TAE684 (NVP-TAE684)

TAE684 (NVP-TAE684)は一種の有効で、選択性的なALK阻害剤で、無細胞試験でIC50値が3 nMです。TAE684 (NVP-TAE684)は、ALKに作用する選択性はInsRに作用する選択性より100倍が高くなります。

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TAE684 (NVP-TAE684) 化学構造
分子量: 614.2

高品質保証

カスタマーフィードバック(4)

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)は一種の有効で、選択性的なALK阻害剤で、無細胞試験でIC50値が3 nMです。TAE684 (NVP-TAE684)は、ALKに作用する選択性はInsRに作用する選択性より100倍が高くなります。
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 MkPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfRUXFKSzVyPUCuNFAxODZyMzFOwG0> MYjTRW5ITVJ?
SF539 NULMXFdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\XTWM2OD1yLkCwNFU3PCEQvF2= MX3TRW5ITVJ?
DEL MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\FTWM2OD1yLkCwNFkzPyEQvF2= MXfTRW5ITVJ?
NB1 M{HvbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3SzbWlEPTB;MD6wNFE3OiEQvF2= MlPVV2FPT0WU
SR MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXxb4JKSzVyPUCuNFAzPzdizszN MmXJV2FPT0WU
KARPAS-299 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;0VlJKSzVyPUCuNFI{QDRizszN M324Z3NCVkeHUh?=
MHH-CALL-2 NWLPdHhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX6UW1KSzVyPUCuNFI6PTJizszN MofDV2FPT0WU
SU-DHL-1 NG\6[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfXe3ZPUUN3ME2wMlA1QDZ3IN88US=> MYnTRW5ITVJ?
A4-Fuk NGTONYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTySJIxUUN3ME2wMlA2PTZ3IN88US=> NV7aUHJ3W0GQR1XS
EW-1 NIH4TYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXTTWM2OD1yLkGwNlU3KM7:TR?= MV\TRW5ITVJ?
NOS-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq3UlU5UUN3ME2wMlExOjl2IN88US=> NE\I[4xUSU6JRWK=
EW-16 M2TINmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwMUC1Olgh|ryP NGPIUIJUSU6JRWK=
TE-11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzBTWM2OD1yLkG2NFk3KM7:TR?= M2fa[nNCVkeHUh?=
SW982 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfOTWM2OD1yLkG2OFc5KM7:TR?= NYjyVXZDW0GQR1XS
LAN-6 NH3ZSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnkNlFtUUN3ME2wMlE4PDR|IN88US=> M3TMU3NCVkeHUh?=
MZ1-PC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWL1RmtMUUN3ME2wMlE4QDN3IN88US=> NF;qSmxUSU6JRWK=
KS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37SOWlEPTB;MD6xPVM1OyEQvF2= NXT0U|NrW0GQR1XS
PSN1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvXWo9nUUN3ME2wMlE6PjNzIN88US=> NYPFcY83W0GQR1XS
LC-2-ad NFn5XodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHi5RnBKSzVyPUCuNVk3QTJizszN MnW1V2FPT0WU
COLO-320-HSR Mn;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHyb3hRUUN3ME2wMlE6Pzd4IN88US=> MV;TRW5ITVJ?
OPM-2 MnfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPnOmpKSzVyPUCuNlI3PjlizszN M2OzW3NCVkeHUh?=
SK-NEP-1 NFzFZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT4TWM2OD1yLkKzOVI1KM7:TR?= M{TaNHNCVkeHUh?=
ALL-PO NUTWNndDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjuUGxKSzVyPUCuNlQ2OjRizszN NFm0[mxUSU6JRWK=
CMK NUjBV3c6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XjT2lEPTB;MD6yOVU{KM7:TR?= M3rCVXNCVkeHUh?=
NCI-H1648 NITwRVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zP[mlEPTB;MD6yO|g2PSEQvF2= NXLIc3kxW0GQR1XS
SIG-M5 NEXvXmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwMkmxOVkh|ryP NWeyTpZFW0GQR1XS
TGBC24TKB NGH0fotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jWZWlEPTB;MD6zNFIyQCEQvF2= M2jQN3NCVkeHUh?=
DOHH-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwM{GyNFQh|ryP MXLTRW5ITVJ?
NB69 Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF61SGlKSzVyPUCuN|E4QDdizszN MlSwV2FPT0WU
MFH-ino M2XaUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4qxSWlEPTB;MD6zNlUzOyEQvF2= NUPFS49PW0GQR1XS
KP-N-RT-BM-1 MlLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[wR4JKSzVyPUCuN|MyOjNizszN MkjDV2FPT0WU
MONO-MAC-6 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DETWlEPTB;MD6zN|I6OSEQvF2= NEHGeZVUSU6JRWK=
ATN-1 NXTRSpJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn0c5RxUUN3ME2wMlM{OzB|IN88US=> Ml;FV2FPT0WU
NTERA-S-cl-D1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwM{OzPVYh|ryP M4e1d3NCVkeHUh?=
L-540 MmjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwM{[5PFgh|ryP NEfwO5FUSU6JRWK=
GB-1 M170bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;uNmlEPTB;MD6zPFg3PyEQvF2= MWHTRW5ITVJ?
MV-4-11 NXzQN3FUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnPXHNKSzVyPUCuN|k1PDZizszN NVnQUlZ[W0GQR1XS
KG-1 MojxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorTTWM2OD1yLkO5OVYyKM7:TR?= NVH5boxEW0GQR1XS
OVCAR-4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XLb2lEPTB;MD60NFU3QSEQvF2= NHjXWpNUSU6JRWK=
NEC8 M{PvN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITKNGJKSzVyPUCuOFEzQTJizszN Mn\FV2FPT0WU
SK-MM-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnvTWM2OD1yLkSxOlA6KM7:TR?= MWnTRW5ITVJ?
TE-8 Mn\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PnPWlEPTB;MD60Nlg5KM7:TR?= MWjTRW5ITVJ?
697 NIPTXVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\jTWM2OD1yLkSzNlE2KM7:TR?= NXrGN5VtW0GQR1XS
NB14 MlHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXzcVVKSzVyPUCuOFM5OjZizszN M2jONHNCVkeHUh?=
GDM-1 NH71SGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwNEexNVYh|ryP Mnj0V2FPT0WU
HUTU-80 NWrI[IVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwNEezO|Uh|ryP MXPTRW5ITVJ?
HL-60 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPiVII6UUN3ME2wMlQ5OTR{IN88US=> MnuzV2FPT0WU
OCI-AML2 M{TPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrWd|VLUUN3ME2wMlQ5OzJ6IN88US=> NILkb3VUSU6JRWK=
ML-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwNEmwN|Eh|ryP MlfkV2FPT0WU
ES4 NGLPXXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwNEmxNFkh|ryP NGPWWmVUSU6JRWK=
NCI-H747 NWLJcHAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPNTWM2OD1yLkS5PFkh|ryP MlrVV2FPT0WU
RL95-2 NV7VTIc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1GySGlEPTB;MD61NFEyOiEQvF2= MYXTRW5ITVJ?
TE-15 M{W1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwNUGxNlQh|ryP MmTMV2FPT0WU
TE-12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLPPXhKSzVyPUCuOVM{PDlizszN MnuzV2FPT0WU
LB1047-RCC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnXSmhKSzVyPUCuOVQ2PDlizszN NF3i[ppUSU6JRWK=
LB831-BLC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DZNGlEPTB;MD61OVAzOyEQvF2= MkfsV2FPT0WU
NCI-H1355 M{TJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPZbVlKSzVyPUCuOVUyQDRizszN MW\TRW5ITVJ?
CTV-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwNUW2NlQh|ryP NEnKfYpUSU6JRWK=
RXF393 NVnmU28{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHVbm9tUUN3ME2wMlU2Pzl2IN88US=> Ml;JV2FPT0WU
SW872 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e3N2lEPTB;MD61OlczPCEQvF2= M2XyNnNCVkeHUh?=
MPP-89 Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTOTWM2OD1yLkW3PFg1KM7:TR?= NYPNOnNxW0GQR1XS
RPMI-8226 M2fmd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7obIxKSzVyPUCuOlM2OjZizszN NInVO|NUSU6JRWK=
LS-1034 M4TyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwNkO1PEDPxE1? MUTTRW5ITVJ?
SJSA-1 M2nwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\TWWlEPTB;MD62N|czPSEQvF2= NGnjfolUSU6JRWK=
HOP-62 NHXWRXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u4[2lEPTB;MD62OVA{OyEQvF2= NVvhXVBEW0GQR1XS
KGN MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nT[2lEPTB;MD62OlE3QCEQvF2= MXHTRW5ITVJ?
D-336MG M3[0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PhSGlEPTB;MD62OlE3QSEQvF2= M{XIW3NCVkeHUh?=
LS-411N NEH6dXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwNke0OlIh|ryP MorhV2FPT0WU
TE-1 NU\keGdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXWRVF{UUN3ME2wMlY6ODd2IN88US=> M4m5eHNCVkeHUh?=
LB996-RCC NGPEWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwNkmzPFkh|ryP MVzTRW5ITVJ?
TE-10 MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTBwN{G0PVYh|ryP NYXXUJpDW0GQR1XS
NCI-SNU-16 NX\rRpk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK4OpVHUUN3ME2wMlczPjZ2IN88US=> NWXzSXNDW0GQR1XS
ES8 NHvEVIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrobpFKSzVyPUCuO|Q6PzVizszN M{nWPXNCVkeHUh?=
COLO-800 M1[5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW5U|lKSzVyPUCuO|Y3QTVizszN NV[wR4F3W0GQR1XS
ES6 NXuw[WRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnaTWM2OD1yLke3OVU6KM7:TR?= NHLOfoJUSU6JRWK=
L-363 NWjnc4xvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwOEKzO|Uh|ryP NUnrfId5W0GQR1XS
NMC-G1 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jMWmlEPTB;MD64N|I{OyEQvF2= MWPTRW5ITVJ?
LU-134-A MoLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPBeWdKSzVyPUCuPFM6OTJizszN MYnTRW5ITVJ?
SF268 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljlTWM2OD1yLki0NFQzKM7:TR?= MoH0V2FPT0WU
KARPAS-45 Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NICzRnZKSzVyPUCuPFQzPjNizszN MYnTRW5ITVJ?
TGW MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPtPXdKSzVyPUCuPFU5PjNizszN MYjTRW5ITVJ?
CHP-126 NV;3PZhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHTNnh6UUN3ME2wMlg2QTV5IN88US=> NIW5PHJUSU6JRWK=
MOLT-16 MmjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3WTWM2OD1yLki3OVg6KM7:TR?= MorGV2FPT0WU
LB771-HNC MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonsTWM2OD1yLki5O|U4KM7:TR?= NUPNb2d[W0GQR1XS
NALM-6 Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwOUC3N|kh|ryP M{DQVHNCVkeHUh?=
GCIY NFHEfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LhfmlEPTB;MD65OVUzPiEQvF2= NYWxd3ZEW0GQR1XS
IST-MES1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUX2cYFwUUN3ME2wMlk5QDJ2IN88US=> M1HaeXNCVkeHUh?=
LB2241-RCC NHXycpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPJTWM2OD1yLkm4PFQh|ryP MUPTRW5ITVJ?
BL-70 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLMTZR7UUN3ME2wMlk6PTN3IN88US=> MV7TRW5ITVJ?
NB17 NF7EdFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXUeoxLUUN3ME2xMlAxPjN7IN88US=> MmjKV2FPT0WU
LXF-289 MmDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHWWINoUUN3ME2xMlA{ODd4IN88US=> MVjTRW5ITVJ?
TK10 M2HDOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFwMEWwOlMh|ryP MV;TRW5ITVJ?
K5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLDTWM2OD1zLkC2Nlc1KM7:TR?= MnHKV2FPT0WU
NCI-H716 MoqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XucmlEPTB;MT6wO|I2QSEQvF2= NGrJR|dUSU6JRWK=
HCE-T M1HqV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n6[WlEPTB;MT6wPFgyQSEQvF2= MoL6V2FPT0WU
GI-1 MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmSyTWM2OD1zLkC5O|k5KM7:TR?= MVHTRW5ITVJ?
KARPAS-422 M3KyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfNZlFKSzVyPUGuNVAxOjJizszN NH\j[|lUSU6JRWK=
TE-9 NVPqSpVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofVTWM2OD1zLkGxN|I5KM7:TR?= NGC5R3hUSU6JRWK=
SF126 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFwMUG1Olgh|ryP MUPTRW5ITVJ?
BB30-HNC MlzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFwMUOxNVIh|ryP NXu5S5FyW0GQR1XS
NCI-H1304 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTFwMUOzN|gh|ryP M2faS3NCVkeHUh?=
HEL M{HBXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwMUS4PVUh|ryP MVLTRW5ITVJ?
HAL-01 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojaTWM2OD1zLkG1Nlg{KM7:TR?= Ml3FV2FPT0WU
SK-LMS-1 NYP6RZhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXw[JN{UUN3ME2xMlE2QTd2IN88US=> MUTTRW5ITVJ?
SW954 NUDY[402T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\EcGlEPTB;MT6xPVU3PyEQvF2= NWTk[lhKW0GQR1XS
D-283MED MoXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13NOWlEPTB;MT6yNlM4QSEQvF2= MXjTRW5ITVJ?
NCI-H1882 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMkO4PUDPxE1? MnHZV2FPT0WU
GI-ME-N NFXqc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2GybGlEPTB;MT6yOVIxQCEQvF2= MVLTRW5ITVJ?
SK-PN-DW NV7zOpBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFwMk[zOFgh|ryP NV3STYtkW0GQR1XS
C2BBe1 M3jxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfITWM2OD1zLkK5NVE4KM7:TR?= MmfMV2FPT0WU
A704 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S0TmlEPTB;MT6zNlY5QSEQvF2= MWLTRW5ITVJ?
KALS-1 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonwTWM2OD1zLkO0NFgh|ryP NGP2O|RUSU6JRWK=
ETK-1 MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWK1UnJFUUN3ME2xMlM1PDh7IN88US=> MUXTRW5ITVJ?
LB647-SCLC M3rrT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jMdGlEPTB;MT6zOFk5PiEQvF2= M4\y[nNCVkeHUh?=
OCUB-M M3vFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHziU4xKSzVyPUGuN|YyPDNizszN M2LrRnNCVkeHUh?=
NCI-H720 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwM{[zO|gh|ryP MV\TRW5ITVJ?
NB13 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwM{eyPVMh|ryP M1zpWXNCVkeHUh?=
GR-ST M3vRXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HUcGlEPTB;MT6zPFc2PyEQvF2= MYHTRW5ITVJ?
DU-4475 MkHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFwNEW4OVMh|ryP MlrQV2FPT0WU
HCC2157 M{\jTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPIcGoyUUN3ME2xMlQ3PjV7IN88US=> NF31TmJUSU6JRWK=
RKO MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTkSJNKSzVyPUGuOFk6OjJizszN MkLaV2FPT0WU
LS-123 M{Cx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD3TWM2OD1zLkWxOVk1KM7:TR?= NVyxUI05W0GQR1XS
NCI-H69 M4P3bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXFR|BKSzVyPUGuOVU5OTFizszN NWPMOVZlW0GQR1XS
SW962 M{Xae2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwNU[xN{DPxE1? NX3pZ3gzW0GQR1XS
PF-382 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvTZ2dKSzVyPUGuOVY6PiEQvF2= MVPTRW5ITVJ?
A101D MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor5TWM2OD1zLkW3NVE{KM7:TR?= M1XZdnNCVkeHUh?=
NB10 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkixTWM2OD1zLkW3N|kzKM7:TR?= M{X1THNCVkeHUh?=
NB5 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrITWM2OD1zLkW4OFc3KM7:TR?= MYHTRW5ITVJ?
HCE-4 MlvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkCzTWM2OD1zLk[wPFUh|ryP NXvUNmdbW0GQR1XS
HT-144 NELBNWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVniT2RZUUN3ME2xMlY{OTlizszN MY\TRW5ITVJ?
NCI-H524 M4jRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPTTWM2OD1zLk[0N|A4KM7:TR?= MWjTRW5ITVJ?
NKM-1 NFrtWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnVS5lMUUN3ME2xMlY5PjZizszN NHHZdXlUSU6JRWK=
KURAMOCHI NHPOeHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoW4TWM2OD1zLk[5OVc{KM7:TR?= M{O4WnNCVkeHUh?=
NCI-H187 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfUdIhqUUN3ME2xMlcxODN4IN88US=> MVjTRW5ITVJ?
U-266 NVXidYtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTFwN{O4OFIh|ryP MkeyV2FPT0WU
BL-41 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PMS2lEPTB;MT63OlI4OiEQvF2= MWPTRW5ITVJ?
SK-N-DZ MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\FWoZKSzVyPUGuO|g{ODlizszN MlewV2FPT0WU
Daudi NXPETVJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPHTWM2OD1zLke4PVY4KM7:TR?= MlPTV2FPT0WU
CPC-N MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jqdmlEPTB;MT64OVA6PiEQvF2= NYjiPWVWW0GQR1XS
EM-2 M1;Tdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLDTWM2OD1zLki1NUDPxE1? MVHTRW5ITVJ?
HCC1187 M4nVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHpbHJKSzVyPUGuPFYzPDFizszN M1fLb3NCVkeHUh?=
LP-1 M{HiXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHMbW5KSzVyPUGuPFcyPDNizszN Mlm3V2FPT0WU
CAS-1 M3HrSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnQ[IZKSzVyPUGuPVgzQTlizszN MnHxV2FPT0WU
NB7 NYm1cHBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWiwe4VLUUN3ME2yMlAxPTV3IN88US=> M2XDe3NCVkeHUh?=
VA-ES-BJ NXnvWFc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\I[HlKSzVyPUKuNFE2OTNizszN M33aSnNCVkeHUh?=
SNU-C2B NX3HPWVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DHeGlEPTB;Mj6wN|M2OSEQvF2= MorkV2FPT0WU
LOXIMVI MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUmyTJF4UUN3ME2yMlA3Pzh4IN88US=> NE\VPVFUSU6JRWK=
NCI-H1581 NXSxWFZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrSfIVZUUN3ME2yMlEyPTV7IN88US=> MkDUV2FPT0WU
IST-SL2 NFzMUIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGSwUW9KSzVyPUKuNVI1PDVizszN MljtV2FPT0WU
NOMO-1 NFPzTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjPSJZKSzVyPUKuNVc3QDNizszN NGr0UIZUSU6JRWK=
TE-6 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\0WHVKSzVyPUKuNVkxPSEQvF2= NXOwe2JHW0GQR1XS
NCI-H526 NHWzdoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJwMUmxOFEh|ryP M2[2VnNCVkeHUh?=
MSTO-211H M{jscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnsfWFKSzVyPUKuNlAxPDFizszN MW\TRW5ITVJ?
LS-513 MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPRTWM2OD1{LkKyNlY6KM7:TR?= M1TWXXNCVkeHUh?=
NCI-SNU-1 MoDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPTTWM2OD1{LkOzNlU3KM7:TR?= MnO1V2FPT0WU
BB65-RCC NH64bWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHizXldKSzVyPUKuN|c1QTNizszN MXvTRW5ITVJ?
GT3TKB NILzNJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXmZnJKSzVyPUKuN|k6PzJizszN Mn7xV2FPT0WU
OS-RC-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITH[4dKSzVyPUKuOFI{PDFizszN NYDRSWZbW0GQR1XS
NCI-H2126 M3PjU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nmU2lEPTB;Mj60N|Y4PCEQvF2= M{XiSHNCVkeHUh?=
SK-UT-1 NWPndI1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TkS2lEPTB;Mj60O|Q3PyEQvF2= NIPLNFNUSU6JRWK=
DMS-114 NXv0OpJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfXT5NyUUN3ME2yMlYyPTJ2IN88US=> NEHrRoJUSU6JRWK=
ONS-76 NXn4W3BRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\jWVRyUUN3ME2yMlY{PjRzIN88US=> MkjOV2FPT0WU
8-MG-BA NIj1dmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\CTWM2OD1{Lk[1OFE1KM7:TR?= NIrGVG9USU6JRWK=
BOKU M3;4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjxSGlFUUN3ME2yMlczPzZ2IN88US=> NYDMfXREW0GQR1XS
LAMA-84 M{nQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;t[2p{UUN3ME2yMlc6QTF{IN88US=> MlHyV2FPT0WU
ES1 NIDzV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:z[W57UUN3ME2yMlgyQDB2IN88US=> MWXTRW5ITVJ?
NCI-H1395 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJwOEKwNVIh|ryP Ml32V2FPT0WU
A388 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPMTWM2OD1{Lkm2NVch|ryP MojxV2FPT0WU
NCCIT NFXiOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYW1c5BwUUN3ME2zMlA5QDZ{IN88US=> M2jUSHNCVkeHUh?=
HD-MY-Z NFrxfnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\iTWM2OD1|LkGzNlA{KM7:TR?= NVT6TVJJW0GQR1XS
NCI-H510A NHK3[YlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPL[pFKSzVyPUOuNVg6PDNizszN Mn2xV2FPT0WU
NCI-N87 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\4TWM2OD1|LkKwNFIh|ryP NX7jXGxuW0GQR1XS
SCLC-21H NVzkO|d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrITWM2OD1|LkK2PFU6KM7:TR?= MUHTRW5ITVJ?
SH-4 NVHGOnh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37wSmlEPTB;Mz6yPFc6PyEQvF2= NF;COWJUSU6JRWK=
QIMR-WIL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr1flNjUUN3ME2zMlMzQDR7IN88US=> MorLV2FPT0WU
KM12 NY\MVGIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLZTWM2OD1|LkOzOVQ1KM7:TR?= M1rBcHNCVkeHUh?=
ST486 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXUTWM2OD1|LkWzPFg{KM7:TR?= NXTxOm1IW0GQR1XS
HC-1 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jn[2lEPTB;Mz62NlAzQCEQvF2= M{nwPHNCVkeHUh?=
BV-173 NUPEWoxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjXU4lKSzVyPUOuOlQxQDhizszN NGPs[GZUSU6JRWK=
EW-24 M2jTZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHaTWM2OD1|Lk[2OFM1KM7:TR?= NWe3S3pCW0GQR1XS
LU-65 NVGwZ2lbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYniVHAyUUN3ME2zMlY5PzFizszN MnP5V2FPT0WU
ECC4 NVKzUWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLZbm5QUUN3ME2zMlc4PTZizszN MoDzV2FPT0WU
ARH-77 M{nzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTRwMUGwOlch|ryP M2nwS3NCVkeHUh?=
BC-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP5dWRKSzVyPUSuNVMxPjhizszN NFftVpFUSU6JRWK=
SNB75 NVf6SGRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLo[|dwUUN3ME20MlI3OTlizszN NXfERXVqW0GQR1XS
MEG-01 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPseoFUUUN3ME20MlI4PDF7IN88US=> Ml\SV2FPT0WU
NCI-H1417 NIDPc5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7jTWM2OD12LkK4OFQ{KM7:TR?= NVzYfmpxW0GQR1XS
MDA-MB-134-VI NX76PGhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTRwM{C2NFEh|ryP Mk\rV2FPT0WU
Becker NFflVWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTRwNEezN|Yh|ryP NXzYXm95W0GQR1XS
DMS-153 M1m2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTRwNk[0O|Uh|ryP MYnTRW5ITVJ?
TGBC1TKB MljtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jUWGlEPTB;ND62PFUyPSEQvF2= M17SbHNCVkeHUh?=
EW-3 NGjkOGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfLeVZKSzVyPUSuO|YzPDhizszN NHniclhUSU6JRWK=
KE-37 NXTtOnNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DoNmlEPTB;ND64OlE6PiEQvF2= M{LRVXNCVkeHUh?=
NCI-H23 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7mb5hKSzVyPUSuPFczOjdizszN M2T2[3NCVkeHUh?=
MC116 NFXqR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LhfGlEPTB;ND65OFEzPiEQvF2= NUm2ZYREW0GQR1XS
NH-12 M1u0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfTTJJ{UUN3ME20Mlk3PDN7IN88US=> Mm\DV2FPT0WU
CTB-1 NYXNXWtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\YfoNKSzVyPUSuPVc4OjFizszN MUXTRW5ITVJ?
KM-H2 Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTVwMEWzNlMh|ryP MVfTRW5ITVJ?
MOLT-4 MnHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHqe2pyUUN3ME21MlEyQDNizszN MX\TRW5ITVJ?
NCI-H2141 NI\pcZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDVfFN4UUN3ME21MlE1OjZ6IN88US=> NGi5SnBUSU6JRWK=
EB-3 M1vkfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\iNIJKSzVyPUWuNVc2ODRizszN NHPndJlUSU6JRWK=
NCI-H1522 NIfpcVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrwTWM2OD13LkK2N|IzKM7:TR?= NYS5RogzW0GQR1XS
MRK-nu-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rCW2lEPTB;NT60N|Y{OyEQvF2= MV7TRW5ITVJ?
no-11 NVnoWYhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nwbmlEPTB;NT60O|A5PyEQvF2= MnrEV2FPT0WU
CESS NIjTVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfrSoV5UUN3ME21MlU5ODN2IN88US=> M4G3bnNCVkeHUh?=
KMOE-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PkO2lEPTB;NT61PFY2QSEQvF2= M4TSdXNCVkeHUh?=
REH M2nNSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml30TWM2OD14LkK1OlE5KM7:TR?= NVT5NZZDW0GQR1XS
KU812 M4DBN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTZwNEK3PVEh|ryP MXLTRW5ITVJ?
SK-N-FI MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTZwNkC2O|Qh|ryP MYPTRW5ITVJ?
MMAC-SF NXrEUokzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnGwTWM2OD15LkC2OFkzKM7:TR?= Moj5V2FPT0WU
RCC10RGB MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPRdWlJUUN3ME23MlIzQTd5IN88US=> M2H2bXNCVkeHUh?=
NCI-H322M M1i0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrPTWM2OD15LkOzN|M2KM7:TR?= MmTqV2FPT0WU
NB6 NY\iRplRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfLTWM2OD15LkW0PFk6KM7:TR?= NHfRUm1USU6JRWK=
MN-60 M3jCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:2WZpKSzVyPUeuOlkzOTVizszN NYDaWGR{W0GQR1XS
NCI-H1092 M3;u[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrVS45mUUN3ME24MlAyPzN2IN88US=> MYrTRW5ITVJ?
EKVX MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nR[GlEPTB;OD60O|A3PiEQvF2= NX20emx[W0GQR1XS
D-263MG Mn7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnKTWM2OD16LkW1N|k3KM7:TR?= MUfTRW5ITVJ?
NCI-H209 Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRThwNkSwNFYh|ryP NFL0Z3hUSU6JRWK=
IST-SL1 NUDHOphVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HmVWlEPTB;OD64PVg6OiEQvF2= M2mwUnNCVkeHUh?=
ACN NG\OWXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXLVplKSzVyPUmuNVkyPTdizszN M2LBNnNCVkeHUh?=
MHH-PREB-1 MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfQSW5NUUN3ME25MlIyOjF7IN88US=> NYL5UFFrW0GQR1XS
EW-11 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrSTWM2OD17Lk[1N|k3KM7:TR?= MUHTRW5ITVJ?
KASUMI-1 M3vDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3HTWM2OD17Lke4O|ch|ryP MoPrV2FPT0WU
KINGS-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;zNog5UUN3ME2xNE4zOzR5IN88US=> MmXHV2FPT0WU
EVSA-T M1rmfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTDcXc5UUN3ME2xNE4{OTl{IN88US=> NEPxfINUSU6JRWK=
DSH1 MkThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLvRVdKSzVyPUGwMlM6PzJizszN NWDPeY9{W0GQR1XS
COLO-824 MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvVTWM2OD1zMD64OlY6KM7:TR?= M{Dm[HNCVkeHUh?=
K052 NH[3[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFyLkmzNlIh|ryP MXjTRW5ITVJ?
SK-MEL-2 M3fF[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f6fWlEPTB;MUCuPVk{QSEQvF2= NH\wT2VUSU6JRWK=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 3 mg/mL (4.88 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

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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