TAE684 (NVP-TAE684)

Catalog No.S1108

TAE684 (NVP-TAE684) Chemical Structure

Molecular Weight(MW): 614.2

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.

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Cited by 39 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.
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 M4juSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTUTWM2OD1yLkCwNFA3ODNizszN NHr6RXFUSU6JRWK=
SF539 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLwZldiUUN3ME2wMlAxODV4NDFOwG0> M{XRc3NCVkeHUh?=
DEL M1TYRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1KxUmlEPTB;MD6wNFA6OjdizszN Ml7LV2FPT0WU
NB1 M4[3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwMECxOlIh|ryP M{POc3NCVkeHUh?=
SR NInSNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX20NGVZUUN3ME2wMlAxOjd5IN88US=> M3e1TnNCVkeHUh?=
KARPAS-299 M1GwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnFZ3VxUUN3ME2wMlAzOzh2IN88US=> MmHEV2FPT0WU
MHH-CALL-2 M{XkVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvrUpdKSzVyPUCuNFI6PTJizszN NGTWWZpUSU6JRWK=
SU-DHL-1 M3vx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwMES4OlUh|ryP M{\MSXNCVkeHUh?=
A4-Fuk MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzIe4g1UUN3ME2wMlA2PTZ3IN88US=> NUjlSVNHW0GQR1XS
EW-1 NUnEPGdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\3[|JKSzVyPUCuNVAzPTZizszN M4LmVXNCVkeHUh?=
NOS-1 NYLObGpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHETWM2OD1yLkGwNlk1KM7:TR?= NYLpZmV6W0GQR1XS
EW-16 MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwMUC1Olgh|ryP MULTRW5ITVJ?
TE-11 NUTheW5YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXEeYR2UUN3ME2wMlE3ODl4IN88US=> MUfTRW5ITVJ?
SW982 NGD6cGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHTTWM2OD1yLkG2OFc5KM7:TR?= MlrWV2FPT0WU
LAN-6 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjFd|BKSzVyPUCuNVc1PDNizszN NGPaU5dUSU6JRWK=
MZ1-PC MmDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C4cWlEPTB;MD6xO|g{PSEQvF2= NHf5TFBUSU6JRWK=
KS-1 MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTxb25MUUN3ME2wMlE6OzR|IN88US=> M13BeXNCVkeHUh?=
PSN1 M2XYNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwMUm2N|Eh|ryP MX;TRW5ITVJ?
LC-2-ad NVHCUWFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG3c41KSzVyPUCuNVk3QTJizszN MkHmV2FPT0WU
COLO-320-HSR M2\aT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;LTWM2OD1yLkG5O|c3KM7:TR?= NVHGW3VRW0GQR1XS
OPM-2 NYLLVJduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG2OlFyUUN3ME2wMlIzPjZ7IN88US=> NVrhfHg1W0GQR1XS
SK-NEP-1 NVjVeXZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfMdoZKSzVyPUCuNlM2OjRizszN M3rzdnNCVkeHUh?=
ALL-PO M3HnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTBwMkS1NlQh|ryP MlrrV2FPT0WU
CMK NEnJe4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFGwcpBKSzVyPUCuNlU2OyEQvF2= NWi3UGZrW0GQR1XS
NCI-H1648 NH\JVHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwMke4OVUh|ryP MnPiV2FPT0WU
SIG-M5 MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVm5OGx5UUN3ME2wMlI6OTV7IN88US=> MVHTRW5ITVJ?
TGBC24TKB M3fLWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\VTGlEPTB;MD6zNFIyQCEQvF2= NX7TUVN7W0GQR1XS
DOHH-2 NGXGWmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwM{GyNFQh|ryP NFfMWGVUSU6JRWK=
NB69 MnvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwM{G3PFch|ryP NWG5dpZKW0GQR1XS
MFH-ino M2PYSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTpTWM2OD1yLkOyOVI{KM7:TR?= MmPkV2FPT0WU
KP-N-RT-BM-1 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLkdmpKSzVyPUCuN|MyOjNizszN NHHQdnRUSU6JRWK=
MONO-MAC-6 NXezZop5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwM{OyPVEh|ryP Mm\HV2FPT0WU
ATN-1 NVy0T5lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[3fVVKSzVyPUCuN|M{ODNizszN MWXTRW5ITVJ?
NTERA-S-cl-D1 M2TYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu0ZlhKSzVyPUCuN|M{QTZizszN Mnz2V2FPT0WU
L-540 Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwM{[5PFgh|ryP MX\TRW5ITVJ?
GB-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP5TWM2OD1yLkO4PFY4KM7:TR?= NYHjTHk5W0GQR1XS
MV-4-11 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLFTWM2OD1yLkO5OFQ3KM7:TR?= MmfxV2FPT0WU
KG-1 NXXNWZloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf0d5FKSzVyPUCuN|k2PjFizszN MWfTRW5ITVJ?
OVCAR-4 MnTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;aeHNKSzVyPUCuOFA2PjlizszN M4fxXHNCVkeHUh?=
NEC8 M3LZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\IfHdbUUN3ME2wMlQyOjl{IN88US=> NUfOR5JJW0GQR1XS
SK-MM-2 NYLqXIdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3m4RWlEPTB;MD60NVYxQSEQvF2= NF75W3JUSU6JRWK=
TE-8 NILaS5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnCNHl5UUN3ME2wMlQzQDhizszN MmHBV2FPT0WU
697 M1nhUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTBwNEOyNVUh|ryP M3PxdHNCVkeHUh?=
NB14 NGnhR2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvhcJRKSzVyPUCuOFM5OjZizszN MkXEV2FPT0WU
GDM-1 NWK0UnZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jJbGlEPTB;MD60O|EyPiEQvF2= M{T1SnNCVkeHUh?=
HUTU-80 MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XlcmlEPTB;MD60O|M4PSEQvF2= NFTneHhUSU6JRWK=
HL-60 NXLZSXFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknaTWM2OD1yLkS4NVQzKM7:TR?= NGfhSmpUSU6JRWK=
OCI-AML2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwNEizNlgh|ryP MlexV2FPT0WU
ML-2 M4HNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rafmlEPTB;MD60PVA{OSEQvF2= NGLMd45USU6JRWK=
ES4 NXnuN5JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILD[lhKSzVyPUCuOFkyODlizszN NF:5SJRUSU6JRWK=
NCI-H747 NX\Ze4hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3OTWM2OD1yLkS5PFkh|ryP NHHKOJlUSU6JRWK=
RL95-2 NGjKPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvRTWM2OD1yLkWwNVEzKM7:TR?= MXzTRW5ITVJ?
TE-15 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H1ZmlEPTB;MD61NVEzPCEQvF2= Mm\aV2FPT0WU
TE-12 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\jOGlEPTB;MD61N|M1QSEQvF2= NUntemhvW0GQR1XS
LB1047-RCC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDUe4E2UUN3ME2wMlU1PTR7IN88US=> NIO5NWNUSU6JRWK=
LB831-BLC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHYeWo1UUN3ME2wMlU2ODJ|IN88US=> NEja[mVUSU6JRWK=
NCI-H1355 M3HzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPEd3RKSzVyPUCuOVUyQDRizszN NWHXSlJ3W0GQR1XS
CTV-1 NEXBfZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDGfotKSzVyPUCuOVU3OjRizszN NEnST4FUSU6JRWK=
RXF393 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwNUW3PVQh|ryP NUX3TmJFW0GQR1XS
SW872 M3XHVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;nTWM2OD1yLkW2O|I1KM7:TR?= M1z4OXNCVkeHUh?=
MPP-89 M{jyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXi[21UUUN3ME2wMlU4QDh2IN88US=> NXHyVXBDW0GQR1XS
RPMI-8226 MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moi1TWM2OD1yLk[zOVI3KM7:TR?= M{HmbXNCVkeHUh?=
LS-1034 Mn3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrMTWM2OD1yLk[zOVgh|ryP MV;TRW5ITVJ?
SJSA-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HIbWlEPTB;MD62N|czPSEQvF2= M3O1NnNCVkeHUh?=
HOP-62 M4jFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwNkWwN|Mh|ryP NVvseo97W0GQR1XS
KGN MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwNk[xOlgh|ryP M3\ZUHNCVkeHUh?=
D-336MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwNk[xOlkh|ryP NGTTSphUSU6JRWK=
LS-411N MmraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwNke0OlIh|ryP M1rXXHNCVkeHUh?=
TE-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwNkmwO|Qh|ryP MVrTRW5ITVJ?
LB996-RCC NXX4XWwyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nmSWlEPTB;MD62PVM5QSEQvF2= MU\TRW5ITVJ?
TE-10 NHq0c4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfKTWM2OD1yLkexOFk3KM7:TR?= M4\p[HNCVkeHUh?=
NCI-SNU-16 MmjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HUfGlEPTB;MD63NlY3PCEQvF2= NEXQPHBUSU6JRWK=
ES8 MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37ob2lEPTB;MD63OFk4PSEQvF2= MnToV2FPT0WU
COLO-800 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\2SmlEPTB;MD63OlY6PSEQvF2= NW\xc2p2W0GQR1XS
ES6 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwN{e1OVkh|ryP MWfTRW5ITVJ?
L-363 MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwOEKzO|Uh|ryP NUe3cXdCW0GQR1XS
NMC-G1 Mlq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIqzO3FKSzVyPUCuPFMzOzNizszN MoHnV2FPT0WU
LU-134-A MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\STWM2OD1yLkizPVEzKM7:TR?= MVzTRW5ITVJ?
SF268 Mm\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn1[41VUUN3ME2wMlg1ODR{IN88US=> MWrTRW5ITVJ?
KARPAS-45 M4TRS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jTZmlEPTB;MD64OFI3OyEQvF2= M{O4dnNCVkeHUh?=
TGW M1;kNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrjTWM2OD1yLki1PFY{KM7:TR?= MmfkV2FPT0WU
CHP-126 NFGwdXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jQNGlEPTB;MD64OVk2PyEQvF2= M{OxW3NCVkeHUh?=
MOLT-16 M4KwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jHUWlEPTB;MD64O|U5QSEQvF2= MVjTRW5ITVJ?
LB771-HNC M3LFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXOSlBKSzVyPUCuPFk4PTdizszN NUfXOpVPW0GQR1XS
NALM-6 M{LCWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwOUC3N|kh|ryP MoHmV2FPT0WU
GCIY MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;wTWM2OD1yLkm1OVI3KM7:TR?= M1S1WnNCVkeHUh?=
IST-MES1 NVfP[JI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X1WmlEPTB;MD65PFgzPCEQvF2= MnfkV2FPT0WU
LB2241-RCC MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwOUi4OEDPxE1? NFOwNVNUSU6JRWK=
BL-70 M4W4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwOUm1N|Uh|ryP NIm1UYpUSU6JRWK=
NB17 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[2TWM2OD1zLkCwOlM6KM7:TR?= MVfTRW5ITVJ?
LXF-289 NWfSTIE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfQTVNKSzVyPUGuNFMxPzZizszN NGn6d|ZUSU6JRWK=
TK10 M3LJW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[xTWM2OD1zLkC1NFY{KM7:TR?= M{fVTHNCVkeHUh?=
K5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfvW29MUUN3ME2xMlA3Ojd2IN88US=> NV\PepJjW0GQR1XS
NCI-H716 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTJTWM2OD1zLkC3NlU6KM7:TR?= NXvSRnNKW0GQR1XS
HCE-T MnzWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXkTWM2OD1zLkC4PFE6KM7:TR?= NUXNOJdYW0GQR1XS
GI-1 NHX2dmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwMEm3PVgh|ryP NUT6TJhjW0GQR1XS
KARPAS-422 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7LTWM2OD1zLkGwNFIzKM7:TR?= MXXTRW5ITVJ?
TE-9 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFwMUGzNlgh|ryP NX:2fYw6W0GQR1XS
SF126 M1rmcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTFwMUG1Olgh|ryP NXy3dphnW0GQR1XS
BB30-HNC MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwMUOxNVIh|ryP MnTpV2FPT0WU
NCI-H1304 M3W0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{SwXGlEPTB;MT6xN|M{QCEQvF2= MnLuV2FPT0WU
HEL M2XLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M373bGlEPTB;MT6xOFg6PSEQvF2= MVPTRW5ITVJ?
HAL-01 MljnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFwMUWyPFMh|ryP NYTRbXdNW0GQR1XS
SK-LMS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLBPGRDUUN3ME2xMlE2QTd2IN88US=> M1PwZ3NCVkeHUh?=
SW954 M4nJW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fiZ2lEPTB;MT6xPVU3PyEQvF2= NH74eVRUSU6JRWK=
D-283MED M1Lxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwMkKzO|kh|ryP MmnKV2FPT0WU
NCI-H1882 NFnDZZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTFwMkO4PUDPxE1? MYHTRW5ITVJ?
GI-ME-N MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vzS2lEPTB;MT6yOVIxQCEQvF2= NF7hS5JUSU6JRWK=
SK-PN-DW M{TXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPITWM2OD1zLkK2N|Q5KM7:TR?= NWKyVWRHW0GQR1XS
C2BBe1 M{\YUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;QV2lEPTB;MT6yPVEyPyEQvF2= MWHTRW5ITVJ?
A704 NH;6XXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\wO2dxUUN3ME2xMlMzPjh7IN88US=> NULLW4Q6W0GQR1XS
KALS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjYTWM2OD1zLkO0NFgh|ryP M1fEXXNCVkeHUh?=
ETK-1 M3y3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfmbHhKSzVyPUGuN|Q1QDlizszN NIXVN2hUSU6JRWK=
LB647-SCLC MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X3NmlEPTB;MT6zOFk5PiEQvF2= NU[2b3ZNW0GQR1XS
OCUB-M M1\iTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7ySI1KSzVyPUGuN|YyPDNizszN MWLTRW5ITVJ?
NCI-H720 MmXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwM{[zO|gh|ryP MofSV2FPT0WU
NB13 M13hd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vBbGlEPTB;MT6zO|I6OyEQvF2= M4PEdnNCVkeHUh?=
GR-ST M1rXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoO3TWM2OD1zLkO4O|U4KM7:TR?= MXLTRW5ITVJ?
DU-4475 NFnIPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFwNEW4OVMh|ryP MluxV2FPT0WU
HCC2157 M3vnTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjvPVdKSzVyPUGuOFY3PTlizszN MVvTRW5ITVJ?
RKO NWnzcnQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\xT2lEPTB;MT60PVkzOiEQvF2= MnXJV2FPT0WU
LS-123 MojES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjQWmNxUUN3ME2xMlUyPTl2IN88US=> NFX4VWFUSU6JRWK=
NCI-H69 M4DVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\BVGlEPTB;MT61OVgyOSEQvF2= MoDCV2FPT0WU
SW962 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEWySJhKSzVyPUGuOVYyOyEQvF2= Ml;GV2FPT0WU
PF-382 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDhTWM2OD1zLkW2PVYh|ryP NXnpSm5RW0GQR1XS
A101D M3vpZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwNUexNVMh|ryP NGLtSXhUSU6JRWK=
NB10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETJb2dKSzVyPUGuOVc{QTJizszN NETafWFUSU6JRWK=
NB5 MmPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjifplKSzVyPUGuOVg1PzZizszN NHjRbVJUSU6JRWK=
HCE-4 NF3JSlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwNkC4OUDPxE1? NETne3BUSU6JRWK=
HT-144 M1Hvfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jxVWlEPTB;MT62N|E6KM7:TR?= M4Xqe3NCVkeHUh?=
NCI-H524 M2jIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfRenpMUUN3ME2xMlY1OzB5IN88US=> M4\VPXNCVkeHUh?=
NKM-1 MlXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzWPFk{UUN3ME2xMlY5PjZizszN MV\TRW5ITVJ?
KURAMOCHI NV2wfHRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jSRmlEPTB;MT62PVU4OyEQvF2= NWH5c45ZW0GQR1XS
NCI-H187 M{Tub2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjQV5hKSzVyPUGuO|AxOzZizszN MWTTRW5ITVJ?
U-266 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;qe2liUUN3ME2xMlc{QDR{IN88US=> M{PpO3NCVkeHUh?=
BL-41 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwN{[yO|Ih|ryP NWflUVF4W0GQR1XS
SK-N-DZ M{jNbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO2TWM2OD1zLke4N|A6KM7:TR?= MkiyV2FPT0WU
Daudi M3f6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDafJJKSzVyPUGuO|g6PjdizszN MlTRV2FPT0WU
CPC-N MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rRUmlEPTB;MT64OVA6PiEQvF2= NEPxUllUSU6JRWK=
EM-2 MlzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3HTWM2OD1zLki1NUDPxE1? NX3oXW17W0GQR1XS
HCC1187 NXP6PIlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLHT|VpUUN3ME2xMlg3OjRzIN88US=> NXLJemo3W0GQR1XS
LP-1 M4P1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXewS|lOUUN3ME2xMlg4OTR|IN88US=> NV34Z4Z{W0GQR1XS
CAS-1 NV23dVZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2izfGlEPTB;MT65PFI6QSEQvF2= MljjV2FPT0WU
NB7 Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjreldtUUN3ME2yMlAxPTV3IN88US=> MW\TRW5ITVJ?
VA-ES-BJ M1rIcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\Wc|JKSzVyPUKuNFE2OTNizszN M4j2bXNCVkeHUh?=
SNU-C2B NXPKXohJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnQOnRrUUN3ME2yMlA{OzVzIN88US=> NWrCOIw5W0GQR1XS
LOXIMVI MmOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPOV4xKSzVyPUKuNFY4QDZizszN MlfqV2FPT0WU
NCI-H1581 Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTJwMUG1OVkh|ryP MV3TRW5ITVJ?
IST-SL2 NY\mSm5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHoTZN4UUN3ME2yMlEzPDR3IN88US=> MY\TRW5ITVJ?
NOMO-1 NIHhe4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3viOmlEPTB;Mj6xO|Y5OyEQvF2= Mlf1V2FPT0WU
TE-6 NWG1Z|BDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlKxTWM2OD1{LkG5NFUh|ryP MYXTRW5ITVJ?
NCI-H526 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorlTWM2OD1{LkG5NVQyKM7:TR?= MXXTRW5ITVJ?
MSTO-211H MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJwMkCwOFEh|ryP MYHTRW5ITVJ?
LS-513 M3vaVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJwMkKyOlkh|ryP MlrxV2FPT0WU
NCI-SNU-1 NGHGTZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPBSI51UUN3ME2yMlM{OjV4IN88US=> NUe1[VVMW0GQR1XS
BB65-RCC NIjYPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHze4JKSzVyPUKuN|c1QTNizszN MmLSV2FPT0WU
GT3TKB MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrvdmZKSzVyPUKuN|k6PzJizszN NVPoTplWW0GQR1XS
OS-RC-2 NYrHSm1HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;5TWM2OD1{LkSyN|QyKM7:TR?= M2PsWHNCVkeHUh?=
NCI-H2126 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XhbGlEPTB;Mj60N|Y4PCEQvF2= MW\TRW5ITVJ?
SK-UT-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i4PGlEPTB;Mj60O|Q3PyEQvF2= NXWxPJFuW0GQR1XS
DMS-114 M1PvS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJwNkG1NlQh|ryP MYfTRW5ITVJ?
ONS-76 Mnz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH6wTG1KSzVyPUKuOlM3PDFizszN MYjTRW5ITVJ?
8-MG-BA MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LnPGlEPTB;Mj62OVQyPCEQvF2= MmriV2FPT0WU
BOKU NWPHUIhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLHcmpKSzVyPUKuO|I4PjRizszN NH7nWJJUSU6JRWK=
LAMA-84 NFfS[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3RW4lKSzVyPUKuO|k6OTJizszN MYHTRW5ITVJ?
ES1 NWiwfVc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fQ[mlEPTB;Mj64NVgxPCEQvF2= MYTTRW5ITVJ?
NCI-H1395 NVezR3A2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmKyTWM2OD1{LkiyNFEzKM7:TR?= NX7vc4RIW0GQR1XS
A388 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TWOGlEPTB;Mj65OlE4KM7:TR?= MV\TRW5ITVJ?
NCCIT M1HyOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFO0OFhKSzVyPUOuNFg5PjJizszN MWXTRW5ITVJ?
HD-MY-Z MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHO5N2lKSzVyPUOuNVMzODNizszN MUnTRW5ITVJ?
NCI-H510A MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:4RmlEPTB;Mz6xPFk1OyEQvF2= Ml7SV2FPT0WU
NCI-N87 Mlv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTNwMkCwNkDPxE1? MWjTRW5ITVJ?
SCLC-21H MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XWZ2lEPTB;Mz6yOlg2QSEQvF2= NFm5R2tUSU6JRWK=
SH-4 M{nPXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXPTWM2OD1|LkK4O|k4KM7:TR?= NVjkT49MW0GQR1XS
QIMR-WIL Mnq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjkdoRKSzVyPUOuN|I5PDlizszN NELK[pNUSU6JRWK=
KM12 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTNwM{O1OFQh|ryP NVTZfW16W0GQR1XS
ST486 NGfvSnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HLc2lEPTB;Mz61N|g5OyEQvF2= M1\pcnNCVkeHUh?=
HC-1 NVvOTZZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETiNnlKSzVyPUOuOlIxOjhizszN MnHJV2FPT0WU
BV-173 M1j6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[1Z2tPUUN3ME2zMlY1ODh6IN88US=> M{P6PHNCVkeHUh?=
EW-24 NUS2ZY5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fyUGlEPTB;Mz62OlQ{PCEQvF2= MVHTRW5ITVJ?
LU-65 NYS3R3lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfnTWM2OD1|Lk[4O|Eh|ryP Mlu1V2FPT0WU
ECC4 M17IXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXOTWM2OD1|Lke3OVYh|ryP NIXBNY1USU6JRWK=
ARH-77 NWfhPIVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PYTWlEPTB;ND6xNVA3PyEQvF2= MlPOV2FPT0WU
BC-3 MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XKcmlEPTB;ND6xN|A3QCEQvF2= MVjTRW5ITVJ?
SNB75 NHH2cmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NESzPYFKSzVyPUSuNlYyQSEQvF2= NH;LbYpUSU6JRWK=
MEG-01 NHfNUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrRRXRKSzVyPUSuNlc1OTlizszN NUPhWVF5W0GQR1XS
NCI-H1417 M{PVWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTRwMki0OFMh|ryP MmqyV2FPT0WU
MDA-MB-134-VI Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHnXXlKSzVyPUSuN|A3ODFizszN NEDLeW1USU6JRWK=
Becker M1m4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTXS3hsUUN3ME20MlQ4OzN4IN88US=> MmHNV2FPT0WU
DMS-153 M4PYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLrTWM2OD12Lk[2OFc2KM7:TR?= MoXmV2FPT0WU
TGBC1TKB M{WwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\SXlFKSzVyPUSuOlg2OTVizszN MnzCV2FPT0WU
EW-3 M1fTZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{npfGlEPTB;ND63OlI1QCEQvF2= MnjDV2FPT0WU
KE-37 M3;KWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTRwOE[xPVYh|ryP NEHRcYhUSU6JRWK=
NCI-H23 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPWW2VnUUN3ME20Mlg4OjJ5IN88US=> M3LzXnNCVkeHUh?=
MC116 MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPKfXlKSzVyPUSuPVQyOjZizszN Mn;TV2FPT0WU
NH-12 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DNSmlEPTB;ND65OlQ{QSEQvF2= NY\qdIdIW0GQR1XS
CTB-1 NWDtbnhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i4d2lEPTB;ND65O|czOSEQvF2= MUTTRW5ITVJ?
KM-H2 NHvrPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fXWmlEPTB;NT6wOVMzOyEQvF2= MYnTRW5ITVJ?
MOLT-4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTwRYZKSzVyPUWuNVE5OyEQvF2= MX3TRW5ITVJ?
NCI-H2141 NGK5NJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HsXmlEPTB;NT6xOFI3QCEQvF2= MkXNV2FPT0WU
EB-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTVwMUe1NFQh|ryP NYH0TXdrW0GQR1XS
NCI-H1522 NVHN[HY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoexTWM2OD13LkK2N|IzKM7:TR?= M2rUVHNCVkeHUh?=
MRK-nu-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\pVWlEPTB;NT60N|Y{OyEQvF2= MXvTRW5ITVJ?
no-11 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHzTWM2OD13LkS3NFg4KM7:TR?= NXjm[pR6W0GQR1XS
CESS M4ewS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LwPWlEPTB;NT61PFA{PCEQvF2= MmewV2FPT0WU
KMOE-2 NFnSbHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPpN5RKSzVyPUWuOVg3PTlizszN NUDhOmtFW0GQR1XS
REH M2TzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4qyRWlEPTB;Nj6yOVYyQCEQvF2= NF:yTGpUSU6JRWK=
KU812 M3jWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\WTWM2OD14LkSyO|kyKM7:TR?= Ml\TV2FPT0WU
SK-N-FI NXG4WWc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:5b2lEPTB;Nj62NFY4PCEQvF2= NFS5TFlUSU6JRWK=
MMAC-SF NHHocJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTdwME[0PVIh|ryP NX3YcI03W0GQR1XS
RCC10RGB NX7BTZc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XaTmlEPTB;Nz6yNlk4PyEQvF2= M{TBNXNCVkeHUh?=
NCI-H322M M3jBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nR[WlEPTB;Nz6zN|M{PSEQvF2= MnXkV2FPT0WU
NB6 M1HDS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzoTWM2OD15LkW0PFk6KM7:TR?= NILK[m9USU6JRWK=
MN-60 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTdwNkmyNVUh|ryP NXvVepBYW0GQR1XS
NCI-H1092 MkjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRThwMEG3N|Qh|ryP MoXUV2FPT0WU
EKVX M{P3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRThwNEewOlYh|ryP M4rodXNCVkeHUh?=
D-263MG M1myWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HHUWlEPTB;OD61OVM6PiEQvF2= MWPTRW5ITVJ?
NCI-H209 NEPFbpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[yTWM2OD16Lk[0NFA3KM7:TR?= MV\TRW5ITVJ?
IST-SL1 NW\qdnZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[5cmVMUUN3ME24Mlg6QDl{IN88US=> M3TsNXNCVkeHUh?=
ACN NXzSblAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTlwMUmxOVch|ryP MlOzV2FPT0WU
MHH-PREB-1 M2roT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHQTWM2OD17LkKxNlE6KM7:TR?= NHzPVmRUSU6JRWK=
EW-11 NFPVbG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ywUWlEPTB;OT62OVM6PiEQvF2= MkC1V2FPT0WU
KASUMI-1 NVfUcGVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTlwN{i3O{DPxE1? Mn3YV2FPT0WU
KINGS-1 NWfDeGl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH3bpZKSzVyPUGwMlI{PDdizszN MnTaV2FPT0WU
EVSA-T NIfTTmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFyLkOxPVIh|ryP NVTRfYg5W0GQR1XS
DSH1 NWq4cm1ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLmfnNvUUN3ME2xNE4{QTd{IN88US=> MVrTRW5ITVJ?
COLO-824 Mo\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TyXWlEPTB;MUCuPFY3QSEQvF2= M1PycXNCVkeHUh?=
K052 M{DhXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\lZ|ZKSzVyPUGwMlk{OjJizszN MnzuV2FPT0WU
SK-MEL-2 M1XEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDpXmNKSzVyPUGwMlk6OzlizszN Mn\HV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
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
Western blot
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.

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. 

25351743 22240786
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.
  • Formulation: Resuspended in 10% 1-methyl-2-pyrrolidinone/90% polyethylene glycol 300 solution
  • 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

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 MSDS / 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
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / 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):
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    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