TAE684 (NVP-TAE684)

Catalog No.S1108

For research use only.

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.

TAE684 (NVP-TAE684) Chemical Structure

CAS No. 761439-42-3

Selleck's TAE684 (NVP-TAE684) has been cited by 74 publications

Purity & Quality Control

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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 M1L2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXITWM2OD1yLkCwNFA3ODNizszN M2rmSnNCVkeHUh?=
SF539 NEXzXItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT2TWM2OD1yLkCwNFU3PCEQvF2= NITMem1USU6JRWK=
DEL NX7KWIx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwMECwPVI4KM7:TR?= MkDnV2FPT0WU
NB1 M4PXNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTBwMECxOlIh|ryP MYPTRW5ITVJ?
SR NIXrSolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwMECyO|ch|ryP M2TpcXNCVkeHUh?=
KARPAS-299 M{Dhdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Tu[WlEPTB;MD6wNlM5PCEQvF2= Mlm4V2FPT0WU
MHH-CALL-2 MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LtdGlEPTB;MD6wNlk2OiEQvF2= MYXTRW5ITVJ?
SU-DHL-1 NWTtb3FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[0TWM2OD1yLkC0PFY2KM7:TR?= Mn6wV2FPT0WU
A4-Fuk Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[zXmlEPTB;MD6wOVU3PSEQvF2= NEj3fHpUSU6JRWK=
EW-1 NWno[2FTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXrO2VvUUN3ME2wMlExOjV4IN88US=> M2TVe3NCVkeHUh?=
NOS-1 M{\mO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PHV2lEPTB;MD6xNFI6PCEQvF2= MVjTRW5ITVJ?
EW-16 MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXThPFBPUUN3ME2wMlExPTZ6IN88US=> MmHhV2FPT0WU
TE-11 NVrLNFRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDLdW9KSzVyPUCuNVYxQTZizszN NWPK[mxYW0GQR1XS
SW982 NFn1dFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrre|lFUUN3ME2wMlE3PDd6IN88US=> Mm\XV2FPT0WU
LAN-6 MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknTTWM2OD1yLkG3OFQ{KM7:TR?= MnnQV2FPT0WU
MZ1-PC M2HYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMUe4N|Uh|ryP MVfTRW5ITVJ?
KS-1 MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrwOGR7UUN3ME2wMlE6OzR|IN88US=> M1\yZnNCVkeHUh?=
PSN1 NEjwTnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfhTWM2OD1yLkG5OlMyKM7:TR?= NYrjN5RiW0GQR1XS
LC-2-ad NH65[IpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHWR2pKUUN3ME2wMlE6Pjl{IN88US=> Mmr2V2FPT0WU
COLO-320-HSR M{jBZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7KcG5KSzVyPUCuNVk4PzZizszN NV3WNGtKW0GQR1XS
OPM-2 M2LQe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3qzZmlEPTB;MD6yNlY3QSEQvF2= NGT0dlRUSU6JRWK=
SK-NEP-1 M1SwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ziOmlEPTB;MD6yN|UzPCEQvF2= MortV2FPT0WU
ALL-PO NGS5PIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELtcGhKSzVyPUCuNlQ2OjRizszN NEDVPIpUSU6JRWK=
CMK NYTkdW1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLzc3RKSzVyPUCuNlU2OyEQvF2= MVfTRW5ITVJ?
NCI-H1648 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DBSGlEPTB;MD6yO|g2PSEQvF2= M4rEOnNCVkeHUh?=
SIG-M5 NUT1RnZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXDTWM2OD1yLkK5NVU6KM7:TR?= NFzJZ|NUSU6JRWK=
TGBC24TKB MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwM{CyNVgh|ryP MX\TRW5ITVJ?
DOHH-2 MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnkbINlUUN3ME2wMlMyOjB2IN88US=> MmHzV2FPT0WU
NB69 M3fGZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwM{G3PFch|ryP MWHTRW5ITVJ?
MFH-ino NXPhRWRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HJOmlEPTB;MD6zNlUzOyEQvF2= NYjTdoxMW0GQR1XS
KP-N-RT-BM-1 MmX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwM{OxNlMh|ryP MV3TRW5ITVJ?
MONO-MAC-6 NFmwb3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFy5bIpKSzVyPUCuN|MzQTFizszN MULTRW5ITVJ?
ATN-1 NEPCZpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvkR4c6UUN3ME2wMlM{OzB|IN88US=> M{TQWnNCVkeHUh?=
NTERA-S-cl-D1 NHPSV3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEThcpVKSzVyPUCuN|M{QTZizszN MUXTRW5ITVJ?
L-540 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn5TWM2OD1yLkO2PVg5KM7:TR?= M4j4O3NCVkeHUh?=
GB-1 NWLQWGdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;UZWlEPTB;MD6zPFg3PyEQvF2= MYfTRW5ITVJ?
MV-4-11 MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O2[2lEPTB;MD6zPVQ1PiEQvF2= MV\TRW5ITVJ?
KG-1 MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzlVpBKSzVyPUCuN|k2PjFizszN MkXxV2FPT0WU
OVCAR-4 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnMT3V2UUN3ME2wMlQxPTZ7IN88US=> M{XSU3NCVkeHUh?=
NEC8 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTBwNEGyPVIh|ryP MoXOV2FPT0WU
SK-MM-2 NEjKdY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3zVW5YUUN3ME2wMlQyPjB7IN88US=> MV3TRW5ITVJ?
TE-8 M3rkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPPTWM2OD1yLkSyPFgh|ryP MWDTRW5ITVJ?
697 NGLUVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwNEOyNVUh|ryP NXrMWWdvW0GQR1XS
NB14 NEPXfmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwNEO4NlYh|ryP NGTvTYxUSU6JRWK=
GDM-1 MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXCb|JKSzVyPUCuOFcyOTZizszN Mm[0V2FPT0WU
HUTU-80 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zZTmlEPTB;MD60O|M4PSEQvF2= NYP1T45XW0GQR1XS
HL-60 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X6UGlEPTB;MD60PFE1OiEQvF2= MWXTRW5ITVJ?
OCI-AML2 NUDQTHpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwNEizNlgh|ryP NFi1VG5USU6JRWK=
ML-2 NHvyNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmO3TWM2OD1yLkS5NFMyKM7:TR?= MkSwV2FPT0WU
ES4 M1;vZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwNEmxNFkh|ryP NFPSVm5USU6JRWK=
NCI-H747 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwNEm4PUDPxE1? MoPHV2FPT0WU
RL95-2 MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfLOVdKSzVyPUCuOVAyOTJizszN MnjWV2FPT0WU
TE-15 NGCxVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwNUGxNlQh|ryP NELMeGlUSU6JRWK=
TE-12 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nIRmlEPTB;MD61N|M1QSEQvF2= NE[yZYpUSU6JRWK=
LB1047-RCC M1jWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEntR5NKSzVyPUCuOVQ2PDlizszN NV;G[oJTW0GQR1XS
LB831-BLC M{WzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HPTGlEPTB;MD61OVAzOyEQvF2= NWLJWZFwW0GQR1XS
NCI-H1355 NXTrRnBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Lub2lEPTB;MD61OVE5PCEQvF2= NWLxSHlNW0GQR1XS
CTV-1 NE\meo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u4emlEPTB;MD61OVYzPCEQvF2= NXy2V2dZW0GQR1XS
RXF393 NHHpcVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwNUW3PVQh|ryP MYrTRW5ITVJ?
SW872 M4XXVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:5cGlEPTB;MD61OlczPCEQvF2= NUezTlVMW0GQR1XS
MPP-89 NHz3ZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwNUe4PFQh|ryP M3i3PHNCVkeHUh?=
RPMI-8226 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X4fWlEPTB;MD62N|UzPiEQvF2= NEjHd|ZUSU6JRWK=
LS-1034 Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37SS2lEPTB;MD62N|U5KM7:TR?= NGrUTnFUSU6JRWK=
SJSA-1 M3TidGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXZdWZ1UUN3ME2wMlY{PzJ3IN88US=> M2DIOHNCVkeHUh?=
HOP-62 MoP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjkSYlZUUN3ME2wMlY2ODN|IN88US=> MXfTRW5ITVJ?
KGN M2TjRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\CfmlEPTB;MD62OlE3QCEQvF2= NWnPNHVoW0GQR1XS
D-336MG M{fFcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfXN201UUN3ME2wMlY3OTZ7IN88US=> MXnTRW5ITVJ?
LS-411N MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwNke0OlIh|ryP NHK1VVJUSU6JRWK=
TE-1 M4e2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{OxW2lEPTB;MD62PVA4PCEQvF2= NV:4cpZoW0GQR1XS
LB996-RCC NXjOUYp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfvdXMxUUN3ME2wMlY6Ozh7IN88US=> NUTYT2xRW0GQR1XS
TE-10 M2rGZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nyXGlEPTB;MD63NVQ6PiEQvF2= NIfHTWhUSU6JRWK=
NCI-SNU-16 MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwN{K2OlQh|ryP MmDPV2FPT0WU
ES8 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LHXGlEPTB;MD63OFk4PSEQvF2= MUDTRW5ITVJ?
COLO-800 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwN{[2PVUh|ryP M1K2Z3NCVkeHUh?=
ES6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHmcoRpUUN3ME2wMlc4PTV7IN88US=> MmfoV2FPT0WU
L-363 NXrUWmVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fHWWlEPTB;MD64NlM4PSEQvF2= NWXlXFRuW0GQR1XS
NMC-G1 NEfsWnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETUU|hKSzVyPUCuPFMzOzNizszN M1HXV3NCVkeHUh?=
LU-134-A M3P3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwOEO5NVIh|ryP NWPFZVhFW0GQR1XS
SF268 Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTLUIVKSzVyPUCuPFQxPDJizszN MWPTRW5ITVJ?
KARPAS-45 MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwOESyOlMh|ryP NFewO|NUSU6JRWK=
TGW NFHxO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPYTWM2OD1yLki1PFY{KM7:TR?= M2Ds[nNCVkeHUh?=
CHP-126 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2no[mlEPTB;MD64OVk2PyEQvF2= NXrkbI9QW0GQR1XS
MOLT-16 M1m3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nVPWlEPTB;MD64O|U5QSEQvF2= NHrY[JNUSU6JRWK=
LB771-HNC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTkTWM2OD1yLki5O|U4KM7:TR?= NYHpSXRVW0GQR1XS
NALM-6 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3CTWM2OD1yLkmwO|M6KM7:TR?= MofGV2FPT0WU
GCIY NYHLXWp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\PbFRKSzVyPUCuPVU2OjZizszN M3T1RXNCVkeHUh?=
IST-MES1 NWTMe3E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xqe2lEPTB;MD65PFgzPCEQvF2= NXz6WVNjW0GQR1XS
LB2241-RCC NX;5fVY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnqdGtKSzVyPUCuPVg5PCEQvF2= MkfXV2FPT0WU
BL-70 NWLMbYl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\Yd|J4UUN3ME2wMlk6PTN3IN88US=> M{DCWHNCVkeHUh?=
NB17 M{niU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HXdmlEPTB;MT6wNFY{QSEQvF2= M1jJUnNCVkeHUh?=
LXF-289 NVO3dWlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojaTWM2OD1zLkCzNFc3KM7:TR?= M3\hN3NCVkeHUh?=
TK10 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7TTWM2OD1zLkC1NFY{KM7:TR?= NVT3Voc5W0GQR1XS
K5 M4PMWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTFwME[yO|Qh|ryP Mn3BV2FPT0WU
NCI-H716 NGi4W|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonYTWM2OD1zLkC3NlU6KM7:TR?= NGL6d2pUSU6JRWK=
HCE-T MkCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;4XmVKSzVyPUGuNFg5OTlizszN NHrhUFhUSU6JRWK=
GI-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTZeFNKSzVyPUGuNFk4QThizszN NXHDUY9wW0GQR1XS
KARPAS-422 M3LZNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jZR2lEPTB;MT6xNFAzOiEQvF2= MmXOV2FPT0WU
TE-9 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[zcolKSzVyPUGuNVE{OjhizszN NV\1XnFtW0GQR1XS
SF126 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwMUG1Olgh|ryP MlexV2FPT0WU
BB30-HNC Mmi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DR[WlEPTB;MT6xN|EyOiEQvF2= M4C2eHNCVkeHUh?=
NCI-H1304 NYXFflF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFwMUOzN|gh|ryP M4DUVnNCVkeHUh?=
HEL MmjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDqTFBKSzVyPUGuNVQ5QTVizszN MVzTRW5ITVJ?
HAL-01 M3\3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r5emlEPTB;MT6xOVI5OyEQvF2= MXrTRW5ITVJ?
SK-LMS-1 NFrJcJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGW0XmdKSzVyPUGuNVU6PzRizszN MWnTRW5ITVJ?
SW954 NEPkTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLmd3hyUUN3ME2xMlE6PTZ5IN88US=> MnWxV2FPT0WU
D-283MED NXvqTIo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\EbJMzUUN3ME2xMlIzOzd7IN88US=> MWnTRW5ITVJ?
NCI-H1882 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7MTWM2OD1zLkKzPFkh|ryP NEiyVIZUSU6JRWK=
GI-ME-N MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwMkWyNFgh|ryP Mnu3V2FPT0WU
SK-PN-DW MnXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwMk[zOFgh|ryP NEPSZpBUSU6JRWK=
C2BBe1 NV7Hd3lTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L3bmlEPTB;MT6yPVEyPyEQvF2= M{G5PHNCVkeHUh?=
A704 MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUn5UpVPUUN3ME2xMlMzPjh7IN88US=> MUnTRW5ITVJ?
KALS-1 NWX5dlRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTWTWM2OD1zLkO0NFgh|ryP MXLTRW5ITVJ?
ETK-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TrR2lEPTB;MT6zOFQ5QSEQvF2= NI[zXVJUSU6JRWK=
LB647-SCLC MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjoTWM2OD1zLkO0PVg3KM7:TR?= M1jSPHNCVkeHUh?=
OCUB-M MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr1TWM2OD1zLkO2NVQ{KM7:TR?= MVPTRW5ITVJ?
NCI-H720 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zZXWlEPTB;MT6zOlM4QCEQvF2= NYTFOpQ5W0GQR1XS
NB13 NIjaR4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwM{eyPVMh|ryP NUnwTZhVW0GQR1XS
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LS-123 M2\ScWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPzTWM2OD1zLkWxOVk1KM7:TR?= NVHDZYxvW0GQR1XS
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PF-382 NFXpU5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwNU[5OkDPxE1? MV7TRW5ITVJ?
A101D NEH3bo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLBbmc1UUN3ME2xMlU4OTF|IN88US=> NF\VVYtUSU6JRWK=
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NB5 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFwNUi0O|Yh|ryP Mk\OV2FPT0WU
HCE-4 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFwNkC4OUDPxE1? MmLKV2FPT0WU
HT-144 NHnJVGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfYcFRKSzVyPUGuOlMyQSEQvF2= MXfTRW5ITVJ?
NCI-H524 NV:wZVZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrhS5RoUUN3ME2xMlY1OzB5IN88US=> NHLkXFVUSU6JRWK=
NKM-1 NH;Q[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzRZ4ViUUN3ME2xMlY5PjZizszN MX;TRW5ITVJ?
KURAMOCHI M3TwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYr5N3o4UUN3ME2xMlY6PTd|IN88US=> NFzsUHVUSU6JRWK=
NCI-H187 NFy3XHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW3[nE6UUN3ME2xMlcxODN4IN88US=> NU\lV4N2W0GQR1XS
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NCI-H1581 NUfXUm1IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe1eIk1UUN3ME2yMlEyPTV7IN88US=> NF\F[IpUSU6JRWK=
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NCI-H526 NFnnTlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJwMUmxOFEh|ryP NU\yNJoxW0GQR1XS
MSTO-211H NVT1clN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInYcm5KSzVyPUKuNlAxPDFizszN NH3OSYNUSU6JRWK=
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NCI-SNU-1 NFfuVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PWUGlEPTB;Mj6zN|I2PiEQvF2= M{LsPHNCVkeHUh?=
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NCI-H2126 NFLlU5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL3WlVKSzVyPUKuOFM3PzRizszN MkS0V2FPT0WU
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DMS-114 M1TPfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJwNkG1NlQh|ryP NEj2d49USU6JRWK=
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NCI-H1395 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTJwOEKwNVIh|ryP M{LLfXNCVkeHUh?=
A388 NGLTfItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHpTWM2OD1{Lkm2NVch|ryP NXrBflhZW0GQR1XS
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NCI-H1417 NVrNdo5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr3d2VKSzVyPUSuNlg1PDNizszN NFLTfW5USU6JRWK=
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Becker NXq1V2pbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;zTGpKSzVyPUSuOFc{OzZizszN MX;TRW5ITVJ?
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TGBC1TKB MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XRS2lEPTB;ND62PFUyPSEQvF2= M17Dc3NCVkeHUh?=
EW-3 NEnXeINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fqXmlEPTB;ND63OlI1QCEQvF2= MmnVV2FPT0WU
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NCI-H23 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTRwOEeyNlch|ryP NUfnT|VRW0GQR1XS
MC116 NXHWVVF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\mfWptUUN3ME20Mlk1OTJ4IN88US=> NETxO3JUSU6JRWK=
NH-12 NF;DU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTRwOU[0N|kh|ryP MmDsV2FPT0WU
CTB-1 NFfWSXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnvdZVFUUN3ME20Mlk4PzJzIN88US=> M2XHXnNCVkeHUh?=
KM-H2 MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K4fGlEPTB;NT6wOVMzOyEQvF2= NHnRNlFUSU6JRWK=
MOLT-4 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDGTWM2OD13LkGxPFMh|ryP NWXXdGdLW0GQR1XS
NCI-H2141 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILzVnRKSzVyPUWuNVQzPjhizszN NV7NOmZ1W0GQR1XS
EB-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jFdWlEPTB;NT6xO|UxPCEQvF2= MljmV2FPT0WU
NCI-H1522 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XPS2lEPTB;NT6yOlMzOiEQvF2= M2\Yb3NCVkeHUh?=
MRK-nu-1 MoOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLWOGZKSzVyPUWuOFM3OzNizszN MnvKV2FPT0WU
no-11 NYnNcmVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTVwNEewPFch|ryP NUfIS45NW0GQR1XS
CESS NIjaTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:wWlJOUUN3ME21MlU5ODN2IN88US=> MVTTRW5ITVJ?
KMOE-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTVwNUi2OVkh|ryP NHz3enRUSU6JRWK=
REH NIH6UnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LpfGlEPTB;Nj6yOVYyQCEQvF2= MWjTRW5ITVJ?
KU812 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjZPJlKSzVyPU[uOFI4QTFizszN NH;6XFZUSU6JRWK=
SK-N-FI MkWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DjeGlEPTB;Nj62NFY4PCEQvF2= MWPTRW5ITVJ?
MMAC-SF Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrLOllGUUN3ME23MlA3PDl{IN88US=> MnG0V2FPT0WU
RCC10RGB NXrhOGFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn3R4pvUUN3ME23MlIzQTd5IN88US=> NYXYNplIW0GQR1XS
NCI-H322M M4rKN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzn[VNKSzVyPUeuN|M{OzVizszN MUHTRW5ITVJ?
NB6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{iyO2lEPTB;Nz61OFg6QSEQvF2= NWjxO|IyW0GQR1XS
MN-60 NVvWflNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPWR5NKSzVyPUeuOlkzOTVizszN MVTTRW5ITVJ?
NCI-H1092 NX\QVmxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q0W2lEPTB;OD6wNVc{PCEQvF2= M1zVbHNCVkeHUh?=
EKVX NFH3dnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HOdWlEPTB;OD60O|A3PiEQvF2= NYrSU|hIW0GQR1XS
D-263MG M2HHN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXYTWM2OD16LkW1N|k3KM7:TR?= M3\BeXNCVkeHUh?=
NCI-H209 NHLL[olIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn63TWM2OD16Lk[0NFA3KM7:TR?= NF;nO|JUSU6JRWK=
IST-SL1 NIPrSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3vWox3UUN3ME24Mlg6QDl{IN88US=> MYfTRW5ITVJ?
ACN Ml\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm1UHlKSzVyPUmuNVkyPTdizszN NYrMO5l{W0GQR1XS
MHH-PREB-1 NFX1[VVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PtbWlEPTB;OT6yNVIyQSEQvF2= NUGxO29qW0GQR1XS
EW-11 NXzBWHNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\FW3ZKSzVyPUmuOlU{QTZizszN M3vyenNCVkeHUh?=
KASUMI-1 NWHSd5NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHz[lBHUUN3ME25Mlc5PzdizszN NVjRbmg1W0GQR1XS
KINGS-1 NXW4bGVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTNTWM2OD1zMD6yN|Q4KM7:TR?= MorYV2FPT0WU
EVSA-T MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nxPGlEPTB;MUCuN|E6OiEQvF2= M2P2VnNCVkeHUh?=
DSH1 NUfmdppST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULURYFuUUN3ME2xNE4{QTd{IN88US=> MlL4V2FPT0WU
COLO-824 NXfrVGViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTFyLki2Olkh|ryP Mn\aV2FPT0WU
K052 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFyLkmzNlIh|ryP M1TTVHNCVkeHUh?=
SK-MEL-2 MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XiV2lEPTB;MUCuPVk{QSEQvF2= MmXMV2FPT0WU
Assay
Methods Test Index PMID
Western blot p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP ; p-ROS1 / ROS1 22240786 25351743
Growth inhibition assay Cell viability 18594010
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 614.2
Formula

C30H40ClN7O3S

CAS No. 761439-42-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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