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 27 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 MlX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\zTWM2OD1yLkCwNFA3ODNizszN M{T3cnNCVkeHUh?=
SF539 NVnOdYs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG4TWM2OD1yLkCwNFU3PCEQvF2= MoHLV2FPT0WU
DEL NFjMXIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfqUVhKSzVyPUCuNFAxQTJ5IN88US=> MWLTRW5ITVJ?
NB1 NFOwVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMECxOlIh|ryP M3TKXnNCVkeHUh?=
SR NVjUbVJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jXV2lEPTB;MD6wNFI4PyEQvF2= NIDHUI9USU6JRWK=
KARPAS-299 MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLwTZZKSzVyPUCuNFI{QDRizszN NUHBbHdXW0GQR1XS
MHH-CALL-2 M3L6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXUTWM2OD1yLkCyPVUzKM7:TR?= MYjTRW5ITVJ?
SU-DHL-1 MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvqNWZKSzVyPUCuNFQ5PjVizszN NV71cIFoW0GQR1XS
A4-Fuk NH3XNlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHMTWM2OD1yLkC1OVY2KM7:TR?= NUH1Sm1oW0GQR1XS
EW-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\zTWM2OD1yLkGwNlU3KM7:TR?= NYjB[I01W0GQR1XS
NOS-1 NWLWTYlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMUCyPVQh|ryP NY\pXWZWW0GQR1XS
EW-16 NHL2XmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\5bYd5UUN3ME2wMlExPTZ6IN88US=> M3[0[XNCVkeHUh?=
TE-11 NVKwe41HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzGTWM2OD1yLkG2NFk3KM7:TR?= Mn;vV2FPT0WU
SW982 NV7pe3pkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH6VoZKSzVyPUCuNVY1PzhizszN NEi0bJpUSU6JRWK=
LAN-6 NEHPOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwMUe0OFMh|ryP MnPlV2FPT0WU
MZ1-PC NXfhNFlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknFTWM2OD1yLkG3PFM2KM7:TR?= NGm0[nFUSU6JRWK=
KS-1 NGLhe4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3DTWM2OD1yLkG5N|Q{KM7:TR?= NIeyWoNUSU6JRWK=
PSN1 NVTQVmhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWGwemlSUUN3ME2wMlE6PjNzIN88US=> MYfTRW5ITVJ?
LC-2-ad NHLTbJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwMUm2PVIh|ryP M4\BXXNCVkeHUh?=
COLO-320-HSR NXjpfotqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTD[WozUUN3ME2wMlE6Pzd4IN88US=> NXrLboJnW0GQR1XS
OPM-2 Ml;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LveGlEPTB;MD6yNlY3QSEQvF2= Mn;OV2FPT0WU
SK-NEP-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMkO1NlQh|ryP NX;nem8{W0GQR1XS
ALL-PO NH3yOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMkS1NlQh|ryP MVzTRW5ITVJ?
CMK NX3XXmZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v4OGlEPTB;MD6yOVU{KM7:TR?= NYT6TWpbW0GQR1XS
NCI-H1648 MkPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknKTWM2OD1yLkK3PFU2KM7:TR?= NVqySGRuW0GQR1XS
SIG-M5 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXB[VVZUUN3ME2wMlI6OTV7IN88US=> NHzjbGxUSU6JRWK=
TGBC24TKB MnnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DITmlEPTB;MD6zNFIyQCEQvF2= NXP0[m53W0GQR1XS
DOHH-2 NFyxfYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwM{GyNFQh|ryP NH;zPIxUSU6JRWK=
NB69 M1TWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwM{G3PFch|ryP MlrkV2FPT0WU
MFH-ino MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwM{K1NlMh|ryP MYjTRW5ITVJ?
KP-N-RT-BM-1 MoflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwM{OxNlMh|ryP Mof6V2FPT0WU
MONO-MAC-6 M1rZZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwM{OyPVEh|ryP MYXTRW5ITVJ?
ATN-1 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnUVlV3UUN3ME2wMlM{OzB|IN88US=> MWTTRW5ITVJ?
NTERA-S-cl-D1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\FOo5KSzVyPUCuN|M{QTZizszN MkjaV2FPT0WU
L-540 NIPhWVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zMR2lEPTB;MD6zOlk5QCEQvF2= Ml3RV2FPT0WU
GB-1 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLJTWM2OD1yLkO4PFY4KM7:TR?= NH7GXWtUSU6JRWK=
MV-4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwM{m0OFYh|ryP NFe5NlRUSU6JRWK=
KG-1 NVu3O4JxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfte5BFUUN3ME2wMlM6PTZzIN88US=> M4Dm[3NCVkeHUh?=
OVCAR-4 NHvPSGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;kRmlEPTB;MD60NFU3QSEQvF2= M1rZRnNCVkeHUh?=
NEC8 NH;TeYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTBwNEGyPVIh|ryP NGCz[25USU6JRWK=
SK-MM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHpcVZWUUN3ME2wMlQyPjB7IN88US=> NHPSZ|RUSU6JRWK=
TE-8 NXLte291T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnPTWM2OD1yLkSyPFgh|ryP MmLkV2FPT0WU
697 MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwNEOyNVUh|ryP NFnOdFJUSU6JRWK=
NB14 NYjk[GF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwNEO4NlYh|ryP NWjlT2VXW0GQR1XS
GDM-1 MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1POWWlEPTB;MD60O|EyPiEQvF2= MVLTRW5ITVJ?
HUTU-80 MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwNEezO|Uh|ryP NGPNRW9USU6JRWK=
HL-60 NX;LW4RoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\Yd5duUUN3ME2wMlQ5OTR{IN88US=> NYT1[ZJCW0GQR1XS
OCI-AML2 NHvQU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7yRo1zUUN3ME2wMlQ5OzJ6IN88US=> NYjK[mI1W0GQR1XS
ML-2 MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwNEmwN|Eh|ryP MmPCV2FPT0WU
ES4 NXPTSIprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwNEmxNFkh|ryP NF7UbJZUSU6JRWK=
NCI-H747 NV7ndFd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXY[IZsUUN3ME2wMlQ6QDlizszN MnLDV2FPT0WU
RL95-2 NW\HfWFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL5WYVmUUN3ME2wMlUxOTF{IN88US=> NEDZTGxUSU6JRWK=
TE-15 M3XsbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LvcmlEPTB;MD61NVEzPCEQvF2= MUjTRW5ITVJ?
TE-12 Mn;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwNUOzOFkh|ryP NWDXemdYW0GQR1XS
LB1047-RCC NVzWcHdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPmZ3dKSzVyPUCuOVQ2PDlizszN MVTTRW5ITVJ?
LB831-BLC NFSyboxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL2TWM2OD1yLkW1NFI{KM7:TR?= NIHnW3FUSU6JRWK=
NCI-H1355 NFPEUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[1TWM2OD1yLkW1NVg1KM7:TR?= MXnTRW5ITVJ?
CTV-1 NUTudlFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfRTWM2OD1yLkW1OlI1KM7:TR?= MoDhV2FPT0WU
RXF393 M1z6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3HTVRlUUN3ME2wMlU2Pzl2IN88US=> NGjybIRUSU6JRWK=
SW872 M4P3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7MTXM2UUN3ME2wMlU3PzJ2IN88US=> NV[0boVnW0GQR1XS
MPP-89 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Hp[WlEPTB;MD61O|g5PCEQvF2= MWXTRW5ITVJ?
RPMI-8226 NULtOY92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LG[mlEPTB;MD62N|UzPiEQvF2= M1fpW3NCVkeHUh?=
LS-1034 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXyW2NHUUN3ME2wMlY{PThizszN NVKxXJRlW0GQR1XS
SJSA-1 NH3PVItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwNkO3NlUh|ryP NYrPRpZYW0GQR1XS
HOP-62 M{L2VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwNkWwN|Mh|ryP NFr2SIxUSU6JRWK=
KGN MkW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwNk[xOlgh|ryP NXrtVlNCW0GQR1XS
D-336MG MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[5eGlEPTB;MD62OlE3QSEQvF2= Mm\BV2FPT0WU
LS-411N MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHG1S3pKSzVyPUCuOlc1PjJizszN M2rzUXNCVkeHUh?=
TE-1 NEjMXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXFeFZKSzVyPUCuOlkxPzRizszN M{PnRnNCVkeHUh?=
LB996-RCC M4nyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fvN2lEPTB;MD62PVM5QSEQvF2= M2rhbXNCVkeHUh?=
TE-10 M{TGWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIO2ellKSzVyPUCuO|E1QTZizszN NGfsbY9USU6JRWK=
NCI-SNU-16 M3;5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTQVXFKSzVyPUCuO|I3PjRizszN MX;TRW5ITVJ?
ES8 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF62cFhKSzVyPUCuO|Q6PzVizszN NVfUZ4t7W0GQR1XS
COLO-800 NF\6Z|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLaTWM2OD1yLke2Olk2KM7:TR?= NIr6eWxUSU6JRWK=
ES6 NYLmU21zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\BWZlKSzVyPUCuO|c2PTlizszN NHOyXGxUSU6JRWK=
L-363 M2W0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnXPHdDUUN3ME2wMlgzOzd3IN88US=> MkT6V2FPT0WU
NMC-G1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwOEOyN|Mh|ryP MXzTRW5ITVJ?
LU-134-A M{jncGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\JbpJEUUN3ME2wMlg{QTF{IN88US=> NVvGRmlRW0GQR1XS
SF268 NHrRN4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLyTWM2OD1yLki0NFQzKM7:TR?= NE\MdVBUSU6JRWK=
KARPAS-45 Mmj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;WeFhmUUN3ME2wMlg1OjZ|IN88US=> Mn7lV2FPT0WU
TGW NH71cFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXOTWM2OD1yLki1PFY{KM7:TR?= MlPvV2FPT0WU
CHP-126 M1naVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTFNYc3UUN3ME2wMlg2QTV5IN88US=> MYrTRW5ITVJ?
MOLT-16 NVW2VlB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD1enB5UUN3ME2wMlg4PTh7IN88US=> NEDyd|dUSU6JRWK=
LB771-HNC NITEdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq5TWM2OD1yLki5O|U4KM7:TR?= M3Pre3NCVkeHUh?=
NALM-6 MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTzUlFVUUN3ME2wMlkxPzN7IN88US=> NIDvWoxUSU6JRWK=
GCIY M2\vVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWzeJFKSzVyPUCuPVU2OjZizszN Mly4V2FPT0WU
IST-MES1 NUK1TnhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwOUi4NlQh|ryP M1vPZnNCVkeHUh?=
LB2241-RCC MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LyNmlEPTB;MD65PFg1KM7:TR?= MkfYV2FPT0WU
BL-70 M3jz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYOy[|NVUUN3ME2wMlk6PTN3IN88US=> MVLTRW5ITVJ?
NB17 NGixUopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwMEC2N|kh|ryP M3jybXNCVkeHUh?=
LXF-289 NV\YVGRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGqwZZNKSzVyPUGuNFMxPzZizszN MVnTRW5ITVJ?
TK10 NUf6ZZVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfkTWM2OD1zLkC1NFY{KM7:TR?= MlvJV2FPT0WU
K5 Mlz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LWPWlEPTB;MT6wOlI4PCEQvF2= MX\TRW5ITVJ?
NCI-H716 NHrVUllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFwMEeyOVkh|ryP NVvUW4ZEW0GQR1XS
HCE-T NVfpNoJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HtcGlEPTB;MT6wPFgyQSEQvF2= NH20SnJUSU6JRWK=
GI-1 M3n2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD4em5KSzVyPUGuNFk4QThizszN MV;TRW5ITVJ?
KARPAS-422 NYq1eJJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq2UXRLUUN3ME2xMlExODJ{IN88US=> MUHTRW5ITVJ?
TE-9 NVj5[2Q3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KyfWlEPTB;MT6xNVMzQCEQvF2= NVL0cGduW0GQR1XS
SF126 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTIRXVKSzVyPUGuNVE2PjhizszN M3i2fHNCVkeHUh?=
BB30-HNC MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH23ToZKSzVyPUGuNVMyOTJizszN MWHTRW5ITVJ?
NCI-H1304 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD5VpR6UUN3ME2xMlE{OzN6IN88US=> NF7STGhUSU6JRWK=
HEL MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;Fd2dKSzVyPUGuNVQ5QTVizszN NVrrPFZUW0GQR1XS
HAL-01 M3XWZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzIdXVlUUN3ME2xMlE2Ojh|IN88US=> M2TZRnNCVkeHUh?=
SK-LMS-1 M{XGfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nBVGlEPTB;MT6xOVk4PCEQvF2= MUHTRW5ITVJ?
SW954 M1G5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGm4Z3JKSzVyPUGuNVk2PjdizszN M2GyUXNCVkeHUh?=
D-283MED MnS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHLTWM2OD1zLkKyN|c6KM7:TR?= NHGzbGlUSU6JRWK=
NCI-H1882 M2jtb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XhcWlEPTB;MT6yN|g6KM7:TR?= NIi2bZFUSU6JRWK=
GI-ME-N NFPveHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu3TWM2OD1zLkK1NlA5KM7:TR?= MmXTV2FPT0WU
SK-PN-DW M3rVZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFwMk[zOFgh|ryP M4roWHNCVkeHUh?=
C2BBe1 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDURXNKSzVyPUGuNlkyOTdizszN NYG5fIJ5W0GQR1XS
A704 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVv3Z3pRUUN3ME2xMlMzPjh7IN88US=> M{S3UHNCVkeHUh?=
KALS-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFwM{SwPEDPxE1? M1rXTHNCVkeHUh?=
ETK-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvWdFlKSzVyPUGuN|Q1QDlizszN M4DNVnNCVkeHUh?=
LB647-SCLC M2rtbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPlfW1KSzVyPUGuN|Q6QDZizszN M2CwfXNCVkeHUh?=
OCUB-M M3jvdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPGTWM2OD1zLkO2NVQ{KM7:TR?= NV;qfZJtW0GQR1XS
NCI-H720 NEXibXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnLTWM2OD1zLkO2N|c5KM7:TR?= NX\UfFhrW0GQR1XS
NB13 M1;Cemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LI[mlEPTB;MT6zO|I6OyEQvF2= M13CO3NCVkeHUh?=
GR-ST MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj1Z4Z7UUN3ME2xMlM5PzV5IN88US=> M{PuXXNCVkeHUh?=
DU-4475 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7ITWM2OD1zLkS1PFU{KM7:TR?= MoW0V2FPT0WU
HCC2157 NHvK[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7j[o1YUUN3ME2xMlQ3PjV7IN88US=> Mnv3V2FPT0WU
RKO NG\meIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwNEm5NlIh|ryP NFjZXJJUSU6JRWK=
LS-123 NYX4WIlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\CdZpMUUN3ME2xMlUyPTl2IN88US=> M3;qXHNCVkeHUh?=
NCI-H69 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T2VGlEPTB;MT61OVgyOSEQvF2= MUjTRW5ITVJ?
SW962 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ZSWlEPTB;MT61OlE{KM7:TR?= M2LsV3NCVkeHUh?=
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A101D MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwNUexNVMh|ryP M{O5VnNCVkeHUh?=
NB10 NFPqdY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTFwNUezPVIh|ryP MoDjV2FPT0WU
NB5 NHnrfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\5N2lEPTB;MT61PFQ4PiEQvF2= M1qydHNCVkeHUh?=
HCE-4 NVPRfGZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TtW2lEPTB;MT62NFg2KM7:TR?= Mln4V2FPT0WU
HT-144 M{TyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFwNkOxPUDPxE1? NWDjWZJQW0GQR1XS
NCI-H524 NELpWXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\SZmhkUUN3ME2xMlY1OzB5IN88US=> MV;TRW5ITVJ?
NKM-1 MnTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzsPJpKSzVyPUGuOlg3PiEQvF2= NV3wbog6W0GQR1XS
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VA-ES-BJ MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTxTWM2OD1{LkCxOVE{KM7:TR?= NH3K[lVUSU6JRWK=
SNU-C2B MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjLcWU4UUN3ME2yMlA{OzVzIN88US=> NI\ySY1USU6JRWK=
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NCI-H526 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D0VWlEPTB;Mj6xPVE1OSEQvF2= NGjqVIpUSU6JRWK=
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NCI-H1395 NF6wTmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DqTWlEPTB;Mj64NlAyOiEQvF2= MWHTRW5ITVJ?
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NCI-H1417 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jhbGlEPTB;ND6yPFQ1OyEQvF2= M4ixOHNCVkeHUh?=
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NCI-H23 NF\0RXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml2wTWM2OD12Lki3NlI4KM7:TR?= MWHTRW5ITVJ?
MC116 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfkTWM2OD12Lkm0NVI3KM7:TR?= MnSxV2FPT0WU
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CTB-1 M4fkVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfGR2lKSzVyPUSuPVc4OjFizszN NHPwSmtUSU6JRWK=
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MOLT-4 NWfhbIJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmGzTWM2OD13LkGxPFMh|ryP M1z4W3NCVkeHUh?=
NCI-H2141 Mlz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTDT5ZHUUN3ME21MlE1OjZ6IN88US=> MlPCV2FPT0WU
EB-3 Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC4dGJKSzVyPUWuNVc2ODRizszN MnzVV2FPT0WU
NCI-H1522 NHzTbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjQXlFPUUN3ME21MlI3OzJ{IN88US=> NU\n[3lGW0GQR1XS
MRK-nu-1 MmryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\HTGlEPTB;NT60N|Y{OyEQvF2= MnntV2FPT0WU
no-11 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTVwNEewPFch|ryP NITNZohUSU6JRWK=
CESS NH7VOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTVwNUiwN|Qh|ryP NV71OGR{W0GQR1XS
KMOE-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjMXoNEUUN3ME21MlU5PjV7IN88US=> M4DKWXNCVkeHUh?=
REH M3zQZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG4dYd5UUN3ME22MlI2PjF6IN88US=> NXLueZl6W0GQR1XS
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NCI-H322M NVXwW5BGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXnVlJsUUN3ME23MlM{OzN3IN88US=> NUDSPJg1W0GQR1XS
NB6 NH3mephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPuSHlKSzVyPUeuOVQ5QTlizszN Mn\0V2FPT0WU
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NCI-H1092 NUTWVIczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TidGlEPTB;OD6wNVc{PCEQvF2= NVrLeXdGW0GQR1XS
EKVX M4jNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37XU2lEPTB;OD60O|A3PiEQvF2= NYC1dlRjW0GQR1XS
D-263MG NV3HWYt1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRThwNUWzPVYh|ryP MnPTV2FPT0WU
NCI-H209 NF7yZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLFN241UUN3ME24MlY1ODB4IN88US=> NVH5OXRrW0GQR1XS
IST-SL1 Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\G[2lEPTB;OD64PVg6OiEQvF2= M2LYfHNCVkeHUh?=
ACN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;aR2lEPTB;OT6xPVE2PyEQvF2= NFOwcVlUSU6JRWK=
MHH-PREB-1 M4rGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;IRVlKSzVyPUmuNlEzOTlizszN MWfTRW5ITVJ?
EW-11 M4HyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK1NlI5UUN3ME25MlY2Ozl4IN88US=> M175SXNCVkeHUh?=
KASUMI-1 NXzkS21oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjOPYZKSzVyPUmuO|g4PyEQvF2= NFW2cZhUSU6JRWK=
KINGS-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rZ[mlEPTB;MUCuNlM1PyEQvF2= MmXJV2FPT0WU
EVSA-T MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGmzTHVKSzVyPUGwMlMyQTJizszN M3ry[nNCVkeHUh?=
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COLO-824 M3HqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PFTGlEPTB;MUCuPFY3QSEQvF2= NWrlOIpjW0GQR1XS
K052 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Pj[WlEPTB;MUCuPVMzOiEQvF2= NFPMUIdUSU6JRWK=
SK-MEL-2 M3:4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFyLkm5N|kh|ryP M{\POHNCVkeHUh?=

... 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 (mg) = Concentration (mM) × Volume (mL) × 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.

  • * Indicates a Required Field

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