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

  • 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 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\wU2lEPTB;MD6wNFAxPjB|IN88US=> NV\BbIxpW0GQR1XS
SF539 NXLLUmhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnexTWM2OD1yLkCwNFU3PCEQvF2= M2DFNnNCVkeHUh?=
DEL MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\zTWM2OD1yLkCwNFkzPyEQvF2= MlzLV2FPT0WU
NB1 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljNTWM2OD1yLkCwNVYzKM7:TR?= NFO5R3FUSU6JRWK=
SR NYX5XogzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDEcnJKSzVyPUCuNFAzPzdizszN MYPTRW5ITVJ?
KARPAS-299 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz4TWM2OD1yLkCyN|g1KM7:TR?= NEjmSXhUSU6JRWK=
MHH-CALL-2 M{XUe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXUTWM2OD1yLkCyPVUzKM7:TR?= NIr0dHJUSU6JRWK=
SU-DHL-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TpRWlEPTB;MD6wOFg3PSEQvF2= NXvBU3JHW0GQR1XS
A4-Fuk NVPHXpJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TSXGlEPTB;MD6wOVU3PSEQvF2= M13mdXNCVkeHUh?=
EW-1 MnS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLOWWNnUUN3ME2wMlExOjV4IN88US=> NX;TRlJMW0GQR1XS
NOS-1 NXvRNGlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYCxZnZCUUN3ME2wMlExOjl2IN88US=> Mk\HV2FPT0WU
EW-16 M2rXcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XF[mlEPTB;MD6xNFU3QCEQvF2= MVXTRW5ITVJ?
TE-11 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\ITXpKSzVyPUCuNVYxQTZizszN NUHYZo1GW0GQR1XS
SW982 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMU[0O|gh|ryP M17we3NCVkeHUh?=
LAN-6 MluyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nremlEPTB;MD6xO|Q1OyEQvF2= M4GzenNCVkeHUh?=
MZ1-PC M3S2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMUe4N|Uh|ryP MnjyV2FPT0WU
KS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwMUmzOFMh|ryP NYmyeGJKW0GQR1XS
PSN1 MlPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHXTWM2OD1yLkG5OlMyKM7:TR?= MorOV2FPT0WU
LC-2-ad MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnJfnRTUUN3ME2wMlE6Pjl{IN88US=> NEnBWYtUSU6JRWK=
COLO-320-HSR NUS1XY5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTBwMUm3O|Yh|ryP MW\TRW5ITVJ?
OPM-2 M3joPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PDdGlEPTB;MD6yNlY3QSEQvF2= NUnkTlYyW0GQR1XS
SK-NEP-1 M2PwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4q3c2lEPTB;MD6yN|UzPCEQvF2= MXTTRW5ITVJ?
ALL-PO MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPsTWM2OD1yLkK0OVI1KM7:TR?= M3LoXXNCVkeHUh?=
CMK MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrBU4k1UUN3ME2wMlI2PTNizszN MU\TRW5ITVJ?
NCI-H1648 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHVTWM2OD1yLkK3PFU2KM7:TR?= MVjTRW5ITVJ?
SIG-M5 NW\0VJhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnJOo41UUN3ME2wMlI6OTV7IN88US=> NUW1OmtoW0GQR1XS
TGBC24TKB NGrQbGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TzVGlEPTB;MD6zNFIyQCEQvF2= MXHTRW5ITVJ?
DOHH-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moi0TWM2OD1yLkOxNlA1KM7:TR?= MXrTRW5ITVJ?
NB69 Mkj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LvTWlEPTB;MD6zNVc5PyEQvF2= Mkf6V2FPT0WU
MFH-ino MmfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\qR2RKSzVyPUCuN|I2OjNizszN M4m2fHNCVkeHUh?=
KP-N-RT-BM-1 M4\Z[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwM{OxNlMh|ryP NHzHPZVUSU6JRWK=
MONO-MAC-6 NYXJbXdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;MTWM2OD1yLkOzNlkyKM7:TR?= NVLxXHo6W0GQR1XS
ATN-1 M4\RfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLpUY1kUUN3ME2wMlM{OzB|IN88US=> M{O3TnNCVkeHUh?=
NTERA-S-cl-D1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fsRWlEPTB;MD6zN|M6PiEQvF2= MVHTRW5ITVJ?
L-540 NED2fW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwM{[5PFgh|ryP NHnMe|FUSU6JRWK=
GB-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;xTWM2OD1yLkO4PFY4KM7:TR?= MUHTRW5ITVJ?
MV-4-11 NHTieo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f6V2lEPTB;MD6zPVQ1PiEQvF2= MYLTRW5ITVJ?
KG-1 MlTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C2WmlEPTB;MD6zPVU3OSEQvF2= MUjTRW5ITVJ?
OVCAR-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPIOI9KSzVyPUCuOFA2PjlizszN NFfVS45USU6JRWK=
NEC8 M3LybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDVTWM2OD1yLkSxNlkzKM7:TR?= M1Xm[HNCVkeHUh?=
SK-MM-2 NYrme4g1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf3UnBoUUN3ME2wMlQyPjB7IN88US=> NIXa[mtUSU6JRWK=
TE-8 MonrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nFc2lEPTB;MD60Nlg5KM7:TR?= MmTmV2FPT0WU
697 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu0c2hKSzVyPUCuOFMzOTVizszN Mmn3V2FPT0WU
NB14 M2TVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr5TWM2OD1yLkSzPFI3KM7:TR?= M4\RcXNCVkeHUh?=
GDM-1 NYTSdm11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLZTWM2OD1yLkS3NVE3KM7:TR?= MXHTRW5ITVJ?
HUTU-80 MkHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3TXJlKSzVyPUCuOFc{PzVizszN M4PIfnNCVkeHUh?=
HL-60 NInvT5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;G[pBrUUN3ME2wMlQ5OTR{IN88US=> M2\ZOHNCVkeHUh?=
OCI-AML2 NF:0bGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n1TWlEPTB;MD60PFMzQCEQvF2= M3nJVXNCVkeHUh?=
ML-2 M2m3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD0TWM2OD1yLkS5NFMyKM7:TR?= NGPPSWRUSU6JRWK=
ES4 NYP2e4lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfDW|ZKSzVyPUCuOFkyODlizszN MoTWV2FPT0WU
NCI-H747 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLIfGxKSzVyPUCuOFk5QSEQvF2= NX31SmlSW0GQR1XS
RL95-2 M3u5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33OPGlEPTB;MD61NFEyOiEQvF2= MWjTRW5ITVJ?
TE-15 M1vTbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwNUGxNlQh|ryP NUXpW|NFW0GQR1XS
TE-12 NV7jTYZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwNUOzOFkh|ryP Mn[0V2FPT0WU
LB1047-RCC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwNUS1OFkh|ryP NWPkfnQ{W0GQR1XS
LB831-BLC NWrjWJlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fDT2lEPTB;MD61OVAzOyEQvF2= MkX2V2FPT0WU
NCI-H1355 NIrrV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwNUWxPFQh|ryP NWG1XXF7W0GQR1XS
CTV-1 NUXtO3BxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvxTWM2OD1yLkW1OlI1KM7:TR?= NGmwUpRUSU6JRWK=
RXF393 NWXtfJFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwNUW3PVQh|ryP Mn75V2FPT0WU
SW872 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDoVmM1UUN3ME2wMlU3PzJ2IN88US=> MUfTRW5ITVJ?
MPP-89 M3XsN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\TUmlEPTB;MD61O|g5PCEQvF2= M2jSV3NCVkeHUh?=
RPMI-8226 NIWydWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nEOGlEPTB;MD62N|UzPiEQvF2= NFK4UVJUSU6JRWK=
LS-1034 MknQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DIfGlEPTB;MD62N|U5KM7:TR?= Mkj6V2FPT0WU
SJSA-1 NILleJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HsV2lEPTB;MD62N|czPSEQvF2= NFPkR4ZUSU6JRWK=
HOP-62 MnnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTZbYNrUUN3ME2wMlY2ODN|IN88US=> M{PNdnNCVkeHUh?=
KGN NXv3Upl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD5bWo5UUN3ME2wMlY3OTZ6IN88US=> MkHoV2FPT0WU
D-336MG M2j6Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3sTWM2OD1yLk[2NVY6KM7:TR?= MlXFV2FPT0WU
LS-411N MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHraSnJKSzVyPUCuOlc1PjJizszN NV\OOGJoW0GQR1XS
TE-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\U[FVKSzVyPUCuOlkxPzRizszN MXXTRW5ITVJ?
LB996-RCC M3m4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\VTWM2OD1yLk[5N|g6KM7:TR?= MmHqV2FPT0WU
TE-10 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXCRYZ6UUN3ME2wMlcyPDl4IN88US=> MoPpV2FPT0WU
NCI-SNU-16 NITlRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPwUGJKSzVyPUCuO|I3PjRizszN M4njcnNCVkeHUh?=
ES8 MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDxWpg3UUN3ME2wMlc1QTd3IN88US=> MYnTRW5ITVJ?
COLO-800 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PxPGlEPTB;MD63OlY6PSEQvF2= MXfTRW5ITVJ?
ES6 NF\3S5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\HZmVvUUN3ME2wMlc4PTV7IN88US=> M2qxcXNCVkeHUh?=
L-363 NVnjbJN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HvUWlEPTB;MD64NlM4PSEQvF2= NYj0[YVrW0GQR1XS
NMC-G1 NYjBS2E4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwOEOyN|Mh|ryP Mn7sV2FPT0WU
LU-134-A MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:zTWM2OD1yLkizPVEzKM7:TR?= NWfqSldUW0GQR1XS
SF268 MkW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwOESwOFIh|ryP NYrLUnJ6W0GQR1XS
KARPAS-45 MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwOESyOlMh|ryP NGPEN29USU6JRWK=
TGW M4W5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MliwTWM2OD1yLki1PFY{KM7:TR?= Ml\YV2FPT0WU
CHP-126 M3rjOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjjTWM2OD1yLki1PVU4KM7:TR?= MofBV2FPT0WU
MOLT-16 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTBwOEe1PFkh|ryP MW\TRW5ITVJ?
LB771-HNC M1ntNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr6TWM2OD1yLki5O|U4KM7:TR?= NIrnSpNUSU6JRWK=
NALM-6 NVHLNHJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLyW4lKSzVyPUCuPVA4OzlizszN NHzyT|dUSU6JRWK=
GCIY MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXiwUYdUUUN3ME2wMlk2PTJ4IN88US=> NFfuVJBUSU6JRWK=
IST-MES1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;SflgzUUN3ME2wMlk5QDJ2IN88US=> M4rwV3NCVkeHUh?=
LB2241-RCC MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVT2Uo53UUN3ME2wMlk5QDRizszN NUHNdmVOW0GQR1XS
BL-70 NFu5[2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z1NWlEPTB;MD65PVU{PSEQvF2= M3PEVXNCVkeHUh?=
NB17 MmH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyzS3kyUUN3ME2xMlAxPjN7IN88US=> NHTafJVUSU6JRWK=
LXF-289 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDHV5cxUUN3ME2xMlA{ODd4IN88US=> MojQV2FPT0WU
TK10 NHnJbFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml72TWM2OD1zLkC1NFY{KM7:TR?= M3HpPHNCVkeHUh?=
K5 NIjFUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFwME[yO|Qh|ryP NIHBbJFUSU6JRWK=
NCI-H716 NWjMbGxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFKyV45KSzVyPUGuNFczPTlizszN MmK1V2FPT0WU
HCE-T NELFfVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwMEi4NVkh|ryP NFGySYJUSU6JRWK=
GI-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\hNZoxUUN3ME2xMlA6Pzl6IN88US=> M4LhXnNCVkeHUh?=
KARPAS-422 Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3sUHVrUUN3ME2xMlExODJ{IN88US=> NEDDRoNUSU6JRWK=
TE-9 M2jw[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDtTWM2OD1zLkGxN|I5KM7:TR?= MYLTRW5ITVJ?
SF126 M3j5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfabZVSUUN3ME2xMlEyPTZ6IN88US=> M4HDfHNCVkeHUh?=
BB30-HNC NYPncm8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrlNJpxUUN3ME2xMlE{OTF{IN88US=> MWPTRW5ITVJ?
NCI-H1304 NFyyeFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\sdHBMUUN3ME2xMlE{OzN6IN88US=> NIHG[VhUSU6JRWK=
HEL MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrYTWM2OD1zLkG0PFk2KM7:TR?= M{HKSnNCVkeHUh?=
HAL-01 NVP5Tm9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\2VWVKSzVyPUGuNVUzQDNizszN NFTTb3JUSU6JRWK=
SK-LMS-1 NFfXSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XaS2lEPTB;MT6xOVk4PCEQvF2= NUHDWpY{W0GQR1XS
SW954 NXjCS4lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUK3d292UUN3ME2xMlE6PTZ5IN88US=> M4HObHNCVkeHUh?=
D-283MED MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEe1SphKSzVyPUGuNlI{PzlizszN M2q5WHNCVkeHUh?=
NCI-H1882 NHPBW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjFeY5SUUN3ME2xMlI{QDlizszN NH\4fHBUSU6JRWK=
GI-ME-N NGrnenpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrvNGtKSzVyPUGuNlUzODhizszN NW\GdVVrW0GQR1XS
SK-PN-DW MkHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r1R2lEPTB;MT6yOlM1QCEQvF2= M{TwNHNCVkeHUh?=
C2BBe1 MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO2TWM2OD1zLkK5NVE4KM7:TR?= NGTUW4xUSU6JRWK=
A704 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTFwM{K2PFkh|ryP MV;TRW5ITVJ?
KALS-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e1[mlEPTB;MT6zOFA5KM7:TR?= NEP2d41USU6JRWK=
ETK-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nnOmlEPTB;MT6zOFQ5QSEQvF2= MUPTRW5ITVJ?
LB647-SCLC MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwM{S5PFYh|ryP M2PXS3NCVkeHUh?=
OCUB-M MnfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjSOGtKSzVyPUGuN|YyPDNizszN MnvEV2FPT0WU
NCI-H720 M1r1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r4eGlEPTB;MT6zOlM4QCEQvF2= M1nKXHNCVkeHUh?=
NB13 NH3jNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwM{eyPVMh|ryP MoLaV2FPT0WU
GR-ST NI\kS3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwM{i3OVch|ryP NYDxOVBsW0GQR1XS
DU-4475 NFjQVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHWTWM2OD1zLkS1PFU{KM7:TR?= M3jD[XNCVkeHUh?=
HCC2157 NFXJeFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwNE[2OVkh|ryP Mn35V2FPT0WU
RKO M4rNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFwNEm5NlIh|ryP NGr6ZXhUSU6JRWK=
LS-123 NFSxUpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzHemNSUUN3ME2xMlUyPTl2IN88US=> MVrTRW5ITVJ?
NCI-H69 M1XPfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwNUW4NVEh|ryP NGfwSlhUSU6JRWK=
SW962 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zvemlEPTB;MT61OlE{KM7:TR?= M{ewcXNCVkeHUh?=
PF-382 NYTxWXZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTPTWM2OD1zLkW2PVYh|ryP MnfBV2FPT0WU
A101D MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwNUexNVMh|ryP Mk\LV2FPT0WU
NB10 NXjBelFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwNUezPVIh|ryP NH74SFdUSU6JRWK=
NB5 Mn7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFwNUi0O|Yh|ryP MV;TRW5ITVJ?
HCE-4 NYXrb|A{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG0eYdZUUN3ME2xMlYxQDVizszN NVnocHhNW0GQR1XS
HT-144 NVLQdY1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\uepVDUUN3ME2xMlY{OTlizszN NWPHXpBMW0GQR1XS
NCI-H524 MoPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFwNkSzNFch|ryP Mn\ZV2FPT0WU
NKM-1 M4HBSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{WzdWlEPTB;MT62PFY3KM7:TR?= NFzObHBUSU6JRWK=
KURAMOCHI NEP2fY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK0W3RNUUN3ME2xMlY6PTd|IN88US=> M2\SSXNCVkeHUh?=
NCI-H187 MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D1WWlEPTB;MT63NFA{PiEQvF2= MXXTRW5ITVJ?
U-266 M2fQW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\3TWM2OD1zLkezPFQzKM7:TR?= MkDXV2FPT0WU
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SK-N-DZ Mn;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LpNWlEPTB;MT63PFMxQSEQvF2= NFTROJlUSU6JRWK=
Daudi NXrFWJcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFwN{i5Olch|ryP MVTTRW5ITVJ?
CPC-N MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D3XmlEPTB;MT64OVA6PiEQvF2= NHXod3BUSU6JRWK=
EM-2 Mnq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4GzV2lEPTB;MT64OVEh|ryP MVfTRW5ITVJ?
HCC1187 Ml;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ny[WlEPTB;MT64OlI1OSEQvF2= NXvX[3RMW0GQR1XS
LP-1 NGf1ZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXsTWM2OD1zLki3NVQ{KM7:TR?= MV7TRW5ITVJ?
CAS-1 M4DYRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTHT3hKSzVyPUGuPVgzQTlizszN MULTRW5ITVJ?
NB7 M1L2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonoTWM2OD1{LkCwOVU2KM7:TR?= NWq5foMzW0GQR1XS
VA-ES-BJ NEPn[nNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm0VnRKSzVyPUKuNFE2OTNizszN M{T5PHNCVkeHUh?=
SNU-C2B MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3TcmZKSzVyPUKuNFM{PTFizszN NXqzSW1pW0GQR1XS
LOXIMVI NEXvZpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJwME[3PFYh|ryP M1rV[HNCVkeHUh?=
NCI-H1581 NEHXUnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf5NoVKSzVyPUKuNVE2PTlizszN NVzMO|VMW0GQR1XS
IST-SL2 NFHZV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PUZmlEPTB;Mj6xNlQ1PSEQvF2= Ml70V2FPT0WU
NOMO-1 NEHrfWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTJwMUe2PFMh|ryP MonrV2FPT0WU
TE-6 NV3YdpY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHTd5hKSzVyPUKuNVkxPSEQvF2= NEe3XYlUSU6JRWK=
NCI-H526 NF\LVpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULrR4RyUUN3ME2yMlE6OTRzIN88US=> M2iyfHNCVkeHUh?=
MSTO-211H NXLzR3JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwMkCwOFEh|ryP M{T3TXNCVkeHUh?=
LS-513 NEDSUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XnVGlEPTB;Mj6yNlI3QSEQvF2= MUPTRW5ITVJ?
NCI-SNU-1 MnrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TkeGlEPTB;Mj6zN|I2PiEQvF2= NIrDb5ZUSU6JRWK=
BB65-RCC NFe3TYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfXTWM2OD1{LkO3OFk{KM7:TR?= NGLWXZlUSU6JRWK=
GT3TKB MlXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\HWVhKSzVyPUKuN|k6PzJizszN M33WeXNCVkeHUh?=
OS-RC-2 NXfyXI5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJwNEKzOFEh|ryP MlnmV2FPT0WU
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SK-UT-1 NFrhTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHhe5h4UUN3ME2yMlQ4PDZ5IN88US=> MWrTRW5ITVJ?
DMS-114 M{XOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJwNkG1NlQh|ryP MUnTRW5ITVJ?
ONS-76 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HSXGlEPTB;Mj62N|Y1OSEQvF2= M1\1[3NCVkeHUh?=
8-MG-BA M1Xte2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX5TWM2OD1{Lk[1OFE1KM7:TR?= NGnQPZNUSU6JRWK=
BOKU M1nOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGSzbWlKSzVyPUKuO|I4PjRizszN MWLTRW5ITVJ?
LAMA-84 MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTJwN{m5NVIh|ryP MYjTRW5ITVJ?
ES1 NVjWVmxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJwOEG4NFQh|ryP NIrG[|ZUSU6JRWK=
NCI-H1395 NUHuNHVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnIWWlZUUN3ME2yMlgzODF{IN88US=> NVHORpRiW0GQR1XS
A388 NV33XVVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfPXFZlUUN3ME2yMlk3OTdizszN MW\TRW5ITVJ?
NCCIT MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjGTWM2OD1|LkC4PFYzKM7:TR?= NYDYR5pYW0GQR1XS
HD-MY-Z M2HHWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTNwMUOyNFMh|ryP M4D0VnNCVkeHUh?=
NCI-H510A NVnwVmdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;SUGlEPTB;Mz6xPFk1OyEQvF2= M1zifnNCVkeHUh?=
NCI-N87 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfEeXliUUN3ME2zMlIxODJizszN NVLkRZVPW0GQR1XS
SCLC-21H NWT3UJNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrqTWM2OD1|LkK2PFU6KM7:TR?= MnX4V2FPT0WU
SH-4 M1vFSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjKTWM2OD1|LkK4O|k4KM7:TR?= NIXOeotUSU6JRWK=
QIMR-WIL M3H5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\Jc2lEPTB;Mz6zNlg1QSEQvF2= NET1VYVUSU6JRWK=
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ST486 MlO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnSwTWM2OD1|LkWzPFg{KM7:TR?= M{nke3NCVkeHUh?=
HC-1 M1nwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTOTXpKSzVyPUOuOlIxOjhizszN NFO4N45USU6JRWK=
BV-173 M{f2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfFN5lKSzVyPUOuOlQxQDhizszN MlyxV2FPT0WU
EW-24 NIXxO3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTNwNk[0N|Qh|ryP NFLaeWxUSU6JRWK=
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ECC4 M2nHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7KOGtKSzVyPUOuO|c2PiEQvF2= NGroNnBUSU6JRWK=
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BC-3 NWT6ZXZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LEXmlEPTB;ND6xN|A3QCEQvF2= M{XTOnNCVkeHUh?=
SNB75 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVyzcFdvUUN3ME20MlI3OTlizszN NUTm[W17W0GQR1XS
MEG-01 M2THd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXFNlFKSzVyPUSuNlc1OTlizszN MlnsV2FPT0WU
NCI-H1417 MnfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnLZ45KSzVyPUSuNlg1PDNizszN MUPTRW5ITVJ?
MDA-MB-134-VI M{\ib2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rZdGlEPTB;ND6zNFYxOSEQvF2= MYLTRW5ITVJ?
Becker NGXwdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iwfGlEPTB;ND60O|M{PiEQvF2= NUHQTFlFW0GQR1XS
DMS-153 MmfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFSx[FZKSzVyPUSuOlY1PzVizszN MXrTRW5ITVJ?
TGBC1TKB MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnWdFVKSzVyPUSuOlg2OTVizszN MnraV2FPT0WU
EW-3 MkTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2npcGlEPTB;ND63OlI1QCEQvF2= Mn20V2FPT0WU
KE-37 MnH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXaTWM2OD12Lki2NVk3KM7:TR?= MWnTRW5ITVJ?
NCI-H23 NWf5foE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTRwOEeyNlch|ryP NGSwdpdUSU6JRWK=
MC116 NET6PGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTmb49jUUN3ME20Mlk1OTJ4IN88US=> NXvnNFVkW0GQR1XS
NH-12 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXPR|BKSzVyPUSuPVY1OzlizszN MkPFV2FPT0WU
CTB-1 M33QUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;FV2lEPTB;ND65O|czOSEQvF2= MnjlV2FPT0WU
KM-H2 M{Xsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojLTWM2OD13LkC1N|I{KM7:TR?= MWjTRW5ITVJ?
MOLT-4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTOTWM2OD13LkGxPFMh|ryP NFfIVYZUSU6JRWK=
NCI-H2141 M37HNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL0OG1nUUN3ME21MlE1OjZ6IN88US=> NYTQc2pvW0GQR1XS
EB-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TyZ2lEPTB;NT6xO|UxPCEQvF2= MlTwV2FPT0WU
NCI-H1522 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfYN5F4UUN3ME21MlI3OzJ{IN88US=> M2r4RXNCVkeHUh?=
MRK-nu-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvI[25KSzVyPUWuOFM3OzNizszN NF\adppUSU6JRWK=
no-11 M2jpXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTVwNEewPFch|ryP Mo\HV2FPT0WU
CESS M4fkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTVwNUiwN|Qh|ryP NHLoZYZUSU6JRWK=
KMOE-2 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTVwNUi2OVkh|ryP NV3GfYl[W0GQR1XS
REH MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCTWM2OD14LkK1OlE5KM7:TR?= MojBV2FPT0WU
KU812 M3XaNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnjOG1iUUN3ME22MlQzPzlzIN88US=> NX\obZo2W0GQR1XS
SK-N-FI NVHrc256T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fHVGlEPTB;Nj62NFY4PCEQvF2= MkfLV2FPT0WU
MMAC-SF NYHjZnhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\iTWM2OD15LkC2OFkzKM7:TR?= M1\MSHNCVkeHUh?=
RCC10RGB NYm5OHpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnNUYdKSzVyPUeuNlI6PzdizszN MYnTRW5ITVJ?
NCI-H322M NWHEW5dZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPvTWM2OD15LkOzN|M2KM7:TR?= NH72Z4dUSU6JRWK=
NB6 M4P0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\DcmlEPTB;Nz61OFg6QSEQvF2= NEPaSVdUSU6JRWK=
MN-60 NIr5SIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u5bGlEPTB;Nz62PVIyPSEQvF2= NUf5bIZTW0GQR1XS
NCI-H1092 M3u0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TIVGlEPTB;OD6wNVc{PCEQvF2= MoH5V2FPT0WU
EKVX NEDqUVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfifGh5UUN3ME24MlQ4ODZ4IN88US=> M1H4dXNCVkeHUh?=
D-263MG NHPQ[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRThwNUWzPVYh|ryP M1nIZ3NCVkeHUh?=
NCI-H209 NVv6epBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRThwNkSwNFYh|ryP NIGyW|hUSU6JRWK=
IST-SL1 M2\UfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXW2UZR3UUN3ME24Mlg6QDl{IN88US=> NXLtSpVzW0GQR1XS
ACN NFn6UpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PseGlEPTB;OT6xPVE2PyEQvF2= MUPTRW5ITVJ?
MHH-PREB-1 M3:3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j0XmlEPTB;OT6yNVIyQSEQvF2= MkjVV2FPT0WU
EW-11 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnUTGtKSzVyPUmuOlU{QTZizszN MXPTRW5ITVJ?
KASUMI-1 M4n0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV34e2R4UUN3ME25Mlc5PzdizszN NEXkTFdUSU6JRWK=
KINGS-1 M{TmUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTFyLkKzOFch|ryP Mn\pV2FPT0WU
EVSA-T M3vFZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljGTWM2OD1zMD6zNVkzKM7:TR?= NUnqSlhOW0GQR1XS
DSH1 NVTITm0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHUW2p4UUN3ME2xNE4{QTd{IN88US=> NUfqNlA3W0GQR1XS
COLO-824 M37mVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NESxNYpKSzVyPUGwMlg3PjlizszN MnvGV2FPT0WU
K052 NEO5dFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvqTWM2OD1zMD65N|IzKM7:TR?= NH3a[VdUSU6JRWK=
SK-MEL-2 M1e1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTVTWM2OD1zMD65PVM6KM7:TR?= M2fVfnNCVkeHUh?=

... 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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