TAE684 (NVP-TAE684)

For research use only.

Catalog No.S1108

60 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.

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Selleck's TAE684 (NVP-TAE684) has been cited by 60 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 NXrLV5RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7Fc|FKSzVyPUCuNFAxODZyMzFOwG0> NXzBUWNNW0GQR1XS
SF539 NWLIRlZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzhTWM2OD1yLkCwNFU3PCEQvF2= M4C5SXNCVkeHUh?=
DEL MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnMTWM2OD1yLkCwNFkzPyEQvF2= MUfTRW5ITVJ?
NB1 NVnlbm9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXDfFMyUUN3ME2wMlAxOTZ{IN88US=> NXnFcXhlW0GQR1XS
SR MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\4OWlEPTB;MD6wNFI4PyEQvF2= MXfTRW5ITVJ?
KARPAS-299 M2XMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMEKzPFQh|ryP NET5UZdUSU6JRWK=
MHH-CALL-2 NXn1OXBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[wcpFKSzVyPUCuNFI6PTJizszN NVvPVVdTW0GQR1XS
SU-DHL-1 NHi5dZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f0TGlEPTB;MD6wOFg3PSEQvF2= NXux[WJ1W0GQR1XS
A4-Fuk NITZbnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfFTWM2OD1yLkC1OVY2KM7:TR?= NGX5RWJUSU6JRWK=
EW-1 M4LyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjrTFZpUUN3ME2wMlExOjV4IN88US=> MnjTV2FPT0WU
NOS-1 NIXrfZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTBwMUCyPVQh|ryP MWXTRW5ITVJ?
EW-16 M3u2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHrTWM2OD1yLkGwOVY5KM7:TR?= NFXLNnhUSU6JRWK=
TE-11 M1y1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzMPGhzUUN3ME2wMlE3ODl4IN88US=> M2e1T3NCVkeHUh?=
SW982 NI[2blVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\vS|l1UUN3ME2wMlE3PDd6IN88US=> MljjV2FPT0WU
LAN-6 NFHNXW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\tNWlEPTB;MD6xO|Q1OyEQvF2= M{\PbnNCVkeHUh?=
MZ1-PC M4q1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHpeYRtUUN3ME2wMlE4QDN3IN88US=> NHi3cJhUSU6JRWK=
KS-1 M4TXcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\0N|RKSzVyPUCuNVk{PDNizszN NV24bXFxW0GQR1XS
PSN1 NEDwcJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HwNmlEPTB;MD6xPVY{OSEQvF2= NH;6[GNUSU6JRWK=
LC-2-ad MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HuUmlEPTB;MD6xPVY6OiEQvF2= M3\BeXNCVkeHUh?=
COLO-320-HSR Mlf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr6cmpNUUN3ME2wMlE6Pzd4IN88US=> NXTX[|lRW0GQR1XS
OPM-2 M1PYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3UUJZRUUN3ME2wMlIzPjZ7IN88US=> M1jr[HNCVkeHUh?=
SK-NEP-1 M2CxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwMkO1NlQh|ryP MWPTRW5ITVJ?
ALL-PO NWH5[HVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwMkS1NlQh|ryP NYPPZmpnW0GQR1XS
CMK MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDaTWM2OD1yLkK1OVMh|ryP MUjTRW5ITVJ?
NCI-H1648 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHaN|FKSzVyPUCuNlc5PTVizszN M3LOW3NCVkeHUh?=
SIG-M5 M3fOdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLoXGJnUUN3ME2wMlI6OTV7IN88US=> NXPZXI54W0GQR1XS
TGBC24TKB M{nqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3nTWM2OD1yLkOwNlE5KM7:TR?= MWXTRW5ITVJ?
DOHH-2 MoTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFK5VHBKSzVyPUCuN|EzODRizszN MVHTRW5ITVJ?
NB69 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoW0TWM2OD1yLkOxO|g4KM7:TR?= MWrTRW5ITVJ?
MFH-ino NIjSO2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwM{K1NlMh|ryP MnvXV2FPT0WU
KP-N-RT-BM-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q3b2lEPTB;MD6zN|EzOyEQvF2= MlrVV2FPT0WU
MONO-MAC-6 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG5TWM2OD1yLkOzNlkyKM7:TR?= NF31TlZUSU6JRWK=
ATN-1 Mo\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jTSmlEPTB;MD6zN|MxOyEQvF2= MmDyV2FPT0WU
NTERA-S-cl-D1 M17HSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S1NWlEPTB;MD6zN|M6PiEQvF2= MUjTRW5ITVJ?
L-540 MkLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHztSY1KSzVyPUCuN|Y6QDhizszN MkfSV2FPT0WU
GB-1 NYT6PZZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrhOI1KSzVyPUCuN|g5PjdizszN M4Hxb3NCVkeHUh?=
MV-4-11 NULQS|hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\qVmlEPTB;MD6zPVQ1PiEQvF2= MnPNV2FPT0WU
KG-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr3coNKSzVyPUCuN|k2PjFizszN M124NHNCVkeHUh?=
OVCAR-4 NXzIPJR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DTTGlEPTB;MD60NFU3QSEQvF2= MWDTRW5ITVJ?
NEC8 Mn\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fEXmlEPTB;MD60NVI6OiEQvF2= M{PhXnNCVkeHUh?=
SK-MM-2 NYDGWpJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf6cJBoUUN3ME2wMlQyPjB7IN88US=> M1fFXnNCVkeHUh?=
TE-8 M3HSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwNEK4PEDPxE1? MVLTRW5ITVJ?
697 M3\uTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwNEOyNVUh|ryP M3X0d3NCVkeHUh?=
NB14 NWOwdIlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn4WIpuUUN3ME2wMlQ{QDJ4IN88US=> M1;LcXNCVkeHUh?=
GDM-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwNEexNVYh|ryP MVvTRW5ITVJ?
HUTU-80 M4\zZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwNEezO|Uh|ryP MkKwV2FPT0WU
HL-60 M3G3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED0PGlKSzVyPUCuOFgyPDJizszN NXrQRpJ1W0GQR1XS
OCI-AML2 NWDTWY5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnHS5NKSzVyPUCuOFg{OjhizszN MX7TRW5ITVJ?
ML-2 NED4[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M131VWlEPTB;MD60PVA{OSEQvF2= MoD3V2FPT0WU
ES4 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXxTWM2OD1yLkS5NVA6KM7:TR?= MYDTRW5ITVJ?
NCI-H747 NITIXXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorRTWM2OD1yLkS5PFkh|ryP NWLlWm9RW0GQR1XS
RL95-2 M2XKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmT6TWM2OD1yLkWwNVEzKM7:TR?= Ml;DV2FPT0WU
TE-15 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTyRmx1UUN3ME2wMlUyOTJ2IN88US=> MmLrV2FPT0WU
TE-12 M4HvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfxTWM2OD1yLkWzN|Q6KM7:TR?= NFPSPWRUSU6JRWK=
LB1047-RCC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;CbnE6UUN3ME2wMlU1PTR7IN88US=> Ml7ZV2FPT0WU
LB831-BLC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwNUWwNlMh|ryP Ml3ZV2FPT0WU
NCI-H1355 NYjUbGdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjWNXFKSzVyPUCuOVUyQDRizszN M{PRNHNCVkeHUh?=
CTV-1 NF3Gc|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj1TWM2OD1yLkW1OlI1KM7:TR?= M3LQOHNCVkeHUh?=
RXF393 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFixU5VKSzVyPUCuOVU4QTRizszN M3G5OnNCVkeHUh?=
SW872 NEfUPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHX[lYyUUN3ME2wMlU3PzJ2IN88US=> M373SHNCVkeHUh?=
MPP-89 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPGOI1KSzVyPUCuOVc5QDRizszN M1Szb3NCVkeHUh?=
RPMI-8226 NW\NSXZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNkO1NlYh|ryP MojXV2FPT0WU
LS-1034 M1:2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofLTWM2OD1yLk[zOVgh|ryP NWG2NmlzW0GQR1XS
SJSA-1 MnzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljVTWM2OD1yLk[zO|I2KM7:TR?= NX[3SFBnW0GQR1XS
HOP-62 NIHBdYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHOOmJKSzVyPUCuOlUxOzNizszN Ml21V2FPT0WU
KGN NFLxOpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV63eGROUUN3ME2wMlY3OTZ6IN88US=> NG\VWVdUSU6JRWK=
D-336MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjIPFd1UUN3ME2wMlY3OTZ7IN88US=> MUfTRW5ITVJ?
LS-411N MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOzPGhKSzVyPUCuOlc1PjJizszN NXT4fmxQW0GQR1XS
TE-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwNkmwO|Qh|ryP NFX2[lVUSU6JRWK=
LB996-RCC NX70PYRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W2PWlEPTB;MD62PVM5QSEQvF2= M4HicXNCVkeHUh?=
TE-10 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDPO|FrUUN3ME2wMlcyPDl4IN88US=> MVvTRW5ITVJ?
NCI-SNU-16 NWfKflU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL6fGlKSzVyPUCuO|I3PjRizszN NVHVflI4W0GQR1XS
ES8 NWH5[IpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXLV3JKSzVyPUCuO|Q6PzVizszN MX;TRW5ITVJ?
COLO-800 NHzQfG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPzTWM2OD1yLke2Olk2KM7:TR?= NY\DT5V7W0GQR1XS
ES6 M1H0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwN{e1OVkh|ryP NHvLPVhUSU6JRWK=
L-363 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTBwOEKzO|Uh|ryP NXPGemhnW0GQR1XS
NMC-G1 NGDVeYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwOEOyN|Mh|ryP M{CwTXNCVkeHUh?=
LU-134-A NXXzPJVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nZdGlEPTB;MD64N|kyOiEQvF2= MUfTRW5ITVJ?
SF268 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfPT41KSzVyPUCuPFQxPDJizszN MXvTRW5ITVJ?
KARPAS-45 MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXNTWM2OD1yLki0NlY{KM7:TR?= MUfTRW5ITVJ?
TGW M{TZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrXRpRKSzVyPUCuPFU5PjNizszN M3\pT3NCVkeHUh?=
CHP-126 NXLRS2d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwOEW5OVch|ryP NF3DOJBUSU6JRWK=
MOLT-16 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPZTWM2OD1yLki3OVg6KM7:TR?= Mon6V2FPT0WU
LB771-HNC NWTPeFkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq5TWM2OD1yLki5O|U4KM7:TR?= M3G4d3NCVkeHUh?=
NALM-6 NX;GU2N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfrZmJvUUN3ME2wMlkxPzN7IN88US=> NIjmcYZUSU6JRWK=
GCIY NHXHSnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwOUW1NlYh|ryP NUXlXFVKW0GQR1XS
IST-MES1 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfvO3R7UUN3ME2wMlk5QDJ2IN88US=> NYP6c2VQW0GQR1XS
LB2241-RCC MkXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjBTWM2OD1yLkm4PFQh|ryP MVzTRW5ITVJ?
BL-70 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPOd49KSzVyPUCuPVk2OzVizszN Mm\RV2FPT0WU
NB17 NW\hOVVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjt[Wo4UUN3ME2xMlAxPjN7IN88US=> NVnMc4FkW0GQR1XS
LXF-289 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:xRoN7UUN3ME2xMlA{ODd4IN88US=> NWTSUY1yW0GQR1XS
TK10 MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\4TWM2OD1zLkC1NFY{KM7:TR?= MYLTRW5ITVJ?
K5 MojnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLVTWM2OD1zLkC2Nlc1KM7:TR?= MkjjV2FPT0WU
NCI-H716 M2Hw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrpOoJtUUN3ME2xMlA4OjV7IN88US=> MlXXV2FPT0WU
HCE-T MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwMEi4NVkh|ryP MX;TRW5ITVJ?
GI-1 M4XGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz3TWM2OD1zLkC5O|k5KM7:TR?= M1vPcXNCVkeHUh?=
KARPAS-422 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofITWM2OD1zLkGwNFIzKM7:TR?= NXjzOItCW0GQR1XS
TE-9 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwMUGzNlgh|ryP M3\scXNCVkeHUh?=
SF126 NIrkPWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDjTWM2OD1zLkGxOVY5KM7:TR?= NEPsRWVUSU6JRWK=
BB30-HNC MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[3eWlEPTB;MT6xN|EyOiEQvF2= M3KwOXNCVkeHUh?=
NCI-H1304 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nNb2lEPTB;MT6xN|M{QCEQvF2= NFm5NWpUSU6JRWK=
HEL NVX1SFZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULCb4RNUUN3ME2xMlE1QDl3IN88US=> MlH0V2FPT0WU
HAL-01 MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULXRpA{UUN3ME2xMlE2Ojh|IN88US=> NY\zT5lsW0GQR1XS
SK-LMS-1 M2W1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwMUW5O|Qh|ryP NXLyOIFkW0GQR1XS
SW954 NFvhdFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUWzUGNMUUN3ME2xMlE6PTZ5IN88US=> NGDT[IRUSU6JRWK=
D-283MED M4fBb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrNTWM2OD1zLkKyN|c6KM7:TR?= M4jZOnNCVkeHUh?=
NCI-H1882 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\6fWlEPTB;MT6yN|g6KM7:TR?= MXLTRW5ITVJ?
GI-ME-N NWXTbnVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFwMkWyNFgh|ryP MkXkV2FPT0WU
SK-PN-DW MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC0W|N{UUN3ME2xMlI3OzR6IN88US=> NWrJZndoW0GQR1XS
C2BBe1 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fyOGlEPTB;MT6yPVEyPyEQvF2= NH;2PIRUSU6JRWK=
A704 NEfZT5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HuOGlEPTB;MT6zNlY5QSEQvF2= NEPTNoZUSU6JRWK=
KALS-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFwM{SwPEDPxE1? Mn75V2FPT0WU
ETK-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnGWm9wUUN3ME2xMlM1PDh7IN88US=> NVvI[pNrW0GQR1XS
LB647-SCLC NV3oNGhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPOR5d3UUN3ME2xMlM1QTh4IN88US=> M1TuWXNCVkeHUh?=
OCUB-M NIfQbXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\oZ2lEPTB;MT6zOlE1OyEQvF2= MX3TRW5ITVJ?
NCI-H720 NELaOoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwM{[zO|gh|ryP M3HqT3NCVkeHUh?=
NB13 M2fNXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTFwM{eyPVMh|ryP MnrjV2FPT0WU
GR-ST MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3Y[mhPUUN3ME2xMlM5PzV5IN88US=> MXPTRW5ITVJ?
DU-4475 NIrJZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fxVWlEPTB;MT60OVg2OyEQvF2= NGrzOG5USU6JRWK=
HCC2157 M2e2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTFwNE[2OVkh|ryP MmjRV2FPT0WU
RKO NV;4N4dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHhXHNVUUN3ME2xMlQ6QTJ{IN88US=> NXy3XpRQW0GQR1XS
LS-123 M4q4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;tNpFKSzVyPUGuOVE2QTRizszN MmWyV2FPT0WU
NCI-H69 Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWH0SYY5UUN3ME2xMlU2QDFzIN88US=> NITJR|JUSU6JRWK=
SW962 NHHGVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXf5[3Y2UUN3ME2xMlU3OTNizszN MUPTRW5ITVJ?
PF-382 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonnTWM2OD1zLkW2PVYh|ryP NG\0WIJUSU6JRWK=
A101D NIXNNoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTOW|h4UUN3ME2xMlU4OTF|IN88US=> MYLTRW5ITVJ?
NB10 M4DLU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G2NGlEPTB;MT61O|M6OiEQvF2= MnrkV2FPT0WU
NB5 Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwNUi0O|Yh|ryP MofNV2FPT0WU
HCE-4 M2X2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvGTWM2OD1zLk[wPFUh|ryP MVnTRW5ITVJ?
HT-144 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\4TWM2OD1zLk[zNVkh|ryP MoL1V2FPT0WU
NCI-H524 NHnlXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLlTWM2OD1zLk[0N|A4KM7:TR?= NFvQOIJUSU6JRWK=
NKM-1 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwNki2OkDPxE1? Mm[zV2FPT0WU
KURAMOCHI NHzNXm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XtRWlEPTB;MT62PVU4OyEQvF2= M3PWXHNCVkeHUh?=
NCI-H187 NICzPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP3PGJYUUN3ME2xMlcxODN4IN88US=> M3HaPXNCVkeHUh?=
U-266 NHXqbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfyNFhEUUN3ME2xMlc{QDR{IN88US=> M4DtNnNCVkeHUh?=
BL-41 NEW5[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\VcGF1UUN3ME2xMlc3Ojd{IN88US=> M33jdXNCVkeHUh?=
SK-N-DZ M3LLdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHLTWM2OD1zLke4N|A6KM7:TR?= MWjTRW5ITVJ?
Daudi NI\v[pRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHv4OG5KSzVyPUGuO|g6PjdizszN NX7UV|V[W0GQR1XS
CPC-N NYDOc|lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS3[4lJUUN3ME2xMlg2ODl4IN88US=> NWC1Vo5yW0GQR1XS
EM-2 NX20Z3NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\kUGlEPTB;MT64OVEh|ryP MmjTV2FPT0WU
HCC1187 M1PnTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\qXWU5UUN3ME2xMlg3OjRzIN88US=> MY\TRW5ITVJ?
LP-1 M1rFUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwOEexOFMh|ryP NFH6RmNUSU6JRWK=
CAS-1 NX30RVZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwOUiyPVkh|ryP M2n5O3NCVkeHUh?=
NB7 M4\VXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPYNohKSzVyPUKuNFA2PTVizszN MX7TRW5ITVJ?
VA-ES-BJ M1vaemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXYO5BKSzVyPUKuNFE2OTNizszN M1T1[XNCVkeHUh?=
SNU-C2B M3HLPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYriTIliUUN3ME2yMlA{OzVzIN88US=> M3yxTXNCVkeHUh?=
LOXIMVI M4T5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJwME[3PFYh|ryP MW\TRW5ITVJ?
NCI-H1581 M4r6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJwMUG1OVkh|ryP NXf4c3NHW0GQR1XS
IST-SL2 NHWzXVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojuTWM2OD1{LkGyOFQ2KM7:TR?= NHrKO|VUSU6JRWK=
NOMO-1 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPucVNKSzVyPUKuNVc3QDNizszN NHXHeZRUSU6JRWK=
TE-6 M4DNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki5TWM2OD1{LkG5NFUh|ryP M{fOW3NCVkeHUh?=
NCI-H526 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXew[3p3UUN3ME2yMlE6OTRzIN88US=> MmOzV2FPT0WU
MSTO-211H NYq3eHVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3vTWM2OD1{LkKwNFQyKM7:TR?= NXf3[4lpW0GQR1XS
LS-513 NXvQU5N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTEdYdKSzVyPUKuNlIzPjlizszN NWnIVpVMW0GQR1XS
NCI-SNU-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJwM{OyOVYh|ryP M37INnNCVkeHUh?=
BB65-RCC MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJwM{e0PVMh|ryP NGjuXXRUSU6JRWK=
GT3TKB MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXqTWM2OD1{LkO5PVczKM7:TR?= NF3SO2RUSU6JRWK=
OS-RC-2 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLVeYdLUUN3ME2yMlQzOzRzIN88US=> MlWwV2FPT0WU
NCI-H2126 M17aW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LxbmlEPTB;Mj60N|Y4PCEQvF2= NI\GOmZUSU6JRWK=
SK-UT-1 NGnobnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJwNEe0Olch|ryP NYXpXlZCW0GQR1XS
DMS-114 Mni5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzxdFdKSzVyPUKuOlE2OjRizszN MXnTRW5ITVJ?
ONS-76 NVTWXVJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmxRpY4UUN3ME2yMlY{PjRzIN88US=> MUXTRW5ITVJ?
8-MG-BA NV\WTVBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfsOHdKSzVyPUKuOlU1OTRizszN MkLLV2FPT0WU
BOKU M3nTemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTJwN{K3OlQh|ryP NHLtUm5USU6JRWK=
LAMA-84 Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v0WWlEPTB;Mj63PVkyOiEQvF2= MlTZV2FPT0WU
ES1 M2G3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[0dJRKSzVyPUKuPFE5ODRizszN NF\QfJdUSU6JRWK=
NCI-H1395 NWrvTHloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\yZWlEPTB;Mj64NlAyOiEQvF2= MWPTRW5ITVJ?
A388 NYDFb5F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3SO2o3UUN3ME2yMlk3OTdizszN MVHTRW5ITVJ?
NCCIT NVLWcXkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTlTWM2OD1|LkC4PFYzKM7:TR?= M4rn[XNCVkeHUh?=
HD-MY-Z M3jLeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r6dmlEPTB;Mz6xN|IxOyEQvF2= NIDtWZhUSU6JRWK=
NCI-H510A MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG0epV3UUN3ME2zMlE5QTR|IN88US=> NYjFOHdUW0GQR1XS
NCI-N87 M1vlbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzQfo1KSzVyPUOuNlAxOiEQvF2= NYrycXJDW0GQR1XS
SCLC-21H M1\SOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[4[GlEPTB;Mz6yOlg2QSEQvF2= NHfW[5NUSU6JRWK=
SH-4 NF\TRoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TXRWlEPTB;Mz6yPFc6PyEQvF2= NUTLO4pJW0GQR1XS
QIMR-WIL MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ruSGlEPTB;Mz6zNlg1QSEQvF2= MUPTRW5ITVJ?
KM12 NFTjU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTNwM{O1OFQh|ryP NFLJ[GNUSU6JRWK=
ST486 NYX2WmhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTNwNUO4PFMh|ryP MUfTRW5ITVJ?
HC-1 NEK1bFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO5fZZKSzVyPUOuOlIxOjhizszN MnjWV2FPT0WU
BV-173 NIrkfVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnDVnhKSzVyPUOuOlQxQDhizszN M{DxNXNCVkeHUh?=
EW-24 NULkVG95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGzRXV{UUN3ME2zMlY3PDN2IN88US=> MmezV2FPT0WU
LU-65 M1PTSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNwNki3NUDPxE1? MVjTRW5ITVJ?
ECC4 MkPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOyR3NpUUN3ME2zMlc4PTZizszN NEjjUoJUSU6JRWK=
ARH-77 NUnsbXYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTRwMUGwOlch|ryP M17VTnNCVkeHUh?=
BC-3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzoTWM2OD12LkGzNFY5KM7:TR?= MoW5V2FPT0WU
SNB75 NFjXNmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLRV5V4UUN3ME20MlI3OTlizszN MWHTRW5ITVJ?
MEG-01 M3K4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NImwclJKSzVyPUSuNlc1OTlizszN MWTTRW5ITVJ?
NCI-H1417 M4Padmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PTdGlEPTB;ND6yPFQ1OyEQvF2= NGfNeJRUSU6JRWK=
MDA-MB-134-VI NEjyS41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHUTWM2OD12LkOwOlAyKM7:TR?= NU\NW5RwW0GQR1XS
Becker NFH3WHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP1TWM2OD12LkS3N|M3KM7:TR?= MYrTRW5ITVJ?
DMS-153 M1XpbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTRwNk[0O|Uh|ryP MXXTRW5ITVJ?
TGBC1TKB M1L2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjPTWM2OD12Lk[4OVE2KM7:TR?= NF;TUZZUSU6JRWK=
EW-3 NWXvVnJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrRUYhKSzVyPUSuO|YzPDhizszN NYfBRlIxW0GQR1XS
KE-37 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;sVG5KSzVyPUSuPFYyQTZizszN NXL4VXNVW0GQR1XS
NCI-H23 M2LtTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfJTWM2OD12Lki3NlI4KM7:TR?= NYn3OHFCW0GQR1XS
MC116 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTRwOUSxNlYh|ryP M4PTUnNCVkeHUh?=
NH-12 MljRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDhUXdKSzVyPUSuPVY1OzlizszN M1j5cHNCVkeHUh?=
CTB-1 NH3JR2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;DS2RWUUN3ME20Mlk4PzJzIN88US=> NU\zdpNDW0GQR1XS
KM-H2 Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVwMEWzNlMh|ryP MmLmV2FPT0WU
MOLT-4 M4HBRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn61TWM2OD13LkGxPFMh|ryP MWHTRW5ITVJ?
NCI-H2141 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjKSW1KSzVyPUWuNVQzPjhizszN NXnUe3c4W0GQR1XS
EB-3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;ETWM2OD13LkG3OVA1KM7:TR?= NYrPfldmW0GQR1XS
NCI-H1522 NWXQV5VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvsTWM2OD13LkK2N|IzKM7:TR?= M4\3UHNCVkeHUh?=
MRK-nu-1 NYPi[WlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjy[|BKSzVyPUWuOFM3OzNizszN MW\TRW5ITVJ?
no-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfyTnRvUUN3ME21MlQ4ODh5IN88US=> NGm5SHJUSU6JRWK=
CESS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlmxTWM2OD13LkW4NFM1KM7:TR?= MUHTRW5ITVJ?
KMOE-2 Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\0PHdIUUN3ME21MlU5PjV7IN88US=> M1XlbnNCVkeHUh?=
REH M4DUTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTZwMkW2NVgh|ryP NYHtWmdNW0GQR1XS
KU812 M{n0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkD2TWM2OD14LkSyO|kyKM7:TR?= NFPRfVBUSU6JRWK=
SK-N-FI MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r3cWlEPTB;Nj62NFY4PCEQvF2= MYXTRW5ITVJ?
MMAC-SF M4m1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHhNpd6UUN3ME23MlA3PDl{IN88US=> MkDEV2FPT0WU
RCC10RGB M2q3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTdwMkK5O|ch|ryP NFq5V41USU6JRWK=
NCI-H322M NWnBVHJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme1TWM2OD15LkOzN|M2KM7:TR?= Mm\SV2FPT0WU
NB6 NYHhWWVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXe2V|YyUUN3ME23MlU1QDl7IN88US=> MVPTRW5ITVJ?
MN-60 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vF[WlEPTB;Nz62PVIyPSEQvF2= MVTTRW5ITVJ?
NCI-H1092 MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRThwMEG3N|Qh|ryP MUPTRW5ITVJ?
EKVX M{XEcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HSSmlEPTB;OD60O|A3PiEQvF2= MX3TRW5ITVJ?
D-263MG NHKwcWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\nb4FlUUN3ME24MlU2Ozl4IN88US=> Mn\BV2FPT0WU
NCI-H209 NGPIbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRThwNkSwNFYh|ryP NHzMeplUSU6JRWK=
IST-SL1 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrtPIE5UUN3ME24Mlg6QDl{IN88US=> NFHx[2FUSU6JRWK=
ACN NHzaeoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS4[|I1UUN3ME25MlE6OTV5IN88US=> M2GzOXNCVkeHUh?=
MHH-PREB-1 NInz[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTtWopxUUN3ME25MlIyOjF7IN88US=> M{fkWnNCVkeHUh?=
EW-11 NVHtNW01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PDdWlEPTB;OT62OVM6PiEQvF2= MoGzV2FPT0WU
KASUMI-1 NHzSNIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LOXWlEPTB;OT63PFc4KM7:TR?= NE\VcXdUSU6JRWK=
KINGS-1 NHi4[Y9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHWxfJBKSzVyPUGwMlI{PDdizszN MkDHV2FPT0WU
EVSA-T MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i5VmlEPTB;MUCuN|E6OiEQvF2= M1nScXNCVkeHUh?=
DSH1 NFHZd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTZTWM2OD1zMD6zPVczKM7:TR?= NGj1[IRUSU6JRWK=
COLO-824 MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP0U|BKSzVyPUGwMlg3PjlizszN NIXNWIJUSU6JRWK=
K052 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFe3V5dKSzVyPUGwMlk{OjJizszN M1[4bHNCVkeHUh?=
SK-MEL-2 NVe0U2EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[2TWM2OD1zMD65PVM6KM7:TR?= MUjTRW5ITVJ?

... 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.
  • 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 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
    V1
    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):
    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