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(税別)  
JPY 26560.00
JPY 48140.00
JPY 127820.00

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 NVjUR|NvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDJTWM2OD1yLkCwNFA3ODNizszN NXLCeW1mW0GQR1XS
SF539 NF\yVXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iybmlEPTB;MD6wNFA2PjRizszN NW\YcGpiW0GQR1XS
DEL NFTGdXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\3TWM2OD1yLkCwNFkzPyEQvF2= M{L4[nNCVkeHUh?=
NB1 M{O4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK4cm9KSzVyPUCuNFAyPjJizszN M2PGdXNCVkeHUh?=
SR M{exWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjjRZBZUUN3ME2wMlAxOjd5IN88US=> MkK5V2FPT0WU
KARPAS-299 NFfN[JFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPN[4dKSzVyPUCuNFI{QDRizszN NEnvdHpUSU6JRWK=
MHH-CALL-2 NYe4fZFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfkTWM2OD1yLkCyPVUzKM7:TR?= M4TRWXNCVkeHUh?=
SU-DHL-1 NFy1eHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLyeI1KSzVyPUCuNFQ5PjVizszN Mln6V2FPT0WU
A4-Fuk MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL2ZlVKSzVyPUCuNFU2PjVizszN M4r0dHNCVkeHUh?=
EW-1 NIXne21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PUOGlEPTB;MD6xNFI2PiEQvF2= MoTYV2FPT0WU
NOS-1 NGfLWW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;neVE4UUN3ME2wMlExOjl2IN88US=> NVrub4x6W0GQR1XS
EW-16 M3;sS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMUC1Olgh|ryP NH7NcnRUSU6JRWK=
TE-11 M3LQS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T4ZmlEPTB;MD6xOlA6PiEQvF2= NFPTVFJUSU6JRWK=
SW982 NW\ZcWpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES3fVdKSzVyPUCuNVY1PzhizszN MVfTRW5ITVJ?
LAN-6 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMUe0OFMh|ryP MknwV2FPT0WU
MZ1-PC Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;GPYlKSzVyPUCuNVc5OzVizszN NH[3TXZUSU6JRWK=
KS-1 NFLWTHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vjPWlEPTB;MD6xPVM1OyEQvF2= NWrJTnVMW0GQR1XS
PSN1 NIi2T5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHj4Z2xKSzVyPUCuNVk3OzFizszN MoP2V2FPT0WU
LC-2-ad MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPFUHpKSzVyPUCuNVk3QTJizszN NXjwVZJ1W0GQR1XS
COLO-320-HSR NILJdnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPtbYtnUUN3ME2wMlE6Pzd4IN88US=> MoK3V2FPT0WU
OPM-2 MkjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\ZO|ZKSzVyPUCuNlI3PjlizszN MlLYV2FPT0WU
SK-NEP-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTBwMkO1NlQh|ryP M1jQNXNCVkeHUh?=
ALL-PO M1eyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTBwMkS1NlQh|ryP MXPTRW5ITVJ?
CMK M3PoNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTJTWM2OD1yLkK1OVMh|ryP MnrVV2FPT0WU
NCI-H1648 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TlZmlEPTB;MD6yO|g2PSEQvF2= MXTTRW5ITVJ?
SIG-M5 NXrzZZJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlO5TWM2OD1yLkK5NVU6KM7:TR?= NGjFblhUSU6JRWK=
TGBC24TKB NVrQR3BjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwM{CyNVgh|ryP M3vwS3NCVkeHUh?=
DOHH-2 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwM{GyNFQh|ryP M3LSOHNCVkeHUh?=
NB69 NVzXWYs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnWTWM2OD1yLkOxO|g4KM7:TR?= MkPMV2FPT0WU
MFH-ino NIrJcVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\iVWlEPTB;MD6zNlUzOyEQvF2= M4\Y[3NCVkeHUh?=
KP-N-RT-BM-1 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwM{OxNlMh|ryP M3fRUXNCVkeHUh?=
MONO-MAC-6 M3j6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjJZnZSUUN3ME2wMlM{OjlzIN88US=> MYnTRW5ITVJ?
ATN-1 MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T2NWlEPTB;MD6zN|MxOyEQvF2= MXLTRW5ITVJ?
NTERA-S-cl-D1 M2HxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwM{OzPVYh|ryP NVHzRZNiW0GQR1XS
L-540 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPHe2tKSzVyPUCuN|Y6QDhizszN MYLTRW5ITVJ?
GB-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInkOphKSzVyPUCuN|g5PjdizszN NVvHeoNmW0GQR1XS
MV-4-11 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwM{m0OFYh|ryP NUXGbFVyW0GQR1XS
KG-1 NV7YPWNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fh[WlEPTB;MD6zPVU3OSEQvF2= NFXoe5hUSU6JRWK=
OVCAR-4 M1SyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXMbm43UUN3ME2wMlQxPTZ7IN88US=> MnjvV2FPT0WU
NEC8 NHTMdIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrzZYxKSzVyPUCuOFEzQTJizszN M{\VZXNCVkeHUh?=
SK-MM-2 NV;LN41ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{mzSGlEPTB;MD60NVYxQSEQvF2= NXTQUmFiW0GQR1XS
TE-8 M2\5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rjeGlEPTB;MD60Nlg5KM7:TR?= NGLr[GRUSU6JRWK=
697 MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjGZ2VwUUN3ME2wMlQ{OjF3IN88US=> NEnEWppUSU6JRWK=
NB14 NUmxOFVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vOUGlEPTB;MD60N|gzPiEQvF2= MoTLV2FPT0WU
GDM-1 NVzMN|V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zqU2lEPTB;MD60O|EyPiEQvF2= M2XwWHNCVkeHUh?=
HUTU-80 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwNEezO|Uh|ryP MXzTRW5ITVJ?
HL-60 NUD0OoRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zCOWlEPTB;MD60PFE1OiEQvF2= NUTaXlFrW0GQR1XS
OCI-AML2 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGS5Zm1KSzVyPUCuOFg{OjhizszN M3r2XHNCVkeHUh?=
ML-2 M3K3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnO0TWM2OD1yLkS5NFMyKM7:TR?= MYnTRW5ITVJ?
ES4 NESxUXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwNEmxNFkh|ryP Mo\TV2FPT0WU
NCI-H747 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHlTWM2OD1yLkS5PFkh|ryP MmLHV2FPT0WU
RL95-2 NYLHcoZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LPc2lEPTB;MD61NFEyOiEQvF2= NYPsT5VZW0GQR1XS
TE-15 M4Djb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPmTWM2OD1yLkWxNVI1KM7:TR?= NHz6WmJUSU6JRWK=
TE-12 NVnjbW9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrNUXNiUUN3ME2wMlU{OzR7IN88US=> MlHyV2FPT0WU
LB1047-RCC M{PhW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXiTWM2OD1yLkW0OVQ6KM7:TR?= MVjTRW5ITVJ?
LB831-BLC M1vZPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDSTWM2OD1yLkW1NFI{KM7:TR?= M3[3eHNCVkeHUh?=
NCI-H1355 Mo\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYCweIdIUUN3ME2wMlU2OTh2IN88US=> NFTt[2xUSU6JRWK=
CTV-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwNUW2NlQh|ryP M3LsRnNCVkeHUh?=
RXF393 MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwNUW3PVQh|ryP NHywW|JUSU6JRWK=
SW872 NIG5d2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTuXpdWUUN3ME2wMlU3PzJ2IN88US=> MkPaV2FPT0WU
MPP-89 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LvdWlEPTB;MD61O|g5PCEQvF2= MkHhV2FPT0WU
RPMI-8226 MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwNkO1NlYh|ryP M2nJbHNCVkeHUh?=
LS-1034 NU\0e3Y3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPYPZJKSzVyPUCuOlM2QCEQvF2= NFLlV3FUSU6JRWK=
SJSA-1 M1;lV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrZTWM2OD1yLk[zO|I2KM7:TR?= M2XOenNCVkeHUh?=
HOP-62 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonwTWM2OD1yLk[1NFM{KM7:TR?= NIrORVZUSU6JRWK=
KGN M1WzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHOSFZKSzVyPUCuOlYyPjhizszN MoriV2FPT0WU
D-336MG M2TDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonITWM2OD1yLk[2NVY6KM7:TR?= MWfTRW5ITVJ?
LS-411N Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PZV2lEPTB;MD62O|Q3OiEQvF2= MVvTRW5ITVJ?
TE-1 MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTBwNkmwO|Qh|ryP M4jFNXNCVkeHUh?=
LB996-RCC NX3KN|RZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DLUmlEPTB;MD62PVM5QSEQvF2= M{ntT3NCVkeHUh?=
TE-10 MnnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nrcGlEPTB;MD63NVQ6PiEQvF2= NHfVfHdUSU6JRWK=
NCI-SNU-16 M3TwWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVThSXlRUUN3ME2wMlczPjZ2IN88US=> NFqy[IFUSU6JRWK=
ES8 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwN{S5O|Uh|ryP NYrJbXZYW0GQR1XS
COLO-800 MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C4WWlEPTB;MD63OlY6PSEQvF2= M33n[XNCVkeHUh?=
ES6 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnjXYFKSzVyPUCuO|c2PTlizszN NWfr[5ZsW0GQR1XS
L-363 MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\SOGZKSzVyPUCuPFI{PzVizszN MXXTRW5ITVJ?
NMC-G1 NWjmb4l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwOEOyN|Mh|ryP M2LpXnNCVkeHUh?=
LU-134-A NEDRWnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzBe4RKSzVyPUCuPFM6OTJizszN M3:1PXNCVkeHUh?=
SF268 M1\4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHTTWM2OD1yLki0NFQzKM7:TR?= Mo\5V2FPT0WU
KARPAS-45 M3XEZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwOESyOlMh|ryP MYfTRW5ITVJ?
TGW MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\rTWM2OD1yLki1PFY{KM7:TR?= MofIV2FPT0WU
CHP-126 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TJWmlEPTB;MD64OVk2PyEQvF2= NHTvOoZUSU6JRWK=
MOLT-16 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r3TGlEPTB;MD64O|U5QSEQvF2= NGL2OZdUSU6JRWK=
LB771-HNC NFTOXFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn32TWM2OD1yLki5O|U4KM7:TR?= NInob|lUSU6JRWK=
NALM-6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y0N2lEPTB;MD65NFc{QSEQvF2= MXPTRW5ITVJ?
GCIY MnnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C4WmlEPTB;MD65OVUzPiEQvF2= NWPsNIkxW0GQR1XS
IST-MES1 NVTTcGlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzvc4g3UUN3ME2wMlk5QDJ2IN88US=> NYflTnJuW0GQR1XS
LB2241-RCC Mn\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnizTWM2OD1yLkm4PFQh|ryP MlXoV2FPT0WU
BL-70 M1jmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUG1OmFbUUN3ME2wMlk6PTN3IN88US=> NILNU3VUSU6JRWK=
NB17 M1;semdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;ITYdKSzVyPUGuNFA3OzlizszN NGPwOplUSU6JRWK=
LXF-289 NFXNNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nZdWlEPTB;MT6wN|A4PiEQvF2= NHrBTZhUSU6JRWK=
TK10 M4PV[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzy[YpKSzVyPUGuNFUxPjNizszN MXPTRW5ITVJ?
K5 NGji[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4riNmlEPTB;MT6wOlI4PCEQvF2= M4XVfXNCVkeHUh?=
NCI-H716 M3TFWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjpTGY1UUN3ME2xMlA4OjV7IN88US=> NHfOR3hUSU6JRWK=
HCE-T MkTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjhXXVKSzVyPUGuNFg5OTlizszN M17OS3NCVkeHUh?=
GI-1 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFwMEm3PVgh|ryP MlTMV2FPT0WU
KARPAS-422 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwMUCwNlIh|ryP Mlz2V2FPT0WU
TE-9 NVj1UXo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPhToNKSzVyPUGuNVE{OjhizszN M1rwc3NCVkeHUh?=
SF126 NVXo[YgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;aTWM2OD1zLkGxOVY5KM7:TR?= MmX0V2FPT0WU
BB30-HNC NY\QOI56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\LTWM2OD1zLkGzNVEzKM7:TR?= MoL5V2FPT0WU
NCI-H1304 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\sTWM2OD1zLkGzN|M5KM7:TR?= NWLrcGszW0GQR1XS
HEL MnSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH6xSJBKSzVyPUGuNVQ5QTVizszN MULTRW5ITVJ?
HAL-01 NWD0O3FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPvO|JKSzVyPUGuNVUzQDNizszN MUHTRW5ITVJ?
SK-LMS-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwMUW5O|Qh|ryP MXrTRW5ITVJ?
SW954 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHER|J1UUN3ME2xMlE6PTZ5IN88US=> NETHNHJUSU6JRWK=
D-283MED M3H6cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33DVmlEPTB;MT6yNlM4QSEQvF2= MXfTRW5ITVJ?
NCI-H1882 NG\MboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvaR4dKSzVyPUGuNlM5QSEQvF2= M4nJN3NCVkeHUh?=
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SK-MEL-2 MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnCfIRKSzVyPUGwMlk6OzlizszN M3nxdXNCVkeHUh?=

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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
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

Related Antibodies

ALK信号経路図

ALK Inhibitors with Unique Features

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