60PFMzQCEQvF2= M{XGd3NCVkeHUh?=
ML-2 NHPKcWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13NRmlEPTB;MD60PVA{OSEQvF2= M{f6NHNCVkeHUh?=
ES4 M3ntbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTVTWM2OD1yLkS5NVA6KM7:TR?= MnfOV2FPT0WU
NCI-H747 M1u0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwNEm4PUDPxE1? MnzQV2FPT0WU
RL95-2 NWLnNo5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXUdW1KSzVyPUCuOVAyOTJizszN MYLTRW5ITVJ?
TE-15 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XIXGlEPTB;MD61NVEzPCEQvF2= Mn3RV2FPT0WU
TE-12 M4frZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[xTWM2OD1yLkWzN|Q6KM7:TR?= NFfmV2pUSU6JRWK=
LB1047-RCC NFzH[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXS3VFRHUUN3ME2wMlU1PTR7IN88US=> NH;hbI9USU6JRWK=
LB831-BLC NIrKZ3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwNUWwNlMh|ryP MlvuV2FPT0WU
NCI-H1355 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYewS4NuUUN3ME2wMlU2OTh2IN88US=> MVTTRW5ITVJ?
CTV-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPycWtKSzVyPUCuOVU3OjRizszN MV;TRW5ITVJ?
RXF393 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DEcWlEPTB;MD61OVc6PCEQvF2= MkPGV2FPT0WU
SW872 M4fRTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwNU[3NlQh|ryP M2XhSXNCVkeHUh?=
MPP-89 MnTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTQSYpKSzVyPUCuOVc5QDRizszN M2fNTnNCVkeHUh?=
RPMI-8226 NInsPHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPBTWM2OD1yLk[zOVI3KM7:TR?= NGK2TIJUSU6JRWK=
LS-1034 NV3WT41ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTqW|VKSzVyPUCuOlM2QCEQvF2= M1i5XHNCVkeHUh?=
SJSA-1 M37lSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwNkO3NlUh|ryP M4HqbXNCVkeHUh?=
HOP-62 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT1TWM2OD1yLk[1NFM{KM7:TR?= NGLtcY5USU6JRWK=
KGN NUDjb41wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHLTWM2OD1yLk[2NVY5KM7:TR?= MoX5V2FPT0WU
D-336MG MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTETWM2OD1yLk[2NVY6KM7:TR?= NXHCbW9[W0GQR1XS
LS-411N Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nyOmlEPTB;MD62O|Q3OiEQvF2= NIHRUmFUSU6JRWK=
TE-1 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorTTWM2OD1yLk[5NFc1KM7:TR?= MmLVV2FPT0WU
LB996-RCC NH;ieodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\qTWM2OD1yLk[5N|g6KM7:TR?= NUPGe2UxW0GQR1XS
TE-10 MorYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XITGlEPTB;MD63NVQ6PiEQvF2= NYPVUIhHW0GQR1XS
NCI-SNU-16 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjXfJR1UUN3ME2wMlczPjZ2IN88US=> MoexV2FPT0WU
ES8 Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnXVVdKSzVyPUCuO|Q6PzVizszN M{fRXnNCVkeHUh?=
COLO-800 NXzOOVZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e2c2lEPTB;MD63OlY6PSEQvF2= MUDTRW5ITVJ?
ES6 M2PxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m2fmlEPTB;MD63O|U2QSEQvF2= NELsNVZUSU6JRWK=
L-363 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF62OHBKSzVyPUCuPFI{PzVizszN M3XYT3NCVkeHUh?=
NMC-G1 M4qxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwOEOyN|Mh|ryP M{LzbnNCVkeHUh?=
LU-134-A M{PUXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILlZ2tKSzVyPUCuPFM6OTJizszN NV\NbVZoW0GQR1XS
SF268 MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L4UmlEPTB;MD64OFA1OiEQvF2= NIjBb3FUSU6JRWK=
KARPAS-45 M2DGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:1OGlEPTB;MD64OFI3OyEQvF2= NH2zTZNUSU6JRWK=
TGW MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULLRndCUUN3ME2wMlg2QDZ|IN88US=> Mn;oV2FPT0WU
CHP-126 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGmyOmhKSzVyPUCuPFU6PTdizszN NHTuUZNUSU6JRWK=
MOLT-16 NYW3[WlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17P[mlEPTB;MD64O|U5QSEQvF2= MmH6V2FPT0WU
LB771-HNC MmPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD2TWM2OD1yLki5O|U4KM7:TR?= NXjvNYR2W0GQR1XS
NALM-6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnq5TWM2OD1yLkmwO|M6KM7:TR?= M3jiZXNCVkeHUh?=
GCIY NW[2b2xWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[3W3A4UUN3ME2wMlk2PTJ4IN88US=> M{PmdXNCVkeHUh?=
IST-MES1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[wTWM2OD1yLkm4PFI1KM7:TR?= Mn7iV2FPT0WU
LB2241-RCC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[1PJRrUUN3ME2wMlk5QDRizszN M{C2bnNCVkeHUh?=
BL-70 NHq4empIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLyTWM2OD1yLkm5OVM2KM7:TR?= NGXFbpFUSU6JRWK=
NB17 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uyXWlEPTB;MT6wNFY{QSEQvF2= MU\TRW5ITVJ?
LXF-289 NWTzZZFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDLSXo2UUN3ME2xMlA{ODd4IN88US=> MoO3V2FPT0WU
TK10 M371fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXLTXRKSzVyPUGuNFUxPjNizszN MoLRV2FPT0WU
K5 NWDDd3VCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwME[yO|Qh|ryP NUjxPGlQW0GQR1XS
NCI-H716 M3L1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDoNm5qUUN3ME2xMlA4OjV7IN88US=> NInBfY9USU6JRWK=
HCE-T NVPWXHdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jMTmlEPTB;MT6wPFgyQSEQvF2= MnPTV2FPT0WU
GI-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTuZll4UUN3ME2xMlA6Pzl6IN88US=> MYTTRW5ITVJ?
KARPAS-422 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f4WmlEPTB;MT6xNFAzOiEQvF2= NIfFeFBUSU6JRWK=
TE-9 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLwTWM2OD1zLkGxN|I5KM7:TR?= NHrMcHdUSU6JRWK=
SF126 M2qwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT4TWM2OD1zLkGxOVY5KM7:TR?= MV3TRW5ITVJ?
BB30-HNC MkLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmH5TWM2OD1zLkGzNVEzKM7:TR?= MXXTRW5ITVJ?
NCI-H1304 M2GzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFwMUOzN|gh|ryP NYjpRoVMW0GQR1XS
HEL NVrEOVVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r2NmlEPTB;MT6xOFg6PSEQvF2= NFvJSYNUSU6JRWK=
HAL-01 NGTuc49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PLd2lEPTB;MT6xOVI5OyEQvF2= MkfDV2FPT0WU
SK-LMS-1 M3jGd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M160WWlEPTB;MT6xOVk4PCEQvF2= MlG1V2FPT0WU
SW954 M37lWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnUS3dKUUN3ME2xMlE6PTZ5IN88US=> Mn:0V2FPT0WU
D-283MED Mk\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILIPYxKSzVyPUGuNlI{PzlizszN NYTycoFYW0GQR1XS
NCI-H1882 NHXtOGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnPTWM2OD1zLkKzPFkh|ryP NGDpdZNUSU6JRWK=
GI-ME-N MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwMkWyNFgh|ryP MkmyV2FPT0WU
SK-PN-DW M3fNPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwMk[zOFgh|ryP M{fNcHNCVkeHUh?=
C2BBe1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnIN4tNUUN3ME2xMlI6OTF5IN88US=> MnXuV2FPT0WU
A704 NXSyOZd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\3W2lEPTB;MT6zNlY5QSEQvF2= M{PtXXNCVkeHUh?=
KALS-1 M1S3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHtTIRKSzVyPUGuN|QxQCEQvF2= MmG4V2FPT0WU
ETK-1 M{fIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwM{S0PFkh|ryP NVPRdnN6W0GQR1XS
LB647-SCLC NEXseWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1i0N2lEPTB;MT6zOFk5PiEQvF2= MX;TRW5ITVJ?
OCUB-M NGPPeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFwM{[xOFMh|ryP M{O5W3NCVkeHUh?=
NCI-H720 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlThTWM2OD1zLkO2N|c5KM7:TR?= MmPVV2FPT0WU
NB13 NWrZUJNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwM{eyPVMh|ryP NXT0WXNyW0GQR1XS
GR-ST MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwM{i3OVch|ryP NUHQPW55W0GQR1XS
DU-4475 NIrQS3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnGXnozUUN3ME2xMlQ2QDV|IN88US=> NVXCT|l4W0GQR1XS
HCC2157 NWLOUGp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3vTWM2OD1zLkS2OlU6KM7:TR?= NWe0SZV2W0GQR1XS
RKO MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj5RW5KSzVyPUGuOFk6OjJizszN NGPXPWNUSU6JRWK=
LS-123 MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\TZmlEPTB;MT61NVU6PCEQvF2= NEDGTnRUSU6JRWK=
NCI-H69 M4DwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj1TWM2OD1zLkW1PFEyKM7:TR?= NYrEVGozW0GQR1XS
SW962 NWjXWlZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTFwNU[xN{DPxE1? Mn7vV2FPT0WU
PF-382 MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r4RWlEPTB;MT61Olk3KM7:TR?= MX7TRW5ITVJ?
A101D MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL5PFdKSzVyPUGuOVcyOTNizszN M1G0NXNCVkeHUh?=
NB10 NUPjb5ByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1G5XWlEPTB;MT61O|M6OiEQvF2= NVPKdVdVW0GQR1XS
NB5 NY\6e5ExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HhOGlEPTB;MT61PFQ4PiEQvF2= M13mbXNCVkeHUh?=
HCE-4 MkXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTFwNkC4OUDPxE1? NETlRlBUSU6JRWK=
HT-144 NETGdldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPP[YF{UUN3ME2xMlY{OTlizszN Mn[4V2FPT0WU
NCI-H524 NVLFb|RZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwNkSzNFch|ryP NVXJfZRRW0GQR1XS
NKM-1 Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\PTWM2OD1zLk[4OlYh|ryP M2rlNnNCVkeHUh?=
KURAMOCHI M1HhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\mTWM2OD1zLk[5OVc{KM7:TR?= NXHpUlg2W0GQR1XS
NCI-H187 M3P3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETmSIRKSzVyPUGuO|AxOzZizszN NU\pdVFYW0GQR1XS
U-266 NUXmVGNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIntWo1KSzVyPUGuO|M5PDJizszN MmfwV2FPT0WU
BL-41 NFP5[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDIT4trUUN3ME2xMlc3Ojd{IN88US=> NUTtOlNzW0GQR1XS
SK-N-DZ NFnxcYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYW1PWY5UUN3ME2xMlc5OzB7IN88US=> MmD4V2FPT0WU
Daudi NX:4SXR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDmdo1KSzVyPUGuO|g6PjdizszN Mn35V2FPT0WU
CPC-N MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfTZYdKSzVyPUGuPFUxQTZizszN NFL3OVBUSU6JRWK=
EM-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm0TWM2OD1zLki1NUDPxE1? MlnOV2FPT0WU
HCC1187 MknWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvBTWM2OD1zLki2NlQyKM7:TR?= MWjTRW5ITVJ?
LP-1 M3GxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTGeWs1UUN3ME2xMlg4OTR|IN88US=> M3HzbHNCVkeHUh?=
CAS-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjVb2JKSzVyPUGuPVgzQTlizszN NGe3[lFUSU6JRWK=
NB7 NWO4[VRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJwMEC1OVUh|ryP MYXTRW5ITVJ?
VA-ES-BJ MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJwMEG1NVMh|ryP M2HFWXNCVkeHUh?=
SNU-C2B M{jz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjicoFKSzVyPUKuNFM{PTFizszN NWfzR2FCW0GQR1XS
LOXIMVI NVi2[5k{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr1TVhPUUN3ME2yMlA3Pzh4IN88US=> NH;hW5BUSU6JRWK=
NCI-H1581 Ml;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTUWnVSUUN3ME2yMlEyPTV7IN88US=> NETPe|dUSU6JRWK=
IST-SL2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnCWZhnUUN3ME2yMlEzPDR3IN88US=> NG\3S4RUSU6JRWK=
NOMO-1 M4HLSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmToTWM2OD1{LkG3Olg{KM7:TR?= NWfkfVRYW0GQR1XS
TE-6 NVXIZnJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJwMUmwOUDPxE1? MXLTRW5ITVJ?
NCI-H526 NHTlcVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJwMUmxOFEh|ryP NFrOSnhUSU6JRWK=
MSTO-211H MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWexc4MzUUN3ME2yMlIxODRzIN88US=> MWTTRW5ITVJ?
LS-513 M1L6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfNTWM2OD1{LkKyNlY6KM7:TR?= NUK2dFJiW0GQR1XS
NCI-SNU-1 NXS5[Gh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPLVXN[UUN3ME2yMlM{OjV4IN88US=> MnHZV2FPT0WU
BB65-RCC NU\OVoVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkGyTWM2OD1{LkO3OFk{KM7:TR?= M4rreHNCVkeHUh?=
GT3TKB NHXDd5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHVW4dWUUN3ME2yMlM6QTd{IN88US=> M1XrfHNCVkeHUh?=
OS-RC-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTJwNEKzOFEh|ryP M{DEXnNCVkeHUh?=
NCI-H2126 NULUenpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkG4TWM2OD1{LkSzOlc1KM7:TR?= NUfVUnhIW0GQR1XS
SK-UT-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7VWmF6UUN3ME2yMlQ4PDZ5IN88US=> NIPDPVlUSU6JRWK=
DMS-114 NX7iU|E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3DR2tOUUN3ME2yMlYyPTJ2IN88US=> NYO3SJpYW0GQR1XS
ONS-76 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG0TWM2OD1{Lk[zOlQyKM7:TR?= NGrVWm9USU6JRWK=
8-MG-BA NYD5UFFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml62TWM2OD1{Lk[1OFE1KM7:TR?= NIXWXJBUSU6JRWK=
BOKU NEXUNW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17vcGlEPTB;Mj63Nlc3PCEQvF2= M1PXcnNCVkeHUh?=
LAMA-84 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnBZ3lSUUN3ME2yMlc6QTF{IN88US=> Mlv6V2FPT0WU
ES1 MljPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jsOWlEPTB;Mj64NVgxPCEQvF2= NFPyWmZUSU6JRWK=
NCI-H1395 NXTqU|E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJwOEKwNVIh|ryP NGmxZZBUSU6JRWK=
A388 NXTtd3doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fvO2lEPTB;Mj65OlE4KM7:TR?= MnzTV2FPT0WU
NCCIT MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjtTWM2OD1|LkC4PFYzKM7:TR?= NYXLbphRW0GQR1XS
HD-MY-Z MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYKzZnRoUUN3ME2zMlE{OjB|IN88US=> NFz5dYZUSU6JRWK=
NCI-H510A Mnn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzkTWM2OD1|LkG4PVQ{KM7:TR?= NVv3TmF1W0GQR1XS
NCI-N87 NVmzT|FGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoO0TWM2OD1|LkKwNFIh|ryP MoDOV2FPT0WU
SCLC-21H MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6wNpVCUUN3ME2zMlI3QDV7IN88US=> MYHTRW5ITVJ?
SH-4 NFnxWZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;Ve2FpUUN3ME2zMlI5Pzl5IN88US=> Mn7XV2FPT0WU
QIMR-WIL NXqwfm1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfFcXRKSzVyPUOuN|I5PDlizszN NFvkNWlUSU6JRWK=
KM12 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK2dWdWUUN3ME2zMlM{PTR2IN88US=> NXLIRY04W0GQR1XS
ST486 NWT5bmViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj2TWM2OD1|LkWzPFg{KM7:TR?= MYPTRW5ITVJ?
HC-1 M{XqNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmOyTWM2OD1|Lk[yNFI5KM7:TR?= MnTDV2FPT0WU
BV-173 NIDaNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGD3[45KSzVyPUOuOlQxQDhizszN MVLTRW5ITVJ?
EW-24 NWHmZYo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3Q[GdCUUN3ME2zMlY3PDN2IN88US=> NUO3enh{W0GQR1XS
LU-65 NV7zbplHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7YTWM2OD1|Lk[4O|Eh|ryP NITPcVRUSU6JRWK=
ECC4 NITh[HhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTNwN{e1OkDPxE1? MYrTRW5ITVJ?
ARH-77 Ml36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf5NGpSUUN3ME20MlEyODZ5IN88US=> M1jXfnNCVkeHUh?=
BC-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnBTWM2OD12LkGzNFY5KM7:TR?= MoTDV2FPT0WU
SNB75 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jRPGlEPTB;ND6yOlE6KM7:TR?= MofJV2FPT0WU
MEG-01 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTRwMke0NVkh|ryP MlnqV2FPT0WU
NCI-H1417 NGrWOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTRwMki0OFMh|ryP NU\PeYJZW0GQR1XS
MDA-MB-134-VI MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVm5bWJWUUN3ME20MlMxPjBzIN88US=> NFfTd5dUSU6JRWK=
Becker M3HFZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTRwNEezN|Yh|ryP MnXsV2FPT0WU
DMS-153 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTRwNk[0O|Uh|ryP NYHTc2llW0GQR1XS
TGBC1TKB NW\CU4NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTRwNki1NVUh|ryP MUTTRW5ITVJ?
EW-3 NFfnfY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTRwN{[yOFgh|ryP MWjTRW5ITVJ?
KE-37 M1PWO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjwXVZKUUN3ME20Mlg3OTl4IN88US=> M{f1bnNCVkeHUh?=
NCI-H23 MlKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PoN2lEPTB;ND64O|IzPyEQvF2= NUDnUm5zW0GQR1XS
MC116 NXfncXhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTRwOUSxNlYh|ryP M1jle3NCVkeHUh?=
NH-12 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTRwOU[0N|kh|ryP NF;MNHhUSU6JRWK=
CTB-1 NWLFUXlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPwWIlvUUN3ME20Mlk4PzJzIN88US=> MVzTRW5ITVJ?
KM-H2 NYG1UVdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTVwMEWzNlMh|ryP NYPkU|VwW0GQR1XS
MOLT-4 M2nJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTVwMUG4N{DPxE1? NXLMU|VpW0GQR1XS
NCI-H2141 NWDxeXhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zUN2lEPTB;NT6xOFI3QCEQvF2= MknlV2FPT0WU
EB-3 MorQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHlWJNsUUN3ME21MlE4PTB2IN88US=> MofqV2FPT0WU
NCI-H1522 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlu1TWM2OD13LkK2N|IzKM7:TR?= NXyzS3E1W0GQR1XS
MRK-nu-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTVwNEO2N|Mh|ryP M2fZTHNCVkeHUh?=
no-11 NVXpe5lNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYi2d|FrUUN3ME21MlQ4ODh5IN88US=> NUfzO4tWW0GQR1XS
CESS MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu0[YVlUUN3ME21MlU5ODN2IN88US=> MoS0V2FPT0WU
KMOE-2 NV;ycIoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfvdYQ1UUN3ME21MlU5PjV7IN88US=> Mk\jV2FPT0WU
REH MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3JTZNMUUN3ME22MlI2PjF6IN88US=> MoPwV2FPT0WU
KU812 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PJTGlEPTB;Nj60Nlc6OSEQvF2= MVTTRW5ITVJ?
SK-N-FI M4P1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX0TWM2OD14Lk[wOlc1KM7:TR?= NF;Vbo5USU6JRWK=
MMAC-SF NFrt[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTdwME[0PVIh|ryP NVjlbmRTW0GQR1XS
RCC10RGB NEDsOIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTdwMkK5O|ch|ryP MXzTRW5ITVJ?
NCI-H322M NVnSSXpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTdwM{OzN|Uh|ryP M2j5WXNCVkeHUh?=
NB6 M{jv[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXCO45KSzVyPUeuOVQ5QTlizszN MlrtV2FPT0WU
MN-60 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTdwNkmyNVUh|ryP M3vJT3NCVkeHUh?=
NCI-H1092 NVfaWYUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRThwMEG3N|Qh|ryP NV6yOIc6W0GQR1XS
EKVX M1L0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPuPJFKSzVyPUiuOFcxPjZizszN NFXhUI9USU6JRWK=
D-263MG MlPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PyNmlEPTB;OD61OVM6PiEQvF2= Ml7vV2FPT0WU
NCI-H209 NEix[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRThwNkSwNFYh|ryP MnXrV2FPT0WU
IST-SL1 MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzkdWdxUUN3ME24Mlg6QDl{IN88US=> MkHaV2FPT0WU
ACN Ml7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnyT3FYUUN3ME25MlE6OTV5IN88US=> NW\BUGNtW0GQR1XS
MHH-PREB-1 NUe1c3cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLSbXZKSzVyPUmuNlEzOTlizszN NUKxUFJoW0GQR1XS
EW-11 NEnR[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP0fIhKSzVyPUmuOlU{QTZizszN MlTYV2FPT0WU
KASUMI-1 NHjUfXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L4SWlEPTB;OT63PFc4KM7:TR?= MmfnV2FPT0WU
KINGS-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HZSWlEPTB;MUCuNlM1PyEQvF2= MkTQV2FPT0WU
EVSA-T MmjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PZWmlEPTB;MUCuN|E6OiEQvF2= NUPCWmV4W0GQR1XS
DSH1 MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPHTWM2OD1zMD6zPVczKM7:TR?= M16wXnNCVkeHUh?=
COLO-824 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFyLki2Olkh|ryP MWnTRW5ITVJ?
K052 NHrSTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFyLkmzNlIh|ryP M4XsUHNCVkeHUh?=
SK-MEL-2 M1LrcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\LbY9XUUN3ME2xNE46QTN7IN88US=> NG\YT3NUSU6JRWK=

... 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

カスタマーフィードバック (4)


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Source Cancer Res , 2011, 71, 4920-31. TAE684 (NVP-TAE684) purchased from Selleck
Method Western blot
Cell Lines H3122 cells
Concentrations 100 nmol/L
Incubation Time 6 h
Results Figure A shows that the primary adaptors for PI3K activation are IRS1 and IRS2 in H3122 mouse xenografts. Interestingly, treatment with TAE-684 eliminates these interactions, suggesting that ALK signals to PI3K via IRS2 and IRS1. This is consistent with previous reports suggesting that NPM-ALK signals to PI3K via IRS proteins. The finding that IRS proteins were utilized to activate PI3K suggested that these cells might activate PI3K in response to IGF-I. Indeed, treatment of H3122 cells with IGF-I, but not EGF or HGF, rescued PI3K-AKT signaling with TAE-684 treatment (Fig. B).

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Rating
Source Neoplasia, 2011, 13, 704-15. TAE684 (NVP-TAE684) purchased from Selleck
Method Western blot
Cell Lines H-1299 cells
Concentrations 0.03-1uM
Incubation Time
Results Treatment efficiently inhibited the cell proliferation and phospho-Y1604 ALK expression of H694R or E1384K mutant ALK, but also to a degree higher than that of wild-type ALK.

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Rating
Source Neoplasia, 2011, 13, 704-15. TAE684 (NVP-TAE684) purchased from Selleck
Method Xenograft
Cell Lines mice
Concentrations
Incubation Time 4 weeks
Results Consistently, TAE684 treatment repressed H694R- and E1384K-induced tumor growth compared with DMSO control.

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Rating
Source Neoplasia, 2011, 13, 704-15. TAE684 (NVP-TAE684) purchased from Selleck
Method Cell Proliferation Assay
Cell Lines H-1299 cells
Concentrations 0-3 uM
Incubation Time
Results Treatment efficiently inhibited the cell proliferation and phospho- Y1604 ALK expression of H694R or E1384K mutant ALK, but also to a degree higher than that of wild-type ALK.

文献中の引用 (17)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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