TAE684 (NVP-TAE684) 化学構造
分子量: 614.2

高品質保証

カスタマーフィードバック(4)

MSDS

製品説明

  • Compare ALK Inhibitors
    ALK製品生物活性の比較
  • 研究分野
  • TAE684 (NVP-TAE684)のメカニズム

製品の説明

生物活性

製品説明 TAE684 (NVP-TAE684)は、3nMのIC50による強力で選択的なALKキナーゼ阻害剤です。
ターゲット ALK
IC50 3 nM [1]
In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SCC-3 NFTVXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{njS2lEPTB;MD6wNFAxPjB|IN88US=> MojkV2FPT0WU
SF539 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLoUVVKSzVyPUCuNFAxPTZ2IN88US=> NFOxV45USU6JRWK=
DEL NXHyPWE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlOyTWM2OD1yLkCwNFkzPyEQvF2= NXX2NlZ{W0GQR1XS
NB1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSwc41NUUN3ME2wMlAxOTZ{IN88US=> Ml;QV2FPT0WU
SR NEPlOodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwMECyO|ch|ryP MVrTRW5ITVJ?
KARPAS-299 NWXQemJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLa[GxKSzVyPUCuNFI{QDRizszN NE\YNIlUSU6JRWK=
MHH-CALL-2 M3z1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMEK5OVIh|ryP M4focnNCVkeHUh?=
SU-DHL-1 M3XqSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDEXHpKSzVyPUCuNFQ5PjVizszN NUm4WHl5W0GQR1XS
A4-Fuk NYWyeXlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zD[mlEPTB;MD6wOVU3PSEQvF2= M2fnT3NCVkeHUh?=
EW-1 NHfONYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMUCyOVYh|ryP NEXNOWVUSU6JRWK=
NOS-1 NUX0[FNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwMUCyPVQh|ryP MWjTRW5ITVJ?
EW-16 M3ro[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjJOpdUUUN3ME2wMlExPTZ6IN88US=> MUDTRW5ITVJ?
TE-11 Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGj1cZFKSzVyPUCuNVYxQTZizszN MmPlV2FPT0WU
SW982 NImwXGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TidmlEPTB;MD6xOlQ4QCEQvF2= MUTTRW5ITVJ?
LAN-6 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvrTWM2OD1yLkG3OFQ{KM7:TR?= NFLPUHRUSU6JRWK=
MZ1-PC M{f6XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\0O4NoUUN3ME2wMlE4QDN3IN88US=> M2\JWHNCVkeHUh?=
KS-1 NFy1WHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPsTWM2OD1yLkG5N|Q{KM7:TR?= NXTUO|lGW0GQR1XS
PSN1 NVzMd5RVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXGTWM2OD1yLkG5OlMyKM7:TR?= MlXzV2FPT0WU
LC-2-ad MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\NbG5KSzVyPUCuNVk3QTJizszN NITQXJFUSU6JRWK=
COLO-320-HSR M1PHdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTBwMUm3O|Yh|ryP Mm\WV2FPT0WU
OPM-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPSbHpWUUN3ME2wMlIzPjZ7IN88US=> MVnTRW5ITVJ?
SK-NEP-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjNU|lKSzVyPUCuNlM2OjRizszN NIHVc5JUSU6JRWK=
ALL-PO NInZWY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:4NWlEPTB;MD6yOFUzPCEQvF2= MWjTRW5ITVJ?
CMK NUXvOHJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlexTWM2OD1yLkK1OVMh|ryP MlzIV2FPT0WU
NCI-H1648 M2jnZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;RS|djUUN3ME2wMlI4QDV3IN88US=> NF\IbI9USU6JRWK=
SIG-M5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHX4TIpKSzVyPUCuNlkyPTlizszN MmmzV2FPT0WU
TGBC24TKB MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrue283UUN3ME2wMlMxOjF6IN88US=> M4n4XXNCVkeHUh?=
DOHH-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfnPFJKSzVyPUCuN|EzODRizszN NYnCfItXW0GQR1XS
NB69 MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED6dZVKSzVyPUCuN|E4QDdizszN MlrwV2FPT0WU
MFH-ino MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjESm4xUUN3ME2wMlMzPTJ|IN88US=> M2[xSHNCVkeHUh?=
KP-N-RT-BM-1 NVK1S2I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjETWM2OD1yLkOzNVI{KM7:TR?= M1TsfXNCVkeHUh?=
MONO-MAC-6 NISzZplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PVT2lEPTB;MD6zN|I6OSEQvF2= MXrTRW5ITVJ?
ATN-1 NUXobGt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLUTWM2OD1yLkOzN|A{KM7:TR?= M17YZnNCVkeHUh?=
NTERA-S-cl-D1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnJTWM2OD1yLkOzN|k3KM7:TR?= NYPBWmNQW0GQR1XS
L-540 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfT[GdKSzVyPUCuN|Y6QDhizszN NWD1Wm1CW0GQR1XS
GB-1 NWTmdGxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzoeZFKSzVyPUCuN|g5PjdizszN MVfTRW5ITVJ?
MV-4-11 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzSNld1UUN3ME2wMlM6PDR4IN88US=> M3y0V3NCVkeHUh?=
KG-1 M4G3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTtVplKSzVyPUCuN|k2PjFizszN MV\TRW5ITVJ?
OVCAR-4 MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULhe3RkUUN3ME2wMlQxPTZ7IN88US=> MVzTRW5ITVJ?
NEC8 M4LHfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Tx[2lEPTB;MD60NVI6OiEQvF2= NGryeYZUSU6JRWK=
SK-MM-2 NWmy[3p7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfTe4RKSzVyPUCuOFE3ODlizszN M{L3XXNCVkeHUh?=
TE-8 NE\CWXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwNEK4PEDPxE1? MU\TRW5ITVJ?
697 M4TIO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TWfmlEPTB;MD60N|IyPSEQvF2= NF\nTZBUSU6JRWK=
NB14 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfsS3pKSzVyPUCuOFM5OjZizszN MoXvV2FPT0WU
GDM-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrFXmRXUUN3ME2wMlQ4OTF4IN88US=> MVjTRW5ITVJ?
HUTU-80 Mlf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\E[mVKSzVyPUCuOFc{PzVizszN NV;ONYVRW0GQR1XS
HL-60 NXHaR4ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTBwNEixOFIh|ryP MWLTRW5ITVJ?
OCI-AML2 NX[1VW5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnTTWM2OD1yLkS4N|I5KM7:TR?= MnrPV2FPT0WU
ML-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoOzTWM2OD1yLkS5NFMyKM7:TR?= MlnqV2FPT0WU
ES4 MkTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny2TWM2OD1yLkS5NVA6KM7:TR?= MVPTRW5ITVJ?
NCI-H747 NUW5[VlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nGUGlEPTB;MD60PVg6KM7:TR?= M{n0UHNCVkeHUh?=
RL95-2 MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HOUmlEPTB;MD61NFEyOiEQvF2= NXTFT4FnW0GQR1XS
TE-15 MmjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\IeYxKSzVyPUCuOVEyOjRizszN NUKxR5ZmW0GQR1XS
TE-12 NVLDNFlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHMTWM2OD1yLkWzN|Q6KM7:TR?= NYfVcHVoW0GQR1XS
LB1047-RCC M1LmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD0cI5LUUN3ME2wMlU1PTR7IN88US=> MVnTRW5ITVJ?
LB831-BLC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwNUWwNlMh|ryP MV7TRW5ITVJ?
NCI-H1355 NFjINFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHHTWM2OD1yLkW1NVg1KM7:TR?= NH[2SnlUSU6JRWK=
CTV-1 NGXvNWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPE[VNUUUN3ME2wMlU2PjJ2IN88US=> NGnjVXVUSU6JRWK=
RXF393 M4HMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\EWGRKSzVyPUCuOVU4QTRizszN NIThVohUSU6JRWK=
SW872 NV71eXR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwNU[3NlQh|ryP M4PGPHNCVkeHUh?=
MPP-89 M{jCbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2WyOmlEPTB;MD61O|g5PCEQvF2= NUTDV|Z2W0GQR1XS
RPMI-8226 NHnYeIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvkTWM2OD1yLk[zOVI3KM7:TR?= NF[0U3lUSU6JRWK=
LS-1034 M372RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37lemlEPTB;MD62N|U5KM7:TR?= MlzEV2FPT0WU
SJSA-1 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTafm9KSzVyPUCuOlM4OjVizszN NXXpUnJ[W0GQR1XS
HOP-62 M2TyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO0bo45UUN3ME2wMlY2ODN|IN88US=> M4D1RnNCVkeHUh?=
KGN NX;HVJFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkGzTWM2OD1yLk[2NVY5KM7:TR?= NGD3cIJUSU6JRWK=
D-336MG M2jQbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwNk[xOlkh|ryP M3T1NHNCVkeHUh?=
LS-411N MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSzOmtKSzVyPUCuOlc1PjJizszN MmfLV2FPT0WU
TE-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnKPW1ZUUN3ME2wMlY6ODd2IN88US=> NIfY[pFUSU6JRWK=
LB996-RCC MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwNkmzPFkh|ryP M2X2cHNCVkeHUh?=
TE-10 NXHtOnRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PBbWlEPTB;MD63NVQ6PiEQvF2= M{LJT3NCVkeHUh?=
NCI-SNU-16 M{\PbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXVTWM2OD1yLkeyOlY1KM7:TR?= NF7yfZZUSU6JRWK=
ES8 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnrTWM2OD1yLke0PVc2KM7:TR?= MX\TRW5ITVJ?
COLO-800 MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfjeFZnUUN3ME2wMlc3Pjl3IN88US=> MmPGV2FPT0WU
ES6 NXW2[IVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DxemlEPTB;MD63O|U2QSEQvF2= M4LlenNCVkeHUh?=
L-363 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17LbmlEPTB;MD64NlM4PSEQvF2= MoHQV2FPT0WU
NMC-G1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7vUZRKSzVyPUCuPFMzOzNizszN MlHGV2FPT0WU
LU-134-A NUW0WnVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfRRpVKSzVyPUCuPFM6OTJizszN Mm\6V2FPT0WU
SF268 NVG2TJpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\MZmlEPTB;MD64OFA1OiEQvF2= MUHTRW5ITVJ?
KARPAS-45 NXW1[IdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D6fGlEPTB;MD64OFI3OyEQvF2= NXLEVJoyW0GQR1XS
TGW Mle0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi1SHFKSzVyPUCuPFU5PjNizszN MnHPV2FPT0WU
CHP-126 NHfUO|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojCTWM2OD1yLki1PVU4KM7:TR?= NYH5So1yW0GQR1XS
MOLT-16 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vmb2lEPTB;MD64O|U5QSEQvF2= MUjTRW5ITVJ?
LB771-HNC NWTUOoxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwOEm3OVch|ryP MWXTRW5ITVJ?
NALM-6 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDCTWM2OD1yLkmwO|M6KM7:TR?= NFP0emxUSU6JRWK=
GCIY NXuyN5gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTKTWM2OD1yLkm1OVI3KM7:TR?= Ml\WV2FPT0WU
IST-MES1 NYTh[oNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu2TWM2OD1yLkm4PFI1KM7:TR?= MVrTRW5ITVJ?
LB2241-RCC NH\TU5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\6XlRnUUN3ME2wMlk5QDRizszN MmT5V2FPT0WU
BL-70 M1nwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TRPGlEPTB;MD65PVU{PSEQvF2= MVvTRW5ITVJ?
NB17 NYfiTJV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwMEC2N|kh|ryP NI\Ec2JUSU6JRWK=
LXF-289 NGe0eIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\ycWlEPTB;MT6wN|A4PiEQvF2= MYTTRW5ITVJ?
TK10 M2rFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLVTWM2OD1zLkC1NFY{KM7:TR?= NETRbVRUSU6JRWK=
K5 M4XsfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTmUXBFUUN3ME2xMlA3Ojd2IN88US=> NWC3Ro1zW0GQR1XS
NCI-H716 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLQTWM2OD1zLkC3NlU6KM7:TR?= Mon6V2FPT0WU
HCE-T MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXmTWM2OD1zLkC4PFE6KM7:TR?= MUPTRW5ITVJ?
GI-1 NVvaRpVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjDXm01UUN3ME2xMlA6Pzl6IN88US=> M1S0R3NCVkeHUh?=
KARPAS-422 M1ruSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2zTWM2OD1zLkGwNFIzKM7:TR?= M1;mUHNCVkeHUh?=
TE-9 NGiwd5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFwMUGzNlgh|ryP MVvTRW5ITVJ?
SF126 NGnr[ZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPMTWM2OD1zLkGxOVY5KM7:TR?= MnL4V2FPT0WU
BB30-HNC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrFOY9TUUN3ME2xMlE{OTF{IN88US=> Mn2wV2FPT0WU
NCI-H1304 Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvrTWM2OD1zLkGzN|M5KM7:TR?= NIXQepZUSU6JRWK=
HEL M4jhOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfkb5VQUUN3ME2xMlE1QDl3IN88US=> NF:3S5ZUSU6JRWK=
HAL-01 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLOSpROUUN3ME2xMlE2Ojh|IN88US=> NEHRdmpUSU6JRWK=
SK-LMS-1 M4HqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWCwUJo1UUN3ME2xMlE2QTd2IN88US=> NVXNRng1W0GQR1XS
SW954 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLtNXFCUUN3ME2xMlE6PTZ5IN88US=> M4\wN3NCVkeHUh?=
D-283MED MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P5c2lEPTB;MT6yNlM4QSEQvF2= MWHTRW5ITVJ?
NCI-H1882 NWO4UpJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILiRXNKSzVyPUGuNlM5QSEQvF2= MlziV2FPT0WU
GI-ME-N NUDCZYw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXQRmpsUUN3ME2xMlI2OjB6IN88US=> MorTV2FPT0WU
SK-PN-DW M1TJO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFwMk[zOFgh|ryP NFnJV|NUSU6JRWK=
C2BBe1 M1TaOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfNTWM2OD1zLkK5NVE4KM7:TR?= M1\UbXNCVkeHUh?=
A704 NWn3Uph3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zEbmlEPTB;MT6zNlY5QSEQvF2= MlLRV2FPT0WU
KALS-1 MnL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPPXIpKSzVyPUGuN|QxQCEQvF2= M4rzPXNCVkeHUh?=
ETK-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LIN2lEPTB;MT6zOFQ5QSEQvF2= NIC5VolUSU6JRWK=
LB647-SCLC MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwM{S5PFYh|ryP MorDV2FPT0WU
OCUB-M MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHBTWM2OD1zLkO2NVQ{KM7:TR?= M2SwfHNCVkeHUh?=
NCI-H720 NVrLdVlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHWTJRKSzVyPUGuN|Y{PzhizszN NYjBb4VKW0GQR1XS
NB13 M2XtW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr3OZI5UUN3ME2xMlM4Ojl|IN88US=> M3XBN3NCVkeHUh?=
GR-ST M1\UWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFwM{i3OVch|ryP MVzTRW5ITVJ?
DU-4475 NFfu[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LLT2lEPTB;MT60OVg2OyEQvF2= M3\TNnNCVkeHUh?=
HCC2157 NY[yZ|RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLMVYRKSzVyPUGuOFY3PTlizszN MXnTRW5ITVJ?
RKO NIr4cXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknJTWM2OD1zLkS5PVIzKM7:TR?= NH7wcFVUSU6JRWK=
LS-123 M{DlTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH0TWM2OD1zLkWxOVk1KM7:TR?= MnLBV2FPT0WU
NCI-H69 NX3PTpVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLvTWM2OD1zLkW1PFEyKM7:TR?= NHHvcHhUSU6JRWK=
SW962 M13aO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfXTWM2OD1zLkW2NVMh|ryP M3zF[HNCVkeHUh?=
PF-382 M331bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnlTGI2UUN3ME2xMlU3QTZizszN NVuzT|NHW0GQR1XS
A101D M3nzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTFwNUexNVMh|ryP NYTJU21IW0GQR1XS
NB10 MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlSzTWM2OD1zLkW3N|kzKM7:TR?= MkHYV2FPT0WU
NB5 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4OxSWlEPTB;MT61PFQ4PiEQvF2= MXTTRW5ITVJ?
HCE-4 NGHaZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2O2NmlEPTB;MT62NFg2KM7:TR?= MorhV2FPT0WU
HT-144 NHGz[HRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFwNkOxPUDPxE1? NGLucIRUSU6JRWK=
NCI-H524 NF2weHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTFwNkSzNFch|ryP MXzTRW5ITVJ?
NKM-1 NYXGS3h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFwNki2OkDPxE1? M1TTNXNCVkeHUh?=
KURAMOCHI MmnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3H1[GlEPTB;MT62PVU4OyEQvF2= NUX1Vod6W0GQR1XS
NCI-H187 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm2TWM2OD1zLkewNFM3KM7:TR?= NEXF[JdUSU6JRWK=
U-266 NFPzUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LqNmlEPTB;MT63N|g1OiEQvF2= MV\TRW5ITVJ?
BL-41 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFwN{[yO|Ih|ryP Mnj1V2FPT0WU
SK-N-DZ NFS3S2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXlb2RQUUN3ME2xMlc5OzB7IN88US=> M36xNHNCVkeHUh?=
Daudi NIe4RZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP2XFE2UUN3ME2xMlc5QTZ5IN88US=> M2iwXHNCVkeHUh?=
CPC-N M4njPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFwOEWwPVYh|ryP NETyT5NUSU6JRWK=
EM-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIOxbZRKSzVyPUGuPFUyKM7:TR?= NWDq[5lOW0GQR1XS
HCC1187 M3\vdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M362PGlEPTB;MT64OlI1OSEQvF2= MV7TRW5ITVJ?
LP-1 M{PKcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\0eZNZUUN3ME2xMlg4OTR|IN88US=> M3fEOXNCVkeHUh?=
CAS-1 NV21S3pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGm4eolKSzVyPUGuPVgzQTlizszN M4PrWXNCVkeHUh?=
NB7 NVzp[JBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXjfZdKSzVyPUKuNFA2PTVizszN MULTRW5ITVJ?
VA-ES-BJ M4C0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf1TWM2OD1{LkCxOVE{KM7:TR?= NIGyXndUSU6JRWK=
SNU-C2B NILLdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n3V2lEPTB;Mj6wN|M2OSEQvF2= NUPzOI8{W0GQR1XS
LOXIMVI NVP3UXhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonRTWM2OD1{LkC2O|g3KM7:TR?= NGTufm9USU6JRWK=
NCI-H1581 NYHqfnhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfVTWM2OD1{LkGxOVU6KM7:TR?= NFH3TIRUSU6JRWK=
IST-SL2 MlzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LQPWlEPTB;Mj6xNlQ1PSEQvF2= M1TI[HNCVkeHUh?=
NOMO-1 M3fJOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJwMUe2PFMh|ryP NWLrOWJzW0GQR1XS
TE-6 NX33SVBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X0ZmlEPTB;Mj6xPVA2KM7:TR?= NFfTfZBUSU6JRWK=
NCI-H526 NIPsRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzyOGFWUUN3ME2yMlE6OTRzIN88US=> MXPTRW5ITVJ?
MSTO-211H NWq5fopLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjDRXNoUUN3ME2yMlIxODRzIN88US=> MlvTV2FPT0WU
LS-513 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PHUmlEPTB;Mj6yNlI3QSEQvF2= NU\yTXY4W0GQR1XS
NCI-SNU-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJwM{OyOVYh|ryP M{m1Z3NCVkeHUh?=
BB65-RCC NIr5Z2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj3c5JGUUN3ME2yMlM4PDl|IN88US=> NGjLN4ZUSU6JRWK=
GT3TKB M1OwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLGTWM2OD1{LkO5PVczKM7:TR?= NFLFVoZUSU6JRWK=
OS-RC-2 NGP1SXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJwNEKzOFEh|ryP MoDmV2FPT0WU
NCI-H2126 M12x[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJwNEO2O|Qh|ryP MVrTRW5ITVJ?
SK-UT-1 M3G2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;Nc2lEPTB;Mj60O|Q3PyEQvF2= MnHIV2FPT0WU
DMS-114 NU\wT|BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHHTXJzUUN3ME2yMlYyPTJ2IN88US=> MWTTRW5ITVJ?
ONS-76 NVmyXYNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1SwSWlEPTB;Mj62N|Y1OSEQvF2= M{O2V3NCVkeHUh?=
8-MG-BA M2jDZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XaS2lEPTB;Mj62OVQyPCEQvF2= NU\pb5NHW0GQR1XS
BOKU Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO4TWM2OD1{LkeyO|Y1KM7:TR?= NVLmVVMxW0GQR1XS
LAMA-84 NWPRXVZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7IPGVKSzVyPUKuO|k6OTJizszN NVm0NpZ[W0GQR1XS
ES1 NGDtO3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHyNZlSUUN3ME2yMlgyQDB2IN88US=> NFrrXW9USU6JRWK=
NCI-H1395 M{PvSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzoPWo{UUN3ME2yMlgzODF{IN88US=> MnLzV2FPT0WU
A388 NHvNfFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXWRmd2UUN3ME2yMlk3OTdizszN NX7qc45QW0GQR1XS
NCCIT MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTNwMEi4OlIh|ryP MkXYV2FPT0WU
HD-MY-Z NGHxOlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ntSmlEPTB;Mz6xN|IxOyEQvF2= NIHLPG1USU6JRWK=
NCI-H510A MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTNwMUi5OFMh|ryP MYXTRW5ITVJ?
NCI-N87 M{PlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\vOmlEPTB;Mz6yNFAzKM7:TR?= NV;lWmM3W0GQR1XS
SCLC-21H NG\ae3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3pSm9uUUN3ME2zMlI3QDV7IN88US=> NXi5WotHW0GQR1XS
SH-4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTNwMki3PVch|ryP NEPkUnJUSU6JRWK=
QIMR-WIL NY\pfYttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfNTJBxUUN3ME2zMlMzQDR7IN88US=> NHL1[ZBUSU6JRWK=
KM12 M4XUc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNwM{O1OFQh|ryP MnPyV2FPT0WU
ST486 M2ThOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHSRo9KSzVyPUOuOVM5QDNizszN M4\rS3NCVkeHUh?=
HC-1 NWnrNW9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK5Xo9KSzVyPUOuOlIxOjhizszN M2nnc3NCVkeHUh?=
BV-173 MlznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDjRYQ4UUN3ME2zMlY1ODh6IN88US=> NEXYOXVUSU6JRWK=
EW-24 MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2r5XmlEPTB;Mz62OlQ{PCEQvF2= MkXxV2FPT0WU
LU-65 NGWzUJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPvc2twUUN3ME2zMlY5PzFizszN NEXzUJFUSU6JRWK=
ECC4 MnXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L6[WlEPTB;Mz63O|U3KM7:TR?= M4XzOHNCVkeHUh?=
ARH-77 NIiwVm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu0TWM2OD12LkGxNFY4KM7:TR?= MoLsV2FPT0WU
BC-3 NWDGVZFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTRwMUOwOlgh|ryP MoLKV2FPT0WU
SNB75 NFHWUIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;3U2lEPTB;ND6yOlE6KM7:TR?= NVzPO29rW0GQR1XS
MEG-01 NFe4VVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTRwMke0NVkh|ryP M1jEcnNCVkeHUh?=
NCI-H1417 NWe2NXdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n4ZmlEPTB;ND6yPFQ1OyEQvF2= M1;qfXNCVkeHUh?=
MDA-MB-134-VI MnO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq2b2szUUN3ME20MlMxPjBzIN88US=> NEPzdGxUSU6JRWK=
Becker NXvGNXBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTRwNEezN|Yh|ryP NW\HZ443W0GQR1XS
DMS-153 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTRwNk[0O|Uh|ryP MU\TRW5ITVJ?
TGBC1TKB MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLN[GdLUUN3ME20MlY5PTF3IN88US=> MmmxV2FPT0WU
EW-3 NFfCNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTRwN{[yOFgh|ryP M{fFPHNCVkeHUh?=
KE-37 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXqwOmRKUUN3ME20Mlg3OTl4IN88US=> MVLTRW5ITVJ?
NCI-H23 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXjTGI3UUN3ME20Mlg4OjJ5IN88US=> NFPIZ4FUSU6JRWK=
MC116 M2PxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTRwOUSxNlYh|ryP MWLTRW5ITVJ?
NH-12 M1;w[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTRwOU[0N|kh|ryP MnPmV2FPT0WU
CTB-1 M3vNPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHZNJlsUUN3ME20Mlk4PzJzIN88US=> MoDGV2FPT0WU
KM-H2 NYnGc2JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\CTWM2OD13LkC1N|I{KM7:TR?= NUDFU5BSW0GQR1XS
MOLT-4 NX7XUJFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\TcZBKSzVyPUWuNVE5OyEQvF2= NEDKcG1USU6JRWK=
NCI-H2141 M2DCfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTVwMUSyOlgh|ryP MYXTRW5ITVJ?
EB-3 NVTkdWVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DiSGlEPTB;NT6xO|UxPCEQvF2= NHXRfJlUSU6JRWK=
NCI-H1522 MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDxVoo6UUN3ME21MlI3OzJ{IN88US=> MYTTRW5ITVJ?
MRK-nu-1 NEjZXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojwTWM2OD13LkSzOlM{KM7:TR?= MnPPV2FPT0WU
no-11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljNTWM2OD13LkS3NFg4KM7:TR?= NYrDUmhDW0GQR1XS
CESS M{H0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEOxSI5KSzVyPUWuOVgxOzRizszN Ml;vV2FPT0WU
KMOE-2 NXfRUnI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLMTWM2OD13LkW4OlU6KM7:TR?= NVy3ZWh7W0GQR1XS
REH MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXQWnQxUUN3ME22MlI2PjF6IN88US=> MVvTRW5ITVJ?
KU812 MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTZwNEK3PVEh|ryP MUHTRW5ITVJ?
SK-N-FI MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1u3fGlEPTB;Nj62NFY4PCEQvF2= MnjQV2FPT0WU
MMAC-SF MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7RTWM2OD15LkC2OFkzKM7:TR?= M{HnZnNCVkeHUh?=
RCC10RGB NUnkZm1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTdwMkK5O|ch|ryP MmHxV2FPT0WU
NCI-H322M MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHIblNKSzVyPUeuN|M{OzVizszN M4PFdXNCVkeHUh?=
NB6 NW\qbGJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrLU2hVUUN3ME23MlU1QDl7IN88US=> M4rUSHNCVkeHUh?=
MN-60 MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTdwNkmyNVUh|ryP M1[wTHNCVkeHUh?=
NCI-H1092 NFKwNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvLV2dKSzVyPUiuNFE4OzRizszN NFX4d4JUSU6JRWK=
EKVX Mk\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXLdllUUUN3ME24MlQ4ODZ4IN88US=> NXy5NnRMW0GQR1XS
D-263MG MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3Zbo5FUUN3ME24MlU2Ozl4IN88US=> M1rEWnNCVkeHUh?=
NCI-H209 NFjjWWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnezTWM2OD16Lk[0NFA3KM7:TR?= NEjnUFdUSU6JRWK=
IST-SL1 NWTVUZRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDzbnM2UUN3ME24Mlg6QDl{IN88US=> MVHTRW5ITVJ?
ACN MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj3TWM2OD17LkG5NVU4KM7:TR?= MXvTRW5ITVJ?
MHH-PREB-1 NEjUblZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S1[GlEPTB;OT6yNVIyQSEQvF2= NGLRN5FUSU6JRWK=
EW-11 M162XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTlwNkWzPVYh|ryP MlXNV2FPT0WU
KASUMI-1 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DBW2lEPTB;OT63PFc4KM7:TR?= MVXTRW5ITVJ?
KINGS-1 NIPjXpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2q2OWlEPTB;MUCuNlM1PyEQvF2= M4\udXNCVkeHUh?=
EVSA-T Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDMTWM2OD1zMD6zNVkzKM7:TR?= M{KyV3NCVkeHUh?=
DSH1 M1GwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTFyLkO5O|Ih|ryP MY\TRW5ITVJ?
COLO-824 M2LCVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFyLki2Olkh|ryP M3;ESnNCVkeHUh?=
K052 NHrkb2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fBW2lEPTB;MUCuPVMzOiEQvF2= NGC2UW9USU6JRWK=
SK-MEL-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP0V2pKSzVyPUGwMlk6OzlizszN MXzTRW5ITVJ?

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

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.

動物実験: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download TAE684 (NVP-TAE684) SDF
分子量 614.2
化学式

C30H40ClN7O3S

CAS No. 761439-42-3
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 3 mg/mL (4.88 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol, pH 4 10 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine

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