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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Cited by 20 Publications

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 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjNbWtqUUN3ME2wMlAxODB4MEOg{txO MVPTRW5ITVJ?
SF539 MnPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfoOYpLUUN3ME2wMlAxODV4NDFOwG0> MnLBV2FPT0WU
DEL MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3GzSWlEPTB;MD6wNFA6OjdizszN Ml71V2FPT0WU
NB1 M{G4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXYVXhvUUN3ME2wMlAxOTZ{IN88US=> MVLTRW5ITVJ?
SR NFLXfJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfpTWM2OD1yLkCwNlc4KM7:TR?= MknNV2FPT0WU
KARPAS-299 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMEKzPFQh|ryP MXnTRW5ITVJ?
MHH-CALL-2 M4\FTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfNTWM2OD1yLkCyPVUzKM7:TR?= MVjTRW5ITVJ?
SU-DHL-1 M{TzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33V[mlEPTB;MD6wOFg3PSEQvF2= Ml3UV2FPT0WU
A4-Fuk Mk\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwMEW1OlUh|ryP M{\JOXNCVkeHUh?=
EW-1 M1;BRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4n0cmlEPTB;MD6xNFI2PiEQvF2= MlH5V2FPT0WU
NOS-1 NH;WRVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PEZmlEPTB;MD6xNFI6PCEQvF2= MmjoV2FPT0WU
EW-16 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPoTWM2OD1yLkGwOVY5KM7:TR?= MV7TRW5ITVJ?
TE-11 M2X4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrJOpRjUUN3ME2wMlE3ODl4IN88US=> M2fxVXNCVkeHUh?=
SW982 NF;4Z5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMU[0O|gh|ryP MWHTRW5ITVJ?
LAN-6 NVywU3hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLUTWM2OD1yLkG3OFQ{KM7:TR?= NWDvOI8{W0GQR1XS
MZ1-PC NVrSeWQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4eyRWlEPTB;MD6xO|g{PSEQvF2= M4PMfnNCVkeHUh?=
KS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXO2[G1bUUN3ME2wMlE6OzR|IN88US=> MVPTRW5ITVJ?
PSN1 MkTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmf3TWM2OD1yLkG5OlMyKM7:TR?= NWnLSYgzW0GQR1XS
LC-2-ad MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMUm2PVIh|ryP M371dnNCVkeHUh?=
COLO-320-HSR M4XwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;LfYRKSzVyPUCuNVk4PzZizszN Mn3tV2FPT0WU
OPM-2 NWnFSm9UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLpU|FKSzVyPUCuNlI3PjlizszN MUfTRW5ITVJ?
SK-NEP-1 Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7oTWM2OD1yLkKzOVI1KM7:TR?= NG\0d2ZUSU6JRWK=
ALL-PO M3e4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTBwMkS1NlQh|ryP M{Lxb3NCVkeHUh?=
CMK M4LSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTBwMkW1N{DPxE1? NU\FRYdEW0GQR1XS
NCI-H1648 NETjb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP3TWM2OD1yLkK3PFU2KM7:TR?= NXX6U|YyW0GQR1XS
SIG-M5 MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;PW4FQUUN3ME2wMlI6OTV7IN88US=> MVHTRW5ITVJ?
TGBC24TKB M{fqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\TR2lEPTB;MD6zNFIyQCEQvF2= MkXIV2FPT0WU
DOHH-2 M{f5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7oPHpUUUN3ME2wMlMyOjB2IN88US=> NY\ZdpVuW0GQR1XS
NB69 NF24PIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwM{G3PFch|ryP Mn;XV2FPT0WU
MFH-ino MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwM{K1NlMh|ryP MVTTRW5ITVJ?
KP-N-RT-BM-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTNTGw{UUN3ME2wMlM{OTJ|IN88US=> MlGwV2FPT0WU
MONO-MAC-6 NYDI[JJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXu0bmFWUUN3ME2wMlM{OjlzIN88US=> NG\5bllUSU6JRWK=
ATN-1 MoTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[4dGlEPTB;MD6zN|MxOyEQvF2= NYCwVJN3W0GQR1XS
NTERA-S-cl-D1 MnjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwM{OzPVYh|ryP NF3GS|BUSU6JRWK=
L-540 NVv4WHQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfyTWM2OD1yLkO2PVg5KM7:TR?= M2noSXNCVkeHUh?=
GB-1 NUHhOWx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwM{i4Olch|ryP MXLTRW5ITVJ?
MV-4-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwM{m0OFYh|ryP NVnmd4d2W0GQR1XS
KG-1 MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnxXoZ6UUN3ME2wMlM6PTZzIN88US=> M4D3XXNCVkeHUh?=
OVCAR-4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHaWlhRUUN3ME2wMlQxPTZ7IN88US=> Mnr2V2FPT0WU
NEC8 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfxb4o5UUN3ME2wMlQyOjl{IN88US=> NYq5cHNvW0GQR1XS
SK-MM-2 MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DieWlEPTB;MD60NVYxQSEQvF2= NWTJ[HhWW0GQR1XS
TE-8 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjNTWM2OD1yLkSyPFgh|ryP MX\TRW5ITVJ?
697 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTUTWM2OD1yLkSzNlE2KM7:TR?= NXexflNXW0GQR1XS
NB14 NXzoSG9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof3TWM2OD1yLkSzPFI3KM7:TR?= NGfuSnBUSU6JRWK=
GDM-1 M3nLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrYTWM2OD1yLkS3NVE3KM7:TR?= M{PFcXNCVkeHUh?=
HUTU-80 MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;aV3pKSzVyPUCuOFc{PzVizszN MlzaV2FPT0WU
HL-60 NFuyOWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[1OW9KSzVyPUCuOFgyPDJizszN NXny[HlUW0GQR1XS
OCI-AML2 M{PHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\DTWM2OD1yLkS4N|I5KM7:TR?= M2K1T3NCVkeHUh?=
ML-2 NWTCUHJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPtTWM2OD1yLkS5NFMyKM7:TR?= NE\zVmlUSU6JRWK=
ES4 NYfqOm1ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWruSWlnUUN3ME2wMlQ6OTB7IN88US=> MnyyV2FPT0WU
NCI-H747 NGLCdlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv4TWM2OD1yLkS5PFkh|ryP M1iwO3NCVkeHUh?=
RL95-2 NVTJO4s3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljGTWM2OD1yLkWwNVEzKM7:TR?= MnLGV2FPT0WU
TE-15 MoO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIezXG1KSzVyPUCuOVEyOjRizszN NWrHeXI5W0GQR1XS
TE-12 MomxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHzTWM2OD1yLkWzN|Q6KM7:TR?= NFfJepZUSU6JRWK=
LB1047-RCC M4\Oemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvzcHVKSzVyPUCuOVQ2PDlizszN NVzPZm9OW0GQR1XS
LB831-BLC NXL5XWFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{e5U2lEPTB;MD61OVAzOyEQvF2= NYi3cHozW0GQR1XS
NCI-H1355 M3z0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrycIV5UUN3ME2wMlU2OTh2IN88US=> MnXwV2FPT0WU
CTV-1 MonSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwNUW2NlQh|ryP Mli4V2FPT0WU
RXF393 Mm\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHzR45SUUN3ME2wMlU2Pzl2IN88US=> NUnvS5pPW0GQR1XS
SW872 MnqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEntd|dKSzVyPUCuOVY4OjRizszN MXHTRW5ITVJ?
MPP-89 Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;5OnpKSzVyPUCuOVc5QDRizszN MlHlV2FPT0WU
RPMI-8226 NH\lSY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXyXppKSzVyPUCuOlM2OjZizszN MWrTRW5ITVJ?
LS-1034 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PwW2lEPTB;MD62N|U5KM7:TR?= M1:5d3NCVkeHUh?=
SJSA-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLHenJKSzVyPUCuOlM4OjVizszN MlexV2FPT0WU
HOP-62 M2HVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETuVFBKSzVyPUCuOlUxOzNizszN M{fSUnNCVkeHUh?=
KGN M{TGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPJU5FDUUN3ME2wMlY3OTZ6IN88US=> NVX2bYpyW0GQR1XS
D-336MG NHzMdWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvNTWM2OD1yLk[2NVY6KM7:TR?= M1XGbXNCVkeHUh?=
LS-411N NVyxbVBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\3OZR6UUN3ME2wMlY4PDZ{IN88US=> MVTTRW5ITVJ?
TE-1 M2PwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\2TWM2OD1yLk[5NFc1KM7:TR?= NYTUNG1kW0GQR1XS
LB996-RCC NIfreYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwNkmzPFkh|ryP M2na[nNCVkeHUh?=
TE-10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETHZW1KSzVyPUCuO|E1QTZizszN M4r0WnNCVkeHUh?=
NCI-SNU-16 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moi1TWM2OD1yLkeyOlY1KM7:TR?= NVHacmVUW0GQR1XS
ES8 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\VTWM2OD1yLke0PVc2KM7:TR?= MXLTRW5ITVJ?
COLO-800 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTOTWM2OD1yLke2Olk2KM7:TR?= NVHjU3Y4W0GQR1XS
ES6 M3m4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL3O2loUUN3ME2wMlc4PTV7IN88US=> Mn3HV2FPT0WU
L-363 M4Xafmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwOEKzO|Uh|ryP MW\TRW5ITVJ?
NMC-G1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLW[|R{UUN3ME2wMlg{OjN|IN88US=> Mn[5V2FPT0WU
LU-134-A NYf3dXNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPVOYdKSzVyPUCuPFM6OTJizszN M2LPUHNCVkeHUh?=
SF268 M4jucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXkW5U6UUN3ME2wMlg1ODR{IN88US=> MnPqV2FPT0WU
KARPAS-45 M37xb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nCbmlEPTB;MD64OFI3OyEQvF2= MUnTRW5ITVJ?
TGW NFXzOFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m3U2lEPTB;MD64OVg3OyEQvF2= NXXnfndtW0GQR1XS
CHP-126 M1rLNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVWxbIhsUUN3ME2wMlg2QTV5IN88US=> NWjadIZOW0GQR1XS
MOLT-16 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz2XGVKSzVyPUCuPFc2QDlizszN MmXuV2FPT0WU
LB771-HNC NYLmS|NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1izXGlEPTB;MD64PVc2PyEQvF2= Mn[2V2FPT0WU
NALM-6 M1Twbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIf4dGlKSzVyPUCuPVA4OzlizszN MWrTRW5ITVJ?
GCIY MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwOUW1NlYh|ryP NGjs[GdUSU6JRWK=
IST-MES1 NUDtenFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXYTWM2OD1yLkm4PFI1KM7:TR?= NHHO[nZUSU6JRWK=
LB2241-RCC MnP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HRNGlEPTB;MD65PFg1KM7:TR?= NUnNUnN6W0GQR1XS
BL-70 NHnhNoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli3TWM2OD1yLkm5OVM2KM7:TR?= M4DSPXNCVkeHUh?=
NB17 M3zR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwMEC2N|kh|ryP NXfiXXB4W0GQR1XS
LXF-289 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX2TWM2OD1zLkCzNFc3KM7:TR?= MXvTRW5ITVJ?
TK10 NFXNN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwMEWwOlMh|ryP NWrBcXpLW0GQR1XS
K5 M4TGbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF75RphKSzVyPUGuNFYzPzRizszN NGn0O3BUSU6JRWK=
NCI-H716 M3vrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwMEeyOVkh|ryP M3:wUnNCVkeHUh?=
HCE-T NUHiU2ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwMEi4NVkh|ryP NFS3U4RUSU6JRWK=
GI-1 NV6y[pBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XFW2lEPTB;MT6wPVc6QCEQvF2= MmfxV2FPT0WU
KARPAS-422 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPCV2x[UUN3ME2xMlExODJ{IN88US=> NFzXfXBUSU6JRWK=
TE-9 NG\QPXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHhNlBKSzVyPUGuNVE{OjhizszN NF\DcZhUSU6JRWK=
SF126 M2ToRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rzemlEPTB;MT6xNVU3QCEQvF2= NVrwPGtGW0GQR1XS
BB30-HNC NEHMUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwMUOxNVIh|ryP NULQeIQ6W0GQR1XS
NCI-H1304 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\5TWM2OD1zLkGzN|M5KM7:TR?= Mo\oV2FPT0WU
HEL Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jLRmlEPTB;MT6xOFg6PSEQvF2= MXHTRW5ITVJ?
HAL-01 M1jBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fpb2lEPTB;MT6xOVI5OyEQvF2= M1XMR3NCVkeHUh?=
SK-LMS-1 NHTBOm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PvXGlEPTB;MT6xOVk4PCEQvF2= NHXMeJlUSU6JRWK=
SW954 NHLRRo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D2WmlEPTB;MT6xPVU3PyEQvF2= NHjxWXBUSU6JRWK=
D-283MED MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwMkKzO|kh|ryP MnjiV2FPT0WU
NCI-H1882 MojTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTrTWM2OD1zLkKzPFkh|ryP NHLVXHhUSU6JRWK=
GI-ME-N NFrrdlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLTTWM2OD1zLkK1NlA5KM7:TR?= MXvTRW5ITVJ?
SK-PN-DW NFnNR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXCTWM2OD1zLkK2N|Q5KM7:TR?= NFXBVHFUSU6JRWK=
C2BBe1 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTFwMkmxNVch|ryP MmC5V2FPT0WU
A704 NEHKU|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXBWlFKSzVyPUGuN|I3QDlizszN MlixV2FPT0WU
KALS-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTJfZJRUUN3ME2xMlM1ODhizszN MmDtV2FPT0WU
ETK-1 NHn0XFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXRTWM2OD1zLkO0OFg6KM7:TR?= NYn4TJFMW0GQR1XS
LB647-SCLC M2TnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH70cW1KSzVyPUGuN|Q6QDZizszN NYDOO5FPW0GQR1XS
OCUB-M MlO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwM{[xOFMh|ryP NEG2R4FUSU6JRWK=
NCI-H720 MmPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTOTWM2OD1zLkO2N|c5KM7:TR?= MVPTRW5ITVJ?
NB13 NXTuPVVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LQcWlEPTB;MT6zO|I6OyEQvF2= MWDTRW5ITVJ?
GR-ST NUXYbmZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTUTWM2OD1zLkO4O|U4KM7:TR?= NXPIZ4xtW0GQR1XS
DU-4475 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXLRXZGUUN3ME2xMlQ2QDV|IN88US=> NV;6cndDW0GQR1XS
HCC2157 MkfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rjVWlEPTB;MT60OlY2QSEQvF2= M3fOS3NCVkeHUh?=
RKO NWfJSmpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLKfld3UUN3ME2xMlQ6QTJ{IN88US=> MWHTRW5ITVJ?
LS-123 M4\EVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HP[2lEPTB;MT61NVU6PCEQvF2= MUnTRW5ITVJ?
NCI-H69 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HGfWlEPTB;MT61OVgyOSEQvF2= MlvWV2FPT0WU
SW962 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFwNU[xN{DPxE1? NETV[pdUSU6JRWK=
PF-382 MlTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;m[G9FUUN3ME2xMlU3QTZizszN M1LBc3NCVkeHUh?=
A101D NIntSG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXuSoZKSzVyPUGuOVcyOTNizszN MV\TRW5ITVJ?
NB10 NImyR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PrVGlEPTB;MT61O|M6OiEQvF2= NHn2W4lUSU6JRWK=
NB5 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHyZZlKSzVyPUGuOVg1PzZizszN MYrTRW5ITVJ?
HCE-4 NHn5Z4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX5cpNwUUN3ME2xMlYxQDVizszN NFnBfFlUSU6JRWK=
HT-144 NFPUfIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwNkOxPUDPxE1? MlvQV2FPT0WU
NCI-H524 M3ruWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\SPZRKSzVyPUGuOlQ{ODdizszN MknUV2FPT0WU
NKM-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfQTWM2OD1zLk[4OlYh|ryP NIHkUYpUSU6JRWK=
KURAMOCHI NULnZVdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\rb2lEPTB;MT62PVU4OyEQvF2= NH3GbY1USU6JRWK=
NCI-H187 NYOyUYlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjETm9QUUN3ME2xMlcxODN4IN88US=> Mn;ZV2FPT0WU
U-266 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLFTWM2OD1zLkezPFQzKM7:TR?= M3\2[HNCVkeHUh?=
BL-41 Ml7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwN{[yO|Ih|ryP M3:3fnNCVkeHUh?=
SK-N-DZ MoXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXriOowzUUN3ME2xMlc5OzB7IN88US=> NIrRN3ZUSU6JRWK=
Daudi NVnHcI1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLoSIlKSzVyPUGuO|g6PjdizszN M4\hV3NCVkeHUh?=
CPC-N MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;KdVVXUUN3ME2xMlg2ODl4IN88US=> MU\TRW5ITVJ?
EM-2 NWrsVoFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXSO5ZKSzVyPUGuPFUyKM7:TR?= NIKzT5dUSU6JRWK=
HCC1187 NXrQTGQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3znSWlEPTB;MT64OlI1OSEQvF2= MYfTRW5ITVJ?
LP-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PLRWlEPTB;MT64O|E1OyEQvF2= NWTiOVVEW0GQR1XS
CAS-1 NHfVW2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jJeGlEPTB;MT65PFI6QSEQvF2= M{LLNHNCVkeHUh?=
NB7 M2i2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJwMEC1OVUh|ryP M3PrWHNCVkeHUh?=
VA-ES-BJ MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILi[ZlKSzVyPUKuNFE2OTNizszN M33RZXNCVkeHUh?=
SNU-C2B NHqzXXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJwMEOzOVEh|ryP Mk\OV2FPT0WU
LOXIMVI MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL5TWM2OD1{LkC2O|g3KM7:TR?= M1fXdHNCVkeHUh?=
NCI-H1581 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnSdoJIUUN3ME2yMlEyPTV7IN88US=> MWXTRW5ITVJ?
IST-SL2 NYLRU2FMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTJwMUK0OFUh|ryP NIrtToNUSU6JRWK=
NOMO-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PiNGlEPTB;Mj6xO|Y5OyEQvF2= NXG3Z|VCW0GQR1XS
TE-6 NXTGWnI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTiTXNYUUN3ME2yMlE6ODVizszN NYq4dnFvW0GQR1XS
NCI-H526 NVXUNZJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi1dYJYUUN3ME2yMlE6OTRzIN88US=> MY\TRW5ITVJ?
MSTO-211H NIf4[WRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFiwfVlKSzVyPUKuNlAxPDFizszN NUfmcplDW0GQR1XS
LS-513 M{[yO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXVTWM2OD1{LkKyNlY6KM7:TR?= NWDuemJGW0GQR1XS
NCI-SNU-1 M3zhRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTJwM{OyOVYh|ryP NUPLZW5ZW0GQR1XS
BB65-RCC Ml\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHhZnBKSzVyPUKuN|c1QTNizszN MnvzV2FPT0WU
GT3TKB NH\UelRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXjTWM2OD1{LkO5PVczKM7:TR?= NHTNNoJUSU6JRWK=
OS-RC-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnx[4RKSzVyPUKuOFI{PDFizszN NYPPS|NuW0GQR1XS
NCI-H2126 M1nI[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLoR4xKSzVyPUKuOFM3PzRizszN MYLTRW5ITVJ?
SK-UT-1 MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJwNEe0Olch|ryP NGW2T|JUSU6JRWK=
DMS-114 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXsTWM2OD1{Lk[xOVI1KM7:TR?= M4DNPHNCVkeHUh?=
ONS-76 MlG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDkRpdKSzVyPUKuOlM3PDFizszN MV3TRW5ITVJ?
8-MG-BA M{\BVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\3[FBVUUN3ME2yMlY2PDF2IN88US=> NVztTm0zW0GQR1XS
BOKU MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljuTWM2OD1{LkeyO|Y1KM7:TR?= M3LBW3NCVkeHUh?=
LAMA-84 NG\wO4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuzTWM2OD1{Lke5PVEzKM7:TR?= NHjzd45USU6JRWK=
ES1 MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJwOEG4NFQh|ryP MWHTRW5ITVJ?
NCI-H1395 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\MTWM2OD1{LkiyNFEzKM7:TR?= MlnWV2FPT0WU
A388 M2fIUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjDTWM2OD1{Lkm2NVch|ryP NXfOV|Q{W0GQR1XS
NCCIT M1\FeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TmemlEPTB;Mz6wPFg3OiEQvF2= NXSzRYpmW0GQR1XS
HD-MY-Z NECweZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nNeGlEPTB;Mz6xN|IxOyEQvF2= MUDTRW5ITVJ?
NCI-H510A M3v5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTNwMUi5OFMh|ryP NVzJZ|NsW0GQR1XS
NCI-N87 MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD2VVZCUUN3ME2zMlIxODJizszN NIn0NWpUSU6JRWK=
SCLC-21H MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonETWM2OD1|LkK2PFU6KM7:TR?= NFv6RVNUSU6JRWK=
SH-4 NG\mZZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HLfmlEPTB;Mz6yPFc6PyEQvF2= M3vpOnNCVkeHUh?=
QIMR-WIL MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nHRWlEPTB;Mz6zNlg1QSEQvF2= M3HTdHNCVkeHUh?=
KM12 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO2TWM2OD1|LkOzOVQ1KM7:TR?= MWHTRW5ITVJ?
ST486 MkD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\0TWM2OD1|LkWzPFg{KM7:TR?= NIPQbFhUSU6JRWK=
HC-1 NXrPZYNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjjTWM2OD1|Lk[yNFI5KM7:TR?= Mn\KV2FPT0WU
BV-173 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fzbWlEPTB;Mz62OFA5QCEQvF2= NWGxSWxRW0GQR1XS
EW-24 NX\mOW5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFiwNGdKSzVyPUOuOlY1OzRizszN NH3sd5BUSU6JRWK=
LU-65 NGraVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTNwNki3NUDPxE1? MkXrV2FPT0WU
ECC4 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIWx[ZhKSzVyPUOuO|c2PiEQvF2= NWX6cld5W0GQR1XS
ARH-77 NWXLSI5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\ITWM2OD12LkGxNFY4KM7:TR?= NXPyfZhTW0GQR1XS
BC-3 NUnreIFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXLeHE4UUN3ME20MlE{ODZ6IN88US=> MlHFV2FPT0WU
SNB75 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXQTWM2OD12LkK2NVkh|ryP MmLXV2FPT0WU
MEG-01 M2[0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[ySlV4UUN3ME20MlI4PDF7IN88US=> MlPUV2FPT0WU
NCI-H1417 MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXvV3JLUUN3ME20MlI5PDR|IN88US=> NVjwWpZWW0GQR1XS
MDA-MB-134-VI MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzJTWM2OD12LkOwOlAyKM7:TR?= Mk\DV2FPT0WU
Becker NY[1b2xkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTRwNEezN|Yh|ryP M1;pXXNCVkeHUh?=
DMS-153 NHLjeJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjhTWM2OD12Lk[2OFc2KM7:TR?= NY\4UWxpW0GQR1XS
TGBC1TKB NEHBNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPXTWM2OD12Lk[4OVE2KM7:TR?= NEDDRodUSU6JRWK=
EW-3 NYT4UXVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq4TWM2OD12Lke2NlQ5KM7:TR?= NXXMdY1kW0GQR1XS
KE-37 NUTQOG1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rYPGlEPTB;ND64OlE6PiEQvF2= NHr3VJVUSU6JRWK=
NCI-H23 M1TCTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[wTWM2OD12Lki3NlI4KM7:TR?= M1ewfnNCVkeHUh?=
MC116 M4rhSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHNUYlpUUN3ME20Mlk1OTJ4IN88US=> NWXFRWt5W0GQR1XS
NH-12 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO5TWM2OD12Lkm2OFM6KM7:TR?= NYrHd5ViW0GQR1XS
CTB-1 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnrTWM2OD12Lkm3O|IyKM7:TR?= MXvTRW5ITVJ?
KM-H2 NIrVTYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DZVWlEPTB;NT6wOVMzOyEQvF2= MlvoV2FPT0WU
MOLT-4 NHPpTmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTVwMUG4N{DPxE1? M3:1fnNCVkeHUh?=
NCI-H2141 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;tTWM2OD13LkG0NlY5KM7:TR?= M3[0UnNCVkeHUh?=
EB-3 M1;NUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTVwMUe1NFQh|ryP NF7LNHhUSU6JRWK=
NCI-H1522 NGjtXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTVwMk[zNlIh|ryP MUnTRW5ITVJ?
MRK-nu-1 M3zJSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTVwNEO2N|Mh|ryP MXjTRW5ITVJ?
no-11 M1nWVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPnTWM2OD13LkS3NFg4KM7:TR?= NGC2VJVUSU6JRWK=
CESS NEXLO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHBN3FjUUN3ME21MlU5ODN2IN88US=> MWLTRW5ITVJ?
KMOE-2 NX\v[3Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7OTWM2OD13LkW4OlU6KM7:TR?= NH\zZlNUSU6JRWK=
REH NUHFN29LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1S3NGlEPTB;Nj6yOVYyQCEQvF2= NUfWSIZUW0GQR1XS
KU812 Mn;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPN[ZFKSzVyPU[uOFI4QTFizszN MnPtV2FPT0WU
SK-N-FI Mn\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTIUGdKSzVyPU[uOlA3PzRizszN NHTnSnVUSU6JRWK=
MMAC-SF NHzFPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTdwME[0PVIh|ryP NEjMZ25USU6JRWK=
RCC10RGB NGHER3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzKS2F4UUN3ME23MlIzQTd5IN88US=> MV;TRW5ITVJ?
NCI-H322M MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjPdVJKUUN3ME23MlM{OzN3IN88US=> MXTTRW5ITVJ?
NB6 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHSfI1KSzVyPUeuOVQ5QTlizszN M4G3dHNCVkeHUh?=
MN-60 NIfNRoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDwOYwzUUN3ME23MlY6OjF3IN88US=> NVOxNZNkW0GQR1XS
NCI-H1092 M3OyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInxdGpKSzVyPUiuNFE4OzRizszN M3rPZnNCVkeHUh?=
EKVX MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PRV2lEPTB;OD60O|A3PiEQvF2= MnLKV2FPT0WU
D-263MG NX35TXQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRThwNUWzPVYh|ryP MlzxV2FPT0WU
NCI-H209 MlzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TpeGlEPTB;OD62OFAxPiEQvF2= MWrTRW5ITVJ?
IST-SL1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPiV3NKUUN3ME24Mlg6QDl{IN88US=> MoHqV2FPT0WU
ACN M3XaV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XMR2lEPTB;OT6xPVE2PyEQvF2= M2nZTHNCVkeHUh?=
MHH-PREB-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr0TVdqUUN3ME25MlIyOjF7IN88US=> NVjocFdEW0GQR1XS
EW-11 Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTlwNkWzPVYh|ryP M{W1PHNCVkeHUh?=
KASUMI-1 NGK0PJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXxUWVTUUN3ME25Mlc5PzdizszN M4OzPXNCVkeHUh?=
KINGS-1 NEHUUXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13WdmlEPTB;MUCuNlM1PyEQvF2= MlPsV2FPT0WU
EVSA-T Ml\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\USYlpUUN3ME2xNE4{OTl{IN88US=> NXvFdINSW0GQR1XS
DSH1 MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXsUoNKSzVyPUGwMlM6PzJizszN NWm5cpJmW0GQR1XS
COLO-824 NHy3T2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTuSpRyUUN3ME2xNE45PjZ7IN88US=> MWrTRW5ITVJ?
K052 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFyLkmzNlIh|ryP M3X0ZXNCVkeHUh?=
SK-MEL-2 NHvqPIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULDW4lUUUN3ME2xNE46QTN7IN88US=> MWrTRW5ITVJ?

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol, pH 4
For best results, use promptly after mixing.
10 mg/mL

* 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)

  • 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
    V1
    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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