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

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    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 NWL3fWU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknzTWM2OD1yLkCwNFA3ODNizszN NIrSOohUSU6JRWK=
SF539 M{C0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMECwOVY1KM7:TR?= M{LibnNCVkeHUh?=
DEL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLQfVhKSzVyPUCuNFAxQTJ5IN88US=> MVLTRW5ITVJ?
NB1 M4TXNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTqTWM2OD1yLkCwNVYzKM7:TR?= MV\TRW5ITVJ?
SR NXPhWoFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwMECyO|ch|ryP M3[zWHNCVkeHUh?=
KARPAS-299 MljnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEKzPFQh|ryP NYfiTlNFW0GQR1XS
MHH-CALL-2 M1raSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrTTZlKSzVyPUCuNFI6PTJizszN M1PY[nNCVkeHUh?=
SU-DHL-1 NFT1flNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT3TWM2OD1yLkC0PFY2KM7:TR?= MYrTRW5ITVJ?
A4-Fuk M2nYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{W4UGlEPTB;MD6wOVU3PSEQvF2= NYmw[3NZW0GQR1XS
EW-1 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMUCyOVYh|ryP Mn;mV2FPT0WU
NOS-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID1TGdKSzVyPUCuNVAzQTRizszN M2LSUHNCVkeHUh?=
EW-16 NUDudohGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULGR5hXUUN3ME2wMlExPTZ6IN88US=> MV3TRW5ITVJ?
TE-11 M{fhdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvFTWM2OD1yLkG2NFk3KM7:TR?= NIHEbJZUSU6JRWK=
SW982 NF:wSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXUc21KSzVyPUCuNVY1PzhizszN NVHWblRYW0GQR1XS
LAN-6 M3f3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\X[3lKSzVyPUCuNVc1PDNizszN M4GzenNCVkeHUh?=
MZ1-PC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfvR|hKSzVyPUCuNVc5OzVizszN NXLBOmlXW0GQR1XS
KS-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHwTWM2OD1yLkG5N|Q{KM7:TR?= NFjV[ZBUSU6JRWK=
PSN1 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPiSIU6UUN3ME2wMlE6PjNzIN88US=> M4XSSnNCVkeHUh?=
LC-2-ad M2TEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwMUm2PVIh|ryP MVTTRW5ITVJ?
COLO-320-HSR MkPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf1bnl3UUN3ME2wMlE6Pzd4IN88US=> NH3ibJJUSU6JRWK=
OPM-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP4TWM2OD1yLkKyOlY6KM7:TR?= MnP5V2FPT0WU
SK-NEP-1 NHzncIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwMkO1NlQh|ryP MmnJV2FPT0WU
ALL-PO NI\rOpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL4VIx4UUN3ME2wMlI1PTJ2IN88US=> NHfBenJUSU6JRWK=
CMK MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\hZYJKSzVyPUCuNlU2OyEQvF2= MWjTRW5ITVJ?
NCI-H1648 NInXTndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwMke4OVUh|ryP NYjiV4NGW0GQR1XS
SIG-M5 MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonNTWM2OD1yLkK5NVU6KM7:TR?= M1rxW3NCVkeHUh?=
TGBC24TKB NWDOU|cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XlVGlEPTB;MD6zNFIyQCEQvF2= NHH6SXFUSU6JRWK=
DOHH-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u3[2lEPTB;MD6zNVIxPCEQvF2= MoPpV2FPT0WU
NB69 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuxTWM2OD1yLkOxO|g4KM7:TR?= MkHTV2FPT0WU
MFH-ino MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm5TWM2OD1yLkOyOVI{KM7:TR?= MofaV2FPT0WU
KP-N-RT-BM-1 M3noOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwM{OxNlMh|ryP MWTTRW5ITVJ?
MONO-MAC-6 M1XqXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUm1fItQUUN3ME2wMlM{OjlzIN88US=> NVHZTXl2W0GQR1XS
ATN-1 M4i0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIixSGtKSzVyPUCuN|M{ODNizszN NVL0Smx7W0GQR1XS
NTERA-S-cl-D1 NWCwOJJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPXTWM2OD1yLkOzN|k3KM7:TR?= MXzTRW5ITVJ?
L-540 MkTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXSy[odXUUN3ME2wMlM3QTh6IN88US=> NFzYVVhUSU6JRWK=
GB-1 MmDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jhOGlEPTB;MD6zPFg3PyEQvF2= M36zN3NCVkeHUh?=
MV-4-11 NVrGO|hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\jTWM2OD1yLkO5OFQ3KM7:TR?= MVjTRW5ITVJ?
KG-1 M{XOUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTVdFhtUUN3ME2wMlM6PTZzIN88US=> MX3TRW5ITVJ?
OVCAR-4 MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrRSGpKSzVyPUCuOFA2PjlizszN NXfUcId4W0GQR1XS
NEC8 M17INWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvmZXBqUUN3ME2wMlQyOjl{IN88US=> NE\PRYtUSU6JRWK=
SK-MM-2 NYXMWlBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3scHZQUUN3ME2wMlQyPjB7IN88US=> M3;HdHNCVkeHUh?=
TE-8 NF[4enVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXBVlBKSzVyPUCuOFI5QCEQvF2= MnnQV2FPT0WU
697 NHfNOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zGT2lEPTB;MD60N|IyPSEQvF2= MUXTRW5ITVJ?
NB14 MmroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkO1TWM2OD1yLkSzPFI3KM7:TR?= M{n5bXNCVkeHUh?=
GDM-1 NVTje2RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPRVmRKSzVyPUCuOFcyOTZizszN NXTzdVRkW0GQR1XS
HUTU-80 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTmeWJQUUN3ME2wMlQ4Ozd3IN88US=> MY\TRW5ITVJ?
HL-60 NVS1T|RzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnXeWs6UUN3ME2wMlQ5OTR{IN88US=> NI[0VHZUSU6JRWK=
OCI-AML2 MlnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLnTWM2OD1yLkS4N|I5KM7:TR?= NHnEOnpUSU6JRWK=
ML-2 MnHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr5T4xMUUN3ME2wMlQ6ODNzIN88US=> M3LpenNCVkeHUh?=
ES4 NH3YTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPZTWM2OD1yLkS5NVA6KM7:TR?= NX3ob|RmW0GQR1XS
NCI-H747 M1;FXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwNEm4PUDPxE1? NYmySWhPW0GQR1XS
RL95-2 M3GycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwNUCxNVIh|ryP NXOzfpVrW0GQR1XS
TE-15 NED6ToJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHRTWM2OD1yLkWxNVI1KM7:TR?= MUDTRW5ITVJ?
TE-12 NHf5Z25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPVTWM2OD1yLkWzN|Q6KM7:TR?= MkPlV2FPT0WU
LB1047-RCC MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwNUS1OFkh|ryP M1;C[nNCVkeHUh?=
LB831-BLC NF\ZT3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPLT|JpUUN3ME2wMlU2ODJ|IN88US=> MVfTRW5ITVJ?
NCI-H1355 MnXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u5T2lEPTB;MD61OVE5PCEQvF2= MoP0V2FPT0WU
CTV-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O3VGlEPTB;MD61OVYzPCEQvF2= NICzZ2JUSU6JRWK=
RXF393 M37VS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHjZ3hKSzVyPUCuOVU4QTRizszN M4fjRXNCVkeHUh?=
SW872 M1;SUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHRU5FZUUN3ME2wMlU3PzJ2IN88US=> M2\yZnNCVkeHUh?=
MPP-89 NF\rS4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwNUe4PFQh|ryP M4W0c3NCVkeHUh?=
RPMI-8226 M{TXZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnKfnlKSzVyPUCuOlM2OjZizszN M4rxfHNCVkeHUh?=
LS-1034 NVTrVmRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmToTWM2OD1yLk[zOVgh|ryP MnHoV2FPT0WU
SJSA-1 M4PQdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTOTWM2OD1yLk[zO|I2KM7:TR?= NEDhe5NUSU6JRWK=
HOP-62 M3PSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy0RWNKSzVyPUCuOlUxOzNizszN NH;Me41USU6JRWK=
KGN NHTxRldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTBwNk[xOlgh|ryP MX\TRW5ITVJ?
D-336MG M4\GU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDrRVF4UUN3ME2wMlY3OTZ7IN88US=> NUm4TXU6W0GQR1XS
LS-411N M2ToN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW0PZNKSzVyPUCuOlc1PjJizszN NWDnSIxGW0GQR1XS
TE-1 M2nLWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3POe2lEPTB;MD62PVA4PCEQvF2= MUPTRW5ITVJ?
LB996-RCC M2nxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2joXGlEPTB;MD62PVM5QSEQvF2= NUG4RmoxW0GQR1XS
TE-10 NW\rSpk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrrSnBKSzVyPUCuO|E1QTZizszN MlPNV2FPT0WU
NCI-SNU-16 MoXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTpSHd[UUN3ME2wMlczPjZ2IN88US=> NI\xRXBUSU6JRWK=
ES8 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv1dIdKSzVyPUCuO|Q6PzVizszN MUDTRW5ITVJ?
COLO-800 M1frcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\STWM2OD1yLke2Olk2KM7:TR?= NHvMRllUSU6JRWK=
ES6 M4jtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzD[XNKSzVyPUCuO|c2PTlizszN MYjTRW5ITVJ?
L-363 NX\jSGsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlv6TWM2OD1yLkiyN|c2KM7:TR?= NVLCclRJW0GQR1XS
NMC-G1 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\sTWM2OD1yLkizNlM{KM7:TR?= MXvTRW5ITVJ?
LU-134-A MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwOEO5NVIh|ryP NWTNcG1UW0GQR1XS
SF268 Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PvN2lEPTB;MD64OFA1OiEQvF2= MmnGV2FPT0WU
KARPAS-45 NX7wTZhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:xTWM2OD1yLki0NlY{KM7:TR?= M33oXnNCVkeHUh?=
TGW NU[4O2R1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTUWZRKSzVyPUCuPFU5PjNizszN MlHnV2FPT0WU
CHP-126 NHTqWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwOEW5OVch|ryP MWXTRW5ITVJ?
MOLT-16 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwOEe1PFkh|ryP NW\lbYc4W0GQR1XS
LB771-HNC NY\SbWtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnEb21KSzVyPUCuPFk4PTdizszN M{X3e3NCVkeHUh?=
NALM-6 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjKNlhKSzVyPUCuPVA4OzlizszN NHrFOWhUSU6JRWK=
GCIY M2XNWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ThR2lEPTB;MD65OVUzPiEQvF2= MUTTRW5ITVJ?
IST-MES1 NEjrW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj6fHhxUUN3ME2wMlk5QDJ2IN88US=> MlSwV2FPT0WU
LB2241-RCC NH\ad2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH3TWM2OD1yLkm4PFQh|ryP M2jyR3NCVkeHUh?=
BL-70 Mn6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PWN2lEPTB;MD65PVU{PSEQvF2= NHzpZ2VUSU6JRWK=
NB17 NVHrVVNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPLTWM2OD1zLkCwOlM6KM7:TR?= MWTTRW5ITVJ?
LXF-289 M3LUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwMEOwO|Yh|ryP NWrmZnVNW0GQR1XS
TK10 M1GzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTFwMEWwOlMh|ryP MXPTRW5ITVJ?
K5 Mle0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jzT2lEPTB;MT6wOlI4PCEQvF2= NGDUcJFUSU6JRWK=
NCI-H716 NVTzUnhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFwMEeyOVkh|ryP NFvXXIdUSU6JRWK=
HCE-T NFPKZpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwMEi4NVkh|ryP MXvTRW5ITVJ?
GI-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHuTWM2OD1zLkC5O|k5KM7:TR?= MmDnV2FPT0WU
KARPAS-422 NV;lRnVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGwS5J7UUN3ME2xMlExODJ{IN88US=> NIDaRnFUSU6JRWK=
TE-9 NWC2R|JVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXlTWM2OD1zLkGxN|I5KM7:TR?= M1HwWXNCVkeHUh?=
SF126 NVjKb5FrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHHemV1UUN3ME2xMlEyPTZ6IN88US=> NYfU[YFZW0GQR1XS
BB30-HNC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTFXXl2UUN3ME2xMlE{OTF{IN88US=> NXXn[JhvW0GQR1XS
NCI-H1304 NEHj[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1X5XWlEPTB;MT6xN|M{QCEQvF2= NHzhSmNUSU6JRWK=
HEL MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojQTWM2OD1zLkG0PFk2KM7:TR?= MnHCV2FPT0WU
HAL-01 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLpT5BLUUN3ME2xMlE2Ojh|IN88US=> MnXHV2FPT0WU
SK-LMS-1 NV20UHdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfkTWM2OD1zLkG1PVc1KM7:TR?= NFH0N|FUSU6JRWK=
SW954 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jyWGlEPTB;MT6xPVU3PyEQvF2= NY\1XW5XW0GQR1XS
D-283MED NVTTTGdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFwMkKzO|kh|ryP NF76[4ZUSU6JRWK=
NCI-H1882 NX76c453T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T1[2lEPTB;MT6yN|g6KM7:TR?= M{\qUXNCVkeHUh?=
GI-ME-N NF[yXWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iz[mlEPTB;MT6yOVIxQCEQvF2= MVzTRW5ITVJ?
SK-PN-DW MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj4bFQxUUN3ME2xMlI3OzR6IN88US=> NEX3cplUSU6JRWK=
C2BBe1 M1\4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPsNZVKSzVyPUGuNlkyOTdizszN MoDmV2FPT0WU
A704 M2\nemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwM{K2PFkh|ryP M3zDenNCVkeHUh?=
KALS-1 M13tXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfO[mMxUUN3ME2xMlM1ODhizszN MlPIV2FPT0WU
ETK-1 M{TCXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHnSFE6UUN3ME2xMlM1PDh7IN88US=> MlzsV2FPT0WU
LB647-SCLC M2LH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC1TWM2OD1zLkO0PVg3KM7:TR?= M2TsVXNCVkeHUh?=
OCUB-M NH6xZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjye2pKSzVyPUGuN|YyPDNizszN MUnTRW5ITVJ?
NCI-H720 M4K4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofsTWM2OD1zLkO2N|c5KM7:TR?= MoG4V2FPT0WU
NB13 NHTYfmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\ye5hKSzVyPUGuN|czQTNizszN M3jTcHNCVkeHUh?=
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DU-4475 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nY[GlEPTB;MT60OVg2OyEQvF2= NED3ZVhUSU6JRWK=
HCC2157 NGr2[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fSNWlEPTB;MT60OlY2QSEQvF2= NEPB[3NUSU6JRWK=
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LS-123 MoTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HTc2lEPTB;MT61NVU6PCEQvF2= MYLTRW5ITVJ?
NCI-H69 NXTO[oFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLQWo1zUUN3ME2xMlU2QDFzIN88US=> M4TCUnNCVkeHUh?=
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PF-382 NVjVdWpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TpWGlEPTB;MT61Olk3KM7:TR?= NVO1VmM{W0GQR1XS
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NB10 MlHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXERpJKSzVyPUGuOVc{QTJizszN NW\pZnM1W0GQR1XS
NB5 NIDJbpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXWOGhVUUN3ME2xMlU5PDd4IN88US=> NUDITlNuW0GQR1XS
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HT-144 M{TjZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTlR5kzUUN3ME2xMlY{OTlizszN NV7wfmg2W0GQR1XS
NCI-H524 NX76VmVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTZSZVPUUN3ME2xMlY1OzB5IN88US=> NG\GfItUSU6JRWK=
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NCI-H187 NWq1VpBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfVTWM2OD1zLkewNFM3KM7:TR?= NW[3UWRNW0GQR1XS
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Daudi MojiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHxWm1KSzVyPUGuO|g6PjdizszN Mn;LV2FPT0WU
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NB7 NEKx[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PtT2lEPTB;Mj6wNFU2PSEQvF2= MXLTRW5ITVJ?
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LOXIMVI NFfQdJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJwME[3PFYh|ryP M3jFOHNCVkeHUh?=
NCI-H1581 M{LL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XnVGlEPTB;Mj6xNVU2QSEQvF2= NUjWeWg6W0GQR1XS
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NCI-H526 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmOxTWM2OD1{LkG5NVQyKM7:TR?= M2WxZ3NCVkeHUh?=
MSTO-211H M1m5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPMTXZ7UUN3ME2yMlIxODRzIN88US=> NUDWemJlW0GQR1XS
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NCI-SNU-1 MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vaO2lEPTB;Mj6zN|I2PiEQvF2= M3nSO3NCVkeHUh?=
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NCI-H1395 M1XkeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTPcmZ[UUN3ME2yMlgzODF{IN88US=> MX3TRW5ITVJ?
A388 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJwOU[xO{DPxE1? NFGzVmhUSU6JRWK=
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HD-MY-Z NGfLb2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCwTWM2OD1|LkGzNlA{KM7:TR?= NUjpU2NzW0GQR1XS
NCI-H510A Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTNwMUi5OFMh|ryP M3rlTXNCVkeHUh?=
NCI-N87 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVixcFBwUUN3ME2zMlIxODJizszN M4Ozd3NCVkeHUh?=
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SH-4 NHnKdphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTNwMki3PVch|ryP NXS5U4tjW0GQR1XS
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KM12 MlTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPaTWM2OD1|LkOzOVQ1KM7:TR?= MoTEV2FPT0WU
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HC-1 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr5RoR1UUN3ME2zMlYzODJ6IN88US=> NFTabYxUSU6JRWK=
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BC-3 M1ziV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDzTWM2OD12LkGzNFY5KM7:TR?= MVLTRW5ITVJ?
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MDA-MB-134-VI NYfR[GVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjsclh6UUN3ME20MlMxPjBzIN88US=> MlzVV2FPT0WU
Becker MmnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjwW|VKSzVyPUSuOFc{OzZizszN NVPKNHB[W0GQR1XS
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TGBC1TKB MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLwSGpKSzVyPUSuOlg2OTVizszN NG\sXHFUSU6JRWK=
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KE-37 NITwe2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XkWmlEPTB;ND64OlE6PiEQvF2= Ml3VV2FPT0WU
NCI-H23 M13pSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fIbWlEPTB;ND64O|IzPyEQvF2= NYXjfHRCW0GQR1XS
MC116 M3f2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rHdmlEPTB;ND65OFEzPiEQvF2= NH3MdGVUSU6JRWK=
NH-12 M{XGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoG5TWM2OD12Lkm2OFM6KM7:TR?= MW\TRW5ITVJ?
CTB-1 M2j2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXR[49KSzVyPUSuPVc4OjFizszN NGnBb5pUSU6JRWK=
KM-H2 NX7UfHJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zCS2lEPTB;NT6wOVMzOyEQvF2= NHjEcplUSU6JRWK=
MOLT-4 M{PNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnweVlKSzVyPUWuNVE5OyEQvF2= NYj2WmY{W0GQR1XS
NCI-H2141 NU[0Z4JWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LuSWlEPTB;NT6xOFI3QCEQvF2= NVrR[nVDW0GQR1XS
EB-3 M370OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7xeZpKSzVyPUWuNVc2ODRizszN M3jVbXNCVkeHUh?=
NCI-H1522 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTVwMk[zNlIh|ryP MnnOV2FPT0WU
MRK-nu-1 Ml;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGKwb2RKSzVyPUWuOFM3OzNizszN MYTTRW5ITVJ?
no-11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPoTWM2OD13LkS3NFg4KM7:TR?= MXTTRW5ITVJ?
CESS MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTVwNUiwN|Qh|ryP MX;TRW5ITVJ?
KMOE-2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTVwNUi2OVkh|ryP MVTTRW5ITVJ?
REH NHyzUIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXUS4hKSzVyPU[uNlU3OThizszN MXPTRW5ITVJ?
KU812 NFKyc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrFbGlKSzVyPU[uOFI4QTFizszN MV\TRW5ITVJ?
SK-N-FI M1nNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILnS21KSzVyPU[uOlA3PzRizszN MYTTRW5ITVJ?
MMAC-SF M1PaVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\BTWM2OD15LkC2OFkzKM7:TR?= NYfqU3ZNW0GQR1XS
RCC10RGB MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTdwMkK5O|ch|ryP MkK4V2FPT0WU
NCI-H322M NWTFVnBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTdwM{OzN|Uh|ryP NUXBWJh1W0GQR1XS
NB6 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjydXBWUUN3ME23MlU1QDl7IN88US=> M{LHVnNCVkeHUh?=
MN-60 M17ER2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTdwNkmyNVUh|ryP MYTTRW5ITVJ?
NCI-H1092 M2jYbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;WclZKSzVyPUiuNFE4OzRizszN MnfGV2FPT0WU
EKVX M{LTdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i4d2lEPTB;OD60O|A3PiEQvF2= MYnTRW5ITVJ?
D-263MG MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvyTppQUUN3ME24MlU2Ozl4IN88US=> M2PRZ3NCVkeHUh?=
NCI-H209 NXTlcm06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRThwNkSwNFYh|ryP NXvyd2VEW0GQR1XS
IST-SL1 NVPUZm1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmOwTWM2OD16Lki5PFkzKM7:TR?= MXnTRW5ITVJ?
ACN MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37ReGlEPTB;OT6xPVE2PyEQvF2= NX7mZ3c5W0GQR1XS
MHH-PREB-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTLWmFFUUN3ME25MlIyOjF7IN88US=> M3PZd3NCVkeHUh?=
EW-11 M3fTemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrDNYhtUUN3ME25MlY2Ozl4IN88US=> MVHTRW5ITVJ?
KASUMI-1 NUmwS3VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S5e2lEPTB;OT63PFc4KM7:TR?= NUXoRXRqW0GQR1XS
KINGS-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjjTWM2OD1zMD6yN|Q4KM7:TR?= NXvaXllMW0GQR1XS
EVSA-T Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\ado1KSzVyPUGwMlMyQTJizszN MVvTRW5ITVJ?
DSH1 NGXI[mVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFyLkO5O|Ih|ryP MlG0V2FPT0WU
COLO-824 Mmi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFyLki2Olkh|ryP NILXSo1USU6JRWK=
K052 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFyLkmzNlIh|ryP MlzwV2FPT0WU
SK-MEL-2 Ml3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFyLkm5N|kh|ryP MVHTRW5ITVJ?

... 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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