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 M3\yUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofZTWM2OD1yLkCwNFA3ODNizszN MXzTRW5ITVJ?
SF539 Ml7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[5TXlKSzVyPUCuNFAxPTZ2IN88US=> NVnqeWFUW0GQR1XS
DEL MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMECwPVI4KM7:TR?= NHHxb4tUSU6JRWK=
NB1 MnHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2OyWmlEPTB;MD6wNFE3OiEQvF2= NIrF[GFUSU6JRWK=
SR NFrLfo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLtPJJDUUN3ME2wMlAxOjd5IN88US=> NXHrdXZpW0GQR1XS
KARPAS-299 Mn3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C0[GlEPTB;MD6wNlM5PCEQvF2= MkLTV2FPT0WU
MHH-CALL-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTQNJluUUN3ME2wMlAzQTV{IN88US=> MonSV2FPT0WU
SU-DHL-1 NFfrdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwMES4OlUh|ryP NIXLclhUSU6JRWK=
A4-Fuk MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPCWoo3UUN3ME2wMlA2PTZ3IN88US=> M{XDOnNCVkeHUh?=
EW-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwMUCyOVYh|ryP NV\nRVNMW0GQR1XS
NOS-1 NXjy[ItqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1r5RmlEPTB;MD6xNFI6PCEQvF2= NYPRb45oW0GQR1XS
EW-16 NVS5[3JFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmWwTWM2OD1yLkGwOVY5KM7:TR?= MlvsV2FPT0WU
TE-11 NXrUVWVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwMU[wPVYh|ryP NUnDOmFUW0GQR1XS
SW982 NFSwT2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwMU[0O|gh|ryP Mk\YV2FPT0WU
LAN-6 MoCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjBTWM2OD1yLkG3OFQ{KM7:TR?= Mmr3V2FPT0WU
MZ1-PC MmPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMUe4N|Uh|ryP NXHqTI9ZW0GQR1XS
KS-1 M1vOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPtcFNKSzVyPUCuNVk{PDNizszN NFfrZYZUSU6JRWK=
PSN1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[wNGlEPTB;MD6xPVY{OSEQvF2= MmXoV2FPT0WU
LC-2-ad M2jPSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO5TJVKSzVyPUCuNVk3QTJizszN Mlr2V2FPT0WU
COLO-320-HSR NIHlU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjwfpI6UUN3ME2wMlE6Pzd4IN88US=> MoPnV2FPT0WU
OPM-2 M1rYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHztbWhKSzVyPUCuNlI3PjlizszN NV;6bXpbW0GQR1XS
SK-NEP-1 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HURmlEPTB;MD6yN|UzPCEQvF2= M2PacXNCVkeHUh?=
ALL-PO NHHWO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHtTWM2OD1yLkK0OVI1KM7:TR?= MVLTRW5ITVJ?
CMK NE[0SZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnUXVR5UUN3ME2wMlI2PTNizszN MlXTV2FPT0WU
NCI-H1648 MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwMke4OVUh|ryP NVK1O4U2W0GQR1XS
SIG-M5 NFj1RVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPGSYZOUUN3ME2wMlI6OTV7IN88US=> MXTTRW5ITVJ?
TGBC24TKB MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwM{CyNVgh|ryP MlXkV2FPT0WU
DOHH-2 MlKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfJZ4tKSzVyPUCuN|EzODRizszN NGqw[lZUSU6JRWK=
NB69 NX3lU28zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zUdmlEPTB;MD6zNVc5PyEQvF2= M4jnWXNCVkeHUh?=
MFH-ino M2\oT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkD5TWM2OD1yLkOyOVI{KM7:TR?= NGnhcmRUSU6JRWK=
KP-N-RT-BM-1 NVyxTWRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwM{OxNlMh|ryP NWH0dWtJW0GQR1XS
MONO-MAC-6 NFLzO2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrCTo9IUUN3ME2wMlM{OjlzIN88US=> NH;hfmtUSU6JRWK=
ATN-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYKwcJRsUUN3ME2wMlM{OzB|IN88US=> NXz4TpptW0GQR1XS
NTERA-S-cl-D1 MoD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnRNJhNUUN3ME2wMlM{Ozl4IN88US=> NVHkbXB7W0GQR1XS
L-540 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O5[2lEPTB;MD6zOlk5QCEQvF2= MmOzV2FPT0WU
GB-1 M1TVZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW1e5FKSzVyPUCuN|g5PjdizszN M4jSbnNCVkeHUh?=
MV-4-11 NVywXVRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwM{m0OFYh|ryP M1z3bXNCVkeHUh?=
KG-1 NXHNVZpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr2TFJKSzVyPUCuN|k2PjFizszN NXXWUnhoW0GQR1XS
OVCAR-4 NWDvfHhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fHbGlEPTB;MD60NFU3QSEQvF2= M{XW[HNCVkeHUh?=
NEC8 NH;UWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwNEGyPVIh|ryP MWLTRW5ITVJ?
SK-MM-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHLTWM2OD1yLkSxOlA6KM7:TR?= M4jSZXNCVkeHUh?=
TE-8 NFnqc5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW5TWM2OD1yLkSyPFgh|ryP M4GzWXNCVkeHUh?=
697 MmXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwNEOyNVUh|ryP NGThc3lUSU6JRWK=
NB14 NIHnXHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;DRoxKSzVyPUCuOFM5OjZizszN NXXaOnFxW0GQR1XS
GDM-1 NWHveo1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TRe2lEPTB;MD60O|EyPiEQvF2= M3XrfHNCVkeHUh?=
HUTU-80 NYqySYxsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n0NWlEPTB;MD60O|M4PSEQvF2= NF;IO25USU6JRWK=
HL-60 NF[0NodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDpb4t2UUN3ME2wMlQ5OTR{IN88US=> NFTweoZUSU6JRWK=
OCI-AML2 M1fzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nDOGlEPTB;MD60PFMzQCEQvF2= MmLOV2FPT0WU
ML-2 NG[3WHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fYW2lEPTB;MD60PVA{OSEQvF2= MYLTRW5ITVJ?
ES4 MorxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrZRppKSzVyPUCuOFkyODlizszN NUTBVYt1W0GQR1XS
NCI-H747 NXXIfJFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYO0W5JGUUN3ME2wMlQ6QDlizszN MX3TRW5ITVJ?
RL95-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwNUCxNVIh|ryP NWPTNHVuW0GQR1XS
TE-15 M2TQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnFT3JKSzVyPUCuOVEyOjRizszN M3LBWHNCVkeHUh?=
TE-12 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfBcZNKSzVyPUCuOVM{PDlizszN M{HnS3NCVkeHUh?=
LB1047-RCC MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPXcXlKSzVyPUCuOVQ2PDlizszN NYLDWIlYW0GQR1XS
LB831-BLC M4SyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPFTWM2OD1yLkW1NFI{KM7:TR?= MlPoV2FPT0WU
NCI-H1355 NGn2SoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XveGlEPTB;MD61OVE5PCEQvF2= M3jKOXNCVkeHUh?=
CTV-1 NFiwOlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH1TWM2OD1yLkW1OlI1KM7:TR?= NUHSR5FiW0GQR1XS
RXF393 NVK2OXg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnJTWM2OD1yLkW1O|k1KM7:TR?= MXjTRW5ITVJ?
SW872 NGPXb5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHKXHVmUUN3ME2wMlU3PzJ2IN88US=> MnftV2FPT0WU
MPP-89 NVPTTJdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2izWGlEPTB;MD61O|g5PCEQvF2= MlXoV2FPT0WU
RPMI-8226 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwNkO1NlYh|ryP MVPTRW5ITVJ?
LS-1034 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrHOGJKSzVyPUCuOlM2QCEQvF2= NEi2[41USU6JRWK=
SJSA-1 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnXcW52UUN3ME2wMlY{PzJ3IN88US=> M3HoR3NCVkeHUh?=
HOP-62 M17YcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwNkWwN|Mh|ryP MVPTRW5ITVJ?
KGN M3vJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTIXox7UUN3ME2wMlY3OTZ6IN88US=> NU[1TZIzW0GQR1XS
D-336MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHkTWM2OD1yLk[2NVY6KM7:TR?= NVL6O41LW0GQR1XS
LS-411N NX3QTnRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTrTWM2OD1yLk[3OFYzKM7:TR?= MoPTV2FPT0WU
TE-1 NVTVbGN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml65TWM2OD1yLk[5NFc1KM7:TR?= M1nnUXNCVkeHUh?=
LB996-RCC M2O3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKxcndYUUN3ME2wMlY6Ozh7IN88US=> MXLTRW5ITVJ?
TE-10 NHvXPZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwN{G0PVYh|ryP NXP2fpNTW0GQR1XS
NCI-SNU-16 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\ob2lEPTB;MD63NlY3PCEQvF2= Mon0V2FPT0WU
ES8 NHjkT3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7PTmNKSzVyPUCuO|Q6PzVizszN MVLTRW5ITVJ?
COLO-800 NFW0fW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\pZlZKSzVyPUCuO|Y3QTVizszN MmHuV2FPT0WU
ES6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnBTWM2OD1yLke3OVU6KM7:TR?= M3HufnNCVkeHUh?=
L-363 NFv4VWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwOEKzO|Uh|ryP NGXnTZpUSU6JRWK=
NMC-G1 NEXBeVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDaXmpTUUN3ME2wMlg{OjN|IN88US=> NFrrU|ZUSU6JRWK=
LU-134-A M{K4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TDSWlEPTB;MD64N|kyOiEQvF2= NEDmRXFUSU6JRWK=
SF268 NHW5UFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\vXW57UUN3ME2wMlg1ODR{IN88US=> MV3TRW5ITVJ?
KARPAS-45 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGD5SItKSzVyPUCuPFQzPjNizszN M3S5R3NCVkeHUh?=
TGW NIj2N5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Xz[mlEPTB;MD64OVg3OyEQvF2= NFPKS4ZUSU6JRWK=
CHP-126 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwOEW5OVch|ryP MojZV2FPT0WU
MOLT-16 NYjVWFhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13Tb2lEPTB;MD64O|U5QSEQvF2= NILwZotUSU6JRWK=
LB771-HNC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwOEm3OVch|ryP NGLnTnVUSU6JRWK=
NALM-6 Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD5TWM2OD1yLkmwO|M6KM7:TR?= MknUV2FPT0WU
GCIY NHPjTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHTfZZWUUN3ME2wMlk2PTJ4IN88US=> NFrCV5FUSU6JRWK=
IST-MES1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK3NoE2UUN3ME2wMlk5QDJ2IN88US=> NGnF[nJUSU6JRWK=
LB2241-RCC NVj4PW9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTle21MUUN3ME2wMlk5QDRizszN MV;TRW5ITVJ?
BL-70 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjNTWM2OD1yLkm5OVM2KM7:TR?= M1S2PHNCVkeHUh?=
NB17 NWDKc2E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jpdmlEPTB;MT6wNFY{QSEQvF2= NUDucllMW0GQR1XS
LXF-289 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrtUoVPUUN3ME2xMlA{ODd4IN88US=> NUDaU2lEW0GQR1XS
TK10 M4O1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvHbHlKSzVyPUGuNFUxPjNizszN NV[2Rm5PW0GQR1XS
K5 MkjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH2U29KSzVyPUGuNFYzPzRizszN NVO2OY1IW0GQR1XS
NCI-H716 M{fIUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwMEeyOVkh|ryP Ml;RV2FPT0WU
HCE-T NFTVWnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonITWM2OD1zLkC4PFE6KM7:TR?= MV;TRW5ITVJ?
GI-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwMEm3PVgh|ryP NWrSN3RuW0GQR1XS
KARPAS-422 NHTNOINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjs[JRKSzVyPUGuNVAxOjJizszN MlnIV2FPT0WU
TE-9 M1zSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHFTWM2OD1zLkGxN|I5KM7:TR?= MVTTRW5ITVJ?
SF126 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnhTYVkUUN3ME2xMlEyPTZ6IN88US=> NG\HPY1USU6JRWK=
BB30-HNC M{\KRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknPTWM2OD1zLkGzNVEzKM7:TR?= M2nzSHNCVkeHUh?=
NCI-H1304 NUDMSVRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFwMUOzN|gh|ryP NH;rNXlUSU6JRWK=
HEL MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;JTWM2OD1zLkG0PFk2KM7:TR?= NG\l[YVUSU6JRWK=
HAL-01 Ml64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\KSohKSzVyPUGuNVUzQDNizszN MYnTRW5ITVJ?
SK-LMS-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;lTWM2OD1zLkG1PVc1KM7:TR?= M3;BVXNCVkeHUh?=
SW954 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnBRVdKSzVyPUGuNVk2PjdizszN MnzBV2FPT0WU
D-283MED MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXLTXlKSzVyPUGuNlI{PzlizszN NFvjXJJUSU6JRWK=
NCI-H1882 NFHkbnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTBTWM2OD1zLkKzPFkh|ryP MWLTRW5ITVJ?
GI-ME-N MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG4TWM2OD1zLkK1NlA5KM7:TR?= M3HRe3NCVkeHUh?=
SK-PN-DW NIDCb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTFwMk[zOFgh|ryP M33G[XNCVkeHUh?=
C2BBe1 M1rOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDLdWs4UUN3ME2xMlI6OTF5IN88US=> NWLt[YUzW0GQR1XS
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D-263MG NH7iPZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXiTWM2OD16LkW1N|k3KM7:TR?= MYLTRW5ITVJ?
NCI-H209 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHGTWM2OD16Lk[0NFA3KM7:TR?= MX7TRW5ITVJ?
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... 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