TAE684 (NVP-TAE684)

製品コードS1108

TAE684 (NVP-TAE684)化学構造

分子量(MW):614.2

TAE684 (NVP-TAE684)は一種の有効で、選択性的なALK阻害剤で、無細胞試験でIC50値が3 nMです。TAE684 (NVP-TAE684)は、ALKに作用する選択性はInsRに作用する選択性より100倍が高くなります。

サイズ 価格 在庫  
JPY 23038.08 あり
JPY 41756.51 あり
JPY 110870.76 あり

カスタマーフィードバック(4)

  • (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.

製品安全説明書

ALK阻害剤の選択性比較

生物活性

製品説明 TAE684 (NVP-TAE684)は一種の有効で、選択性的なALK阻害剤で、無細胞試験でIC50値が3 nMです。TAE684 (NVP-TAE684)は、ALKに作用する選択性はInsRに作用する選択性より100倍が高くなります。
ターゲット
ALK [1]
(Cell-free assay)
3 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCC-3 NYfjTW9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXjO4ZKSzVyPUCuNFAxODZyMzFOwG0> MmraV2FPT0WU
SF539 NVL0S2p{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i4NGlEPTB;MD6wNFA2PjRizszN M{S0NHNCVkeHUh?=
DEL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLFTWM2OD1yLkCwNFkzPyEQvF2= NHLiSZNUSU6JRWK=
NB1 NVHzOHdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTOTZFKSzVyPUCuNFAyPjJizszN NVHNNXdVW0GQR1XS
SR MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz2SY9FUUN3ME2wMlAxOjd5IN88US=> NWi0cHNoW0GQR1XS
KARPAS-299 NIP0bWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml6xTWM2OD1yLkCyN|g1KM7:TR?= MYrTRW5ITVJ?
MHH-CALL-2 M1HYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33KfGlEPTB;MD6wNlk2OiEQvF2= M1u4NnNCVkeHUh?=
SU-DHL-1 NXPk[JRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXCTWM2OD1yLkC0PFY2KM7:TR?= MWTTRW5ITVJ?
A4-Fuk M4fHc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwMEW1OlUh|ryP NX;scIo6W0GQR1XS
EW-1 M2LWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvkTWM2OD1yLkGwNlU3KM7:TR?= NV7tfGRYW0GQR1XS
NOS-1 NWPqZ3pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PGNmlEPTB;MD6xNFI6PCEQvF2= M1TObHNCVkeHUh?=
EW-16 NVvkb5ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zmc2lEPTB;MD6xNFU3QCEQvF2= M3HsV3NCVkeHUh?=
TE-11 M2fRVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrhTWM2OD1yLkG2NFk3KM7:TR?= NHPMNVNUSU6JRWK=
SW982 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSzTWM2OD1yLkG2OFc5KM7:TR?= MljwV2FPT0WU
LAN-6 M2\OXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLNZoIyUUN3ME2wMlE4PDR|IN88US=> NFXrO3dUSU6JRWK=
MZ1-PC MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwMUe4N|Uh|ryP MnvZV2FPT0WU
KS-1 NV3DVWw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nwSGlEPTB;MD6xPVM1OyEQvF2= Mn3JV2FPT0WU
PSN1 NHHP[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPLTWM2OD1yLkG5OlMyKM7:TR?= MlSxV2FPT0WU
LC-2-ad MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;CXXRsUUN3ME2wMlE6Pjl{IN88US=> MXTTRW5ITVJ?
COLO-320-HSR MlnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTwTWM2OD1yLkG5O|c3KM7:TR?= NV\2R4Z1W0GQR1XS
OPM-2 NHrHUYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnoSoR1UUN3ME2wMlIzPjZ7IN88US=> NUjkZnhNW0GQR1XS
SK-NEP-1 NFe4THNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwMkO1NlQh|ryP M4jCWnNCVkeHUh?=
ALL-PO M4TOZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVm3S|ZYUUN3ME2wMlI1PTJ2IN88US=> NIfIT|FUSU6JRWK=
CMK NFznVmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfnbY9oUUN3ME2wMlI2PTNizszN NY\yPIhbW0GQR1XS
NCI-H1648 NYmyOIUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPpSXg1UUN3ME2wMlI4QDV3IN88US=> NGX4R|BUSU6JRWK=
SIG-M5 NUL3T5RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7DTWM2OD1yLkK5NVU6KM7:TR?= MV7TRW5ITVJ?
TGBC24TKB NIPSbGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnJTWM2OD1yLkOwNlE5KM7:TR?= NU\nXoNiW0GQR1XS
DOHH-2 MlX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2q2RmlEPTB;MD6zNVIxPCEQvF2= Mk\WV2FPT0WU
NB69 M2ryc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwM{G3PFch|ryP M2m2dXNCVkeHUh?=
MFH-ino M3rjS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:1dW9KSzVyPUCuN|I2OjNizszN NWfzZZZKW0GQR1XS
KP-N-RT-BM-1 M1TnXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHXWZZqUUN3ME2wMlM{OTJ|IN88US=> NIrkZ|ZUSU6JRWK=
MONO-MAC-6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfRXJdyUUN3ME2wMlM{OjlzIN88US=> MlfxV2FPT0WU
ATN-1 NUDpb2tGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7QPWdjUUN3ME2wMlM{OzB|IN88US=> NI\lcYhUSU6JRWK=
NTERA-S-cl-D1 NFXMdnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwM{OzPVYh|ryP M{nuenNCVkeHUh?=
L-540 NYjPfWFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXi4b5hPUUN3ME2wMlM3QTh6IN88US=> MlLlV2FPT0WU
GB-1 NVnkTGJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnjTWM2OD1yLkO4PFY4KM7:TR?= NWnrSIcyW0GQR1XS
MV-4-11 M362dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHySYZKSzVyPUCuN|k1PDZizszN MlrHV2FPT0WU
KG-1 M2nBWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP5eHJKSzVyPUCuN|k2PjFizszN Mnv5V2FPT0WU
OVCAR-4 M{\uZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYL5TJpQUUN3ME2wMlQxPTZ7IN88US=> MVTTRW5ITVJ?
NEC8 NGjYc|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwNEGyPVIh|ryP NVf0eGxkW0GQR1XS
SK-MM-2 M{fucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nFfWlEPTB;MD60NVYxQSEQvF2= NF7JZYNUSU6JRWK=
TE-8 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwNEK4PEDPxE1? MW\TRW5ITVJ?
697 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rRUmlEPTB;MD60N|IyPSEQvF2= MXfTRW5ITVJ?
NB14 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NET0RnlKSzVyPUCuOFM5OjZizszN NX;WeXI2W0GQR1XS
GDM-1 NEWzO3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHXeGZKUUN3ME2wMlQ4OTF4IN88US=> NGL4[FBUSU6JRWK=
HUTU-80 NGXTeJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmq0TWM2OD1yLkS3N|c2KM7:TR?= NHnnco5USU6JRWK=
HL-60 NHvUO25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwNEixOFIh|ryP NH24e3hUSU6JRWK=
OCI-AML2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{OzVmlEPTB;MD60PFMzQCEQvF2= MmfsV2FPT0WU
ML-2 M2frN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vvTWlEPTB;MD60PVA{OSEQvF2= MnrpV2FPT0WU
ES4 NEnCdYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwNEmxNFkh|ryP MYrTRW5ITVJ?
NCI-H747 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nvNWlEPTB;MD60PVg6KM7:TR?= NWfJRll2W0GQR1XS
RL95-2 NF6xe4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPqdlZKSzVyPUCuOVAyOTJizszN MX7TRW5ITVJ?
TE-15 NG\nUW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjrTWM2OD1yLkWxNVI1KM7:TR?= NFz2T21USU6JRWK=
TE-12 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwNUOzOFkh|ryP MkG3V2FPT0WU
LB1047-RCC M2KyPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwNUS1OFkh|ryP Mle1V2FPT0WU
LB831-BLC NVfLTW5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXSTWM2OD1yLkW1NFI{KM7:TR?= NHn4V3hUSU6JRWK=
NCI-H1355 NXLSWlhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwNUWxPFQh|ryP NIrLXWlUSU6JRWK=
CTV-1 NV[2UWxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwNUW2NlQh|ryP NVGzUmFHW0GQR1XS
RXF393 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwNUW3PVQh|ryP NXPxc291W0GQR1XS
SW872 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP6dWxKSzVyPUCuOVY4OjRizszN M{T1bXNCVkeHUh?=
MPP-89 M3\FPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTmbVU1UUN3ME2wMlU4QDh2IN88US=> M{LLVXNCVkeHUh?=
RPMI-8226 NFq1OJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP3Wo9DUUN3ME2wMlY{PTJ4IN88US=> NX\HemJvW0GQR1XS
LS-1034 M33NbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwNkO1PEDPxE1? MX3TRW5ITVJ?
SJSA-1 NFXNWGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrrfJl{UUN3ME2wMlY{PzJ3IN88US=> NYjacI9yW0GQR1XS
HOP-62 NHS4bIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[3TGlEPTB;MD62OVA{OyEQvF2= M4nieHNCVkeHUh?=
KGN NGPv[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yyc2lEPTB;MD62OlE3QCEQvF2= NIjxW|VUSU6JRWK=
D-336MG NV6zOmdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j6UGlEPTB;MD62OlE3QSEQvF2= NYKxRoVKW0GQR1XS
LS-411N M1vzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXWTWM2OD1yLk[3OFYzKM7:TR?= NEHjWFlUSU6JRWK=
TE-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTlTWM2OD1yLk[5NFc1KM7:TR?= MVPTRW5ITVJ?
LB996-RCC MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL4PZFLUUN3ME2wMlY6Ozh7IN88US=> NGrVSW1USU6JRWK=
TE-10 NVTGNWZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ryVWlEPTB;MD63NVQ6PiEQvF2= MljRV2FPT0WU
NCI-SNU-16 MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfJTWM2OD1yLkeyOlY1KM7:TR?= NXTQcWxMW0GQR1XS
ES8 NUXieIhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;PXY5KSzVyPUCuO|Q6PzVizszN MULTRW5ITVJ?
COLO-800 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwN{[2PVUh|ryP NHjRdGZUSU6JRWK=
ES6 M3HrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7kRms{UUN3ME2wMlc4PTV7IN88US=> NXXtVXU4W0GQR1XS
L-363 M1zwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP3TXVKSzVyPUCuPFI{PzVizszN MV7TRW5ITVJ?
NMC-G1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwOEOyN|Mh|ryP MV7TRW5ITVJ?
LU-134-A NH3lNpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3KPFZKSzVyPUCuPFM6OTJizszN M4DqXXNCVkeHUh?=
SF268 NIXRUHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3od2NKSzVyPUCuPFQxPDJizszN NYLzVnRPW0GQR1XS
KARPAS-45 NX;lNZp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwOESyOlMh|ryP NH3UOJlUSU6JRWK=
TGW MoTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XpXmlEPTB;MD64OVg3OyEQvF2= MYXTRW5ITVJ?
CHP-126 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3n2UmlEPTB;MD64OVk2PyEQvF2= NXj3U4hkW0GQR1XS
MOLT-16 NE\VTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvCUpV{UUN3ME2wMlg4PTh7IN88US=> M1rTfXNCVkeHUh?=
LB771-HNC M4\SWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjyN49KSzVyPUCuPFk4PTdizszN NGO0cGdUSU6JRWK=
NALM-6 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwOUC3N|kh|ryP NWHZTlJVW0GQR1XS
GCIY NHPmd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXe4[3h{UUN3ME2wMlk2PTJ4IN88US=> MUPTRW5ITVJ?
IST-MES1 NUfsRYt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDLVotKSzVyPUCuPVg5OjRizszN MX3TRW5ITVJ?
LB2241-RCC NEL5XlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjUTIJKSzVyPUCuPVg5PCEQvF2= NUHHe2VVW0GQR1XS
BL-70 M1zRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluyTWM2OD1yLkm5OVM2KM7:TR?= M2XsTnNCVkeHUh?=
NB17 NYjU[mZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLlfmVKSzVyPUGuNFA3OzlizszN M3fmZXNCVkeHUh?=
LXF-289 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS2TWM2OD1zLkCzNFc3KM7:TR?= NGr4[XFUSU6JRWK=
TK10 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zw[mlEPTB;MT6wOVA3OyEQvF2= NWDFeXRUW0GQR1XS
K5 NIDYO2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYe3OnFJUUN3ME2xMlA3Ojd2IN88US=> M{HlO3NCVkeHUh?=
NCI-H716 MnHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfYTWM2OD1zLkC3NlU6KM7:TR?= NYO5UIpMW0GQR1XS
HCE-T M3Kwe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nKeGlEPTB;MT6wPFgyQSEQvF2= NUDWVYE6W0GQR1XS
GI-1 M2jnWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojUTWM2OD1zLkC5O|k5KM7:TR?= M4[3ZnNCVkeHUh?=
KARPAS-422 NEjJeYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3LTWM2OD1zLkGwNFIzKM7:TR?= MlvIV2FPT0WU
TE-9 NFvubmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPDTWM2OD1zLkGxN|I5KM7:TR?= Mn3mV2FPT0WU
SF126 M1XBT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X3XGlEPTB;MT6xNVU3QCEQvF2= M{PZc3NCVkeHUh?=
BB30-HNC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKxTWM2OD1zLkGzNVEzKM7:TR?= MWjTRW5ITVJ?
NCI-H1304 NXX5UGpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PPUmlEPTB;MT6xN|M{QCEQvF2= NX3wZmZbW0GQR1XS
HEL MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzpSI9KSzVyPUGuNVQ5QTVizszN NVXm[JNJW0GQR1XS
HAL-01 NHzSbnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX5TWM2OD1zLkG1Nlg{KM7:TR?= NVjvZ|VpW0GQR1XS
SK-LMS-1 NX7TOHJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFwMUW5O|Qh|ryP NWLK[Jg4W0GQR1XS
SW954 NFvId49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwMUm1Olch|ryP NXXWZW5UW0GQR1XS
D-283MED NX3ndmFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni4TWM2OD1zLkKyN|c6KM7:TR?= NWTWZWRIW0GQR1XS
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K052 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\sW21[UUN3ME2xNE46OzJ{IN88US=> Ml3nV2FPT0WU
SK-MEL-2 MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fpbWlEPTB;MUCuPVk{QSEQvF2= MVjTRW5ITVJ?

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[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.
細胞試験: [1]
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  • 細胞株: 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.
  • 濃度: 1 nM-10 μM
  • 反応時間: 2–3 days
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
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  • 動物モデル: Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice.
  • 製剤: Resuspended in 10% 1-methyl-2-pyrrolidinone/90% polyethylene glycol 300 solution
  • 投薬量: 1, 3, and 10 mg/kg
  • 投与方法: Once daily by oral gavage for 3 weeks
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 3 mg/mL (4.88 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol, pH 4
10 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 614.2
化学式

C30H40ClN7O3S

CAS No. 761439-42-3
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

ALK信号経路図

ALK Inhibitors with Unique Features

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