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 M1jLbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LBTmlEPTB;MD6wNFAxPjB|IN88US=> NVPxSoxVW0GQR1XS
SF539 NIXrPWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLLTWM2OD1yLkCwNFU3PCEQvF2= MWDTRW5ITVJ?
DEL M2niXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrx[Xl{UUN3ME2wMlAxODl{NzFOwG0> Ml3aV2FPT0WU
NB1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;3TWM2OD1yLkCwNVYzKM7:TR?= NX;WVHpqW0GQR1XS
SR MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLiU4ZFUUN3ME2wMlAxOjd5IN88US=> NXLO[JF1W0GQR1XS
KARPAS-299 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XocWlEPTB;MD6wNlM5PCEQvF2= NI\idppUSU6JRWK=
MHH-CALL-2 M{DsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;qTpFKSzVyPUCuNFI6PTJizszN MmTDV2FPT0WU
SU-DHL-1 MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPqe21EUUN3ME2wMlA1QDZ3IN88US=> MoPjV2FPT0WU
A4-Fuk MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\pNY9mUUN3ME2wMlA2PTZ3IN88US=> NWqwNmJOW0GQR1XS
EW-1 M3P3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMUCyOVYh|ryP MWXTRW5ITVJ?
NOS-1 M4nmcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwMUCyPVQh|ryP MnrEV2FPT0WU
EW-16 M{LWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMUC1Olgh|ryP Mlq0V2FPT0WU
TE-11 MkLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXrd4tKSzVyPUCuNVYxQTZizszN Ml61V2FPT0WU
SW982 M{TxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPwNoNKSzVyPUCuNVY1PzhizszN Ml[xV2FPT0WU
LAN-6 MnXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDKelJKSzVyPUCuNVc1PDNizszN NEHJVHlUSU6JRWK=
MZ1-PC NEm3cHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMUe4N|Uh|ryP MVjTRW5ITVJ?
KS-1 NIXzT2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTkTWM2OD1yLkG5N|Q{KM7:TR?= Mn3OV2FPT0WU
PSN1 NVPWSphRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLlblY6UUN3ME2wMlE6PjNzIN88US=> NFnqTVhUSU6JRWK=
LC-2-ad NEOxRVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPkTWM2OD1yLkG5OlkzKM7:TR?= NIPQWmJUSU6JRWK=
COLO-320-HSR NXf0SZJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3Ld2NKSzVyPUCuNVk4PzZizszN MnPjV2FPT0WU
OPM-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G2[WlEPTB;MD6yNlY3QSEQvF2= M3X3VXNCVkeHUh?=
SK-NEP-1 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C4d2lEPTB;MD6yN|UzPCEQvF2= NUG0e|ZTW0GQR1XS
ALL-PO Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDZXotMUUN3ME2wMlI1PTJ2IN88US=> M2XQN3NCVkeHUh?=
CMK NYr6Z4dFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M160XWlEPTB;MD6yOVU{KM7:TR?= MVrTRW5ITVJ?
NCI-H1648 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnYWnJJUUN3ME2wMlI4QDV3IN88US=> M2G0R3NCVkeHUh?=
SIG-M5 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXMTWM2OD1yLkK5NVU6KM7:TR?= NHrV[YZUSU6JRWK=
TGBC24TKB M2LVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljkTWM2OD1yLkOwNlE5KM7:TR?= MU\TRW5ITVJ?
DOHH-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rTbmlEPTB;MD6zNVIxPCEQvF2= MoDOV2FPT0WU
NB69 M3\Xdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fROWlEPTB;MD6zNVc5PyEQvF2= M4\xenNCVkeHUh?=
MFH-ino M{jQUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwM{K1NlMh|ryP NX:1d4s5W0GQR1XS
KP-N-RT-BM-1 NH7tNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX1emFIUUN3ME2wMlM{OTJ|IN88US=> MV\TRW5ITVJ?
MONO-MAC-6 MkXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHmTWM2OD1yLkOzNlkyKM7:TR?= NYnvOYxyW0GQR1XS
ATN-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwM{OzNFMh|ryP NUXYdZAxW0GQR1XS
NTERA-S-cl-D1 Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHaOlFKSzVyPUCuN|M{QTZizszN MX7TRW5ITVJ?
L-540 M2n0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vwWmlEPTB;MD6zOlk5QCEQvF2= NF\L[IxUSU6JRWK=
GB-1 M1PwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVmx[pZmUUN3ME2wMlM5QDZ5IN88US=> NGq0N3NUSU6JRWK=
MV-4-11 NFP5dWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO5TWM2OD1yLkO5OFQ3KM7:TR?= NIrs[IxUSU6JRWK=
KG-1 NWPtepdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwM{m1OlEh|ryP MVrTRW5ITVJ?
OVCAR-4 Mn64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jKfWlEPTB;MD60NFU3QSEQvF2= MlrIV2FPT0WU
NEC8 NFHyVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\nTWM2OD1yLkSxNlkzKM7:TR?= MnHRV2FPT0WU
SK-MM-2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml60TWM2OD1yLkSxOlA6KM7:TR?= MoHjV2FPT0WU
TE-8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXqfHlKSzVyPUCuOFI5QCEQvF2= NUn5[IF2W0GQR1XS
697 NHXTe2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3S5PWlEPTB;MD60N|IyPSEQvF2= NVz3NpRKW0GQR1XS
NB14 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnMXWZKSzVyPUCuOFM5OjZizszN MXjTRW5ITVJ?
GDM-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH4TWM2OD1yLkS3NVE3KM7:TR?= NXfvbJJzW0GQR1XS
HUTU-80 M1j5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnOTWM2OD1yLkS3N|c2KM7:TR?= NXXiXolbW0GQR1XS
HL-60 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\uc3RxUUN3ME2wMlQ5OTR{IN88US=> MXPTRW5ITVJ?
OCI-AML2 NH76RmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDFbpZKSzVyPUCuOFg{OjhizszN MlXkV2FPT0WU
ML-2 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV6zcIt7UUN3ME2wMlQ6ODNzIN88US=> MXLTRW5ITVJ?
ES4 NIDBOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH4cFFNUUN3ME2wMlQ6OTB7IN88US=> M{O5XXNCVkeHUh?=
NCI-H747 NUfFUZpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLtTWM2OD1yLkS5PFkh|ryP NGK4b2hUSU6JRWK=
RL95-2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwNUCxNVIh|ryP MVXTRW5ITVJ?
TE-15 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zYPGlEPTB;MD61NVEzPCEQvF2= NEPMTXJUSU6JRWK=
TE-12 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DnWmlEPTB;MD61N|M1QSEQvF2= NFHpNIxUSU6JRWK=
LB1047-RCC M4m4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPhVFBsUUN3ME2wMlU1PTR7IN88US=> MojhV2FPT0WU
LB831-BLC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTXd4tFUUN3ME2wMlU2ODJ|IN88US=> MlHFV2FPT0WU
NCI-H1355 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwNUWxPFQh|ryP MYLTRW5ITVJ?
CTV-1 Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PjWmlEPTB;MD61OVYzPCEQvF2= Mn[2V2FPT0WU
RXF393 NIfobJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwNUW3PVQh|ryP NITRNpBUSU6JRWK=
SW872 NVn6coJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fETWlEPTB;MD61OlczPCEQvF2= MlfjV2FPT0WU
MPP-89 NHjaXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfoTWM2OD1yLkW3PFg1KM7:TR?= M1vjR3NCVkeHUh?=
RPMI-8226 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlr4TWM2OD1yLk[zOVI3KM7:TR?= MUTTRW5ITVJ?
LS-1034 NVnkeGs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonwTWM2OD1yLk[zOVgh|ryP NGDKdXRUSU6JRWK=
SJSA-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXkTWM2OD1yLk[zO|I2KM7:TR?= NH7V[4dUSU6JRWK=
HOP-62 M1XNWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXPNVZSUUN3ME2wMlY2ODN|IN88US=> MlfQV2FPT0WU
KGN M4m3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwNk[xOlgh|ryP NHPKRXVUSU6JRWK=
D-336MG MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXX[YJKSzVyPUCuOlYyPjlizszN MljtV2FPT0WU
LS-411N MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu2TWM2OD1yLk[3OFYzKM7:TR?= NIrJfGtUSU6JRWK=
TE-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP5SoFKSzVyPUCuOlkxPzRizszN NInTR4hUSU6JRWK=
LB996-RCC NYTxNGRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrKTWM2OD1yLk[5N|g6KM7:TR?= NE\WOmNUSU6JRWK=
TE-10 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj3SplNUUN3ME2wMlcyPDl4IN88US=> NHrPZndUSU6JRWK=
NCI-SNU-16 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGP2NoxKSzVyPUCuO|I3PjRizszN MXzTRW5ITVJ?
ES8 MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPuRYhkUUN3ME2wMlc1QTd3IN88US=> NFjWPJJUSU6JRWK=
COLO-800 M{G2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG3TWM2OD1yLke2Olk2KM7:TR?= MoPOV2FPT0WU
ES6 M{jFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHhTZJKSzVyPUCuO|c2PTlizszN MnjVV2FPT0WU
L-363 NWfKV3NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfuPJdKSzVyPUCuPFI{PzVizszN NWLhcJpLW0GQR1XS
NMC-G1 NIS5PGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7McZJKSzVyPUCuPFMzOzNizszN MkXxV2FPT0WU
LU-134-A Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jFSGlEPTB;MD64N|kyOiEQvF2= NXXybYc6W0GQR1XS
SF268 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXFTWM2OD1yLki0NFQzKM7:TR?= M4Po[XNCVkeHUh?=
KARPAS-45 NUHFdYl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LYXmlEPTB;MD64OFI3OyEQvF2= MXjTRW5ITVJ?
TGW NH3DN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXaUpViUUN3ME2wMlg2QDZ|IN88US=> M1f0WnNCVkeHUh?=
CHP-126 NEDFV5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPseo9KSzVyPUCuPFU6PTdizszN NIDkTpVUSU6JRWK=
MOLT-16 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwOEe1PFkh|ryP M4XmSXNCVkeHUh?=
LB771-HNC MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DXSmlEPTB;MD64PVc2PyEQvF2= NX21NGx4W0GQR1XS
NALM-6 NWjoWI54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTNeGtLUUN3ME2wMlkxPzN7IN88US=> NYnsepBIW0GQR1XS
GCIY MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwOUW1NlYh|ryP NF\Le3lUSU6JRWK=
IST-MES1 M1;nUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwOUi4NlQh|ryP MVjTRW5ITVJ?
LB2241-RCC NWjXWXRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PZRmlEPTB;MD65PFg1KM7:TR?= MYDTRW5ITVJ?
BL-70 NInGU|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDWTWM2OD1yLkm5OVM2KM7:TR?= NI\1[ZpUSU6JRWK=
NB17 NGX3[VVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfsOWVKSzVyPUGuNFA3OzlizszN NUXNWVRlW0GQR1XS
LXF-289 NF;HeotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;D[ZBKSzVyPUGuNFMxPzZizszN MmPCV2FPT0WU
TK10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6wTWM2OD1zLkC1NFY{KM7:TR?= MoCwV2FPT0WU
K5 MnjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[wTWM2OD1zLkC2Nlc1KM7:TR?= NGDHN3hUSU6JRWK=
NCI-H716 MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjEUYpKSzVyPUGuNFczPTlizszN MXTTRW5ITVJ?
HCE-T NWH6XnhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDzXVlKSzVyPUGuNFg5OTlizszN M4S2V3NCVkeHUh?=
GI-1 NGjOPIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwMEm3PVgh|ryP NGXq[mVUSU6JRWK=
KARPAS-422 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3LTWM2OD1zLkGwNFIzKM7:TR?= MYTTRW5ITVJ?
TE-9 NFz5bY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTFwMUGzNlgh|ryP NHzJTmxUSU6JRWK=
SF126 M2OzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwMUG1Olgh|ryP NX\tToY{W0GQR1XS
BB30-HNC M4W5OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rSRWlEPTB;MT6xN|EyOiEQvF2= NHz6NnJUSU6JRWK=
NCI-H1304 M{D2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTFwMUOzN|gh|ryP MWfTRW5ITVJ?
HEL NGrsVJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TaUWlEPTB;MT6xOFg6PSEQvF2= M2GyWHNCVkeHUh?=
HAL-01 NWSwbJo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPJWY9ZUUN3ME2xMlE2Ojh|IN88US=> MnrzV2FPT0WU
SK-LMS-1 MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrvdXh4UUN3ME2xMlE2QTd2IN88US=> NYj5RpZMW0GQR1XS
SW954 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvjdJpKSzVyPUGuNVk2PjdizszN NWP2[m9lW0GQR1XS
D-283MED M3HQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DS[2lEPTB;MT6yNlM4QSEQvF2= MnXXV2FPT0WU
NCI-H1882 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\QTWM2OD1zLkKzPFkh|ryP M4DMd3NCVkeHUh?=
GI-ME-N M2\MeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjuTWM2OD1zLkK1NlA5KM7:TR?= M4e5XnNCVkeHUh?=
SK-PN-DW NETseFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfnS3BCUUN3ME2xMlI3OzR6IN88US=> M1rYenNCVkeHUh?=
C2BBe1 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;LTWM2OD1zLkK5NVE4KM7:TR?= NVXXVmgzW0GQR1XS
A704 M4Dyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXlTWM2OD1zLkOyOlg6KM7:TR?= MUnTRW5ITVJ?
KALS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL2TWM2OD1zLkO0NFgh|ryP MojwV2FPT0WU
ETK-1 NVvXUoloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXQTWM2OD1zLkO0OFg6KM7:TR?= MYXTRW5ITVJ?
LB647-SCLC M{TLN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TENGlEPTB;MT6zOFk5PiEQvF2= NF7GcmdUSU6JRWK=
OCUB-M MnPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjkbZhKSzVyPUGuN|YyPDNizszN MYDTRW5ITVJ?
NCI-H720 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M36wWGlEPTB;MT6zOlM4QCEQvF2= MYrTRW5ITVJ?
NB13 NXXwXnlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS4XXFkUUN3ME2xMlM4Ojl|IN88US=> M3TwNnNCVkeHUh?=
GR-ST NITEVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknJTWM2OD1zLkO4O|U4KM7:TR?= NEDvfFZUSU6JRWK=
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NCI-H524 NULaW|JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnDTVl3UUN3ME2xMlY1OzB5IN88US=> NIrlN5NUSU6JRWK=
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NCI-H1581 M{Dwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXmS2ZKSzVyPUKuNVE2PTlizszN NXm0NpNyW0GQR1XS
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TE-6 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwMUmwOUDPxE1? M2ThdXNCVkeHUh?=
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NCI-H510A MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLON3VOUUN3ME2zMlE5QTR|IN88US=> NVrkTo43W0GQR1XS
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SCLC-21H MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWftUYg4UUN3ME2zMlI3QDV7IN88US=> M4\MU3NCVkeHUh?=
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BC-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETrXGxKSzVyPUSuNVMxPjhizszN MYfTRW5ITVJ?
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NCI-H1417 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfBdVZKSzVyPUSuNlg1PDNizszN MXvTRW5ITVJ?
MDA-MB-134-VI NFvLOWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7JV45ZUUN3ME20MlMxPjBzIN88US=> NWPFRoFVW0GQR1XS
Becker NVTnc3BPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3QTWM2OD12LkS3N|M3KM7:TR?= Mmr2V2FPT0WU
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TGBC1TKB NVHSVW5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjBTWM2OD12Lk[4OVE2KM7:TR?= MUfTRW5ITVJ?
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KE-37 M1vaPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7UeJFTUUN3ME20Mlg3OTl4IN88US=> MVXTRW5ITVJ?
NCI-H23 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnNUGVXUUN3ME20Mlg4OjJ5IN88US=> NUn1RWduW0GQR1XS
MC116 NYrrR5ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTRwOUSxNlYh|ryP Ml;hV2FPT0WU
NH-12 NF\lSoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXzTW9KSzVyPUSuPVY1OzlizszN NGDoWoNUSU6JRWK=
CTB-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELvUWxKSzVyPUSuPVc4OjFizszN NY\6UnpjW0GQR1XS
KM-H2 NH;sN|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrjVVNZUUN3ME21MlA2OzJ|IN88US=> MoPBV2FPT0WU
MOLT-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXXOZRKSzVyPUWuNVE5OyEQvF2= NXnzSppnW0GQR1XS
NCI-H2141 NYjNVJFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;qVWlEPTB;NT6xOFI3QCEQvF2= NVPwVmNmW0GQR1XS
EB-3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC1cGc{UUN3ME21MlE4PTB2IN88US=> NF3xToNUSU6JRWK=
NCI-H1522 M{S4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3qwZmlEPTB;NT6yOlMzOiEQvF2= MVvTRW5ITVJ?
MRK-nu-1 MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rKe2lEPTB;NT60N|Y{OyEQvF2= MUTTRW5ITVJ?
no-11 NY\YVmtST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnuyTWM2OD13LkS3NFg4KM7:TR?= MX3TRW5ITVJ?
CESS MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTVwNUiwN|Qh|ryP M3O1PHNCVkeHUh?=
KMOE-2 NXPlVlM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnvRXZKSzVyPUWuOVg3PTlizszN M{nIZ3NCVkeHUh?=
REH M4PjeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETT[YJKSzVyPU[uNlU3OThizszN NHTrcpFUSU6JRWK=
KU812 M{HuVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHUZmxKSzVyPU[uOFI4QTFizszN Ml\5V2FPT0WU
SK-N-FI M1rLeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWToc4pWUUN3ME22MlYxPjd2IN88US=> NUToS21VW0GQR1XS
MMAC-SF NFfH[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli0TWM2OD15LkC2OFkzKM7:TR?= NIP0V2FUSU6JRWK=
RCC10RGB NGDGZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjPSVNPUUN3ME23MlIzQTd5IN88US=> MVHTRW5ITVJ?
NCI-H322M NXzZUHFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4joTGlEPTB;Nz6zN|M{PSEQvF2= M2jWb3NCVkeHUh?=
NB6 NFnuZWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTdwNUS4PVkh|ryP NHfTcVhUSU6JRWK=
MN-60 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jOTWlEPTB;Nz62PVIyPSEQvF2= M{DV[XNCVkeHUh?=
NCI-H1092 NILBdHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRThwMEG3N|Qh|ryP NICzO2VUSU6JRWK=
EKVX MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRThwNEewOlYh|ryP MmPRV2FPT0WU
D-263MG M1;kSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLP[mI1UUN3ME24MlU2Ozl4IN88US=> M1OySnNCVkeHUh?=
NCI-H209 NF7heWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXqTWM2OD16Lk[0NFA3KM7:TR?= M3LR[nNCVkeHUh?=
IST-SL1 NY\1bXdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T1b2lEPTB;OD64PVg6OiEQvF2= NFn0c4NUSU6JRWK=
ACN MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnKTWM2OD17LkG5NVU4KM7:TR?= NIrCb29USU6JRWK=
MHH-PREB-1 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTlwMkGyNVkh|ryP NEm0OJVUSU6JRWK=
EW-11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTlwNkWzPVYh|ryP NFT2VpVUSU6JRWK=
KASUMI-1 NHPieWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTlwN{i3O{DPxE1? M1LBW3NCVkeHUh?=
KINGS-1 M{TCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr1PYVRUUN3ME2xNE4zOzR5IN88US=> NWjQdGR5W0GQR1XS
EVSA-T MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3SNYFKSzVyPUGwMlMyQTJizszN NWLObmtXW0GQR1XS
DSH1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFyLkO5O|Ih|ryP NXrDfVlUW0GQR1XS
COLO-824 M1v1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT3TWM2OD1zMD64OlY6KM7:TR?= NE\LdZFUSU6JRWK=
K052 NImydINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[2UGlEPTB;MUCuPVMzOiEQvF2= M2\3c3NCVkeHUh?=
SK-MEL-2 NVjPd|RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3aWllOUUN3ME2xNE46QTN7IN88US=> NYXPbHdrW0GQR1XS

... 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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