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 MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnXO2RKSzVyPUCuNFAxODZyMzFOwG0> MYXTRW5ITVJ?
SF539 NUjlSWNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HBS2lEPTB;MD6wNFA2PjRizszN M4TRN3NCVkeHUh?=
DEL M1fUcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37NWGlEPTB;MD6wNFA6OjdizszN NVjFdJZuW0GQR1XS
NB1 NUS2U2d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPiTWM2OD1yLkCwNVYzKM7:TR?= NWfzR4tiW0GQR1XS
SR NXHpSnBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7z[IFKSzVyPUCuNFAzPzdizszN Mn:2V2FPT0WU
KARPAS-299 NHPifo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz4[5VsUUN3ME2wMlAzOzh2IN88US=> NF7DbHhUSU6JRWK=
MHH-CALL-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzKTWM2OD1yLkCyPVUzKM7:TR?= NWDySWM2W0GQR1XS
SU-DHL-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMES4OlUh|ryP Ml36V2FPT0WU
A4-Fuk NYfJNI9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\JTWM2OD1yLkC1OVY2KM7:TR?= Mkm3V2FPT0WU
EW-1 M1XqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlriTWM2OD1yLkGwNlU3KM7:TR?= MVrTRW5ITVJ?
NOS-1 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXKZ|dKSzVyPUCuNVAzQTRizszN NXjUZXlvW0GQR1XS
EW-16 NWTZb2hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LUPGlEPTB;MD6xNFU3QCEQvF2= NIrIUWJUSU6JRWK=
TE-11 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\SO2lEPTB;MD6xOlA6PiEQvF2= MXXTRW5ITVJ?
SW982 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrudmM6UUN3ME2wMlE3PDd6IN88US=> Mn6zV2FPT0WU
LAN-6 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD6TWM2OD1yLkG3OFQ{KM7:TR?= NUnqcmU{W0GQR1XS
MZ1-PC NGH0V4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XBdGlEPTB;MD6xO|g{PSEQvF2= NVfCVYNXW0GQR1XS
KS-1 MknlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDLOZFQUUN3ME2wMlE6OzR|IN88US=> M336UnNCVkeHUh?=
PSN1 M4jqV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljGTWM2OD1yLkG5OlMyKM7:TR?= MlW2V2FPT0WU
LC-2-ad MnHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzQbGRUUUN3ME2wMlE6Pjl{IN88US=> MnzZV2FPT0WU
COLO-320-HSR Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnBZ2RKSzVyPUCuNVk4PzZizszN M1;WPXNCVkeHUh?=
OPM-2 MmnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTBwMkK2Olkh|ryP MV;TRW5ITVJ?
SK-NEP-1 NUTwWZZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPHZ5lKSzVyPUCuNlM2OjRizszN M3fkenNCVkeHUh?=
ALL-PO MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzt[o9VUUN3ME2wMlI1PTJ2IN88US=> NIi0UHNUSU6JRWK=
CMK MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHO3fXdKSzVyPUCuNlU2OyEQvF2= MUjTRW5ITVJ?
NCI-H1648 NE\ZeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnQWm5KSzVyPUCuNlc5PTVizszN Mn25V2FPT0WU
SIG-M5 NX\SfZc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjMbmVKSzVyPUCuNlkyPTlizszN M3L5ZnNCVkeHUh?=
TGBC24TKB NGr2SVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrMboxKSzVyPUCuN|AzOThizszN MXzTRW5ITVJ?
DOHH-2 NH2wNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV71eItlUUN3ME2wMlMyOjB2IN88US=> NVHUSlJJW0GQR1XS
NB69 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLjXmNKSzVyPUCuN|E4QDdizszN MX;TRW5ITVJ?
MFH-ino M1:z[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PKbWlEPTB;MD6zNlUzOyEQvF2= M4nRbnNCVkeHUh?=
KP-N-RT-BM-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwM{OxNlMh|ryP MWnTRW5ITVJ?
MONO-MAC-6 NETNWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\QTWM2OD1yLkOzNlkyKM7:TR?= NEHobG5USU6JRWK=
ATN-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjnTWM2OD1yLkOzN|A{KM7:TR?= MmTXV2FPT0WU
NTERA-S-cl-D1 NV7zfYU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;DSWlEPTB;MD6zN|M6PiEQvF2= MnHIV2FPT0WU
L-540 M3zSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fkRmlEPTB;MD6zOlk5QCEQvF2= MXLTRW5ITVJ?
GB-1 M2TFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m3d2lEPTB;MD6zPFg3PyEQvF2= NEWwb3ZUSU6JRWK=
MV-4-11 NYGzd4VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHhfmNRUUN3ME2wMlM6PDR4IN88US=> NFO5XG5USU6JRWK=
KG-1 NWjjcIpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYmySYVMUUN3ME2wMlM6PTZzIN88US=> M2PUcHNCVkeHUh?=
OVCAR-4 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWL5VWsxUUN3ME2wMlQxPTZ7IN88US=> M4L1e3NCVkeHUh?=
NEC8 NHfYVJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrtd|FRUUN3ME2wMlQyOjl{IN88US=> NV3zbnBrW0GQR1XS
SK-MM-2 NYjqSZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvxUmtiUUN3ME2wMlQyPjB7IN88US=> Mom3V2FPT0WU
TE-8 MnfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu0TWM2OD1yLkSyPFgh|ryP MoL3V2FPT0WU
697 M3K4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfrbWRKSzVyPUCuOFMzOTVizszN NILlNmhUSU6JRWK=
NB14 NYjpR|dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwNEO4NlYh|ryP NYXIbWxUW0GQR1XS
GDM-1 NFnOb4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwNEexNVYh|ryP MVvTRW5ITVJ?
HUTU-80 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i2dGlEPTB;MD60O|M4PSEQvF2= NH;zS|hUSU6JRWK=
HL-60 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTBwNEixOFIh|ryP MUHTRW5ITVJ?
OCI-AML2 NUXmc4hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W0PWlEPTB;MD60PFMzQCEQvF2= NYPXN2FZW0GQR1XS
ML-2 NV3Me5p1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjQUldKUUN3ME2wMlQ6ODNzIN88US=> M1PQUnNCVkeHUh?=
ES4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13DZWlEPTB;MD60PVExQSEQvF2= M3;PbnNCVkeHUh?=
NCI-H747 NYP5c|BuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NECxfWFKSzVyPUCuOFk5QSEQvF2= NX\pV3N{W0GQR1XS
RL95-2 NX;ucmR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7TNJZ6UUN3ME2wMlUxOTF{IN88US=> MljiV2FPT0WU
TE-15 M{XNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDyTWM2OD1yLkWxNVI1KM7:TR?= MVfTRW5ITVJ?
TE-12 NWjjNIJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrzXXpXUUN3ME2wMlU{OzR7IN88US=> MX\TRW5ITVJ?
LB1047-RCC MlTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLUOXJKSzVyPUCuOVQ2PDlizszN NX:zSVNLW0GQR1XS
LB831-BLC NGH3d45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHuepBKSzVyPUCuOVUxOjNizszN MXzTRW5ITVJ?
NCI-H1355 NHHnUVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rjVGlEPTB;MD61OVE5PCEQvF2= Mkj1V2FPT0WU
CTV-1 NELwTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVKyXGRFUUN3ME2wMlU2PjJ2IN88US=> Mk\aV2FPT0WU
RXF393 M2\OVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK5OpZKSzVyPUCuOVU4QTRizszN M1S1U3NCVkeHUh?=
SW872 M2qyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGm2NGlKSzVyPUCuOVY4OjRizszN NGXMVHBUSU6JRWK=
MPP-89 M17w[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPXeIF4UUN3ME2wMlU4QDh2IN88US=> MYDTRW5ITVJ?
RPMI-8226 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LYeGlEPTB;MD62N|UzPiEQvF2= MlfMV2FPT0WU
LS-1034 M336[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzkbpZ7UUN3ME2wMlY{PThizszN M4PDdXNCVkeHUh?=
SJSA-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwNkO3NlUh|ryP MXXTRW5ITVJ?
HOP-62 NYSyUZc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK5cJdlUUN3ME2wMlY2ODN|IN88US=> M3jJWnNCVkeHUh?=
KGN NUfR[mV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfDTWM2OD1yLk[2NVY5KM7:TR?= MXnTRW5ITVJ?
D-336MG NIToeXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwNk[xOlkh|ryP NU\McHJKW0GQR1XS
LS-411N MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoewTWM2OD1yLk[3OFYzKM7:TR?= NVO2emxJW0GQR1XS
TE-1 M3e3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHviUYtKSzVyPUCuOlkxPzRizszN M4\YUnNCVkeHUh?=
LB996-RCC NEnBPJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzSTWM2OD1yLk[5N|g6KM7:TR?= NX\md4Y2W0GQR1XS
TE-10 M1\U[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3XXWFKSzVyPUCuO|E1QTZizszN M3;6U3NCVkeHUh?=
NCI-SNU-16 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwN{K2OlQh|ryP MUjTRW5ITVJ?
ES8 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkmwTWM2OD1yLke0PVc2KM7:TR?= MlPkV2FPT0WU
COLO-800 NV\XTGJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjGcIdKSzVyPUCuO|Y3QTVizszN M{TvS3NCVkeHUh?=
ES6 NFH4V5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofnTWM2OD1yLke3OVU6KM7:TR?= MnntV2FPT0WU
L-363 MmjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFT5WGVKSzVyPUCuPFI{PzVizszN MmK4V2FPT0WU
NMC-G1 NYTuWXR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwOEOyN|Mh|ryP NEnWeVhUSU6JRWK=
LU-134-A M2jK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j5eGlEPTB;MD64N|kyOiEQvF2= MXHTRW5ITVJ?
SF268 NWTENoxPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[zUmlEPTB;MD64OFA1OiEQvF2= NIfvO2FUSU6JRWK=
KARPAS-45 NHq2O2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH71O3hKSzVyPUCuPFQzPjNizszN MmeyV2FPT0WU
TGW NXX3TIpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjoTWM2OD1yLki1PFY{KM7:TR?= M1HIW3NCVkeHUh?=
CHP-126 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrSTWM2OD1yLki1PVU4KM7:TR?= M1Xk[3NCVkeHUh?=
MOLT-16 MofKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHtTWM2OD1yLki3OVg6KM7:TR?= MWTTRW5ITVJ?
LB771-HNC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7vTWM2OD1yLki5O|U4KM7:TR?= NV;reI9{W0GQR1XS
NALM-6 Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwOUC3N|kh|ryP MXfTRW5ITVJ?
GCIY M1XFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF73d|hKSzVyPUCuPVU2OjZizszN NHr2UY5USU6JRWK=
IST-MES1 NXjFOWdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M12zV2lEPTB;MD65PFgzPCEQvF2= M1W2d3NCVkeHUh?=
LB2241-RCC NGH6RlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPwcYRKSzVyPUCuPVg5PCEQvF2= MlTvV2FPT0WU
BL-70 NWG0TWUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwOUm1N|Uh|ryP NEPjb|BUSU6JRWK=
NB17 NYrDfGxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfhTWM2OD1zLkCwOlM6KM7:TR?= MV;TRW5ITVJ?
LXF-289 NWXTWXplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjLNXFKSzVyPUGuNFMxPzZizszN NGjJR|NUSU6JRWK=
TK10 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nCZWlEPTB;MT6wOVA3OyEQvF2= MVzTRW5ITVJ?
K5 NFfufWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\Eb4NKSzVyPUGuNFYzPzRizszN NW\TSmFYW0GQR1XS
NCI-H716 NEjoW2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PpN2lEPTB;MT6wO|I2QSEQvF2= MojvV2FPT0WU
HCE-T M1iyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1e0WmlEPTB;MT6wPFgyQSEQvF2= MnniV2FPT0WU
GI-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3GwS2lEPTB;MT6wPVc6QCEQvF2= MUTTRW5ITVJ?
KARPAS-422 M4H4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHLTWM2OD1zLkGwNFIzKM7:TR?= NX:xUnJyW0GQR1XS
TE-9 NIDyNJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj2VY5KSzVyPUGuNVE{OjhizszN MX7TRW5ITVJ?
SF126 NHzZWItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFwMUG1Olgh|ryP M1fkfHNCVkeHUh?=
BB30-HNC M3jPTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTUTWM2OD1zLkGzNVEzKM7:TR?= M{[2[3NCVkeHUh?=
NCI-H1304 M4e3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq5TWM2OD1zLkGzN|M5KM7:TR?= MlG4V2FPT0WU
HEL NGHiWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITPSo5KSzVyPUGuNVQ5QTVizszN Ml;5V2FPT0WU
HAL-01 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInsOZhKSzVyPUGuNVUzQDNizszN NX3LNFN7W0GQR1XS
SK-LMS-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fBbmlEPTB;MT6xOVk4PCEQvF2= Mn:yV2FPT0WU
SW954 NGXDb3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe1N|lKSzVyPUGuNVk2PjdizszN M1T2RXNCVkeHUh?=
D-283MED MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;2TWM2OD1zLkKyN|c6KM7:TR?= NH;sfGlUSU6JRWK=
NCI-H1882 NELGT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrITWM2OD1zLkKzPFkh|ryP MkTZV2FPT0WU
GI-ME-N NY[xU5hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HEZmlEPTB;MT6yOVIxQCEQvF2= MXXTRW5ITVJ?
SK-PN-DW MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFwMk[zOFgh|ryP MoDQV2FPT0WU
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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
    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID