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 38 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 MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLSTWM2OD1yLkCwNFA3ODNizszN NF;qd|lUSU6JRWK=
SF539 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[zTpdSUUN3ME2wMlAxODV4NDFOwG0> MULTRW5ITVJ?
DEL NHvsd4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D3bGlEPTB;MD6wNFA6OjdizszN NIfhNIdUSU6JRWK=
NB1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTBwMECxOlIh|ryP NI\UZWlUSU6JRWK=
SR MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELleFNKSzVyPUCuNFAzPzdizszN NIju[JJUSU6JRWK=
KARPAS-299 NYT4UllUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHaephGUUN3ME2wMlAzOzh2IN88US=> M2PUeXNCVkeHUh?=
MHH-CALL-2 M4Ttc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG4PWNKSzVyPUCuNFI6PTJizszN NXLkVYZ4W0GQR1XS
SU-DHL-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDOcG5KSzVyPUCuNFQ5PjVizszN M3jiW3NCVkeHUh?=
A4-Fuk NH\PW29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX0TWM2OD1yLkC1OVY2KM7:TR?= MVfTRW5ITVJ?
EW-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\tWHdLUUN3ME2wMlExOjV4IN88US=> NYPkWG1pW0GQR1XS
NOS-1 M4\pRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vjWGlEPTB;MD6xNFI6PCEQvF2= MlTlV2FPT0WU
EW-16 M3XL[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1e4e2lEPTB;MD6xNFU3QCEQvF2= MojVV2FPT0WU
TE-11 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwMU[wPVYh|ryP Mor2V2FPT0WU
SW982 NXq3e2J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz1TWM2OD1yLkG2OFc5KM7:TR?= MYXTRW5ITVJ?
LAN-6 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjKTWM2OD1yLkG3OFQ{KM7:TR?= NIP0b5lUSU6JRWK=
MZ1-PC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHTbFM3UUN3ME2wMlE4QDN3IN88US=> M4jvdHNCVkeHUh?=
KS-1 NYS1RpN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwMUmzOFMh|ryP M4LTfHNCVkeHUh?=
PSN1 M{faWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfDTWM2OD1yLkG5OlMyKM7:TR?= MnXVV2FPT0WU
LC-2-ad M2Dl[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwMUm2PVIh|ryP MX3TRW5ITVJ?
COLO-320-HSR NVTnUJZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwMUm3O|Yh|ryP NHfUR2lUSU6JRWK=
OPM-2 NF;peZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvHOmx4UUN3ME2wMlIzPjZ7IN88US=> NVTnOlJnW0GQR1XS
SK-NEP-1 NETzfWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TNbWlEPTB;MD6yN|UzPCEQvF2= NVGwS4ZyW0GQR1XS
ALL-PO NX\NWYRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwMkS1NlQh|ryP NYjVfndLW0GQR1XS
CMK NYP0UmxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUe2fHQ4UUN3ME2wMlI2PTNizszN M{HhNXNCVkeHUh?=
NCI-H1648 NFHSTZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS4TWM2OD1yLkK3PFU2KM7:TR?= MYTTRW5ITVJ?
SIG-M5 NFXsUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwMkmxOVkh|ryP NIHUR5NUSU6JRWK=
TGBC24TKB NYP4T2lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PJbGlEPTB;MD6zNFIyQCEQvF2= NFrSTW9USU6JRWK=
DOHH-2 NVThTo4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF75RY9KSzVyPUCuN|EzODRizszN M4OyT3NCVkeHUh?=
NB69 M1;lU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTMdm9oUUN3ME2wMlMyPzh5IN88US=> Ml;yV2FPT0WU
MFH-ino NXXkSVJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwM{K1NlMh|ryP NWrvRpZ[W0GQR1XS
KP-N-RT-BM-1 M1rTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlniTWM2OD1yLkOzNVI{KM7:TR?= MUTTRW5ITVJ?
MONO-MAC-6 NELuXW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwM{OyPVEh|ryP NUPtb|ZVW0GQR1XS
ATN-1 NGT6dmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nTUWlEPTB;MD6zN|MxOyEQvF2= MX3TRW5ITVJ?
NTERA-S-cl-D1 M{LGZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXxTWM2OD1yLkOzN|k3KM7:TR?= M1L2VnNCVkeHUh?=
L-540 NYjCZWN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX6xVGFXUUN3ME2wMlM3QTh6IN88US=> MYXTRW5ITVJ?
GB-1 NG[zdnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vTN2lEPTB;MD6zPFg3PyEQvF2= MWHTRW5ITVJ?
MV-4-11 M2rwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTVTWM2OD1yLkO5OFQ3KM7:TR?= MonWV2FPT0WU
KG-1 M2TEZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjJTWM2OD1yLkO5OVYyKM7:TR?= MoXEV2FPT0WU
OVCAR-4 MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn3bmptUUN3ME2wMlQxPTZ7IN88US=> NV;0VmVTW0GQR1XS
NEC8 NYPuTotFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:xSmZ7UUN3ME2wMlQyOjl{IN88US=> MWHTRW5ITVJ?
SK-MM-2 MnywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XJ[2lEPTB;MD60NVYxQSEQvF2= Mn7ZV2FPT0WU
TE-8 M3;1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXMTWM2OD1yLkSyPFgh|ryP NIfhRYpUSU6JRWK=
697 M4D1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm4OJoyUUN3ME2wMlQ{OjF3IN88US=> NETwTI9USU6JRWK=
NB14 NGTsPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHvTWM2OD1yLkSzPFI3KM7:TR?= M4C0dXNCVkeHUh?=
GDM-1 NI\qVopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL2cFFGUUN3ME2wMlQ4OTF4IN88US=> NGDJcnpUSU6JRWK=
HUTU-80 NFHuWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILJWWpKSzVyPUCuOFc{PzVizszN M3PM[3NCVkeHUh?=
HL-60 MlKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPSTWM2OD1yLkS4NVQzKM7:TR?= M4Hye3NCVkeHUh?=
OCI-AML2 NIH0[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwNEizNlgh|ryP MYjTRW5ITVJ?
ML-2 NEHteY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHkWIUzUUN3ME2wMlQ6ODNzIN88US=> MojIV2FPT0WU
ES4 M3nRZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[4[WlEPTB;MD60PVExQSEQvF2= M13QPXNCVkeHUh?=
NCI-H747 NXSzVJhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHlTWM2OD1yLkS5PFkh|ryP Mnr3V2FPT0WU
RL95-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXaWodoUUN3ME2wMlUxOTF{IN88US=> M2HX[HNCVkeHUh?=
TE-15 NELERppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzifJFnUUN3ME2wMlUyOTJ2IN88US=> M3PRPHNCVkeHUh?=
TE-12 NXLCdIJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmK4TWM2OD1yLkWzN|Q6KM7:TR?= MnuyV2FPT0WU
LB1047-RCC MkXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrNd49SUUN3ME2wMlU1PTR7IN88US=> NVL1d4FWW0GQR1XS
LB831-BLC NXflVFFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDoZ5dKSzVyPUCuOVUxOjNizszN MnPEV2FPT0WU
NCI-H1355 NF76WGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjVTHlKUUN3ME2wMlU2OTh2IN88US=> MnnkV2FPT0WU
CTV-1 NUTlNI9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwNUW2NlQh|ryP MljSV2FPT0WU
RXF393 M4PYemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrlbXdkUUN3ME2wMlU2Pzl2IN88US=> MnS5V2FPT0WU
SW872 NXzGc5VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXDTWM2OD1yLkW2O|I1KM7:TR?= MlrlV2FPT0WU
MPP-89 NYDuO2JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O5UGlEPTB;MD61O|g5PCEQvF2= M{LRO3NCVkeHUh?=
RPMI-8226 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrsTWM2OD1yLk[zOVI3KM7:TR?= MkHEV2FPT0WU
LS-1034 NVPMNJhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rXU2lEPTB;MD62N|U5KM7:TR?= NV3WV|ZSW0GQR1XS
SJSA-1 NEDVNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDLbXI5UUN3ME2wMlY{PzJ3IN88US=> M2K4ZXNCVkeHUh?=
HOP-62 M4qx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\LTWM2OD1yLk[1NFM{KM7:TR?= NInpV|NUSU6JRWK=
KGN M3PTeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\JWlVKSzVyPUCuOlYyPjhizszN NV76d4pvW0GQR1XS
D-336MG NHrxW41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHld|E1UUN3ME2wMlY3OTZ7IN88US=> MoXSV2FPT0WU
LS-411N Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjVTWM2OD1yLk[3OFYzKM7:TR?= M2PuWnNCVkeHUh?=
TE-1 NYTl[oVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnuTWM2OD1yLk[5NFc1KM7:TR?= NEHSd3FUSU6JRWK=
LB996-RCC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwNkmzPFkh|ryP NIflSnpUSU6JRWK=
TE-10 NXHuTWROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwN{G0PVYh|ryP NX7acFNyW0GQR1XS
NCI-SNU-16 NET5U2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOxTWM2OD1yLkeyOlY1KM7:TR?= NHO2[mdUSU6JRWK=
ES8 M4DOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S2TmlEPTB;MD63OFk4PSEQvF2= MnrWV2FPT0WU
COLO-800 NWC2VlEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF6xZ3NKSzVyPUCuO|Y3QTVizszN NYK1d5poW0GQR1XS
ES6 M333Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLGTWM2OD1yLke3OVU6KM7:TR?= NWLPR21XW0GQR1XS
L-363 Mn;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwOEKzO|Uh|ryP MkLlV2FPT0WU
NMC-G1 M1\rSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3NNXlOUUN3ME2wMlg{OjN|IN88US=> MV7TRW5ITVJ?
LU-134-A NE\rUotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXOzeWhbUUN3ME2wMlg{QTF{IN88US=> NVjybnN3W0GQR1XS
SF268 M1rTdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXWTWM2OD1yLki0NFQzKM7:TR?= MVPTRW5ITVJ?
KARPAS-45 MojFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;LUm9KSzVyPUCuPFQzPjNizszN NVLWWVI{W0GQR1XS
TGW NWrUUmo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELPd2JKSzVyPUCuPFU5PjNizszN M3SyRnNCVkeHUh?=
CHP-126 NWH0SXFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwOEW5OVch|ryP MonZV2FPT0WU
MOLT-16 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj0TWM2OD1yLki3OVg6KM7:TR?= NITMVIJUSU6JRWK=
LB771-HNC NVjjbmlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzJOZdIUUN3ME2wMlg6PzV5IN88US=> M4niVHNCVkeHUh?=
NALM-6 M2G1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[yUWlEPTB;MD65NFc{QSEQvF2= NID4bVhUSU6JRWK=
GCIY Ml7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwOUW1NlYh|ryP MmDkV2FPT0WU
IST-MES1 M3voTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mke0TWM2OD1yLkm4PFI1KM7:TR?= Mo\LV2FPT0WU
LB2241-RCC MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DOfmlEPTB;MD65PFg1KM7:TR?= MYHTRW5ITVJ?
BL-70 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPUe3ZYUUN3ME2wMlk6PTN3IN88US=> M2jl[XNCVkeHUh?=
NB17 MnXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;CZWlEPTB;MT6wNFY{QSEQvF2= M1rBN3NCVkeHUh?=
LXF-289 M2i3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HvWGlEPTB;MT6wN|A4PiEQvF2= MnO3V2FPT0WU
TK10 M2L2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTFwMEWwOlMh|ryP NWfRfWRmW0GQR1XS
K5 M{jrVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\XPHR2UUN3ME2xMlA3Ojd2IN88US=> M1;wOHNCVkeHUh?=
NCI-H716 NI\wcXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjmTWM2OD1zLkC3NlU6KM7:TR?= NW[xPVlbW0GQR1XS
HCE-T M1jnfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTFwMEi4NVkh|ryP MWPTRW5ITVJ?
GI-1 M3OzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PwcWlEPTB;MT6wPVc6QCEQvF2= M{\NV3NCVkeHUh?=
KARPAS-422 MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jrSWlEPTB;MT6xNFAzOiEQvF2= NVrRd2xDW0GQR1XS
TE-9 NHfucmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW2TWM2OD1zLkGxN|I5KM7:TR?= MUfTRW5ITVJ?
SF126 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzMdZROUUN3ME2xMlEyPTZ6IN88US=> NYrQRpNpW0GQR1XS
BB30-HNC NIjPb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYexNldxUUN3ME2xMlE{OTF{IN88US=> NX7qOllLW0GQR1XS
NCI-H1304 M4HyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnQc|ZKSzVyPUGuNVM{OzhizszN M3HOc3NCVkeHUh?=
HEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjITWM2OD1zLkG0PFk2KM7:TR?= NUP6[FNCW0GQR1XS
HAL-01 M4\seWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfvOXJKSzVyPUGuNVUzQDNizszN NGrUVmpUSU6JRWK=
SK-LMS-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjJTWM2OD1zLkG1PVc1KM7:TR?= NIDpdFJUSU6JRWK=
SW954 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwMUm1Olch|ryP NWLNO5JtW0GQR1XS
D-283MED NFSwNJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfKTWM2OD1zLkKyN|c6KM7:TR?= NVzPTlZvW0GQR1XS
NCI-H1882 NV7OTIg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HUfmlEPTB;MT6yN|g6KM7:TR?= NHWwWXdUSU6JRWK=
GI-ME-N MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLWTWM2OD1zLkK1NlA5KM7:TR?= MoD1V2FPT0WU
SK-PN-DW NXrXN2NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jYOmlEPTB;MT6yOlM1QCEQvF2= NXTYdWJOW0GQR1XS
C2BBe1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwMkmxNVch|ryP MULTRW5ITVJ?
A704 NIfp[mJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XIZ2lEPTB;MT6zNlY5QSEQvF2= MkPDV2FPT0WU
KALS-1 NFrIfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHiTWM2OD1zLkO0NFgh|ryP M2n6bnNCVkeHUh?=
ETK-1 NWjJb3dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjsd4xKSzVyPUGuN|Q1QDlizszN MnLGV2FPT0WU
LB647-SCLC NIDjcoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFwM{S5PFYh|ryP NXjte|JzW0GQR1XS
OCUB-M NYjkZVc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFwM{[xOFMh|ryP M1zkcHNCVkeHUh?=
NCI-H720 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3myfGlEPTB;MT6zOlM4QCEQvF2= MlKxV2FPT0WU
NB13 NUDOfWJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[xTWM2OD1zLkO3Nlk{KM7:TR?= Mon1V2FPT0WU
GR-ST MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u4[mlEPTB;MT6zPFc2PyEQvF2= M1;iNnNCVkeHUh?=
DU-4475 NYfucXB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwNEW4OVMh|ryP NEjFe|ZUSU6JRWK=
HCC2157 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH2XlR6UUN3ME2xMlQ3PjV7IN88US=> NGPFSpFUSU6JRWK=
RKO NU\BdpZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTFwNEm5NlIh|ryP NFf0ZZZUSU6JRWK=
LS-123 NUiwUoRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLWd4FKSzVyPUGuOVE2QTRizszN M2e4[nNCVkeHUh?=
NCI-H69 NXTINHBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LLS2lEPTB;MT61OVgyOSEQvF2= NG\oVpNUSU6JRWK=
SW962 NIS4VIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfBTWM2OD1zLkW2NVMh|ryP MoW2V2FPT0WU
PF-382 NYDtN2o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;ONoJKSzVyPUGuOVY6PiEQvF2= NYHXWox2W0GQR1XS
A101D NIPleHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvXOY1KSzVyPUGuOVcyOTNizszN M4C4dHNCVkeHUh?=
NB10 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfEfXJKSzVyPUGuOVc{QTJizszN MkDoV2FPT0WU
NB5 NYHidGx4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHVV2lIUUN3ME2xMlU5PDd4IN88US=> MUnTRW5ITVJ?
HCE-4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDxTWM2OD1zLk[wPFUh|ryP NUHvdHdnW0GQR1XS
HT-144 NEnvUGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fkTmlEPTB;MT62N|E6KM7:TR?= MnfiV2FPT0WU
NCI-H524 MkHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwNkSzNFch|ryP M{juXXNCVkeHUh?=
NKM-1 NUXoPYNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS0NXozUUN3ME2xMlY5PjZizszN MYrTRW5ITVJ?
KURAMOCHI MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwNkm1O|Mh|ryP MkDrV2FPT0WU
NCI-H187 NXjidWg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;4b|czUUN3ME2xMlcxODN4IN88US=> NV;0WWxIW0GQR1XS
U-266 Mk[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTFwN{O4OFIh|ryP NY\iOVdVW0GQR1XS
BL-41 NVzHcnZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3GTWM2OD1zLke2NlczKM7:TR?= Ml70V2FPT0WU
SK-N-DZ MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHq[mRHUUN3ME2xMlc5OzB7IN88US=> MlLjV2FPT0WU
Daudi M1rLb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vF[WlEPTB;MT63PFk3PyEQvF2= M17BWHNCVkeHUh?=
CPC-N NHPkbWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nsUmlEPTB;MT64OVA6PiEQvF2= NX;hPIVoW0GQR1XS
EM-2 NEeyfGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvVTWM2OD1zLki1NUDPxE1? NVv1ZohQW0GQR1XS
HCC1187 NGDPb|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7nT2dKSzVyPUGuPFYzPDFizszN MXjTRW5ITVJ?
LP-1 NWe0dXZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{exVWlEPTB;MT64O|E1OyEQvF2= MX;TRW5ITVJ?
CAS-1 Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGwbJY{UUN3ME2xMlk5Ojl7IN88US=> NWi1Vpk6W0GQR1XS
NB7 NX\zV2F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX75OI1[UUN3ME2yMlAxPTV3IN88US=> Mlf2V2FPT0WU
VA-ES-BJ M{\RN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTrSVAxUUN3ME2yMlAyPTF|IN88US=> MUHTRW5ITVJ?
SNU-C2B NF;4dZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTSbmpKSzVyPUKuNFM{PTFizszN NEm2VVVUSU6JRWK=
LOXIMVI Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPjblR7UUN3ME2yMlA3Pzh4IN88US=> MUPTRW5ITVJ?
NCI-H1581 Ml\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETrelFKSzVyPUKuNVE2PTlizszN NW\xd3UyW0GQR1XS
IST-SL2 M{jTZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fObGlEPTB;Mj6xNlQ1PSEQvF2= NIW2UpBUSU6JRWK=
NOMO-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDrW2hKSzVyPUKuNVc3QDNizszN MlHzV2FPT0WU
TE-6 NYrONXN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXXbG1KSzVyPUKuNVkxPSEQvF2= NE\4VWhUSU6JRWK=
NCI-H526 NF3BOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLabYFKSzVyPUKuNVkyPDFizszN MVTTRW5ITVJ?
MSTO-211H M2fud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;hV2lEPTB;Mj6yNFA1OSEQvF2= MnTPV2FPT0WU
LS-513 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJwMkKyOlkh|ryP NGewfJhUSU6JRWK=
NCI-SNU-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjQSW93UUN3ME2yMlM{OjV4IN88US=> NXvycWE{W0GQR1XS
BB65-RCC NIrzUXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPmV5BKSzVyPUKuN|c1QTNizszN M4\VZ3NCVkeHUh?=
GT3TKB MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT0cnRKSzVyPUKuN|k6PzJizszN NULzSlhJW0GQR1XS
OS-RC-2 NFXkVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGi1U3JKSzVyPUKuOFI{PDFizszN MWnTRW5ITVJ?
NCI-H2126 NGjjXJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImzdXZKSzVyPUKuOFM3PzRizszN MlfiV2FPT0WU
SK-UT-1 NXHxeFRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq3TWM2OD1{LkS3OFY4KM7:TR?= M3;TVHNCVkeHUh?=
DMS-114 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nVTGlEPTB;Mj62NVUzPCEQvF2= M3;YZXNCVkeHUh?=
ONS-76 NXjsSFJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJwNkO2OFEh|ryP MkjIV2FPT0WU
8-MG-BA MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTNVnREUUN3ME2yMlY2PDF2IN88US=> MVLTRW5ITVJ?
BOKU M13IdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnEPGVKSzVyPUKuO|I4PjRizszN Ml21V2FPT0WU
LAMA-84 M3zEeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJwN{m5NVIh|ryP NFT2eWJUSU6JRWK=
ES1 MmH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPTOZpwUUN3ME2yMlgyQDB2IN88US=> NHv2WJVUSU6JRWK=
NCI-H1395 NFHvW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJwOEKwNVIh|ryP MULTRW5ITVJ?
A388 Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFGw[I1KSzVyPUKuPVYyPyEQvF2= NFHGU45USU6JRWK=
NCCIT MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DMR2lEPTB;Mz6wPFg3OiEQvF2= NYTNTms5W0GQR1XS
HD-MY-Z MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ezRmlEPTB;Mz6xN|IxOyEQvF2= M4rwZnNCVkeHUh?=
NCI-H510A NFXqTlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNwMUi5OFMh|ryP NIL5WVJUSU6JRWK=
NCI-N87 M3zzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PXXWlEPTB;Mz6yNFAzKM7:TR?= M3;VZ3NCVkeHUh?=
SCLC-21H NVL0Z3U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3KRYp5UUN3ME2zMlI3QDV7IN88US=> MVnTRW5ITVJ?
SH-4 M3TBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYriUWZqUUN3ME2zMlI5Pzl5IN88US=> MYLTRW5ITVJ?
QIMR-WIL M3Hj[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jqcGlEPTB;Mz6zNlg1QSEQvF2= M4fVXnNCVkeHUh?=
KM12 M2HaT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XXSGlEPTB;Mz6zN|U1PCEQvF2= MXfTRW5ITVJ?
ST486 NVrMfnppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTNwNUO4PFMh|ryP Mnz0V2FPT0WU
HC-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXMXlJwUUN3ME2zMlYzODJ6IN88US=> NX;tRmtlW0GQR1XS
BV-173 NVz5XmhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1uxb2lEPTB;Mz62OFA5QCEQvF2= MUDTRW5ITVJ?
EW-24 NFjFNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjsTWM2OD1|Lk[2OFM1KM7:TR?= MXLTRW5ITVJ?
LU-65 NU\5fXI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[5TWM2OD1|Lk[4O|Eh|ryP NFTDbHBUSU6JRWK=
ECC4 M1fWcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP6SFRKSzVyPUOuO|c2PiEQvF2= M4PwcHNCVkeHUh?=
ARH-77 MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUn3Upp2UUN3ME20MlEyODZ5IN88US=> Mnz1V2FPT0WU
BC-3 MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrOT|lKSzVyPUSuNVMxPjhizszN NUfGUXBHW0GQR1XS
SNB75 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTRwMk[xPUDPxE1? NYLuSohEW0GQR1XS
MEG-01 M2XT[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTRwMke0NVkh|ryP NX3CblB{W0GQR1XS
NCI-H1417 NETLTpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTRwMki0OFMh|ryP MkPXV2FPT0WU
MDA-MB-134-VI NF3jT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHUcI41UUN3ME20MlMxPjBzIN88US=> NWfSZWdVW0GQR1XS
Becker NVfscHpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zGdGlEPTB;ND60O|M{PiEQvF2= NU\NW|I1W0GQR1XS
DMS-153 MoL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrzTYdKSzVyPUSuOlY1PzVizszN NGexSpFUSU6JRWK=
TGBC1TKB MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTRwNki1NVUh|ryP M37zTHNCVkeHUh?=
EW-3 NELlenBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXh[GJKSzVyPUSuO|YzPDhizszN NVvmXplDW0GQR1XS
KE-37 MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof4TWM2OD12Lki2NVk3KM7:TR?= MkHWV2FPT0WU
NCI-H23 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPt[nhxUUN3ME20Mlg4OjJ5IN88US=> MW\TRW5ITVJ?
MC116 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Lvd2lEPTB;ND65OFEzPiEQvF2= NV[yc2oxW0GQR1XS
NH-12 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C0[GlEPTB;ND65OlQ{QSEQvF2= M4\QSHNCVkeHUh?=
CTB-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFX1[5NKSzVyPUSuPVc4OjFizszN NFzkW3lUSU6JRWK=
KM-H2 NY[ySXRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7OTFRKSzVyPUWuNFU{OjNizszN Ml;2V2FPT0WU
MOLT-4 NE\VS21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXPWW5KSzVyPUWuNVE5OyEQvF2= MnW0V2FPT0WU
NCI-H2141 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnLNpRKSzVyPUWuNVQzPjhizszN Mn;uV2FPT0WU
EB-3 NYr2SYtZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zibWlEPTB;NT6xO|UxPCEQvF2= NY\ubpd{W0GQR1XS
NCI-H1522 NHnqbWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULlRZJwUUN3ME21MlI3OzJ{IN88US=> M{DhRXNCVkeHUh?=
MRK-nu-1 NXjDN|U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfaPJBpUUN3ME21MlQ{PjN|IN88US=> MnzoV2FPT0WU
no-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHNXYJKSzVyPUWuOFcxQDdizszN MlrjV2FPT0WU
CESS NETqfHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHlenpKSzVyPUWuOVgxOzRizszN M4riZ3NCVkeHUh?=
KMOE-2 M{LFO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj6U4JvUUN3ME21MlU5PjV7IN88US=> M3vBN3NCVkeHUh?=
REH MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTZwMkW2NVgh|ryP NITOXIpUSU6JRWK=
KU812 NHLROG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTZwNEK3PVEh|ryP NHm0e5lUSU6JRWK=
SK-N-FI M3zB[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvHc4FKSzVyPU[uOlA3PzRizszN MnHNV2FPT0WU
MMAC-SF MoCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTDeFVLUUN3ME23MlA3PDl{IN88US=> MnnlV2FPT0WU
RCC10RGB NEHFOlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HQZWlEPTB;Nz6yNlk4PyEQvF2= NEPwSJpUSU6JRWK=
NCI-H322M M4qx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y5NmlEPTB;Nz6zN|M{PSEQvF2= MlHQV2FPT0WU
NB6 M{HpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr5TWM2OD15LkW0PFk6KM7:TR?= MWrTRW5ITVJ?
MN-60 NULyXlhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDpUGhWUUN3ME23MlY6OjF3IN88US=> M3XHWXNCVkeHUh?=
NCI-H1092 M2jYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDUN|FTUUN3ME24MlAyPzN2IN88US=> MnzuV2FPT0WU
EKVX MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRThwNEewOlYh|ryP NV;rO3FlW0GQR1XS
D-263MG NEHGPXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRThwNUWzPVYh|ryP MUXTRW5ITVJ?
NCI-H209 NXfJeGN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvsTWM2OD16Lk[0NFA3KM7:TR?= MojwV2FPT0WU
IST-SL1 NFfhdWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7mWG1KSzVyPUiuPFk5QTJizszN MYrTRW5ITVJ?
ACN NYnkO4VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S4UWlEPTB;OT6xPVE2PyEQvF2= Mm[5V2FPT0WU
MHH-PREB-1 MljiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkX4TWM2OD17LkKxNlE6KM7:TR?= MYDTRW5ITVJ?
EW-11 NVrL[pliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2NoJGUUN3ME25MlY2Ozl4IN88US=> MoTlV2FPT0WU
KASUMI-1 NGrTTIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLPZ2lOUUN3ME25Mlc5PzdizszN NGTZeYNUSU6JRWK=
KINGS-1 NGTiRWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEW1ZppKSzVyPUGwMlI{PDdizszN MlfFV2FPT0WU
EVSA-T MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnwdnlKSzVyPUGwMlMyQTJizszN MXzTRW5ITVJ?
DSH1 NYn1T3liT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\SWlBnUUN3ME2xNE4{QTd{IN88US=> MXjTRW5ITVJ?
COLO-824 NX3ES4RlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDHcW41UUN3ME2xNE45PjZ7IN88US=> NIjXT|hUSU6JRWK=
K052 NXj6XFdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFyLkmzNlIh|ryP NGe0N4dUSU6JRWK=
SK-MEL-2 NXz0SYF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;RTWM2OD1zMD65PVM6KM7:TR?= MULTRW5ITVJ?

... 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