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 Ml;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3PbmVKSzVyPUCuNFAxODZyMzFOwG0> MW\TRW5ITVJ?
SF539 NX;DN|JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTBwMECwOVY1KM7:TR?= MljSV2FPT0WU
DEL MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwMECwPVI4KM7:TR?= M{W0UHNCVkeHUh?=
NB1 NF3LZYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXQclg2UUN3ME2wMlAxOTZ{IN88US=> NH60SoZUSU6JRWK=
SR MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMECyO|ch|ryP M2rlfHNCVkeHUh?=
KARPAS-299 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLXWG1KSzVyPUCuNFI{QDRizszN MWHTRW5ITVJ?
MHH-CALL-2 M1X3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\EbmlEPTB;MD6wNlk2OiEQvF2= MVnTRW5ITVJ?
SU-DHL-1 NYm4Ro5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn0T2RKSzVyPUCuNFQ5PjVizszN M{TwUHNCVkeHUh?=
A4-Fuk NVrkOmxjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jveGlEPTB;MD6wOVU3PSEQvF2= M4jW[nNCVkeHUh?=
EW-1 Mmm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTtZWRKSzVyPUCuNVAzPTZizszN NHzYUo9USU6JRWK=
NOS-1 NGPReW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnaV2lKSzVyPUCuNVAzQTRizszN MUTTRW5ITVJ?
EW-16 MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\E[nZKSzVyPUCuNVA2PjhizszN M1\aNHNCVkeHUh?=
TE-11 M2PrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDsdYlKSzVyPUCuNVYxQTZizszN M2DNSHNCVkeHUh?=
SW982 NGfiV5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzLTWM2OD1yLkG2OFc5KM7:TR?= M3LVOHNCVkeHUh?=
LAN-6 NUnveoZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH23UG5KSzVyPUCuNVc1PDNizszN NWjzUlR3W0GQR1XS
MZ1-PC M3v4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3yySWlEPTB;MD6xO|g{PSEQvF2= NF2xRWFUSU6JRWK=
KS-1 NF7WcppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jXc2lEPTB;MD6xPVM1OyEQvF2= NUCyT5FYW0GQR1XS
PSN1 NX35[HhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPLeo92UUN3ME2wMlE6PjNzIN88US=> MX3TRW5ITVJ?
LC-2-ad MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMUm2PVIh|ryP M3\RfnNCVkeHUh?=
COLO-320-HSR NGfUdG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\YZW9wUUN3ME2wMlE6Pzd4IN88US=> MmrpV2FPT0WU
OPM-2 NXz4O4x{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jqeGlEPTB;MD6yNlY3QSEQvF2= NYi4TVZbW0GQR1XS
SK-NEP-1 NYTaT|d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMkO1NlQh|ryP M2jaOHNCVkeHUh?=
ALL-PO MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O5T2lEPTB;MD6yOFUzPCEQvF2= NYnlemhTW0GQR1XS
CMK NELtXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwMkW1N{DPxE1? NITxTo9USU6JRWK=
NCI-H1648 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHKydpBKSzVyPUCuNlc5PTVizszN M1nTcXNCVkeHUh?=
SIG-M5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3RXHlKSzVyPUCuNlkyPTlizszN M3i0SXNCVkeHUh?=
TGBC24TKB NV31bIJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37wXGlEPTB;MD6zNFIyQCEQvF2= NFfv[GZUSU6JRWK=
DOHH-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HYemlEPTB;MD6zNVIxPCEQvF2= MUPTRW5ITVJ?
NB69 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonJTWM2OD1yLkOxO|g4KM7:TR?= M2LDPHNCVkeHUh?=
MFH-ino MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ixcmlEPTB;MD6zNlUzOyEQvF2= NEXJXXlUSU6JRWK=
KP-N-RT-BM-1 NV3JXFdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXrbYhKSzVyPUCuN|MyOjNizszN MX;TRW5ITVJ?
MONO-MAC-6 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH4[VVKSzVyPUCuN|MzQTFizszN NITlOZNUSU6JRWK=
ATN-1 NVLEdFhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nRd2lEPTB;MD6zN|MxOyEQvF2= NWraNVZ7W0GQR1XS
NTERA-S-cl-D1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nYWmlEPTB;MD6zN|M6PiEQvF2= Mnr1V2FPT0WU
L-540 NVn2[VU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLLTWM2OD1yLkO2PVg5KM7:TR?= M2XSfHNCVkeHUh?=
GB-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzUUXdKSzVyPUCuN|g5PjdizszN NWHQUJZDW0GQR1XS
MV-4-11 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXlc3p1UUN3ME2wMlM6PDR4IN88US=> M3;ndXNCVkeHUh?=
KG-1 NIfWblhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzTeYVKSzVyPUCuN|k2PjFizszN M3rqOHNCVkeHUh?=
OVCAR-4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDpSVZKSzVyPUCuOFA2PjlizszN MWLTRW5ITVJ?
NEC8 NWSzWVhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonGTWM2OD1yLkSxNlkzKM7:TR?= NIfsTFhUSU6JRWK=
SK-MM-2 NF;XeIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwNEG2NFkh|ryP MYXTRW5ITVJ?
TE-8 NEXaTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GzZmlEPTB;MD60Nlg5KM7:TR?= M123e3NCVkeHUh?=
697 NF;rSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DSWGlEPTB;MD60N|IyPSEQvF2= NFT0[IlUSU6JRWK=
NB14 M2i2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHGZndkUUN3ME2wMlQ{QDJ4IN88US=> MoDGV2FPT0WU
GDM-1 M4fiNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwNEexNVYh|ryP NGniUWFUSU6JRWK=
HUTU-80 NGOwbYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSwOJlTUUN3ME2wMlQ4Ozd3IN88US=> NGO1fG5USU6JRWK=
HL-60 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qyRWlEPTB;MD60PFE1OiEQvF2= NIrmdYhUSU6JRWK=
OCI-AML2 MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH0VHFKSzVyPUCuOFg{OjhizszN MYPTRW5ITVJ?
ML-2 NY\2co0{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf0UHNWUUN3ME2wMlQ6ODNzIN88US=> NWP3b2VFW0GQR1XS
ES4 M4\2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4THWGlEPTB;MD60PVExQSEQvF2= NVrOc4w1W0GQR1XS
NCI-H747 M3juRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLmTWM2OD1yLkS5PFkh|ryP NX;4fY81W0GQR1XS
RL95-2 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\xeIxKSzVyPUCuOVAyOTJizszN M3TR[3NCVkeHUh?=
TE-15 NYLU[FVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\2cGlEPTB;MD61NVEzPCEQvF2= MmPNV2FPT0WU
TE-12 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwNUOzOFkh|ryP NILYc|hUSU6JRWK=
LB1047-RCC NVrKOnU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHr6dotKSzVyPUCuOVQ2PDlizszN NUjkVYx7W0GQR1XS
LB831-BLC NFXqOnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjYOIFiUUN3ME2wMlU2ODJ|IN88US=> MV\TRW5ITVJ?
NCI-H1355 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rRfmlEPTB;MD61OVE5PCEQvF2= NVvPd3JYW0GQR1XS
CTV-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjUW5N4UUN3ME2wMlU2PjJ2IN88US=> MkjLV2FPT0WU
RXF393 NH7Xe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwNUW3PVQh|ryP Mom4V2FPT0WU
SW872 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PjNGlEPTB;MD61OlczPCEQvF2= M{LRZ3NCVkeHUh?=
MPP-89 M1zIN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnm1TWM2OD1yLkW3PFg1KM7:TR?= M3GyO3NCVkeHUh?=
RPMI-8226 NV3BXYt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnyTYVKSzVyPUCuOlM2OjZizszN MVLTRW5ITVJ?
LS-1034 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPvZnBxUUN3ME2wMlY{PThizszN MlTOV2FPT0WU
SJSA-1 M1[3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLKblhRUUN3ME2wMlY{PzJ3IN88US=> MoO5V2FPT0WU
HOP-62 NH7KRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TiOWlEPTB;MD62OVA{OyEQvF2= MmLRV2FPT0WU
KGN MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17BeGlEPTB;MD62OlE3QCEQvF2= NXi0dm5ZW0GQR1XS
D-336MG MkDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwNk[xOlkh|ryP Mn7qV2FPT0WU
LS-411N NVfOPI9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTBwNke0OlIh|ryP NV6yOo1GW0GQR1XS
TE-1 NYm0fWVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwNkmwO|Qh|ryP NWT6XHdyW0GQR1XS
LB996-RCC NHeyb49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX33S5p{UUN3ME2wMlY6Ozh7IN88US=> MnHDV2FPT0WU
TE-10 MofSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnTTWM2OD1yLkexOFk3KM7:TR?= MlflV2FPT0WU
NCI-SNU-16 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwN{K2OlQh|ryP MXHTRW5ITVJ?
ES8 NHLTbYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETkeHBKSzVyPUCuO|Q6PzVizszN NHrkfFZUSU6JRWK=
COLO-800 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkK3TWM2OD1yLke2Olk2KM7:TR?= NYS4RXRkW0GQR1XS
ES6 NEi1W2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fkS2lEPTB;MD63O|U2QSEQvF2= MYLTRW5ITVJ?
L-363 NXjXO2t7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwOEKzO|Uh|ryP MkDyV2FPT0WU
NMC-G1 M2fQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW1c243UUN3ME2wMlg{OjN|IN88US=> M2fwNnNCVkeHUh?=
LU-134-A MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvsWY5EUUN3ME2wMlg{QTF{IN88US=> M4[3XXNCVkeHUh?=
SF268 MnmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf0[pF4UUN3ME2wMlg1ODR{IN88US=> Ml\zV2FPT0WU
KARPAS-45 NXS3OW05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrHS2NzUUN3ME2wMlg1OjZ|IN88US=> MVHTRW5ITVJ?
TGW NWPoXlBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS4TWM2OD1yLki1PFY{KM7:TR?= NIG2[3lUSU6JRWK=
CHP-126 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ziOGlEPTB;MD64OVk2PyEQvF2= MW\TRW5ITVJ?
MOLT-16 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rRSWlEPTB;MD64O|U5QSEQvF2= MoO4V2FPT0WU
LB771-HNC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f0ZmlEPTB;MD64PVc2PyEQvF2= MmnSV2FPT0WU
NALM-6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwOUC3N|kh|ryP M4PxNHNCVkeHUh?=
GCIY NV\1dXUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzNZ2lKSzVyPUCuPVU2OjZizszN NVvqfnJRW0GQR1XS
IST-MES1 NFzZ[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwOUi4NlQh|ryP MUDTRW5ITVJ?
LB2241-RCC NXLnWmg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TMemlEPTB;MD65PFg1KM7:TR?= NHzFcYlUSU6JRWK=
BL-70 NFyxVoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELtN2lKSzVyPUCuPVk2OzVizszN M1;rTXNCVkeHUh?=
NB17 NYW4d|NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwMEC2N|kh|ryP MU\TRW5ITVJ?
LXF-289 NITVcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFwMEOwO|Yh|ryP MUXTRW5ITVJ?
TK10 M1r4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\ubYU2UUN3ME2xMlA2ODZ|IN88US=> NVHMXoU4W0GQR1XS
K5 NVvTZW5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmqxTWM2OD1zLkC2Nlc1KM7:TR?= MnTHV2FPT0WU
NCI-H716 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjtWVVjUUN3ME2xMlA4OjV7IN88US=> MoPLV2FPT0WU
HCE-T NX3DO2JoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zJcmlEPTB;MT6wPFgyQSEQvF2= NF\XWGJUSU6JRWK=
GI-1 NIO3eHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHDeWdKSzVyPUGuNFk4QThizszN MnWwV2FPT0WU
KARPAS-422 NFPyR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnf3TWM2OD1zLkGwNFIzKM7:TR?= NYrvbW04W0GQR1XS
TE-9 NGnyS4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf3UIxKSzVyPUGuNVE{OjhizszN M{HTbXNCVkeHUh?=
SF126 M1nySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXabZZKSzVyPUGuNVE2PjhizszN NYDUNYE{W0GQR1XS
BB30-HNC NXPBe4lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\ORoN6UUN3ME2xMlE{OTF{IN88US=> M1K1RXNCVkeHUh?=
NCI-H1304 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3SwdGlEPTB;MT6xN|M{QCEQvF2= MYfTRW5ITVJ?
HEL M3jGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwMUS4PVUh|ryP MUHTRW5ITVJ?
HAL-01 MlPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDRPI5pUUN3ME2xMlE2Ojh|IN88US=> M2jabXNCVkeHUh?=
SK-LMS-1 M4jHcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTZPHBCUUN3ME2xMlE2QTd2IN88US=> NUHtcJBqW0GQR1XS
SW954 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLYTWM2OD1zLkG5OVY4KM7:TR?= MVPTRW5ITVJ?
D-283MED NFrLTVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\XVIZKSzVyPUGuNlI{PzlizszN Mm\wV2FPT0WU
NCI-H1882 NI[xbYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfuTWM2OD1zLkKzPFkh|ryP NEXBbnFUSU6JRWK=
GI-ME-N NGXsW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P5fmlEPTB;MT6yOVIxQCEQvF2= NUDIO2ZWW0GQR1XS
SK-PN-DW NGnRWZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mme5TWM2OD1zLkK2N|Q5KM7:TR?= NEjDcmJUSU6JRWK=
C2BBe1 M1zLUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFwMkmxNVch|ryP NWTYeJVOW0GQR1XS
A704 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFm2ZVhKSzVyPUGuN|I3QDlizszN M4j1TnNCVkeHUh?=
KALS-1 M{Ho[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWe3Xos{UUN3ME2xMlM1ODhizszN MnXvV2FPT0WU
ETK-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFwM{S0PFkh|ryP MmL0V2FPT0WU
LB647-SCLC NEnHSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7CfY02UUN3ME2xMlM1QTh4IN88US=> MULTRW5ITVJ?
OCUB-M NXGzb5pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj5TFU{UUN3ME2xMlM3OTR|IN88US=> M17xWXNCVkeHUh?=
NCI-H720 M{nGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fqN2lEPTB;MT6zOlM4QCEQvF2= MXPTRW5ITVJ?
NB13 NWTDSoJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PyNGlEPTB;MT6zO|I6OyEQvF2= NWDX[npIW0GQR1XS
GR-ST NXzzN|N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPJTWM2OD1zLkO4O|U4KM7:TR?= MlLrV2FPT0WU
DU-4475 MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr0fXpMUUN3ME2xMlQ2QDV|IN88US=> MkLEV2FPT0WU
HCC2157 NIKydHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\JZmpKSzVyPUGuOFY3PTlizszN MYrTRW5ITVJ?
RKO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFwNEm5NlIh|ryP MVnTRW5ITVJ?
LS-123 M1n0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzYTFJKSzVyPUGuOVE2QTRizszN M1mwNXNCVkeHUh?=
NCI-H69 NEPEcWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTFwNUW4NVEh|ryP MWDTRW5ITVJ?
SW962 NUjkfVdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\RNGlEPTB;MT61OlE{KM7:TR?= MljpV2FPT0WU
PF-382 M3\4Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLHTWM2OD1zLkW2PVYh|ryP MWnTRW5ITVJ?
A101D NFew[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlntTWM2OD1zLkW3NVE{KM7:TR?= MojCV2FPT0WU
NB10 NWfE[2g{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT1ZpVCUUN3ME2xMlU4Ozl{IN88US=> NETJd5dUSU6JRWK=
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HCE-4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGwbHRKSzVyPUGuOlA5PSEQvF2= M{e0VnNCVkeHUh?=
HT-144 M1S3bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDWXoFKSzVyPUGuOlMyQSEQvF2= NWf6WWxbW0GQR1XS
NCI-H524 NYjLdVAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Lv[GlEPTB;MT62OFMxPyEQvF2= MVvTRW5ITVJ?
NKM-1 MmK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPGOJF{UUN3ME2xMlY5PjZizszN NGjBNo1USU6JRWK=
KURAMOCHI NV65R292T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP5TWM2OD1zLk[5OVc{KM7:TR?= Mnf2V2FPT0WU
NCI-H187 NV3EemxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTFwN{CwN|Yh|ryP NGPsbXpUSU6JRWK=
U-266 M37LcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\UTWlEPTB;MT63N|g1OiEQvF2= M{\mNHNCVkeHUh?=
BL-41 NI\sNZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLJ[4ZRUUN3ME2xMlc3Ojd{IN88US=> NGLBNYhUSU6JRWK=
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Daudi NGLYNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[zXmlEPTB;MT63PFk3PyEQvF2= NXnyeFQ6W0GQR1XS
CPC-N MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFwOEWwPVYh|ryP M1nVdnNCVkeHUh?=
EM-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoqyTWM2OD1zLki1NUDPxE1? M3jHUnNCVkeHUh?=
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LP-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vtXmlEPTB;MT64O|E1OyEQvF2= NI\kNpVUSU6JRWK=
CAS-1 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[0VmdpUUN3ME2xMlk5Ojl7IN88US=> MWLTRW5ITVJ?
NB7 NH\tbGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTlTWM2OD1{LkCwOVU2KM7:TR?= NXnWZXZ1W0GQR1XS
VA-ES-BJ MnnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwMEG1NVMh|ryP MkDkV2FPT0WU
SNU-C2B M1\NcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPUVVVTUUN3ME2yMlA{OzVzIN88US=> NXXr[2NIW0GQR1XS
LOXIMVI NI\sb|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HFeGlEPTB;Mj6wOlc5PiEQvF2= NV7HeJlOW0GQR1XS
NCI-H1581 NXT5S4xpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTGTWM2OD1{LkGxOVU6KM7:TR?= M12yRXNCVkeHUh?=
IST-SL2 NEPNTGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT3THBxUUN3ME2yMlEzPDR3IN88US=> NWC5O2F7W0GQR1XS
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TE-6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPHTWM2OD1{LkG5NFUh|ryP MoLEV2FPT0WU
NCI-H526 NVroUmtUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfYd45KSzVyPUKuNVkyPDFizszN NIr4PGdUSU6JRWK=
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NCI-SNU-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHoTWM2OD1{LkOzNlU3KM7:TR?= NUHzVmF4W0GQR1XS
BB65-RCC M3HEfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJwM{e0PVMh|ryP MofUV2FPT0WU
GT3TKB Mn\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrRTWM2OD1{LkO5PVczKM7:TR?= NHPBdXRUSU6JRWK=
OS-RC-2 M3zM[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXDTWM2OD1{LkSyN|QyKM7:TR?= MX7TRW5ITVJ?
NCI-H2126 NWn3UJdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLOU2czUUN3ME2yMlQ{Pjd2IN88US=> MlTBV2FPT0WU
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DMS-114 NGHwV|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DBe2lEPTB;Mj62NVUzPCEQvF2= MmD4V2FPT0WU
ONS-76 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXm2fJRxUUN3ME2yMlY{PjRzIN88US=> NEHp[4NUSU6JRWK=
8-MG-BA MmPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrYTWM2OD1{Lk[1OFE1KM7:TR?= MknFV2FPT0WU
BOKU MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7ocG1CUUN3ME2yMlczPzZ2IN88US=> MoHOV2FPT0WU
LAMA-84 NUHk[XRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfUTWM2OD1{Lke5PVEzKM7:TR?= MkfzV2FPT0WU
ES1 MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETSUmtKSzVyPUKuPFE5ODRizszN MYLTRW5ITVJ?
NCI-H1395 NVTFVY9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXSTWM2OD1{LkiyNFEzKM7:TR?= MWnTRW5ITVJ?
A388 NF\kepNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;0T2pKSzVyPUKuPVYyPyEQvF2= MoDMV2FPT0WU
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HD-MY-Z NYjrVIRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\pRmNKSzVyPUOuNVMzODNizszN M1;VeXNCVkeHUh?=
NCI-H510A MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rjV2lEPTB;Mz6xPFk1OyEQvF2= NFfjU2ZUSU6JRWK=
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SCLC-21H NWG2TmozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm4NnpKSzVyPUOuNlY5PTlizszN NGCzdnRUSU6JRWK=
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KM12 MmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTNwM{O1OFQh|ryP MXXTRW5ITVJ?
ST486 NFLB[ZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH2XZZ3UUN3ME2zMlU{QDh|IN88US=> NEDPeoZUSU6JRWK=
HC-1 NFPX[FBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrWRnB{UUN3ME2zMlYzODJ6IN88US=> NHzUdZpUSU6JRWK=
BV-173 NFOxUlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP2codKSzVyPUOuOlQxQDhizszN MWXTRW5ITVJ?
EW-24 MlfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTNwNk[0N|Qh|ryP MX\TRW5ITVJ?
LU-65 NFvaeWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU[2eWF{UUN3ME2zMlY5PzFizszN MY\TRW5ITVJ?
ECC4 NF34e2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\qTWM2OD1|Lke3OVYh|ryP M1jRfnNCVkeHUh?=
ARH-77 M{XWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIS5cYtKSzVyPUSuNVExPjdizszN Mn7HV2FPT0WU
BC-3 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTRwMUOwOlgh|ryP M3zlRXNCVkeHUh?=
SNB75 NETkfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTRwMk[xPUDPxE1? MoLVV2FPT0WU
MEG-01 Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnKwTWM2OD12LkK3OFE6KM7:TR?= M4HHT3NCVkeHUh?=
NCI-H1417 NHfUe4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH4SpJKSzVyPUSuNlg1PDNizszN MlrMV2FPT0WU
MDA-MB-134-VI M3e0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7tTWM2OD12LkOwOlAyKM7:TR?= MXjTRW5ITVJ?
Becker NUntfG5YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TlOmlEPTB;ND60O|M{PiEQvF2= Mmi4V2FPT0WU
DMS-153 NVzVcpRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTRwNk[0O|Uh|ryP M1PBNnNCVkeHUh?=
TGBC1TKB M1T6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTRwNki1NVUh|ryP MWnTRW5ITVJ?
EW-3 MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnG5TWM2OD12Lke2NlQ5KM7:TR?= MVnTRW5ITVJ?
KE-37 MnLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[3R4FKSzVyPUSuPFYyQTZizszN MYPTRW5ITVJ?
NCI-H23 NWHkOZg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zVN2lEPTB;ND64O|IzPyEQvF2= M2Tw[3NCVkeHUh?=
MC116 M1\0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkGzTWM2OD12Lkm0NVI3KM7:TR?= M{PiUnNCVkeHUh?=
NH-12 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36wemlEPTB;ND65OlQ{QSEQvF2= MoWxV2FPT0WU
CTB-1 MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjPTWM2OD12Lkm3O|IyKM7:TR?= MVrTRW5ITVJ?
KM-H2 MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnxW3FKSzVyPUWuNFU{OjNizszN MmW3V2FPT0WU
MOLT-4 NUXFbpVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXtTWM2OD13LkGxPFMh|ryP M2qyUXNCVkeHUh?=
NCI-H2141 NYD0dmVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHXTWM2OD13LkG0NlY5KM7:TR?= M4XrcHNCVkeHUh?=
EB-3 MnvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTVwMUe1NFQh|ryP MlPlV2FPT0WU
NCI-H1522 NVqxeno2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTVwMk[zNlIh|ryP MXfTRW5ITVJ?
MRK-nu-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHITWM2OD13LkSzOlM{KM7:TR?= MXvTRW5ITVJ?
no-11 Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTuTmU1UUN3ME21MlQ4ODh5IN88US=> NYXkco5nW0GQR1XS
CESS Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3JNnAyUUN3ME21MlU5ODN2IN88US=> M4\2enNCVkeHUh?=
KMOE-2 NFX5NGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGW2PJpKSzVyPUWuOVg3PTlizszN NHnx[oZUSU6JRWK=
REH Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPLNJlKSzVyPU[uNlU3OThizszN M{fLXnNCVkeHUh?=
KU812 NVvrOZpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTLfVhRUUN3ME22MlQzPzlzIN88US=> MWPTRW5ITVJ?
SK-N-FI NWPGe|JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz0TWM2OD14Lk[wOlc1KM7:TR?= Mn3iV2FPT0WU
MMAC-SF NGX3SndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn4TWM2OD15LkC2OFkzKM7:TR?= NEjD[IdUSU6JRWK=
RCC10RGB NIjVfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTdwMkK5O|ch|ryP NIO4NpFUSU6JRWK=
NCI-H322M NGrIN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i5Z2lEPTB;Nz6zN|M{PSEQvF2= M{KwZ3NCVkeHUh?=
NB6 NHPGXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrKUWlKSzVyPUeuOVQ5QTlizszN NUjld4NKW0GQR1XS
MN-60 NIfQeHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jZcGlEPTB;Nz62PVIyPSEQvF2= NVrERVVpW0GQR1XS
NCI-H1092 NWnI[nk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHFdVFjUUN3ME24MlAyPzN2IN88US=> NYHZUVhkW0GQR1XS
EKVX M1jabWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRThwNEewOlYh|ryP M1n1TnNCVkeHUh?=
D-263MG M1u5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPHTWM2OD16LkW1N|k3KM7:TR?= M1m1UXNCVkeHUh?=
NCI-H209 NV6zcI1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRThwNkSwNFYh|ryP MknrV2FPT0WU
IST-SL1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRThwOEm4PVIh|ryP MYfTRW5ITVJ?
ACN Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTDTWM2OD17LkG5NVU4KM7:TR?= MV;TRW5ITVJ?
MHH-PREB-1 NYf1RZRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fjWWlEPTB;OT6yNVIyQSEQvF2= M1yxO3NCVkeHUh?=
EW-11 NULKTFZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PFUWlEPTB;OT62OVM6PiEQvF2= M1ezUnNCVkeHUh?=
KASUMI-1 M3e3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TRemlEPTB;OT63PFc4KM7:TR?= NH\oVpJUSU6JRWK=
KINGS-1 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\BTWM2OD1zMD6yN|Q4KM7:TR?= M3XXOnNCVkeHUh?=
EVSA-T NVnYVWNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDPd2FKSzVyPUGwMlMyQTJizszN NE\zdG1USU6JRWK=
DSH1 NIqwbJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HTemlEPTB;MUCuN|k4OiEQvF2= NHTObpZUSU6JRWK=
COLO-824 MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjafJBXUUN3ME2xNE45PjZ7IN88US=> M{LEfXNCVkeHUh?=
K052 NILkfW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HWdGlEPTB;MUCuPVMzOiEQvF2= NHrLdHNUSU6JRWK=
SK-MEL-2 M2PhVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHS5bnhKSzVyPUGwMlk6OzlizszN MoPIV2FPT0WU

... 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