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、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 NHnieY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwMECwNFYxOyEQvF2= M2PmXnNCVkeHUh?=
SF539 NWrmdlNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH64TIFKSzVyPUCuNFAxPTZ2IN88US=> NWWwVo9lW0GQR1XS
DEL NFLKbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHnR3NKSzVyPUCuNFAxQTJ5IN88US=> M1fsbnNCVkeHUh?=
NB1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwMECxOlIh|ryP MnHIV2FPT0WU
SR Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwMECyO|ch|ryP MYrTRW5ITVJ?
KARPAS-299 NYLlS5hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrYcYNKSzVyPUCuNFI{QDRizszN MXfTRW5ITVJ?
MHH-CALL-2 MnLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwMEK5OVIh|ryP MlXZV2FPT0WU
SU-DHL-1 MlviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjzTWM2OD1yLkC0PFY2KM7:TR?= MoHCV2FPT0WU
A4-Fuk MnfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHGfZE2UUN3ME2wMlA2PTZ3IN88US=> MnjlV2FPT0WU
EW-1 NFfXT21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXlTWM2OD1yLkGwNlU3KM7:TR?= MoPOV2FPT0WU
NOS-1 NXHnOHc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPyTlJKSzVyPUCuNVAzQTRizszN NXrDd3FZW0GQR1XS
EW-16 MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHH[XBKSzVyPUCuNVA2PjhizszN NIP5fnBUSU6JRWK=
TE-11 NYHmcHZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTkTWM2OD1yLkG2NFk3KM7:TR?= NEDvNohUSU6JRWK=
SW982 M3Prfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\hTWM2OD1yLkG2OFc5KM7:TR?= M{LWNXNCVkeHUh?=
LAN-6 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn4TWc5UUN3ME2wMlE4PDR|IN88US=> NHL6NohUSU6JRWK=
MZ1-PC MonMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPHTWM2OD1yLkG3PFM2KM7:TR?= M4jxWXNCVkeHUh?=
KS-1 M1nKZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj3ToJvUUN3ME2wMlE6OzR|IN88US=> M4i1e3NCVkeHUh?=
PSN1 M4LsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX3W2pHUUN3ME2wMlE6PjNzIN88US=> Mk\VV2FPT0WU
LC-2-ad NUXIcGF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfWdJZSUUN3ME2wMlE6Pjl{IN88US=> Mor2V2FPT0WU
COLO-320-HSR MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzCflJKSzVyPUCuNVk4PzZizszN MXjTRW5ITVJ?
OPM-2 MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMkK2Olkh|ryP MWTTRW5ITVJ?
SK-NEP-1 M1jkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr1VHRKSzVyPUCuNlM2OjRizszN M{XzfHNCVkeHUh?=
ALL-PO MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnNVm9KSzVyPUCuNlQ2OjRizszN NUfKPVhoW0GQR1XS
CMK M1e5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHk[4xKSzVyPUCuNlU2OyEQvF2= NULrW3Y{W0GQR1XS
NCI-H1648 M1rkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwMke4OVUh|ryP NYW4WHRxW0GQR1XS
SIG-M5 NIXUO2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfrOVRiUUN3ME2wMlI6OTV7IN88US=> MnfvV2FPT0WU
TGBC24TKB MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1npO2lEPTB;MD6zNFIyQCEQvF2= MoH4V2FPT0WU
DOHH-2 MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwM{GyNFQh|ryP MXjTRW5ITVJ?
NB69 NYfLN2V[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\4RWlEPTB;MD6zNVc5PyEQvF2= MlW5V2FPT0WU
MFH-ino M3TCT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfzTWM2OD1yLkOyOVI{KM7:TR?= NEXjUolUSU6JRWK=
KP-N-RT-BM-1 NXm1XmRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnlT5h7UUN3ME2wMlM{OTJ|IN88US=> MlzSV2FPT0WU
MONO-MAC-6 M3zDN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPEe25KSzVyPUCuN|MzQTFizszN MWLTRW5ITVJ?
ATN-1 NV6w[YVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnOyTWM2OD1yLkOzN|A{KM7:TR?= Mmj6V2FPT0WU
NTERA-S-cl-D1 NIL0T|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTxTWM2OD1yLkOzN|k3KM7:TR?= NH7DeWNUSU6JRWK=
L-540 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUL1T5J3UUN3ME2wMlM3QTh6IN88US=> M1LQb3NCVkeHUh?=
GB-1 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETneHpKSzVyPUCuN|g5PjdizszN M4jaRXNCVkeHUh?=
MV-4-11 MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwM{m0OFYh|ryP M1O1O3NCVkeHUh?=
KG-1 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwM{m1OlEh|ryP Moi3V2FPT0WU
OVCAR-4 NU\6cIFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn0TWM2OD1yLkSwOVY6KM7:TR?= MWXTRW5ITVJ?
NEC8 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjiN5Y2UUN3ME2wMlQyOjl{IN88US=> M1jOWHNCVkeHUh?=
SK-MM-2 NV;hXopET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPxTWM2OD1yLkSxOlA6KM7:TR?= NYjxWJV4W0GQR1XS
TE-8 M1jNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojiTWM2OD1yLkSyPFgh|ryP NEXhfIlUSU6JRWK=
697 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:0TWM2OD1yLkSzNlE2KM7:TR?= MYnTRW5ITVJ?
NB14 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LudmlEPTB;MD60N|gzPiEQvF2= MUjTRW5ITVJ?
GDM-1 NFfwZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnviTWM2OD1yLkS3NVE3KM7:TR?= Ml\IV2FPT0WU
HUTU-80 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjyOXVKSzVyPUCuOFc{PzVizszN MmXwV2FPT0WU
HL-60 NGqweFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwNEixOFIh|ryP MX7TRW5ITVJ?
OCI-AML2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G0XGlEPTB;MD60PFMzQCEQvF2= Ml;mV2FPT0WU
ML-2 NUD4PZVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DWWmlEPTB;MD60PVA{OSEQvF2= MoHZV2FPT0WU
ES4 M4r1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnjTWM2OD1yLkS5NVA6KM7:TR?= M1e1c3NCVkeHUh?=
NCI-H747 NWTzOnk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPkXWpKSzVyPUCuOFk5QSEQvF2= MoTIV2FPT0WU
RL95-2 M{K0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwNUCxNVIh|ryP Mn3mV2FPT0WU
TE-15 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLzSJdKSzVyPUCuOVEyOjRizszN NUXNPIJoW0GQR1XS
TE-12 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rmXGlEPTB;MD61N|M1QSEQvF2= MVHTRW5ITVJ?
LB1047-RCC M4LCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\MTWM2OD1yLkW0OVQ6KM7:TR?= NFHhfZJUSU6JRWK=
LB831-BLC Mnf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LvTmlEPTB;MD61OVAzOyEQvF2= NVG1cIJbW0GQR1XS
NCI-H1355 MlzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHMcIVKSzVyPUCuOVUyQDRizszN MkHtV2FPT0WU
CTV-1 M1fqZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwNUW2NlQh|ryP NG\LZmdUSU6JRWK=
RXF393 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvHTWM2OD1yLkW1O|k1KM7:TR?= NVz6ZpJzW0GQR1XS
SW872 M{\4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TBTGlEPTB;MD61OlczPCEQvF2= NYfVcYtjW0GQR1XS
MPP-89 NHrvZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXXc|VKSzVyPUCuOVc5QDRizszN NHfJbWZUSU6JRWK=
RPMI-8226 M13VVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwNkO1NlYh|ryP M2qxTnNCVkeHUh?=
LS-1034 Ml;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGni[ppKSzVyPUCuOlM2QCEQvF2= NHL4Wo5USU6JRWK=
SJSA-1 NXLTV5l1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TxZWlEPTB;MD62N|czPSEQvF2= MkO3V2FPT0WU
HOP-62 MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1yxUmlEPTB;MD62OVA{OyEQvF2= M2PrWXNCVkeHUh?=
KGN MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrreJBOUUN3ME2wMlY3OTZ6IN88US=> NFLidnNUSU6JRWK=
D-336MG MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTBwNk[xOlkh|ryP MWLTRW5ITVJ?
LS-411N NILX[INIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\YTWM2OD1yLk[3OFYzKM7:TR?= MoLyV2FPT0WU
TE-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;JcmlEPTB;MD62PVA4PCEQvF2= MoPGV2FPT0WU
LB996-RCC NYTyeVZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrBUVJGUUN3ME2wMlY6Ozh7IN88US=> NVnWSoR4W0GQR1XS
TE-10 NH:0TllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu5NmhKSzVyPUCuO|E1QTZizszN M3iycXNCVkeHUh?=
NCI-SNU-16 NYW5Uog1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwN{K2OlQh|ryP MVXTRW5ITVJ?
ES8 NFnBVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zJcmlEPTB;MD63OFk4PSEQvF2= M17uVHNCVkeHUh?=
COLO-800 NE[3S5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwN{[2PVUh|ryP MXjTRW5ITVJ?
ES6 NG\lVGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfMT3VZUUN3ME2wMlc4PTV7IN88US=> NGLDUGVUSU6JRWK=
L-363 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\aTmlEPTB;MD64NlM4PSEQvF2= Ml3CV2FPT0WU
NMC-G1 NF3JbXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\MbWlEPTB;MD64N|I{OyEQvF2= MVPTRW5ITVJ?
LU-134-A MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwOEO5NVIh|ryP MkPtV2FPT0WU
SF268 NH;oclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\KUllKSzVyPUCuPFQxPDJizszN M4XDO3NCVkeHUh?=
KARPAS-45 MmW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwOESyOlMh|ryP NV3uNogzW0GQR1XS
TGW MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLONGhNUUN3ME2wMlg2QDZ|IN88US=> M3nrc3NCVkeHUh?=
CHP-126 NGfxRnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHTenJKSzVyPUCuPFU6PTdizszN MUPTRW5ITVJ?
MOLT-16 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:1TWM2OD1yLki3OVg6KM7:TR?= NETET5JUSU6JRWK=
LB771-HNC NIr6b5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3qNmRKUUN3ME2wMlg6PzV5IN88US=> NGn0enlUSU6JRWK=
NALM-6 NEL0ZpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLWTWM2OD1yLkmwO|M6KM7:TR?= MV\TRW5ITVJ?
GCIY M3fFemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlToTWM2OD1yLkm1OVI3KM7:TR?= MWrTRW5ITVJ?
IST-MES1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljmTWM2OD1yLkm4PFI1KM7:TR?= MXjTRW5ITVJ?
LB2241-RCC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwOUi4OEDPxE1? MUHTRW5ITVJ?
BL-70 Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfFWVhuUUN3ME2wMlk6PTN3IN88US=> MYrTRW5ITVJ?
NB17 NGHLZ|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTFwMEC2N|kh|ryP NV7MOWxCW0GQR1XS
LXF-289 NXTEN3JGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n4XmlEPTB;MT6wN|A4PiEQvF2= MXTTRW5ITVJ?
TK10 M1XWbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;KcIpKSzVyPUGuNFUxPjNizszN MnTOV2FPT0WU
K5 NXvPfllmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HuZ2lEPTB;MT6wOlI4PCEQvF2= MlrmV2FPT0WU
NCI-H716 NFvCZ4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFwMEeyOVkh|ryP MmPOV2FPT0WU
HCE-T NXPUZ3FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{juT2lEPTB;MT6wPFgyQSEQvF2= M37l[3NCVkeHUh?=
GI-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPm[4dKSzVyPUGuNFk4QThizszN MWjTRW5ITVJ?
KARPAS-422 NXzEXm1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTjXGZKSzVyPUGuNVAxOjJizszN MXjTRW5ITVJ?
TE-9 MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjCRZRKSzVyPUGuNVE{OjhizszN NGPHbIVUSU6JRWK=
SF126 NGjs[lFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPhdpBKSzVyPUGuNVE2PjhizszN MX7TRW5ITVJ?
BB30-HNC MnTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXBdm9KSzVyPUGuNVMyOTJizszN MVrTRW5ITVJ?
NCI-H1304 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFwMUOzN|gh|ryP M4m4b3NCVkeHUh?=
HEL NInGR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXNWYJKSzVyPUGuNVQ5QTVizszN NXi2bHpMW0GQR1XS
HAL-01 M3vVWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjpNVllUUN3ME2xMlE2Ojh|IN88US=> NXvMeW9[W0GQR1XS
SK-LMS-1 MlzmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WyVWlEPTB;MT6xOVk4PCEQvF2= MWfTRW5ITVJ?
SW954 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XWe2lEPTB;MT6xPVU3PyEQvF2= NE\xU3dUSU6JRWK=
D-283MED NHr2U5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFwMkKzO|kh|ryP NU\1doRzW0GQR1XS
NCI-H1882 M{C3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTFwMkO4PUDPxE1? Mn:wV2FPT0WU
GI-ME-N M2rkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DKN2lEPTB;MT6yOVIxQCEQvF2= NE\DcnBUSU6JRWK=
SK-PN-DW NYHGSGcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj0T2hKSzVyPUGuNlY{PDhizszN NVrNenNbW0GQR1XS
C2BBe1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ToXWlEPTB;MT6yPVEyPyEQvF2= NFK5[4VUSU6JRWK=
A704 M{HuOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S0XGlEPTB;MT6zNlY5QSEQvF2= NHLTepRUSU6JRWK=
KALS-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTFwM{SwPEDPxE1? NFi1b45USU6JRWK=
ETK-1 NUDocHlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nDe2lEPTB;MT6zOFQ5QSEQvF2= MmXNV2FPT0WU
LB647-SCLC MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13XbGlEPTB;MT6zOFk5PiEQvF2= Mnm3V2FPT0WU
OCUB-M NVjjWlRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzoUHBKSzVyPUGuN|YyPDNizszN MV7TRW5ITVJ?
NCI-H720 MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFwM{[zO|gh|ryP NGKyTG9USU6JRWK=
NB13 NUDZRXV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[0OmlEPTB;MT6zO|I6OyEQvF2= M3O4cnNCVkeHUh?=
GR-ST MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2qxSmlEPTB;MT6zPFc2PyEQvF2= NFP3R4RUSU6JRWK=
DU-4475 NWXHOFVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\ue2lEPTB;MT60OVg2OyEQvF2= MV3TRW5ITVJ?
HCC2157 NWTiOJVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7oVFBKSzVyPUGuOFY3PTlizszN MYjTRW5ITVJ?
RKO NUT1VINrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwNEm5NlIh|ryP M1vaXnNCVkeHUh?=
LS-123 M4nsTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwNUG1PVQh|ryP MoDRV2FPT0WU
NCI-H69 NFTQd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnsbmFyUUN3ME2xMlU2QDFzIN88US=> M1HLbnNCVkeHUh?=
SW962 NW\iV2w3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELacW1KSzVyPUGuOVYyOyEQvF2= M1fjVXNCVkeHUh?=
PF-382 NH21NXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LOOWlEPTB;MT61Olk3KM7:TR?= NWfxXGJ6W0GQR1XS
A101D MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTIcGRZUUN3ME2xMlU4OTF|IN88US=> NInCR|BUSU6JRWK=
NB10 NXv2NG1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHkZpBKSzVyPUGuOVc{QTJizszN NY\tcWdnW0GQR1XS
NB5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPRb4hKSzVyPUGuOVg1PzZizszN MV7TRW5ITVJ?
HCE-4 M3nXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHrTWM2OD1zLk[wPFUh|ryP M4nrenNCVkeHUh?=
HT-144 MmrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwNkOxPUDPxE1? M{fwVHNCVkeHUh?=
NCI-H524 M1Lx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[zTWM2OD1zLk[0N|A4KM7:TR?= NUfwOJZHW0GQR1XS
NKM-1 M3PFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HINGlEPTB;MT62PFY3KM7:TR?= M1HNNHNCVkeHUh?=
KURAMOCHI M4TnbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFwNkm1O|Mh|ryP NVzwSoZ7W0GQR1XS
NCI-H187 NHPzR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXLTWM2OD1zLkewNFM3KM7:TR?= MYXTRW5ITVJ?
U-266 NIjleIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYroU5ZJUUN3ME2xMlc{QDR{IN88US=> NIL2XZRUSU6JRWK=
BL-41 MmrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HQVWlEPTB;MT63OlI4OiEQvF2= MWTTRW5ITVJ?
SK-N-DZ M2LFWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES2[XdKSzVyPUGuO|g{ODlizszN MUDTRW5ITVJ?
Daudi MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnSflNKSzVyPUGuO|g6PjdizszN NG\mPXdUSU6JRWK=
CPC-N NX7FOVl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TEO2lEPTB;MT64OVA6PiEQvF2= NGXPe|BUSU6JRWK=
EM-2 NE\ScYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPYZZlKSzVyPUGuPFUyKM7:TR?= MkS3V2FPT0WU
HCC1187 NFK5WI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLhTWM2OD1zLki2NlQyKM7:TR?= NFLXW2pUSU6JRWK=
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CAS-1 M13qdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHGR3ZZUUN3ME2xMlk5Ojl7IN88US=> MnHTV2FPT0WU
NB7 M1HaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn6OVc5UUN3ME2yMlAxPTV3IN88US=> MWjTRW5ITVJ?
VA-ES-BJ NIXxfXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrINHljUUN3ME2yMlAyPTF|IN88US=> NVz3ZXI1W0GQR1XS
SNU-C2B NH[2OZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD1{LkCzN|UyKM7:TR?= NFzpfopUSU6JRWK=
LOXIMVI MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnwTWM2OD1{LkC2O|g3KM7:TR?= MonKV2FPT0WU
NCI-H1581 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v3OGlEPTB;Mj6xNVU2QSEQvF2= NGrQc4pUSU6JRWK=
IST-SL2 NUnJN2lmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rjZ2lEPTB;Mj6xNlQ1PSEQvF2= M4jrT3NCVkeHUh?=
NOMO-1 M3m5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ns[2lEPTB;Mj6xO|Y5OyEQvF2= NU\m[oQ3W0GQR1XS
TE-6 NXjvblZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDpV4drUUN3ME2yMlE6ODVizszN NHmxOmNUSU6JRWK=
NCI-H526 M1jBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJwMUmxOFEh|ryP NYTiRVdTW0GQR1XS
MSTO-211H NWTw[VdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnkcW5KSzVyPUKuNlAxPDFizszN NYLDUWk4W0GQR1XS
LS-513 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P6fmlEPTB;Mj6yNlI3QSEQvF2= NYnYbY9mW0GQR1XS
NCI-SNU-1 M4O4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnjTWM2OD1{LkOzNlU3KM7:TR?= M{LYWXNCVkeHUh?=
BB65-RCC MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTJwM{e0PVMh|ryP M{HSNHNCVkeHUh?=
GT3TKB NInnOFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIH2VG9KSzVyPUKuN|k6PzJizszN NF7CNW5USU6JRWK=
OS-RC-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4OzUmlEPTB;Mj60NlM1OSEQvF2= M4HmdHNCVkeHUh?=
NCI-H2126 MoLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXQTWM2OD1{LkSzOlc1KM7:TR?= NHTvTlhUSU6JRWK=
SK-UT-1 MoL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrCfWlKSzVyPUKuOFc1PjdizszN MnPGV2FPT0WU
DMS-114 NXnIbnFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzhTHpKSzVyPUKuOlE2OjRizszN MV3TRW5ITVJ?
ONS-76 NFH0R2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJwNkO2OFEh|ryP M3r1PXNCVkeHUh?=
8-MG-BA M{Ts[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwNkW0NVQh|ryP MmTnV2FPT0WU
BOKU NIXwUYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLmeJlKSzVyPUKuO|I4PjRizszN M3fOXXNCVkeHUh?=
LAMA-84 NVH0VWVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJwN{m5NVIh|ryP NXWwZod7W0GQR1XS
ES1 Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG2SWdPUUN3ME2yMlgyQDB2IN88US=> NV7ET2c2W0GQR1XS
NCI-H1395 M4HsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDv[3hKSzVyPUKuPFIxOTJizszN Ml\FV2FPT0WU
A388 MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XabWlEPTB;Mj65OlE4KM7:TR?= NUPvWZlTW0GQR1XS
NCCIT M1TrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\1Wo9tUUN3ME2zMlA5QDZ{IN88US=> M{DxUXNCVkeHUh?=
HD-MY-Z MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3TfFdKSzVyPUOuNVMzODNizszN M3f6V3NCVkeHUh?=
NCI-H510A MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUm4RWkxUUN3ME2zMlE5QTR|IN88US=> Mn;SV2FPT0WU
NCI-N87 NULjdI9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfsTWM2OD1|LkKwNFIh|ryP MYXTRW5ITVJ?
SCLC-21H MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\iUmduUUN3ME2zMlI3QDV7IN88US=> MnfDV2FPT0WU
SH-4 M2HKW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT4TWM2OD1|LkK4O|k4KM7:TR?= NYm3UIxvW0GQR1XS
QIMR-WIL NWrH[XZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXUSXZtUUN3ME2zMlMzQDR7IN88US=> NXv1enlpW0GQR1XS
KM12 NUDpbHBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj0TWM2OD1|LkOzOVQ1KM7:TR?= MkHuV2FPT0WU
ST486 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFSyNphKSzVyPUOuOVM5QDNizszN M2nyeHNCVkeHUh?=
HC-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNwNkKwNlgh|ryP M4PJZnNCVkeHUh?=
BV-173 MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTNwNkSwPFgh|ryP MkntV2FPT0WU
EW-24 NHvS[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTXe4M1UUN3ME2zMlY3PDN2IN88US=> Ml30V2FPT0WU
LU-65 Mk\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTWTWM2OD1|Lk[4O|Eh|ryP NGnrVWxUSU6JRWK=
ECC4 M3;ObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vMTGlEPTB;Mz63O|U3KM7:TR?= NUS0PJJyW0GQR1XS
ARH-77 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLqZZRKSzVyPUSuNVExPjdizszN MV;TRW5ITVJ?
BC-3 M1Sz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;RTWM2OD12LkGzNFY5KM7:TR?= NGXSZ5FUSU6JRWK=
SNB75 NFTMd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTRwMk[xPUDPxE1? MXTTRW5ITVJ?
MEG-01 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXhTWM2OD12LkK3OFE6KM7:TR?= NWSwXVJuW0GQR1XS
NCI-H1417 M2TOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXBTWM2OD12LkK4OFQ{KM7:TR?= M1G2O3NCVkeHUh?=
MDA-MB-134-VI MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KwRmlEPTB;ND6zNFYxOSEQvF2= M{SzRnNCVkeHUh?=
Becker NX[5VFFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXFUHdJUUN3ME20MlQ4OzN4IN88US=> NYfjd3k5W0GQR1XS
DMS-153 NGLvW|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{SxTmlEPTB;ND62OlQ4PSEQvF2= MYHTRW5ITVJ?
TGBC1TKB MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTRwNki1NVUh|ryP NF7ldGNUSU6JRWK=
EW-3 NF\nVnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zOcGlEPTB;ND63OlI1QCEQvF2= MoXUV2FPT0WU
KE-37 NXnwZnNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHnTWM2OD12Lki2NVk3KM7:TR?= NILlPWtUSU6JRWK=
NCI-H23 NYjOW2FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3xTWM2OD12Lki3NlI4KM7:TR?= MX7TRW5ITVJ?
MC116 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2eweWlEPTB;ND65OFEzPiEQvF2= M2ToN3NCVkeHUh?=
NH-12 MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj1TWM2OD12Lkm2OFM6KM7:TR?= NUXNPY5OW0GQR1XS
CTB-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDaUJFXUUN3ME20Mlk4PzJzIN88US=> NH;yWHZUSU6JRWK=
KM-H2 NIP1W5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHacJdKSzVyPUWuNFU{OjNizszN NHS0e|RUSU6JRWK=
MOLT-4 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnJSpF5UUN3ME21MlEyQDNizszN NVz3NVRbW0GQR1XS
NCI-H2141 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\ZbGlEPTB;NT6xOFI3QCEQvF2= M1L5fXNCVkeHUh?=
EB-3 M4HHemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3VTWM2OD13LkG3OVA1KM7:TR?= MYPTRW5ITVJ?
NCI-H1522 NX;MTZZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLFcFBXUUN3ME21MlI3OzJ{IN88US=> MXXTRW5ITVJ?
MRK-nu-1 NHfOR4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S0OGlEPTB;NT60N|Y{OyEQvF2= NX3Nc2N6W0GQR1XS
no-11 M1TFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HtRWlEPTB;NT60O|A5PyEQvF2= MX7TRW5ITVJ?
CESS MnLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;OXnVKSzVyPUWuOVgxOzRizszN MlnjV2FPT0WU
KMOE-2 M2q2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTVwNUi2OVkh|ryP NUn0dJJWW0GQR1XS
REH MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInjcWdKSzVyPU[uNlU3OThizszN NX3qWZg4W0GQR1XS
KU812 NHHabm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G5UWlEPTB;Nj60Nlc6OSEQvF2= NFnhS2hUSU6JRWK=
SK-N-FI NYrEeGJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTZwNkC2O|Qh|ryP NEfub|RUSU6JRWK=
MMAC-SF NGXXc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEf4endKSzVyPUeuNFY1QTJizszN M33KRXNCVkeHUh?=
RCC10RGB NX33O3B4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTdwMkK5O|ch|ryP MWnTRW5ITVJ?
NCI-H322M NH;WSWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S2OmlEPTB;Nz6zN|M{PSEQvF2= NIHGNGhUSU6JRWK=
NB6 NV[4T5F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7JZ5JKSzVyPUeuOVQ5QTlizszN M3jLVnNCVkeHUh?=
MN-60 NUP0SXB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX5epBKSzVyPUeuOlkzOTVizszN MY\TRW5ITVJ?
NCI-H1092 NVXleXNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInCdVVKSzVyPUiuNFE4OzRizszN NEjTOmFUSU6JRWK=
EKVX MlvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRThwNEewOlYh|ryP NE[2OmNUSU6JRWK=
D-263MG M4TXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;DTWM2OD16LkW1N|k3KM7:TR?= NWj0N3cxW0GQR1XS
NCI-H209 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHRTWM2OD16Lk[0NFA3KM7:TR?= M{nL[XNCVkeHUh?=
IST-SL1 Mn7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRThwOEm4PVIh|ryP NFq0ZoFUSU6JRWK=
ACN NWWx[HhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LFZ2lEPTB;OT6xPVE2PyEQvF2= M1[4dHNCVkeHUh?=
MHH-PREB-1 MkXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnRTGZKSzVyPUmuNlEzOTlizszN M{ew[XNCVkeHUh?=
EW-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTlwNkWzPVYh|ryP MYrTRW5ITVJ?
KASUMI-1 NInlNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTlwN{i3O{DPxE1? MWfTRW5ITVJ?
KINGS-1 M1vVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFyLkKzOFch|ryP NX;sb3h4W0GQR1XS
EVSA-T M1OxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFyLkOxPVIh|ryP NGDNbldUSU6JRWK=
DSH1 NXLONJNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTiUnJiUUN3ME2xNE4{QTd{IN88US=> M2XjTnNCVkeHUh?=
COLO-824 NUHoNIRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHtTWM2OD1zMD64OlY6KM7:TR?= MWjTRW5ITVJ?
K052 NIr0[VNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUD3U3V2UUN3ME2xNE46OzJ{IN88US=> M4Ta[HNCVkeHUh?=
SK-MEL-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFyLkm5N|kh|ryP M374UHNCVkeHUh?=

... 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

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