TAE684 (NVP-TAE684)

Catalog No.S1108

TAE684 (NVP-TAE684) Chemical Structure

Molecular Weight(MW): 614.2

TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR.

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  • (A) H3122 xenografts harboring the EML4-ALK translocation were treated with control vehicle or the ALK inhibitor, TAE-684, for 2 days; the tumors were excised and lysates were prepared. The TIMM results for the control and treated animals are shown. (B) H3122 cells were treated in the presence or absence of TAE-684 (100 nM) for 6 hours in the presence or absence of the indicated ligands [EGF (50 ng/mL), IGF1 (50 ng/mL), and HGF (50 ng/mL)]. Extracts were probed with the indicated antibodies.

    Cancer Res 2011 71, 4920-31. TAE684 (NVP-TAE684) purchased from Selleck.

    Therapeutic effects of ALK inhibitor TAE684 on H694R- and E1384K-mediated tumorigenesis of H1299 transfectants. (B) Dosage effects of TAE684 on phospho-Y1604 ALK expression of wild-type, H694R, and E1384K transfectants by Western blot analysis (top panel). Quantitative results of phospho-Y1604 ALK intensity are also (bottom panel).

    Neoplasia 2011 13, 704-15. TAE684 (NVP-TAE684) purchased from Selleck.

  • Therapeutic effects of ALK inhibitor TAE684 on H694R- and E1384K-mediated tumorigenesis of H1299 transfectants. (C) Suppressive effects of TAE684 on H694R- and E1384K-induced tumors in vivo. Photographs and tumor growth curves are shown in the top and bottom panels, respectively (four mice per group).

    Neoplasia 2011 13, 704-15. TAE684 (NVP-TAE684) purchased from Selleck.

    Therapeutic effects of ALK inhibitor TAE684 on H694R- and E1384K-mediated tumorigenesis of H1299 transfectants. (A) Dosage effects of TAE684 on H694R- and E1384K-induced cell proliferation measured with WST-1 activity. 

    Neoplasia 2011 13, 704-15. TAE684 (NVP-TAE684) purchased from Selleck.

Purity & Quality Control

Choose Selective ALK Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFezcINKSzVyPUCuNFAxODZyMzFOwG0> M4LIUnNCVkeHUh?=
SF539 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzOTWM2OD1yLkCwNFU3PCEQvF2= NEfrT|JUSU6JRWK=
DEL M3;MSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXUSW9UUUN3ME2wMlAxODl{NzFOwG0> NHLZWmpUSU6JRWK=
NB1 NGjaTmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrMTWM2OD1yLkCwNVYzKM7:TR?= M2jCWnNCVkeHUh?=
SR NYTvXZR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1u5T2lEPTB;MD6wNFI4PyEQvF2= NUjKPXFTW0GQR1XS
KARPAS-299 NUj6TWdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXlU4dKSzVyPUCuNFI{QDRizszN MnvhV2FPT0WU
MHH-CALL-2 NYXRfZJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwMEK5OVIh|ryP MnnpV2FPT0WU
SU-DHL-1 NW\jRWNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorjTWM2OD1yLkC0PFY2KM7:TR?= MV7TRW5ITVJ?
A4-Fuk NV[3N3dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwMEW1OlUh|ryP NGj2XoNUSU6JRWK=
EW-1 MmjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\idWZKSzVyPUCuNVAzPTZizszN MXPTRW5ITVJ?
NOS-1 NHXxe2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjXe3RLUUN3ME2wMlExOjl2IN88US=> MY\TRW5ITVJ?
EW-16 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELFe3NKSzVyPUCuNVA2PjhizszN MUXTRW5ITVJ?
TE-11 MonYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ixZWlEPTB;MD6xOlA6PiEQvF2= MU\TRW5ITVJ?
SW982 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHLPW1KSzVyPUCuNVY1PzhizszN MnjGV2FPT0WU
LAN-6 NUTiPGJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTBwMUe0OFMh|ryP NVfFdG5xW0GQR1XS
MZ1-PC NGDFdVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwMUe4N|Uh|ryP NVLSUnVwW0GQR1XS
KS-1 NID4[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu0[XJKSzVyPUCuNVk{PDNizszN M{PIcXNCVkeHUh?=
PSN1 M{DHW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwMUm2N|Eh|ryP M{Tu[3NCVkeHUh?=
LC-2-ad M3rs[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMUm2PVIh|ryP MVrTRW5ITVJ?
COLO-320-HSR MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\mXmlEPTB;MD6xPVc4PiEQvF2= MVXTRW5ITVJ?
OPM-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rOXmlEPTB;MD6yNlY3QSEQvF2= M32xO3NCVkeHUh?=
SK-NEP-1 M1PGU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\nT2lEPTB;MD6yN|UzPCEQvF2= NFT2epJUSU6JRWK=
ALL-PO MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NECwVGdKSzVyPUCuNlQ2OjRizszN MmexV2FPT0WU
CMK NU\QRVIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\2TWM2OD1yLkK1OVMh|ryP M1LkZXNCVkeHUh?=
NCI-H1648 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr6PJpCUUN3ME2wMlI4QDV3IN88US=> MkLZV2FPT0WU
SIG-M5 NEHXfZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWeyU|VyUUN3ME2wMlI6OTV7IN88US=> NILNbmlUSU6JRWK=
TGBC24TKB MnP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnHWYdKSzVyPUCuN|AzOThizszN NG\4UHJUSU6JRWK=
DOHH-2 NEfieYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTnR|doUUN3ME2wMlMyOjB2IN88US=> MonIV2FPT0WU
NB69 NFPpSoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHryWoxKSzVyPUCuN|E4QDdizszN MUnTRW5ITVJ?
MFH-ino MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwM{K1NlMh|ryP MoHKV2FPT0WU
KP-N-RT-BM-1 NH\BXopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwM{OxNlMh|ryP MUXTRW5ITVJ?
MONO-MAC-6 M3yyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Ps[mlEPTB;MD6zN|I6OSEQvF2= NIPoSI1USU6JRWK=
ATN-1 M3P6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHiW3VnUUN3ME2wMlM{OzB|IN88US=> MVHTRW5ITVJ?
NTERA-S-cl-D1 NWf0e21HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\5eFdKSzVyPUCuN|M{QTZizszN Moi0V2FPT0WU
L-540 NWnUTFJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjSTWM2OD1yLkO2PVg5KM7:TR?= NHewNo9USU6JRWK=
GB-1 NVLFXIx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT6TWM2OD1yLkO4PFY4KM7:TR?= MnjNV2FPT0WU
MV-4-11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDRTWM2OD1yLkO5OFQ3KM7:TR?= NVu1THJtW0GQR1XS
KG-1 NVnweIxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rLeWlEPTB;MD6zPVU3OSEQvF2= NEe5SplUSU6JRWK=
OVCAR-4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwNEC1Olkh|ryP M1PQOHNCVkeHUh?=
NEC8 NIXOd3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\2WWR[UUN3ME2wMlQyOjl{IN88US=> NH7jdWhUSU6JRWK=
SK-MM-2 NGnwWXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwNEG2NFkh|ryP MUfTRW5ITVJ?
TE-8 NXvOVpd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwNEK4PEDPxE1? M4q3RnNCVkeHUh?=
697 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwNEOyNVUh|ryP NFnQSoxUSU6JRWK=
NB14 MlLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnv4TWM2OD1yLkSzPFI3KM7:TR?= MoO4V2FPT0WU
GDM-1 NInJNYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGzbZlJUUN3ME2wMlQ4OTF4IN88US=> MX3TRW5ITVJ?
HUTU-80 NVvQUG5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;GTWM2OD1yLkS3N|c2KM7:TR?= M2PaeXNCVkeHUh?=
HL-60 NH;C[INIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfNc49KSzVyPUCuOFgyPDJizszN NXHBfol7W0GQR1XS
OCI-AML2 MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\OdFlKSzVyPUCuOFg{OjhizszN MVPTRW5ITVJ?
ML-2 M2PvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jrN2lEPTB;MD60PVA{OSEQvF2= MmPHV2FPT0WU
ES4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3oVoxLUUN3ME2wMlQ6OTB7IN88US=> NF7mfmNUSU6JRWK=
NCI-H747 MonuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vmbWlEPTB;MD60PVg6KM7:TR?= MknXV2FPT0WU
RL95-2 NXfMVFR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC1VpJwUUN3ME2wMlUxOTF{IN88US=> MWDTRW5ITVJ?
TE-15 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL6TWM2OD1yLkWxNVI1KM7:TR?= M1zofHNCVkeHUh?=
TE-12 NWrvcGpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOyeYF3UUN3ME2wMlU{OzR7IN88US=> M3fGUHNCVkeHUh?=
LB1047-RCC M3TVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEP0cXJKSzVyPUCuOVQ2PDlizszN MmP3V2FPT0WU
LB831-BLC NILq[GdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1L1fGlEPTB;MD61OVAzOyEQvF2= M17iTHNCVkeHUh?=
NCI-H1355 NFjsUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rCPGlEPTB;MD61OVE5PCEQvF2= MX;TRW5ITVJ?
CTV-1 MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNUW2NlQh|ryP MXvTRW5ITVJ?
RXF393 M3XUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\U[mlEPTB;MD61OVc6PCEQvF2= MWfTRW5ITVJ?
SW872 MkLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXHWGVrUUN3ME2wMlU3PzJ2IN88US=> NWK2U4FsW0GQR1XS
MPP-89 M3jjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHoXJdDUUN3ME2wMlU4QDh2IN88US=> NX3venNEW0GQR1XS
RPMI-8226 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwNkO1NlYh|ryP NE\Rd5BUSU6JRWK=
LS-1034 M2m3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwNkO1PEDPxE1? NVTlXFk4W0GQR1XS
SJSA-1 M3e4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{i1PWlEPTB;MD62N|czPSEQvF2= MoDqV2FPT0WU
HOP-62 NVW3bFdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rYRmlEPTB;MD62OVA{OyEQvF2= Mn\rV2FPT0WU
KGN M1zDOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES3NGpKSzVyPUCuOlYyPjhizszN MkHvV2FPT0WU
D-336MG NGXUWWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwNk[xOlkh|ryP NHnGS2pUSU6JRWK=
LS-411N M37BZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;xfWlEPTB;MD62O|Q3OiEQvF2= MXzTRW5ITVJ?
TE-1 NVW4bmxET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml71TWM2OD1yLk[5NFc1KM7:TR?= M1nFdnNCVkeHUh?=
LB996-RCC M{PBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlq5TWM2OD1yLk[5N|g6KM7:TR?= M1TXSXNCVkeHUh?=
TE-10 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zKOGlEPTB;MD63NVQ6PiEQvF2= MkHGV2FPT0WU
NCI-SNU-16 M3LtW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXYcXVKSzVyPUCuO|I3PjRizszN MUPTRW5ITVJ?
ES8 M33BR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nxVmlEPTB;MD63OFk4PSEQvF2= MYnTRW5ITVJ?
COLO-800 Mn\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37ob2lEPTB;MD63OlY6PSEQvF2= M4e5eXNCVkeHUh?=
ES6 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnQWFNxUUN3ME2wMlc4PTV7IN88US=> MXvTRW5ITVJ?
L-363 NGPaWmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwOEKzO|Uh|ryP MoPiV2FPT0WU
NMC-G1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rDW2lEPTB;MD64N|I{OyEQvF2= NVTRToRCW0GQR1XS
LU-134-A MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwOEO5NVIh|ryP Mm\RV2FPT0WU
SF268 NGPK[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL5S4hKSzVyPUCuPFQxPDJizszN NILiSFNUSU6JRWK=
KARPAS-45 MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1G3cWlEPTB;MD64OFI3OyEQvF2= NX\aXnhOW0GQR1XS
TGW NWDmUppFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PtNmlEPTB;MD64OVg3OyEQvF2= NYXxepE2W0GQR1XS
CHP-126 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLSbYN5UUN3ME2wMlg2QTV5IN88US=> NYDSV45kW0GQR1XS
MOLT-16 NXTLZ41XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDHTWM2OD1yLki3OVg6KM7:TR?= NHz5bo1USU6JRWK=
LB771-HNC NIDiXXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwOEm3OVch|ryP NFvJ[XNUSU6JRWK=
NALM-6 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPYTY5KSzVyPUCuPVA4OzlizszN MWTTRW5ITVJ?
GCIY NHLvSZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwOUW1NlYh|ryP MmLRV2FPT0WU
IST-MES1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rETmlEPTB;MD65PFgzPCEQvF2= MoHYV2FPT0WU
LB2241-RCC M1\jOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7Hc|dKSzVyPUCuPVg5PCEQvF2= Mn[4V2FPT0WU
BL-70 NGraVndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[0[HdKSzVyPUCuPVk2OzVizszN NFu2WFNUSU6JRWK=
NB17 NX7iXplLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XGSmlEPTB;MT6wNFY{QSEQvF2= NXW0U3ZPW0GQR1XS
LXF-289 M{D4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPFZoRwUUN3ME2xMlA{ODd4IN88US=> NHThXVlUSU6JRWK=
TK10 NULuXW0{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTFwMEWwOlMh|ryP M2nBVXNCVkeHUh?=
K5 MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfOUlBKSzVyPUGuNFYzPzRizszN MXXTRW5ITVJ?
NCI-H716 MkWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLhTWM2OD1zLkC3NlU6KM7:TR?= M1;YeXNCVkeHUh?=
HCE-T MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzSVIRvUUN3ME2xMlA5QDF7IN88US=> MoTvV2FPT0WU
GI-1 MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoKwTWM2OD1zLkC5O|k5KM7:TR?= MmfLV2FPT0WU
KARPAS-422 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwMUCwNlIh|ryP M4nWenNCVkeHUh?=
TE-9 NWHhTYhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MniwTWM2OD1zLkGxN|I5KM7:TR?= M3jBcnNCVkeHUh?=
SF126 M3jlU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwMUG1Olgh|ryP NVrkN49QW0GQR1XS
BB30-HNC NV\KTINFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHObm96UUN3ME2xMlE{OTF{IN88US=> MnT5V2FPT0WU
NCI-H1304 M37xOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTsVW9zUUN3ME2xMlE{OzN6IN88US=> NIfI[GZUSU6JRWK=
HEL M3\teGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWKybIJOUUN3ME2xMlE1QDl3IN88US=> NGS1RoNUSU6JRWK=
HAL-01 NXPpe5B6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[1TWM2OD1zLkG1Nlg{KM7:TR?= MWrTRW5ITVJ?
SK-LMS-1 MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm1dXRKSzVyPUGuNVU6PzRizszN NF3HZ25USU6JRWK=
SW954 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf2TWM2OD1zLkG5OVY4KM7:TR?= M3XFPHNCVkeHUh?=
D-283MED M{C1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwMkKzO|kh|ryP MV7TRW5ITVJ?
NCI-H1882 NIrjdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr6TWM2OD1zLkKzPFkh|ryP MYfTRW5ITVJ?
GI-ME-N NIrlUlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjTZnpKSzVyPUGuNlUzODhizszN M4LkVHNCVkeHUh?=
SK-PN-DW M4DYSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwMk[zOFgh|ryP MYTTRW5ITVJ?
C2BBe1 M4TUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTFwMkmxNVch|ryP Mo\sV2FPT0WU
A704 NEi0SHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrFbVdrUUN3ME2xMlMzPjh7IN88US=> NU[xO2w5W0GQR1XS
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ETK-1 M{LzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nCN2lEPTB;MT6zOFQ5QSEQvF2= NF[wSHdUSU6JRWK=
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OCUB-M M{TFUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnBUXdKSzVyPUGuN|YyPDNizszN M1vpOnNCVkeHUh?=
NCI-H720 NW[2NnR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTFwM{[zO|gh|ryP MX3TRW5ITVJ?
NB13 NGL3SJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnHOlZKSzVyPUGuN|czQTNizszN MnPjV2FPT0WU
GR-ST NESwZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln5TWM2OD1zLkO4O|U4KM7:TR?= M1zkc3NCVkeHUh?=
DU-4475 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y0d2lEPTB;MT60OVg2OyEQvF2= MXnTRW5ITVJ?
HCC2157 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vqT2lEPTB;MT60OlY2QSEQvF2= M4nFUHNCVkeHUh?=
RKO NIK0SGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFwNEm5NlIh|ryP M{\QXnNCVkeHUh?=
LS-123 Ml21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\SS2dmUUN3ME2xMlUyPTl2IN88US=> NFvOZppUSU6JRWK=
NCI-H69 NVXDbmk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TBU2lEPTB;MT61OVgyOSEQvF2= MYPTRW5ITVJ?
SW962 MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwNU[xN{DPxE1? NVjEXHE6W0GQR1XS
PF-382 NHvkPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH0dZhKSzVyPUGuOVY6PiEQvF2= NYXqOnhiW0GQR1XS
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NB10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M32zPWlEPTB;MT61O|M6OiEQvF2= NF7XUmZUSU6JRWK=
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HCE-4 Mn\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljNTWM2OD1zLk[wPFUh|ryP M4XhNHNCVkeHUh?=
HT-144 NH\CXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrjTWM2OD1zLk[zNVkh|ryP M2HBVHNCVkeHUh?=
NCI-H524 MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[2e|RoUUN3ME2xMlY1OzB5IN88US=> NXrObZl4W0GQR1XS
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U-266 M1r6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLFZ5JKSzVyPUGuO|M5PDJizszN MX7TRW5ITVJ?
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CAS-1 M{PoVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfCTWM2OD1zLkm4Nlk6KM7:TR?= Mn7jV2FPT0WU
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NCI-H1581 NGHQVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XaUmlEPTB;Mj6xNVU2QSEQvF2= M4TmTHNCVkeHUh?=
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NCI-H526 NIfRcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[xTWM2OD1{LkG5NVQyKM7:TR?= MXnTRW5ITVJ?
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NCI-SNU-1 NGXYWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwM{OyOVYh|ryP MYfTRW5ITVJ?
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SK-UT-1 NUi3epVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonwTWM2OD1{LkS3OFY4KM7:TR?= NVHadIZHW0GQR1XS
DMS-114 NGnrZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPnTWM2OD1{Lk[xOVI1KM7:TR?= NXjnZYllW0GQR1XS
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NCI-N87 M1rlSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTNwMkCwNkDPxE1? NYXLNVg{W0GQR1XS
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KM12 NEC1PGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLMenVoUUN3ME2zMlM{PTR2IN88US=> MnG3V2FPT0WU
ST486 NH3JVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTNwNUO4PFMh|ryP NYDZcXlUW0GQR1XS
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NCI-H1417 MnjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\jTWM2OD12LkK4OFQ{KM7:TR?= NFzvblhUSU6JRWK=
MDA-MB-134-VI M4DWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DzR2lEPTB;ND6zNFYxOSEQvF2= NFjm[YdUSU6JRWK=
Becker M3\1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTRwNEezN|Yh|ryP NWnY[4ZTW0GQR1XS
DMS-153 MoG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\nXlFsUUN3ME20MlY3PDd3IN88US=> MUjTRW5ITVJ?
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KE-37 Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3qTWM2OD12Lki2NVk3KM7:TR?= NH;yOYFUSU6JRWK=
NCI-H23 NU\uPGRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nQ[2lEPTB;ND64O|IzPyEQvF2= MnvvV2FPT0WU
MC116 M{\LdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLD[4VVUUN3ME20Mlk1OTJ4IN88US=> NI\jeGVUSU6JRWK=
NH-12 M3XMO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljKTWM2OD12Lkm2OFM6KM7:TR?= MVXTRW5ITVJ?
CTB-1 M4ThXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LWdGlEPTB;ND65O|czOSEQvF2= M3PzVHNCVkeHUh?=
KM-H2 M33jUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17KOmlEPTB;NT6wOVMzOyEQvF2= M2T6bnNCVkeHUh?=
MOLT-4 M4TZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTVwMUG4N{DPxE1? MmqxV2FPT0WU
NCI-H2141 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjGTWM2OD13LkG0NlY5KM7:TR?= M1;Fd3NCVkeHUh?=
EB-3 NUXRZpdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTVwMUe1NFQh|ryP M3m1e3NCVkeHUh?=
NCI-H1522 M3LuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrITWM2OD13LkK2N|IzKM7:TR?= NWHleWlrW0GQR1XS
MRK-nu-1 M4\1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXsTWM2OD13LkSzOlM{KM7:TR?= Ml;EV2FPT0WU
no-11 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P2[WlEPTB;NT60O|A5PyEQvF2= NHHaPZBUSU6JRWK=
CESS M4CyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTBeJFxUUN3ME21MlU5ODN2IN88US=> MmfOV2FPT0WU
KMOE-2 Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVntNnlsUUN3ME21MlU5PjV7IN88US=> MYnTRW5ITVJ?
REH M2i3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;FcGlEPTB;Nj6yOVYyQCEQvF2= NHznWVNUSU6JRWK=
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RCC10RGB NFLIUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fK[GlEPTB;Nz6yNlk4PyEQvF2= MlHYV2FPT0WU
NCI-H322M NGq4Z2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHXTY5QUUN3ME23MlM{OzN3IN88US=> MkXXV2FPT0WU
NB6 M2rncGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHhOZFJUUN3ME23MlU1QDl7IN88US=> MoGwV2FPT0WU
MN-60 M{W1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnuyTWM2OD15Lk[5NlE2KM7:TR?= Ml\DV2FPT0WU
NCI-H1092 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRThwMEG3N|Qh|ryP NECxd45USU6JRWK=
EKVX NWTRfWhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13YNWlEPTB;OD60O|A3PiEQvF2= MVnTRW5ITVJ?
D-263MG MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\zZ5NKSzVyPUiuOVU{QTZizszN MYnTRW5ITVJ?
NCI-H209 NVO5ZZF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13yTGlEPTB;OD62OFAxPiEQvF2= NY\1[5h3W0GQR1XS
IST-SL1 NXTiZY9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvYeXNKSzVyPUiuPFk5QTJizszN MYrTRW5ITVJ?
ACN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHHSnd1UUN3ME25MlE6OTV5IN88US=> NHfDfXFUSU6JRWK=
MHH-PREB-1 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrtR5pYUUN3ME25MlIyOjF7IN88US=> MYDTRW5ITVJ?
EW-11 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPITWM2OD17Lk[1N|k3KM7:TR?= NVzQVVdoW0GQR1XS
KASUMI-1 Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjZOpJyUUN3ME25Mlc5PzdizszN M33aZXNCVkeHUh?=
KINGS-1 NWfwOFZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\pfWlEPTB;MUCuNlM1PyEQvF2= MUPTRW5ITVJ?
EVSA-T MnvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFyLkOxPVIh|ryP M1jq[3NCVkeHUh?=
DSH1 NITuXGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[1TWM2OD1zMD6zPVczKM7:TR?= NUTaSXJQW0GQR1XS
COLO-824 NVq3WFJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vhN2lEPTB;MUCuPFY3QSEQvF2= MkHIV2FPT0WU
K052 NWTUb2lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XjUmlEPTB;MUCuPVMzOiEQvF2= NUTOSIk{W0GQR1XS
SK-MEL-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fwSmlEPTB;MUCuPVk{QSEQvF2= M4DkdHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo After 4 weeks of treatment with TAE684 at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. TAE684 treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression. [1] TAE684 also shows impressive antitumor activity against H3122 CR xenograft tumors. [2] Furthermore, treatment with TAE684 improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q, whereas Crizotinib has little effect on either phenotype. [3]

Protocol

Kinase Assay:[1]
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In vitro Enzyme Assays.:

All in vitro enzyme assays are done at Upstate Biotechnology with the exception of InsR and IGF-1R. To determine the IC50 of TAE684 against InsR and IGF-1R a homogeneous time-resolved fluorescence assay is performed. ATP (10 mM) and 20 mg/ml biotinylated PolyEY (Glu, Tyr 4:1) are combined with 50 nL of serial dilutions of TAE684 (10-500 nM) and 4 ng of InsR enzyme in the presence of the kinase reaction buffer (20 mM Tris譎Cl, pH 7.5/10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA). Assays are incubated for 1 hour at ambient temperature. Reactions are terminated by adding 10 mL of the detection solution containing 50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/mL Eu3+ cryptate-labeled anti-phosphotyrosine antibody Mab PT66-K, and 5 mg/mL Streptavidin-XLent. The reaction is incubated for half an hour, and fluorescence signals are read on Analyst GT.
Cell Research:[1]
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  • Cell lines: Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, Bcr-Abl, or TEL-kinase fusion constructs.
  • Concentrations: 1 nM-10 μM
  • Incubation Time: 2–3 days
  • Method: Cells are seeded in 384-well plates (2.5×104 cells per well) and incubated with serial dilutions of TAE684 or DMSO for 2–3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice.
  • Formulation: Resuspended in 10% 1-methyl-2-pyrrolidinone/90% polyethylene glycol 300 solution
  • Dosages: 1, 3, and 10 mg/kg
  • Administration: Once daily by oral gavage for 3 weeks
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL (4.88 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol, pH 4 10 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 614.2
Formula

C30H40ClN7O3S

CAS No. 761439-42-3
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*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 )

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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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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

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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