réservé à la recherche
PF-4708671 S6 Kinase inhibiteur
N° Cat.S2163
Structure chimique
Poids moléculaire: 390.41
Contrôle qualité
| Cibles apparentées | PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A |
|---|---|
| Autre S6 Kinase Inhibiteurs | BI-D1870 LY2584702 LY2584702 Tosylate LJH685 LJI308 S6K-18 3'-Hydroxypterostilbene L-Norvaline BRD7389 Gingerenone A |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | ||||
| UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | ||||
| A427 | Growth Inhibition Assay | IC50=5.72567 μM | ||||
| OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | ||||
| SW684 | Growth Inhibition Assay | IC50=7.52268 μM | ||||
| SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | ||||
| CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | ||||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | ||||
| ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | ||||
| OE19 | Growth Inhibition Assay | IC50=10.1733 μM | ||||
| DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | ||||
| SW13 | Growth Inhibition Assay | IC50=11.9319 μM | ||||
| MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | ||||
| 647-V | Growth Inhibition Assay | IC50=12.3582 μM | ||||
| NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | ||||
| LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | ||||
| UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | ||||
| NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | ||||
| FADU | Growth Inhibition Assay | IC50=13.6992 μM | ||||
| A2780 | Growth Inhibition Assay | IC50=13.8041 μM | ||||
| NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | ||||
| TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | ||||
| HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | ||||
| MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | ||||
| Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | ||||
| HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | ||||
| SAS | Growth Inhibition Assay | IC50=18.6455 μM | ||||
| IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | ||||
| C3A | Growth Inhibition Assay | IC50=18.7919 μM | ||||
| ES3 | Growth Inhibition Assay | IC50=18.8364 μM | ||||
| HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | ||||
| T47D | Growth Inhibition Assay | IC50=20.1485 μM | ||||
| EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | ||||
| LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | ||||
| U031 | Growth Inhibition Assay | IC50=21.4802 μM | ||||
| A549 | Growth Inhibition Assay | IC50=21.8491 μM | ||||
| RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | ||||
| BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | ||||
| NB69 | Growth Inhibition Assay | IC50=23.152 μM | ||||
| NB7 | Growth Inhibition Assay | IC50=24.188 μM | ||||
| HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | ||||
| MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | ||||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | ||||
| HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | ||||
| Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | ||||
| KGN | Growth Inhibition Assay | IC50=25.7547 μM | ||||
| LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | ||||
| NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | ||||
| D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | ||||
| DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | ||||
| NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | ||||
| KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | ||||
| C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | ||||
| SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | ||||
| MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | ||||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | ||||
| CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | ||||
| GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | ||||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | ||||
| KLE | Growth Inhibition Assay | IC50=33.4334 μM | ||||
| KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | ||||
| DOK | Growth Inhibition Assay | IC50=34.6612 μM | ||||
| ACHN | Growth Inhibition Assay | IC50=35.1588 μM | ||||
| KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | ||||
| SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | ||||
| NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | ||||
| ES7 | Growth Inhibition Assay | IC50=36.2249 μM | ||||
| A172 | Growth Inhibition Assay | IC50=36.4187 μM | ||||
| UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | ||||
| LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | ||||
| KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | ||||
| TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | ||||
| G-402 | Growth Inhibition Assay | IC50=40.061 μM | ||||
| 786-0 | Growth Inhibition Assay | IC50=40.9096 μM | ||||
| K5 | Growth Inhibition Assay | IC50=41.3686 μM | ||||
| SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | ||||
| OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | ||||
| T84 | Growth Inhibition Assay | IC50=42.1263 μM | ||||
| GCIY | Growth Inhibition Assay | IC50=43.0803 μM | ||||
| BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | ||||
| SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | ||||
| TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | ||||
| 23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | ||||
| DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | ||||
| ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | ||||
| DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | ||||
| COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | ||||
| DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | ||||
| YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | ||||
| RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | ||||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | ||||
| NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | ||||
| OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | ||||
| NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | ||||
| 22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | ||||
| G-401 | Growth Inhibition Assay | IC50=48.4415 μM | ||||
| YAPC | Growth Inhibition Assay | IC50=49.8073 μM | ||||
| SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | ||||
| COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | ||||
| KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | ||||
| NB5 | Growth Inhibition Assay | IC50=51.4509 μM | ||||
| CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | ||||
| CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | ||||
| CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | ||||
| 8305C | Growth Inhibition Assay | IC50=52.315 μM | ||||
| Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | ||||
| AU565 | Growth Inhibition Assay | IC50=52.5509 μM | ||||
| CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | ||||
| BEN | Growth Inhibition Assay | IC50=53.7862 μM | ||||
| NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | ||||
| HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | ||||
| SH-4 | Growth Inhibition Assay | IC50=54.138 μM | ||||
| NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | ||||
| BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | ||||
| CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | ||||
| A388 | Growth Inhibition Assay | IC50=56.0985 μM | ||||
| C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | ||||
| GAMG | Growth Inhibition Assay | IC50=56.5955 μM | ||||
| MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | ||||
| VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | ||||
| HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | ||||
| BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | ||||
| LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | ||||
| LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | ||||
| NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | ||||
| COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | ||||
| OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | ||||
| SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | ||||
| MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | ||||
| SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | ||||
| EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | ||||
| GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | ||||
| HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | ||||
| MLMA | Growth Inhibition Assay | IC50=61.6163 μM | ||||
| D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | ||||
| SF295 | Growth Inhibition Assay | IC50=63.6655 μM | ||||
| ES4 | Growth Inhibition Assay | IC50=64.4719 μM | ||||
| CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | ||||
| OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | ||||
| NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | ||||
| JAR | Growth Inhibition Assay | IC50=65.5516 μM | ||||
| SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | ||||
| D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | ||||
| EW-22 | Growth Inhibition Assay | IC50=66.395 μM | ||||
| GCT | Growth Inhibition Assay | IC50=67.0443 μM | ||||
| NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | ||||
| RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | ||||
| HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | ||||
| NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | ||||
| IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | ||||
| SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | ||||
| SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | ||||
| LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | ||||
| U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | ||||
| KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | ||||
| U251 | Growth Inhibition Assay | IC50=73.8168 μM | ||||
| HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | ||||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | ||||
| HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | ||||
| Becker | Growth Inhibition Assay | IC50=75.1105 μM | ||||
| PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | ||||
| TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | ||||
| SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | ||||
| NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | ||||
| S-117 | Growth Inhibition Assay | IC50=75.755 μM | ||||
| HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | ||||
| CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | ||||
| BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | ||||
| LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | ||||
| LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | ||||
| ES8 | Growth Inhibition Assay | IC50=78.0073 μM | ||||
| UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | ||||
| NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | ||||
| IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | ||||
| BHY | Growth Inhibition Assay | IC50=79.596 μM | ||||
| MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | ||||
| IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | ||||
| WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | ||||
| VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | ||||
| NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | ||||
| MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | ||||
| 639-V | Growth Inhibition Assay | IC50=84.6129 μM | ||||
| RT4 | Growth Inhibition Assay | IC50=85.2403 μM | ||||
| NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | ||||
| CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | ||||
| BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | ||||
| HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | ||||
| G-361 | Growth Inhibition Assay | IC50=88.1474 μM | ||||
| LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | ||||
| HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | ||||
| DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | ||||
| CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | ||||
| MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | ||||
| HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | ||||
| SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | ||||
| NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | ||||
| SW872 | Growth Inhibition Assay | IC50=100.456 μM | ||||
| COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | ||||
| MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | ||||
| Cliquez pour voir plus de données expérimentales sur les lignées cellulaires | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 390.41 | Formule | C19H21F3N6 |
Stockage (À partir de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 1255517-76-0 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | N/A | Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
Solubilité
|
In vitro |
DMSO
: 30 mg/mL
(76.84 mM)
Ethanol : 8 mg/mL Water : Insoluble |
Calculateur de molarité
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Entrez la formulation in vivo (Ceci nest que 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, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.
Remarque : 1. Assurez-vous 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 peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Targets/IC50/Ki |
p70 S6K1
(Cell-free assay) 160 nM
|
|---|---|
| In vitro |
Le PF-4708671 est un analogue pipérazinyl-pyrimidine et le premier inhibiteur spécifique de S6K1. Ce composé n'inhibe pas significativement l'activité de l'isoforme S6K2 étroitement apparentée ou d'un certain nombre d'autres kinases AGC (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 ou SGK1). Il empêche la phosphorylation médiée par S6K1 de la protéine S6 en réponse à l'IGF-1 (facteur de croissance analogue à l'insuline 1), tout en n'ayant aucun effet sur la phosphorylation induite par le PMA des substrats des kinases RSK (p90 ribosomal S6 kinase) et MSK (mitogen- and stress-activated kinase) très apparentées. Il est également démontré que cette substance chimique induit la phosphorylation de la boucle T et du motif hydrophobe de S6K1, un effet qui dépend de mTORC1 (mTOR complex 1). Il n'affecte pas l'activité de mTORC1.
|
Références |
Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | p-mTOR / mTOR / p-p70S6K / p70S6K pS6 / S6 / pS6K / S6K1 / pAKT / AKT |
|
30423811 |
| Growth inhibition assay | Cell viability |
|
30423811 |
Support technique
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Questions fréquemment posées
Question 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for it is suitable for i.p. or not?
Réponse :
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one for this compound. It is a suspension.
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