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 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwMECwNFYxOyEQvF2= NX;2c4ljW0GQR1XS
SF539 MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMECwOVY1KM7:TR?= M3\vWHNCVkeHUh?=
DEL NEjYdGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrK[JpZUUN3ME2wMlAxODl{NzFOwG0> MmL3V2FPT0WU
NB1 M3HpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMECxOlIh|ryP NVHDW2o5W0GQR1XS
SR NHHoTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnT6TWM2OD1yLkCwNlc4KM7:TR?= NGXpfHpUSU6JRWK=
KARPAS-299 M1PKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwMEKzPFQh|ryP NIC0d4xUSU6JRWK=
MHH-CALL-2 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7Rd|g6UUN3ME2wMlAzQTV{IN88US=> M1\PT3NCVkeHUh?=
SU-DHL-1 NV\PR3B3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf3O5pZUUN3ME2wMlA1QDZ3IN88US=> MUPTRW5ITVJ?
A4-Fuk NXP4OItTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DIOmlEPTB;MD6wOVU3PSEQvF2= M1zQfHNCVkeHUh?=
EW-1 Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX2yOVllUUN3ME2wMlExOjV4IN88US=> NYjmXlA{W0GQR1XS
NOS-1 NYfi[3B4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFKzVXlKSzVyPUCuNVAzQTRizszN MWDTRW5ITVJ?
EW-16 M3u0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwMUC1Olgh|ryP NIP2O4tUSU6JRWK=
TE-11 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPUWWFnUUN3ME2wMlE3ODl4IN88US=> M1W4enNCVkeHUh?=
SW982 Mn\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHu[GJKSzVyPUCuNVY1PzhizszN MWfTRW5ITVJ?
LAN-6 NGLTOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPseG5YUUN3ME2wMlE4PDR|IN88US=> M3vP[XNCVkeHUh?=
MZ1-PC NUjRcGF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTmdnluUUN3ME2wMlE4QDN3IN88US=> MX3TRW5ITVJ?
KS-1 Ml2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSwcmVKSzVyPUCuNVk{PDNizszN MWXTRW5ITVJ?
PSN1 M4C1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;oVXozUUN3ME2wMlE6PjNzIN88US=> M2LoWHNCVkeHUh?=
LC-2-ad NYHp[pUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mxOWlEPTB;MD6xPVY6OiEQvF2= MmfVV2FPT0WU
COLO-320-HSR Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYO4W5JkUUN3ME2wMlE6Pzd4IN88US=> MYTTRW5ITVJ?
OPM-2 NGXoR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHriOnNKSzVyPUCuNlI3PjlizszN MWfTRW5ITVJ?
SK-NEP-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PFW2lEPTB;MD6yN|UzPCEQvF2= MWnTRW5ITVJ?
ALL-PO MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe1S3djUUN3ME2wMlI1PTJ2IN88US=> NGfQO2hUSU6JRWK=
CMK MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwMkW1N{DPxE1? NYrsSIg2W0GQR1XS
NCI-H1648 NGnCOpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH0TWM2OD1yLkK3PFU2KM7:TR?= MVnTRW5ITVJ?
SIG-M5 NWLMSnZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjhW2JnUUN3ME2wMlI6OTV7IN88US=> MWfTRW5ITVJ?
TGBC24TKB NF\vR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwM{CyNVgh|ryP NUPx[5FSW0GQR1XS
DOHH-2 M1niWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HKSmlEPTB;MD6zNVIxPCEQvF2= NYK1Z|NbW0GQR1XS
NB69 M3q2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXDNVNKSzVyPUCuN|E4QDdizszN NV3J[nRbW0GQR1XS
MFH-ino NXG0O4c5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwM{K1NlMh|ryP MX\TRW5ITVJ?
KP-N-RT-BM-1 Mm\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDrWZRKSzVyPUCuN|MyOjNizszN MnPnV2FPT0WU
MONO-MAC-6 MlrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PEOmlEPTB;MD6zN|I6OSEQvF2= NWezTYxSW0GQR1XS
ATN-1 M4TTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfJTodqUUN3ME2wMlM{OzB|IN88US=> NFy3VmhUSU6JRWK=
NTERA-S-cl-D1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPETWM2OD1yLkOzN|k3KM7:TR?= Ml;EV2FPT0WU
L-540 M2rn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwM{[5PFgh|ryP MkSxV2FPT0WU
GB-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwM{i4Olch|ryP NUDWbVVUW0GQR1XS
MV-4-11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr4NnJEUUN3ME2wMlM6PDR4IN88US=> NWDacos3W0GQR1XS
KG-1 MoXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyybVUyUUN3ME2wMlM6PTZzIN88US=> MWrTRW5ITVJ?
OVCAR-4 NE\ZPYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm3RWJMUUN3ME2wMlQxPTZ7IN88US=> M{juVnNCVkeHUh?=
NEC8 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwNEGyPVIh|ryP M1LCfXNCVkeHUh?=
SK-MM-2 MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHN[WVKSzVyPUCuOFE3ODlizszN MorEV2FPT0WU
TE-8 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rjbWlEPTB;MD60Nlg5KM7:TR?= MnTBV2FPT0WU
697 NXPwUWpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwNEOyNVUh|ryP M3y4OHNCVkeHUh?=
NB14 NULn[YRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvDT4hvUUN3ME2wMlQ{QDJ4IN88US=> MkPMV2FPT0WU
GDM-1 M1f4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNEexNVYh|ryP Mm[2V2FPT0WU
HUTU-80 NIPKcXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL3RW9KSzVyPUCuOFc{PzVizszN NVnaRWd{W0GQR1XS
HL-60 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPQU|EyUUN3ME2wMlQ5OTR{IN88US=> NGHEcJJUSU6JRWK=
OCI-AML2 NHG1TIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fp[2lEPTB;MD60PFMzQCEQvF2= M2fuc3NCVkeHUh?=
ML-2 NGTVPGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK4OpdHUUN3ME2wMlQ6ODNzIN88US=> M3f5OnNCVkeHUh?=
ES4 NV7kcHd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDuVmlKSzVyPUCuOFkyODlizszN Mnu2V2FPT0WU
NCI-H747 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;Ld3FTUUN3ME2wMlQ6QDlizszN NFzkZmNUSU6JRWK=
RL95-2 M3foWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwNUCxNVIh|ryP NY\6e41TW0GQR1XS
TE-15 M1;vUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjDdIgzUUN3ME2wMlUyOTJ2IN88US=> NEnrclBUSU6JRWK=
TE-12 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\VcphKSzVyPUCuOVM{PDlizszN NGLCV|RUSU6JRWK=
LB1047-RCC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3XboNKSzVyPUCuOVQ2PDlizszN M4G3ZnNCVkeHUh?=
LB831-BLC NHLUeGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HVd2lEPTB;MD61OVAzOyEQvF2= Mlf3V2FPT0WU
NCI-H1355 MmCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwNUWxPFQh|ryP MULTRW5ITVJ?
CTV-1 MmHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3n4[2lEPTB;MD61OVYzPCEQvF2= NGn6UYpUSU6JRWK=
RXF393 NELqcIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj4SpRKSzVyPUCuOVU4QTRizszN NH2z[pJUSU6JRWK=
SW872 MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4joPGlEPTB;MD61OlczPCEQvF2= NWH2XJpmW0GQR1XS
MPP-89 MnjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfoTGIxUUN3ME2wMlU4QDh2IN88US=> NGPhNnJUSU6JRWK=
RPMI-8226 NYjIcYt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwNkO1NlYh|ryP M12wXHNCVkeHUh?=
LS-1034 M1T6T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;jbHFKSzVyPUCuOlM2QCEQvF2= MX3TRW5ITVJ?
SJSA-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnZcmIyUUN3ME2wMlY{PzJ3IN88US=> MlH5V2FPT0WU
HOP-62 M{SzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnUTWM2OD1yLk[1NFM{KM7:TR?= NUfGOHVbW0GQR1XS
KGN M{jxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPWbFlKSzVyPUCuOlYyPjhizszN MYLTRW5ITVJ?
D-336MG NFf1clBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjm[GVrUUN3ME2wMlY3OTZ7IN88US=> MWjTRW5ITVJ?
LS-411N MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XIS2lEPTB;MD62O|Q3OiEQvF2= MYLTRW5ITVJ?
TE-1 NHHQb5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnrTWM2OD1yLk[5NFc1KM7:TR?= NFziPWhUSU6JRWK=
LB996-RCC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfMPGt4UUN3ME2wMlY6Ozh7IN88US=> MmrLV2FPT0WU
TE-10 NGnuPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwN{G0PVYh|ryP NFe1Z4NUSU6JRWK=
NCI-SNU-16 MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TL[2lEPTB;MD63NlY3PCEQvF2= MUTTRW5ITVJ?
ES8 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrpTWM2OD1yLke0PVc2KM7:TR?= MUTTRW5ITVJ?
COLO-800 NGnQUoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LWd2lEPTB;MD63OlY6PSEQvF2= NWXUV|VWW0GQR1XS
ES6 NVrLWoV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\PSndyUUN3ME2wMlc4PTV7IN88US=> NXi5TGRjW0GQR1XS
L-363 M17DNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4SzbmlEPTB;MD64NlM4PSEQvF2= M3PLNnNCVkeHUh?=
NMC-G1 M3m3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HV[GlEPTB;MD64N|I{OyEQvF2= NXe2XHh1W0GQR1XS
LU-134-A MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzLWY1nUUN3ME2wMlg{QTF{IN88US=> NYrhfJRbW0GQR1XS
SF268 M{nHd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwOESwOFIh|ryP M3i5VHNCVkeHUh?=
KARPAS-45 MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXC[ZR2UUN3ME2wMlg1OjZ|IN88US=> MYnTRW5ITVJ?
TGW NI[1XXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO3[Y9KSzVyPUCuPFU5PjNizszN MXjTRW5ITVJ?
CHP-126 NF:xVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPGcJdWUUN3ME2wMlg2QTV5IN88US=> NUXkdFNWW0GQR1XS
MOLT-16 NXjJPGVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwOEe1PFkh|ryP MnPBV2FPT0WU
LB771-HNC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwOEm3OVch|ryP Ml7nV2FPT0WU
NALM-6 NI\ObIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwOUC3N|kh|ryP MkXyV2FPT0WU
GCIY NYfZVJBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C1WmlEPTB;MD65OVUzPiEQvF2= MWHTRW5ITVJ?
IST-MES1 NUTGc|VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwOUi4NlQh|ryP NFvSXZJUSU6JRWK=
LB2241-RCC MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nONGlEPTB;MD65PFg1KM7:TR?= MV;TRW5ITVJ?
BL-70 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHhRZp4UUN3ME2wMlk6PTN3IN88US=> MXHTRW5ITVJ?
NB17 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rneGlEPTB;MT6wNFY{QSEQvF2= MXfTRW5ITVJ?
LXF-289 NWe0elBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFwMEOwO|Yh|ryP MVPTRW5ITVJ?
TK10 NHnEZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwMEWwOlMh|ryP Mlr2V2FPT0WU
K5 NU\tVHA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIiyN|BKSzVyPUGuNFYzPzRizszN MUfTRW5ITVJ?
NCI-H716 M2HMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPXdXNKSzVyPUGuNFczPTlizszN NFnw[2pUSU6JRWK=
HCE-T MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTFwMEi4NVkh|ryP NUTxPIZbW0GQR1XS
GI-1 NXv6R2R6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfmTWM2OD1zLkC5O|k5KM7:TR?= NUDMNItvW0GQR1XS
KARPAS-422 M{DmPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jPZ2lEPTB;MT6xNFAzOiEQvF2= NVew[XdjW0GQR1XS
TE-9 M2S4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLYRotKSzVyPUGuNVE{OjhizszN MXnTRW5ITVJ?
SF126 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[zTWM2OD1zLkGxOVY5KM7:TR?= NXXSRXdiW0GQR1XS
BB30-HNC NEnqfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjxS3plUUN3ME2xMlE{OTF{IN88US=> MYDTRW5ITVJ?
NCI-H1304 NIXiSWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFwMUOzN|gh|ryP Mn;GV2FPT0WU
HEL NWXKcpl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojQTWM2OD1zLkG0PFk2KM7:TR?= M{jacnNCVkeHUh?=
HAL-01 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ixR2lEPTB;MT6xOVI5OyEQvF2= NGGyVmhUSU6JRWK=
SK-LMS-1 M3\HXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\oO2lEPTB;MT6xOVk4PCEQvF2= NUfwbVRFW0GQR1XS
SW954 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj3TWM2OD1zLkG5OVY4KM7:TR?= M3nZV3NCVkeHUh?=
D-283MED NH\YcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TmeGlEPTB;MT6yNlM4QSEQvF2= M2m3RnNCVkeHUh?=
NCI-H1882 NV;3fZR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHmTWM2OD1zLkKzPFkh|ryP NF;UZ3NUSU6JRWK=
GI-ME-N MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnaTWM2OD1zLkK1NlA5KM7:TR?= NY\0e3NNW0GQR1XS
SK-PN-DW NHjRPWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPZUllKSzVyPUGuNlY{PDhizszN MknHV2FPT0WU
C2BBe1 M2fsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjXV2t3UUN3ME2xMlI6OTF5IN88US=> MWrTRW5ITVJ?
A704 NX7HV4pFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXMb5BKSzVyPUGuN|I3QDlizszN MYLTRW5ITVJ?
KALS-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwM{SwPEDPxE1? NETLXHpUSU6JRWK=
ETK-1 M{Hq[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFwM{S0PFkh|ryP NH3hWYJUSU6JRWK=
LB647-SCLC NGP3cJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fxbWlEPTB;MT6zOFk5PiEQvF2= NWH5UnY5W0GQR1XS
OCUB-M M4\MXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTMN|VKSzVyPUGuN|YyPDNizszN NXvDem9SW0GQR1XS
NCI-H720 NV21WolST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DEVWlEPTB;MT6zOlM4QCEQvF2= NUDFUG1WW0GQR1XS
NB13 MlLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwM{eyPVMh|ryP MWHTRW5ITVJ?
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NCI-H1522 NYm5Xo9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTVwMk[zNlIh|ryP MWjTRW5ITVJ?
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REH M4ja[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT0TWM2OD14LkK1OlE5KM7:TR?= MX;TRW5ITVJ?
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ACN NFW2XFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS2TWM2OD17LkG5NVU4KM7:TR?= M1G4fXNCVkeHUh?=
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K052 MkTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjkTWM2OD1zMD65N|IzKM7:TR?= MmHMV2FPT0WU
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... 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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