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 M{ezWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XVUmlEPTB;MD6wNFAxPjB|IN88US=> M1vSc3NCVkeHUh?=
SF539 M17PUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1juUWlEPTB;MD6wNFA2PjRizszN MmnnV2FPT0WU
DEL M{LOSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnaRlZKSzVyPUCuNFAxQTJ5IN88US=> NFXCe4lUSU6JRWK=
NB1 M1fVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XXdGlEPTB;MD6wNFE3OiEQvF2= NYfXTHp5W0GQR1XS
SR Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HlNGlEPTB;MD6wNFI4PyEQvF2= MYfTRW5ITVJ?
KARPAS-299 MoXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjlTWM2OD1yLkCyN|g1KM7:TR?= M4nxW3NCVkeHUh?=
MHH-CALL-2 M17Vfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHXTWM2OD1yLkCyPVUzKM7:TR?= NHrDUI9USU6JRWK=
SU-DHL-1 M{CxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:wcnFKSzVyPUCuNFQ5PjVizszN NU\SZ3hoW0GQR1XS
A4-Fuk NX3r[3J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInmb5dKSzVyPUCuNFU2PjVizszN M1HnZ3NCVkeHUh?=
EW-1 MljjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3FVFBKSzVyPUCuNVAzPTZizszN MW\TRW5ITVJ?
NOS-1 M4\ObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS2PXhQUUN3ME2wMlExOjl2IN88US=> MnLDV2FPT0WU
EW-16 M1Pze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mor6TWM2OD1yLkGwOVY5KM7:TR?= MXrTRW5ITVJ?
TE-11 NYWyOmxjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzlV4s{UUN3ME2wMlE3ODl4IN88US=> NX;RNmFFW0GQR1XS
SW982 MkHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwMU[0O|gh|ryP NHnBVHpUSU6JRWK=
LAN-6 NGfsR2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwMUe0OFMh|ryP MnXzV2FPT0WU
MZ1-PC NHrkRYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjYOmZKSzVyPUCuNVc5OzVizszN NI\CV5NUSU6JRWK=
KS-1 MoLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfLXIFXUUN3ME2wMlE6OzR|IN88US=> MmPsV2FPT0WU
PSN1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXNTWM2OD1yLkG5OlMyKM7:TR?= MmG3V2FPT0WU
LC-2-ad Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPjdWtKSzVyPUCuNVk3QTJizszN NWPSdGNsW0GQR1XS
COLO-320-HSR NXrvZlNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwMUm3O|Yh|ryP MlrLV2FPT0WU
OPM-2 NH7oWmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMkK2Olkh|ryP NXrleVVyW0GQR1XS
SK-NEP-1 NHfq[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LWcGlEPTB;MD6yN|UzPCEQvF2= M2juU3NCVkeHUh?=
ALL-PO M1jvbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm3fWpKSzVyPUCuNlQ2OjRizszN MU\TRW5ITVJ?
CMK NFrJOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwMkW1N{DPxE1? M1rJNHNCVkeHUh?=
NCI-H1648 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvuTWM2OD1yLkK3PFU2KM7:TR?= MmLTV2FPT0WU
SIG-M5 NYX1T2hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHCTWM2OD1yLkK5NVU6KM7:TR?= MXzTRW5ITVJ?
TGBC24TKB M1jzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwM{CyNVgh|ryP M2O0UHNCVkeHUh?=
DOHH-2 NU\zUFFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLvdXRKSzVyPUCuN|EzODRizszN NVPPemtMW0GQR1XS
NB69 NGCzOVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLSbo5KSzVyPUCuN|E4QDdizszN M4qyZ3NCVkeHUh?=
MFH-ino NH\jcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPNWlloUUN3ME2wMlMzPTJ|IN88US=> MlOyV2FPT0WU
KP-N-RT-BM-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLKNJpKSzVyPUCuN|MyOjNizszN MkLHV2FPT0WU
MONO-MAC-6 NU\TVHFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTVTWM2OD1yLkOzNlkyKM7:TR?= MorEV2FPT0WU
ATN-1 M4PxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnsPItKSzVyPUCuN|M{ODNizszN NIPRPGJUSU6JRWK=
NTERA-S-cl-D1 NXPBZpZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorzTWM2OD1yLkOzN|k3KM7:TR?= MVPTRW5ITVJ?
L-540 Mlr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTjOVBvUUN3ME2wMlM3QTh6IN88US=> MXPTRW5ITVJ?
GB-1 Ml7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPPOHRKSzVyPUCuN|g5PjdizszN NXnxW|hHW0GQR1XS
MV-4-11 NV7xdGo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme3TWM2OD1yLkO5OFQ3KM7:TR?= MVrTRW5ITVJ?
KG-1 Mn;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvweXl7UUN3ME2wMlM6PTZzIN88US=> NVnJNlRJW0GQR1XS
OVCAR-4 NGHJfJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwNEC1Olkh|ryP NVz4NlhVW0GQR1XS
NEC8 NIrUfXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPYWGpmUUN3ME2wMlQyOjl{IN88US=> NUjHOWlkW0GQR1XS
SK-MM-2 M4r2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwNEG2NFkh|ryP M3\xN3NCVkeHUh?=
TE-8 NYrubWp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwNEK4PEDPxE1? M3S2SXNCVkeHUh?=
697 NIjiNppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe1Z5ZKSzVyPUCuOFMzOTVizszN MXHTRW5ITVJ?
NB14 NH\BcoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXtNXVKSzVyPUCuOFM5OjZizszN NYPMVYJFW0GQR1XS
GDM-1 Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nWWGlEPTB;MD60O|EyPiEQvF2= Mn3FV2FPT0WU
HUTU-80 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj6TWM2OD1yLkS3N|c2KM7:TR?= MX\TRW5ITVJ?
HL-60 NXrnN3p{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\rNpRKSzVyPUCuOFgyPDJizszN NYfBRlE3W0GQR1XS
OCI-AML2 MoLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwNEizNlgh|ryP MkDQV2FPT0WU
ML-2 NWfrZZVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwNEmwN|Eh|ryP MljtV2FPT0WU
ES4 Ml\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC5[nFKSzVyPUCuOFkyODlizszN MkTnV2FPT0WU
NCI-H747 NUPzd2VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLDTWM2OD1yLkS5PFkh|ryP NEHvZZVUSU6JRWK=
RL95-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DsRWlEPTB;MD61NFEyOiEQvF2= MY\TRW5ITVJ?
TE-15 MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn5TW1sUUN3ME2wMlUyOTJ2IN88US=> NXO3dFc2W0GQR1XS
TE-12 NXzUPGNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTBwNUOzOFkh|ryP M{fQd3NCVkeHUh?=
LB1047-RCC MorPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnIR|VKSzVyPUCuOVQ2PDlizszN NIrLcm9USU6JRWK=
LB831-BLC MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXjTWM2OD1yLkW1NFI{KM7:TR?= NU\rfnkxW0GQR1XS
NCI-H1355 M{fCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXzO49EUUN3ME2wMlU2OTh2IN88US=> MorxV2FPT0WU
CTV-1 NYPxb|FrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvmXJl{UUN3ME2wMlU2PjJ2IN88US=> NH\WTWxUSU6JRWK=
RXF393 MnfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwNUW3PVQh|ryP M3PlPXNCVkeHUh?=
SW872 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXOXGRKSzVyPUCuOVY4OjRizszN NVfaTVVWW0GQR1XS
MPP-89 M1;0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwNUe4PFQh|ryP MnTsV2FPT0WU
RPMI-8226 NWnKfGNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDOOoFKSzVyPUCuOlM2OjZizszN M4frZnNCVkeHUh?=
LS-1034 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTBwNkO1PEDPxE1? NIP5[mtUSU6JRWK=
SJSA-1 NWDB[IRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwNkO3NlUh|ryP M2DvOXNCVkeHUh?=
HOP-62 M32yOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PI[GlEPTB;MD62OVA{OyEQvF2= MVTTRW5ITVJ?
KGN M3LOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfNTINKSzVyPUCuOlYyPjhizszN M1HjVXNCVkeHUh?=
D-336MG NFG4UGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwNk[xOlkh|ryP M4C3[HNCVkeHUh?=
LS-411N NV7LTYx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTJR4VKSzVyPUCuOlc1PjJizszN MYrTRW5ITVJ?
TE-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DkRWlEPTB;MD62PVA4PCEQvF2= NGLabIVUSU6JRWK=
LB996-RCC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3MeYVmUUN3ME2wMlY6Ozh7IN88US=> NIfUfVdUSU6JRWK=
TE-10 NXHENXFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXj4Z4xQUUN3ME2wMlcyPDl4IN88US=> M2C5[nNCVkeHUh?=
NCI-SNU-16 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHxbZVkUUN3ME2wMlczPjZ2IN88US=> MlH5V2FPT0WU
ES8 MoDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInzUYFKSzVyPUCuO|Q6PzVizszN NVTMVlZOW0GQR1XS
COLO-800 M3fMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYeyW5dLUUN3ME2wMlc3Pjl3IN88US=> NIjxdFdUSU6JRWK=
ES6 NETLfZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPjbmtjUUN3ME2wMlc4PTV7IN88US=> NVTBbHBNW0GQR1XS
L-363 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHJTWM2OD1yLkiyN|c2KM7:TR?= MYHTRW5ITVJ?
NMC-G1 MmTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7uTWM2OD1yLkizNlM{KM7:TR?= MUXTRW5ITVJ?
LU-134-A MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwOEO5NVIh|ryP NF24UodUSU6JRWK=
SF268 M4XDOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHlWphsUUN3ME2wMlg1ODR{IN88US=> NYe3SlJoW0GQR1XS
KARPAS-45 M3vSXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2zTWM2OD1yLki0NlY{KM7:TR?= M4nCdHNCVkeHUh?=
TGW M2LrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmToTWM2OD1yLki1PFY{KM7:TR?= M3jHS3NCVkeHUh?=
CHP-126 NYjN[5lbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HDSmlEPTB;MD64OVk2PyEQvF2= NEGyWYNUSU6JRWK=
MOLT-16 M1HjUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwOEe1PFkh|ryP NWjGOGFJW0GQR1XS
LB771-HNC NFjuRlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfBTWM2OD1yLki5O|U4KM7:TR?= NV33O2tzW0GQR1XS
NALM-6 NWq0So1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkO3TWM2OD1yLkmwO|M6KM7:TR?= NI\keVJUSU6JRWK=
GCIY NXWxSWdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfYdm9KSzVyPUCuPVU2OjZizszN M4XCenNCVkeHUh?=
IST-MES1 M2XH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\BTWM2OD1yLkm4PFI1KM7:TR?= MoHoV2FPT0WU
LB2241-RCC M1HhNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjid4NKSzVyPUCuPVg5PCEQvF2= MnW4V2FPT0WU
BL-70 NW\aVoZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvhSJFOUUN3ME2wMlk6PTN3IN88US=> NWjEbmUzW0GQR1XS
NB17 MmPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDTSmJKSzVyPUGuNFA3OzlizszN MXPTRW5ITVJ?
LXF-289 M{Tu[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\lR2lEPTB;MT6wN|A4PiEQvF2= MVLTRW5ITVJ?
TK10 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moe1TWM2OD1zLkC1NFY{KM7:TR?= NFz3OolUSU6JRWK=
K5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;6R|VKSzVyPUGuNFYzPzRizszN MWPTRW5ITVJ?
NCI-H716 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\lflFKSzVyPUGuNFczPTlizszN NVm5To52W0GQR1XS
HCE-T NFOx[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTjOWdCUUN3ME2xMlA5QDF7IN88US=> M1eyeXNCVkeHUh?=
GI-1 NUXl[HN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPNTWFKSzVyPUGuNFk4QThizszN M1XMWXNCVkeHUh?=
KARPAS-422 NF;WeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHtVmdKSzVyPUGuNVAxOjJizszN NVT1fGRnW0GQR1XS
TE-9 M{nhO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDrTWM2OD1zLkGxN|I5KM7:TR?= MnrOV2FPT0WU
SF126 NHf0TFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHuzeY9KSzVyPUGuNVE2PjhizszN M4nWRXNCVkeHUh?=
BB30-HNC NX7uRWN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjVZY1TUUN3ME2xMlE{OTF{IN88US=> MVrTRW5ITVJ?
NCI-H1304 NUnXSnVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwMUOzN|gh|ryP M1Tk[HNCVkeHUh?=
HEL MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[2SmcxUUN3ME2xMlE1QDl3IN88US=> MYDTRW5ITVJ?
HAL-01 NGjyW4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTFwMUWyPFMh|ryP M4O5dXNCVkeHUh?=
SK-LMS-1 NH\DWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwMUW5O|Qh|ryP MnSzV2FPT0WU
SW954 NEfnSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7lTWM2OD1zLkG5OVY4KM7:TR?= M2XiTHNCVkeHUh?=
D-283MED M2H1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFwMkKzO|kh|ryP Mn3UV2FPT0WU
NCI-H1882 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFwMkO4PUDPxE1? MV;TRW5ITVJ?
GI-ME-N MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml24TWM2OD1zLkK1NlA5KM7:TR?= MXjTRW5ITVJ?
SK-PN-DW NXHOWXBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3mcVVKSzVyPUGuNlY{PDhizszN NFPibJpUSU6JRWK=
C2BBe1 MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFwMkmxNVch|ryP NG\IXGJUSU6JRWK=
A704 M3vY[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDUVFJKSzVyPUGuN|I3QDlizszN MnjYV2FPT0WU
KALS-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwM{SwPEDPxE1? MX;TRW5ITVJ?
ETK-1 NUnwbY5NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv0VWFuUUN3ME2xMlM1PDh7IN88US=> MnTnV2FPT0WU
LB647-SCLC NX25VIJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTWTWM2OD1zLkO0PVg3KM7:TR?= MUfTRW5ITVJ?
OCUB-M NHrYfFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTtTWM2OD1zLkO2NVQ{KM7:TR?= MV;TRW5ITVJ?
NCI-H720 M{P5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXWdoRKSzVyPUGuN|Y{PzhizszN NXPsRZV6W0GQR1XS
NB13 MnO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFwM{eyPVMh|ryP NUPsdHBQW0GQR1XS
GR-ST NFuyPYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFwM{i3OVch|ryP NEHxe29USU6JRWK=
DU-4475 M1vtRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvybZZKSzVyPUGuOFU5PTNizszN NX3Jc3hmW0GQR1XS
HCC2157 MkjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O0cWlEPTB;MT60OlY2QSEQvF2= MWnTRW5ITVJ?
RKO NVjuOoVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTxTWM2OD1zLkS5PVIzKM7:TR?= NHz5XFBUSU6JRWK=
LS-123 NUnOWJlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvlTm5CUUN3ME2xMlUyPTl2IN88US=> NWHqfVFXW0GQR1XS
NCI-H69 NWr2NVhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXwfnFSUUN3ME2xMlU2QDFzIN88US=> MnLHV2FPT0WU
SW962 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DWOmlEPTB;MT61OlE{KM7:TR?= MVvTRW5ITVJ?
PF-382 MmX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPScVVKSzVyPUGuOVY6PiEQvF2= MUHTRW5ITVJ?
A101D NGXCdXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwNUexNVMh|ryP M1i1WXNCVkeHUh?=
NB10 NXvLcGNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3PTWM2OD1zLkW3N|kzKM7:TR?= M37ic3NCVkeHUh?=
NB5 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwNUi0O|Yh|ryP NHSxVm5USU6JRWK=
HCE-4 NUDuTlhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFwNkC4OUDPxE1? MnfBV2FPT0WU
HT-144 NXm1TGJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7oTWM2OD1zLk[zNVkh|ryP MnvoV2FPT0WU
NCI-H524 NVTpNVJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTFwNkSzNFch|ryP NI\kZpJUSU6JRWK=
NKM-1 NYLqWotUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnkTXd4UUN3ME2xMlY5PjZizszN MX7TRW5ITVJ?
KURAMOCHI MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFwNkm1O|Mh|ryP MljZV2FPT0WU
NCI-H187 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDrTWM2OD1zLkewNFM3KM7:TR?= M4C3R3NCVkeHUh?=
U-266 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDoT4dbUUN3ME2xMlc{QDR{IN88US=> MkizV2FPT0WU
BL-41 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDSTWM2OD1zLke2NlczKM7:TR?= MYLTRW5ITVJ?
SK-N-DZ MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX70UodyUUN3ME2xMlc5OzB7IN88US=> M2nyUHNCVkeHUh?=
Daudi M4nGTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwN{i5Olch|ryP NIrwfmNUSU6JRWK=
CPC-N NXjKbFBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTFwOEWwPVYh|ryP Ml7yV2FPT0WU
EM-2 NXriU|FOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPabJlKSzVyPUGuPFUyKM7:TR?= MV7TRW5ITVJ?
HCC1187 M{PId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTFwOE[yOFEh|ryP NFvx[ZNUSU6JRWK=
LP-1 NFP0S3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTFwOEexOFMh|ryP M2DTWXNCVkeHUh?=
CAS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWf3UYRKUUN3ME2xMlk5Ojl7IN88US=> MW\TRW5ITVJ?
NB7 NEDUUnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjlOGJKSzVyPUKuNFA2PTVizszN NVS0XFNoW0GQR1XS
VA-ES-BJ MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Tqd2lEPTB;Mj6wNVUyOyEQvF2= NIS4bGNUSU6JRWK=
SNU-C2B NGDLb5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITUWZJKSzVyPUKuNFM{PTFizszN MYfTRW5ITVJ?
LOXIMVI NUXYfYh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPVTWM2OD1{LkC2O|g3KM7:TR?= NX3vW4dWW0GQR1XS
NCI-H1581 M4TxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH2TWM2OD1{LkGxOVU6KM7:TR?= MX;TRW5ITVJ?
IST-SL2 NGXGO|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJwMUK0OFUh|ryP NHrLSZlUSU6JRWK=
NOMO-1 M37Be2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPq[oVKSzVyPUKuNVc3QDNizszN MV\TRW5ITVJ?
TE-6 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr0TWM2OD1{LkG5NFUh|ryP NGfvVYdUSU6JRWK=
NCI-H526 NWHPcnI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFS1dXBKSzVyPUKuNVkyPDFizszN MYPTRW5ITVJ?
MSTO-211H NYjZXYVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\PR5llUUN3ME2yMlIxODRzIN88US=> Mn\nV2FPT0WU
LS-513 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;GO3JKSzVyPUKuNlIzPjlizszN MXrTRW5ITVJ?
NCI-SNU-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojrTWM2OD1{LkOzNlU3KM7:TR?= NYXUWmN3W0GQR1XS
BB65-RCC NH7KPGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjE[I5JUUN3ME2yMlM4PDl|IN88US=> M2TQd3NCVkeHUh?=
GT3TKB MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nHc2lEPTB;Mj6zPVk4OiEQvF2= MXjTRW5ITVJ?
OS-RC-2 MlnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLNSmpOUUN3ME2yMlQzOzRzIN88US=> MmXIV2FPT0WU
NCI-H2126 NYn5WmJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n1PWlEPTB;Mj60N|Y4PCEQvF2= NYOxXVRxW0GQR1XS
SK-UT-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG4PHFlUUN3ME2yMlQ4PDZ5IN88US=> NFfPVmFUSU6JRWK=
DMS-114 NXX4WmExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnWXHhKSzVyPUKuOlE2OjRizszN M{\hUHNCVkeHUh?=
ONS-76 M3fFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTyNFFKUUN3ME2yMlY{PjRzIN88US=> NEjzdVJUSU6JRWK=
8-MG-BA MoP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;KXmlEPTB;Mj62OVQyPCEQvF2= NHq4WYVUSU6JRWK=
BOKU MnjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3KVZNLUUN3ME2yMlczPzZ2IN88US=> MYLTRW5ITVJ?
LAMA-84 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jkRmlEPTB;Mj63PVkyOiEQvF2= NWKxVphmW0GQR1XS
ES1 M{XsWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jSfWlEPTB;Mj64NVgxPCEQvF2= NVLEcoFRW0GQR1XS
NCI-H1395 NIHrSVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJwOEKwNVIh|ryP MUfTRW5ITVJ?
A388 Mn7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHufmlFUUN3ME2yMlk3OTdizszN NXG0WZpmW0GQR1XS
NCCIT NHPOOIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfJTWM2OD1|LkC4PFYzKM7:TR?= Ml:zV2FPT0WU
HD-MY-Z M2LVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jYdWlEPTB;Mz6xN|IxOyEQvF2= NFHp[YNUSU6JRWK=
NCI-H510A NUeyPYZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTNwMUi5OFMh|ryP M{\pdHNCVkeHUh?=
NCI-N87 NGPFWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j0eGlEPTB;Mz6yNFAzKM7:TR?= NELvbXZUSU6JRWK=
SCLC-21H NVS4fZNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj5TWM2OD1|LkK2PFU6KM7:TR?= MULTRW5ITVJ?
SH-4 NXTCPZJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HISmlEPTB;Mz6yPFc6PyEQvF2= NHHXem5USU6JRWK=
QIMR-WIL MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XxPWlEPTB;Mz6zNlg1QSEQvF2= NWHmfW04W0GQR1XS
KM12 M3LrSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\VNI0{UUN3ME2zMlM{PTR2IN88US=> NELxSINUSU6JRWK=
ST486 NGX2dGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVn1RoQ3UUN3ME2zMlU{QDh|IN88US=> NH\UUYVUSU6JRWK=
HC-1 NWDz[nR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTNwNkKwNlgh|ryP MXfTRW5ITVJ?
BV-173 NFH5fYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjGSHVKSzVyPUOuOlQxQDhizszN MXjTRW5ITVJ?
EW-24 M4DnfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\sTWlEPTB;Mz62OlQ{PCEQvF2= MX3TRW5ITVJ?
LU-65 NF\QWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LoNWlEPTB;Mz62PFcyKM7:TR?= NHTrcm9USU6JRWK=
ECC4 MofGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVu1R5lYUUN3ME2zMlc4PTZizszN MV\TRW5ITVJ?
ARH-77 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTRwMUGwOlch|ryP MUPTRW5ITVJ?
BC-3 M3nTPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInheVhKSzVyPUSuNVMxPjhizszN NVzyW5E1W0GQR1XS
SNB75 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTRwMk[xPUDPxE1? NFe5U2lUSU6JRWK=
MEG-01 NET1dIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTRwMke0NVkh|ryP M2rzNXNCVkeHUh?=
NCI-H1417 M{fHd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlniTWM2OD12LkK4OFQ{KM7:TR?= NUDlSllLW0GQR1XS
MDA-MB-134-VI Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vFXWlEPTB;ND6zNFYxOSEQvF2= M3;PWHNCVkeHUh?=
Becker M{Gyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j6RmlEPTB;ND60O|M{PiEQvF2= MYDTRW5ITVJ?
DMS-153 MoqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TCcGlEPTB;ND62OlQ4PSEQvF2= NFnRVpFUSU6JRWK=
TGBC1TKB M33KfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjXWI5vUUN3ME20MlY5PTF3IN88US=> MkfKV2FPT0WU
EW-3 NH7LOYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPwd4JKSzVyPUSuO|YzPDhizszN NEjrbVhUSU6JRWK=
KE-37 M2LFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHhTWM2OD12Lki2NVk3KM7:TR?= NWezPFkxW0GQR1XS
NCI-H23 M3[1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTRwOEeyNlch|ryP NITxVoNUSU6JRWK=
MC116 NYfDVXRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13hSGlEPTB;ND65OFEzPiEQvF2= MmG5V2FPT0WU
NH-12 NYHlfI93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTRwOU[0N|kh|ryP Mmi3V2FPT0WU
CTB-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jXcGlEPTB;ND65O|czOSEQvF2= M4HuZ3NCVkeHUh?=
KM-H2 M4TNWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPJTWM2OD13LkC1N|I{KM7:TR?= NHfxS4xUSU6JRWK=
MOLT-4 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:1OYhiUUN3ME21MlEyQDNizszN NULnR3M2W0GQR1XS
NCI-H2141 MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DjPGlEPTB;NT6xOFI3QCEQvF2= M2LKc3NCVkeHUh?=
EB-3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj5[YtKSzVyPUWuNVc2ODRizszN MmX0V2FPT0WU
NCI-H1522 M{DIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTVwMk[zNlIh|ryP M3;WeXNCVkeHUh?=
MRK-nu-1 NWL3N2psT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H0cWlEPTB;NT60N|Y{OyEQvF2= MUHTRW5ITVJ?
no-11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnHW5VKSzVyPUWuOFcxQDdizszN M33jeXNCVkeHUh?=
CESS NXLMT49IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXpR4RKSzVyPUWuOVgxOzRizszN NH3YTWdUSU6JRWK=
KMOE-2 NH3HdVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jCUGlEPTB;NT61PFY2QSEQvF2= MWHTRW5ITVJ?
REH M12yS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTZwMkW2NVgh|ryP M4mwPXNCVkeHUh?=
KU812 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LPW2lEPTB;Nj60Nlc6OSEQvF2= NYHRVG91W0GQR1XS
SK-N-FI MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTZwNkC2O|Qh|ryP NYP5WW9yW0GQR1XS
MMAC-SF M2LXbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXGTWM2OD15LkC2OFkzKM7:TR?= MofVV2FPT0WU
RCC10RGB NXjZ[ms3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFmwT|RKSzVyPUeuNlI6PzdizszN NXPFc4JZW0GQR1XS
NCI-H322M MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fIUGlEPTB;Nz6zN|M{PSEQvF2= MnLSV2FPT0WU
NB6 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYGzNnFqUUN3ME23MlU1QDl7IN88US=> NU\wcnZRW0GQR1XS
MN-60 NWD1bZRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jDTmlEPTB;Nz62PVIyPSEQvF2= MkTDV2FPT0WU
NCI-H1092 NFLWUHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRThwMEG3N|Qh|ryP NFK1NXRUSU6JRWK=
EKVX MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD5TWM2OD16LkS3NFY3KM7:TR?= M1TEdXNCVkeHUh?=
D-263MG MorhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlKyTWM2OD16LkW1N|k3KM7:TR?= MnTlV2FPT0WU
NCI-H209 MmKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\EOWlEPTB;OD62OFAxPiEQvF2= NGfZPZFUSU6JRWK=
IST-SL1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HBemlEPTB;OD64PVg6OiEQvF2= Mo[xV2FPT0WU
ACN NG\qfm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ju[mlEPTB;OT6xPVE2PyEQvF2= MWnTRW5ITVJ?
MHH-PREB-1 NWLtblhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC4TWM2OD17LkKxNlE6KM7:TR?= NFvMeHpUSU6JRWK=
EW-11 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\PRXZKSzVyPUmuOlU{QTZizszN Mn;lV2FPT0WU
KASUMI-1 NGfRcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTlwN{i3O{DPxE1? NHzDXnZUSU6JRWK=
KINGS-1 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfQTWM2OD1zMD6yN|Q4KM7:TR?= NIX2NXJUSU6JRWK=
EVSA-T M1jqT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfIZo95UUN3ME2xNE4{OTl{IN88US=> NILUR5VUSU6JRWK=
DSH1 M1zq[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPJT3hKSzVyPUGwMlM6PzJizszN MlG1V2FPT0WU
COLO-824 NHvoSIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDneJlTUUN3ME2xNE45PjZ7IN88US=> MlHBV2FPT0WU
K052 Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\Fb2lEPTB;MUCuPVMzOiEQvF2= NYqyO3dWW0GQR1XS
SK-MEL-2 M1fXUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DmR2lEPTB;MUCuPVk{QSEQvF2= MV\TRW5ITVJ?

... 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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