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 NG\CTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHINY1KSzVyPUCuNFAxODZyMzFOwG0> MUPTRW5ITVJ?
SF539 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDsRZVQUUN3ME2wMlAxODV4NDFOwG0> MVjTRW5ITVJ?
DEL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTUXWkzUUN3ME2wMlAxODl{NzFOwG0> MVrTRW5ITVJ?
NB1 M4GxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPsXIx1UUN3ME2wMlAxOTZ{IN88US=> MXnTRW5ITVJ?
SR MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXFTWM2OD1yLkCwNlc4KM7:TR?= M{m4TXNCVkeHUh?=
KARPAS-299 NHHFWXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\XTWM2OD1yLkCyN|g1KM7:TR?= MlrkV2FPT0WU
MHH-CALL-2 NX\WUFlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LvTWlEPTB;MD6wNlk2OiEQvF2= MVvTRW5ITVJ?
SU-DHL-1 NXHZe4JIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwMES4OlUh|ryP NVXyPW5uW0GQR1XS
A4-Fuk M2\LO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\JRWZUUUN3ME2wMlA2PTZ3IN88US=> M4fkWXNCVkeHUh?=
EW-1 NUnzbolLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TlZmlEPTB;MD6xNFI2PiEQvF2= M2PmbHNCVkeHUh?=
NOS-1 NVz5UJdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMUCyPVQh|ryP MnmxV2FPT0WU
EW-16 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMUC1Olgh|ryP NFfHRWhUSU6JRWK=
TE-11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzXOnRKSzVyPUCuNVYxQTZizszN MnjiV2FPT0WU
SW982 NVXqXVBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXHTWM2OD1yLkG2OFc5KM7:TR?= MX7TRW5ITVJ?
LAN-6 NIDqdVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwMUe0OFMh|ryP NV\MfWh6W0GQR1XS
MZ1-PC MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPTTWM2OD1yLkG3PFM2KM7:TR?= NGfR[YFUSU6JRWK=
KS-1 M3rJXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMUmzOFMh|ryP MXvTRW5ITVJ?
PSN1 NEPlZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;zUXZtUUN3ME2wMlE6PjNzIN88US=> NV;h[lUxW0GQR1XS
LC-2-ad MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwMUm2PVIh|ryP MVjTRW5ITVJ?
COLO-320-HSR NV;hU|dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\2WmVKSzVyPUCuNVk4PzZizszN NFvrSm5USU6JRWK=
OPM-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMkK2Olkh|ryP MXTTRW5ITVJ?
SK-NEP-1 NYK3dYRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDMTWM2OD1yLkKzOVI1KM7:TR?= NEfv[lBUSU6JRWK=
ALL-PO NEHmXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\JTXZKSzVyPUCuNlQ2OjRizszN M4Pob3NCVkeHUh?=
CMK MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;SWI9KSzVyPUCuNlU2OyEQvF2= M3TTdnNCVkeHUh?=
NCI-H1648 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHISo43UUN3ME2wMlI4QDV3IN88US=> NVntPJRXW0GQR1XS
SIG-M5 MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\XbGlEPTB;MD6yPVE2QSEQvF2= M1Xm[nNCVkeHUh?=
TGBC24TKB M1zHWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvFTWM2OD1yLkOwNlE5KM7:TR?= MWnTRW5ITVJ?
DOHH-2 NGqydYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDkTWM2OD1yLkOxNlA1KM7:TR?= NX\HSGsxW0GQR1XS
NB69 NHH5SJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwM{G3PFch|ryP Ml64V2FPT0WU
MFH-ino Mmj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwM{K1NlMh|ryP MoPxV2FPT0WU
KP-N-RT-BM-1 NXvyTI82T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rOWGlEPTB;MD6zN|EzOyEQvF2= Mn\oV2FPT0WU
MONO-MAC-6 MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwM{OyPVEh|ryP M2GxbnNCVkeHUh?=
ATN-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHFRnFWUUN3ME2wMlM{OzB|IN88US=> NYf2ZVhLW0GQR1XS
NTERA-S-cl-D1 NEXBS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXNTWM2OD1yLkOzN|k3KM7:TR?= NIn6RXFUSU6JRWK=
L-540 M37IOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwM{[5PFgh|ryP M4PVfHNCVkeHUh?=
GB-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW0OGUzUUN3ME2wMlM5QDZ5IN88US=> NUjs[4cyW0GQR1XS
MV-4-11 NGnUXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwM{m0OFYh|ryP MljRV2FPT0WU
KG-1 MmLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHYc4tKSzVyPUCuN|k2PjFizszN NULa[ZYxW0GQR1XS
OVCAR-4 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwNEC1Olkh|ryP NHrHTnFUSU6JRWK=
NEC8 NHnabVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwNEGyPVIh|ryP NF;TPIpUSU6JRWK=
SK-MM-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrGcZRzUUN3ME2wMlQyPjB7IN88US=> MXnTRW5ITVJ?
TE-8 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDnOHJKSzVyPUCuOFI5QCEQvF2= NG\XO4tUSU6JRWK=
697 NEPMcodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoCwTWM2OD1yLkSzNlE2KM7:TR?= NIPPW2NUSU6JRWK=
NB14 MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXmc3JKSzVyPUCuOFM5OjZizszN MlzJV2FPT0WU
GDM-1 NYj6TFZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[xZmF6UUN3ME2wMlQ4OTF4IN88US=> MYfTRW5ITVJ?
HUTU-80 NIHERYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz1VYdKSzVyPUCuOFc{PzVizszN NWL3SolQW0GQR1XS
HL-60 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zQNGlEPTB;MD60PFE1OiEQvF2= MlTmV2FPT0WU
OCI-AML2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDIO|FKSzVyPUCuOFg{OjhizszN MlfFV2FPT0WU
ML-2 NYn3XI5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq3TWM2OD1yLkS5NFMyKM7:TR?= NISzTWVUSU6JRWK=
ES4 NWK3NZJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjvOlNKSzVyPUCuOFkyODlizszN M4D4enNCVkeHUh?=
NCI-H747 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjBdVd1UUN3ME2wMlQ6QDlizszN M2jmO3NCVkeHUh?=
RL95-2 NVjJc3k2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHDfVdoUUN3ME2wMlUxOTF{IN88US=> NIfR[JBUSU6JRWK=
TE-15 M2\LeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\iV5JLUUN3ME2wMlUyOTJ2IN88US=> NXLpZWxJW0GQR1XS
TE-12 NH3yfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjHTWM2OD1yLkWzN|Q6KM7:TR?= MlHSV2FPT0WU
LB1047-RCC Ml\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPsTWM2OD1yLkW0OVQ6KM7:TR?= NXzySIJEW0GQR1XS
LB831-BLC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPzN3RKSzVyPUCuOVUxOjNizszN MorlV2FPT0WU
NCI-H1355 NWP0T|NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33Ne2lEPTB;MD61OVE5PCEQvF2= NFrW[oNUSU6JRWK=
CTV-1 NUPmWXN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zBR2lEPTB;MD61OVYzPCEQvF2= MUDTRW5ITVJ?
RXF393 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonGTWM2OD1yLkW1O|k1KM7:TR?= M13wSXNCVkeHUh?=
SW872 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\qPXdwUUN3ME2wMlU3PzJ2IN88US=> MWPTRW5ITVJ?
MPP-89 MofDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7nTpBKSzVyPUCuOVc5QDRizszN MkXYV2FPT0WU
RPMI-8226 MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v1c2lEPTB;MD62N|UzPiEQvF2= MmjLV2FPT0WU
LS-1034 NFLsSHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTJO4pKSzVyPUCuOlM2QCEQvF2= MWfTRW5ITVJ?
SJSA-1 M{jNd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjqTWM2OD1yLk[zO|I2KM7:TR?= NVH2bHJ3W0GQR1XS
HOP-62 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HHWWlEPTB;MD62OVA{OyEQvF2= NEHBV2pUSU6JRWK=
KGN M3fCRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwNk[xOlgh|ryP NI\0eJdUSU6JRWK=
D-336MG M{PHXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\GV5BpUUN3ME2wMlY3OTZ7IN88US=> NWHjOW9PW0GQR1XS
LS-411N MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwNke0OlIh|ryP NEfBd41USU6JRWK=
TE-1 MlLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwNkmwO|Qh|ryP MUnTRW5ITVJ?
LB996-RCC M4nBOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jVdmlEPTB;MD62PVM5QSEQvF2= M4rnc3NCVkeHUh?=
TE-10 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTBwN{G0PVYh|ryP MWfTRW5ITVJ?
NCI-SNU-16 NYrEfHZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfUeo9KSzVyPUCuO|I3PjRizszN Mm\SV2FPT0WU
ES8 NUjrfJF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jBbGlEPTB;MD63OFk4PSEQvF2= MY\TRW5ITVJ?
COLO-800 M3i0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjDR3BQUUN3ME2wMlc3Pjl3IN88US=> NIjYfHFUSU6JRWK=
ES6 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTWTWM2OD1yLke3OVU6KM7:TR?= NXf4PVh[W0GQR1XS
L-363 NHj4[5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwOEKzO|Uh|ryP M1f4R3NCVkeHUh?=
NMC-G1 M{Dtc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHOblYxUUN3ME2wMlg{OjN|IN88US=> NXPoenFbW0GQR1XS
LU-134-A MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jVWGlEPTB;MD64N|kyOiEQvF2= NH7uRZlUSU6JRWK=
SF268 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGGzRYNKSzVyPUCuPFQxPDJizszN MnqzV2FPT0WU
KARPAS-45 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvld4cyUUN3ME2wMlg1OjZ|IN88US=> MUDTRW5ITVJ?
TGW MnfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TEPWlEPTB;MD64OVg3OyEQvF2= MkO1V2FPT0WU
CHP-126 M3zBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;ITWM2OD1yLki1PVU4KM7:TR?= MVHTRW5ITVJ?
MOLT-16 NGL0dmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwOEe1PFkh|ryP M1vrfnNCVkeHUh?=
LB771-HNC NXTpe3RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33rV2lEPTB;MD64PVc2PyEQvF2= M{LMd3NCVkeHUh?=
NALM-6 MoH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwOUC3N|kh|ryP NX;NO4lzW0GQR1XS
GCIY M{TpbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnGXmR5UUN3ME2wMlk2PTJ4IN88US=> M4DaVnNCVkeHUh?=
IST-MES1 NFHTRldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwOUi4NlQh|ryP NHzS[lhUSU6JRWK=
LB2241-RCC NFWwcGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDlTWM2OD1yLkm4PFQh|ryP NYXDUYFZW0GQR1XS
BL-70 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfBOoJKSzVyPUCuPVk2OzVizszN M2jnN3NCVkeHUh?=
NB17 NEjZZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\EZ2lEPTB;MT6wNFY{QSEQvF2= NXfhPIl6W0GQR1XS
LXF-289 NU\6W2RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jmSmlEPTB;MT6wN|A4PiEQvF2= MVvTRW5ITVJ?
TK10 NITmc2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvJTWM2OD1zLkC1NFY{KM7:TR?= MoW3V2FPT0WU
K5 NIPaZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3T5T2lEPTB;MT6wOlI4PCEQvF2= Mmf2V2FPT0WU
NCI-H716 M2XtR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwMEeyOVkh|ryP MWPTRW5ITVJ?
HCE-T NYTieIQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFwMEi4NVkh|ryP NXribItXW0GQR1XS
GI-1 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTFwMEm3PVgh|ryP Ml7WV2FPT0WU
KARPAS-422 M{jXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDpVFdQUUN3ME2xMlExODJ{IN88US=> MmPnV2FPT0WU
TE-9 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13yRWlEPTB;MT6xNVMzQCEQvF2= NU\TOWR1W0GQR1XS
SF126 NEjDVplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1f1WGlEPTB;MT6xNVU3QCEQvF2= MXPTRW5ITVJ?
BB30-HNC M3zPSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XMd2lEPTB;MT6xN|EyOiEQvF2= NYTve45lW0GQR1XS
NCI-H1304 M3;pdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWGzRmZPUUN3ME2xMlE{OzN6IN88US=> NI\JSIxUSU6JRWK=
HEL MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXqTWM2OD1zLkG0PFk2KM7:TR?= M37M[XNCVkeHUh?=
HAL-01 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXaUpJKSzVyPUGuNVUzQDNizszN NWDVbmtPW0GQR1XS
SK-LMS-1 NVXGbo1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELmeFhKSzVyPUGuNVU6PzRizszN MVzTRW5ITVJ?
SW954 NHPZbYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDSU4hKSzVyPUGuNVk2PjdizszN NHnYOVVUSU6JRWK=
D-283MED MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFwMkKzO|kh|ryP NV7DRm5oW0GQR1XS
NCI-H1882 NYK4bmhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFwMkO4PUDPxE1? NW\kVm9YW0GQR1XS
GI-ME-N MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPZ[IFKSzVyPUGuNlUzODhizszN MlTrV2FPT0WU
SK-PN-DW MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTFwMk[zOFgh|ryP NVP5NFZrW0GQR1XS
C2BBe1 NGDWcmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jPZWlEPTB;MT6yPVEyPyEQvF2= MX\TRW5ITVJ?
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DMS-114 MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nFVGlEPTB;Mj62NVUzPCEQvF2= MljmV2FPT0WU
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BC-3 M{DvdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3vV|g{UUN3ME20MlE{ODZ6IN88US=> MYLTRW5ITVJ?
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MEG-01 Ml\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljlTWM2OD12LkK3OFE6KM7:TR?= NF31XHBUSU6JRWK=
NCI-H1417 MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\xVlNKSzVyPUSuNlg1PDNizszN NHzBNIdUSU6JRWK=
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NCI-H23 NXTR[JhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\wTWM2OD12Lki3NlI4KM7:TR?= MkLUV2FPT0WU
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NCI-H1522 NUm2SVd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT0d|BGUUN3ME21MlI3OzJ{IN88US=> NYfLW2hrW0GQR1XS
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no-11 NGDZSJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTVwNEewPFch|ryP MXPTRW5ITVJ?
CESS NXvjNoRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzYWJNLUUN3ME21MlU5ODN2IN88US=> NH\ycG5USU6JRWK=
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REH MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTZwMkW2NVgh|ryP MmrCV2FPT0WU
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RCC10RGB Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTdwMkK5O|ch|ryP M3nObXNCVkeHUh?=
NCI-H322M NH:5S4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG1VlY2UUN3ME23MlM{OzN3IN88US=> MV;TRW5ITVJ?
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MN-60 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXZTWM2OD15Lk[5NlE2KM7:TR?= M1nFNHNCVkeHUh?=
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NCI-H209 NGmxSJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTKNG1KSzVyPUiuOlQxODZizszN NYHzWpdDW0GQR1XS
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MHH-PREB-1 NGnPcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fVd2lEPTB;OT6yNVIyQSEQvF2= NHz1fGdUSU6JRWK=
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KASUMI-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD2TWM2OD17Lke4O|ch|ryP MWPTRW5ITVJ?
KINGS-1 NUDMZXVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S0NGlEPTB;MUCuNlM1PyEQvF2= NWXoVlltW0GQR1XS
EVSA-T MmP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v3[GlEPTB;MUCuN|E6OiEQvF2= NXPRc4VnW0GQR1XS
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COLO-824 NGTHRZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonJTWM2OD1zMD64OlY6KM7:TR?= MorOV2FPT0WU
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SK-MEL-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELOfI1KSzVyPUGwMlk6OzlizszN M1O2bXNCVkeHUh?=

... 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
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
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)

  • 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
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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):
    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