TAE684 (NVP-TAE684)

For research use only.

Catalog No.S1108

43 publications

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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Selleck's TAE684 (NVP-TAE684) has been cited by 43 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 NUDIdlc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\zSVNKSzVyPUCuNFAxODZyMzFOwG0> MoX3V2FPT0WU
SF539 NVXSOZZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MniyTWM2OD1yLkCwNFU3PCEQvF2= MmfZV2FPT0WU
DEL M{Lj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjpNZJ1UUN3ME2wMlAxODl{NzFOwG0> NF71XotUSU6JRWK=
NB1 M1Hh[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LYbWlEPTB;MD6wNFE3OiEQvF2= M3fjXnNCVkeHUh?=
SR NF7SWJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XaUGlEPTB;MD6wNFI4PyEQvF2= MoXlV2FPT0WU
KARPAS-299 NH\HR3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\MSGRKSzVyPUCuNFI{QDRizszN MXfTRW5ITVJ?
MHH-CALL-2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;xS2lEPTB;MD6wNlk2OiEQvF2= M1PKfnNCVkeHUh?=
SU-DHL-1 NFnUVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXjfIxKSzVyPUCuNFQ5PjVizszN MkDQV2FPT0WU
A4-Fuk MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwMEW1OlUh|ryP M2ribHNCVkeHUh?=
EW-1 M1jB[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LVO2lEPTB;MD6xNFI2PiEQvF2= MlvqV2FPT0WU
NOS-1 NGHzcZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwMUCyPVQh|ryP NIj6W|JUSU6JRWK=
EW-16 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGzTWM2OD1yLkGwOVY5KM7:TR?= MWPTRW5ITVJ?
TE-11 M1i0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LBPWlEPTB;MD6xOlA6PiEQvF2= MnzsV2FPT0WU
SW982 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r4fGlEPTB;MD6xOlQ4QCEQvF2= NUDTclJ4W0GQR1XS
LAN-6 M3LldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fGTGlEPTB;MD6xO|Q1OyEQvF2= M2Xje3NCVkeHUh?=
MZ1-PC MkHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL1TWM2OD1yLkG3PFM2KM7:TR?= M{DDUnNCVkeHUh?=
KS-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLNSI5DUUN3ME2wMlE6OzR|IN88US=> M{PBR3NCVkeHUh?=
PSN1 M{i4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULweVRYUUN3ME2wMlE6PjNzIN88US=> MlL6V2FPT0WU
LC-2-ad MkLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPOTWM2OD1yLkG5OlkzKM7:TR?= MnTyV2FPT0WU
COLO-320-HSR M4rHT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnCc2QyUUN3ME2wMlE6Pzd4IN88US=> NGnmcVFUSU6JRWK=
OPM-2 NWnlVZVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPXZVBOUUN3ME2wMlIzPjZ7IN88US=> NX7mVm1MW0GQR1XS
SK-NEP-1 NF\lNldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3pTWM2OD1yLkKzOVI1KM7:TR?= NF3nXHhUSU6JRWK=
ALL-PO MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PGPWlEPTB;MD6yOFUzPCEQvF2= M4iwSHNCVkeHUh?=
CMK MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkmyTWM2OD1yLkK1OVMh|ryP MYDTRW5ITVJ?
NCI-H1648 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7GTWM2OD1yLkK3PFU2KM7:TR?= M2rTXHNCVkeHUh?=
SIG-M5 NFHjRVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwMkmxOVkh|ryP NHjXfWRUSU6JRWK=
TGBC24TKB M3;pPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7hTWM2OD1yLkOwNlE5KM7:TR?= M{PSPHNCVkeHUh?=
DOHH-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXRTWM2OD1yLkOxNlA1KM7:TR?= NXPpXmtUW0GQR1XS
NB69 NYrvbJc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILDRoNKSzVyPUCuN|E4QDdizszN NFLsbo9USU6JRWK=
MFH-ino NH\adJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITpbnhKSzVyPUCuN|I2OjNizszN MVrTRW5ITVJ?
KP-N-RT-BM-1 M{\sOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\vZoJKSzVyPUCuN|MyOjNizszN M1fVeXNCVkeHUh?=
MONO-MAC-6 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXrenVKSzVyPUCuN|MzQTFizszN MYHTRW5ITVJ?
ATN-1 MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Vcmh7UUN3ME2wMlM{OzB|IN88US=> MkXMV2FPT0WU
NTERA-S-cl-D1 Mo\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4iyOWlEPTB;MD6zN|M6PiEQvF2= NY\1R5B4W0GQR1XS
L-540 MmG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:xOVNpUUN3ME2wMlM3QTh6IN88US=> M4D5dHNCVkeHUh?=
GB-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXzOZJKSzVyPUCuN|g5PjdizszN NEPsbWpUSU6JRWK=
MV-4-11 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwM{m0OFYh|ryP NVPkUY5FW0GQR1XS
KG-1 Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[wTWM2OD1yLkO5OVYyKM7:TR?= M1zsUXNCVkeHUh?=
OVCAR-4 NFHGbnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DPSGlEPTB;MD60NFU3QSEQvF2= MVzTRW5ITVJ?
NEC8 NYnPNGtET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfHXZM5UUN3ME2wMlQyOjl{IN88US=> M2q0XnNCVkeHUh?=
SK-MM-2 M1Lacmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\XTWM2OD1yLkSxOlA6KM7:TR?= M1HVbHNCVkeHUh?=
TE-8 Mmj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjxTWM2OD1yLkSyPFgh|ryP M1TlcnNCVkeHUh?=
697 M1T1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vzWGlEPTB;MD60N|IyPSEQvF2= M2q0XXNCVkeHUh?=
NB14 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUW3UGhrUUN3ME2wMlQ{QDJ4IN88US=> NV\Wb4FKW0GQR1XS
GDM-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3MblVKSzVyPUCuOFcyOTZizszN NVHoN4RZW0GQR1XS
HUTU-80 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe1cFRJUUN3ME2wMlQ4Ozd3IN88US=> M1fuOXNCVkeHUh?=
HL-60 NWX5dZRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M124fWlEPTB;MD60PFE1OiEQvF2= Ml3OV2FPT0WU
OCI-AML2 M2HjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f2O2lEPTB;MD60PFMzQCEQvF2= M{K1O3NCVkeHUh?=
ML-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XR[mlEPTB;MD60PVA{OSEQvF2= NWn1SWd7W0GQR1XS
ES4 NX7JcIhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrwTWM2OD1yLkS5NVA6KM7:TR?= NGG5Z|lUSU6JRWK=
NCI-H747 NX3nUFhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHIdlh4UUN3ME2wMlQ6QDlizszN M1SwS3NCVkeHUh?=
RL95-2 NV\POHJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSwWGRKSzVyPUCuOVAyOTJizszN M3rwUHNCVkeHUh?=
TE-15 M322Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwNUGxNlQh|ryP M{X5PHNCVkeHUh?=
TE-12 NGjUUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;nPGlEPTB;MD61N|M1QSEQvF2= M1HIVXNCVkeHUh?=
LB1047-RCC M2fmcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HKUmlEPTB;MD61OFU1QSEQvF2= NYPTe2VnW0GQR1XS
LB831-BLC Mni2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\XTWM2OD1yLkW1NFI{KM7:TR?= NVHZVYl2W0GQR1XS
NCI-H1355 NVG5[mE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHVcpdEUUN3ME2wMlU2OTh2IN88US=> NWPBNmhJW0GQR1XS
CTV-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTPU2JKSzVyPUCuOVU3OjRizszN Ml3EV2FPT0WU
RXF393 M1jacWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwNUW3PVQh|ryP M3jSXHNCVkeHUh?=
SW872 NFjLfWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TV[GlEPTB;MD61OlczPCEQvF2= NUDqOmxZW0GQR1XS
MPP-89 NXfofGpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFGyOFdKSzVyPUCuOVc5QDRizszN M2LYNXNCVkeHUh?=
RPMI-8226 M3HSVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD6WXN[UUN3ME2wMlY{PTJ4IN88US=> MWjTRW5ITVJ?
LS-1034 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rmOGlEPTB;MD62N|U5KM7:TR?= NF73VJBUSU6JRWK=
SJSA-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPRUpBDUUN3ME2wMlY{PzJ3IN88US=> MnvxV2FPT0WU
HOP-62 NHn6WXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\DTWM2OD1yLk[1NFM{KM7:TR?= NIjwbVhUSU6JRWK=
KGN NVrOTIRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS2UoplUUN3ME2wMlY3OTZ6IN88US=> M1qzbHNCVkeHUh?=
D-336MG M3T6[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwNk[xOlkh|ryP NXW4UmRyW0GQR1XS
LS-411N M1XrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzCTWM2OD1yLk[3OFYzKM7:TR?= MWLTRW5ITVJ?
TE-1 MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj5c2ZKSzVyPUCuOlkxPzRizszN MorLV2FPT0WU
LB996-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTBwNkmzPFkh|ryP MnL1V2FPT0WU
TE-10 M{XxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwN{G0PVYh|ryP MmH6V2FPT0WU
NCI-SNU-16 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLtTWM2OD1yLkeyOlY1KM7:TR?= M2nFOXNCVkeHUh?=
ES8 NGD0So1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jRN2lEPTB;MD63OFk4PSEQvF2= NYXabW97W0GQR1XS
COLO-800 NGqxWJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnqTWM2OD1yLke2Olk2KM7:TR?= MYTTRW5ITVJ?
ES6 NILwc|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj5d|AzUUN3ME2wMlc4PTV7IN88US=> M1T4XnNCVkeHUh?=
L-363 NHL5bm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\TSWpKSzVyPUCuPFI{PzVizszN MYPTRW5ITVJ?
NMC-G1 NF;UV2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrjbZFKSzVyPUCuPFMzOzNizszN M1Lp[3NCVkeHUh?=
LU-134-A NEC2RYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDaPFdKSzVyPUCuPFM6OTJizszN M1nJ[HNCVkeHUh?=
SF268 NHPtWnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7vVlR7UUN3ME2wMlg1ODR{IN88US=> NE\2V3NUSU6JRWK=
KARPAS-45 NXm1e3ViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDZOo5sUUN3ME2wMlg1OjZ|IN88US=> M3nZNnNCVkeHUh?=
TGW NIP3UIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXSU25KSzVyPUCuPFU5PjNizszN MXzTRW5ITVJ?
CHP-126 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj5U4tKSzVyPUCuPFU6PTdizszN MUHTRW5ITVJ?
MOLT-16 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3oTWM2OD1yLki3OVg6KM7:TR?= MXXTRW5ITVJ?
LB771-HNC NH7S[lFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DCPGlEPTB;MD64PVc2PyEQvF2= NXjRUHVmW0GQR1XS
NALM-6 NHfKRYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3IS2ZKSzVyPUCuPVA4OzlizszN NIe2[VNUSU6JRWK=
GCIY NIHZdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\YN2pKSzVyPUCuPVU2OjZizszN NHPpUGRUSU6JRWK=
IST-MES1 M4e0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXMfoJlUUN3ME2wMlk5QDJ2IN88US=> NWXuVIVqW0GQR1XS
LB2241-RCC NIT5e5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwOUi4OEDPxE1? NGCyZXdUSU6JRWK=
BL-70 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jRb2lEPTB;MD65PVU{PSEQvF2= MlvKV2FPT0WU
NB17 M4GyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXqT29yUUN3ME2xMlAxPjN7IN88US=> MkLDV2FPT0WU
LXF-289 MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Pac2lEPTB;MT6wN|A4PiEQvF2= M{XKT3NCVkeHUh?=
TK10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1frN2lEPTB;MT6wOVA3OyEQvF2= M{LpU3NCVkeHUh?=
K5 M4jie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlOxTWM2OD1zLkC2Nlc1KM7:TR?= M4D4PXNCVkeHUh?=
NCI-H716 NIrOXWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwMEeyOVkh|ryP NFnMOIlUSU6JRWK=
HCE-T M1HNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXITWM2OD1zLkC4PFE6KM7:TR?= MVvTRW5ITVJ?
GI-1 NWXqRmlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmSxTWM2OD1zLkC5O|k5KM7:TR?= NXzKeFRJW0GQR1XS
KARPAS-422 MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELMe5RKSzVyPUGuNVAxOjJizszN NIXzS|JUSU6JRWK=
TE-9 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljJTWM2OD1zLkGxN|I5KM7:TR?= MkfEV2FPT0WU
SF126 MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPwS454UUN3ME2xMlEyPTZ6IN88US=> NYTkRo1XW0GQR1XS
BB30-HNC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzZTWM2OD1zLkGzNVEzKM7:TR?= MYPTRW5ITVJ?
NCI-H1304 NF\neW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwMUOzN|gh|ryP NFnaVFhUSU6JRWK=
HEL M3\vSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\PTWM2OD1zLkG0PFk2KM7:TR?= M1PmenNCVkeHUh?=
HAL-01 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PyS2lEPTB;MT6xOVI5OyEQvF2= MW\TRW5ITVJ?
SK-LMS-1 NF72e5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LSZmlEPTB;MT6xOVk4PCEQvF2= NV\sVIsxW0GQR1XS
SW954 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWxO|J3UUN3ME2xMlE6PTZ5IN88US=> M{nkVHNCVkeHUh?=
D-283MED M{LTTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\SUo9KSzVyPUGuNlI{PzlizszN NEjkbFlUSU6JRWK=
NCI-H1882 M3Podmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TQZ2lEPTB;MT6yN|g6KM7:TR?= NXLOeVFYW0GQR1XS
GI-ME-N MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTFwMkWyNFgh|ryP NVzHeZBRW0GQR1XS
SK-PN-DW MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3w[2dKSzVyPUGuNlY{PDhizszN NXrVPZFkW0GQR1XS
C2BBe1 NXzvT4hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MniwTWM2OD1zLkK5NVE4KM7:TR?= NIrYU5FUSU6JRWK=
A704 NF:1[otIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XsOWlEPTB;MT6zNlY5QSEQvF2= NXnxbWxkW0GQR1XS
KALS-1 NXXQSFRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHMTWM2OD1zLkO0NFgh|ryP MXnTRW5ITVJ?
ETK-1 NHTUS45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfHTWM2OD1zLkO0OFg6KM7:TR?= MVPTRW5ITVJ?
LB647-SCLC M2DFbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnXUY9KSzVyPUGuN|Q6QDZizszN Ml7NV2FPT0WU
OCUB-M Mon4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXGe3VKSzVyPUGuN|YyPDNizszN MnzJV2FPT0WU
NCI-H720 M{LXR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HzRWlEPTB;MT6zOlM4QCEQvF2= MVjTRW5ITVJ?
NB13 NYHNSZRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGr3XZBKSzVyPUGuN|czQTNizszN NEnFcIZUSU6JRWK=
GR-ST MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwM{i3OVch|ryP MWnTRW5ITVJ?
DU-4475 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofXTWM2OD1zLkS1PFU{KM7:TR?= MkT0V2FPT0WU
HCC2157 MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTFwNE[2OVkh|ryP NVr1cmFbW0GQR1XS
RKO NGnZT4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrGcmJKSzVyPUGuOFk6OjJizszN M4DadHNCVkeHUh?=
LS-123 NELORnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwNUG1PVQh|ryP MlPsV2FPT0WU
NCI-H69 M4G1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfCTWM2OD1zLkW1PFEyKM7:TR?= NYWyPHpkW0GQR1XS
SW962 Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\NTWM2OD1zLkW2NVMh|ryP NYqw[GczW0GQR1XS
PF-382 NHLEUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHLTWM2OD1zLkW2PVYh|ryP MkiyV2FPT0WU
A101D MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX61WYRtUUN3ME2xMlU4OTF|IN88US=> NUPTXVlMW0GQR1XS
NB10 M3y1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP5b21KSzVyPUGuOVc{QTJizszN MkLtV2FPT0WU
NB5 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnGTWM2OD1zLkW4OFc3KM7:TR?= Mln1V2FPT0WU
HCE-4 MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTFwNkC4OUDPxE1? MWnTRW5ITVJ?
HT-144 NIHWWVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\lemZiUUN3ME2xMlY{OTlizszN MlLVV2FPT0WU
NCI-H524 Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLUTWM2OD1zLk[0N|A4KM7:TR?= MUjTRW5ITVJ?
NKM-1 M3HJPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\IN3NzUUN3ME2xMlY5PjZizszN MkHXV2FPT0WU
KURAMOCHI NIrNV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTV[phoUUN3ME2xMlY6PTd|IN88US=> MYPTRW5ITVJ?
NCI-H187 M3nPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELUZmJKSzVyPUGuO|AxOzZizszN MlHmV2FPT0WU
U-266 MkjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfMdlZKSzVyPUGuO|M5PDJizszN MnGwV2FPT0WU
BL-41 NX\B[YQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu4dVlKSzVyPUGuO|YzPzJizszN M3rkR3NCVkeHUh?=
SK-N-DZ MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHpbItKSzVyPUGuO|g{ODlizszN MojMV2FPT0WU
Daudi MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny5TWM2OD1zLke4PVY4KM7:TR?= NYLS[2tQW0GQR1XS
CPC-N M2\ScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPYU41KSzVyPUGuPFUxQTZizszN NWjWR21LW0GQR1XS
EM-2 NV6wVpRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn1b21WUUN3ME2xMlg2OSEQvF2= NX\ROYJmW0GQR1XS
HCC1187 NFrYUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFwOE[yOFEh|ryP MWfTRW5ITVJ?
LP-1 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITkV|BKSzVyPUGuPFcyPDNizszN MWjTRW5ITVJ?
CAS-1 M2HQdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfTOYNYUUN3ME2xMlk5Ojl7IN88US=> Mof6V2FPT0WU
NB7 NH[0dY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnaTWM2OD1{LkCwOVU2KM7:TR?= M4HjdXNCVkeHUh?=
VA-ES-BJ NH3aRmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3uOpQ2UUN3ME2yMlAyPTF|IN88US=> Ml\xV2FPT0WU
SNU-C2B M1;XcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fT[GlEPTB;Mj6wN|M2OSEQvF2= NHz1XWZUSU6JRWK=
LOXIMVI MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJwME[3PFYh|ryP Mn2zV2FPT0WU
NCI-H1581 MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYCyVmNRUUN3ME2yMlEyPTV7IN88US=> NHzLeoRUSU6JRWK=
IST-SL2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGCyV29KSzVyPUKuNVI1PDVizszN MV;TRW5ITVJ?
NOMO-1 MoL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYraR3FEUUN3ME2yMlE4Pjh|IN88US=> M{XoeXNCVkeHUh?=
TE-6 Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJwMUmwOUDPxE1? NWPGOIVIW0GQR1XS
NCI-H526 NGPsbmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJwMUmxOFEh|ryP NGfSZlJUSU6JRWK=
MSTO-211H NH3JO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHiz[nNKSzVyPUKuNlAxPDFizszN M{HFRnNCVkeHUh?=
LS-513 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvoU2M{UUN3ME2yMlIzOjZ7IN88US=> MYHTRW5ITVJ?
NCI-SNU-1 NFzJUFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP2TWM2OD1{LkOzNlU3KM7:TR?= NY\VWm84W0GQR1XS
BB65-RCC NILWWlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJwM{e0PVMh|ryP MUHTRW5ITVJ?
GT3TKB MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTFTWM2OD1{LkO5PVczKM7:TR?= M4rN[nNCVkeHUh?=
OS-RC-2 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D1RWlEPTB;Mj60NlM1OSEQvF2= M3nzbnNCVkeHUh?=
NCI-H2126 NXq5cGc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nH[2lEPTB;Mj60N|Y4PCEQvF2= MkDWV2FPT0WU
SK-UT-1 M4T6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYr5eJBxUUN3ME2yMlQ4PDZ5IN88US=> M3HuTHNCVkeHUh?=
DMS-114 NFSwOW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJwNkG1NlQh|ryP MXHTRW5ITVJ?
ONS-76 NGDFTJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwNkO2OFEh|ryP MV\TRW5ITVJ?
8-MG-BA Mmi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HVOWlEPTB;Mj62OVQyPCEQvF2= MU\TRW5ITVJ?
BOKU MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJwN{K3OlQh|ryP NEmwNY1USU6JRWK=
LAMA-84 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33aSGlEPTB;Mj63PVkyOiEQvF2= MoDuV2FPT0WU
ES1 M135TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XVO2lEPTB;Mj64NVgxPCEQvF2= M2DlPHNCVkeHUh?=
NCI-H1395 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly4TWM2OD1{LkiyNFEzKM7:TR?= NUPFW3E5W0GQR1XS
A388 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJwOU[xO{DPxE1? M3\4NHNCVkeHUh?=
NCCIT NYqxOo9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXBTWM2OD1|LkC4PFYzKM7:TR?= NHL2d4NUSU6JRWK=
HD-MY-Z NVnRXohlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC3TWM2OD1|LkGzNlA{KM7:TR?= MnrBV2FPT0WU
NCI-H510A MmH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTvTWM2OD1|LkG4PVQ{KM7:TR?= MknhV2FPT0WU
NCI-N87 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjZTWM2OD1|LkKwNFIh|ryP M4f4c3NCVkeHUh?=
SCLC-21H MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW4TZpKSzVyPUOuNlY5PTlizszN NYTPXmxpW0GQR1XS
SH-4 NGf4SIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:0TWM2OD1|LkK4O|k4KM7:TR?= NYXUTopVW0GQR1XS
QIMR-WIL NHK2SHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzRc|FKSzVyPUOuN|I5PDlizszN MljhV2FPT0WU
KM12 NU\s[4JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTNwM{O1OFQh|ryP NImyTFdUSU6JRWK=
ST486 M2P6e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LBTGlEPTB;Mz61N|g5OyEQvF2= MXPTRW5ITVJ?
HC-1 Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTNwNkKwNlgh|ryP M2[4cHNCVkeHUh?=
BV-173 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1roRmlEPTB;Mz62OFA5QCEQvF2= NFn3NHRUSU6JRWK=
EW-24 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPtW2VKSzVyPUOuOlY1OzRizszN NWTFWWh[W0GQR1XS
LU-65 M3fubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTNwNki3NUDPxE1? MoD1V2FPT0WU
ECC4 NYDCV4VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTNwN{e1OkDPxE1? NH[0OWhUSU6JRWK=
ARH-77 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfDSHVKSzVyPUSuNVExPjdizszN NWPXXYVmW0GQR1XS
BC-3 M1raSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfWT2JKSzVyPUSuNVMxPjhizszN MVTTRW5ITVJ?
SNB75 NGDQUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\EfGlEPTB;ND6yOlE6KM7:TR?= MoTkV2FPT0WU
MEG-01 M2\SUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rlU2lEPTB;ND6yO|QyQSEQvF2= NXTpUlVtW0GQR1XS
NCI-H1417 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;2TWM2OD12LkK4OFQ{KM7:TR?= NWHQS5RqW0GQR1XS
MDA-MB-134-VI MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jRNmlEPTB;ND6zNFYxOSEQvF2= NVLic4lKW0GQR1XS
Becker MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPLTWM2OD12LkS3N|M3KM7:TR?= MYfTRW5ITVJ?
DMS-153 M3XkeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fNdmlEPTB;ND62OlQ4PSEQvF2= MVzTRW5ITVJ?
TGBC1TKB M1v0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u1WWlEPTB;ND62PFUyPSEQvF2= NXLENGZtW0GQR1XS
EW-3 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:xV25NUUN3ME20Mlc3OjR6IN88US=> MoDxV2FPT0WU
KE-37 M3zuO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLLXIlKSzVyPUSuPFYyQTZizszN Ml\FV2FPT0WU
NCI-H23 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\NTWM2OD12Lki3NlI4KM7:TR?= NFvIT5hUSU6JRWK=
MC116 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTRwOUSxNlYh|ryP NITSWotUSU6JRWK=
NH-12 NYXEZoFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjEbGxKSzVyPUSuPVY1OzlizszN NGLKd4RUSU6JRWK=
CTB-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NICxZ2NKSzVyPUSuPVc4OjFizszN MVrTRW5ITVJ?
KM-H2 M1u3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETSbWhKSzVyPUWuNFU{OjNizszN MY\TRW5ITVJ?
MOLT-4 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTVwMUG4N{DPxE1? NEfSblRUSU6JRWK=
NCI-H2141 M4TMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnvb5l5UUN3ME21MlE1OjZ6IN88US=> MXHTRW5ITVJ?
EB-3 M3XpU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTVwMUe1NFQh|ryP MmrzV2FPT0WU
NCI-H1522 NFvKWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTVwMk[zNlIh|ryP M1XvfnNCVkeHUh?=
MRK-nu-1 M2jPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DIOWlEPTB;NT60N|Y{OyEQvF2= M3S0ZnNCVkeHUh?=
no-11 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfDSXdnUUN3ME21MlQ4ODh5IN88US=> NV;TVYw4W0GQR1XS
CESS M{nicGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTVwNUiwN|Qh|ryP NYDu[29QW0GQR1XS
KMOE-2 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjlOoxVUUN3ME21MlU5PjV7IN88US=> MYXTRW5ITVJ?
REH M37tSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;FOIdKSzVyPU[uNlU3OThizszN MUHTRW5ITVJ?
KU812 NGX1ZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUOxZZppUUN3ME22MlQzPzlzIN88US=> NV\rS3dTW0GQR1XS
SK-N-FI MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnR[VhCUUN3ME22MlYxPjd2IN88US=> M3j5WnNCVkeHUh?=
MMAC-SF MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TaOWlEPTB;Nz6wOlQ6OiEQvF2= NIDnfpZUSU6JRWK=
RCC10RGB M3\Y[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTtdYJOUUN3ME23MlIzQTd5IN88US=> MorRV2FPT0WU
NCI-H322M M3nT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33uPWlEPTB;Nz6zN|M{PSEQvF2= NWnVXllSW0GQR1XS
NB6 MoP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEniS4lKSzVyPUeuOVQ5QTlizszN M2DRbHNCVkeHUh?=
MN-60 NIDIU5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELGfWdKSzVyPUeuOlkzOTVizszN NVjRfZFLW0GQR1XS
NCI-H1092 NFfMW4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TxVGlEPTB;OD6wNVc{PCEQvF2= NWTHNWVYW0GQR1XS
EKVX MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRThwNEewOlYh|ryP NH3OO4tUSU6JRWK=
D-263MG MmniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRThwNUWzPVYh|ryP M2jhNHNCVkeHUh?=
NCI-H209 M2jLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:0d2lEPTB;OD62OFAxPiEQvF2= MX\TRW5ITVJ?
IST-SL1 MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTHfXJKSzVyPUiuPFk5QTJizszN NUDROVloW0GQR1XS
ACN NGnKeo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTlwMUmxOVch|ryP MUHTRW5ITVJ?
MHH-PREB-1 MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjPcYRKSzVyPUmuNlEzOTlizszN NGf6endUSU6JRWK=
EW-11 MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzwOIRRUUN3ME25MlY2Ozl4IN88US=> NI\lVYhUSU6JRWK=
KASUMI-1 NVXufYtwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XkcWlEPTB;OT63PFc4KM7:TR?= MkLUV2FPT0WU
KINGS-1 MlX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvGfJp6UUN3ME2xNE4zOzR5IN88US=> MWnTRW5ITVJ?
EVSA-T M{H5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljLTWM2OD1zMD6zNVkzKM7:TR?= NWD0Z5E1W0GQR1XS
DSH1 MmexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\VZmlEPTB;MUCuN|k4OiEQvF2= M4fnS3NCVkeHUh?=
COLO-824 NXrZRWVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFyLki2Olkh|ryP MkThV2FPT0WU
K052 M4\y[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTFyLkmzNlIh|ryP NV\lR2x[W0GQR1XS
SK-MEL-2 MnnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFyLkm5N|kh|ryP M17YbnNCVkeHUh?=

... 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 COC1=C(NC2=NC=C(Cl)C(=N2)NC3=C(C=CC=C3)[S](=O)(=O)C(C)C)C=CC(=C1)N4CCC(CC4)N5CCN(C)CC5

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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