pour la recherche uniquement
TAE684 (NVP-TAE684) ALK inhibiteur
Réf. CatalogueS1108
Structure chimique
Poids moléculaire: 614.2
Contrôle Qualité
| Cibles apparentées | EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 |
|---|---|
| Autre ALK Inhibiteurs | GSK1838705A Repotrectinib (TPX-0005) AZD3463 Ensartinib dihydrochloride AP26113-analog (ALK-IN-1) ASP3026 NVL-655 (Neladalkib) Envonalkib Belizatinib (TSR-011) HG-14-10-04 |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| SCC-3 | Growth Inhibition Assay | IC50=0.0000603 μM | ||||
| SF539 | Growth Inhibition Assay | IC50=0.000564 μM | ||||
| DEL | Growth Inhibition Assay | IC50=0.000927 μM | ||||
| NB1 | Growth Inhibition Assay | IC50=0.00162 μM | ||||
| SR | Growth Inhibition Assay | IC50=0.00277 μM | ||||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.02384 μM | ||||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=0.02952 μM | ||||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.04865 μM | ||||
| A4-Fuk | Growth Inhibition Assay | IC50=0.05565 μM | ||||
| EW-1 | Growth Inhibition Assay | IC50=0.10256 μM | ||||
| NOS-1 | Growth Inhibition Assay | IC50=0.10294 μM | ||||
| EW-16 | Growth Inhibition Assay | IC50=0.10568 μM | ||||
| TE-11 | Growth Inhibition Assay | IC50=0.16096 μM | ||||
| SW982 | Growth Inhibition Assay | IC50=0.16478 μM | ||||
| LAN-6 | Growth Inhibition Assay | IC50=0.17443 μM | ||||
| MZ1-PC | Growth Inhibition Assay | IC50=0.17835 μM | ||||
| KS-1 | Growth Inhibition Assay | IC50=0.19343 μM | ||||
| PSN1 | Growth Inhibition Assay | IC50=0.19631 μM | ||||
| LC-2-ad | Growth Inhibition Assay | IC50=0.19692 μM | ||||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.19776 μM | ||||
| OPM-2 | Growth Inhibition Assay | IC50=0.22669 μM | ||||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.23524 μM | ||||
| ALL-PO | Growth Inhibition Assay | IC50=0.24524 μM | ||||
| CMK | Growth Inhibition Assay | IC50=0.2553 μM | ||||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.27855 μM | ||||
| SIG-M5 | Growth Inhibition Assay | IC50=0.29159 μM | ||||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.30218 μM | ||||
| DOHH-2 | Growth Inhibition Assay | IC50=0.31204 μM | ||||
| NB69 | Growth Inhibition Assay | IC50=0.31787 μM | ||||
| MFH-ino | Growth Inhibition Assay | IC50=0.32523 μM | ||||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=0.33123 μM | ||||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.33291 μM | ||||
| ATN-1 | Growth Inhibition Assay | IC50=0.33303 μM | ||||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.33396 μM | ||||
| L-540 | Growth Inhibition Assay | IC50=0.36988 μM | ||||
| GB-1 | Growth Inhibition Assay | IC50=0.38867 μM | ||||
| MV-4-11 | Growth Inhibition Assay | IC50=0.39446 μM | ||||
| KG-1 | Growth Inhibition Assay | IC50=0.39561 μM | ||||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.40569 μM | ||||
| NEC8 | Growth Inhibition Assay | IC50=0.41292 μM | ||||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.41609 μM | ||||
| TE-8 | Growth Inhibition Assay | IC50=0.4288 μM | ||||
| 697 | Growth Inhibition Assay | IC50=0.43215 μM | ||||
| NB14 | Growth Inhibition Assay | IC50=0.43826 μM | ||||
| GDM-1 | Growth Inhibition Assay | IC50=0.47116 μM | ||||
| HUTU-80 | Growth Inhibition Assay | IC50=0.47375 μM | ||||
| HL-60 | Growth Inhibition Assay | IC50=0.48142 μM | ||||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.48328 μM | ||||
| ML-2 | Growth Inhibition Assay | IC50=0.49031 μM | ||||
| ES4 | Growth Inhibition Assay | IC50=0.49109 μM | ||||
| NCI-H747 | Growth Inhibition Assay | IC50=0.4989 μM | ||||
| RL95-2 | Growth Inhibition Assay | IC50=0.50112 μM | ||||
| TE-15 | Growth Inhibition Assay | IC50=0.51124 μM | ||||
| TE-12 | Growth Inhibition Assay | IC50=0.53349 μM | ||||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.54549 μM | ||||
| LB831-BLC | Growth Inhibition Assay | IC50=0.55023 μM | ||||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.55184 μM | ||||
| CTV-1 | Growth Inhibition Assay | IC50=0.55624 μM | ||||
| RXF393 | Growth Inhibition Assay | IC50=0.55794 μM | ||||
| SW872 | Growth Inhibition Assay | IC50=0.56724 μM | ||||
| MPP-89 | Growth Inhibition Assay | IC50=0.57884 μM | ||||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.63526 μM | ||||
| LS-1034 | Growth Inhibition Assay | IC50=0.6358 μM | ||||
| SJSA-1 | Growth Inhibition Assay | IC50=0.63725 μM | ||||
| HOP-62 | Growth Inhibition Assay | IC50=0.65033 μM | ||||
| KGN | Growth Inhibition Assay | IC50=0.66168 μM | ||||
| D-336MG | Growth Inhibition Assay | IC50=0.66169 μM | ||||
| LS-411N | Growth Inhibition Assay | IC50=0.67462 μM | ||||
| TE-1 | Growth Inhibition Assay | IC50=0.69074 μM | ||||
| LB996-RCC | Growth Inhibition Assay | IC50=0.69389 μM | ||||
| TE-10 | Growth Inhibition Assay | IC50=0.71496 μM | ||||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.72664 μM | ||||
| ES8 | Growth Inhibition Assay | IC50=0.74975 μM | ||||
| COLO-800 | Growth Inhibition Assay | IC50=0.76695 μM | ||||
| ES6 | Growth Inhibition Assay | IC50=0.77559 μM | ||||
| L-363 | Growth Inhibition Assay | IC50=0.82375 μM | ||||
| NMC-G1 | Growth Inhibition Assay | IC50=0.83233 μM | ||||
| LU-134-A | Growth Inhibition Assay | IC50=0.83912 μM | ||||
| SF268 | Growth Inhibition Assay | IC50=0.84042 μM | ||||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.84263 μM | ||||
| TGW | Growth Inhibition Assay | IC50=0.85863 μM | ||||
| CHP-126 | Growth Inhibition Assay | IC50=0.85957 μM | ||||
| MOLT-16 | Growth Inhibition Assay | IC50=0.87589 μM | ||||
| LB771-HNC | Growth Inhibition Assay | IC50=0.89757 μM | ||||
| NALM-6 | Growth Inhibition Assay | IC50=0.90739 μM | ||||
| GCIY | Growth Inhibition Assay | IC50=0.95526 μM | ||||
| IST-MES1 | Growth Inhibition Assay | IC50=0.98824 μM | ||||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.9884 μM | ||||
| BL-70 | Growth Inhibition Assay | IC50=0.99535 μM | ||||
| NB17 | Growth Inhibition Assay | IC50=1.00639 μM | ||||
| LXF-289 | Growth Inhibition Assay | IC50=1.03076 μM | ||||
| TK10 | Growth Inhibition Assay | IC50=1.05063 μM | ||||
| K5 | Growth Inhibition Assay | IC50=1.06274 μM | ||||
| NCI-H716 | Growth Inhibition Assay | IC50=1.07259 μM | ||||
| HCE-T | Growth Inhibition Assay | IC50=1.08819 μM | ||||
| GI-1 | Growth Inhibition Assay | IC50=1.09798 μM | ||||
| KARPAS-422 | Growth Inhibition Assay | IC50=1.10022 μM | ||||
| TE-9 | Growth Inhibition Assay | IC50=1.11328 μM | ||||
| SF126 | Growth Inhibition Assay | IC50=1.11568 μM | ||||
| BB30-HNC | Growth Inhibition Assay | IC50=1.13112 μM | ||||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.13338 μM | ||||
| HEL | Growth Inhibition Assay | IC50=1.14895 μM | ||||
| HAL-01 | Growth Inhibition Assay | IC50=1.15283 μM | ||||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.15974 μM | ||||
| SW954 | Growth Inhibition Assay | IC50=1.19567 μM | ||||
| D-283MED | Growth Inhibition Assay | IC50=1.22379 μM | ||||
| NCI-H1882 | Growth Inhibition Assay | IC50=1.2389 μM | ||||
| GI-ME-N | Growth Inhibition Assay | IC50=1.25208 μM | ||||
| SK-PN-DW | Growth Inhibition Assay | IC50=1.26348 μM | ||||
| C2BBe1 | Growth Inhibition Assay | IC50=1.29117 μM | ||||
| A704 | Growth Inhibition Assay | IC50=1.32689 μM | ||||
| KALS-1 | Growth Inhibition Assay | IC50=1.3408 μM | ||||
| ETK-1 | Growth Inhibition Assay | IC50=1.34489 μM | ||||
| LB647-SCLC | Growth Inhibition Assay | IC50=1.34986 μM | ||||
| OCUB-M | Growth Inhibition Assay | IC50=1.36143 μM | ||||
| NCI-H720 | Growth Inhibition Assay | IC50=1.36378 μM | ||||
| NB13 | Growth Inhibition Assay | IC50=1.37293 μM | ||||
| GR-ST | Growth Inhibition Assay | IC50=1.38757 μM | ||||
| DU-4475 | Growth Inhibition Assay | IC50=1.45853 μM | ||||
| HCC2157 | Growth Inhibition Assay | IC50=1.46659 μM | ||||
| RKO | Growth Inhibition Assay | IC50=1.49922 μM | ||||
| LS-123 | Growth Inhibition Assay | IC50=1.51594 μM | ||||
| NCI-H69 | Growth Inhibition Assay | IC50=1.55811 μM | ||||
| SW962 | Growth Inhibition Assay | IC50=1.5613 μM | ||||
| PF-382 | Growth Inhibition Assay | IC50=1.5696 μM | ||||
| A101D | Growth Inhibition Assay | IC50=1.57113 μM | ||||
| NB10 | Growth Inhibition Assay | IC50=1.57392 μM | ||||
| NB5 | Growth Inhibition Assay | IC50=1.58476 μM | ||||
| HCE-4 | Growth Inhibition Assay | IC50=1.6085 μM | ||||
| HT-144 | Growth Inhibition Assay | IC50=1.6319 μM | ||||
| NCI-H524 | Growth Inhibition Assay | IC50=1.64307 μM | ||||
| NKM-1 | Growth Inhibition Assay | IC50=1.6866 μM | ||||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.69573 μM | ||||
| NCI-H187 | Growth Inhibition Assay | IC50=1.70036 μM | ||||
| U-266 | Growth Inhibition Assay | IC50=1.73842 μM | ||||
| BL-41 | Growth Inhibition Assay | IC50=1.76272 μM | ||||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.78309 μM | ||||
| Daudi | Growth Inhibition Assay | IC50=1.78967 μM | ||||
| CPC-N | Growth Inhibition Assay | IC50=1.85096 μM | ||||
| EM-2 | Growth Inhibition Assay | IC50=1.851 μM | ||||
| HCC1187 | Growth Inhibition Assay | IC50=1.86241 μM | ||||
| LP-1 | Growth Inhibition Assay | IC50=1.87143 μM | ||||
| CAS-1 | Growth Inhibition Assay | IC50=1.98299 μM | ||||
| NB7 | Growth Inhibition Assay | IC50=2.00555 μM | ||||
| VA-ES-BJ | Growth Inhibition Assay | IC50=2.01513 μM | ||||
| SNU-C2B | Growth Inhibition Assay | IC50=2.03351 μM | ||||
| LOXIMVI | Growth Inhibition Assay | IC50=2.06786 μM | ||||
| NCI-H1581 | Growth Inhibition Assay | IC50=2.11559 μM | ||||
| IST-SL2 | Growth Inhibition Assay | IC50=2.12445 μM | ||||
| NOMO-1 | Growth Inhibition Assay | IC50=2.17683 μM | ||||
| TE-6 | Growth Inhibition Assay | IC50=2.1905 μM | ||||
| NCI-H526 | Growth Inhibition Assay | IC50=2.19141 μM | ||||
| MSTO-211H | Growth Inhibition Assay | IC50=2.20041 μM | ||||
| LS-513 | Growth Inhibition Assay | IC50=2.22269 μM | ||||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.33256 μM | ||||
| BB65-RCC | Growth Inhibition Assay | IC50=2.37493 μM | ||||
| GT3TKB | Growth Inhibition Assay | IC50=2.39972 μM | ||||
| OS-RC-2 | Growth Inhibition Assay | IC50=2.42341 μM | ||||
| NCI-H2126 | Growth Inhibition Assay | IC50=2.43674 μM | ||||
| SK-UT-1 | Growth Inhibition Assay | IC50=2.47467 μM | ||||
| DMS-114 | Growth Inhibition Assay | IC50=2.61524 μM | ||||
| ONS-76 | Growth Inhibition Assay | IC50=2.63641 μM | ||||
| 8-MG-BA | Growth Inhibition Assay | IC50=2.65414 μM | ||||
| BOKU | Growth Inhibition Assay | IC50=2.72764 μM | ||||
| LAMA-84 | Growth Inhibition Assay | IC50=2.79912 μM | ||||
| ES1 | Growth Inhibition Assay | IC50=2.81804 μM | ||||
| NCI-H1395 | Growth Inhibition Assay | IC50=2.82012 μM | ||||
| A388 | Growth Inhibition Assay | IC50=2.9617 μM | ||||
| NCCIT | Growth Inhibition Assay | IC50=3.08862 μM | ||||
| HD-MY-Z | Growth Inhibition Assay | IC50=3.13203 μM | ||||
| NCI-H510A | Growth Inhibition Assay | IC50=3.18943 μM | ||||
| NCI-N87 | Growth Inhibition Assay | IC50=3.2002 μM | ||||
| SCLC-21H | Growth Inhibition Assay | IC50=3.26859 μM | ||||
| SH-4 | Growth Inhibition Assay | IC50=3.28797 μM | ||||
| QIMR-WIL | Growth Inhibition Assay | IC50=3.32849 μM | ||||
| KM12 | Growth Inhibition Assay | IC50=3.33544 μM | ||||
| ST486 | Growth Inhibition Assay | IC50=3.53883 μM | ||||
| HC-1 | Growth Inhibition Assay | IC50=3.62028 μM | ||||
| BV-173 | Growth Inhibition Assay | IC50=3.64088 μM | ||||
| EW-24 | Growth Inhibition Assay | IC50=3.66434 μM | ||||
| LU-65 | Growth Inhibition Assay | IC50=3.6871 μM | ||||
| ECC4 | Growth Inhibition Assay | IC50=3.7756 μM | ||||
| ARH-77 | Growth Inhibition Assay | IC50=4.11067 μM | ||||
| BC-3 | Growth Inhibition Assay | IC50=4.13068 μM | ||||
| SNB75 | Growth Inhibition Assay | IC50=4.2619 μM | ||||
| MEG-01 | Growth Inhibition Assay | IC50=4.27419 μM | ||||
| NCI-H1417 | Growth Inhibition Assay | IC50=4.28443 μM | ||||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=4.30601 μM | ||||
| Becker | Growth Inhibition Assay | IC50=4.47336 μM | ||||
| DMS-153 | Growth Inhibition Assay | IC50=4.66475 μM | ||||
| TGBC1TKB | Growth Inhibition Assay | IC50=4.68515 μM | ||||
| EW-3 | Growth Inhibition Assay | IC50=4.76248 μM | ||||
| KE-37 | Growth Inhibition Assay | IC50=4.86196 μM | ||||
| NCI-H23 | Growth Inhibition Assay | IC50=4.87227 μM | ||||
| MC116 | Growth Inhibition Assay | IC50=4.94126 μM | ||||
| NH-12 | Growth Inhibition Assay | IC50=4.96439 μM | ||||
| CTB-1 | Growth Inhibition Assay | IC50=4.97721 μM | ||||
| KM-H2 | Growth Inhibition Assay | IC50=5.05323 μM | ||||
| MOLT-4 | Growth Inhibition Assay | IC50=5.1183 μM | ||||
| NCI-H2141 | Growth Inhibition Assay | IC50=5.14268 μM | ||||
| EB-3 | Growth Inhibition Assay | IC50=5.17504 μM | ||||
| NCI-H1522 | Growth Inhibition Assay | IC50=5.26322 μM | ||||
| MRK-nu-1 | Growth Inhibition Assay | IC50=5.43633 μM | ||||
| no-11 | Growth Inhibition Assay | IC50=5.47087 μM | ||||
| CESS | Growth Inhibition Assay | IC50=5.58034 μM | ||||
| KMOE-2 | Growth Inhibition Assay | IC50=5.58659 μM | ||||
| REH | Growth Inhibition Assay | IC50=6.25618 μM | ||||
| KU812 | Growth Inhibition Assay | IC50=6.42791 μM | ||||
| SK-N-FI | Growth Inhibition Assay | IC50=6.60674 μM | ||||
| MMAC-SF | Growth Inhibition Assay | IC50=7.06492 μM | ||||
| RCC10RGB | Growth Inhibition Assay | IC50=7.22977 μM | ||||
| NCI-H322M | Growth Inhibition Assay | IC50=7.33335 μM | ||||
| NB6 | Growth Inhibition Assay | IC50=7.54899 μM | ||||
| MN-60 | Growth Inhibition Assay | IC50=7.69215 μM | ||||
| NCI-H1092 | Growth Inhibition Assay | IC50=8.01734 μM | ||||
| EKVX | Growth Inhibition Assay | IC50=8.47066 μM | ||||
| D-263MG | Growth Inhibition Assay | IC50=8.55396 μM | ||||
| NCI-H209 | Growth Inhibition Assay | IC50=8.64006 μM | ||||
| IST-SL1 | Growth Inhibition Assay | IC50=8.89892 μM | ||||
| ACN | Growth Inhibition Assay | IC50=9.19157 μM | ||||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=9.21219 μM | ||||
| EW-11 | Growth Inhibition Assay | IC50=9.65396 μM | ||||
| KASUMI-1 | Growth Inhibition Assay | IC50=9.7877 μM | ||||
| KINGS-1 | Growth Inhibition Assay | IC50=10.2347 μM | ||||
| EVSA-T | Growth Inhibition Assay | IC50=10.3192 μM | ||||
| DSH1 | Growth Inhibition Assay | IC50=10.3972 μM | ||||
| COLO-824 | Growth Inhibition Assay | IC50=10.8669 μM | ||||
| K052 | Growth Inhibition Assay | IC50=10.9322 μM | ||||
| SK-MEL-2 | Growth Inhibition Assay | IC50=10.9939 μM | ||||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 614.2 | Formule | C30H40ClN7O3S |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 761439-42-3 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | N/A | Smiles | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC | ||
Solubilité
|
In vitro |
DMSO
: 10 mg/mL
(16.28 mM)
Water : Insoluble Ethanol : Insoluble |
Calculateur de molarité
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Targets/IC50/Ki |
ALK
(Cell lines) 2-10 nM
|
|---|---|
| In vitro |
TAE684 (NVP-TAE684) ne présente pas de réactivité croisée significative avec d'autres kinases. Ce composé inhibe puissamment la prolifération des cellules Ba/F3 NPM-ALK avec une IC50 de 3 nM, sans affecter la survie des cellules Ba/F3 même à 1 µM. Il inhibe également la prolifération des lignées cellulaires ALCL humaines exprimant NPM-ALK, y compris Karpas-299 et SU-DHL-1, avec une IC50 de 2 à 5 nM. La modélisation moléculaire révèle que L258 pourrait être l'un des principaux déterminants de la sélectivité de cette kinase pour cette substance chimique. Son traitement entraîne une inhibition rapide et soutenue de la phosphorylation de NPM-ALK. Le composé induit l'apoptose et l'arrêt en phase G1 dans les cellules Ba/F3 exprimant NPM-ALK et les lignées cellulaires de patients ALCL. Il surmonte de manière significative la résistance des cellules H3122 CR, hébergeant l'oncogène de fusion EML4-ALK, diminuant la croissance cellulaire, supprimant la phosphorylation d'ALK et induisant l'apoptose. La croissance des neurites induite par l'expression du mutant mALK R1279Q pourrait être complètement inhibée par ce composé à 30 nM. |
| Essai kinase |
Tests enzymatiques in vitro.
|
|
Tous les tests enzymatiques in vitro sont réalisés chez Upstate Biotechnology à l'exception de l'InsR et de l'IGF-1R. Pour déterminer l'IC50 de TAE684 (NVP-TAE684) contre l'InsR et l'IGF-1R, un test de fluorescence résolue dans le temps homogène est effectué. L'ATP (10 mM) et 20 mg/ml de PolyEY biotinylé (Glu, Tyr 4:1) sont combinés avec 50 nL de dilutions en série de ce composé (10-500 nM) et 4 ng d'enzyme InsR en présence du tampon de réaction de la kinase (20 mM Tris-Cl, pH 7,5/10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0,1 mg/ml de BSA). Les essais sont incubés pendant 1 heure à température ambiante. Les réactions sont terminées par l'ajout de 10 mL de la solution de détection contenant 50 mM d'EDTA, 500 mM de KF, 0,5 mg/ml de BSA, 5 mg/mL d'anticorps anti-phosphotyrosine Mab PT66-K marqué au cryptate Eu3+ et 5 mg/mL de Streptavidine-XLent. La réaction est incubée pendant une demi-heure, et les signaux de fluorescence sont lus sur Analyst GT.
|
|
| In vivo |
Après 4 semaines de traitement avec TAE684 (NVP-TAE684) à 3 et 10 mg/kg, il y a un retard significatif dans le développement du lymphome et une réduction du signal de luminescence de 100 à 1 000 fois, sans aucun signe de toxicité liée au composé ou à la maladie dans le modèle de lymphome de Karpas-299. Ce traitement composé induit également une régression de la maladie dans les lymphomes Karpas-299 établis et régule à la baisse l'expression de CD30. Il montre également une activité antitumorale impressionnante contre les tumeurs de xénogreffe H3122 CR. De plus, le traitement avec ce produit chimique améliore le phénotype des yeux rugueux des deux mutants ALK, en particulier celui observé avec ALKR1275Q. |
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Growth inhibition assay | Cell viability |
|
18594010 |
| Western blot | p-ROS1 / ROS1 p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP |
|
25351743 |
Support technique
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