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 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwMECwNFYxOyEQvF2= M2XqWXNCVkeHUh?=
SF539 NYnKSGZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwMECwOVY1KM7:TR?= M1jqVnNCVkeHUh?=
DEL MofiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TMNWlEPTB;MD6wNFA6OjdizszN NELsVlNUSU6JRWK=
NB1 MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwMECxOlIh|ryP M{DMfHNCVkeHUh?=
SR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vsOmlEPTB;MD6wNFI4PyEQvF2= MV7TRW5ITVJ?
KARPAS-299 NE[4fmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DrZmlEPTB;MD6wNlM5PCEQvF2= NVrXcJFPW0GQR1XS
MHH-CALL-2 MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vpbGlEPTB;MD6wNlk2OiEQvF2= M3vuTXNCVkeHUh?=
SU-DHL-1 MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwMES4OlUh|ryP M33E[HNCVkeHUh?=
A4-Fuk NW[xVGc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD2TWM2OD1yLkC1OVY2KM7:TR?= NYftXJVGW0GQR1XS
EW-1 NYTCco43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnVOFVKSzVyPUCuNVAzPTZizszN MVrTRW5ITVJ?
NOS-1 NEHySWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;rVGlEPTB;MD6xNFI6PCEQvF2= NFyxXWtUSU6JRWK=
EW-16 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwMUC1Olgh|ryP M3PwSnNCVkeHUh?=
TE-11 M1HwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwMU[wPVYh|ryP NXnCfGZiW0GQR1XS
SW982 NGXiZWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwMU[0O|gh|ryP Mkj3V2FPT0WU
LAN-6 M1P6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwMUe0OFMh|ryP M3zXZ3NCVkeHUh?=
MZ1-PC NIjSdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOxTWM2OD1yLkG3PFM2KM7:TR?= NH7pdFBUSU6JRWK=
KS-1 M2m4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInOTWNKSzVyPUCuNVk{PDNizszN MYnTRW5ITVJ?
PSN1 NYryWphLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:5emlEPTB;MD6xPVY{OSEQvF2= NFvkU2JUSU6JRWK=
LC-2-ad NEW0SHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwMUm2PVIh|ryP M3vaNnNCVkeHUh?=
COLO-320-HSR NFPp[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonXTWM2OD1yLkG5O|c3KM7:TR?= MYTTRW5ITVJ?
OPM-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPmXoJKUUN3ME2wMlIzPjZ7IN88US=> M2fRZnNCVkeHUh?=
SK-NEP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMkO1NlQh|ryP MWnTRW5ITVJ?
ALL-PO NGj2W3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;ueGV5UUN3ME2wMlI1PTJ2IN88US=> NV;5NZJCW0GQR1XS
CMK NVfrWIlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPCVIxCUUN3ME2wMlI2PTNizszN M1nCVXNCVkeHUh?=
NCI-H1648 NIHBfIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwMke4OVUh|ryP MULTRW5ITVJ?
SIG-M5 M3X1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWqzRmlZUUN3ME2wMlI6OTV7IN88US=> MlPvV2FPT0WU
TGBC24TKB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;vcVJKSzVyPUCuN|AzOThizszN MYfTRW5ITVJ?
DOHH-2 NH3JdG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy0OXNKSzVyPUCuN|EzODRizszN MYnTRW5ITVJ?
NB69 Mn:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7UTWM2OD1yLkOxO|g4KM7:TR?= NFTnfYRUSU6JRWK=
MFH-ino M{nFNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nOWmlEPTB;MD6zNlUzOyEQvF2= M33VdXNCVkeHUh?=
KP-N-RT-BM-1 NG\YVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jDbmlEPTB;MD6zN|EzOyEQvF2= NWT1c5B{W0GQR1XS
MONO-MAC-6 NHv0blRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC0fWFCUUN3ME2wMlM{OjlzIN88US=> NIfFUpVUSU6JRWK=
ATN-1 NFf0cVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO0e4xQUUN3ME2wMlM{OzB|IN88US=> NUHrSY1nW0GQR1XS
NTERA-S-cl-D1 NGXvTVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwM{OzPVYh|ryP NHfzUZJUSU6JRWK=
L-540 NWS4XWNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwM{[5PFgh|ryP Ml3GV2FPT0WU
GB-1 MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwM{i4Olch|ryP NXywfY1oW0GQR1XS
MV-4-11 NEjHXVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOyTWM2OD1yLkO5OFQ3KM7:TR?= M{TjS3NCVkeHUh?=
KG-1 MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\TPWlEPTB;MD6zPVU3OSEQvF2= MljEV2FPT0WU
OVCAR-4 NFfmWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fhbmlEPTB;MD60NFU3QSEQvF2= NXvDSFRXW0GQR1XS
NEC8 NUDLZ|VlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjsPXBKSzVyPUCuOFEzQTJizszN NXPudWxPW0GQR1XS
SK-MM-2 M{K3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL6TWM2OD1yLkSxOlA6KM7:TR?= MnzyV2FPT0WU
TE-8 M4LsTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwNEK4PEDPxE1? M4\NS3NCVkeHUh?=
697 NV\QOVdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjpTWM2OD1yLkSzNlE2KM7:TR?= MnjRV2FPT0WU
NB14 NILkW45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXGTWM2OD1yLkSzPFI3KM7:TR?= MlTXV2FPT0WU
GDM-1 MnrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwNEexNVYh|ryP M4WyXnNCVkeHUh?=
HUTU-80 M1PEbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe5[3dKSzVyPUCuOFc{PzVizszN NVfPb|ZVW0GQR1XS
HL-60 M1Lxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LkN2lEPTB;MD60PFE1OiEQvF2= NGHpUHNUSU6JRWK=
OCI-AML2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfqdZJDUUN3ME2wMlQ5OzJ6IN88US=> NETIeY5USU6JRWK=
ML-2 M2DaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwNEmwN|Eh|ryP MYTTRW5ITVJ?
ES4 NW\2[mRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwNEmxNFkh|ryP M4fLVHNCVkeHUh?=
NCI-H747 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq4fG5ZUUN3ME2wMlQ6QDlizszN MnviV2FPT0WU
RL95-2 NEnsc5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHziPXhKSzVyPUCuOVAyOTJizszN MUnTRW5ITVJ?
TE-15 MoP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfUNWlQUUN3ME2wMlUyOTJ2IN88US=> MkW3V2FPT0WU
TE-12 M4fQdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3STWM2OD1yLkWzN|Q6KM7:TR?= NWLWeW12W0GQR1XS
LB1047-RCC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXqe5VKSzVyPUCuOVQ2PDlizszN NYDvcpZuW0GQR1XS
LB831-BLC Mo\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnzTWM2OD1yLkW1NFI{KM7:TR?= NVzVenRZW0GQR1XS
NCI-H1355 NU\lSG1bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXwTWM2OD1yLkW1NVg1KM7:TR?= MU\TRW5ITVJ?
CTV-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULRNXhqUUN3ME2wMlU2PjJ2IN88US=> Mm\SV2FPT0WU
RXF393 Mln3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\sdXdKSzVyPUCuOVU4QTRizszN MYfTRW5ITVJ?
SW872 NXuyN2p7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXm3cI0xUUN3ME2wMlU3PzJ2IN88US=> NWLie2NFW0GQR1XS
MPP-89 M{XZbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GyNWlEPTB;MD61O|g5PCEQvF2= NITmOJNUSU6JRWK=
RPMI-8226 M4f4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf0T4FWUUN3ME2wMlY{PTJ4IN88US=> NGn0cnpUSU6JRWK=
LS-1034 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXtflRKSzVyPUCuOlM2QCEQvF2= Mn3WV2FPT0WU
SJSA-1 NXj5c4xOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvaSWtCUUN3ME2wMlY{PzJ3IN88US=> NITrb3lUSU6JRWK=
HOP-62 M2nFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwNkWwN|Mh|ryP MWnTRW5ITVJ?
KGN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPpfZVFUUN3ME2wMlY3OTZ6IN88US=> MWnTRW5ITVJ?
D-336MG M1[4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;rcldRUUN3ME2wMlY3OTZ7IN88US=> MnjqV2FPT0WU
LS-411N M2jHSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfZNVJTUUN3ME2wMlY4PDZ{IN88US=> M1XuWXNCVkeHUh?=
TE-1 M2LpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\nXndqUUN3ME2wMlY6ODd2IN88US=> MlGyV2FPT0WU
LB996-RCC NVj5O3d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNkmzPFkh|ryP NF\yXJhUSU6JRWK=
TE-10 NUfnZZc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkToTWM2OD1yLkexOFk3KM7:TR?= NIjtS|JUSU6JRWK=
NCI-SNU-16 NH;a[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTUTWM2OD1yLkeyOlY1KM7:TR?= NHjsZWxUSU6JRWK=
ES8 MnnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvYTWM2OD1yLke0PVc2KM7:TR?= MV;TRW5ITVJ?
COLO-800 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3WNXVzUUN3ME2wMlc3Pjl3IN88US=> MljMV2FPT0WU
ES6 Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwN{e1OVkh|ryP MmXmV2FPT0WU
L-363 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwOEKzO|Uh|ryP MlfTV2FPT0WU
NMC-G1 NYPST|BHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHZUWhsUUN3ME2wMlg{OjN|IN88US=> MYXTRW5ITVJ?
LU-134-A NF63O2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwOEO5NVIh|ryP MoHtV2FPT0WU
SF268 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInITlZKSzVyPUCuPFQxPDJizszN NHzuNmdUSU6JRWK=
KARPAS-45 M2q0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXe5NJJ3UUN3ME2wMlg1OjZ|IN88US=> M{\kWHNCVkeHUh?=
TGW NFHrO5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILZT5NKSzVyPUCuPFU5PjNizszN MYHTRW5ITVJ?
CHP-126 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwOEW5OVch|ryP Mm\pV2FPT0WU
MOLT-16 M{LBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwOEe1PFkh|ryP M4nwN3NCVkeHUh?=
LB771-HNC M3nLbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml33TWM2OD1yLki5O|U4KM7:TR?= NGTqWWhUSU6JRWK=
NALM-6 NUDBUFdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml35TWM2OD1yLkmwO|M6KM7:TR?= MXHTRW5ITVJ?
GCIY M4r4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwOUW1NlYh|ryP MYDTRW5ITVJ?
IST-MES1 M1v6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLacIhIUUN3ME2wMlk5QDJ2IN88US=> NHu2[VBUSU6JRWK=
LB2241-RCC NY\j[2xKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwOUi4OEDPxE1? NHvMZ3VUSU6JRWK=
BL-70 M17oVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTWeodxUUN3ME2wMlk6PTN3IN88US=> MV;TRW5ITVJ?
NB17 NIXBWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwMEC2N|kh|ryP NEnjR3NUSU6JRWK=
LXF-289 NFi0VYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkOwTWM2OD1zLkCzNFc3KM7:TR?= Ml\sV2FPT0WU
TK10 NXPpdZlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[yb45{UUN3ME2xMlA2ODZ|IN88US=> Ml7PV2FPT0WU
K5 M1XrW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\TRpNKSzVyPUGuNFYzPzRizszN NUHJNIRzW0GQR1XS
NCI-H716 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkO3TWM2OD1zLkC3NlU6KM7:TR?= Mm\PV2FPT0WU
HCE-T NVvVOG5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7OTWM2OD1zLkC4PFE6KM7:TR?= M4XFfHNCVkeHUh?=
GI-1 NVPDR|NyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT6TWM2OD1zLkC5O|k5KM7:TR?= NXzpZmlIW0GQR1XS
KARPAS-422 MoLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{G0VmlEPTB;MT6xNFAzOiEQvF2= MYXTRW5ITVJ?
TE-9 M2PsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjtV4xKSzVyPUGuNVE{OjhizszN MVfTRW5ITVJ?
SF126 NUi2[oxJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrBOGFKSzVyPUGuNVE2PjhizszN M4PiWXNCVkeHUh?=
BB30-HNC M1\1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;4R2lEPTB;MT6xN|EyOiEQvF2= M4T2d3NCVkeHUh?=
NCI-H1304 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGKxWIdKSzVyPUGuNVM{OzhizszN NYq3R|c{W0GQR1XS
HEL M{jvc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTFwMUS4PVUh|ryP M4XW[nNCVkeHUh?=
HAL-01 NFG1V|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHwWoRXUUN3ME2xMlE2Ojh|IN88US=> MWPTRW5ITVJ?
SK-LMS-1 NV21WpFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPkSXdKSzVyPUGuNVU6PzRizszN MoPDV2FPT0WU
SW954 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTFwMUm1Olch|ryP MV7TRW5ITVJ?
D-283MED MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TBfGlEPTB;MT6yNlM4QSEQvF2= NHrYfZBUSU6JRWK=
NCI-H1882 MlnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW5TWM2OD1zLkKzPFkh|ryP NIj3V|JUSU6JRWK=
GI-ME-N NHjvTVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljkTWM2OD1zLkK1NlA5KM7:TR?= Mm\EV2FPT0WU
SK-PN-DW NFjxOZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLXdIFrUUN3ME2xMlI3OzR6IN88US=> NWS4[IxLW0GQR1XS
C2BBe1 M{nHRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD4eHZOUUN3ME2xMlI6OTF5IN88US=> Mn7IV2FPT0WU
A704 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjYNVREUUN3ME2xMlMzPjh7IN88US=> M4\6fnNCVkeHUh?=
KALS-1 NHzwenNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nxTGlEPTB;MT6zOFA5KM7:TR?= NHrUO4pUSU6JRWK=
ETK-1 MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwM{S0PFkh|ryP MXLTRW5ITVJ?
LB647-SCLC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\ScmE1UUN3ME2xMlM1QTh4IN88US=> M1LvPXNCVkeHUh?=
OCUB-M M4rsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLTTWM2OD1zLkO2NVQ{KM7:TR?= NEnMRVVUSU6JRWK=
NCI-H720 MnrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFwM{[zO|gh|ryP M{nEdXNCVkeHUh?=
NB13 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFwM{eyPVMh|ryP NYCwfHR6W0GQR1XS
GR-ST NEPlSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7Ldo9EUUN3ME2xMlM5PzV5IN88US=> MmK4V2FPT0WU
DU-4475 M33XWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLBTWM2OD1zLkS1PFU{KM7:TR?= NWnaXGhGW0GQR1XS
HCC2157 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf4XnBPUUN3ME2xMlQ3PjV7IN88US=> Mn3PV2FPT0WU
RKO M3PCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfVSJpGUUN3ME2xMlQ6QTJ{IN88US=> MYjTRW5ITVJ?
LS-123 M2rNSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrKUllKSzVyPUGuOVE2QTRizszN MWXTRW5ITVJ?
NCI-H69 MnrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXqeWlKSzVyPUGuOVU5OTFizszN MYfTRW5ITVJ?
SW962 M{jtbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkWzTWM2OD1zLkW2NVMh|ryP M1WwcXNCVkeHUh?=
PF-382 M{PUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;hTWM2OD1zLkW2PVYh|ryP MW\TRW5ITVJ?
A101D Mm\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjBTWM2OD1zLkW3NVE{KM7:TR?= MonTV2FPT0WU
NB10 M3T1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwNUezPVIh|ryP NGLveGVUSU6JRWK=
NB5 M3j5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXK4NGdoUUN3ME2xMlU5PDd4IN88US=> NUfIRZlKW0GQR1XS
HCE-4 MmrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XGbmlEPTB;MT62NFg2KM7:TR?= NHXrOFVUSU6JRWK=
HT-144 NUDle2RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwNkOxPUDPxE1? NWTxRXVCW0GQR1XS
NCI-H524 MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG3W4pNUUN3ME2xMlY1OzB5IN88US=> MYXTRW5ITVJ?
NKM-1 NFm5R|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fZO2lEPTB;MT62PFY3KM7:TR?= Mn7JV2FPT0WU
KURAMOCHI M{[4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjxcmlKSzVyPUGuOlk2PzNizszN Mo\CV2FPT0WU
NCI-H187 NV7CWIR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LYXWlEPTB;MT63NFA{PiEQvF2= MnzOV2FPT0WU
U-266 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS2TWM2OD1zLkezPFQzKM7:TR?= MWnTRW5ITVJ?
BL-41 NWHaNW84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTFwN{[yO|Ih|ryP NUDrbnBGW0GQR1XS
SK-N-DZ MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS3TZJKSzVyPUGuO|g{ODlizszN NEDCSJlUSU6JRWK=
Daudi MmHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILGdJpKSzVyPUGuO|g6PjdizszN NFnM[HBUSU6JRWK=
CPC-N MnK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkSwTWM2OD1zLki1NFk3KM7:TR?= NGLDS5RUSU6JRWK=
EM-2 NGC5OHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP6eI5KSzVyPUGuPFUyKM7:TR?= M3\hVnNCVkeHUh?=
HCC1187 NVqyWlJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD1TWM2OD1zLki2NlQyKM7:TR?= NYraZZBOW0GQR1XS
LP-1 NX6wV3NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofQTWM2OD1zLki3NVQ{KM7:TR?= NWDUWXd5W0GQR1XS
CAS-1 M1O5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnmwTWM2OD1zLkm4Nlk6KM7:TR?= Mnu3V2FPT0WU
NB7 MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3uU4o4UUN3ME2yMlAxPTV3IN88US=> Mn35V2FPT0WU
VA-ES-BJ Mn7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDrXFVKSzVyPUKuNFE2OTNizszN NVrkdHFkW0GQR1XS
SNU-C2B MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfFSoI6UUN3ME2yMlA{OzVzIN88US=> M3n1fHNCVkeHUh?=
LOXIMVI MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJwME[3PFYh|ryP MX7TRW5ITVJ?
NCI-H1581 NGHTRZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYqzPZBGUUN3ME2yMlEyPTV7IN88US=> MWXTRW5ITVJ?
IST-SL2 NWLjeFR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjzT29KSzVyPUKuNVI1PDVizszN MVLTRW5ITVJ?
NOMO-1 M1rpZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:1UFFZUUN3ME2yMlE4Pjh|IN88US=> NGexVYVUSU6JRWK=
TE-6 M4e3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrv[FFKSzVyPUKuNVkxPSEQvF2= NIfmUmpUSU6JRWK=
NCI-H526 NWfEUZF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m5OmlEPTB;Mj6xPVE1OSEQvF2= M3r4fHNCVkeHUh?=
MSTO-211H NVfaN4ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoiyTWM2OD1{LkKwNFQyKM7:TR?= NYDucY9[W0GQR1XS
LS-513 MmfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJwMkKyOlkh|ryP M4fwTHNCVkeHUh?=
NCI-SNU-1 M4WydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHq0fW5KSzVyPUKuN|MzPTZizszN MUnTRW5ITVJ?
BB65-RCC Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTyTlFrUUN3ME2yMlM4PDl|IN88US=> M{DaeXNCVkeHUh?=
GT3TKB NG\4e5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXOTpNKSzVyPUKuN|k6PzJizszN NHH4Z4tUSU6JRWK=
OS-RC-2 M2LVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\XSWlEPTB;Mj60NlM1OSEQvF2= NHvENGtUSU6JRWK=
NCI-H2126 NIP0fFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnjb5VKSzVyPUKuOFM3PzRizszN MXjTRW5ITVJ?
SK-UT-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJwNEe0Olch|ryP NFPjeHhUSU6JRWK=
DMS-114 M1HMcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJwNkG1NlQh|ryP NGXubphUSU6JRWK=
ONS-76 M3LhV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzDTWM2OD1{Lk[zOlQyKM7:TR?= NHPmNFJUSU6JRWK=
8-MG-BA NWi2Oo17T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLhTWM2OD1{Lk[1OFE1KM7:TR?= NXHyeGdZW0GQR1XS
BOKU NGjSVGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnjTWM2OD1{LkeyO|Y1KM7:TR?= M2PT[HNCVkeHUh?=
LAMA-84 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\JO|BsUUN3ME2yMlc6QTF{IN88US=> Mom5V2FPT0WU
ES1 NHX4OmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTsb2xoUUN3ME2yMlgyQDB2IN88US=> M1f1T3NCVkeHUh?=
NCI-H1395 NIjNUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTJTWM2OD1{LkiyNFEzKM7:TR?= NYTReWVKW0GQR1XS
A388 MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nwWGlEPTB;Mj65OlE4KM7:TR?= M3n0eXNCVkeHUh?=
NCCIT M4nVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nwXWlEPTB;Mz6wPFg3OiEQvF2= M2[y[XNCVkeHUh?=
HD-MY-Z M3nneWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jyO2lEPTB;Mz6xN|IxOyEQvF2= MWDTRW5ITVJ?
NCI-H510A MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f0S2lEPTB;Mz6xPFk1OyEQvF2= NYjIbIo1W0GQR1XS
NCI-N87 NUPxeZhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnZUoxlUUN3ME2zMlIxODJizszN MoLSV2FPT0WU
SCLC-21H NH3kNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi1NZBIUUN3ME2zMlI3QDV7IN88US=> M4HOPXNCVkeHUh?=
SH-4 NUPUOVhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3RXnlKSzVyPUOuNlg4QTdizszN NHz3[pVUSU6JRWK=
QIMR-WIL MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDoTWM2OD1|LkOyPFQ6KM7:TR?= M3rhO3NCVkeHUh?=
KM12 M1vrTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIC5ZWtKSzVyPUOuN|M2PDRizszN MV7TRW5ITVJ?
ST486 NFjrV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTNwNUO4PFMh|ryP NWrESG02W0GQR1XS
HC-1 NFm2WmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXr[YJKSzVyPUOuOlIxOjhizszN NXvKPXhLW0GQR1XS
BV-173 M2\meWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTNwNkSwPFgh|ryP M2H2cHNCVkeHUh?=
EW-24 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTNwNk[0N|Qh|ryP MlfmV2FPT0WU
LU-65 M2ji[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj4RlJlUUN3ME2zMlY5PzFizszN MlLEV2FPT0WU
ECC4 NFrkS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHp[GZpUUN3ME2zMlc4PTZizszN MnG2V2FPT0WU
ARH-77 M3HBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jXRWlEPTB;ND6xNVA3PyEQvF2= MVnTRW5ITVJ?
BC-3 NIHGdnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPEW|NKSzVyPUSuNVMxPjhizszN M4HNW3NCVkeHUh?=
SNB75 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDnZmVKSzVyPUSuNlYyQSEQvF2= MVrTRW5ITVJ?
MEG-01 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fIO2lEPTB;ND6yO|QyQSEQvF2= NYDmOFVGW0GQR1XS
NCI-H1417 M2HCRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTRwMki0OFMh|ryP NUfqWpplW0GQR1XS
MDA-MB-134-VI MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrZTWM2OD12LkOwOlAyKM7:TR?= NHfSe2FUSU6JRWK=
Becker NXrHPWd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTRwNEezN|Yh|ryP MnjIV2FPT0WU
DMS-153 NH;nbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn1TWM2OD12Lk[2OFc2KM7:TR?= NVr4S5JwW0GQR1XS
TGBC1TKB MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjlT3VKSzVyPUSuOlg2OTVizszN NUPlUoF1W0GQR1XS
EW-3 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTRwN{[yOFgh|ryP MXjTRW5ITVJ?
KE-37 NFjNeVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3GeIh{UUN3ME20Mlg3OTl4IN88US=> MXfTRW5ITVJ?
NCI-H23 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{npN2lEPTB;ND64O|IzPyEQvF2= Ml\vV2FPT0WU
MC116 M3fOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M320T2lEPTB;ND65OFEzPiEQvF2= NUX0VHQ3W0GQR1XS
NH-12 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTRwOU[0N|kh|ryP NYnzd5JSW0GQR1XS
CTB-1 M4G0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWqwTWhlUUN3ME20Mlk4PzJzIN88US=> NWK5PFRLW0GQR1XS
KM-H2 Mn3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jtVmlEPTB;NT6wOVMzOyEQvF2= M2PYdXNCVkeHUh?=
MOLT-4 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTVwMUG4N{DPxE1? NVvtfotmW0GQR1XS
NCI-H2141 M2XwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n6OWlEPTB;NT6xOFI3QCEQvF2= MY\TRW5ITVJ?
EB-3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLLTWM2OD13LkG3OVA1KM7:TR?= M4HUO3NCVkeHUh?=
NCI-H1522 NWTiSot7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq2fnVKSzVyPUWuNlY{OjJizszN Ml3yV2FPT0WU
MRK-nu-1 M322UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\BU3RGUUN3ME21MlQ{PjN|IN88US=> NEnnNWpUSU6JRWK=
no-11 NX7VRldpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX5[o1KSzVyPUWuOFcxQDdizszN M17sSnNCVkeHUh?=
CESS M4S1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTVwNUiwN|Qh|ryP Ml74V2FPT0WU
KMOE-2 NV7zV2p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfZTWM2OD13LkW4OlU6KM7:TR?= MV7TRW5ITVJ?
REH MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\EZo9WUUN3ME22MlI2PjF6IN88US=> Mn\0V2FPT0WU
KU812 Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPqR45KSzVyPU[uOFI4QTFizszN MWfTRW5ITVJ?
SK-N-FI MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSzdWtnUUN3ME22MlYxPjd2IN88US=> Mlm3V2FPT0WU
MMAC-SF NWjiNJFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\lbY1KSzVyPUeuNFY1QTJizszN NVPyUlhmW0GQR1XS
RCC10RGB NYXTUYRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnybZVKSzVyPUeuNlI6PzdizszN NGPjN25USU6JRWK=
NCI-H322M M176d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTRTWM2OD15LkOzN|M2KM7:TR?= NUjmfYFZW0GQR1XS
NB6 M2LHZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn4PY5pUUN3ME23MlU1QDl7IN88US=> NYHu[5lPW0GQR1XS
MN-60 NXr0VY82T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XqfGlEPTB;Nz62PVIyPSEQvF2= NWfEUm1uW0GQR1XS
NCI-H1092 NXzBTnhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2izOWlEPTB;OD6wNVc{PCEQvF2= M4X0PXNCVkeHUh?=
EKVX MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRThwNEewOlYh|ryP MnTOV2FPT0WU
D-263MG NEHNXVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXtTWM2OD16LkW1N|k3KM7:TR?= M1O0TnNCVkeHUh?=
NCI-H209 M{nT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPxT4dKSzVyPUiuOlQxODZizszN M2nicXNCVkeHUh?=
IST-SL1 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXoTWM2OD16Lki5PFkzKM7:TR?= NV3oS2dZW0GQR1XS
ACN MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjOO2dKSzVyPUmuNVkyPTdizszN MYrTRW5ITVJ?
MHH-PREB-1 MoTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7ITWM2OD17LkKxNlE6KM7:TR?= M4f0[HNCVkeHUh?=
EW-11 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ntSGlEPTB;OT62OVM6PiEQvF2= NWHzSpZxW0GQR1XS
KASUMI-1 NUDtNFFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfkTWM2OD17Lke4O|ch|ryP NV2xOnNkW0GQR1XS
KINGS-1 NHruTYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFyLkKzOFch|ryP NHXJZWVUSU6JRWK=
EVSA-T NXvDRZlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\yTWM2OD1zMD6zNVkzKM7:TR?= Mn7EV2FPT0WU
DSH1 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nldWlEPTB;MUCuN|k4OiEQvF2= MkfwV2FPT0WU
COLO-824 M12yT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELTW3ZKSzVyPUGwMlg3PjlizszN NILqOoxUSU6JRWK=
K052 MmTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{n0eGlEPTB;MUCuPVMzOiEQvF2= MmLTV2FPT0WU
SK-MEL-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTFyLkm5N|kh|ryP NF;OcnhUSU6JRWK=

... 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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