TAE684 (NVP-TAE684)

For research use only.

Catalog No.S1108

65 publications

TAE684 (NVP-TAE684) Chemical Structure

CAS No. 761439-42-3

TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.

Selleck's TAE684 (NVP-TAE684) has been cited by 65 publications

Purity & Quality Control

Choose Selective ALK Inhibitors

Biological Activity

Description TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
Targets
ALK [1]
(Cell-free assay)
3 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCC-3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3zTWM2OD1yLkCwNFA3ODNizszN MVLTRW5ITVJ?
SF539 NFqxNppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILFNoRKSzVyPUCuNFAxPTZ2IN88US=> NHrtWIxUSU6JRWK=
DEL NGnnWZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fo[mlEPTB;MD6wNFA6OjdizszN Ml7YV2FPT0WU
NB1 MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3YTWM2OD1yLkCwNVYzKM7:TR?= NXzzUJBxW0GQR1XS
SR MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjmPYdKSzVyPUCuNFAzPzdizszN NXHqXXZsW0GQR1XS
KARPAS-299 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33vPGlEPTB;MD6wNlM5PCEQvF2= M2HNe3NCVkeHUh?=
MHH-CALL-2 NWDRZlJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVG1UppEUUN3ME2wMlAzQTV{IN88US=> M134b3NCVkeHUh?=
SU-DHL-1 NIXD[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwMES4OlUh|ryP MXfTRW5ITVJ?
A4-Fuk NYnWdohXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\reIdKSzVyPUCuNFU2PjVizszN MYrTRW5ITVJ?
EW-1 M33BXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHifmMzUUN3ME2wMlExOjV4IN88US=> NELMNnhUSU6JRWK=
NOS-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjZWm5DUUN3ME2wMlExOjl2IN88US=> MVrTRW5ITVJ?
EW-16 NX61eYZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMUC1Olgh|ryP NF7GT49USU6JRWK=
TE-11 NYf2R5dPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln0TWM2OD1yLkG2NFk3KM7:TR?= Mn\PV2FPT0WU
SW982 NV2xV2VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\CeXNKSzVyPUCuNVY1PzhizszN Mn\MV2FPT0WU
LAN-6 NYrBZmdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMUe0OFMh|ryP NWXD[Zp4W0GQR1XS
MZ1-PC MlrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f0V2lEPTB;MD6xO|g{PSEQvF2= M1;udXNCVkeHUh?=
KS-1 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Lxb2lEPTB;MD6xPVM1OyEQvF2= NEnmb2RUSU6JRWK=
PSN1 M1nhUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HVbWlEPTB;MD6xPVY{OSEQvF2= MVvTRW5ITVJ?
LC-2-ad NFj3XYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPHTWM2OD1yLkG5OlkzKM7:TR?= NVnEWZZVW0GQR1XS
COLO-320-HSR MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrsVoZKSzVyPUCuNVk4PzZizszN NILCfZlUSU6JRWK=
OPM-2 NYjZflIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XSSmlEPTB;MD6yNlY3QSEQvF2= NFO3UVBUSU6JRWK=
SK-NEP-1 M2Lydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDreIhPUUN3ME2wMlI{PTJ2IN88US=> MXrTRW5ITVJ?
ALL-PO M{nFU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2SwemlEPTB;MD6yOFUzPCEQvF2= MkjVV2FPT0WU
CMK NF:wfVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4CwVGlEPTB;MD6yOVU{KM7:TR?= M2ThTXNCVkeHUh?=
NCI-H1648 Ml63S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi5dY9KSzVyPUCuNlc5PTVizszN MXPTRW5ITVJ?
SIG-M5 M4DXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[xdnpKSzVyPUCuNlkyPTlizszN M1u4bXNCVkeHUh?=
TGBC24TKB MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwM{CyNVgh|ryP Moi5V2FPT0WU
DOHH-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVK3S283UUN3ME2wMlMyOjB2IN88US=> NFr3fIFUSU6JRWK=
NB69 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwM{G3PFch|ryP MUnTRW5ITVJ?
MFH-ino MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwM{K1NlMh|ryP M1\oeHNCVkeHUh?=
KP-N-RT-BM-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f6TGlEPTB;MD6zN|EzOyEQvF2= NY\nTFBnW0GQR1XS
MONO-MAC-6 NEG1SnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH31[2NKSzVyPUCuN|MzQTFizszN NHPnT2VUSU6JRWK=
ATN-1 MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;ZTWM2OD1yLkOzN|A{KM7:TR?= NUT4S5M4W0GQR1XS
NTERA-S-cl-D1 MoTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17hb2lEPTB;MD6zN|M6PiEQvF2= Mn\PV2FPT0WU
L-540 MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPiV2ExUUN3ME2wMlM3QTh6IN88US=> MnnaV2FPT0WU
GB-1 M4D1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rPTGlEPTB;MD6zPFg3PyEQvF2= M4TOU3NCVkeHUh?=
MV-4-11 NGTmOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnOeotKSzVyPUCuN|k1PDZizszN NXPMSm5CW0GQR1XS
KG-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHy2d5RKSzVyPUCuN|k2PjFizszN Mk\xV2FPT0WU
OVCAR-4 NHHNS45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjQO2xKSzVyPUCuOFA2PjlizszN M3PubHNCVkeHUh?=
NEC8 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwNEGyPVIh|ryP MWfTRW5ITVJ?
SK-MM-2 NHf5NHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK3TWM2OD1yLkSxOlA6KM7:TR?= MWnTRW5ITVJ?
TE-8 NHfwWopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwNEK4PEDPxE1? MnTkV2FPT0WU
697 MkjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnzW4pZUUN3ME2wMlQ{OjF3IN88US=> NELMXZlUSU6JRWK=
NB14 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jT[2lEPTB;MD60N|gzPiEQvF2= MW\TRW5ITVJ?
GDM-1 NFzxNm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj0TWM2OD1yLkS3NVE3KM7:TR?= NV:0UIttW0GQR1XS
HUTU-80 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HLNmlEPTB;MD60O|M4PSEQvF2= NIf1fI5USU6JRWK=
HL-60 M4raOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml33TWM2OD1yLkS4NVQzKM7:TR?= MnLwV2FPT0WU
OCI-AML2 NHTpXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwNEizNlgh|ryP NEfoeYZUSU6JRWK=
ML-2 M1rtVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S4T2lEPTB;MD60PVA{OSEQvF2= NHPyTYtUSU6JRWK=
ES4 NE\PSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHJ[JpKSzVyPUCuOFkyODlizszN NGXlSo1USU6JRWK=
NCI-H747 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTBwNEm4PUDPxE1? MUnTRW5ITVJ?
RL95-2 NFnqbHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHFTWM2OD1yLkWwNVEzKM7:TR?= NXTEO4FQW0GQR1XS
TE-15 NH3oPFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrZT3BLUUN3ME2wMlUyOTJ2IN88US=> MVHTRW5ITVJ?
TE-12 NEj6blFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLCcXE5UUN3ME2wMlU{OzR7IN88US=> NWLnXoVLW0GQR1XS
LB1047-RCC MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PZNWlEPTB;MD61OFU1QSEQvF2= M1TrPXNCVkeHUh?=
LB831-BLC NFjWfWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jhdWlEPTB;MD61OVAzOyEQvF2= MmTuV2FPT0WU
NCI-H1355 Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnyTWM2OD1yLkW1NVg1KM7:TR?= M3rkOnNCVkeHUh?=
CTV-1 NVjNNnZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjBTWM2OD1yLkW1OlI1KM7:TR?= NYmyVVA4W0GQR1XS
RXF393 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwNUW3PVQh|ryP NVqyeYhSW0GQR1XS
SW872 M3zNPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHrc4dKSzVyPUCuOVY4OjRizszN NVv1PJhGW0GQR1XS
MPP-89 M3W5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLZTWM2OD1yLkW3PFg1KM7:TR?= NYLzRWF7W0GQR1XS
RPMI-8226 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXWbm9{UUN3ME2wMlY{PTJ4IN88US=> M{TGVHNCVkeHUh?=
LS-1034 NH7PSXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfEOoM5UUN3ME2wMlY{PThizszN M4rtTXNCVkeHUh?=
SJSA-1 NF;ROmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLH[JlKSzVyPUCuOlM4OjVizszN MVPTRW5ITVJ?
HOP-62 NVnKTnA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\NcItxUUN3ME2wMlY2ODN|IN88US=> M3KzSnNCVkeHUh?=
KGN NFvkTGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LOO2lEPTB;MD62OlE3QCEQvF2= MmriV2FPT0WU
D-336MG NILyVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwNk[xOlkh|ryP NXj6U2dDW0GQR1XS
LS-411N MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;Ib4xKSzVyPUCuOlc1PjJizszN M3O3dnNCVkeHUh?=
TE-1 M2SwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfkNZg4UUN3ME2wMlY6ODd2IN88US=> MUXTRW5ITVJ?
LB996-RCC M1vJemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnubHg4UUN3ME2wMlY6Ozh7IN88US=> MojNV2FPT0WU
TE-10 M4jz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nxbmlEPTB;MD63NVQ6PiEQvF2= NYT1ZlBSW0GQR1XS
NCI-SNU-16 NILXdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwN{K2OlQh|ryP NYGxPGt4W0GQR1XS
ES8 MorvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[zPZlqUUN3ME2wMlc1QTd3IN88US=> NFLhUZdUSU6JRWK=
COLO-800 NEXkU|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmWxTWM2OD1yLke2Olk2KM7:TR?= MVLTRW5ITVJ?
ES6 M2Xxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nrbGlEPTB;MD63O|U2QSEQvF2= M3nH[3NCVkeHUh?=
L-363 NIG2cIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwOEKzO|Uh|ryP NGjZUG1USU6JRWK=
NMC-G1 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;MRYVNUUN3ME2wMlg{OjN|IN88US=> NUDqb2tDW0GQR1XS
LU-134-A M4q2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvoOJd{UUN3ME2wMlg{QTF{IN88US=> M3LrenNCVkeHUh?=
SF268 NIfCd2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDNN2VFUUN3ME2wMlg1ODR{IN88US=> NH;nS|JUSU6JRWK=
KARPAS-45 NUW0WpFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHwTWxKSzVyPUCuPFQzPjNizszN NEXxTGNUSU6JRWK=
TGW NXnDZpNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H1TWlEPTB;MD64OVg3OyEQvF2= NIfJWFRUSU6JRWK=
CHP-126 NX;MW|B3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml23TWM2OD1yLki1PVU4KM7:TR?= NYfsZpFLW0GQR1XS
MOLT-16 NIPLcHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jvXWlEPTB;MD64O|U5QSEQvF2= NFHEfmRUSU6JRWK=
LB771-HNC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;rTWM2OD1yLki5O|U4KM7:TR?= NUHFSGtuW0GQR1XS
NALM-6 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\OOZZKSzVyPUCuPVA4OzlizszN M{TFVHNCVkeHUh?=
GCIY NVvsdFczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrxTWM2OD1yLkm1OVI3KM7:TR?= MlfWV2FPT0WU
IST-MES1 NHjtfZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPMPGxFUUN3ME2wMlk5QDJ2IN88US=> M1LXOHNCVkeHUh?=
LB2241-RCC NFfZclhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnabGxUUUN3ME2wMlk5QDRizszN MYnTRW5ITVJ?
BL-70 MnniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnZTWM2OD1yLkm5OVM2KM7:TR?= MXzTRW5ITVJ?
NB17 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LkTWlEPTB;MT6wNFY{QSEQvF2= MlXqV2FPT0WU
LXF-289 NV7GXWxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LL[GlEPTB;MT6wN|A4PiEQvF2= MVjTRW5ITVJ?
TK10 NWjudWFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\hTo5CUUN3ME2xMlA2ODZ|IN88US=> MWDTRW5ITVJ?
K5 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPhUHZKSzVyPUGuNFYzPzRizszN NGXvelhUSU6JRWK=
NCI-H716 MojFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFwMEeyOVkh|ryP M3HUVHNCVkeHUh?=
HCE-T MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFwMEi4NVkh|ryP MmXEV2FPT0WU
GI-1 M1PTSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjrcXIyUUN3ME2xMlA6Pzl6IN88US=> NGPr[I9USU6JRWK=
KARPAS-422 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm5dYF1UUN3ME2xMlExODJ{IN88US=> M1fpRnNCVkeHUh?=
TE-9 M2Kyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3EPGg2UUN3ME2xMlEyOzJ6IN88US=> NXXQUW16W0GQR1XS
SF126 Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjpR|RKSzVyPUGuNVE2PjhizszN Mmr5V2FPT0WU
BB30-HNC NW\yNVZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K2eWlEPTB;MT6xN|EyOiEQvF2= NEPPOXVUSU6JRWK=
NCI-H1304 NIPvfm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFwMUOzN|gh|ryP M4rtWHNCVkeHUh?=
HEL M1\PdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn0NYpIUUN3ME2xMlE1QDl3IN88US=> MWjTRW5ITVJ?
HAL-01 NFvzfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLJW3pKSzVyPUGuNVUzQDNizszN Mln2V2FPT0WU
SK-LMS-1 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPjXINKSzVyPUGuNVU6PzRizszN Mn;vV2FPT0WU
SW954 M2Owb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFwMUm1Olch|ryP NIjRXWFUSU6JRWK=
D-283MED NHvEblFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTFwMkKzO|kh|ryP Mn;1V2FPT0WU
NCI-H1882 M1XVXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\xTYVKSzVyPUGuNlM5QSEQvF2= MXPTRW5ITVJ?
GI-ME-N NYHpU49vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnf5TWM2OD1zLkK1NlA5KM7:TR?= NFnUTohUSU6JRWK=
SK-PN-DW M2HKSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDXXZBDUUN3ME2xMlI3OzR6IN88US=> NHjL[mhUSU6JRWK=
C2BBe1 M{nEcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13zb2lEPTB;MT6yPVEyPyEQvF2= M17ud3NCVkeHUh?=
A704 MkToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnzXWJFUUN3ME2xMlMzPjh7IN88US=> MVLTRW5ITVJ?
KALS-1 NIS2[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwM{SwPEDPxE1? NUjNZ2ZsW0GQR1XS
ETK-1 M37jeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILWRnlKSzVyPUGuN|Q1QDlizszN NI\2SGtUSU6JRWK=
LB647-SCLC NWDJVosxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTrZYJKSzVyPUGuN|Q6QDZizszN MXLTRW5ITVJ?
OCUB-M Ml7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwM{[xOFMh|ryP NH;lPGtUSU6JRWK=
NCI-H720 Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrPR3BxUUN3ME2xMlM3Ozd6IN88US=> MmrTV2FPT0WU
NB13 NYXZeWpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\TeWlEPTB;MT6zO|I6OyEQvF2= M13ie3NCVkeHUh?=
GR-ST MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v1cmlEPTB;MT6zPFc2PyEQvF2= M3fWfnNCVkeHUh?=
DU-4475 NHj6Z41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPsVGlKSzVyPUGuOFU5PTNizszN MnXtV2FPT0WU
HCC2157 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7ZSIlKSzVyPUGuOFY3PTlizszN MWHTRW5ITVJ?
RKO MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nQ[GlEPTB;MT60PVkzOiEQvF2= NWHKcHVjW0GQR1XS
LS-123 MmrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;WT5VKSzVyPUGuOVE2QTRizszN M4i2NXNCVkeHUh?=
NCI-H69 NHHleHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL2[5lKUUN3ME2xMlU2QDFzIN88US=> NXTaOpp3W0GQR1XS
SW962 NWTZdG5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzoTWM2OD1zLkW2NVMh|ryP NVmxc5d[W0GQR1XS
PF-382 M3:2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjhTWM2OD1zLkW2PVYh|ryP MWnTRW5ITVJ?
A101D M4TjTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37QWGlEPTB;MT61O|EyOyEQvF2= NFjsVpZUSU6JRWK=
NB10 MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nnSGlEPTB;MT61O|M6OiEQvF2= NELud5BUSU6JRWK=
NB5 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G1Z2lEPTB;MT61PFQ4PiEQvF2= NVHFV|BTW0GQR1XS
HCE-4 NXjkfXlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwNkC4OUDPxE1? MnzuV2FPT0WU
HT-144 M4O0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XyU2lEPTB;MT62N|E6KM7:TR?= MUPTRW5ITVJ?
NCI-H524 MkD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPiTWM2OD1zLk[0N|A4KM7:TR?= NEi0UGpUSU6JRWK=
NKM-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LtfmlEPTB;MT62PFY3KM7:TR?= NVnZNo13W0GQR1XS
KURAMOCHI M{\LRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{myWGlEPTB;MT62PVU4OyEQvF2= NHTWc5FUSU6JRWK=
NCI-H187 NFrSSVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:yeI1KSzVyPUGuO|AxOzZizszN M4SySXNCVkeHUh?=
U-266 M3LIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLxTWM2OD1zLkezPFQzKM7:TR?= M3njZXNCVkeHUh?=
BL-41 MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVu0TZlUUUN3ME2xMlc3Ojd{IN88US=> NVLGXZVjW0GQR1XS
SK-N-DZ MmHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnv0TWM2OD1zLke4N|A6KM7:TR?= MkDtV2FPT0WU
Daudi NFm1T|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPI[4lKSzVyPUGuO|g6PjdizszN Mm\0V2FPT0WU
CPC-N M2\VeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvKfHJKSzVyPUGuPFUxQTZizszN M3KyTHNCVkeHUh?=
EM-2 M1nITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTFwOEWxJO69VQ>? MnTlV2FPT0WU
HCC1187 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFwOE[yOFEh|ryP MkXNV2FPT0WU
LP-1 M2TBZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFwOEexOFMh|ryP NFe2dVZUSU6JRWK=
CAS-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwOUiyPVkh|ryP M3\4V3NCVkeHUh?=
NB7 NGCyb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLwTWM2OD1{LkCwOVU2KM7:TR?= M4i5UXNCVkeHUh?=
VA-ES-BJ NFS5OndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJwMEG1NVMh|ryP NFr2Z|RUSU6JRWK=
SNU-C2B MkjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT3TWM2OD1{LkCzN|UyKM7:TR?= NFHTUJNUSU6JRWK=
LOXIMVI NIXoZmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fQbWlEPTB;Mj6wOlc5PiEQvF2= M3jIbnNCVkeHUh?=
NCI-H1581 NXH2[nZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmO3TWM2OD1{LkGxOVU6KM7:TR?= MmfXV2FPT0WU
IST-SL2 NGTHNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XrTWlEPTB;Mj6xNlQ1PSEQvF2= NYHLNXJiW0GQR1XS
NOMO-1 NHPyUnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\1TZh7UUN3ME2yMlE4Pjh|IN88US=> NELLXZhUSU6JRWK=
TE-6 NWDnb4lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fJbWlEPTB;Mj6xPVA2KM7:TR?= NYfvbYxMW0GQR1XS
NCI-H526 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\JTWM2OD1{LkG5NVQyKM7:TR?= MkTBV2FPT0WU
MSTO-211H NVPVXIZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DFS2lEPTB;Mj6yNFA1OSEQvF2= M3;HfXNCVkeHUh?=
LS-513 NX\yc2N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDWTWM2OD1{LkKyNlY6KM7:TR?= MXHTRW5ITVJ?
NCI-SNU-1 NWjpW5ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HuO2lEPTB;Mj6zN|I2PiEQvF2= NFWwUZVUSU6JRWK=
BB65-RCC M1PoXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjxOm1GUUN3ME2yMlM4PDl|IN88US=> MnPjV2FPT0WU
GT3TKB NXf0dpZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzmUndLUUN3ME2yMlM6QTd{IN88US=> NWTxSGI1W0GQR1XS
OS-RC-2 NXTScJRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLFV5VbUUN3ME2yMlQzOzRzIN88US=> NXrze|NMW0GQR1XS
NCI-H2126 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnXfJE1UUN3ME2yMlQ{Pjd2IN88US=> M2TSWXNCVkeHUh?=
SK-UT-1 M2\PSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXpTWM2OD1{LkS3OFY4KM7:TR?= NHLlfGhUSU6JRWK=
DMS-114 NGfHdYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPL[GhKSzVyPUKuOlE2OjRizszN MnzsV2FPT0WU
ONS-76 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTJwNkO2OFEh|ryP NVLHXnRIW0GQR1XS
8-MG-BA NEewR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJwNkW0NVQh|ryP NVnGOHVPW0GQR1XS
BOKU MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJwN{K3OlQh|ryP MWTTRW5ITVJ?
LAMA-84 M1S5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTCTWM2OD1{Lke5PVEzKM7:TR?= NF;HNYFUSU6JRWK=
ES1 Mn;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrqUZNKSzVyPUKuPFE5ODRizszN M1n4NnNCVkeHUh?=
NCI-H1395 Mk\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r0[2lEPTB;Mj64NlAyOiEQvF2= NEXQbVZUSU6JRWK=
A388 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJwOU[xO{DPxE1? M{nJOnNCVkeHUh?=
NCCIT MmPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37mbmlEPTB;Mz6wPFg3OiEQvF2= M1LpNnNCVkeHUh?=
HD-MY-Z M3HP[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DEdGlEPTB;Mz6xN|IxOyEQvF2= M1XxNHNCVkeHUh?=
NCI-H510A M{K2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W0ZmlEPTB;Mz6xPFk1OyEQvF2= NY[xcpI1W0GQR1XS
NCI-N87 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTNwMkCwNkDPxE1? NXu2eoVsW0GQR1XS
SCLC-21H MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvDcZlvUUN3ME2zMlI3QDV7IN88US=> M{TEPHNCVkeHUh?=
SH-4 NE\4R|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LS[GlEPTB;Mz6yPFc6PyEQvF2= NVrj[FI6W0GQR1XS
QIMR-WIL NXHpXlN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTNwM{K4OFkh|ryP MULTRW5ITVJ?
KM12 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTNwM{O1OFQh|ryP M3n3VXNCVkeHUh?=
ST486 M3;kO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XwSWlEPTB;Mz61N|g5OyEQvF2= Mk\lV2FPT0WU
HC-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTNwNkKwNlgh|ryP M1HPU3NCVkeHUh?=
BV-173 MmrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL6XHNPUUN3ME2zMlY1ODh6IN88US=> MUDTRW5ITVJ?
EW-24 MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTNwNk[0N|Qh|ryP Mm\nV2FPT0WU
LU-65 Mm\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPBfWJKSzVyPUOuOlg4OSEQvF2= NGXHZZpUSU6JRWK=
ECC4 NHf1eoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTNwN{e1OkDPxE1? NFPkWJhUSU6JRWK=
ARH-77 MlTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTvTWM2OD12LkGxNFY4KM7:TR?= M{TJUHNCVkeHUh?=
BC-3 M3znOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HiXGlEPTB;ND6xN|A3QCEQvF2= M3\Ue3NCVkeHUh?=
SNB75 NV7UUm9kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv3d2YxUUN3ME20MlI3OTlizszN NEHRbmpUSU6JRWK=
MEG-01 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TYR2lEPTB;ND6yO|QyQSEQvF2= NEXB[nJUSU6JRWK=
NCI-H1417 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHxNopKSzVyPUSuNlg1PDNizszN NV7sOXNpW0GQR1XS
MDA-MB-134-VI NVmx[mMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHUTWM2OD12LkOwOlAyKM7:TR?= MlviV2FPT0WU
Becker Ml\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn74TWM2OD12LkS3N|M3KM7:TR?= MoX6V2FPT0WU
DMS-153 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTRwNk[0O|Uh|ryP M3W0WHNCVkeHUh?=
TGBC1TKB MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{e2SWlEPTB;ND62PFUyPSEQvF2= MWLTRW5ITVJ?
EW-3 NULqTIdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFm0U3hKSzVyPUSuO|YzPDhizszN MX3TRW5ITVJ?
KE-37 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTRwOE[xPVYh|ryP NVXnS4JEW0GQR1XS
NCI-H23 NHexfG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH33NGxKSzVyPUSuPFczOjdizszN M2jFb3NCVkeHUh?=
MC116 NUi1cmtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTRwOUSxNlYh|ryP NFLiVFRUSU6JRWK=
NH-12 NF\6NHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfnTWM2OD12Lkm2OFM6KM7:TR?= NFy0U25USU6JRWK=
CTB-1 NVrmdFNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr2[IloUUN3ME20Mlk4PzJzIN88US=> MYnTRW5ITVJ?
KM-H2 M{ftW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTVwMEWzNlMh|ryP NIjkPXhUSU6JRWK=
MOLT-4 NVPZSVVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjFVlVKSzVyPUWuNVE5OyEQvF2= MmDmV2FPT0WU
NCI-H2141 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTVwMUSyOlgh|ryP MljzV2FPT0WU
EB-3 M4f3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\UZmFKSzVyPUWuNVc2ODRizszN M1vTSnNCVkeHUh?=
NCI-H1522 NHjOfohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTVwMk[zNlIh|ryP NIe0SXVUSU6JRWK=
MRK-nu-1 NV\FZmJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\MTWM2OD13LkSzOlM{KM7:TR?= Mm\uV2FPT0WU
no-11 M3jId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\QW2lEPTB;NT60O|A5PyEQvF2= M4LWUnNCVkeHUh?=
CESS NVHGSnlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfxOmc3UUN3ME21MlU5ODN2IN88US=> MUHTRW5ITVJ?
KMOE-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTVwNUi2OVkh|ryP M3;l[XNCVkeHUh?=
REH MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTZwMkW2NVgh|ryP M1rBT3NCVkeHUh?=
KU812 Ml7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XhVmlEPTB;Nj60Nlc6OSEQvF2= MWXTRW5ITVJ?
SK-N-FI NYLvZ|FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;2Noo2UUN3ME22MlYxPjd2IN88US=> NHe5TnZUSU6JRWK=
MMAC-SF NYW1VZNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P3bmlEPTB;Nz6wOlQ6OiEQvF2= NGjWSVdUSU6JRWK=
RCC10RGB M1rV[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrYNJdRUUN3ME23MlIzQTd5IN88US=> M4THSHNCVkeHUh?=
NCI-H322M NHLyNHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO4RVZKSzVyPUeuN|M{OzVizszN MkTHV2FPT0WU
NB6 M33k[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTdwNUS4PVkh|ryP MkXjV2FPT0WU
MN-60 Mn;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvyTWM2OD15Lk[5NlE2KM7:TR?= NITBWlVUSU6JRWK=
NCI-H1092 M2[xXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRThwMEG3N|Qh|ryP NH\UWW5USU6JRWK=
EKVX Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXwTWM2OD16LkS3NFY3KM7:TR?= NHjQVGdUSU6JRWK=
D-263MG MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHniRplKSzVyPUiuOVU{QTZizszN Mkj4V2FPT0WU
NCI-H209 NH3GOWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHFXnE6UUN3ME24MlY1ODB4IN88US=> MYDTRW5ITVJ?
IST-SL1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK0PVF6UUN3ME24Mlg6QDl{IN88US=> MUnTRW5ITVJ?
ACN MlvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXFTWM2OD17LkG5NVU4KM7:TR?= MoK5V2FPT0WU
MHH-PREB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLnOIdvUUN3ME25MlIyOjF7IN88US=> NHPwRm5USU6JRWK=
EW-11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ixfGlEPTB;OT62OVM6PiEQvF2= MonTV2FPT0WU
KASUMI-1 NHzYSWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HteWlEPTB;OT63PFc4KM7:TR?= M3jPN3NCVkeHUh?=
KINGS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2P4XGlEPTB;MUCuNlM1PyEQvF2= NXviUYFFW0GQR1XS
EVSA-T MnT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzpZ2ZpUUN3ME2xNE4{OTl{IN88US=> NYS5RnA5W0GQR1XS
DSH1 M{PwWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFyLkO5O|Ih|ryP NI\ITJFUSU6JRWK=
COLO-824 MmLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLMfGhKSzVyPUGwMlg3PjlizszN M1PtcXNCVkeHUh?=
K052 M1;WUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzCTWM2OD1zMD65N|IzKM7:TR?= MVHTRW5ITVJ?
SK-MEL-2 NInKeHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTFyLkm5N|kh|ryP NH24OGlUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP ; 

PubMed: 22240786     


H3122 or H2228 cells were incubated with the indicated concentrations of TAE684 for 48 h, after which cell lysates were prepared and subjected to immunoblot analysis with antibodies to phosphorylated (p) or total forms of ALK, STAT3, ERK, or AKT as well as with those to BIM, to survivin, to PARP, or to β-actin (loading control). The positions of the bands for EML4–ALK, BIMEL, and intact and cleaved forms of PARP are shown for the corresponding antibodies. 

p-ROS1 / ROS1 ; 

PubMed: 25351743     


Inhibition of phospho-ROS1 by various identified ROS1 inhibitors selected from the high throughput screening. CD74-ROS1-WT-expressing (clone 6) or CD74-ROS1-G2032R-expressing Ba/F3 cells were exposed to increasing concentrations of cabozantinib (XL184), TAE684, or foretinib (B) for 2 h. Following treatment, the cell lysates were immunoblotted to detect the indicated proteins.

22240786 25351743
Growth inhibition assay
Cell viability; 

PubMed: 18594010     


NSCLC cells were treated with TAE-684 at the indicated concentrations, and viable cells were measured after 72 hours of treatment. The percentage of viable cells is shown relative to untreated controls. A549 (KRAS G12S); PC9 (EGFRdelE746_A750); H2228 (EML4-ALK variant 3); H3122 (EML4-ALK variant 1); DFCI032 (EML4-ALK variant 1). 

18594010
In vivo 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]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: 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.
  • Concentrations: 1 nM-10 μM
  • Incubation Time: 2–3 days
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice.
  • Dosages: 1, 3, and 10 mg/kg
  • Administration: Once daily by oral gavage for 3 weeks
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL (4.88 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol, pH 4
For best results, use promptly after mixing.
10 mg/mL

* 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.

Chemical Information

Molecular Weight 614.2
Formula

C30H40ClN7O3S

CAS No. 761439-42-3
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID