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

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 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;n[HJKSzVyPUCuNFAxODZyMzFOwG0> NEjscIdUSU6JRWK=
SF539 M3vmOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\qWoRXUUN3ME2wMlAxODV4NDFOwG0> NELqbYhUSU6JRWK=
DEL MkHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInUfHlKSzVyPUCuNFAxQTJ5IN88US=> MmezV2FPT0WU
NB1 NGjXdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvTfpdKSzVyPUCuNFAyPjJizszN NHHU[ItUSU6JRWK=
SR MnnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwMECyO|ch|ryP NGLHfYhUSU6JRWK=
KARPAS-299 NVfmToQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M124UWlEPTB;MD6wNlM5PCEQvF2= NVnJNJBIW0GQR1XS
MHH-CALL-2 NYnKWpAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljHTWM2OD1yLkCyPVUzKM7:TR?= NEizNXBUSU6JRWK=
SU-DHL-1 M1zVTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrTcnp3UUN3ME2wMlA1QDZ3IN88US=> MmrHV2FPT0WU
A4-Fuk NGLzSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH0TWM2OD1yLkC1OVY2KM7:TR?= MlHyV2FPT0WU
EW-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzHTWM2OD1yLkGwNlU3KM7:TR?= M1\PNHNCVkeHUh?=
NOS-1 NHrwTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\DTWM2OD1yLkGwNlk1KM7:TR?= Ml;MV2FPT0WU
EW-16 NH\j[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMUC1Olgh|ryP MnPGV2FPT0WU
TE-11 Mlj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwMU[wPVYh|ryP M4nCdHNCVkeHUh?=
SW982 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LRUGlEPTB;MD6xOlQ4QCEQvF2= M1vJ[3NCVkeHUh?=
LAN-6 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HkZWlEPTB;MD6xO|Q1OyEQvF2= MUfTRW5ITVJ?
MZ1-PC MoXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3mTWM2OD1yLkG3PFM2KM7:TR?= NGLi[GJUSU6JRWK=
KS-1 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvBTWM2OD1yLkG5N|Q{KM7:TR?= NGDlc4RUSU6JRWK=
PSN1 M1O3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnycYVKSzVyPUCuNVk3OzFizszN MnvWV2FPT0WU
LC-2-ad NY\Md4dlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzwTWM2OD1yLkG5OlkzKM7:TR?= MWTTRW5ITVJ?
COLO-320-HSR MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES0U|ZKSzVyPUCuNVk4PzZizszN MnTmV2FPT0WU
OPM-2 MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LGdWlEPTB;MD6yNlY3QSEQvF2= MkPPV2FPT0WU
SK-NEP-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DzfmlEPTB;MD6yN|UzPCEQvF2= NYC2WmoyW0GQR1XS
ALL-PO NX3NbHByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPnOZJKSzVyPUCuNlQ2OjRizszN NXzEXHRGW0GQR1XS
CMK MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwMkW1N{DPxE1? NV;zNFd5W0GQR1XS
NCI-H1648 NFvRW45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{G2NGlEPTB;MD6yO|g2PSEQvF2= MkTUV2FPT0WU
SIG-M5 NVTnU3J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwMkmxOVkh|ryP MnHtV2FPT0WU
TGBC24TKB M1fFVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki2TWM2OD1yLkOwNlE5KM7:TR?= MYXTRW5ITVJ?
DOHH-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwM{GyNFQh|ryP Mn7DV2FPT0WU
NB69 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TIcmlEPTB;MD6zNVc5PyEQvF2= NIrMOIRUSU6JRWK=
MFH-ino NWPudHNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwM{K1NlMh|ryP MVPTRW5ITVJ?
KP-N-RT-BM-1 MonvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT4TWM2OD1yLkOzNVI{KM7:TR?= MVLTRW5ITVJ?
MONO-MAC-6 NWjFZ3dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwM{OyPVEh|ryP NXricXZXW0GQR1XS
ATN-1 NXPjUmtHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1GwfGlEPTB;MD6zN|MxOyEQvF2= MnHnV2FPT0WU
NTERA-S-cl-D1 M4LqbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vER2lEPTB;MD6zN|M6PiEQvF2= MlfIV2FPT0WU
L-540 NWXZUGZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrpd4pKSzVyPUCuN|Y6QDhizszN M{L2Z3NCVkeHUh?=
GB-1 NUfmRWpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W3NWlEPTB;MD6zPFg3PyEQvF2= MV3TRW5ITVJ?
MV-4-11 NWDHToZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrXWnNlUUN3ME2wMlM6PDR4IN88US=> NHTGRWlUSU6JRWK=
KG-1 NHnqSVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LhbGlEPTB;MD6zPVU3OSEQvF2= NVKxXpQyW0GQR1XS
OVCAR-4 M4PIVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwNEC1Olkh|ryP M2W1OnNCVkeHUh?=
NEC8 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\UXWhKSzVyPUCuOFEzQTJizszN MVrTRW5ITVJ?
SK-MM-2 NFjwd2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjN[4IyUUN3ME2wMlQyPjB7IN88US=> MVzTRW5ITVJ?
TE-8 NEX3b2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfWTWM2OD1yLkSyPFgh|ryP NVvBfXRFW0GQR1XS
697 NYfDZnhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwNEOyNVUh|ryP NHfCR4ZUSU6JRWK=
NB14 NILnSFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\5TWM2OD1yLkSzPFI3KM7:TR?= MXrTRW5ITVJ?
GDM-1 M2Hzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\2VJJKSzVyPUCuOFcyOTZizszN MlXyV2FPT0WU
HUTU-80 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO2RYdmUUN3ME2wMlQ4Ozd3IN88US=> MkLsV2FPT0WU
HL-60 NXGyNmJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULod5JvUUN3ME2wMlQ5OTR{IN88US=> NW\sc4dvW0GQR1XS
OCI-AML2 NHPqR2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDHVFNLUUN3ME2wMlQ5OzJ6IN88US=> NF3XXGdUSU6JRWK=
ML-2 M{TsUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwNEmwN|Eh|ryP M3fwd3NCVkeHUh?=
ES4 NGXicIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSyTWM2OD1yLkS5NVA6KM7:TR?= M1;zOXNCVkeHUh?=
NCI-H747 NUXFNIdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwNEm4PUDPxE1? NW\rXXdKW0GQR1XS
RL95-2 Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwNUCxNVIh|ryP M1e0S3NCVkeHUh?=
TE-15 Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH2xdFBKSzVyPUCuOVEyOjRizszN NGHW[3NUSU6JRWK=
TE-12 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ftU2lEPTB;MD61N|M1QSEQvF2= NX:4blFZW0GQR1XS
LB1047-RCC NFGxTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\aTWM2OD1yLkW0OVQ6KM7:TR?= MWPTRW5ITVJ?
LB831-BLC MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPy[ohKSzVyPUCuOVUxOjNizszN M3HFRXNCVkeHUh?=
NCI-H1355 MkOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXUSZZKSzVyPUCuOVUyQDRizszN MUfTRW5ITVJ?
CTV-1 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;MVmlEPTB;MD61OVYzPCEQvF2= NXz1WJhFW0GQR1XS
RXF393 NV;PTWhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\wRnpKSzVyPUCuOVU4QTRizszN NXG5RlV[W0GQR1XS
SW872 M4TvN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwNU[3NlQh|ryP NF3TN2pUSU6JRWK=
MPP-89 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3JXoJCUUN3ME2wMlU4QDh2IN88US=> MmXjV2FPT0WU
RPMI-8226 NWXlRWhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHOTWM2OD1yLk[zOVI3KM7:TR?= MUDTRW5ITVJ?
LS-1034 NHHPcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL5UFJKSzVyPUCuOlM2QCEQvF2= M1HxWnNCVkeHUh?=
SJSA-1 NYL5PXpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwNkO3NlUh|ryP M1\PSHNCVkeHUh?=
HOP-62 MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPvTWM2OD1yLk[1NFM{KM7:TR?= MV;TRW5ITVJ?
KGN M13KXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3DOJhKSzVyPUCuOlYyPjhizszN M1K5fHNCVkeHUh?=
D-336MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1THXGlEPTB;MD62OlE3QSEQvF2= MU\TRW5ITVJ?
LS-411N MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPOc2tKSzVyPUCuOlc1PjJizszN MkLuV2FPT0WU
TE-1 NGXkd2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[1fGNKSzVyPUCuOlkxPzRizszN NGfv[|ZUSU6JRWK=
LB996-RCC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTBwNkmzPFkh|ryP M4PDXHNCVkeHUh?=
TE-10 NWfRTplvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC4TWM2OD1yLkexOFk3KM7:TR?= M1zBNnNCVkeHUh?=
NCI-SNU-16 NGDPTY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrsb2RKSzVyPUCuO|I3PjRizszN NUDudoVbW0GQR1XS
ES8 M1PlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG2fWxKSzVyPUCuO|Q6PzVizszN MYfTRW5ITVJ?
COLO-800 NF7zV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPi[lRKSzVyPUCuO|Y3QTVizszN NGHYSnlUSU6JRWK=
ES6 MkLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwN{e1OVkh|ryP M3vpZXNCVkeHUh?=
L-363 NWW2WHVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTKTWM2OD1yLkiyN|c2KM7:TR?= M3n4SXNCVkeHUh?=
NMC-G1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrYVGNKSzVyPUCuPFMzOzNizszN MnP4V2FPT0WU
LU-134-A M4LEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwOEO5NVIh|ryP MWnTRW5ITVJ?
SF268 M{jSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPQUnJbUUN3ME2wMlg1ODR{IN88US=> M4H6XXNCVkeHUh?=
KARPAS-45 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLlWI9LUUN3ME2wMlg1OjZ|IN88US=> MUPTRW5ITVJ?
TGW MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\pU|FKSzVyPUCuPFU5PjNizszN NHK2TZFUSU6JRWK=
CHP-126 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwOEW5OVch|ryP NUHkW4EzW0GQR1XS
MOLT-16 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXwTnJLUUN3ME2wMlg4PTh7IN88US=> MYPTRW5ITVJ?
LB771-HNC NIHNTYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fmUGlEPTB;MD64PVc2PyEQvF2= M12xfXNCVkeHUh?=
NALM-6 Ml72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HnUmlEPTB;MD65NFc{QSEQvF2= NGjGeFhUSU6JRWK=
GCIY MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIS5[ItKSzVyPUCuPVU2OjZizszN M4XMPHNCVkeHUh?=
IST-MES1 NGexXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzrTWM2OD1yLkm4PFI1KM7:TR?= M3TiXHNCVkeHUh?=
LB2241-RCC Mne0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwOUi4OEDPxE1? Mkj0V2FPT0WU
BL-70 NYLRPGRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILQNIdKSzVyPUCuPVk2OzVizszN M4D6TnNCVkeHUh?=
NB17 NYPvRYR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFwMEC2N|kh|ryP MlX5V2FPT0WU
LXF-289 NFPISYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzCPJhKSzVyPUGuNFMxPzZizszN NYHleolJW0GQR1XS
TK10 NYXCb|BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK1eJF4UUN3ME2xMlA2ODZ|IN88US=> M3\JeHNCVkeHUh?=
K5 Mlj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrYTWM2OD1zLkC2Nlc1KM7:TR?= NYPQbJRxW0GQR1XS
NCI-H716 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPse49MUUN3ME2xMlA4OjV7IN88US=> MmL6V2FPT0WU
HCE-T MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFwMEi4NVkh|ryP NEnjN5VUSU6JRWK=
GI-1 M2PLRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIS2SINKSzVyPUGuNFk4QThizszN MkT5V2FPT0WU
KARPAS-422 NHnMO|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjv[o9MUUN3ME2xMlExODJ{IN88US=> NYi2e2h1W0GQR1XS
TE-9 Ml\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrQbmNKSzVyPUGuNVE{OjhizszN NUnCbFZ[W0GQR1XS
SF126 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTFwMUG1Olgh|ryP MXrTRW5ITVJ?
BB30-HNC NX;TVoNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTSTWM2OD1zLkGzNVEzKM7:TR?= MXLTRW5ITVJ?
NCI-H1304 M2n5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLlTWM2OD1zLkGzN|M5KM7:TR?= M{Lq[nNCVkeHUh?=
HEL NUezW41HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFwMUS4PVUh|ryP NGjIe5dUSU6JRWK=
HAL-01 M{fURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFwMUWyPFMh|ryP NED0UHVUSU6JRWK=
SK-LMS-1 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInncFNKSzVyPUGuNVU6PzRizszN MmLqV2FPT0WU
SW954 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzWfZpKSzVyPUGuNVk2PjdizszN NHvUT41USU6JRWK=
D-283MED MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfrUmJKSzVyPUGuNlI{PzlizszN NX7JNJNuW0GQR1XS
NCI-H1882 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq5dIhUUUN3ME2xMlI{QDlizszN NXrycYE2W0GQR1XS
GI-ME-N NV3ldG1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPTfGZKSzVyPUGuNlUzODhizszN MXrTRW5ITVJ?
SK-PN-DW MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zwRmlEPTB;MT6yOlM1QCEQvF2= MVPTRW5ITVJ?
C2BBe1 MlzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTFwMkmxNVch|ryP MY\TRW5ITVJ?
A704 NUnl[plVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\mTWM2OD1zLkOyOlg6KM7:TR?= MVHTRW5ITVJ?
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ETK-1 M4W1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\lUGlEPTB;MT6zOFQ5QSEQvF2= NEfo[4RUSU6JRWK=
LB647-SCLC Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH74W49KSzVyPUGuN|Q6QDZizszN MoH0V2FPT0WU
OCUB-M NHjPPGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDkXVBKSzVyPUGuN|YyPDNizszN MWXTRW5ITVJ?
NCI-H720 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLWZ25NUUN3ME2xMlM3Ozd6IN88US=> MWLTRW5ITVJ?
NB13 M1WwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofUTWM2OD1zLkO3Nlk{KM7:TR?= Mn;FV2FPT0WU
GR-ST MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHQTWlZUUN3ME2xMlM5PzV5IN88US=> NVO3V3dKW0GQR1XS
DU-4475 NG\Q[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHFdJZCUUN3ME2xMlQ2QDV|IN88US=> MkXIV2FPT0WU
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RKO MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYCzTW41UUN3ME2xMlQ6QTJ{IN88US=> NGXvelJUSU6JRWK=
LS-123 NEHvfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml23TWM2OD1zLkWxOVk1KM7:TR?= M{mz[XNCVkeHUh?=
NCI-H69 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFwNUW4NVEh|ryP NVnTNFZyW0GQR1XS
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PF-382 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2POfGlEPTB;MT61Olk3KM7:TR?= MYDTRW5ITVJ?
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NB10 NEP3SlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwNUezPVIh|ryP MWnTRW5ITVJ?
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NCI-H524 MmPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjqbmpXUUN3ME2xMlY1OzB5IN88US=> MmXTV2FPT0WU
NKM-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoWzTWM2OD1zLk[4OlYh|ryP NXTidZluW0GQR1XS
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CPC-N MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzFSWJMUUN3ME2xMlg2ODl4IN88US=> Mn7NV2FPT0WU
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VA-ES-BJ NUKwbHVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[2U2lVUUN3ME2yMlAyPTF|IN88US=> M2rBWHNCVkeHUh?=
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NCI-H526 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PKSGlEPTB;Mj6xPVE1OSEQvF2= NHrXNFVUSU6JRWK=
MSTO-211H NF3ad41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrWTWM2OD1{LkKwNFQyKM7:TR?= NIrMUGFUSU6JRWK=
LS-513 NITW[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwMkKyOlkh|ryP MmrKV2FPT0WU
NCI-SNU-1 NVrPeJd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLCTWM2OD1{LkOzNlU3KM7:TR?= MWrTRW5ITVJ?
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NCI-H2126 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHMeIlFUUN3ME2yMlQ{Pjd2IN88US=> NYjMRoh5W0GQR1XS
SK-UT-1 M{nVXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlm4TWM2OD1{LkS3OFY4KM7:TR?= NWjOdIl{W0GQR1XS
DMS-114 NGHuO3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJwNkG1NlQh|ryP M1\zcHNCVkeHUh?=
ONS-76 NVz0b21YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYexOJFQUUN3ME2yMlY{PjRzIN88US=> Mlj6V2FPT0WU
8-MG-BA MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPCZ5FYUUN3ME2yMlY2PDF2IN88US=> NVmxTGpDW0GQR1XS
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LAMA-84 NW\Yb2VKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\x[ZY2UUN3ME2yMlc6QTF{IN88US=> NHjkPW9USU6JRWK=
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A388 NI\E[5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;ic2lEPTB;Mj65OlE4KM7:TR?= MlLxV2FPT0WU
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BV-173 NFzDOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n4XGlEPTB;Mz62OFA5QCEQvF2= MWPTRW5ITVJ?
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ARH-77 M2L3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrXTWM2OD12LkGxNFY4KM7:TR?= MUPTRW5ITVJ?
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NCI-H1417 M4rWbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4myZmlEPTB;ND6yPFQ1OyEQvF2= M1jZWnNCVkeHUh?=
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Becker MkjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrTTWM2OD12LkS3N|M3KM7:TR?= NGDDNpdUSU6JRWK=
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EW-3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTRwN{[yOFgh|ryP MoL5V2FPT0WU
KE-37 NFHaS4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnsTWM2OD12Lki2NVk3KM7:TR?= NHW1UpVUSU6JRWK=
NCI-H23 MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTRwOEeyNlch|ryP MX7TRW5ITVJ?
MC116 MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vRXWlEPTB;ND65OFEzPiEQvF2= MkHIV2FPT0WU
NH-12 NHPTVpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLrTWM2OD12Lkm2OFM6KM7:TR?= NX7QfmM{W0GQR1XS
CTB-1 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF73emxKSzVyPUSuPVc4OjFizszN MmfsV2FPT0WU
KM-H2 M3LhVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzBfopKSzVyPUWuNFU{OjNizszN MVPTRW5ITVJ?
MOLT-4 M37Yb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEezSWFKSzVyPUWuNVE5OyEQvF2= NYK3fIRjW0GQR1XS
NCI-H2141 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H4ZWlEPTB;NT6xOFI3QCEQvF2= M4riW3NCVkeHUh?=
EB-3 MmrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\uTWM2OD13LkG3OVA1KM7:TR?= NWi0V3pTW0GQR1XS
NCI-H1522 NV;1c|BrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHGZXFQUUN3ME21MlI3OzJ{IN88US=> M3\qd3NCVkeHUh?=
MRK-nu-1 MnzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTVwNEO2N|Mh|ryP M4fUWHNCVkeHUh?=
no-11 NVLZO29DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn1TFVRUUN3ME21MlQ4ODh5IN88US=> M1nkeXNCVkeHUh?=
CESS MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS3[YgzUUN3ME21MlU5ODN2IN88US=> MWrTRW5ITVJ?
KMOE-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3JToRpUUN3ME21MlU5PjV7IN88US=> Mk\LV2FPT0WU
REH M33QO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTZwMkW2NVgh|ryP MlnYV2FPT0WU
KU812 NHXXcllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoroTWM2OD14LkSyO|kyKM7:TR?= NIjydoxUSU6JRWK=
SK-N-FI NY\oXpJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTZwNkC2O|Qh|ryP MoLKV2FPT0WU
MMAC-SF M1\BR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnmyTWM2OD15LkC2OFkzKM7:TR?= M3rFd3NCVkeHUh?=
RCC10RGB NVjjcVVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3qw[WlEPTB;Nz6yNlk4PyEQvF2= M4nL[3NCVkeHUh?=
NCI-H322M M4joVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3GU|lNUUN3ME23MlM{OzN3IN88US=> MWjTRW5ITVJ?
NB6 MlXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WzXmlEPTB;Nz61OFg6QSEQvF2= M4nzcHNCVkeHUh?=
MN-60 M2DFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[2WmlEPTB;Nz62PVIyPSEQvF2= NV\VWmNUW0GQR1XS
NCI-H1092 NUnpNGhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRThwMEG3N|Qh|ryP MknPV2FPT0WU
EKVX M1nxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHH1TXFKSzVyPUiuOFcxPjZizszN NVzNe4NkW0GQR1XS
D-263MG NWPoeXlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjFdG9KSzVyPUiuOVU{QTZizszN NGq0fmJUSU6JRWK=
NCI-H209 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnyU3RzUUN3ME24MlY1ODB4IN88US=> MknYV2FPT0WU
IST-SL1 NW[xclRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HSbWlEPTB;OD64PVg6OiEQvF2= M3PK[3NCVkeHUh?=
ACN NV74O2F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH2dJFKSzVyPUmuNVkyPTdizszN MXfTRW5ITVJ?
MHH-PREB-1 NGLDVpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ZTWM2OD17LkKxNlE6KM7:TR?= M1jmSHNCVkeHUh?=
EW-11 NG\kWpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTlwNkWzPVYh|ryP NE\NfHRUSU6JRWK=
KASUMI-1 M2\SVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rtWGlEPTB;OT63PFc4KM7:TR?= MmrSV2FPT0WU
KINGS-1 NHXTSFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFyLkKzOFch|ryP M{nnNXNCVkeHUh?=
EVSA-T MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFyLkOxPVIh|ryP M1mxZXNCVkeHUh?=
DSH1 MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\CTWM2OD1zMD6zPVczKM7:TR?= NWC4bZJDW0GQR1XS
COLO-824 NHvv[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTFyLki2Olkh|ryP MUDTRW5ITVJ?
K052 M4XQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnzSZNKSzVyPUGwMlk{OjJizszN NWjsW452W0GQR1XS
SK-MEL-2 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfEdWRKSzVyPUGwMlk6OzlizszN MY\TRW5ITVJ?

... 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