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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 269 In stock
USD 160 In stock
USD 290 In stock
USD 770 In stock
USD 1870 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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 NV7INmFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnT5TWM2OD1yLkCwNFA3ODNizszN NXS4UVBSW0GQR1XS
SF539 NHjHSI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXSWG5KUUN3ME2wMlAxODV4NDFOwG0> MmnYV2FPT0WU
DEL NHH1ZpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMECwPVI4KM7:TR?= NGDGTIpUSU6JRWK=
NB1 MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLsc2F6UUN3ME2wMlAxOTZ{IN88US=> MV;TRW5ITVJ?
SR MnfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnHWlJkUUN3ME2wMlAxOjd5IN88US=> MkjwV2FPT0WU
KARPAS-299 NH3ESIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ntUGlEPTB;MD6wNlM5PCEQvF2= M1SzfnNCVkeHUh?=
MHH-CALL-2 NIi4TWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT2TWM2OD1yLkCyPVUzKM7:TR?= MXzTRW5ITVJ?
SU-DHL-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPx[ppKSzVyPUCuNFQ5PjVizszN M3e0NHNCVkeHUh?=
A4-Fuk M1XCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHUPW5nUUN3ME2wMlA2PTZ3IN88US=> MX3TRW5ITVJ?
EW-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwMUCyOVYh|ryP NIXPVXZUSU6JRWK=
NOS-1 NHPETGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHnWVRHUUN3ME2wMlExOjl2IN88US=> NYO1TYJiW0GQR1XS
EW-16 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmxdIVKSzVyPUCuNVA2PjhizszN MYHTRW5ITVJ?
TE-11 NELnSGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMU[wPVYh|ryP MkHwV2FPT0WU
SW982 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvmTI1KSzVyPUCuNVY1PzhizszN NFTRbXRUSU6JRWK=
LAN-6 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwMUe0OFMh|ryP MVTTRW5ITVJ?
MZ1-PC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfkT5BKSzVyPUCuNVc5OzVizszN NXO0dGV[W0GQR1XS
KS-1 NELrXolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrEXWN6UUN3ME2wMlE6OzR|IN88US=> M{TjSnNCVkeHUh?=
PSN1 M{TnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;vU|JbUUN3ME2wMlE6PjNzIN88US=> MYHTRW5ITVJ?
LC-2-ad NUjsOoU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEmz[ZpKSzVyPUCuNVk3QTJizszN NWjnRlcyW0GQR1XS
COLO-320-HSR NWLWc3BmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMUm3O|Yh|ryP M4W1XnNCVkeHUh?=
OPM-2 NHPBbHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMkK2Olkh|ryP M3jMNHNCVkeHUh?=
SK-NEP-1 NF7OZXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwMkO1NlQh|ryP NF7Oc2lUSU6JRWK=
ALL-PO M{exSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMkS1NlQh|ryP M2DQbnNCVkeHUh?=
CMK MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki1TWM2OD1yLkK1OVMh|ryP M1XDfXNCVkeHUh?=
NCI-H1648 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr3Vo1KSzVyPUCuNlc5PTVizszN Mni1V2FPT0WU
SIG-M5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFm4TWhKSzVyPUCuNlkyPTlizszN NHv6VIhUSU6JRWK=
TGBC24TKB MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXS0S3dDUUN3ME2wMlMxOjF6IN88US=> MWfTRW5ITVJ?
DOHH-2 M1P2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwM{GyNFQh|ryP MXHTRW5ITVJ?
NB69 NWPHN5I6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPYTWM2OD1yLkOxO|g4KM7:TR?= M3ruSHNCVkeHUh?=
MFH-ino MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnz3TWM2OD1yLkOyOVI{KM7:TR?= NYr0ZYJvW0GQR1XS
KP-N-RT-BM-1 NUnTbnJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfvTWM2OD1yLkOzNVI{KM7:TR?= M{DU[HNCVkeHUh?=
MONO-MAC-6 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK3[HNWUUN3ME2wMlM{OjlzIN88US=> NELDW|dUSU6JRWK=
ATN-1 NFLld3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzKTnp{UUN3ME2wMlM{OzB|IN88US=> MnvXV2FPT0WU
NTERA-S-cl-D1 Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwM{OzPVYh|ryP NE\ndXhUSU6JRWK=
L-540 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwM{[5PFgh|ryP NV7tT|RMW0GQR1XS
GB-1 NHm2WlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\PXJFnUUN3ME2wMlM5QDZ5IN88US=> M33vNHNCVkeHUh?=
MV-4-11 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwM{m0OFYh|ryP NXXSO4k6W0GQR1XS
KG-1 NUK2dVRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwM{m1OlEh|ryP M1jEV3NCVkeHUh?=
OVCAR-4 MnfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rGNGlEPTB;MD60NFU3QSEQvF2= MWTTRW5ITVJ?
NEC8 NUHrSohpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLId5ZxUUN3ME2wMlQyOjl{IN88US=> M{HLPHNCVkeHUh?=
SK-MM-2 NXX0WFY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWzd|lIUUN3ME2wMlQyPjB7IN88US=> MWDTRW5ITVJ?
TE-8 NUXnb5BUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jwTGlEPTB;MD60Nlg5KM7:TR?= MWjTRW5ITVJ?
697 M2L3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfBTWM2OD1yLkSzNlE2KM7:TR?= M3fLUHNCVkeHUh?=
NB14 NFX6VFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m5UmlEPTB;MD60N|gzPiEQvF2= MoTjV2FPT0WU
GDM-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPROmZKSzVyPUCuOFcyOTZizszN MUfTRW5ITVJ?
HUTU-80 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknsTWM2OD1yLkS3N|c2KM7:TR?= M4jVeHNCVkeHUh?=
HL-60 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KxVWlEPTB;MD60PFE1OiEQvF2= M1;0S3NCVkeHUh?=
OCI-AML2 NUOxNHJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGny[W5KSzVyPUCuOFg{OjhizszN NGnHcIxUSU6JRWK=
ML-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\EW3dKSzVyPUCuOFkxOzFizszN NECzcXVUSU6JRWK=
ES4 NXu1NHhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHxcoNXUUN3ME2wMlQ6OTB7IN88US=> NX[4Um41W0GQR1XS
NCI-H747 NETzT3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXDTWM2OD1yLkS5PFkh|ryP NXHY[HZrW0GQR1XS
RL95-2 NYGwOJkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjFeVVKSzVyPUCuOVAyOTJizszN Mlu0V2FPT0WU
TE-15 M{TOe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwNUGxNlQh|ryP M4jQR3NCVkeHUh?=
TE-12 NVqzUVlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfDNFZKSzVyPUCuOVM{PDlizszN MkXSV2FPT0WU
LB1047-RCC MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjzXXFIUUN3ME2wMlU1PTR7IN88US=> M{TMPHNCVkeHUh?=
LB831-BLC NHGzdIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwNUWwNlMh|ryP M2Dh[3NCVkeHUh?=
NCI-H1355 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K4bWlEPTB;MD61OVE5PCEQvF2= MmXXV2FPT0WU
CTV-1 M2rFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jNbWlEPTB;MD61OVYzPCEQvF2= MmO3V2FPT0WU
RXF393 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jR[WlEPTB;MD61OVc6PCEQvF2= NU\P[|JTW0GQR1XS
SW872 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPSb2pKSzVyPUCuOVY4OjRizszN M4i5VXNCVkeHUh?=
MPP-89 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwNUe4PFQh|ryP NVzYfJhPW0GQR1XS
RPMI-8226 NEn0NVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDzTWM2OD1yLk[zOVI3KM7:TR?= NFjafFFUSU6JRWK=
LS-1034 NIjKd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwNkO1PEDPxE1? M1T0VHNCVkeHUh?=
SJSA-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfYR5BKSzVyPUCuOlM4OjVizszN MofQV2FPT0WU
HOP-62 NG\FNGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPoTWM2OD1yLk[1NFM{KM7:TR?= MnPiV2FPT0WU
KGN MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrTPYlKSzVyPUCuOlYyPjhizszN MnnhV2FPT0WU
D-336MG M2XmcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3ENno4UUN3ME2wMlY3OTZ7IN88US=> NWrkZnBVW0GQR1XS
LS-411N NVnBVFJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHXTHZKSzVyPUCuOlc1PjJizszN M175[nNCVkeHUh?=
TE-1 NVG0XZd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn2TWM2OD1yLk[5NFc1KM7:TR?= NHrsW|ZUSU6JRWK=
LB996-RCC NVH3S5IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LQb2lEPTB;MD62PVM5QSEQvF2= M3rIdXNCVkeHUh?=
TE-10 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTDNphkUUN3ME2wMlcyPDl4IN88US=> MkO3V2FPT0WU
NCI-SNU-16 M3vidWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\JSmlEPTB;MD63NlY3PCEQvF2= M1\KN3NCVkeHUh?=
ES8 M17TW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfn[XNKSzVyPUCuO|Q6PzVizszN Mlr5V2FPT0WU
COLO-800 M3zocWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwN{[2PVUh|ryP NH3HOY5USU6JRWK=
ES6 M1nifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LqbWlEPTB;MD63O|U2QSEQvF2= MlPJV2FPT0WU
L-363 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHruNWhKSzVyPUCuPFI{PzVizszN MkXZV2FPT0WU
NMC-G1 NGDaRphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTBwOEOyN|Mh|ryP M13VeHNCVkeHUh?=
LU-134-A M{TXZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XmUmlEPTB;MD64N|kyOiEQvF2= MVXTRW5ITVJ?
SF268 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwOESwOFIh|ryP MkfGV2FPT0WU
KARPAS-45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfiSlRKSzVyPUCuPFQzPjNizszN M{T5fHNCVkeHUh?=
TGW MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnLeYpKSzVyPUCuPFU5PjNizszN MoLoV2FPT0WU
CHP-126 M2rQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTBwOEW5OVch|ryP MYPTRW5ITVJ?
MOLT-16 Ml;IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwOEe1PFkh|ryP NWPWbWx5W0GQR1XS
LB771-HNC NFnFephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PUUGlEPTB;MD64PVc2PyEQvF2= NYmwN2dwW0GQR1XS
NALM-6 NGXKcoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXsTWM2OD1yLkmwO|M6KM7:TR?= NUnNUmJHW0GQR1XS
GCIY NIP5c|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGCxd2JKSzVyPUCuPVU2OjZizszN MnP6V2FPT0WU
IST-MES1 NYTEe24{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDjN3pKSzVyPUCuPVg5OjRizszN Mon3V2FPT0WU
LB2241-RCC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TVbWlEPTB;MD65PFg1KM7:TR?= MlXvV2FPT0WU
BL-70 NUnIWIl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzJTWM2OD1yLkm5OVM2KM7:TR?= NWmwSolGW0GQR1XS
NB17 NIOxNXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f6d2lEPTB;MT6wNFY{QSEQvF2= NF\KPYZUSU6JRWK=
LXF-289 NVm4bXNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTFwMEOwO|Yh|ryP MYPTRW5ITVJ?
TK10 MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jOTGlEPTB;MT6wOVA3OyEQvF2= MWrTRW5ITVJ?
K5 M1y4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwME[yO|Qh|ryP MkftV2FPT0WU
NCI-H716 NWLxN|lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7MTWM2OD1zLkC3NlU6KM7:TR?= NXrQPZhzW0GQR1XS
HCE-T MlHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP2eHRRUUN3ME2xMlA5QDF7IN88US=> MlTlV2FPT0WU
GI-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTFwMEm3PVgh|ryP NE\pcXpUSU6JRWK=
KARPAS-422 MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwMUCwNlIh|ryP NIjFVZRUSU6JRWK=
TE-9 MlrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjQSYR5UUN3ME2xMlEyOzJ6IN88US=> MYHTRW5ITVJ?
SF126 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITneI9KSzVyPUGuNVE2PjhizszN MWDTRW5ITVJ?
BB30-HNC Ml7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwMUOxNVIh|ryP Mly4V2FPT0WU
NCI-H1304 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwMUOzN|gh|ryP M4G1dXNCVkeHUh?=
HEL NUjrRZZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3XTWM2OD1zLkG0PFk2KM7:TR?= NH\D[4JUSU6JRWK=
HAL-01 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f2XWlEPTB;MT6xOVI5OyEQvF2= NXeyeoVGW0GQR1XS
SK-LMS-1 MkTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojaTWM2OD1zLkG1PVc1KM7:TR?= NGrrWHpUSU6JRWK=
SW954 NV2yWVdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jxN2lEPTB;MT6xPVU3PyEQvF2= MXvTRW5ITVJ?
D-283MED NIjR[|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzyTWM2OD1zLkKyN|c6KM7:TR?= NVzjT2RwW0GQR1XS
NCI-H1882 M1HIO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HnU2lEPTB;MT6yN|g6KM7:TR?= MWrTRW5ITVJ?
GI-ME-N M4XJRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwMkWyNFgh|ryP MmPhV2FPT0WU
SK-PN-DW M{P2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETwXGtKSzVyPUGuNlY{PDhizszN M4nXR3NCVkeHUh?=
C2BBe1 MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrSfJlKSzVyPUGuNlkyOTdizszN MknLV2FPT0WU
A704 NGfCPZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHSTWM2OD1zLkOyOlg6KM7:TR?= NH;SRWJUSU6JRWK=
KALS-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3hTWM2OD1zLkO0NFgh|ryP M3jxcHNCVkeHUh?=
ETK-1 NFnSN45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i1WWlEPTB;MT6zOFQ5QSEQvF2= MYXTRW5ITVJ?
LB647-SCLC NGnE[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVWwdmRTUUN3ME2xMlM1QTh4IN88US=> NXXocJNXW0GQR1XS
OCUB-M M1P0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3SR5NGUUN3ME2xMlM3OTR|IN88US=> M4rPVnNCVkeHUh?=
NCI-H720 NITLfGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwM{[zO|gh|ryP MXHTRW5ITVJ?
NB13 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnaW|hoUUN3ME2xMlM4Ojl|IN88US=> NFW0So9USU6JRWK=
GR-ST MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwM{i3OVch|ryP MmLxV2FPT0WU
DU-4475 M1;6O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\nXmlNUUN3ME2xMlQ2QDV|IN88US=> M4XqZ3NCVkeHUh?=
HCC2157 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7iVlRKSzVyPUGuOFY3PTlizszN MnnTV2FPT0WU
RKO M3fsU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkT3TWM2OD1zLkS5PVIzKM7:TR?= M3zvdnNCVkeHUh?=
LS-123 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rkVmlEPTB;MT61NVU6PCEQvF2= M{nNdHNCVkeHUh?=
NCI-H69 MoToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q5W2lEPTB;MT61OVgyOSEQvF2= MmjvV2FPT0WU
SW962 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGO5VoZKSzVyPUGuOVYyOyEQvF2= NIjpfXJUSU6JRWK=
PF-382 NEPMRYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTFwNU[5OkDPxE1? NF;FcHJUSU6JRWK=
A101D NX7tWGRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\wTWM2OD1zLkW3NVE{KM7:TR?= M3qydXNCVkeHUh?=
NB10 NFnF[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm3ZYNKSzVyPUGuOVc{QTJizszN NVi3RWt3W0GQR1XS
NB5 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTFwNUi0O|Yh|ryP Mny3V2FPT0WU
HCE-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD3TWM2OD1zLk[wPFUh|ryP MWjTRW5ITVJ?
HT-144 NVW5N2dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3kTWM2OD1zLk[zNVkh|ryP MYjTRW5ITVJ?
NCI-H524 NEjG[olIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITrN4RKSzVyPUGuOlQ{ODdizszN MXjTRW5ITVJ?
NKM-1 NFLWRWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq5XnRKSzVyPUGuOlg3PiEQvF2= MWnTRW5ITVJ?
KURAMOCHI NIC2NXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTFwNkm1O|Mh|ryP MXXTRW5ITVJ?
NCI-H187 M1j6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7ETWM2OD1zLkewNFM3KM7:TR?= Mn3mV2FPT0WU
U-266 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoiyTWM2OD1zLkezPFQzKM7:TR?= MoXXV2FPT0WU
BL-41 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwN{[yO|Ih|ryP NIX3fmNUSU6JRWK=
SK-N-DZ M4jrbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvKTWM2OD1zLke4N|A6KM7:TR?= MX7TRW5ITVJ?
Daudi NEDC[mxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K3TWlEPTB;MT63PFk3PyEQvF2= M3\4TXNCVkeHUh?=
CPC-N NHfyTGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPPcoZKSzVyPUGuPFUxQTZizszN MmL1V2FPT0WU
EM-2 NHy1TIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HDPWlEPTB;MT64OVEh|ryP MoXBV2FPT0WU
HCC1187 MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTFwOE[yOFEh|ryP MVTTRW5ITVJ?
LP-1 NGX3N49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\WT2lEPTB;MT64O|E1OyEQvF2= MWPTRW5ITVJ?
CAS-1 Mlu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHZN3ZKSzVyPUGuPVgzQTlizszN NXruRYN3W0GQR1XS
NB7 NXfGSZdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\JSZdpUUN3ME2yMlAxPTV3IN88US=> NISyNYpUSU6JRWK=
VA-ES-BJ M{OyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\SZ|lKSzVyPUKuNFE2OTNizszN MknTV2FPT0WU
SNU-C2B M2DS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7VVJFKSzVyPUKuNFM{PTFizszN MkXkV2FPT0WU
LOXIMVI MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTJwME[3PFYh|ryP M3\EZnNCVkeHUh?=
NCI-H1581 NFWxRZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJwMUG1OVkh|ryP NEXQ[2ZUSU6JRWK=
IST-SL2 NV\tZVVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTOZoltUUN3ME2yMlEzPDR3IN88US=> NGiwbVRUSU6JRWK=
NOMO-1 M{O1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYCxWVRGUUN3ME2yMlE4Pjh|IN88US=> M4noSXNCVkeHUh?=
TE-6 MnT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PSdGlEPTB;Mj6xPVA2KM7:TR?= MWnTRW5ITVJ?
NCI-H526 NXT5R3hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7GTWM2OD1{LkG5NVQyKM7:TR?= MVTTRW5ITVJ?
MSTO-211H M{\1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\zc2lEPTB;Mj6yNFA1OSEQvF2= MV\TRW5ITVJ?
LS-513 M4DRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\ofHN[UUN3ME2yMlIzOjZ7IN88US=> MnPWV2FPT0WU
NCI-SNU-1 NWTveINET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX3clVwUUN3ME2yMlM{OjV4IN88US=> NFi2OZNUSU6JRWK=
BB65-RCC MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q3[WlEPTB;Mj6zO|Q6OyEQvF2= M2LJd3NCVkeHUh?=
GT3TKB MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPLTWM2OD1{LkO5PVczKM7:TR?= NFvyXlRUSU6JRWK=
OS-RC-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DvbGlEPTB;Mj60NlM1OSEQvF2= MV\TRW5ITVJ?
NCI-H2126 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXmfYVlUUN3ME2yMlQ{Pjd2IN88US=> MkO4V2FPT0WU
SK-UT-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUG1Uo1FUUN3ME2yMlQ4PDZ5IN88US=> M4TMNXNCVkeHUh?=
DMS-114 NXr1Wm9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH0VnJKSzVyPUKuOlE2OjRizszN NFXQTWtUSU6JRWK=
ONS-76 M{jhdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnJTWM2OD1{Lk[zOlQyKM7:TR?= MUnTRW5ITVJ?
8-MG-BA NH;VeXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz2TWM2OD1{Lk[1OFE1KM7:TR?= NIfYO3FUSU6JRWK=
BOKU M4PPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrITWM2OD1{LkeyO|Y1KM7:TR?= M3XJNnNCVkeHUh?=
LAMA-84 NYnKTVQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTJwN{m5NVIh|ryP NVXrTpVOW0GQR1XS
ES1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:wTWM2OD1{LkixPFA1KM7:TR?= Ml7ZV2FPT0WU
NCI-H1395 NFTYT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJwOEKwNVIh|ryP MlnJV2FPT0WU
A388 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLSemRtUUN3ME2yMlk3OTdizszN MmHOV2FPT0WU
NCCIT NIW4bFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTNwMEi4OlIh|ryP MkDSV2FPT0WU
HD-MY-Z NXOzfnRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULUblRoUUN3ME2zMlE{OjB|IN88US=> NHTWNmNUSU6JRWK=
NCI-H510A M3fjUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTU[IViUUN3ME2zMlE5QTR|IN88US=> M3e1b3NCVkeHUh?=
NCI-N87 NIPmWYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNwMkCwNkDPxE1? MULTRW5ITVJ?
SCLC-21H MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\nbmlEPTB;Mz6yOlg2QSEQvF2= MWHTRW5ITVJ?
SH-4 NVvaRWNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDIO2E6UUN3ME2zMlI5Pzl5IN88US=> NY[0WmlyW0GQR1XS
QIMR-WIL NE\XXmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vDZWlEPTB;Mz6zNlg1QSEQvF2= MmnLV2FPT0WU
KM12 NHP2eGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTNwM{O1OFQh|ryP M3;MOnNCVkeHUh?=
ST486 NGi3OJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7KWmZKSzVyPUOuOVM5QDNizszN M2DwfnNCVkeHUh?=
HC-1 NWXVWlJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTNwNkKwNlgh|ryP MX3TRW5ITVJ?
BV-173 NIn6WWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTNwNkSwPFgh|ryP M1LIWnNCVkeHUh?=
EW-24 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\CT4VPUUN3ME2zMlY3PDN2IN88US=> NWf2VYlIW0GQR1XS
LU-65 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LafmlEPTB;Mz62PFcyKM7:TR?= M4S4OXNCVkeHUh?=
ECC4 M2nK[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXkTWM2OD1|Lke3OVYh|ryP MoLPV2FPT0WU
ARH-77 M3LlVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPzTWp5UUN3ME20MlEyODZ5IN88US=> MoHYV2FPT0WU
BC-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\SZXR{UUN3ME20MlE{ODZ6IN88US=> NFfMTHZUSU6JRWK=
SNB75 MlP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTRwMk[xPUDPxE1? MVfTRW5ITVJ?
MEG-01 NVjFdlRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;GTWM2OD12LkK3OFE6KM7:TR?= NHnIVIpUSU6JRWK=
NCI-H1417 NITMNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPWRWtXUUN3ME20MlI5PDR|IN88US=> MkXmV2FPT0WU
MDA-MB-134-VI MmPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nDPGlEPTB;ND6zNFYxOSEQvF2= NGfscmtUSU6JRWK=
Becker NHjPZYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j1eGlEPTB;ND60O|M{PiEQvF2= Ml3rV2FPT0WU
DMS-153 M33Wbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULTZ|lDUUN3ME20MlY3PDd3IN88US=> NV\iV2JXW0GQR1XS
TGBC1TKB MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTRwNki1NVUh|ryP NHLvfHBUSU6JRWK=
EW-3 NIfaXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnQcmdKSzVyPUSuO|YzPDhizszN NV3mPYQyW0GQR1XS
KE-37 NHLvUZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrxTWM2OD12Lki2NVk3KM7:TR?= NV7ne5dwW0GQR1XS
NCI-H23 NVqye|NxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;sdmlEPTB;ND64O|IzPyEQvF2= NVvpeYFuW0GQR1XS
MC116 M33NVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DKPWlEPTB;ND65OFEzPiEQvF2= NV3a[IJyW0GQR1XS
NH-12 M1Xyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jQTmlEPTB;ND65OlQ{QSEQvF2= M3LqeHNCVkeHUh?=
CTB-1 MmrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rLXWlEPTB;ND65O|czOSEQvF2= NIXZNodUSU6JRWK=
KM-H2 NVrwR2Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTVwMEWzNlMh|ryP M1Pi[nNCVkeHUh?=
MOLT-4 NHnRNXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXFTWM2OD13LkGxPFMh|ryP MXjTRW5ITVJ?
NCI-H2141 M3HU[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe5fG5wUUN3ME21MlE1OjZ6IN88US=> MlrvV2FPT0WU
EB-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv2dpNKSzVyPUWuNVc2ODRizszN MX\TRW5ITVJ?
NCI-H1522 M1jzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfBTWM2OD13LkK2N|IzKM7:TR?= NFizVHVUSU6JRWK=
MRK-nu-1 NXf4[m16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXJTWM2OD13LkSzOlM{KM7:TR?= M1HwdXNCVkeHUh?=
no-11 NV\OemsyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH4eZNSUUN3ME21MlQ4ODh5IN88US=> NV[ydWRIW0GQR1XS
CESS M2DQTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHSbJFuUUN3ME21MlU5ODN2IN88US=> MV7TRW5ITVJ?
KMOE-2 M{Hyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:xTWM2OD13LkW4OlU6KM7:TR?= NX34VZRoW0GQR1XS
REH NXfodJhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HVcGlEPTB;Nj6yOVYyQCEQvF2= MV7TRW5ITVJ?
KU812 NIjKfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7ET5JTUUN3ME22MlQzPzlzIN88US=> MUnTRW5ITVJ?
SK-N-FI NIixUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TyOmlEPTB;Nj62NFY4PCEQvF2= MYDTRW5ITVJ?
MMAC-SF MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTdwME[0PVIh|ryP NHT2dFBUSU6JRWK=
RCC10RGB MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTdwMkK5O|ch|ryP NYWw[GtRW0GQR1XS
NCI-H322M NIToTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHQTWM2OD15LkOzN|M2KM7:TR?= NGnnV3NUSU6JRWK=
NB6 NIr3PVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;SbZRIUUN3ME23MlU1QDl7IN88US=> MU\TRW5ITVJ?
MN-60 M3L2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTdwNkmyNVUh|ryP NWP4bFViW0GQR1XS
NCI-H1092 Ml20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzEVFVPUUN3ME24MlAyPzN2IN88US=> MoKxV2FPT0WU
EKVX MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPYdJpZUUN3ME24MlQ4ODZ4IN88US=> NIPvZnJUSU6JRWK=
D-263MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRThwNUWzPVYh|ryP NXPQTlZkW0GQR1XS
NCI-H209 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRThwNkSwNFYh|ryP Mlq0V2FPT0WU
IST-SL1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrieHZ7UUN3ME24Mlg6QDl{IN88US=> NYP0S|dMW0GQR1XS
ACN M33r[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6xVlNHUUN3ME25MlE6OTV5IN88US=> NUK5d|VRW0GQR1XS
MHH-PREB-1 Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnS2TWM2OD17LkKxNlE6KM7:TR?= NXntdHh3W0GQR1XS
EW-11 NX7TdVRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTlwNkWzPVYh|ryP MXzTRW5ITVJ?
KASUMI-1 M3\zW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X0cGlEPTB;OT63PFc4KM7:TR?= M3zOUXNCVkeHUh?=
KINGS-1 Moj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS3TWM2OD1zMD6yN|Q4KM7:TR?= NUH5O3hOW0GQR1XS
EVSA-T M4SySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfNTWM2OD1zMD6zNVkzKM7:TR?= MoPyV2FPT0WU
DSH1 M{HKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLxSFVKSzVyPUGwMlM6PzJizszN MUHTRW5ITVJ?
COLO-824 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFyLki2Olkh|ryP NYfqWFlVW0GQR1XS
K052 NFHTd4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrYSWRKSzVyPUGwMlk{OjJizszN NY\xNGdqW0GQR1XS
SK-MEL-2 NGD0[HdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXGTWM2OD1zMD65PVM6KM7:TR?= MmraV2FPT0WU

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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.

  • * Indicates a Required Field

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

Related ALK Products

Tags: buy TAE684 (NVP-TAE684) | TAE684 (NVP-TAE684) supplier | purchase TAE684 (NVP-TAE684) | TAE684 (NVP-TAE684) cost | TAE684 (NVP-TAE684) manufacturer | order TAE684 (NVP-TAE684) | TAE684 (NVP-TAE684) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID