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 MmDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fDSmlEPTB;MD6wNFAxPjB|IN88US=> MYnTRW5ITVJ?
SF539 NI\CO45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\RdpdKSzVyPUCuNFAxPTZ2IN88US=> NHrIe|hUSU6JRWK=
DEL MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\ITWM2OD1yLkCwNFkzPyEQvF2= M1vpd3NCVkeHUh?=
NB1 M2\ZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnLWIFUUUN3ME2wMlAxOTZ{IN88US=> NXTEPYRqW0GQR1XS
SR NEnIUYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfMcGt1UUN3ME2wMlAxOjd5IN88US=> NHzQfnBUSU6JRWK=
KARPAS-299 M1H5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwMEKzPFQh|ryP NEHIUFZUSU6JRWK=
MHH-CALL-2 M2DrVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf4V5BnUUN3ME2wMlAzQTV{IN88US=> MkDZV2FPT0WU
SU-DHL-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnMTWM2OD1yLkC0PFY2KM7:TR?= M4rJOHNCVkeHUh?=
A4-Fuk NWLNfHlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfkR25EUUN3ME2wMlA2PTZ3IN88US=> NWj2OXpmW0GQR1XS
EW-1 NVjuU5JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXSTWM2OD1yLkGwNlU3KM7:TR?= MkPpV2FPT0WU
NOS-1 NXfzbXR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwMUCyPVQh|ryP Mn30V2FPT0WU
EW-16 NX;1S2R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[2V2lEPTB;MD6xNFU3QCEQvF2= MkHFV2FPT0WU
TE-11 MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzkNWx7UUN3ME2wMlE3ODl4IN88US=> NIPVbpFUSU6JRWK=
SW982 NVT2bJlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzZ[5p6UUN3ME2wMlE3PDd6IN88US=> NEK1PJpUSU6JRWK=
LAN-6 M2rEXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMUe0OFMh|ryP Mni2V2FPT0WU
MZ1-PC NVfNXWhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXVdm8yUUN3ME2wMlE4QDN3IN88US=> M3PSZ3NCVkeHUh?=
KS-1 NUTuRVBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HBR2lEPTB;MD6xPVM1OyEQvF2= Mmf4V2FPT0WU
PSN1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHuZXBKSzVyPUCuNVk3OzFizszN NETrVllUSU6JRWK=
LC-2-ad MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPGSJAxUUN3ME2wMlE6Pjl{IN88US=> M3zsZnNCVkeHUh?=
COLO-320-HSR Mnn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zrNmlEPTB;MD6xPVc4PiEQvF2= MVzTRW5ITVJ?
OPM-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHSdXltUUN3ME2wMlIzPjZ7IN88US=> MX\TRW5ITVJ?
SK-NEP-1 M2TVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LwZWlEPTB;MD6yN|UzPCEQvF2= Mo\IV2FPT0WU
ALL-PO M1LwRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUO4Wpk{UUN3ME2wMlI1PTJ2IN88US=> NHvzUoVUSU6JRWK=
CMK NWW1VIZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTCcnRKSzVyPUCuNlU2OyEQvF2= MWPTRW5ITVJ?
NCI-H1648 NYTs[mFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLPTWM2OD1yLkK3PFU2KM7:TR?= NGLtbHFUSU6JRWK=
SIG-M5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7LTWM2OD1yLkK5NVU6KM7:TR?= MXTTRW5ITVJ?
TGBC24TKB NYqzSnZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTsTXFLUUN3ME2wMlMxOjF6IN88US=> NV\XTnhMW0GQR1XS
DOHH-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETi[olKSzVyPUCuN|EzODRizszN Mn7pV2FPT0WU
NB69 NGnjPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL2V41KSzVyPUCuN|E4QDdizszN MVvTRW5ITVJ?
MFH-ino NVK0T2J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPETWM2OD1yLkOyOVI{KM7:TR?= NX2xUlQ3W0GQR1XS
KP-N-RT-BM-1 M{PXeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TMeWlEPTB;MD6zN|EzOyEQvF2= Mnz6V2FPT0WU
MONO-MAC-6 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwM{OyPVEh|ryP NYrvcGRuW0GQR1XS
ATN-1 NU\6fFRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7BTWM2OD1yLkOzN|A{KM7:TR?= NEjIO3NUSU6JRWK=
NTERA-S-cl-D1 M4TtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwM{OzPVYh|ryP MnjqV2FPT0WU
L-540 NF3ufZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\kN5ZMUUN3ME2wMlM3QTh6IN88US=> NH65W5RUSU6JRWK=
GB-1 NHzXVplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K4e2lEPTB;MD6zPFg3PyEQvF2= MlfoV2FPT0WU
MV-4-11 NUHTR5lkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPxTWM2OD1yLkO5OFQ3KM7:TR?= M13aUHNCVkeHUh?=
KG-1 M3XS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTBwM{m1OlEh|ryP MlnTV2FPT0WU
OVCAR-4 MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXWfmhKSzVyPUCuOFA2PjlizszN NFK3UG5USU6JRWK=
NEC8 NWPGfYR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwNEGyPVIh|ryP NF\wNmdUSU6JRWK=
SK-MM-2 NXHIXFAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUP2V|Q{UUN3ME2wMlQyPjB7IN88US=> Mof3V2FPT0WU
TE-8 NFPhdY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vEZmlEPTB;MD60Nlg5KM7:TR?= M4jI[nNCVkeHUh?=
697 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vpcWlEPTB;MD60N|IyPSEQvF2= M3zwUHNCVkeHUh?=
NB14 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljNTWM2OD1yLkSzPFI3KM7:TR?= M4O0ZXNCVkeHUh?=
GDM-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnCWm5KSzVyPUCuOFcyOTZizszN MWXTRW5ITVJ?
HUTU-80 NHnFeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwNEezO|Uh|ryP MWDTRW5ITVJ?
HL-60 NEmxXppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTBwNEixOFIh|ryP NUXo[YpLW0GQR1XS
OCI-AML2 M4XLSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjuZZNKSzVyPUCuOFg{OjhizszN NEHTRoNUSU6JRWK=
ML-2 MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvFWmpKSzVyPUCuOFkxOzFizszN Mn7lV2FPT0WU
ES4 NXLKbIg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jZS2lEPTB;MD60PVExQSEQvF2= M1XsT3NCVkeHUh?=
NCI-H747 M{SxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwNEm4PUDPxE1? MkfWV2FPT0WU
RL95-2 MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLR[pJKSzVyPUCuOVAyOTJizszN NGHkZZlUSU6JRWK=
TE-15 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXTTWM2OD1yLkWxNVI1KM7:TR?= NE\mSm5USU6JRWK=
TE-12 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvjbXpKSzVyPUCuOVM{PDlizszN MYXTRW5ITVJ?
LB1047-RCC NE\P[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwNUS1OFkh|ryP NXjISIV3W0GQR1XS
LB831-BLC MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL2TmE3UUN3ME2wMlU2ODJ|IN88US=> NI\2c5pUSU6JRWK=
NCI-H1355 NVjhfW4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nGPWlEPTB;MD61OVE5PCEQvF2= NEHXUHRUSU6JRWK=
CTV-1 NWrl[HpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwNUW2NlQh|ryP M3ntR3NCVkeHUh?=
RXF393 M37Le2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\DZYNpUUN3ME2wMlU2Pzl2IN88US=> MkLFV2FPT0WU
SW872 M1vsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTDb5J6UUN3ME2wMlU3PzJ2IN88US=> NWf5WWNXW0GQR1XS
MPP-89 M13vRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwNUe4PFQh|ryP MkfpV2FPT0WU
RPMI-8226 NIKx[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfs[FRjUUN3ME2wMlY{PTJ4IN88US=> NI\WcXJUSU6JRWK=
LS-1034 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nNcWlEPTB;MD62N|U5KM7:TR?= NYHIXIlkW0GQR1XS
SJSA-1 NVLqXWlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXSyZnp2UUN3ME2wMlY{PzJ3IN88US=> NUntW2VkW0GQR1XS
HOP-62 M4\4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwNkWwN|Mh|ryP M1\LNnNCVkeHUh?=
KGN Mk\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwNk[xOlgh|ryP NULIRVR2W0GQR1XS
D-336MG MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\tTWM2OD1yLk[2NVY6KM7:TR?= NYrtUnluW0GQR1XS
LS-411N MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXiNopoUUN3ME2wMlY4PDZ{IN88US=> M17Nb3NCVkeHUh?=
TE-1 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PwZWlEPTB;MD62PVA4PCEQvF2= Mnv4V2FPT0WU
LB996-RCC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\uTXZYUUN3ME2wMlY6Ozh7IN88US=> NWD0eoFrW0GQR1XS
TE-10 Mn;aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPoUGl6UUN3ME2wMlcyPDl4IN88US=> NYXMVYdnW0GQR1XS
NCI-SNU-16 MnrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwN{K2OlQh|ryP M2\TNnNCVkeHUh?=
ES8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnyxTWM2OD1yLke0PVc2KM7:TR?= Mm\5V2FPT0WU
COLO-800 NInxN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwN{[2PVUh|ryP MkHBV2FPT0WU
ES6 NHLYVZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwN{e1OVkh|ryP MULTRW5ITVJ?
L-363 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfjSYVKSzVyPUCuPFI{PzVizszN MVLTRW5ITVJ?
NMC-G1 NY[3NIxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3ZTWM2OD1yLkizNlM{KM7:TR?= MonCV2FPT0WU
LU-134-A Mof1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwOEO5NVIh|ryP NH3zcpdUSU6JRWK=
SF268 MmHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOwOVVSUUN3ME2wMlg1ODR{IN88US=> MkK3V2FPT0WU
KARPAS-45 NVzXe41OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W1VWlEPTB;MD64OFI3OyEQvF2= NX3x[WtHW0GQR1XS
TGW M1jZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwOEW4OlMh|ryP MXHTRW5ITVJ?
CHP-126 NGix[XFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HIcWlEPTB;MD64OVk2PyEQvF2= Ml3WV2FPT0WU
MOLT-16 NFLSU5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q2dmlEPTB;MD64O|U5QSEQvF2= M4TzeXNCVkeHUh?=
LB771-HNC NXfDeYRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDHTWM2OD1yLki5O|U4KM7:TR?= NVi3e3o1W0GQR1XS
NALM-6 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PSXGlEPTB;MD65NFc{QSEQvF2= M1nkdXNCVkeHUh?=
GCIY NGPrZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwOUW1NlYh|ryP Mnj0V2FPT0WU
IST-MES1 NWLKenJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfWfWF1UUN3ME2wMlk5QDJ2IN88US=> NFnMZYhUSU6JRWK=
LB2241-RCC MlPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHlWGdYUUN3ME2wMlk5QDRizszN Ml6xV2FPT0WU
BL-70 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3QfXZjUUN3ME2wMlk6PTN3IN88US=> MVnTRW5ITVJ?
NB17 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP4UXZKSzVyPUGuNFA3OzlizszN MkfuV2FPT0WU
LXF-289 M1LKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3mSoNDUUN3ME2xMlA{ODd4IN88US=> MmXoV2FPT0WU
TK10 MmPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFwMEWwOlMh|ryP MXLTRW5ITVJ?
K5 MnPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwME[yO|Qh|ryP MnfyV2FPT0WU
NCI-H716 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnpTWM2OD1zLkC3NlU6KM7:TR?= MY\TRW5ITVJ?
HCE-T NGm0cIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwMEi4NVkh|ryP MWnTRW5ITVJ?
GI-1 NGXiTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnCRmVKSzVyPUGuNFk4QThizszN NV\nTWUyW0GQR1XS
KARPAS-422 MkTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTvTWM2OD1zLkGwNFIzKM7:TR?= MmnKV2FPT0WU
TE-9 NHnBOnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwMUGzNlgh|ryP NFHGeVVUSU6JRWK=
SF126 Mkn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFwMUG1Olgh|ryP NYDJe41TW0GQR1XS
BB30-HNC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7KeWxWUUN3ME2xMlE{OTF{IN88US=> NFXNbWlUSU6JRWK=
NCI-H1304 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XCd2lEPTB;MT6xN|M{QCEQvF2= NUfpVoVKW0GQR1XS
HEL MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[xU2lEPTB;MT6xOFg6PSEQvF2= NHrmU49USU6JRWK=
HAL-01 MoDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTVTWM2OD1zLkG1Nlg{KM7:TR?= NWewSo1XW0GQR1XS
SK-LMS-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrvcVE6UUN3ME2xMlE2QTd2IN88US=> MXjTRW5ITVJ?
SW954 NV\pOnlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojYTWM2OD1zLkG5OVY4KM7:TR?= MVXTRW5ITVJ?
D-283MED NGP4UG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELtc3pKSzVyPUGuNlI{PzlizszN MUPTRW5ITVJ?
NCI-H1882 MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPSZ3M1UUN3ME2xMlI{QDlizszN MVrTRW5ITVJ?
GI-ME-N NHG2ZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknPTWM2OD1zLkK1NlA5KM7:TR?= NWDafGVHW0GQR1XS
SK-PN-DW MluwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHTU2hKSzVyPUGuNlY{PDhizszN NWTufXpYW0GQR1XS
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HCC2157 NF36[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC5WHlKSzVyPUGuOFY3PTlizszN NF3SXmlUSU6JRWK=
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HCE-4 NH;JRlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7FemdKSzVyPUGuOlA5PSEQvF2= MorIV2FPT0WU
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NCI-H526 M33sNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jTe2lEPTB;Mj6xPVE1OSEQvF2= M4K1UXNCVkeHUh?=
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NCI-H1417 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmCzTWM2OD12LkK4OFQ{KM7:TR?= NEjCWpRUSU6JRWK=
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Becker NV;UUGVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3qTWM2OD12LkS3N|M3KM7:TR?= MXHTRW5ITVJ?
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KE-37 M4DSVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTRwOE[xPVYh|ryP MYTTRW5ITVJ?
NCI-H23 MlHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTRwOEeyNlch|ryP MmTFV2FPT0WU
MC116 NEHSOotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1H0N2lEPTB;ND65OFEzPiEQvF2= MWTTRW5ITVJ?
NH-12 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTkTWM2OD12Lkm2OFM6KM7:TR?= MoLTV2FPT0WU
CTB-1 M3PjSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTRwOUe3NlEh|ryP NYf4dFhXW0GQR1XS
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NCI-H2141 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf5V3VKSzVyPUWuNVQzPjhizszN M3PDXnNCVkeHUh?=
EB-3 Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVH3V|RkUUN3ME21MlE4PTB2IN88US=> Ml7CV2FPT0WU
NCI-H1522 NVu1OGhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC4ZXpKSzVyPUWuNlY{OjJizszN Mn7DV2FPT0WU
MRK-nu-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETmeFNKSzVyPUWuOFM3OzNizszN MkPDV2FPT0WU
no-11 M3jnbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HZVGlEPTB;NT60O|A5PyEQvF2= NX20VVJ5W0GQR1XS
CESS MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfDTWM2OD13LkW4NFM1KM7:TR?= NU\q[Xh[W0GQR1XS
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MMAC-SF MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPxW2hKSzVyPUeuNFY1QTJizszN MoTTV2FPT0WU
RCC10RGB NITKeJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3aTWM2OD15LkKyPVc4KM7:TR?= M33lZ3NCVkeHUh?=
NCI-H322M NYnYRZlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLUTWM2OD15LkOzN|M2KM7:TR?= M3nnZ3NCVkeHUh?=
NB6 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnUSWJKSzVyPUeuOVQ5QTlizszN MXfTRW5ITVJ?
MN-60 MnnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTdwNkmyNVUh|ryP MVrTRW5ITVJ?
NCI-H1092 NVrRdno5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLFTWM2OD16LkCxO|M1KM7:TR?= NVLqOYh{W0GQR1XS
EKVX Mn64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M163VWlEPTB;OD60O|A3PiEQvF2= NVvxeXQyW0GQR1XS
D-263MG NFjIU5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jMbWlEPTB;OD61OVM6PiEQvF2= M{DJOXNCVkeHUh?=
NCI-H209 NUPX[21GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvYNGNKSzVyPUiuOlQxODZizszN MUPTRW5ITVJ?
IST-SL1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf6TWM2OD16Lki5PFkzKM7:TR?= NXfWN4Z4W0GQR1XS
ACN M2DLV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIX6b3JKSzVyPUmuNVkyPTdizszN NG[4blFUSU6JRWK=
MHH-PREB-1 NXnOeZdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHFSnN5UUN3ME25MlIyOjF7IN88US=> M3jwXXNCVkeHUh?=
EW-11 NUHyZZNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXnOo9KSzVyPUmuOlU{QTZizszN NISzS2tUSU6JRWK=
KASUMI-1 M1:0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\DOm5KSzVyPUmuO|g4PyEQvF2= MVzTRW5ITVJ?
KINGS-1 NFOwWW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFyLkKzOFch|ryP MWDTRW5ITVJ?
EVSA-T MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:zNpdvUUN3ME2xNE4{OTl{IN88US=> MlHWV2FPT0WU
DSH1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jyZ2lEPTB;MUCuN|k4OiEQvF2= MWrTRW5ITVJ?
COLO-824 M{Kxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTKWW5KSzVyPUGwMlg3PjlizszN M4LoZXNCVkeHUh?=
K052 MoqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHFTWM2OD1zMD65N|IzKM7:TR?= NXTk[2dpW0GQR1XS
SK-MEL-2 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom3TWM2OD1zMD65PVM6KM7:TR?= M2jSSXNCVkeHUh?=

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol, pH 4
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
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    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):
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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:

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

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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